2.4.1.17: glucuronosyltransferase

Results	in table
97	Activating Compound
13717	AA Sequence
12	Application
7	CAS Registry Number
176	Cloned(Commentary)
1	Crystallization (Commentary)
5420	Disease/ Diagnostics
11	Expression
58	General Information
2	General Stability
473	IC50 Value
518	Inhibitors
6	kcat/KM [mM/s]
161	Ki Value [mM]
820	KM Value [mM]
300	Localization
111	Metals/Ions
70	Molecular Weight [Da]
214	Natural Substrates/ Products (Substrates)
5420	Organism
19	Pathway
14	PDB ID
98	pH Optimum
2	pH Range
2	pH Stability
18	Posttranslational Modification
200	Protein Variants
52	Purification (Commentary)
7	Reaction
1	Reaction Type
489	Reference
2	Renatured (Commentary)
557	Source Tissue
120	Specific Activity [micromol/min/mg]
21	Storage Stability
1650	Substrates and Products (Substrate)
132	Subunits
1011	Synonyms
1	Systematic Name
83	Temperature Optimum [°C]
2	Temperature Range [°C]
19	Temperature Stability [°C]
6	Turnover Number [1/s]

0.0073

(+-)-11-hydroxy-DELTA9-tetrahydrocannabinol

Homo sapiens

-

isoform UGT1A9, pH 7.4, 37°C

703407

0.072

-

isoform UGT1A10, pH 7.4, 37°C

703407

0.068

(-)-11-nor-9-carboxy-DELTA9-tetrahydrocannabinol

Homo sapiens

-

isoform UGT1A3, pH 7.4, 37°C

703407

0.17

-

isoform UGT1A1, pH 7.4, 37°C

703407

0.044

(R)-7-hydroxywarfarin

Homo sapiens

-

isoform UGT1A10, pH 7.6, 37°C

720303

0.13

-

isoform UGT1A1, pH 7.6, 37°C

720303

0.16

(R)-propanolol

Homo sapiens

-

isoform UGT1A9, pH 7.4, 37°C

706097

0.263

-

isoform UGT2B7, pH 7.4, 37°C

706097

1.21

-

isoform UGT2B4, pH 7.4, 37°C

706097

0.16

(S)-7-hydroxywarfarin

Homo sapiens

-

isoform UGT1A10, pH 7.6, 37°C

720303

0.23

-

isoform UGT1A1, pH 7.6, 37°C

720303

0.507

(S)-naproxen

Homo sapiens

-

mutant M33V, pH 7.4, 37°C

718805

0.62

-

mutant M33I, pH 7.4, 37°C

718805

0.66

-

mutant M33Q, pH 7.4, 37°C

718805

0.79

-

wildtype, pH 7.4, 37°C

718805

1.013

-

mutant M33T, pH 7.4, 37°C

718805

0.135

(S)-propanolol

Homo sapiens

-

isoform UGT1A9, pH 7.4, 37°C

706097

0.289

-

isoform UGT2B7, pH 7.4, 37°C

706097

0.515

-

isoform UGT2B4, pH 7.4, 37°C

706097

0.247

1-hydroxy-benzo(a)pyrene

Homo sapiens

-

wild-type, pH 7.4, 37°C

720625

0.263

-

mutant K75R, pH 7.4, 37°C

720625

0.0061

1-hydroxy-benzo[a]pyrene

Homo sapiens

Q3SY77, Q6NUS8

with UDP-D-xylose, recombinant enzyme in microsomes, pH 7.4, 37°C

759116

0.011

Q3SY77, Q6NUS8

with UDP-D-glucose, recombinant enzyme in microsomes, pH 7.4, 37°C

759116

0.0012

1-hydroxy-pyrene

Homo sapiens

Q3SY77, Q6NUS8

with UDP-D-xylose, recombinant enzyme in microsomes, pH 7.4, 37°C

759116

0.0033

Q3SY77, Q6NUS8

with UDP-D-glucose, recombinant enzyme in microsomes, pH 7.4, 37°C

759116

0.0113

1-hydroxybenzo(a)pyrene

Homo sapiens

O60656, O75795, P16662, P22309, P35503, P54855, Q9HAW7, Q9HAW8, Q9HAW9

37°C, pH 7.5

673300

0.0299

O60656, O75795, P16662, P22309, P35503, P54855, Q9HAW7, Q9HAW8, Q9HAW9

37°C, pH 7.5

673300

0.0342

O60656, O75795, P16662, P22309, P35503, P54855, Q9HAW7, Q9HAW8, Q9HAW9

37°C, pH 7.5

673300

0.087

O60656, O75795, P16662, P22309, P35503, P54855, Q9HAW7, Q9HAW8, Q9HAW9

37°C, pH 7.5

673300

0.0963

O60656, O75795, P16662, P22309, P35503, P54855, Q9HAW7, Q9HAW8, Q9HAW9

37°C, pH 7.5

673300

0.169

O60656, O75795, P16662, P22309, P35503, P54855, Q9HAW7, Q9HAW8, Q9HAW9

37°C, pH 7.5

673300

0.854

O60656, O75795, P16662, P22309, P35503, P54855, Q9HAW7, Q9HAW8, Q9HAW9

37°C, pH 7.5

673300

1.526

O60656, O75795, P16662, P22309, P35503, P54855, Q9HAW7, Q9HAW8, Q9HAW9

37°C, pH 7.5

673300

2.869

O60656, O75795, P16662, P22309, P35503, P54855, Q9HAW7, Q9HAW8, Q9HAW9

37°C, pH 7.5

673300

0.003188

1-hydroxypyrene

Struthio camelus

-

at pH 7.4 and 38.5°C

756511

0.019

Serinus canaria

-

at pH 7.4 and 38.5°C

756511

0.02548

Haliaeetus albicilla

-

at pH 7.4 and 40.5°C

756511

0.03662

Meleagris gallopavo

-

at pH 7.4 and 41.5°C

756511

0.06745

Rattus norvegicus

-

at pH 7.4 and 38.5°C

756511

0.091

Homo sapiens

-

wild-type, pH 7.4, 37°C

720625

0.111

-

mutant K75R, pH 7.4, 37°C

720625

0.1137

Gallus gallus

-

at pH 7.4 and 42°C

756511

2.326

Spheniscus humboldti

-

at pH 7.4 and 39°C

756511

0.00246

1-naphthol

Rattus norvegicus

-

apparent Km for UGT1A6, 3mM UDP-glucuronic acid, mutants that retained activity shows similar Km values

488787

0.015

-

no activator present

488724

0.03

-

presence of 50 mM MgCl2 as activator

488724

0.03

Homo sapiens

-

wild-type, pH 7.4, 37°C

720625

0.037

Bos taurus

-

alveolar macrophages

488800

0.044

Homo sapiens

-

mutant K75R, pH 7.4, 37°C

720625

0.048

-

H379A mutant isozyme UGT1A6

694254

0.061

Bos taurus

-

liver

488800

0.067

Rattus norvegicus

-

presence of 50 mM MgCl2, 0.1% Triton X-100 as activator

488724

0.083

Homo sapiens

-

H371A mutant isozyme UGT1A6

694254

0.084

-

isoform UGT1A6, pH 7.4, 37°C

720115

0.092

Bos taurus

-

lung

488800

0.129

Homo sapiens

Q3SY77, Q6NUS8

with UDP-D-xylose, recombinant enzyme in microsomes, pH 7.4, 37°C

759116

0.22

Canis lupus familiaris

pH 7.4, 37°C

0.225

with UDP-D-glucose, recombinant enzyme in microsomes, pH 7.4, 37°C

759116

0.265

-

pH 7.4, 37°C

657879

0.33

Macaca mulatta

-

apparent Km for microsomal preparation

488797

27

Homo sapiens

-

wild-type isozyme UGT1A6

694254

0.0178

10-gingerol

Homo sapiens

O60656, O75795, P06133, P16662, P19224, P22309, P22310, P35503, P54855, Q9HAW7, Q9HAW8, Q9HAW9

pH 7.4, temperature not specified in the publication, isozyme UGT1A9

736680

0.0224

O60656, O75795, P06133, P16662, P19224, P22309, P22310, P35503, P54855, Q9HAW7, Q9HAW8, Q9HAW9

pH 7.4, temperature not specified in the publication, isozyme UGT2B7

736680

0.0308

O60656, O75795, P06133, P16662, P19224, P22309, P22310, P35503, P54855, Q9HAW7, Q9HAW8, Q9HAW9

pH 7.4, temperature not specified in the publication, isozyme UGT1A1

736680

0.0313

O60656, O75795, P06133, P16662, P19224, P22309, P22310, P35503, P54855, Q9HAW7, Q9HAW8, Q9HAW9

pH 7.4, temperature not specified in the publication, isozyme UGT2B17

736680

0.033

O60656, O75795, P06133, P16662, P19224, P22309, P22310, P35503, P54855, Q9HAW7, Q9HAW8, Q9HAW9

pH 7.4, temperature not specified in the publication, isozyme UGT1A8

736680

0.0353

O60656, O75795, P06133, P16662, P19224, P22309, P22310, P35503, P54855, Q9HAW7, Q9HAW8, Q9HAW9

pH 7.4, temperature not specified in the publication, isozyme UGT1A8

736680

0.0069

11alpha-hydroxyprogesterone

Homo sapiens

O60656, O75795, P16662, P22310, P54855

37°C, pH 7.4

673304

0.093

O60656, O75795, P16662, P22310, P54855

37°C, pH 7.4

673304

0.073

16alpha-hydroxyprogesterone

Homo sapiens

O60656, O75795, P16662, P22310, P54855

37°C, pH 7.4

673304

0.211

O60656, O75795, P16662, P22310, P54855

37°C, pH 7.4

673304

0.042

17-epiestriol

native UGT2B4

0.052

native UGT2B4

0.063

mutant UGT2B4(Y33L)

0.071

mutant UGT2B4(F33Y)

0.093

mutant UGT2B4(F33L)

0.159

mutant UGT2B4(Y33F)

0.00192

17beta-estradiol

Homo sapiens

Q9HAW8

recombinant mutant M59I, pH 7.5, 37°C

658519

0.00233

Q9HAW8

recombinant mutant T202I, pH 7.5, 37°C

658519

0.00234

Q9HAW8

recombinant wild-type enzyme, pH 7.5, 37°C

658519

0.00318

Mus musculus

Q3UEP4, Q63886, Q8K154, Q8VCN3

isoform Ugt1a1, at pH 7.4 and 37°C

757475

0.0143

Homo sapiens

-

isoform UGT1A10, pH 7.4, 37°C

720334

0.0297

-

isoform UGT2B7, pH 7.4, 37°C

0.045

-

0.0975

-

isoform UGT2A1, pH 7.4, 37°C

720334

0.0073

1alpha,25-dihydroxyvitamin D3

Homo sapiens

P22310

25-O-glucuronidation of 1alpha,25-dihydroxyvitamin D3 by UGT1A4 supersomes

690850

0.0112

P22310

25-O-glucuronidation of 1alpha,25-dihydroxyvitamin D3 by liver microsomes

690850

0.00298

2',4,4'-trihydroxychalcone

Homo sapiens

-

isoform UGT1A1, product 2',4,4'-trihydroxychalcone 2'-O-glucoside

703403

0.00315

-

isoform UGT1A9, product 2',4,4'-trihydroxychalcone 4'-O-glucoside

703403

0.0043

-

isoform UGT1A1, product 2',4,4'-trihydroxychalcone 4'-O-glucoside

703403

0.0258

-

isoform UGT1A10, product 2',4,4'-trihydroxychalcone 2'-O-glucoside

703403

0.0119

2-(4-chlorophenyl)-5-(2-furyl)-4-oxazoleacetic acid

Homo sapiens

O60656, P16662, P22309, P35503

Hill equation

673310

0.0456

O60656, P16662, P22309, P35503

Hill equation

673310

0.138

O60656, P16662, P22309, P35503

-

673310

0.293

O60656, P16662, P22309, P35503

Hill equation

673310

0.014

2-hydroxyestradiol

Homo sapiens

-

apparent Km on expressed UGT2B7Y, 2 mM UDP glucuronic acid

488785

0.024

P19224

apparent Km for UGT1A3

488790

0.025

P19224

apparent Km for UGT1A1

488790

0.026

-

apparent Km on expressed UGT1A3, 2 mM UDP glucuronic acid

488785

0.027

-

apparent Km on expressed UGT1A1, 2 mM UDP glucuronic acid

488785

5

Platyrrhini

-

488795

0.0102

2-hydroxyestrone

Homo sapiens

Q9HAW8

37°C, pH 8.0, mutant enzyme F93A

677147

0.021

P19224

apparent Km for UGT1A3

488790

0.024

-

apparent Km on expressed UGT1A3, 2 mM UDP glucuronic acid

488785

0.024

P19224

apparent Km for UGT1A1

488790

0.026

-

apparent Km on expressed UGT1A1, 2 mM UDP glucuronic acid

488785

0.066

-

apparent Km on expressed UGT2B7Y, 2 mM UDP glucuronic acid

488785

0.0823

Q9HAW8

37°C, pH 8.0, mutant enzyme F93L

677147

0.1305

Q9HAW8

37°C, pH 8.0, wild-type enzyme

677147

0.291

Q9HAW8

37°C, pH 8.0, mutant enzyme F90L

677147

6

Platyrrhini

-

488795

0.551

3'-azido-3'-deoxythymidine

Homo sapiens

P16662

pH 7.4, 37°C

693343

0.77

-

isozyme UGT2B7, pH 7.5, 37°C

11.6

-

13.4

-

0.271

3-hydroxy-benzo(a)pyrene

Homo sapiens

-

wild-type, pH 7.4, 37°C

720625

0.278

-

mutant K75R, pH 7.4, 37°C

720625

0.0072

3-hydroxy-benzo[a]pyrene

Homo sapiens

Q3SY77, Q6NUS8

with UDP-D-xylose, recombinant enzyme in microsomes, pH 7.4, 37°C

759116

0.0075

Q3SY77, Q6NUS8

with UDP-D-glucose, recombinant enzyme in microsomes, pH 7.4, 37°C

759116

0.0097

3-hydroxybenzo(a)pyrene

Homo sapiens

O60656, O75795, P16662, P22309, P35503, P54855, Q9HAW7, Q9HAW8, Q9HAW9

37°C, pH 7.5

673300

0.0556

O60656, O75795, P16662, P22309, P35503, P54855, Q9HAW7, Q9HAW8, Q9HAW9

37°C, pH 7.5

673300

0.0635

O60656, O75795, P16662, P22309, P35503, P54855, Q9HAW7, Q9HAW8, Q9HAW9

37°C, pH 7.5

673300

0.115

O60656, O75795, P16662, P22309, P35503, P54855, Q9HAW7, Q9HAW8, Q9HAW9

37°C, pH 7.5

673300

0.234

O60656, O75795, P16662, P22309, P35503, P54855, Q9HAW7, Q9HAW8, Q9HAW9

37°C, pH 7.5

673300

0.295

O60656, O75795, P16662, P22309, P35503, P54855, Q9HAW7, Q9HAW8, Q9HAW9

37°C, pH 7.5

673300

0.348

O60656, O75795, P16662, P22309, P35503, P54855, Q9HAW7, Q9HAW8, Q9HAW9

37°C, pH 7.5

673300

0.497

O60656, O75795, P16662, P22309, P35503, P54855, Q9HAW7, Q9HAW8, Q9HAW9

37°C, pH 7.5

673300

0.583

O60656, O75795, P16662, P22309, P35503, P54855, Q9HAW7, Q9HAW8, Q9HAW9

37°C, pH 7.5

673300

0.00197

3alpha,5beta-tetrahydroaldosterone

Homo sapiens

P16662

isozyme UGT2B7Y268, pH 7.5, 37°C

658558

0.0047

P16662

isozyme UGT2B7H268, pH 7.5, 37°C

658558

0.0588

4-aminobiphenyl

-

0.2275

-

0.251

-

mutant D148A

706582

0.269

-

wild-type

706582

0.286

-

mutant H37A

706582

0.006

4-hydroxyestradiol

Homo sapiens

-

apparent Km on expressed UGT1A1, 2 mM UDP glucuronic acid

488785

0.007

-

apparent Km on expressed UGT2B7Y, 2 mM UDP glucuronic acid

488785

0.01

P19224

apparent Km for UGT2B7

488790

0.038

-

apparent Km on expressed UGT1A3, 2 mM UDP glucuronic acid

488785

0.0401

Q9HAW8

37°C, pH 8.0, mutant enzyme F93A

677147

0.2338

Q9HAW8

37°C, pH 8.0, wild-type enzyme

677147

0.292

Q9HAW8

37°C, pH 8.0, mutant enzyme F90L

677147

0.014

4-hydroxyestrone

Homo sapiens

P19224

apparent Km for UGT2B7

488790

0.016

-

apparent Km on expressed UGT2B7Y, 2 mM UDP glucuronic acid

488785

0.019

-

apparent Km on expressed UGT1A1, 2 mM UDP glucuronic acid

488785

0.0401

Q9HAW8

37°C, pH 8.0, mutant enzyme F93A

677147

0.053

-

apparent Km on expressed UGT1A3, 2 mM UDP glucuronic acid

488785

0.1182

Q9HAW8

37°C, pH 8.0, wild-type enzyme

677147

0.011

4-methylumbeliferone

Homo sapiens

-

wildtype, pH 7.4, 37°C

718805

0.228

-

mutant M33Q, pH 7.4, 37°C

718805

0.233

-

mutant M33I, pH 7.4, 37°C

718805

0.234

-

mutant M33V, pH 7.4, 37°C

718805

1.621

-

mutant M33T, pH 7.4, 37°C

718805

0.00012

4-Methylumbelliferone

Homo sapiens

P19224, P22309, P22310, P35503

pH 7.4, 37°C, recombinant wild-type isozyme UGT1A6

693017

0.0021

O60656, Q9HAW7, Q9HAW8, Q9HAW9

mutant L173A, pH 7.4, 37°C

692047

0.0029

O60656

pH 7.4, 37°C, isozyme UGT1A9 in presence of 2% fatty acid-free human serum albumin

692035

0.0036

O60656, Q9HAW7, Q9HAW8, Q9HAW9

mutant K91M/A92D, pH 7.4, 37°C

692047

0.0044

O60656, Q9HAW7, Q9HAW8, Q9HAW9

wild-type, pH 7.4, 37°C

692047

0.0044

O60656, Q9HAW7, Q9HAW8, Q9HAW9

mutant E241A, pH 7.4, 37°C

692047

0.0056

O60656, Q9HAW7, Q9HAW8, Q9HAW9

mutant Y106F/G111S/D115G, pH 7.4, 37°C

692047

0.0059

O60656, Q9HAW7, Q9HAW8, Q9HAW9

mutant L219F/H221Q/R222Y, pH 7.4, 37°C

692047

0.008

O60656, P16662, P22309, P22310, P35503, P54855, Q9HAW7, Q9HAW8, Q9HAW9

isozyme UGT1A9, pH 7.4, 37°C

658524

0.009

O60656, P16662, P22309, P22310, P35503, P54855, Q9HAW7, Q9HAW8, Q9HAW9

isozyme UGT1A6, Michaelis-Menten kinetic, pH 7.4, 37°C

658524

0.0091

O60656, Q9HAW7, Q9HAW8, Q9HAW9

mutant N152A, pH 7.4, 37°C

692047

0.0101

O60656, Q9HAW7, Q9HAW8, Q9HAW9

mutant R42Q, pH 7.4, 37°C

692047

0.0134

O60656

pH 7.4, 37°C, isozyme UGT1A9

692035

0.014

O60656, P16662, P22309, P22310, P35503, P54855, Q9HAW7, Q9HAW8, Q9HAW9

isozyme UGT1A7, Michaelis-Menten kinetic, pH 7.4, 37°C

658524

0.015

-

mutant D143A

706582

0.021

-

wild-type

706582

0.031

O60656, P16662, P22309, P22310, P35503, P54855, Q9HAW7, Q9HAW8, Q9HAW9

isozyme UGT1A10, Michaelis-Menten kinetic, pH 7.4, 37°C

658524

0.0522

O60656, P19224, P22309, Q9HAW7, Q9HAW8, Q9HAW9

37°C, pH 7.4

672123

0.054

P22309

pH 7.5, 37°C, 0.2 mM propofol, isozyme UGT1A1

690683

0.0766

O60656, P19224, P22309, Q9HAW7, Q9HAW8, Q9HAW9

37°C, pH 7.4

672123

0.0924

O60656, P19224, P22309, Q9HAW7, Q9HAW8, Q9HAW9

37°C, pH 7.4

672123

0.101

P22309

pH 7.5, 37°C, isozyme UGT1A1

690683

0.108

P19224

37°C, pH 7.4

673033

0.113

O60656, P16662, P22309, P22310, P35503, P54855, Q9HAW7, Q9HAW8, Q9HAW9

isozyme UGT1A1, Michaelis-Menten kinetic, pH 7.4, 37°C

658524

0.115

O60656, P16662, P22309, P35503, P54855

isozyme UGT1A1, pH 7.4, 37°C

657537

0.1226

O60656, P19224, P22309, Q9HAW7, Q9HAW8, Q9HAW9

37°C

672123

0.149

O60656, P16662, P22309, P35503, P54855

isozyme UGT2B15, pH 7.4, 37°C

657537

0.157

O60656, P16662, P22309, P35503, P54855

isozyme UGT1A6, pH 7.4, 37°C

657537

0.164

Mus musculus

-

pH 7.4, 37°C

692039

0.17

Homo sapiens

-

wild-type isozyme UGT1A6

694254

0.18

O60656, P16662, P22309, P35503, P54855

isozyme UGT1A9, pH 7.4, 37°C

657537

0.1917

O60656, Q9HAW7, Q9HAW8, Q9HAW9

isoform UGT1A8, pH 7.4, 37°C

692047

0.206

Macaca fascicularis

-

37°C, pH 7.4

673033

0.2376

Homo sapiens

O60656, P19224, P22309, Q9HAW7, Q9HAW8, Q9HAW9

37°C, pH 7.4

672123

0.253

O60656, P16662, P22309, P22310, P35503, P54855, Q9HAW7, Q9HAW8, Q9HAW9

isozyme UGT2B15, pH 7.4, 37°C

658524

0.335

O60656, P16662, P22309, P35503, P54855

isozyme UGT1A3, pH 7.4, 37°C

657537

0.335

O60656, P16662, P22309, P22310, P35503, P54855, Q9HAW7, Q9HAW8, Q9HAW9

isozyme UGT2B7, Hill equation, pH 7.4, 37°C

658524

0.416

Rattus norvegicus

-

pH 7.4, 37°C

692039

0.58

Homo sapiens

-

H379A mutant isozyme UGT1A6

694254

0.66

-

H371A mutant isozyme UGT1A6

694254

0.73

O60656, P16662, P22309, P22310, P35503, P54855, Q9HAW7, Q9HAW8, Q9HAW9

isozyme UGT1A8, pH 7.4, 37°C

658524

0.967

-

mutant D148A

706582

1.159

O60656, P16662, P22309, P22310, P35503, P54855, Q9HAW7, Q9HAW8, Q9HAW9

isozyme UGT1A3, pH 7.4, 37°C

658524

4.204

O60656, P16662, P22309, P22310, P35503, P54855, Q9HAW7, Q9HAW8, Q9HAW9

isozyme UGT2B17, pH 7.4, 37°C

658524

0.0102

4-nitrophenol

Homo sapiens

O60656, Q9HAW7, Q9HAW8, Q9HAW9

mutant Y106F/G111S/D115G, pH 7.4, 37°C

692047

0.0152

O60656, Q9HAW7, Q9HAW8, Q9HAW9

mutant L219F/H221Q/R222Y, pH 7.4, 37°C

692047

0.0157

O60656, Q9HAW7, Q9HAW8, Q9HAW9

mutant L173A, pH 7.4, 37°C

692047

0.0169

O60656, Q9HAW7, Q9HAW8, Q9HAW9

wild-type, pH 7.4, 37°C

692047

0.0178

O60656, Q9HAW7, Q9HAW8, Q9HAW9

mutant K91M/A92D, pH 7.4, 37°C

692047

0.0188

O60656, Q9HAW7, Q9HAW8, Q9HAW9

mutant E241A, pH 7.4, 37°C

692047

0.03

O60656, Q9HAW7, Q9HAW8, Q9HAW9

mutant R42Q, pH 7.4, 37°C

692047

0.0492

O60656, Q9HAW7, Q9HAW8, Q9HAW9

mutant N152A, pH 7.4, 37°C

692047

0.0496

O60656, P19224, P22309, Q9HAW7, Q9HAW8, Q9HAW9

37°C, pH 7.4

672123

0.1508

O60656, P19224, P22309, Q9HAW7, Q9HAW8, Q9HAW9

37°C, pH 7.4

672123

0.3359

O60656, P19224, P22309, Q9HAW7, Q9HAW8, Q9HAW9

37°C, pH 7.4

672123

0.494

Rattus norvegicus

-

above, pH 7.4, 37°C

692039

0.5191

Homo sapiens

O60656, P19224, P22309, Q9HAW7, Q9HAW8, Q9HAW9

37°C, pH 7.4

672123

0.73

-

pH 7.5, 37°C, genetic variant UGT1A6*1, co-expression of splice variants i1 and i2

703415

0.77

-

pH 7.5, 37°C, genetic variant UGT1A6*1

703415

0.803

O60656, P19224, P22309, Q9HAW7, Q9HAW8, Q9HAW9

37°C, pH 7.4

672123

1.034

O60656, P19224, P22309, Q9HAW7, Q9HAW8, Q9HAW9

37°C, pH 7.4

672123

1.5

Oryctolagus cuniculus

-

488728

1.5

Mus musculus

-

above, pH 7.4, 37°C

692039

2

Rattus norvegicus

-

no difference between Sprague-Dawley and Wistar strains

488697

0.0293

5-diethylaminoethylamino-8-hydroxyimidazoacridinone

Homo sapiens

-

isoform UGT1A7, pH not specified in the publication, temperature not specified in the publication

719349

0.0546

-

isoform UGT1A9, pH not specified in the publication, temperature not specified in the publication

719349

0.094

-

isoform UGT1A10, pH not specified in the publication, temperature not specified in the publication

719349

0.149

-

isoform UGT1A1, pH not specified in the publication, temperature not specified in the publication

719349

0.0289

5-dimethylaminopropylamino-8-hydroxytriazoloacridinone

Homo sapiens

-

isoform UGT1A1, pH not specified in the publication, temperature not specified in the publication

719349

0.0633

-

isoform UGT1A9, pH not specified in the publication, temperature not specified in the publication

719349

0.0706

-

isoform UGT1A10, pH not specified in the publication, temperature not specified in the publication

719349

0.135

5-hydroxytryptophol

Homo sapiens

P19224

isozyme UGT1A6, pH 7.5, 37°C

658527

3.674

P19224

isozyme UGT1A9, pH 7.5, 37°C

658527

0.124

5-methylchrysene-1,2-diol

Homo sapiens

Q3SY77, Q6NUS8

with UDP-D-xylose, recombinant enzyme in microsomes, pH 7.4, 37°C

759116

0.27

-

wild-type, pH 7.4, 37°C

720625

0.381

-

mutant K75R, pH 7.4, 37°C

720625

1.25

Q3SY77, Q6NUS8

with UDP-D-glucose, recombinant enzyme in microsomes, pH 7.4, 37°C

759116

0.00023

5alpha-dihydroaldosterone

Homo sapiens

P16662

isozyme UGT2B7H268, pH 7.5, 37°C

658558

0.00036

P16662

isozyme UGT2B7Y268, pH 7.5, 37°C

658558

0.0646

5beta-tetrahydrocortisone

Homo sapiens

P16662

isozyme UGT2B7H268, pH 7.5, 37°C

658558

0.0647

P16662

isozyme UGT2B7Y268, pH 7.5, 37°C

658558

0.0253

6-gingerol

Homo sapiens

O60656, O75795, P06133, P16662, P19224, P22309, P22310, P35503, P54855, Q9HAW7, Q9HAW8, Q9HAW9

pH 7.4, temperature not specified in the publication, isozyme UGT2B15

736680

0.0488

O60656, O75795, P06133, P16662, P19224, P22309, P22310, P35503, P54855, Q9HAW7, Q9HAW8, Q9HAW9

pH 7.4, temperature not specified in the publication, isozyme UGT2B17

736680

0.0543

O60656, O75795, P06133, P16662, P19224, P22309, P22310, P35503, P54855, Q9HAW7, Q9HAW8, Q9HAW9

pH 7.4, temperature not specified in the publication, isozyme UGT1A8

736680

0.138

O60656, O75795, P06133, P16662, P19224, P22309, P22310, P35503, P54855, Q9HAW7, Q9HAW8, Q9HAW9

pH 7.4, temperature not specified in the publication, isozyme UGT1A8

736680

0.158

O60656, O75795, P06133, P16662, P19224, P22309, P22310, P35503, P54855, Q9HAW7, Q9HAW8, Q9HAW9

pH 7.4, temperature not specified in the publication, isozyme UGT1A9

736680

0.206

O60656, O75795, P06133, P16662, P19224, P22309, P22310, P35503, P54855, Q9HAW7, Q9HAW8, Q9HAW9

pH 7.4, temperature not specified in the publication, isozyme UGT1A10

736680

0.232

O60656, O75795, P06133, P16662, P19224, P22309, P22310, P35503, P54855, Q9HAW7, Q9HAW8, Q9HAW9

pH 7.4, temperature not specified in the publication, isozyme UGT1A1

736680

0.404

O60656, O75795, P06133, P16662, P19224, P22309, P22310, P35503, P54855, Q9HAW7, Q9HAW8, Q9HAW9

pH 7.4, temperature not specified in the publication, isozyme UGT2B7

736680

0.48

6-hydroxywarfarin

Homo sapiens

-

wild-type, pH 7.4, 37°C

703404

0.7

-

mutant V92A, pH 7.4, 37°C

703404

0.72

-

mutant F93A, pH 7.4, 37°C

703404

0.003

6alpha-hydroxyprogesterone

Homo sapiens

O60656, O75795, P16662, P22310, P54855

37°C, pH 7.4

673304

0.055

O60656, O75795, P16662, P22310, P54855

37°C, pH 7.4

673304

19.3

7-ethyl-10-hydroxycampothecin

Homo sapiens

O60656

recombinant wild-type isozyme UGT1A9, pH.4, 37°C

659783

44.4

O60656

recombinant UGT1A9 mutant D256N isozyme, pH.4, 37°C

659783

0.0098

7-hydroxy benzo(a)pyrene

Homo sapiens

O60656, O75795, P16662, P22309, P35503, P54855, Q9HAW7, Q9HAW8, Q9HAW9

37°C, pH 7.5

673300

0.0501

O60656, O75795, P16662, P22309, P35503, P54855, Q9HAW7, Q9HAW8, Q9HAW9

37°C, pH 7.5

673300

0.0621

O60656, O75795, P16662, P22309, P35503, P54855, Q9HAW7, Q9HAW8, Q9HAW9

37°C, pH 7.5

673300

0.127

O60656, O75795, P16662, P22309, P35503, P54855, Q9HAW7, Q9HAW8, Q9HAW9

37°C, pH 7.5

673300

0.129

O60656, O75795, P16662, P22309, P35503, P54855, Q9HAW7, Q9HAW8, Q9HAW9

37°C, pH 7.5

673300

0.19

O60656, O75795, P16662, P22309, P35503, P54855, Q9HAW7, Q9HAW8, Q9HAW9

37°C, pH 7.5

673300

0.281

O60656, O75795, P16662, P22309, P35503, P54855, Q9HAW7, Q9HAW8, Q9HAW9

37°C, pH 7.5

673300

0.542

O60656, O75795, P16662, P22309, P35503, P54855, Q9HAW7, Q9HAW8, Q9HAW9

37°C, pH 7.5

673300

1.588

O60656, O75795, P16662, P22309, P35503, P54855, Q9HAW7, Q9HAW8, Q9HAW9

37°C, pH 7.5

673300

0.00418

7-hydroxy-4-trifluoromethylcoumarin

Homo sapiens

Q9HAW8

recombinant mutant M59I, pH 7.5, 37°C

658519

0.00491

Q9HAW8

recombinant wild-type enzyme, pH 7.5, 37°C

658519

0.00537

Q9HAW8

recombinant mutant T202I, pH 7.5, 37°C

658519

0.151

Macaca fascicularis

Q9TSL7

recombinant isoform UGT1A1, pH 7.4, 37°C

720355

0.198

Homo sapiens

P22309

recombinant isoform UGT1A1, pH 7.4, 37°C

720355

0.261

7-hydroxy-benzo(a)pyrene

Homo sapiens

-

wild-type, pH 7.4, 37°C

720625

0.334

-

mutant K75R, pH 7.4, 37°C

720625

0.0078

7-hydroxy-benzo[a]pyrene

Homo sapiens

Q3SY77, Q6NUS8

with UDP-D-glucose, recombinant enzyme in microsomes, pH 7.4, 37°C

759116

0.0085

Q3SY77, Q6NUS8

with UDP-D-xylose, recombinant enzyme in microsomes, pH 7.4, 37°C

759116

0.17

7-hydroxywarfarin

Homo sapiens

-

wild-type, pH 7.4, 37°C

703404

0.56

-

mutant V92A, pH 7.4, 37°C

703404

0.0132

8-gingerol

Homo sapiens

O60656, O75795, P06133, P16662, P19224, P22309, P22310, P35503, P54855, Q9HAW7, Q9HAW8, Q9HAW9

pH 7.4, temperature not specified in the publication, isozyme UGT1A9

736680

0.0211

O60656, O75795, P06133, P16662, P19224, P22309, P22310, P35503, P54855, Q9HAW7, Q9HAW8, Q9HAW9

pH 7.4, temperature not specified in the publication, isozyme UGT2B17

736680

0.0235

O60656, O75795, P06133, P16662, P19224, P22309, P22310, P35503, P54855, Q9HAW7, Q9HAW8, Q9HAW9

pH 7.4, temperature not specified in the publication, isozyme UGT2B7

736680

0.0293

O60656, O75795, P06133, P16662, P19224, P22309, P22310, P35503, P54855, Q9HAW7, Q9HAW8, Q9HAW9

pH 7.4, temperature not specified in the publication, isozyme UGT1A1

736680

0.0314

O60656, O75795, P06133, P16662, P19224, P22309, P22310, P35503, P54855, Q9HAW7, Q9HAW8, Q9HAW9

pH 7.4, temperature not specified in the publication, isozyme UGT1A8

736680

0.308

8-hydroxy-benzo(a)pyrene

Homo sapiens

-

wild-type, pH 7.4, 37°C

720625

0.368

-

mutant K75R, pH 7.4, 37°C

720625

0.00048

8-hydroxyquinoline

Homo sapiens

O60656, P16662, P22309, P35503, P54855

isozyme UGT1A9, pH 7.4, 37°C

657537

0.0065

O60656, P16662, P22309, P35503, P54855

isozyme UGT1A6, pH 7.4, 37°C

657537

0.016

O60656, P16662, P22309, P35503, P54855

isozyme UGT2B15, pH 7.4, 37°C

657537

0.301

O60656, P16662, P22309, P35503, P54855

isozyme UGT2B7, pH 7.4, 37°C

657537

0.494

O60656, P16662, P22309, P35503, P54855

isozyme UGT1A3, pH 7.4, 37°C

657537

0.19

8-hydroxywarfarin

Homo sapiens

-

mutant F90A, pH 7.4, 37°C

703404

0.304

-

mutant F93A, pH 7.4, 37°C

703404

0.39

-

wild-type, pH 7.4, 37°C

703404

0.39

-

mutant V92A, pH 7.4, 37°C

703404

0.0096

9-hydroxy-benzo[a]pyrene

Homo sapiens

Q3SY77, Q6NUS8

with UDP-D-xylose, recombinant enzyme in microsomes, pH 7.4, 37°C

759116

0.012

Q3SY77, Q6NUS8

with UDP-D-glucose, recombinant enzyme in microsomes, pH 7.4, 37°C

759116

0.0301

9-hydroxybenzo(a)pyrene

Homo sapiens

O60656, O75795, P16662, P22309, P35503, P54855, Q9HAW7, Q9HAW8, Q9HAW9

37°C, pH 7.5

673300

0.0382

O60656, O75795, P16662, P22309, P35503, P54855, Q9HAW7, Q9HAW8, Q9HAW9

37°C, pH 7.5

673300

0.0633

O60656, O75795, P16662, P22309, P35503, P54855, Q9HAW7, Q9HAW8, Q9HAW9

37°C, pH 7.5

673300

0.0918

O60656, O75795, P16662, P22309, P35503, P54855, Q9HAW7, Q9HAW8, Q9HAW9

37°C, pH 7.5

673300

0.125

O60656, O75795, P16662, P22309, P35503, P54855, Q9HAW7, Q9HAW8, Q9HAW9

37°C, pH 7.5

673300

0.208

O60656, O75795, P16662, P22309, P35503, P54855, Q9HAW7, Q9HAW8, Q9HAW9

37°C, pH 7.5

673300

0.209

O60656, O75795, P16662, P22309, P35503, P54855, Q9HAW7, Q9HAW8, Q9HAW9

37°C, pH 7.5

673300

0.481

O60656, O75795, P16662, P22309, P35503, P54855, Q9HAW7, Q9HAW8, Q9HAW9

37°C, pH 7.5

673300

0.615

O60656, O75795, P16662, P22309, P35503, P54855, Q9HAW7, Q9HAW8, Q9HAW9

37°C, pH 7.5

673300

0.004951

acetaminophen

Gallus gallus

-

at pH 7.4 and 42°C

756511

0.005299

Rattus norvegicus

-

at pH 7.4 and 38.5°C

756511

0.01108

Bubo virginianus

-

at pH 7.4 and 39.5°C

756511

0.01591

Serinus canaria

-

at pH 7.4 and 38.5°C

756511

0.02364

Haliaeetus albicilla

-

at pH 7.4 and 40.5°C

756511

0.04134

Meleagris gallopavo

-

at pH 7.4 and 41.5°C

756511

0.09979

Struthio camelus

-

at pH 7.4 and 38.5°C

2

-

0.00036

aldosterone

Homo sapiens

P16662

isozyme UGT2B7Y268, pH 7.5, 37°C

658558

0.00076

P16662

isozyme UGT2B7H268, pH 7.5, 37°C

658558

0.0075

amitriptyline

Homo sapiens

P22310, P35503, P36537

pH 7.4, 37°C

736005

0.45

P22310, P35503, P36537

pH 7.4, 37°C

736005

0.49

P22310, P35503, P36537

pH 7.4, 37°C

736005

0.013

androstanediol

Canis lupus familiaris

Q6K1J1

pH 7.4, 37°C

657879

0.0175

Homo sapiens

-

pH 7.4, 37°C

657879

0.006

androsterone

Rattus norvegicus

-

3alpha-hydroxysteroid UDP-glucuronosyltransferase, Wistar strain

488697

0.0066

Homo sapiens

P19224

apparent Km for UGT2B7

488790

0.009

Rattus norvegicus

-

3alpha-hydroxysteroid UDP-glucuronosyltransferase activity, Sprague-Dawley strain

488697

0.01

Homo sapiens

P19224

apparent Km for UGT2B7(H)

488790

0.12

Rattus norvegicus

-

3alpha-hydroxysteroid UDP-glucuronosyltransferase activity, Wistar strain

488697

0.01

anthraflavic acid

Homo sapiens

O60656, P22309, Q9HAW7, Q9HAW9

isozyme UGT1A1, pH 6.4 or pH 7.6, 37°C

659315

0.01

O60656, P22309, Q9HAW7, Q9HAW9

isozyme UGT1A9, pH 7.6, 37°C

659315

0.0035

bakuchiol

Homo sapiens

P22309, P35503, P54855

isoform UGT2B15, at pH 7.4 and 37°C

758545

0.00441

P22309, P35503, P54855

isoform Ugt1a1, at pH 7.4 and 37°C

758545

0.01005

P22309, P35503, P54855

isoform UGT1A3, at pH 7.4 and 37°C

758545

0.397

benzo(a)pyrene-7,8-diol

Homo sapiens

-

wild-type, pH 7.4, 37°C

720625

0.426

-

mutant K75R, pH 7.4, 37°C

720625

0.168

Benzo[a]pyrene-7,8-diol

Homo sapiens

Q3SY77, Q6NUS8

with UDP-D-xylose, recombinant enzyme in microsomes, pH 7.4, 37°C

759116

0.397

Q3SY77, Q6NUS8

with UDP-D-glucose, recombinant enzyme in microsomes, pH 7.4, 37°C

759116

0.12

benzo[a]pyrene-9,10-diol

Homo sapiens

Q3SY77, Q6NUS8

with UDP-D-xylose, recombinant enzyme in microsomes, pH 7.4, 37°C

759116

0.19

Q3SY77, Q6NUS8

with UDP-D-glucose, recombinant enzyme in microsomes, pH 7.4, 37°C

759116

0.004246

beta-estradiol

Spheniscus humboldti

-

at pH 7.4 and 39°C

756511

0.00787

Gallus gallus

-

at pH 7.4 and 42°C

756511

0.01214

Rattus norvegicus

-

at pH 7.4 and 38.5°C

756511

0.01251

Haliaeetus albicilla

-

at pH 7.4 and 40.5°C

756511

0.01412

Meleagris gallopavo

-

at pH 7.4 and 41.5°C

756511

0.021

Homo sapiens

-

isoform UGT1A1, pH 7.4, 37°C

720115

0.02304

Bubo virginianus

-

at pH 7.4 and 39.5°C

756511

0.02908

Serinus canaria

-

at pH 7.4 and 38.5°C

756511

0.03512

Struthio camelus

-

at pH 7.4 and 38.5°C

756511

0.004

bilirubin

Homo sapiens

-

pH 7.5, 37°C, recombinant UGT1A1

673288

0.0062

-

pH 7.5, 37°C, liver UGT1A1

673288

0.0137

Rattus norvegicus

-

conversion to bilirubin monoglucuronide

488700

0.014

Homo sapiens

-

apparent Km for UGT1.1

488780

0.0193

Rattus norvegicus

-

conversion to bilirubin diglucuronide

488700

0.024

Homo sapiens

P19224

apparent Km for UGT1A1

488790

0.04

Macaca mulatta

-

apparent Km for microsomal preparation

488797

0.064

Rattus norvegicus

-

2.35 mM UDPglucuronate added

488720

0.0034

cannabinol

Homo sapiens

-

isoform UGT1A9, pH 7.4, 37°C

703407

0.019

-

isoform UGT1A7, pH 7.4, 37°C

703407

0.044

-

isoform UGT1A8, pH 7.4, 37°C

703407

0.059

-

isoform UGT1A10, pH 7.4, 37°C

703407

0.071

carvacrol

Homo sapiens

-

isoform UGT1A3, pH 7.4, 37°C

721114

0.078

-

isoform UGT1A9, pH 7.4, 37°C

721114

0.14

-

isoform UGT1A6, pH 7.4, 37°C

721114

0.282

-

isoform UGT1A7, pH 7.4, 37°C

721114

0.368

-

isoform UGT2B7, pH 7.4, 37°C

721114

0.004

chrysin

Homo sapiens

O60656, P22309, Q9HAW7, Q9HAW9

isozyme UGT1A1, pH 7.6, 37°C

659315

0.005

O60656, P22309, Q9HAW7, Q9HAW9

isozyme UGT1A1, pH 6.4, 37°C

659315

0.0074

cis-4-hydroxytamoxifen

Homo sapiens

O75795, P22309, P35503, P54855, Q9HAW7, Q9HAW8, Q9HAW9

pH 7.4, 37°C, isozyme UGT1A7

692033

0.015

O75795, P22309, P35503, P54855, Q9HAW7, Q9HAW8, Q9HAW9

pH 7.4, 37°C, isozyme UGT2B7

692033

0.018

O75795, P22309, P35503, P54855, Q9HAW7, Q9HAW8, Q9HAW9

pH 7.4, 37°C, isozyme UGT2B17

692033

0.02

O75795, P22309, P35503, P54855, Q9HAW7, Q9HAW8, Q9HAW9

pH 7.4, 37°C, isozyme UGT2B15

692033

0.03

O75795, P22309, P35503, P54855, Q9HAW7, Q9HAW8, Q9HAW9

pH 7.4, 37°C, isozyme UGT1A10

692033

0.041

O75795, P22309, P35503, P54855, Q9HAW7, Q9HAW8, Q9HAW9

pH 7.4, 37°C, isozyme UGT2B17

692033

0.056

O75795, P22309, P35503, P54855, Q9HAW7, Q9HAW8, Q9HAW9

pH 7.4, 37°C, isozyme UGT1A8

692033

0.07

O75795, P22309, P35503, P54855, Q9HAW7, Q9HAW8, Q9HAW9

pH 7.4, 37°C, isozyme UGT1A9

692033

0.165

O75795, P22309, P35503, P54855, Q9HAW7, Q9HAW8, Q9HAW9

pH 7.4, 37°C, isozyme UGT1A3

692033

0.193

O75795, P22309, P35503, P54855, Q9HAW7, Q9HAW8, Q9HAW9

pH 7.4, 37°C, isozyme UGT1A1

692033

0.025

clozapine

Homo sapiens

P22310

recombinant mutant isozyme UGT1A4 L48V, pH 8.4, 37°C

658530

0.049

P22310

recombinant wild-type isozyme UGT1A4, pH 8.4, 37°C

658530

0.156

codeine

Macaca fascicularis

-

apparent Km for UGT1B9, second determination

488783

0.239

-

apparent Km for UGT1B9

488783

0.4

Homo sapiens

-

isozyme UGT2B7, pH 7.5, 37°C

658516

0.1

curcumin

Homo sapiens

O60656, P22309, Q9HAW7, Q9HAW9

isozyme UGT1A1, pH 6.4, 37°C

659315

0.1

O60656, P22309, Q9HAW7, Q9HAW9

isozyme UGT1A7, pH 7.6, 37°C

659315

0.1

O60656, P22309, Q9HAW7, Q9HAW9

isozyme UGT1A8, pH 7.0, 37°C

659315

0.1

O60656, P22309, Q9HAW7, Q9HAW9

isozymes UGT1A1 and UGT1A10, pH 6.4, 37°C

659315

0.086

cyproheptadine

Homo sapiens

P22310

recombinant mutant isozyme UGT1A4 L48V, pH 8.4, 37°C

658530

0.228

P22310

recombinant wild-type isozyme UGT1A4, pH 8.4, 37°C

658530

7.4

deferiprone

Homo sapiens

-

pH 7.5, 37°C, genetic variant UGT1A6*3

703415

8.2

-

pH 7.5, 37°C, genetic variant UGT1A6*2

703415

8.2

-

pH 7.5, 37°C, genetic variant UGT1A6*4

703415

8.2

-

pH 7.5, 37°C, genetic variant UGT1A6*5

703415

10

-

pH 7.5, 37°C, genetic variant UGT1A6*1

703415

19.3

-

pH 7.5, 37°C, genetic variant UGT1A6*1, co-expression of splice variants i1 and i2

703415

0.0018

denopamine

Oryctolagus cuniculus

-

liver microsomes, substrate denopamine, pH 7.5, 37°C

658529

0.0022

Rattus norvegicus

-

liver microsomes, substrate denopamine, pH 7.5, 37°C

658529

1.48

Homo sapiens

O60656, O75795, P16662, P22309, P22310, P35503, P54855, Q9HAW7, Q9HAW8, Q9HAW9

recombinant isozyme UGT2B7, substrate denopamine, pH 7.5, 37°C

658529

1.84

Macaca fascicularis

-

liver microsomes, substrate denopamine, formation of G2 product, pH 7.5, 37°C

658529

2.87

Homo sapiens

O60656, O75795, P16662, P22309, P22310, P35503, P54855, Q9HAW7, Q9HAW8, Q9HAW9

liver micosomes, substrate denopamine, pH 7.5, 37°C

658529

2.99

O60656, O75795, P16662, P22309, P22310, P35503, P54855, Q9HAW7, Q9HAW8, Q9HAW9

jejunum microsomes, substrate denopamine, pH 7.5, 37°C

658529

3.51

Canis lupus familiaris

-

liver microsomes, substrate denopamine, formation of G2 product, pH 7.5, 37°C

658529

3.91

Macaca fascicularis

-

liver microsomes, substrate denopamine, formation of G1 product, pH 7.5, 37°C

658529

10.18

Canis lupus familiaris

-

liver microsomes, substrate denopamine, formation of G1 product, pH 7.5, 37°C

658529

3.133

desmethylnaproxen

Homo sapiens

O60656, P16662, P19224, P22309, P35503, Q9HAW7, Q9HAW9

37°C, pH 7.4

672823

3.384

O60656, P16662, P19224, P22309, P35503, Q9HAW7, Q9HAW9

37°C, pH 7.4

672823

7.724

O60656, P16662, P19224, P22309, P35503, Q9HAW7, Q9HAW9

37°C, pH 7.4

672823

0.284

dibenzo(a,l)pyrene-11,12-diol

Homo sapiens

-

wild-type, pH 7.4, 37°C

720625

0.307

-

mutant K75R, pH 7.4, 37°C

720625

0.096

dibenzo[a,1]pyrene-11,12-diol

Homo sapiens

Q3SY77, Q6NUS8

with UDP-D-glucose, recombinant enzyme in microsomes, pH 7.4, 37°C

759116

0.143

Q3SY77, Q6NUS8

with UDP-D-xylose, recombinant enzyme in microsomes, pH 7.4, 37°C

759116

0.007

diclofenac

Rattus norvegicus

-

UGT2B1

488793

0.013

-

liver microsomes

488793

0.013

Homo sapiens

-

UGT2B7

0.016

-

0.016

-

UGT1A9

488793

0.02

-

liver microsomes

488793

0.056

-

isoform UGT2B10, pH 7.4, 37°C

720115

0.069

-

isoform UGT2B7, pH 7.4, 37°C

720115

0.0023

dihydrotestosterone

Macaca fascicularis

-

apparent Km for UGT2B20

488786

0.0196

Homo sapiens

-

isoform UGT1A4, pH 7.4, 37°C

719346

0.037

diphenhydramine

Homo sapiens

P22310, P35503, P36537

pH 7.4, 37°C

736005

0.47

P22310, P35503, P36537

pH 7.4, 37°C

736005

1.89

dopamine

Homo sapiens

-

formation of dopamine-4-O-glucuronide, mutant F90A

703419

1.95

-

formation of dopamine-4-O-glucuronide, wild-type

703419

1.99

-

formation of dopamine-3-O-glucuronide, mutant F90A

703419

2.19

-

formation of dopamine-3-O-glucuronide, wild-type

703419

2.31

-

formation of dopamine-3-O-glucuronide, mutant F90L

703419

2.59

-

formation of dopamine-4-O-glucuronide, mutant F90L

703419

2.63

-

formation of dopamine-4-O-glucuronide, mutant F93A

703419

2.67

-

formation of dopamine-3-O-glucuronide, mutant F93L

703419

2.91

-

formation of dopamine-3-O-glucuronide, mutant F93A

703419

3.11

-

formation of dopamine-4-O-glucuronide, mutant F93L

703419

0.021

entacapone

Homo sapiens

O60656, P16662, P22309, P35503, P54855

isozyme UGT1A9, pH 7.4, 37°C

657537

0.0457

-

membrane-bound recombinant isoform UGT1A10 from CHO cells, at pH 7.4 and 37°C

756560

0.0569

-

membrane-bound recombinant isoform UGT1A10 from HEK-293 cells, at pH 7.4 and 37°C

756560

0.294

O60656, P16662, P22309, P35503, P54855

isozyme UGT1A3, pH 7.4, 37°C

657537

0.554

-

with phospholipid purified recombinant isoform UGT1A10 from CHO cells, at pH 7.4 and 37°C

756560

0.703

-

without phospholipid purified recombinant isoform UGT1A10 from CHO cells, at pH 7.4 and 37°C

756560

0.0017

Epitestosterone

Homo sapiens

-

isoform UGT2B7, pH 7.4, 37°C

703416

0.0116

-

isoform UGT2A1, pH 7.4, 37°C

703416

0.0049

estradiol

Homo sapiens

Q9HAW8

37°C, pH 8.0, mutant enzyme F90L

677147

0.0078

Q9HAW8

37°C, pH 8.0, mutant enzyme F93A

677147

0.0095

Macaca fascicularis

A0A4Y1K7J9, A0A4Y1KAF7

isoform UGT2B30, at pH 7.4, temperature not specified in the publication

756022

0.013

A0A4Y1K7J9, A0A4Y1KAF7

isoform UGT2B9, at pH 7.4, temperature not specified in the publication

756022

0.0138

Homo sapiens

Q9HAW8

37°C, pH 8.0, wild-type enzyme

677147

0.035

Rattus norvegicus

-

pH 7.4, 37°C

692039

0.042

Mus musculus

-

pH 7.4, 37°C

692039

2.3

Macaca fascicularis

A0A4Y1K7J9, A0A4Y1KAF7

enzyme from liver microsome, at pH 7.4, temperature not specified in the publication

756022

13

Platyrrhini

-

488795

0.0388

estriol

Homo sapiens

Q9HAW8

37°C, pH 8.0, wild-type enzyme

677147

0.0467

Q9HAW8

37°C, pH 8.0, mutant enzyme F93A

677147

0.0035

estrone

-

0.0063

37°C, pH 8.0, mutant enzyme F93A

677147

0.015

Oryctolagus cuniculus

-

488728

0.0421

Homo sapiens

Q9HAW8

37°C, pH 8.0, wild-type enzyme

677147

8.03

ethanol

Homo sapiens

O60656, P16662, P19224, P22309, P22310, P35503, P36537, P54855

pH 7.4, 37°C, enzyme UGT2B15

735425

10.33

O60656, P16662, P19224, P22309, P22310, P35503, P36537, P54855

pH 7.4, 37°C, enzyme UGT1A1

735425

12.05

O60656, P16662, P19224, P22309, P22310, P35503, P36537, P54855

pH 7.4, 37°C, enzyme UGT1A4

735425

21.46

O60656, P16662, P19224, P22309, P22310, P35503, P36537, P54855

pH 7.4, 37°C, enzyme UGT1A6

735425

26.17

O60656, P16662, P19224, P22309, P22310, P35503, P36537, P54855

pH 7.4, 37°C, enzyme UGT1A9

735425

32.41

O60656, P16662, P19224, P22309, P22310, P35503, P36537, P54855

pH 7.4, 37°C, enzyme UGT2B7

735425

35.07

O60656, P16662, P19224, P22309, P22310, P35503, P36537, P54855

pH 7.4, 37°C, enzyme UGT2B10

735425

40.04

O60656, P16662, P19224, P22309, P22310, P35503, P36537, P54855

pH 7.4, 37°C, enzyme UGT1A3

735425

0.44

etoposide

Homo sapiens

P22309

liver microsomes, pH 7.4, 37°C

658521

0.5

P22309

recombinant isozyme UGT1A1, pH 7.4, 37°C

658521

0.0084

eugenol

Homo sapiens

O60656, P22309, Q9HAW7, Q9HAW9

isozyme UGT1A10, pH 7.6, 37°C

659315

0.0159

O60656, P22309, Q9HAW7, Q9HAW9

isozyme UGT1A7, pH 6.4, 37°C

659315

0.0245

O60656, P22309, Q9HAW7, Q9HAW9

isozyme UGT1A10, pH 6.4, 37°C

659315

0.0257

O60656, P22309, Q9HAW7, Q9HAW9

isozyme UGT1A7, pH 8.5, 37°C

659315

0.0209

frusemide

Homo sapiens

-

mutant M33T, pH 7.4, 37°C

718805

0.129

-

mutant M33V, pH 7.4, 37°C

718805

0.183

-

mutant M33Q, pH 7.4, 37°C

718805

0.187

-

mutant M33I, pH 7.4, 37°C

718805

0.229

-

wildtype, pH 7.4, 37°C

718805

0.0022

gemfibrozil

Homo sapiens

-

pH 7.5, 37°C, isozyme UGT2B7

692034

0.0195

-

pH 7.4, 37°C

657879

0.139

Canis lupus familiaris

Q6K1J1

pH 7.4, 37°C

657879

2.1

grepafloxacin

Homo sapiens

O60656, P22309, P35503, Q9HAW7

isozyme UGT1A9, pH 7.4, 37°C

658531

2.7

O60656, P22309, P35503, Q9HAW7

isozyme UGT1A1, pH 7.4, 37°C

658531

5.2

O60656, P22309, P35503, Q9HAW7

liver microsomes, pH 7.4, 37°C

658531

0.011

hyodeoxycholic acid

Homo sapiens

P19224

apparent Km for UGT2B7(H)

0.021

native UGT2B4

0.025

native UGT2B4

0.029

mutant UGT2B4(Y33L)

0.039

mutant UGT2B4(Y33F)

0.044

recombinant genetic variant UGT2A3.2

694264

0.069

Q6UWM9

recombinant genetic variant UGT2A3.1

0.091

mutant UGT2B4(F33Y)

0.27

apparent Km for UGT2B4

488790

0.0072

imipramine

Homo sapiens

P22310, P35503, P36537

pH 7.4, 37°C

736005

0.037

Oryctolagus cuniculus

-

UGT1A41

488782

0.071

Homo sapiens

-

UGT1A4 expressed on B lymphoblastoid cells

488799

0.097

-

high affinity component from liver microsomes

488799

0.14

Oryctolagus cuniculus

-

UGT1A71

488782

0.276

Homo sapiens

P22310

recombinant mutant isozyme UGT1A4 L48V, pH 8.4, 37°C

658530

0.5

P22310, P35503, P36537

pH 7.4, 37°C

736005

0.7

-

low affinity component from liver microsomes

488799

0.76

P22310, P35503, P36537

pH 7.4, 37°C

736005

1.1

P22310

imipramine N-glucuronide formation

692032

1.4

P22310

imipramine N-glucuronide formation, 1A4 co-expressed with isoform 1A4

692032

1.4

P22310

imipramine N-glucuronide formation, 1A4 co-expressed with isoform 1A6

692032

1.442

P22310

recombinant wild-type isozyme UGT1A4, pH 8.4, 37°C

658530

0.48

Ketoprofen

Homo sapiens

-

pH 7.4, 37°C

657879

1.695

Canis lupus familiaris

Q6K1J1

pH 7.4, 37°C

657879

0.368

labetalol

Homo sapiens

O60656, P06133, P16662, P19224, P22309, P22310

pH 7.5, 37°C, recombinant isozyme UGT1A9

695271

0.386

O60656, P06133, P16662, P19224, P22309, P22310

pH 7.5, 37°C, recombinant isozyme UGT2B7

695271

0.956

O60656, P06133, P16662, P19224, P22309, P22310

pH 7.5, 37°C, recombinant isozyme UGT1A1

695271

0.774

lamotrigine

Homo sapiens

-

isoform UGT1A1 mutant H39P

703410

1.564

-

isoform UGT1A4, pH 7.4, 37°C

719346

1.579

-

isoform UGT1A4

703410

3.812

-

isoform UGT1A9 mutant H37P

703410

2.6

levofloxacin

Homo sapiens

O60656, P22309, P35503, Q9HAW7

isozyme UGT1A9, pH 7.4, 37°C

658531

6

O60656, P22309, P35503, Q9HAW7

isozyme UGT1A1, pH 7.4, 37°C

658531

10

O60656, P22309, P35503, Q9HAW7

liver microsomes, pH 7.4, 37°C

658531

0.028

MOCAc-Lys-Arg-Gly-Leu-Tyr-Phe-Ile-Thr-His-Lys(Dnp)

native UGT2B4

0.117

mutant UGT2B4(Y33F)

0.131

mutant UGT2B4(F33Y)

0.173

mutant UGT2B4(F33L)

0.012

montanoyl-CoA

mutant UGT2B4(Y33L)

0.081

native UGT2B4

0.0355

morphine

Homo sapiens

P22309

pH 7.5, 37°C, isozyme UGT1A8, at 0.05 mM morphine

692045

0.0404

P22309

pH 7.5, 37°C, isozyme UGT1A1, at 0.05 mM morphine

692045

0.0679

P22309

pH 7.5, 37°C, isozyme UGT1A1, at 2.5 mM morphine

692045

0.0681

P22309

pH 7.5, 37°C, isozyme UGT1A8, at 2.5 mM morphine

692045

0.2

P16662

isozyme UGT2B7 in COS-1 cell microsomes, pH 7.8, 37°C, in presence with CYP2C9

659973

0.24

Mus musculus

Q3UEP4, Q63886, Q8K154, Q8VCN3

isoform Ugt2b36, at pH 7.4 and 37°C

757475

0.32

Rattus norvegicus

-

pH 7.4, 37°C

692039

0.33

Macaca fascicularis

-

apparent Km for UGT1B9, formation of 3-glucuronide

488783

0.38

Homo sapiens

P16662

isozyme UGT2B7 in COS-1 cell microsomes, pH 7.8, 37°C

659973

0.42

-

morphine 3-glucuronide formation, recombinant isozyme UGT2B7, pH 7.4, 37°C

658515

0.48

P16662

isozyme UGT2B7 in COS-1 cell microsomes, pH 7.8, 37°C, in presence with CYP1A2

659973

0.63

-

morphine 6-glucuronide formation, isozyme UGT2B7, pH 7.5, 37°C

658516

0.67

-

morphine 3-glucuronide formation, isozyme UGT2B7, pH 7.5, 37°C

658516

0.97

-

morphine 6-glucuronide formation, recombinant isozyme UGT2B7, pH 7.4, 37°C

658515

1.18

P16662

liver microsomes, pH 7.8, 37°C

659973

1.2

Macaca fascicularis

A0A4Y1K7J9, A0A4Y1KAF7

isoform UGT2B30, at pH 7.4, temperature not specified in the publication

756022

1.3

A0A4Y1K7J9, A0A4Y1KAF7

isoform UGT2B9, at pH 7.4, temperature not specified in the publication

756022

2.38

Mus musculus

-

pH 7.4, 37°C

692039

2.6

Homo sapiens

-

morphine 3-glucuronide formation, recombinant isozyme UGT1A8, pH 7.4, 37°C

658515

2.7

Macaca fascicularis

A0A4Y1K7J9, A0A4Y1KAF7

enzyme from liver microsome, at pH 7.4, temperature not specified in the publication

756022

3.2

Homo sapiens

-

morphine 3-glucuronide formation, recombinant isozyme UGT1A3, pH 7.4, 37°C

658515

3.71

P16662

isozyme UGT2B7 in COS-1 cell microsomes, pH 7.8, 37°C, in presence with CYP3A4

659973

7.3

-

membrane-bound recombinant isoform UGT1A10 from CHO cells, at pH 7.4 and 37°C

756560

10.4

-

membrane-bound recombinant isoform UGT1A10 from HEK-293 cells, at pH 7.4 and 37°C

756560

12.6

-

morphine 3-glucuronide formation, recombinant isozyme UGT1A10, pH 7.4, 37°C

658515

18

-

morphine 3-glucuronide formation, recombinant isozyme UGT1A6, pH 7.4, 37°C

658515

18.7

-

morphine 3-glucuronide formation, recombinant isozyme UGT1A1, pH 7.4, 37°C

658515

37.4

-

morphine 3-glucuronide formation, recombinant isozyme UGT1A9, pH 7.4, 37°C

658515

1.15

morphine 3-glucuronide

Homo sapiens

-

pH 7.4, 37°C

657879

1.425

Canis lupus familiaris

Q6K1J1

pH 7.4, 37°C

657879

1.9

moxifloxacin

Homo sapiens

O60656, P22309, P35503, Q9HAW7

liver microsomes, pH 7.4, 37°C

658531

2.1

O60656, P22309, P35503, Q9HAW7

isozyme UGT1A9, pH 7.4, 37°C

658531

3.4

O60656, P22309, P35503, Q9HAW7

isozyme UGT1A1, pH 7.4, 37°C

658531

0.34

mycophenolate

Rattus norvegicus

-

pH 7.4, 37°C

692039

1.272

Mus musculus

-

pH 7.4, 37°C

692039

0.046

Mycophenolic acid

Homo sapiens

-

mutant M33Q, pH 7.4, 37°C

718805

0.087

-

wildtype, pH 7.4, 37°C

718805

0.157

-

mutant M33I, pH 7.4, 37°C

718805

0.16

-

isozyme UGT1A9

658528

0.18

-

liver microsomes

658528

0.2

-

mutant M33V, pH 7.4, 37°C

718805

0.336

-

mutant M33T, pH 7.4, 37°C

718805

0.06

nalorphine

Macaca fascicularis

-

apparent Km for UGT1B9

488783

0.065

-

apparent Km for UGT1B9, second determination

488783

0.045

naloxone

Macaca fascicularis

-

apparent Km for UGT1B9

488783

0.048

-

apparent Km for UGT1B9, second determination

488783

0.05

Naltrexone

Macaca fascicularis

-

apparent Km for UGT1B9

488783

0.067

-

apparent Km for UGT1B9, second determination

488783

0.072

naproxen

Homo sapiens

O60656, P16662, P19224, P22309, P35503, Q9HAW7, Q9HAW9

37°C, pH 7.4

672823

0.25

-

pH 7.4, 37°C

657879

0.58

Canis lupus familiaris

Q6K1J1

pH 7.4, 37°C

657879

0.855

Homo sapiens

O60656, P16662, P19224, P22309, P35503, Q9HAW7, Q9HAW9

37°C, pH 7.4

672823

4.375

O60656, P16662, P19224, P22309, P35503, Q9HAW7, Q9HAW9

37°C, pH 7.4

672823

0.135

niflumic acid

-

7.344

-

0.702

oxymorphone

Macaca fascicularis

-

apparent Km for UGT1B9

488783

0.775

-

apparent Km for UGT1B9, second determination

488783

5.06

p-ethoxyphenylurea

Homo sapiens

O60656, P19224, P22309, P22310, P35503, Q9HAW7

-

671661

6.99

O60656, P19224, P22309, P22310, P35503, Q9HAW7

-

671661

0.0198

Phenylbutazone

C-glucuronidation

0.1951

O-glucuronidation

0.0068

phloretin

Homo sapiens

O60656, P22309, Q9HAW7, Q9HAW9

isozyme UGT1A8, pH 7.0, 37°C

659315

0.045

O60656, P22309, Q9HAW7, Q9HAW9

isozyme UGT1A10, pH 6.4, 37°C

659315

0.0964

O60656, P22309, Q9HAW7, Q9HAW9

isozyme UGT1A7, pH 6.4, 37°C

659315

0.0072

propofol

Homo sapiens

O60656

pH 7.4, 37°C, isozyme UGT1A9 in presence of 2% fatty acid-free human serum albumin

692035

0.0106

O60656

pH 7.4, 37°C, liver microsomes in presence of 2% fatty acid-free human serum albumin

692035

0.026

-

wildtype, pH 7.4, 37°C

718805

0.041

O60656

pH 7.4, 37°C, isozyme UGT1A9

692035

0.07

-

mutant M33Q, pH 7.4, 37°C

718805

0.109

-

mutant M33V, pH 7.4, 37°C

718805

0.113

-

mutant M33I, pH 7.4, 37°C

718805

0.113

-

mutant M33T, pH 7.4, 37°C

718805

0.127

O60656

pH 7.4, 37°C, liver microsomes

692035

0.17

-

pH 7.5, 37°C, isozyme UGT1A9

694249

0.211

Protocatechuic aldehyde

Homo sapiens

P19224

pH 7.5, 37°C, recombinant isozyme UGT1A6, formation of product M2

692038

0.2385

P19224

pH 7.5, 37°C, recombinant isozyme UGT1A9, formation of product M2

692038

0.337

P19224

pH 7.5, 37°C, liver microsomes, formation of product M2

692038

0.3675

P19224

pH 7.5, 37°C, recombinant isozyme UGT1A6, formation of product M1

692038

0.38

P19224

pH 7.5, 37°C, recombinant isozyme UGT1A9, formation of product M1

692038

0.433

P19224

pH 7.5, 37°C, liver microsomes, formation of product M1

692038

0.494

P19224

pH 7.5, 37°C, intestine microsomes, formation of product M2

692038

0.627

P19224

pH 7.5, 37°C, intestine microsomes, formation of product M1

692038

0.032

retigabine

Homo sapiens

-

wildtype, pH 7.4, 37°C

718805

0.055

-

mutant M33Q, pH 7.4, 37°C

718805

0.058

-

mutant H37A

706582

0.062

-

mutant M33V, pH 7.4, 37°C

718805

0.068

-

mutant M33T, pH 7.4, 37°C

718805

0.09

-

wild-type

706582

0.099

-

mutant M33I, pH 7.4, 37°C

718805

0.034

S-naproxen

Homo sapiens

-

pH 7.4, 37°C, renal cortex microsomes

693814

0.045

-

pH 7.4, 37°C, renal medulla microsomes

693814

0.061

scopoletin

Homo sapiens

-

apparent Km for membrane-bound UGT1AB

488801

0.062

-

mutant D143A

706582

0.08

-

wild-type isozyme UGT1A9

694254

0.083

-

wild-type

706582

0.29

-

wild-type isozyme UGT1A6

694254

0.629

-

mutant D148A

706582

0.79

-

apparent Km for purified UGT1AB

488801

0.954

-

mutant H37A

706582

1.64

-

H369A mutant isozyme UGT1A9

694254

3.88

-

H371A mutant isozyme UGT1A6

694254

7.64

-

H379A mutant isozyme UGT1A6

694254

3.7

serotonin

Homo sapiens

P22310

serotonin O-glucuronide formation, 1A4 co-expressed with isoform 1A6

692032

4.4

P22310

serotonin O-glucuronide formation, 1A4 co-expressed with isoform 1A4

692032

4.6

P22310

serotonin O-glucuronide formation

692032

4.9

P19224

lung UGT1A6, pH 7.5, 37°C

658518

5.2 - 8.8

P19224

liver UGT1A6, pH 7.5, 37°C

658518

5.73

Macaca fascicularis

-

37°C, pH 7.4

673033

6.5

Homo sapiens

P19224

kidney UGT1A6, pH 7.5, 37°C

658518

8.6

P19224

37°C, pH 7.4

673033

9.8

-

pH 7.5, 37°C, genetic variant UGT1A6*1

703415

9.9

-

pH 7.5, 37°C, genetic variant UGT1A6*1, co-expression of splice variants i1 and i2

703415

12.4

P19224

intestine UGT1A6, pH 7.5, 37°C

658518

55.9

P19224

recombinant UGT1A6 from lymphoblasts or insect cells, pH 7.5, 37°C

658518

1.9

Sitafloxacin

Homo sapiens

O60656, P22309, P35503, Q9HAW7

isozyme UGT1A1, pH 7.4, 37°C

658531

3.7

O60656, P22309, P35503, Q9HAW7

liver microsomes, pH 7.4, 37°C

658531

6.3

O60656, P22309, P35503, Q9HAW7

isozyme UGT1A9, pH 7.4, 37°C

658531

0.014

sulfinpyrazone

Homo sapiens

-

wildtype, pH 7.4, 37°C

718805

0.032

-

mutant M33I, pH 7.4, 37°C

718805

0.033

-

mutant M33Q, pH 7.4, 37°C

718805

0.039

-

mutant M33V, pH 7.4, 37°C

718805

0.053

-

mutant M33T, pH 7.4, 37°C

718805

0.0038

testosterone

Homo sapiens

O60656, O75795, P16662, P22310, P54855

37°C, pH 7.4

673304

0.0046

Macaca fascicularis

-

apparent Km for UGT2B20

488786

0.0057

Homo sapiens

O60656, O75795, P16662, P22310, P54855

37°C, pH 7.4

673304

0.01

-

isoform UGT2B17, pH 7.4, 37°C

703416

0.012

Rattus norvegicus

-

17beta-hydroxysteroid UDP-glucuronosyltransferase activity, Wistar strain

488697

0.012

-

1-naphthol added, in presence of 5 mM MgCl2 as activator

488724

0.013

-

17beta-hydroxysteroid UDP-glucuronosyltransferase activity, Sprague-Dawley strain

488697

0.02

-

17beta-hydroxysteroid UDP-glucuronosyltransferase activity, Wistar strain

488697

0.0387

Homo sapiens

-

isoform UGT2A1, pH 7.4, 37°C

703416

0.007

tigogenin

Homo sapiens

P22310

recombinant mutant isozyme UGT1A4 L48V, pH 8.4, 37°C

658530

0.008

P22310

recombinant wild-type isozyme UGT1A4, pH 8.4, 37°C

658530

0.0506

tranilast

Homo sapiens

P22309

activity in human jejunum microsomes

673306

0.0515

P22309

activity in human liver microsomes

673306

0.0037

trans-4-hydroxytamoxifen

Homo sapiens

-

isoform UGT2B7, variant 268His, pH 7.4, 37°C

703017

0.004

O75795, P22309, P35503, P54855, Q9HAW7, Q9HAW8, Q9HAW9

pH 7.4, 37°C, isozyme UGT2B7

692033

0.0087

-

isoform UGT2B7, variant 268Tyr, pH 7.4, 37°C

703017

0.023

O75795, P22309, P35503, P54855, Q9HAW7, Q9HAW8, Q9HAW9

pH 7.4, 37°C, isozyme UGT1A8

692033

0.023

-

isoform UGT1A8, variant 173Ala/277Cys, pH 7.4, 37°C

703017

0.043

-

isoform UGT1A8, variant 173Gly/277Cys, pH 7.4, 37°C

703017

0.052

-

isoform UGTA10, variant 139Lys, pH 7.4, 37°C

703017

0.094

O75795, P22309, P35503, P54855, Q9HAW7, Q9HAW8, Q9HAW9

pH 7.4, 37°C, isozyme UGT1A3

692033

0.096

O75795, P22309, P35503, P54855, Q9HAW7, Q9HAW8, Q9HAW9

pH 7.4, 37°C, isozyme UGT1A10

692033

0.096

-

isoform UGTA10, variant 139Glu, pH 7.4, 37°C

703017

0.124

O75795, P22309, P35503, P54855, Q9HAW7, Q9HAW8, Q9HAW9

pH 7.4, 37°C, isozyme UGT1A1

692033

0.166

O75795, P22309, P35503, P54855, Q9HAW7, Q9HAW8, Q9HAW9

pH 7.4, 37°C, isozyme UGT1A7

692033

0.319

O75795, P22309, P35503, P54855, Q9HAW7, Q9HAW8, Q9HAW9

pH 7.4, 37°C, isozyme UGT1A9

692033

0.008

trans-androsterone

Homo sapiens

P22310

recombinant mutant isozyme UGT1A4 L48V, pH 8.4, 37°C

658530

0.0236

-

isoform UGT1A4, pH 7.4, 37°C

719346

0.255

P22310

recombinant wild-type isozyme UGT1A4, pH 8.4, 37°C

658530

0.013

trans-endoxifen

Homo sapiens

-

isoform UGTA10, variant 139Lys, pH 7.4, 37°C

703017

0.04

-

isoform UGTA10, variant 139Glu, pH 7.4, 37°C

703017

0.098

-

isoform UGT1A8, variant 173Ala/277Cys, pH 7.4, 37°C

703017

0.101

-

isoform UGT2B7, variant 268His, pH 7.4, 37°C

703017

0.101

-

isoform UGT2B7, variant 268Tyr, pH 7.4, 37°C

703017

0.135

-

isoform UGT1A8, variant 173Gly/277Cys, pH 7.4, 37°C

703017

0.0197

Trifluoperazine

Homo sapiens

P22310

trifluoperazine N-glucuronide formation

692032

0.0198

P22310

trifluoperazine N-glucuronide formation, 1A4 co-expressed with isoform 1A4

692032

0.044

-

isoform UGT1A4

703410

0.048

P22310

trifluoperazine N-glucuronide formation, 1A4 co-expressed with isoform 1A6

692032

0.305

-

isoform UGT1A1 mutant H39P

703410

0.136

troglitazone

-

0.136

-

0.138

UDP-glucuronate

Homo sapiens

-

mutant D143A

706582

0.173

-

mutant H37A

706582

0.179

-

wild-type

706582

0.184

-

mutant D148A

706582

0.229

UDP-glucuronic acid

Homo sapiens

-

apparent Km for membrane-bound UGT1AB

488801

0.26

Rattus norvegicus

-

apparent Km for UGT1A6, 50mM 1-naphthol, mutants that retained activity shows similar Km values

488787

0.704

Homo sapiens

-

apparent Km for purified UGT1AB

488801

0.3

UDPglucuronate

Rattus norvegicus

-

488697

0.36

Felis catus

-

0.017 mM bilirubin monoglucuronide added, at pH 6.5

488699

0.37

Rattus norvegicus

-

2 mM 1-naphthol added, in presence of 50 mM MgCl2

488724

0.44

Felis catus

-

0.016 mM bilirubin monoglucuronide added, at pH 8.1

488699

0.59

Rattus norvegicus

-

0.2 mM 1-naphthol added, no activator present

488724

0.71

-

0.2 mM 1-naphthol added, in presence of 50 mM MgCl2, 0.1% Triton X-100 as activator

488724

1

-

488756

1.06

-

0.125 mM bilirubin added

488720

0.0036

UDPglucuronic acid

Oryctolagus cuniculus

-

1.5 mM morphine added, ethanol-induced enzyme

488713

0.0054

-

1.5 mM morphine added, non-induced enzyme

488713

0.0065

-

0.75 mM 1-naphthol added, ethanol-induced enzyme

488713

0.0084

-

0.76 mM 1-naphthol added, non-induced enzyme

488713

0.025

Sus scrofa

-

488742

0.16

-

488753

0.22

-

0.96

-

5.4

-

0.111

umbelliferone

Homo sapiens

O60656, P16662, P22309, P35503, P54855

isozyme UGT1A9, pH 7.4, 37°C

657537

0.294

O60656, P16662, P22309, P35503, P54855

isozyme UGT1A1, pH 7.4, 37°C

657537

0.339

O60656, P16662, P22309, P35503, P54855

isozyme UGT2B15, pH 7.4, 37°C

657537

0.00579

xanthotoxol

Homo sapiens

P16662, P19224, P22309, P35503, Q9HAW8, Q9HAW9

enzyme from liver microsomes, at pH 7.4 and 37°C

758547

0.0125

P16662, P19224, P22309, P35503, Q9HAW8, Q9HAW9

isoform UGT1A10, at pH 7.4 and 37°C

758547

0.0345

P16662, P19224, P22309, P35503, Q9HAW8, Q9HAW9

enzyme from intestinal microsomes, at pH 7.4 and 37°C

758547

0.04191

P16662, P19224, P22309, P35503, Q9HAW8, Q9HAW9

isoform UGT1A6, at pH 7.4 and 37°C

758547

0.2024

P16662, P19224, P22309, P35503, Q9HAW8, Q9HAW9

isoform UGT1A8, at pH 7.4 and 37°C

758547

0.2586

P16662, P19224, P22309, P35503, Q9HAW8, Q9HAW9

isoform UGT1A3, at pH 7.4 and 37°C

758547

0.4593

P16662, P19224, P22309, P35503, Q9HAW8, Q9HAW9

isoform Ugt1a1, at pH 7.4 and 37°C

758547

0.508

zidovudine

Homo sapiens

P16662

pH 7.4, 37°C, recombinant HA-tagged wild-type dimer

735648

0.519

P16662

pH 7.4, 37°C, recombinant CFP-tagged mutant H268Y dimer

735648

0.534

P16662

pH 7.4, 37°C, recombinant HA-tagged mutant A71S dimer

735648

0.54

P16662

pH 7.4, 37°C, recombinant dimer of CFP-tagged H268Y and HA-tagged D398N mutant monomers

735648

0.57

P16662

pH 7.4, 37°C, recombinant HA-tagged mutant H268Y dimer

735648

0.589

P16662

pH 7.4, 37°C, recombinant dimer of CFP-tagged A71S and HA-tagged D398N mutant monomers

735648

0.605

P16662

pH 7.4, 37°C, recombinant CFP-tagged wild-type dimer

735648

0.605

P16662

pH 7.4, 37°C, recombinant dimer of CFP-tagged wild-type and HA-tagged D398N mutant monomers

735648

0.609

P16662

pH 7.4, 37°C, recombinant dimer of CFP-tagged A71S and HA-tagged H268Y mutant monomers

735648

0.634

P16662

pH 7.4, 37°C, recombinant CFP-tagged mutant A71S dimer

735648

0.706

P16662

pH 7.4, 37°C, recombinant dimer of CFP-tagged wild-type and HA-tagged A71S mutant monomers

735648

0.841

P16662

pH 7.4, 37°C, recombinant dimer of CFP-tagged wild-type and HA-tagged H268Y mutant monomers

735648

additional information

-

-

-

-

-

-

-

-

-

-

-

-

kinetics

-

kinetics

-

kinetics

-

kinetics

-

kinetics

-

kinetics

-

kinetics

657879

-

kinetics

658515

-

kinetics

660431

-

kinetics

-

kinetics

-

kinetics

-

kinetics

-

Canis lupus familiaris

Q6K1J1

kinetics

657879

-

kinetics

-

kinetics

-

kinetics

658558

-

P19224

kinetics

658518

-

kinetics

-

kinetics

-

kinetics

-

kinetics

-

kinetics

-

kinetics

659315

-

O60656

kinetics

659971

-

kinetics

659971

-

Sus scrofa

-

effect of temperature

488714

-

Homo sapiens

P19224

Km values for 31 xenobiotics reported

488790

-

Km values for all endogenous substrates for UGT2B7 range from 0.006 to 0.1 mM

488794

-

Platyrrhini

-

kinetic analysis of UGT2B15, UGT2B17 and UGT2B20 mutant proteins for 5 alpha-androstane-3alpha-17beta-diol, dihydrotestosterone and testosterone

488791

-

Homo sapiens

O75795

kinetic analysis of UGT2B15, UGT2B17 and UGT2B20 mutant proteins for 5 alpha-androstane-3alpha-17beta-diol, dihydrotestosterone and testosterone

488791

-

kinetic analysis of UGT2B15, UGT2B17 and UGT2B20 mutant proteins for 5 alpha-androstane-3alpha-17beta-diol, dihydrotestosterone and testosterone

488791

-

Gallus gallus

-

effect of UDP-N-acetylglucosamine as activator

488746

-

Mus musculus

-

effect of UDP-N-acetylglucosamine as activator

488746

-

Cavia porcellus

-

kinetics of phospholipase-treated, UDP-N-acetylglucosamine-activated, detergent-activated and sonicated enzyme

488750

-

Mus musculus

-

kinetics of phospholipase-treated, UDP-N-acetylglucosamine-activated, detergent-activated and sonicated enzyme

488750

-

Rattus norvegicus

-

kinetics of phospholipase-treated, UDP-N-acetylglucosamine-activated, detergent-activated and sonicated enzyme

488750

-

Homo sapiens

P36537

Michaelis-Menten kinetics

736012

-

Michaelis-Menten kinetics

736012

-

Q3SY77

Michaelis-Menten kinetics

759116

-

Q6NUS8

Michaelis-Menten kinetics

759116

-

Michaelis-Menten kinetics

759116

-

different kinetic profiles of isozymes with different hormone substrates, overview

659571

-

hyperbolic and sigmoidal kinetics for 4-methylumbelliferone and 1-naphthol for different isozymes, empirical and two-site models, overview

658524

-

O60656

hyperbolic and sigmoidal kinetics for 4-methylumbelliferone and 1-naphthol for different isozymes, empirical and two-site models, overview

658524

-

P16662

hyperbolic and sigmoidal kinetics for 4-methylumbelliferone and 1-naphthol for different isozymes, empirical and two-site models, overview

658524

-

P22309

hyperbolic and sigmoidal kinetics for 4-methylumbelliferone and 1-naphthol for different isozymes, empirical and two-site models, overview

658524

-

P22310

hyperbolic and sigmoidal kinetics for 4-methylumbelliferone and 1-naphthol for different isozymes, empirical and two-site models, overview

658524

-

P35503

hyperbolic and sigmoidal kinetics for 4-methylumbelliferone and 1-naphthol for different isozymes, empirical and two-site models, overview

658524

-

P54855

hyperbolic and sigmoidal kinetics for 4-methylumbelliferone and 1-naphthol for different isozymes, empirical and two-site models, overview

658524

-

Q9HAW7

hyperbolic and sigmoidal kinetics for 4-methylumbelliferone and 1-naphthol for different isozymes, empirical and two-site models, overview

658524

-

Q9HAW8

hyperbolic and sigmoidal kinetics for 4-methylumbelliferone and 1-naphthol for different isozymes, empirical and two-site models, overview

658524

-

Q9HAW9

hyperbolic and sigmoidal kinetics for 4-methylumbelliferone and 1-naphthol for different isozymes, empirical and two-site models, overview

658524

-

kinetics of microsomes from different tissues

658528

-

kinetics, at different conditions with different activators and different substrates, microsomes or recombinant isozymes, overview

658522

-

kinetics, different isozymes

658516

-

O60656

kinetics, different isozymes, pH-values, and substrates

659315

-

P22309

kinetics, different isozymes, pH-values, and substrates

659315

-

Q9HAW7

kinetics, different isozymes, pH-values, and substrates

659315

-

Q9HAW9

kinetics, different isozymes, pH-values, and substrates

659315

-

kinetics, different isozymes, pH-values, and substrates

659315

-

O60656

Michaelis-Menten kinetics, overview

735425

-

P16662

Michaelis-Menten kinetics, overview

735425

-

P19224

Michaelis-Menten kinetics, overview

735425

-

P22309

Michaelis-Menten kinetics, overview

735425

-

P22310

Michaelis-Menten kinetics, overview

735425

-

P35503

Michaelis-Menten kinetics, overview

735425

-

P36537

Michaelis-Menten kinetics, overview

735425

-

P54855

Michaelis-Menten kinetics, overview

735425

-

Michaelis-Menten kinetics, overview

735425

-

P16662

kinetic analysis, overview

693343

-

kinetic analysis, overview

693343

-

bisubstrate kinetics of wild-type and mutant isozyme UGT1A6

694254

-

co-expression of both UGT1A1 and UGT1A4 increases the Vmax values of UGT1A6-catalyzed serotonin and diclofenac O-glucuronide formation

692032

-

P22310

co-expression of both UGT1A1 and UGT1A4 increases the Vmax values of UGT1A6-catalyzed serotonin and diclofenac O-glucuronide formation

692032

-

coexpression of UGT1A1 decreases the Vmax value of UGT1A4-catalyzed imipramine N-glucuronide formation but has no effect on UGT1A4-catalyzed trifluoperazine N-glucuronide formation. Coexpression of UGT1A6 has no effect on UGT1A4-catalyzed imipramine N-glucuronide formation but increases the Km and Vmax of UGT1A4-catalyzed trifluoperazine N-glucuronide formation

692032

-

P22310

coexpression of UGT1A1 decreases the Vmax value of UGT1A4-catalyzed imipramine N-glucuronide formation but has no effect on UGT1A4-catalyzed trifluoperazine N-glucuronide formation. Coexpression of UGT1A6 has no effect on UGT1A4-catalyzed imipramine N-glucuronide formation but increases the Km and Vmax of UGT1A4-catalyzed trifluoperazine N-glucuronide formation

692032

-

enzyme kinetics with substrate gemfibrozil follow Michaelis-Menten kinetics

692034

-

frusemide glucuronidation followed MichaelisMenten kinetics in all tissues, kinetics of different microsome types from liver and kidney, overview

690855

-

P16662

glucuronidation of the non-selective substrate 4-methylumbelliferone by mutant chimeric UGT2B7-15(61194)-7 and isozyme UGT2B15 followed MichaelisMenten and weak substrate inhibition kinetics, respectively, overview

690847

-

P54855

glucuronidation of the non-selective substrate 4-methylumbelliferone by mutant chimeric UGT2B7-15(61194)-7 and isozyme UGT2B15 followed MichaelisMenten and weak substrate inhibition kinetics, respectively, overview

690847

-

glucuronidation of the non-selective substrate 4-methylumbelliferone by mutant chimeric UGT2B7-15(61194)-7 and isozyme UGT2B15 followed MichaelisMenten and weak substrate inhibition kinetics, respectively, overview

690847

-

P16662

glucuronidation of the non-selective substrate 4-methylumbelliferone by mutant chimeric UGT2B7-15(61194)-7 follows MichaelisMenten and weak substrate inhibition kinetics, respectively, whereas 4-methylumbelliferone glucuronidation by isozyme UGT2B7 exhibited sigmoidal kinetics characteristic of autoactivation, overview

690847

-

P54855

glucuronidation of the non-selective substrate 4-methylumbelliferone by mutant chimeric UGT2B7-15(61194)-7 follows MichaelisMenten and weak substrate inhibition kinetics, respectively, whereas 4-methylumbelliferone glucuronidation by isozyme UGT2B7 exhibited sigmoidal kinetics characteristic of autoactivation, overview

690847

-

glucuronidation of the non-selective substrate 4-methylumbelliferone by mutant chimeric UGT2B7-15(61194)-7 follows MichaelisMenten and weak substrate inhibition kinetics, respectively, whereas 4-methylumbelliferone glucuronidation by isozyme UGT2B7 exhibited sigmoidal kinetics characteristic of autoactivation, overview

690847

-

imipramine N-glucuronide formation: Vmax (pmol/min/unit): 134.9, 110.4 (1A4 co-expressed with isoform 1A1), 126 (1A4 co-expressed with isoform 1A6). Trifluoperazine N-glucuronide formation: 2.1, 2.0 (1A4 co-expressed with isoform 1A1), 5.1 (1A4 co-expressed with isoform 1A6)

692032

-

P22310

imipramine N-glucuronide formation: Vmax (pmol/min/unit): 134.9, 110.4 (1A4 co-expressed with isoform 1A1), 126 (1A4 co-expressed with isoform 1A6). Trifluoperazine N-glucuronide formation: 2.1, 2.0 (1A4 co-expressed with isoform 1A1), 5.1 (1A4 co-expressed with isoform 1A6)

692032

-

P22310

isozyme UGT1A4 with substrates nicotine and cotinine in liver and intestine microsomes

694256

-

P36537

isozyme UGT1A4 with substrates nicotine and cotinine in liver and intestine microsomes

694256

-

isozyme UGT1A4 with substrates nicotine and cotinine in liver and intestine microsomes

694256

-

P22310

isozyme UGT2B10 with substrates nicotine and cotinine in liver and intestine microsomes

694256

-

P36537

isozyme UGT2B10 with substrates nicotine and cotinine in liver and intestine microsomes

694256

-

isozyme UGT2B10 with substrates nicotine and cotinine in liver and intestine microsomes

694256

-

kinetic analysis of wild-type isozyme UGT1A9 and mutants expressed in HEK293 cells, overview

692047

-

O60656

kinetic analysis of wild-type isozyme UGT1A9 and mutants expressed in HEK293 cells, overview

692047

-

Q9HAW7

kinetic analysis of wild-type isozyme UGT1A9 and mutants expressed in HEK293 cells, overview

692047

-

Q9HAW8

kinetic analysis of wild-type isozyme UGT1A9 and mutants expressed in HEK293 cells, overview

692047

-

Q9HAW9

kinetic analysis of wild-type isozyme UGT1A9 and mutants expressed in HEK293 cells, overview

692047

-

kinetic analysis, isozyme UGT1A1 shows biphasic Michaelis-Menten kinetic behavior with substrate morphine, overview

692045

-

P22309

kinetic analysis, isozyme UGT1A1 shows biphasic Michaelis-Menten kinetic behavior with substrate morphine, overview

692045

-

kinetic analysis, isozyme UGT1A8 shows biphasic Michaelis-Menten kinetic behavior with substrate morphine, overview

692045

-

P22309

kinetic analysis, isozyme UGT1A8 shows biphasic Michaelis-Menten kinetic behavior with substrate morphine, overview

692045

-

kinetic analysis, recombinant isozyme UGT1A4, and liver microsomes, with substrates dexmedetomidine and levomedetomidine, overview

692037

-

P36537

kinetic analysis, recombinant isozyme UGT1A4, and liver microsomes, with substrates dexmedetomidine and levomedetomidine, overview

692037

-

kinetic analysis, recombinant isozyme UGT2B10, and liver microsomes, with substrates dexmedetomidine and levomedetomidine, overview

692037

-

P36537

kinetic analysis, recombinant isozyme UGT2B10, and liver microsomes, with substrates dexmedetomidine and levomedetomidine, overview

692037

-

P16662

kinetic modeling of the interactions between 4-methylumbelliferone, 1-naphthol, and zidovudine glucuronidation by UGT2B7 provides evidence for multiple substrate binding and effector sites, multisite kinetic equilibria models and two-site inhibition model for a substrate exhibiting Michaelis-Menten kinetics, three-site model for heteroactivation, overview

694261

-

P19224

kinetics analysis using ecombinant isozymes UGT1A6 and UGT1A9, and liver and intestine microsomes, overview

692038

-

kinetics analysis using ecombinant isozymes UGT1A6 and UGT1A9, and liver and intestine microsomes, overview

692038

-

P19224

kinetics of wild-type UGT1A6 and mutants, overview

693017

-

P22309

kinetics of wild-type UGT1A6 and mutants, overview

693017

-

P22310

kinetics of wild-type UGT1A6 and mutants, overview

693017

-

P35503

kinetics of wild-type UGT1A6 and mutants, overview

693017

-

kinetics of wild-type UGT1A6 and mutants, overview

693017

-

serotonin O-glucuronide formation: Vmax (nmol/min/unit): 1.5, 2.1 (1A6 co-expressed with isoform 1A1), 6.1 (1A6 co-expressed with isoform 1A4). Diclofenac O-glucuronide formation: 0.0284, 0.088 (1A6 co-expressed with isoform 1A1), 0.0758 (1A6 co-expressed with isoform 1A4)

692032

-

P22310

serotonin O-glucuronide formation: Vmax (nmol/min/unit): 1.5, 2.1 (1A6 co-expressed with isoform 1A1), 6.1 (1A6 co-expressed with isoform 1A4). Diclofenac O-glucuronide formation: 0.0284, 0.088 (1A6 co-expressed with isoform 1A1), 0.0758 (1A6 co-expressed with isoform 1A4)

692032

-

steady-state kinetics, Michaelis-Menten kinetics

735944

-

O60656

Km values of isozymes using different specific substrates at different concentrations with healthy and hepatitis B virus-positive liver microsomes, overview

737080

-

P16662

Km values of isozymes using different specific substrates at different concentrations with healthy and hepatitis B virus-positive liver microsomes, overview

737080

-

P22309

Km values of isozymes using different specific substrates at different concentrations with healthy and hepatitis B virus-positive liver microsomes, overview

737080

-

P22310

Km values of isozymes using different specific substrates at different concentrations with healthy and hepatitis B virus-positive liver microsomes, overview

737080

-

Km values of isozymes using different specific substrates at different concentrations with healthy and hepatitis B virus-positive liver microsomes, overview

737080

-

P22310

Michaelis-Menten and Hill kinetics

736005

-

P35503

Michaelis-Menten and Hill kinetics

736005

-

P36537

Michaelis-Menten and Hill kinetics

736005

-

Michaelis-Menten and Hill kinetics

736005

-

Michaelis-Menten kinetic modeling, overview

736006

-

Q6UWM9

Michaelis-Menten kinetic modeling, overview

736006

-

Q9Y4X1

Michaelis-Menten kinetic modeling, overview

736006

-

O60656

Michaelis-Menten kinetic profile, overview

736680

-

O75795

Michaelis-Menten kinetic profile, overview

736680

-

P06133

Michaelis-Menten kinetic profile, overview

736680

-

P16662

Michaelis-Menten kinetic profile, overview

736680

-

P19224

Michaelis-Menten kinetic profile, overview

736680

-

P22309

Michaelis-Menten kinetic profile, overview

736680

-

P22310

Michaelis-Menten kinetic profile, overview

736680

-

P35503

Michaelis-Menten kinetic profile, overview

736680

-

P54855

Michaelis-Menten kinetic profile, overview

736680

-

Q9HAW7

Michaelis-Menten kinetic profile, overview

736680

-

Q9HAW8

Michaelis-Menten kinetic profile, overview

736680

-

Q9HAW9

Michaelis-Menten kinetic profile, overview

736680

-

Michaelis-Menten kinetic profile, overview

736680

-

P16662

Michaelis-Menten kinetics with substrate 3-epideacetycinobufagin

737232

-

O60656