3.4.14.1: dipeptidyl-peptidase I

This is an abbreviated version!
For detailed information about dipeptidyl-peptidase I, go to the full flat file.

Reaction

Release of an N-terminal dipeptide, Xaa-Yaa-/-Zaa-, except when Xaa is Arg or Lys, or Yaa or Zaa is Pro =

Synonyms

Cat C, CATC, cathepsin C, cathepsin J, CTSC, DAP I, DDPI, dipeptide arylamidase I, dipeptidyl aminopeptidase I, dipeptidyl peptidase I, dipeptidyl peptidase I/cathepsin C, dipeptidyl transferase, DPAP1, DPAP2, DPP I, DPP-I, DPPI, EC 3.4.4.9, hDPPI, PBANKA_146070, PFL2290w

ECTree

     3 Hydrolases

         3.4 Acting on peptide bonds (peptidases)

             3.4.14 Dipeptidyl-peptidases and tripeptidyl-peptidases

                3.4.14.1 dipeptidyl-peptidase I

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Results	in table
13	Activating Compound
958	AA Sequence
9	Application
1	CAS Registry Number
11	Cloned(Commentary)
2	Crystallization (Commentary)
535	Disease/ Diagnostics
2	Expression
10	General Information
1	General Stability
64	IC50 Value
129	Inhibitors
12	kcat/KM [mM/s]
12	Ki Value [mM]
34	KM Value [mM]
21	Localization
18	Metals/Ions
14	Molecular Weight [Da]
21	Natural Substrates/ Products (Substrates)
90	Organism
72	PDB ID
14	pH Optimum
5	pH Range
5	pH Stability
1	pI Value
5	Posttranslational Modification
2	Protein Variants
16	Purification (Commentary)
1	Reaction
4	Reaction Type
90	Reference
100	Source Tissue
6	Specific Activity [micromol/min/mg]
2	Storage Stability
155	Substrates and Products (Substrate)
5	Subunits
65	Synonyms
3	Temperature Optimum [°C]
4	Temperature Stability [°C]
24	Turnover Number [1/s]

IC50 Value

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IC50 Value on EC 3.4.14.1 - dipeptidyl-peptidase I

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IC50 VALUE [mM]

INHIBITOR

ORGANISM

UNIPROT

COMMENTARY

LITERATURE

IMAGE

0.01

(2S)-2-amino-N-[(1S)-2-(biphenyl-4-yl)-1-cyanoethyl]butanamide

Homo sapiens

-

-

707715

0.0000017

(4R)-N-[(1S)-1-cyano-2-phenylethyl]-4-(methylsulfanyl)-4-phenyl-L-prolinamide

Homo sapiens

-

-

707677

0.0000082

(4R)-N-[(1S)-1-cyano-2-phenylethyl]-4-fluoro-4-phenyl-L-prolinamide

Homo sapiens

-

-

707677

0.000495

(4S)-4-chloro-N-[(1S)-1-cyano-2-phenylethyl]-L-prolinamide

Homo sapiens

-

-

707677

0.000336

(4S)-N-(1-cyanocyclopropyl)-4-(methylsulfanyl)-L-prolinamide

Homo sapiens

-

-

707677

0.00088

(4S)-N-(1-cyanocyclopropyl)-4-fluoro-L-prolinamide

Homo sapiens

-

-

707677

0.000192

(4S)-N-[(1R,2S)-2-benzyl-1-cyanocyclopropyl]-4-(methylsulfanyl)-L-prolinamide

Homo sapiens

-

-

707677

0.000523

(4S)-N-[(1R,2S)-2-benzyl-1-cyanocyclopropyl]-4-fluoro-L-prolinamide

Homo sapiens

-

-

707677

0.000271

(4S)-N-[(1S)-1-cyano-2-phenylethyl]-4-(ethylsulfanyl)-L-prolinamide

Homo sapiens

-

-

707677

0.000029

(4S)-N-[(1S)-1-cyano-2-phenylethyl]-4-(methylsulfanyl)-L-prolinamide

Homo sapiens

-

-

707677

0.000133

(4S)-N-[(1S)-1-cyano-2-phenylethyl]-4-fluoro-L-prolinamide

Homo sapiens

-

-

707677

0.001081

(4S)-N-[(1S)-1-cyano-2-phenylethyl]-4-methoxy-L-prolinamide

Homo sapiens

-

-

707677

0.002502

(4S)-N-[(1S)-1-cyano-2-phenylethyl]-4-methyl-L-prolinamide

Homo sapiens

-

-

707677

0.000067

(4S)-N-[(1S,2R)-2-benzyl-1-cyanocyclopropyl]-4-(methylsulfanyl)-L-prolinamide

Homo sapiens

-

-

707677

0.00025

(4S)-N-[(1S,2R)-2-benzyl-1-cyanocyclopropyl]-4-fluoro-L-prolinamide

Homo sapiens

-

-

707677

0.002193

(4S)-N-[(1S,2S)-1-cyano-2-phenylcyclopropyl]-4-fluoro-L-prolinamide

Homo sapiens

-

-

707677

0.000019

1-(2S-2-aminobutanoyl)-4-(2S-N-(2S-3-(2-naphthyl)propan-2-yl-amide)4-phenylbutan-2-yl-amide)semicarbazide

Homo sapiens

-

IC50: 19 nM

664305

0.000022

1-(2S-2-aminobutanoyl)-4-(2S-N-(2S-3-(benzo[b]-thiophen-3-yl)propan-2-yl-amide)4-phenylbutan-2-yl-amide)semicarbazide

Homo sapiens

-

IC50: 22 nM

664305

0.000021

1-(2S-2-aminobutanoyl)-4-(2S-N-(2S-3-(indol-3-yl)propan-2-yl-amide)4-phenylbutan-2-yl-amide)semicarbazide

Homo sapiens

-

IC50: 21 nM

664305

0.000031

1-(2S-2-aminobutanoyl)-4-(2S-N-(2S-3-(m-fluorophenyl)propan-2-yl-amide)4-phenylbutan-2-yl-amide)semicarbazide

Homo sapiens

-

IC50: 31 nM, competitive inhibition, selective for DPP I over other cysteine and serine proteases, noncytotoxic

664305

0.000039

1-(2S-2-aminobutanoyl)-4-(2S-N-(2S-3-(m-methoxyphenyl)propan-2-yl-amide)4-phenylbutan-2-yl-amide)semicarbazide

Homo sapiens

-

IC50: 39 nM

664305

0.000045

1-(2S-2-aminobutanoyl)-4-(2S-N-(2S-3-(p-chlorophenyl)propan-2-yl-amide)4-phenylbutan-2-yl-amide)semicarbazide

Homo sapiens

-

IC50: 45 nM

664305

0.000186

3-[4-(1-amino-1-cyclopentylethyl)-1H-1,2,3-triazol-1-yl]-1-(2,3,5,6-tetrafluorophenoxy)heptan-2-one

Plasmodium falciparum

-

determined after 30 min incubation of parasite lysate with 5 nM to 0.1 mM inhibitor, pH not specified in the publication, 25°C

717480

0.074

3-[4-(1-amino-2-phenylethyl)-1H-1,2,3-triazol-1-yl]-1-(2,3,5,6-tetrafluorophenoxy)heptan-2-one

Plasmodium falciparum

-

determined after 30 min incubation of parasite lysate with 5 nM to 0.1 mM inhibitor, pH not specified in the publication, 25°C

717480

0.00056

3-[4-(1-aminocyclohexyl)-1H-1,2,3-triazol-1-yl]-1-(2,3,5,6-tetrafluorophenoxy)heptan-2-one

Plasmodium falciparum

-

determined after 30 min incubation of parasite lysate with 5 nM to 0.1 mM inhibitor, pH not specified in the publication, 25°C

717480

0.011

3-[4-(1-aminocyclohexyl)-1H-1,2,3-triazol-1-yl]-2-oxoheptyl 2,6-dimethylbenzoate

Plasmodium falciparum

-

determined after 30 min incubation of parasite lysate with 5 nM to 0.1 mM inhibitor, pH not specified in the publication, 25°C

717480

0.0007

3-[4-(1-aminoethyl)-1H-1,2,3-triazol-1-yl]-1-(2,3,5,6-tetrafluorophenoxy)heptan-2-one

Plasmodium falciparum

-

determined after 30 min incubation of parasite lysate with 5 nM to 0.1 mM inhibitor, pH not specified in the publication, 25°C

717480

0.00041

3-[4-(2-aminopentan-2-yl)-1H-1,2,3-triazol-1-yl]-1-(2,3,5,6-tetrafluorophenoxy)heptan-2-one

Plasmodium falciparum

-

determined after 30 min incubation of parasite lysate with 5 nM to 0.1 mM inhibitor, pH not specified in the publication, 25°C

717480

0.0011

3-[4-(2-aminopropan-2-yl)-1H-1,2,3-triazol-1-yl]-1-(2,3,5,6-tetrafluorophenoxy)heptan-2-one

Plasmodium falciparum

-

determined after 30 min incubation of parasite lysate with 5 nM to 0.1 mM inhibitor, pH not specified in the publication, 25°C

717480

0.00042

3-[4-(2-methylpyrrolidin-2-yl)-1H-1,2,3-triazol-1-yl]-1-(2,3,5,6-tetrafluorophenoxy)heptan-2-one

Plasmodium falciparum

-

determined after 30 min incubation of parasite lysate with 5 nM to 0.1 mM inhibitor, pH not specified in the publication, 25°C

717480

0.00041

3-[4-(3-aminopentan-3-yl)-1H-1,2,3-triazol-1-yl]-1-(2,3,5,6-tetrafluorophenoxy)heptan-2-one

Plasmodium falciparum

-

determined after 30 min incubation of parasite lysate with 5 nM to 0.1 mM inhibitor, pH not specified in the publication, 25°C

717480

0.0007

3-[4-(4-aminoheptan-4-yl)-1H-1,2,3-triazol-1-yl]-1-(2,3,5,6-tetrafluorophenoxy)heptan-2-one

Plasmodium falciparum

-

determined after 30 min incubation of parasite lysate with 5 nM to 0.1 mM inhibitor, pH not specified in the publication, 25°C

717480

0.000019

3-[4-[(1R)-1-amino-1-cyclopentylethyl]-1H-1,2,3-triazol-1-yl]-1-(2,3,5,6-tetrafluorophenoxy)heptan-2-one

Plasmodium falciparum

-

determined after 30 min incubation of parasite lysate with 5 nM to 0.1 mM inhibitor, pH not specified in the publication, 25°C

717480

0.0007

3-[4-[(1S)-1-amino-1-cyclohexylethyl]-1H-1,2,3-triazol-1-yl]-1-(2,3,5,6-tetrafluorophenoxy)heptan-2-one

Plasmodium falciparum

-

determined after 30 min incubation of parasite lysate with 5 nM to 0.1 mM inhibitor, pH not specified in the publication, 25°C

717480

0.014

3-[4-[(1S)-1-amino-1-cyclopentylethyl]-1H-1,2,3-triazol-1-yl]-1-(2,3,5,6-tetrafluorophenoxy)heptan-2-one

Plasmodium falciparum

-

determined after 30 min incubation of parasite lysate with 5 nM to 0.1 mM inhibitor, pH not specified in the publication, 25°C

717480

0.0077

3-[4-[4-(methylamino)heptan-4-yl]-1H-1,2,3-triazol-1-yl]-1-(2,3,5,6-tetrafluorophenoxy)heptan-2-one

Plasmodium falciparum

-

determined after 30 min incubation of parasite lysate with 5 nM to 0.1 mM inhibitor, pH not specified in the publication, 25°C

717480

0.000063

N-(1-cyano-2,2-dimethylcyclopropyl)-3-thiophen-2-yl-L-alaninamide

Homo sapiens

-

-

707677

0.00123

N-(1-cyano-2-phenylcyclopropyl)-3-thiophen-2-yl-L-alaninamide

Homo sapiens

-

-

707677

0.001832

N-(1-cyanocyclobutyl)-3-thiophen-2-yl-L-alaninamide

Homo sapiens

-

-

707677

0.000012

N-(1-cyanocyclopropyl)-3-thiophen-2-yl-L-alaninamide

Homo sapiens

-

-

707677

0.001419

N-(2-cyanopropan-2-yl)-3-thiophen-2-yl-L-alaninamide

Homo sapiens

-

-

707677

0.000017

N-(cyanomethyl)-3-thiophen-2-yl-L-alaninamide

Homo sapiens

-

-

707677

0.0001

N-[(1E,3S)-5-phenyl-1-(phenylsulfonyl)pent-1-en-3-yl]-L-norvalinamide

Homo sapiens

-

-

707715

0.000014

N-[(1R,2R)-1-cyano-2-phenylcyclopropyl]-3-thiophen-2-yl-L-alaninamide

Homo sapiens

-

-

707677

0.0000038

N-[(1S)-1-cyano-2,2-diphenylethyl]-3-thiophen-2-yl-L-alaninamide

Homo sapiens

-

-

707677

0.0000058

N-[(1S)-1-cyano-2-(1H-indol-3-yl)ethyl]-3-thiophen-2-yl-L-alaninamide

Homo sapiens

-

-

707677

0.0002

N-[(1S)-1-cyano-2-(1H-indol-3-yl)ethyl]-L-methioninamide

Homo sapiens

-

-

707677

0.00033

N-[(1S)-1-cyano-2-(1H-indol-3-yl)ethyl]-L-valinamide

Homo sapiens

-

-

707677

0.00063

N-[(1S)-1-cyano-2-(1H-indol-3-yl)ethyl]-S-ethyl-L-cysteinamide

Homo sapiens

-

-

707677

0.00158

N-[(1S)-1-cyano-2-(1H-indol-3-yl)ethyl]-S-ethyl-L-homocysteinamide

Homo sapiens

-

-

707677

0.0000003

N-[(1S)-1-cyano-2-(5-phenylthiophen-2-yl)ethyl]-3-thiophen-2-yl-L-alaninamide

Homo sapiens

-

-

707677

0.000001

N-[(1S)-1-cyano-2-(naphthalen-2-yl)ethyl]-3-thiophen-2-yl-L-alaninamide

Homo sapiens

-

-

707677

0.0000051

N-[(1S)-1-cyano-2-cyclohexylethyl]-3-thiophen-2-yl-L-alaninamide

Homo sapiens

-

-

707677

0.000215

N-[(1S)-1-cyano-2-methylpropyl]-3-thiophen-2-yl-L-alaninamide

Homo sapiens

-

-

707677

0.0000009

N-[(1S)-1-cyano-2-phenylethyl]-3-thiophen-2-yl-L-alaninamide

Homo sapiens

-

-

707677

0.004806

N-[(1S)-1-cyano-2-phenylethyl]-L-prolinamide

Homo sapiens

-

-

707677

0.002545

N-[(1S)-1-cyano-2-[4-(methylsulfanyl)phenyl]ethyl]-L-prolinamide

Homo sapiens

-

-

707677

0.000011

N-[(1S)-1-cyano-3-phenylpropyl]-3-thiophen-2-yl-L-alaninamide

Homo sapiens

-

-

707677

0.0000007

N-[(1S)-2-(1,3-benzothiazol-2-yl)-1-cyanoethyl]-3-thiophen-2-yl-L-alaninamide

Homo sapiens

-

-

707677

0.000017

N-[(1S,2S)-1-cyano-2-phenylcyclopropyl]-3-thiophen-2-yl-L-alaninamide

Homo sapiens

-

-

707677

0.011

N-[2-(1H-indol-3-yl)ethyl]-L-methioninamide

Homo sapiens

-

-

707677

0.004

N2-(morpholin-4-ylcarbonyl)-N-[(1E,3S)-5-phenyl-1-(phenylsulfonyl)pent-1-en-3-yl]-L-leucinamide

Homo sapiens

-

-

707715

additional information

N-[(1S)-1-cyano-2,2-dimethylpropyl]-3-thiophen-2-yl-L-alaninamide

2 entries

additional information

N-[(1S)-1-cyano-2,2-dimethylpropyl]-3-thiophen-2-yl-L-alaninamide

Homo sapiens

-

value above 0.003 mM

707677

additional information

N-[(1S)-1-cyano-2-(4-fluorophenyl)ethyl]-L-prolinamide

Homo sapiens

-

value above 0.01 mM

707677