Literature summary for 2.3.2.13 extracted from

Prime, M.E.; Andersen, O.A.; Barker, J.J.; Brooks, M.A.; Cheng, R.K.; Toogood-Johnson, I.; Courtney, S.M.; Brookfield, F.A.; Yarnold, C.J.; Marston, R.W.; Johnson, P.D.; Johnsen, S.F.; Palfrey, J.J.; Vaidya, D.; Erfan, S.; Ichihara, O.; Felicetti, B.; Palan, S.; Pedret-Dunn, A.; Schaertl, S.; Sternberger, I.
Discovery and structure-activity relationship of potent and selective covalent inhibitors of transglutaminase 2 for Huntingtons disease (2012), J. Med. Chem., 55, 1021-1046.

Cloned(Commentary)

Cloned (Comment)	Organism
expressed in Escherichia coli Rosetta 2 (DE3) cells	Homo sapiens

Inhibitors

Inhibitors	Comment	Organism
(5-bromothiophen-2-yl)(4-methyl-1H-pyrazol-1-yl)methanone	-	Homo sapiens
1-acetyl-L-prolyl-6-imino-5-oxo-L-norleucyl-L-leucyl-L-prolyl-L-phenylalaninamide	-	Homo sapiens
1-ethyl-3-(4-methoxyphenyl)-6-methylpyrimido[5,4-e][1,2,4]triazine-5,7(1H,6H)-dione	-	Homo sapiens
3-(4-acryloylaminobenzenesulfonylamino)-(R)-pyrrolidine-1-carboxylic acid benzyl ester	-	Homo sapiens
3-(4-acryloylaminobenzenesulfonylamino)-(S)-pyrrolidine-1-carboxylic acid benzyl ester	-	Homo sapiens
3-[benzyl(tert-butyl)amino]-1-(5-bromothiophen-2-yl)propan-1-one	-	Homo sapiens
4-(2-acryloylaminopyrimidine-5-sulfonyl)piperazine-1-carboxylic acid benzyl ester	-	Homo sapiens
4-(2-acryloylaminopyrimidine-5-sulfonyl)piperazine-1-carboxylic acid tert-butyl ester	-	Homo sapiens
4-(3-acryloylaminobenzenesulfonyl)piperazine-1-carboxylicacid benzyl ester	-	Homo sapiens
4-(4-acryloylamino-2-chlorobenzenesulfonyl)piperazine-1-carboxylic acid tert-butyl ester	-	Homo sapiens
4-(4-acryloylamino-2-fluorobenzenesulfonyl)piperazine-1-carboxylic acid tert-butyl ester	-	Homo sapiens
4-(4-acryloylamino-2-methoxybenzenesulfonyl)piperazine-1-carboxylic acid tert-butyl ester	-	Homo sapiens
4-(4-acryloylamino-2-methylbenzenesulfonyl)piperazine-1-carboxylic acid tert-butyl ester	-	Homo sapiens
4-(4-acryloylamino-2-trifluoromethylbenzenesulfonyl)-piperazine-1-carboxylic acid benzyl ester	-	Homo sapiens
4-(4-acryloylamino-3-fluorobenzenesulfonyl)piperazine-1-carboxylic acid benzyl ester	-	Homo sapiens
4-(4-acryloylaminobenzenesulfonyl)piperazine-1-carboxylic acid 2-chlorobenzyl ester	-	Homo sapiens
4-(4-acryloylaminobenzenesulfonyl)piperazine-1-carboxylic acid 2-methylbenzyl ester	-	Homo sapiens
4-(4-acryloylaminobenzenesulfonyl)piperazine-1-carboxylic acid 2-trifluoromethylbenzyl ester	-	Homo sapiens
4-(4-acryloylaminobenzenesulfonyl)piperazine-1-carboxylic acid 3,5-difluorobenzyl ester	-	Homo sapiens
4-(4-acryloylaminobenzenesulfonyl)piperazine-1-carboxylic acid benzyl ester	-	Homo sapiens
4-(4-acryloylaminobenzenesulfonyl)piperazine-1-carboxylic acid cyclopentyl ester	-	Homo sapiens
4-(4-acryloylaminobenzenesulfonyl)piperazine-1-carboxylic acid methyl ester	-	Homo sapiens
4-(4-acryloylaminobenzenesulfonyl)piperazine-1-carboxylic acid naphthalen-1-ylmethyl ester	-	Homo sapiens
4-(4-acryloylaminobenzenesulfonyl)piperazine-1-carboxylic acid naphthalen-2-ylmethyl ester	-	Homo sapiens
4-(4-acryloylaminobenzenesulfonyl)piperazine-1-carboxylic acid tert-butyl ester	-	Homo sapiens
4-(4-acryloylaminobenzenesulfonyl)piperazine-1-carboxylicacid 2,3-difluorobenzyl ester	-	Homo sapiens
4-(4-acryloylaminobenzenesulfonyl)piperazine-1-carboxylicacid 4-fluorobenzyl ester	-	Homo sapiens
4-(4-acryloylaminobenzenesulfonyl)piperazine-1-carboxylicacid ethyl ester	-	Homo sapiens
4-(4-acryloylaminobenzenesulfonyl)[1,4]diazepane-1-carboxylicacid benzyl ester	-	Homo sapiens
4-(4-acryloylaminobenzenesulfonylamino)piperidine-1-carboxylic acid benzyl ester	-	Homo sapiens
4-(4-but-2-enoylaminobenzenesulfonyl)piperazine-1-carboxylic acid tert-butyl ester	-	Homo sapiens
4-(4-cyanobenzenesulfonyl)piperazine-1-carboxylic acid tert-butyl ester	-	Homo sapiens
4-(6-acryloylaminopyridine-3-sulfonyl)piperazine-1-carboxylic acid benzyl ester	-	Homo sapiens
4-(6-acryloylaminopyridine-3-sulfonyl)piperazine-1-carboxylic acid tert-butyl ester	-	Homo sapiens
4-[(4-acryloylaminobenzenesulfonylamino)methyl]-piperidine-1-carboxylic acid benzyl ester	-	Homo sapiens
4-[4-(1-oxobut-2-ynylamino)benzenesulfonyl]piperazine-1-carboxylic acid tert-butyl ester	-	Homo sapiens
4-[4-(2-cyanoacetylamino)benzenesulfonyl]piperazine-1-carboxylic acid tert-butyl ester	-	Homo sapiens
4-[4-(2-ethoxycarbonylvinyl)benzenesulfonyl]piperazine-1-carboxylic acid benzyl ester	-	Homo sapiens
4-[4-(2-fluoroacryloylamino)benzenesulfonyl]piperazine-1-carboxylic acid tert-butyl ester	-	Homo sapiens
4-[4-(2-methylacryloylamino)benzenesulfonyl]piperazine-1-carboxylic acid tert-butyl ester	-	Homo sapiens
4-[4-(2-methylbut-2-enoylamino)benzenesulfonyl]-piperazine-1-carboxylic acid tert-butyl ester	-	Homo sapiens
4-[4-(2-oxopropionylamino)benzenesulfonyl]piperazine-1-carboxylic acid tert-butyl ester	-	Homo sapiens
4-[4-(3-(E)-chloroacryloylamino)benzenesulfonyl]-piperazine-1-carboxylic acid tert-butyl ester	-	Homo sapiens
4-[4-(3-(Z)-chloroacryloylamino)benzenesulfonyl]-piperazine-1-carboxylic acid tert-butyl ester	-	Homo sapiens
4-[4-(3-cyanomethylureido)benzenesulfonyl]piperazine-1-carboxylic acid tert-butyl ester	-	Homo sapiens
4-[4-(3-diazo-2-oxopropyl)benzenesulfonyl]piperazine-1-carboxylic acid benzyl ester	-	Homo sapiens
4-[4-(3-ethoxycarbonylallyl)benzenesulfonyl]piperazine-1-carboxylic acid benzyl ester	-	Homo sapiens
4-[4-(4,4,4-trifluoro-3-methylbut-2-enoylamino)-benzenesulfonyl]piperazine-1-carboxylic acid tert-butyl ester	-	Homo sapiens
4-[4-(4,4,4-trifluorobut-2-enoylamino)benzenesulfonyl]-piperazine-1-carboxylic acid tert-butyl ester	-	Homo sapiens
4-[4-(4-diazo-3-oxobutyl)benzenesulfonyl]piperazine-1-carboxylic acid benzyl ester	-	Homo sapiens
4-[4-(acryloylmethyl-amino)benzenesulfonyl]piperazine-1-carboxylic acid tert-butyl ester	-	Homo sapiens
4-[4-(cyanomethylcarbamoyl)benzenesulfonyl]piperazine-1-carboxylic acid tert-butyl ester	-	Homo sapiens
4-[4-(ethoxycarbonylmethylamino)benzenesulfonyl]-piperazine-1-carboxylic acid tert-butyl ester	-	Homo sapiens
4-[4-acryloylamino-3-(isobutylmethylamino)-benzenesulfonyl]piperazine-1-carboxylic acid benzyl ester	-	Homo sapiens
5-(4-acryloylaminobenzenesulfonyl)-2,5-diazabicyclo-[2.2.1]heptane-2-carboxylic acid tert-butyl ester	-	Homo sapiens
5-(4-acryloylaminobenzenesulfonyl)hexahydropyrrolo[3,4-c]pyrrole-2-carboxylic acid benzyl ester	-	Homo sapiens
ethenesulfonic acid (4-bromophenyl)amide	-	Homo sapiens
LDN-27219	-	Homo sapiens
N-(2-bromophenyl)acrylamide	-	Homo sapiens
N-(3-bromophenyl)acrylamide	-	Homo sapiens
N-(4-bromobenzyl)acrylamide	-	Homo sapiens
N-(4-bromophenyl)acrylamide	-	Homo sapiens
N-(4-bromophenyl)propionamide	-	Homo sapiens
N-(4-fluorophenyl)acrylamide	-	Homo sapiens
N-(4-[4-[2-(2-phenoxyphenyl)acetyl]piperazine-1-sulfonyl]-phenyl)acrylamide	-	Homo sapiens
N-(4-[4-[2-(3-phenoxyphenyl)acetyl]piperazine-1-sulfonyl]-phenyl)acrylamide	-	Homo sapiens
N-(4-[4-[2-(4-phenoxyphenyl)acetyl]piperazine-1-sulfonyl]- phenyl)acrylamide	-	Homo sapiens
N-(4-[4-[2-(4-phenoxyphenyl)acetyl]piperazine-1-sulfonyl]-phenyl)acrylamide	-	Homo sapiens
N-phenylacrylamide	-	Homo sapiens
N-[4-(4-cyclopentanecarbonylpiperazine-1-sulfonyl)-phenyl]acrylamide	-	Homo sapiens
N-[4-(4-cyclopropanecarbonylpiperazine-1-sulfonyl)-phenyl]acrylamide	-	Homo sapiens
N-[4-(4-phenylpiperazine-1-sulfonyl)phenyl]acrylamide	-	Homo sapiens
N-[4-(4-pyridin-2-ylpiperazine-1-sulfonyl)phenyl]acrylamide	-	Homo sapiens
N-[4-(aminomethyl)benzyl]-3-(5-[[[[(E)-2-phenylethenyl]sulfonyl](pyridin-2-ylmethyl)amino]methyl]-1,2,4-oxadiazol-3-yl)benzamide	-	Homo sapiens
N-[4-(piperazine-1-sulfonyl)phenyl]acrylamide	-	Homo sapiens
N-[4-(pyrrolidine-1-sulfonyl)phenyl]acrylamide	-	Homo sapiens
N-[4-methanesulfonylphenyl]acrylamide	-	Homo sapiens
N-[4-methoxyphenyl]acrylamide	-	Homo sapiens
N-[4-nitrophenyl]acrylamide	-	Homo sapiens
N-[4-phenoxyphenyl]acrylamide	-	Homo sapiens
N-[4-toluyl]acrylamide	-	Homo sapiens
N-[4-trifluoromethylphenyl]acrylamide	-	Homo sapiens
N-[4-[4-(2-phenylcyclopropanecarbonyl)piperazine-1-sulfonyl]phenyl]acrylamide	-	Homo sapiens
N-[4-[4-(2-trifluoromethylphenyl)piperazine-1-sulfonyl]-phenyl]acrylamide	-	Homo sapiens
N-[4-[4-(3-methylpyridin-2-yl)piperazine-1-sulfonyl]phenyl]-acrylamide	-	Homo sapiens
N-[4-[4-(3-phenylpropionyl)piperazine-1-sulfonyl]phenyl]-acrylamide	-	Homo sapiens
N-[4-[4-(3-phenylpropyl)piperazine-1-sulfonyl]phenyl]-acrylamide	-	Homo sapiens
N-[4-[4-(3-trifluoromethylpyridin-2-yl)piperazine-1-sulfonyl]phenyl]acrylamide	-	Homo sapiens
N-[4-[4-(4,4-difluoropiperidine-1-carbonyl)piperazine-1-sulfonyl]phenyl]acrylamide	-	Homo sapiens
N-[4-[4-(4-phenylbutyl)piperazine-1-sulfonyl]phenyl]-acrylamide	-	Homo sapiens
N-[4-[4-(6-methylpyridin-2-yl)piperazine-1-sulfonyl]phenyl]-acrylamide	-	Homo sapiens
N-[4-[4-(6-trifluoromethylpyridin-3-yl)piperazine-1-sulfonyl]phenyl]acrylamide	-	Homo sapiens
N-[4-[4-(adamantane-1-carbonyl)piperazine-1-sulfonyl]-phenyl]acrylamide	-	Homo sapiens
N-[4-[4-(octahydroisoquinoline-2-carbonyl)piperazine-1-sulfonyl]phenyl]acrylamide	-	Homo sapiens
N-[4-[4-(octahydroquinoline-1-carbonyl)piperazine-1-sulfonyl]phenyl]acrylamide	-	Homo sapiens
N-[4-[4-(piperidine-1-carbonyl)piperazine-1-sulfonyl]-phenyl]acrylamide	-	Homo sapiens
N-[4-[4-(pyrrolidine-1-carbonyl)piperazine-1-sulfonyl]-phenyl]acrylamide	-	Homo sapiens
N-[5-(4-cyclopropanecarbonylpiperazine-1-sulfonyl)-pyridin-2-yl]acrylamide	-	Homo sapiens
N-[5-[4-(adamantane-1-carbonyl)piperazine-1-sulfonyl]-pyridin-2-yl]acrylamide	-	Homo sapiens
N-[5-[4-(adamantane-1-carbonyl)piperazine-1-sulfonyl]-pyrimidin-2-yl]acrylamide	-	Homo sapiens
N-{[(5S)-3-bromo-4,5-dihydro-1,2-oxazol-5-yl]methyl}-5-fluoro-Nalpha-[(quinolin-3-ylmethoxy)carbonyl]-L-tryptophanamide	-	Homo sapiens
pyrrolidine-1-carboxylic acid (4-acryloylaminophenyl)-amide	-	Homo sapiens
tert-butyl N6-acryloyl-N2-[(benzyloxy)carbonyl]-L-lysylglycinate	-	Homo sapiens
[(5R,8S)-8-{[(benzyloxy)carbonyl]amino}-5-(methoxycarbonyl)-2,7-dioxo-9-phenylnonyl](dimethyl)sulfonium bromide	-	Homo sapiens
[1-(4-acryloylaminobenzenesulfonyl)piperidin-4-ylmethyl]-carbamic acid benzyl ester	-	Homo sapiens
[1-(4-acryloylaminobenzenesulfonyl)piperidin-4-yl]-carbamic acid benzyl ester	-	Homo sapiens
[2-[(4-acryloylaminobenzenesulfonyl)methylamino]ethyl]-methylcarbamic acid benzyl ester	-	Homo sapiens
[4-(4-acryloylpiperazine-1-sulfonyl)phenyl]carbamic acid benzyl ester	-	Homo sapiens
[4-[(4-aminophenyl)sulfonyl]piperazin-1-yl](cyclopropyl)methanone	-	Homo sapiens

Metals/Ions

Metals/Ions	Comment	Organism	Structure
Ca2+	dependent on	Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates	Organism	Comment (Nat. Sub.)	Natural Products	Comment (Nat. Pro.)	Rev.	Reac.
N,N-dimethylated casein-bound gamma-glutamine + dansyl-labeled amine nucleophile	Homo sapiens	-	?	-	?

Organism

Organism	UniProt	Comment	Textmining
Homo sapiens	P21980	-	-

Purification (Commentary)

Purification (Comment)	Organism
TALON resin column chromatography and Superdex 200 gel filtration	Homo sapiens

Substrates and Products (Substrate)

Substrates	Comment Substrates	Organism	Products	Comment (Products)	Rev.	Reac.
N,N-dimethylated casein-bound gamma-glutamine + dansyl-labeled amine nucleophile	-	Homo sapiens	?	-	?

Synonyms

Synonyms	Comment	Organism
TG2	-	Homo sapiens
TGM2	-	Homo sapiens
tissue transglutaminase 2	-	Homo sapiens
transglutaminase 2	-	Homo sapiens

IC50 Value

IC50 Value	IC50 Value Maximum	Comment	Organism	Inhibitor
0.00001	-	in 25 mM HEPES, pH 7.4, 250 mM NaCl, 2 mM MgCl2, 10 mM CaCl2, 0.2 mM dithiothreitol, and 0.05% (v/v) Pluronic F-127 at 37°C	Homo sapiens	N-[4-[4-(adamantane-1-carbonyl)piperazine-1-sulfonyl]-phenyl]acrylamide
0.000014	-	in 25 mM HEPES, pH 7.4, 250 mM NaCl, 2 mM MgCl2, 10 mM CaCl2, 0.2 mM dithiothreitol, and 0.05% (v/v) Pluronic F-127 at 37°C	Homo sapiens	N-[5-[4-(adamantane-1-carbonyl)piperazine-1-sulfonyl]-pyrimidin-2-yl]acrylamide
0.000015	-	in 25 mM HEPES, pH 7.4, 250 mM NaCl, 2 mM MgCl2, 10 mM CaCl2, 0.2 mM dithiothreitol, and 0.05% (v/v) Pluronic F-127 at 37°C	Homo sapiens	N-[5-[4-(adamantane-1-carbonyl)piperazine-1-sulfonyl]-pyridin-2-yl]acrylamide
0.00002	-	in 25 mM HEPES, pH 7.4, 250 mM NaCl, 2 mM MgCl2, 10 mM CaCl2, 0.2 mM dithiothreitol, and 0.05% (v/v) Pluronic F-127 at 37°C	Homo sapiens	N-[4-[4-(octahydroisoquinoline-2-carbonyl)piperazine-1-sulfonyl]phenyl]acrylamide
0.000025	-	in 25 mM HEPES, pH 7.4, 250 mM NaCl, 2 mM MgCl2, 10 mM CaCl2, 0.2 mM dithiothreitol, and 0.05% (v/v) Pluronic F-127 at 37°C	Homo sapiens	N-[4-[4-(3-methylpyridin-2-yl)piperazine-1-sulfonyl]phenyl]-acrylamide
0.000025	-	in 25 mM HEPES, pH 7.4, 250 mM NaCl, 2 mM MgCl2, 10 mM CaCl2, 0.2 mM dithiothreitol, and 0.05% (v/v) Pluronic F-127 at 37°C	Homo sapiens	1-ethyl-3-(4-methoxyphenyl)-6-methylpyrimido[5,4-e][1,2,4]triazine-5,7(1H,6H)-dione
0.000026	-	in 25 mM HEPES, pH 7.4, 250 mM NaCl, 2 mM MgCl2, 10 mM CaCl2, 0.2 mM dithiothreitol, and 0.05% (v/v) Pluronic F-127 at 37°C	Homo sapiens	N-[4-[4-(octahydroquinoline-1-carbonyl)piperazine-1-sulfonyl]phenyl]acrylamide
0.000026	-	in 25 mM HEPES, pH 7.4, 250 mM NaCl, 2 mM MgCl2, 10 mM CaCl2, 0.2 mM dithiothreitol, and 0.05% (v/v) Pluronic F-127 at 37°C	Homo sapiens	4-(2-acryloylaminopyrimidine-5-sulfonyl)piperazine-1-carboxylic acid tert-butyl ester
0.000032	-	in 25 mM HEPES, pH 7.4, 250 mM NaCl, 2 mM MgCl2, 10 mM CaCl2, 0.2 mM dithiothreitol, and 0.05% (v/v) Pluronic F-127 at 37°C	Homo sapiens	N-[4-(4-cyclopentanecarbonylpiperazine-1-sulfonyl)-phenyl]acrylamide
0.000034	-	in 25 mM HEPES, pH 7.4, 250 mM NaCl, 2 mM MgCl2, 10 mM CaCl2, 0.2 mM dithiothreitol, and 0.05% (v/v) Pluronic F-127 at 37°C	Homo sapiens	N-[4-[4-(2-phenylcyclopropanecarbonyl)piperazine-1-sulfonyl]phenyl]acrylamide
0.000035	-	in 25 mM HEPES, pH 7.4, 250 mM NaCl, 2 mM MgCl2, 10 mM CaCl2, 0.2 mM dithiothreitol, and 0.05% (v/v) Pluronic F-127 at 37°C	Homo sapiens	N-[4-[4-(6-methylpyridin-2-yl)piperazine-1-sulfonyl]phenyl]-acrylamide
0.000037	-	in 25 mM HEPES, pH 7.4, 250 mM NaCl, 2 mM MgCl2, 10 mM CaCl2, 0.2 mM dithiothreitol, and 0.05% (v/v) Pluronic F-127 at 37°C	Homo sapiens	N-[4-[4-(piperidine-1-carbonyl)piperazine-1-sulfonyl]-phenyl]acrylamide
0.000041	-	in 25 mM HEPES, pH 7.4, 250 mM NaCl, 2 mM MgCl2, 10 mM CaCl2, 0.2 mM dithiothreitol, and 0.05% (v/v) Pluronic F-127 at 37°C	Homo sapiens	N-[4-[4-(4,4-difluoropiperidine-1-carbonyl)piperazine-1-sulfonyl]phenyl]acrylamide
0.000044	-	in 25 mM HEPES, pH 7.4, 250 mM NaCl, 2 mM MgCl2, 10 mM CaCl2, 0.2 mM dithiothreitol, and 0.05% (v/v) Pluronic F-127 at 37°C	Homo sapiens	4-(4-acryloylaminobenzenesulfonyl)piperazine-1-carboxylic acid cyclopentyl ester
0.000046	-	in 25 mM HEPES, pH 7.4, 250 mM NaCl, 2 mM MgCl2, 10 mM CaCl2, 0.2 mM dithiothreitol, and 0.05% (v/v) Pluronic F-127 at 37°C	Homo sapiens	4-(4-acryloylaminobenzenesulfonyl)piperazine-1-carboxylicacid 2,3-difluorobenzyl ester
0.000052	-	in 25 mM HEPES, pH 7.4, 250 mM NaCl, 2 mM MgCl2, 10 mM CaCl2, 0.2 mM dithiothreitol, and 0.05% (v/v) Pluronic F-127 at 37°C	Homo sapiens	N-[4-[4-(3-trifluoromethylpyridin-2-yl)piperazine-1-sulfonyl]phenyl]acrylamide
0.000054	-	in 25 mM HEPES, pH 7.4, 250 mM NaCl, 2 mM MgCl2, 10 mM CaCl2, 0.2 mM dithiothreitol, and 0.05% (v/v) Pluronic F-127 at 37°C	Homo sapiens	4-(4-acryloylaminobenzenesulfonyl)piperazine-1-carboxylicacid 4-fluorobenzyl ester
0.000054	-	in 25 mM HEPES, pH 7.4, 250 mM NaCl, 2 mM MgCl2, 10 mM CaCl2, 0.2 mM dithiothreitol, and 0.05% (v/v) Pluronic F-127 at 37°C	Homo sapiens	N-(4-[4-[2-(3-phenoxyphenyl)acetyl]piperazine-1-sulfonyl]-phenyl)acrylamide
0.000055	-	in 25 mM HEPES, pH 7.4, 250 mM NaCl, 2 mM MgCl2, 10 mM CaCl2, 0.2 mM dithiothreitol, and 0.05% (v/v) Pluronic F-127 at 37°C	Homo sapiens	N-[4-(4-pyridin-2-ylpiperazine-1-sulfonyl)phenyl]acrylamide
0.000057	-	in 25 mM HEPES, pH 7.4, 250 mM NaCl, 2 mM MgCl2, 10 mM CaCl2, 0.2 mM dithiothreitol, and 0.05% (v/v) Pluronic F-127 at 37°C	Homo sapiens	N-[4-[4-(pyrrolidine-1-carbonyl)piperazine-1-sulfonyl]-phenyl]acrylamide
0.00006	-	in 25 mM HEPES, pH 7.4, 250 mM NaCl, 2 mM MgCl2, 10 mM CaCl2, 0.2 mM dithiothreitol, and 0.05% (v/v) Pluronic F-127 at 37°C	Homo sapiens	N-(4-[4-[2-(4-phenoxyphenyl)acetyl]piperazine-1-sulfonyl]-phenyl)acrylamide
0.000069	-	in 25 mM HEPES, pH 7.4, 250 mM NaCl, 2 mM MgCl2, 10 mM CaCl2, 0.2 mM dithiothreitol, and 0.05% (v/v) Pluronic F-127 at 37°C	Homo sapiens	4-(2-acryloylaminopyrimidine-5-sulfonyl)piperazine-1-carboxylic acid benzyl ester
0.00007	-	in 25 mM HEPES, pH 7.4, 250 mM NaCl, 2 mM MgCl2, 10 mM CaCl2, 0.2 mM dithiothreitol, and 0.05% (v/v) Pluronic F-127 at 37°C	Homo sapiens	4-(4-acryloylaminobenzenesulfonyl)piperazine-1-carboxylic acid 3,5-difluorobenzyl ester
0.00007	-	in 25 mM HEPES, pH 7.4, 250 mM NaCl, 2 mM MgCl2, 10 mM CaCl2, 0.2 mM dithiothreitol, and 0.05% (v/v) Pluronic F-127 at 37°C	Homo sapiens	4-(4-acryloylaminobenzenesulfonyl)piperazine-1-carboxylic acid 2-methylbenzyl ester
0.000072	-	in 25 mM HEPES, pH 7.4, 250 mM NaCl, 2 mM MgCl2, 10 mM CaCl2, 0.2 mM dithiothreitol, and 0.05% (v/v) Pluronic F-127 at 37°C	Homo sapiens	4-(4-acryloylaminobenzenesulfonyl)piperazine-1-carboxylicacid ethyl ester
0.000076	-	in 25 mM HEPES, pH 7.4, 250 mM NaCl, 2 mM MgCl2, 10 mM CaCl2, 0.2 mM dithiothreitol, and 0.05% (v/v) Pluronic F-127 at 37°C	Homo sapiens	N-[4-[4-(6-trifluoromethylpyridin-3-yl)piperazine-1-sulfonyl]phenyl]acrylamide
0.000078	-	in 25 mM HEPES, pH 7.4, 250 mM NaCl, 2 mM MgCl2, 10 mM CaCl2, 0.2 mM dithiothreitol, and 0.05% (v/v) Pluronic F-127 at 37°C	Homo sapiens	4-(6-acryloylaminopyridine-3-sulfonyl)piperazine-1-carboxylic acid benzyl ester
0.0000821	-	in 25 mM HEPES, pH 7.4, 250 mM NaCl, 2 mM MgCl2, 10 mM CaCl2, 0.2 mM dithiothreitol, and 0.05% (v/v) Pluronic F-127 at 37°C	Homo sapiens	4-(4-acryloylaminobenzenesulfonyl)piperazine-1-carboxylic acid naphthalen-1-ylmethyl ester
0.000094	-	in 25 mM HEPES, pH 7.4, 250 mM NaCl, 2 mM MgCl2, 10 mM CaCl2, 0.2 mM dithiothreitol, and 0.05% (v/v) Pluronic F-127 at 37°C	Homo sapiens	4-(4-acryloylaminobenzenesulfonyl)piperazine-1-carboxylic acid 2-chlorobenzyl ester
0.000096	-	in 25 mM HEPES, pH 7.4, 250 mM NaCl, 2 mM MgCl2, 10 mM CaCl2, 0.2 mM dithiothreitol, and 0.05% (v/v) Pluronic F-127 at 37°C	Homo sapiens	3-(4-acryloylaminobenzenesulfonylamino)-(S)-pyrrolidine-1-carboxylic acid benzyl ester
0.000097	-	in 25 mM HEPES, pH 7.4, 250 mM NaCl, 2 mM MgCl2, 10 mM CaCl2, 0.2 mM dithiothreitol, and 0.05% (v/v) Pluronic F-127 at 37°C	Homo sapiens	4-(6-acryloylaminopyridine-3-sulfonyl)piperazine-1-carboxylic acid tert-butyl ester
0.00011	-	in 25 mM HEPES, pH 7.4, 250 mM NaCl, 2 mM MgCl2, 10 mM CaCl2, 0.2 mM dithiothreitol, and 0.05% (v/v) Pluronic F-127 at 37°C	Homo sapiens	4-(4-acryloylaminobenzenesulfonyl)piperazine-1-carboxylic acid 2-trifluoromethylbenzyl ester
0.00011	-	in 25 mM HEPES, pH 7.4, 250 mM NaCl, 2 mM MgCl2, 10 mM CaCl2, 0.2 mM dithiothreitol, and 0.05% (v/v) Pluronic F-127 at 37°C	Homo sapiens	4-(4-acryloylaminobenzenesulfonyl)piperazine-1-carboxylic acid methyl ester
0.00011	-	in 25 mM HEPES, pH 7.4, 250 mM NaCl, 2 mM MgCl2, 10 mM CaCl2, 0.2 mM dithiothreitol, and 0.05% (v/v) Pluronic F-127 at 37°C	Homo sapiens	N-[4-(4-cyclopropanecarbonylpiperazine-1-sulfonyl)-phenyl]acrylamide
0.00011	-	in 25 mM HEPES, pH 7.4, 250 mM NaCl, 2 mM MgCl2, 10 mM CaCl2, 0.2 mM dithiothreitol, and 0.05% (v/v) Pluronic F-127 at 37°C	Homo sapiens	4-(4-acryloylamino-2-chlorobenzenesulfonyl)piperazine-1-carboxylic acid tert-butyl ester
0.00012	-	in 25 mM HEPES, pH 7.4, 250 mM NaCl, 2 mM MgCl2, 10 mM CaCl2, 0.2 mM dithiothreitol, and 0.05% (v/v) Pluronic F-127 at 37°C	Homo sapiens	4-(4-acryloylaminobenzenesulfonyl)piperazine-1-carboxylic acid benzyl ester
0.00013	-	in 25 mM HEPES, pH 7.4, 250 mM NaCl, 2 mM MgCl2, 10 mM CaCl2, 0.2 mM dithiothreitol, and 0.05% (v/v) Pluronic F-127 at 37°C	Homo sapiens	N-(4-[4-[2-(2-phenoxyphenyl)acetyl]piperazine-1-sulfonyl]-phenyl)acrylamide
0.00014	-	in 25 mM HEPES, pH 7.4, 250 mM NaCl, 2 mM MgCl2, 10 mM CaCl2, 0.2 mM dithiothreitol, and 0.05% (v/v) Pluronic F-127 at 37°C	Homo sapiens	5-(4-acryloylaminobenzenesulfonyl)hexahydropyrrolo[3,4-c]pyrrole-2-carboxylic acid benzyl ester
0.00014	-	in 25 mM HEPES, pH 7.4, 250 mM NaCl, 2 mM MgCl2, 10 mM CaCl2, 0.2 mM dithiothreitol, and 0.05% (v/v) Pluronic F-127 at 37°C	Homo sapiens	4-[4-(3-(Z)-chloroacryloylamino)benzenesulfonyl]-piperazine-1-carboxylic acid tert-butyl ester
0.00016	-	in 25 mM HEPES, pH 7.4, 250 mM NaCl, 2 mM MgCl2, 10 mM CaCl2, 0.2 mM dithiothreitol, and 0.05% (v/v) Pluronic F-127 at 37°C	Homo sapiens	N-[4-[4-(3-phenylpropionyl)piperazine-1-sulfonyl]phenyl]-acrylamide
0.00018	-	in 25 mM HEPES, pH 7.4, 250 mM NaCl, 2 mM MgCl2, 10 mM CaCl2, 0.2 mM dithiothreitol, and 0.05% (v/v) Pluronic F-127 at 37°C	Homo sapiens	N-[4-(4-phenylpiperazine-1-sulfonyl)phenyl]acrylamide
0.00018	-	in 25 mM HEPES, pH 7.4, 250 mM NaCl, 2 mM MgCl2, 10 mM CaCl2, 0.2 mM dithiothreitol, and 0.05% (v/v) Pluronic F-127 at 37°C	Homo sapiens	N-[5-(4-cyclopropanecarbonylpiperazine-1-sulfonyl)-pyridin-2-yl]acrylamide
0.00018	-	in 25 mM HEPES, pH 7.4, 250 mM NaCl, 2 mM MgCl2, 10 mM CaCl2, 0.2 mM dithiothreitol, and 0.05% (v/v) Pluronic F-127 at 37°C	Homo sapiens	4-(4-acryloylamino-2-trifluoromethylbenzenesulfonyl)-piperazine-1-carboxylic acid benzyl ester
0.00019	-	in 25 mM HEPES, pH 7.4, 250 mM NaCl, 2 mM MgCl2, 10 mM CaCl2, 0.2 mM dithiothreitol, and 0.05% (v/v) Pluronic F-127 at 37°C	Homo sapiens	N-[4-[4-(2-trifluoromethylphenyl)piperazine-1-sulfonyl]-phenyl]acrylamide
0.00019	-	in 25 mM HEPES, pH 7.4, 250 mM NaCl, 2 mM MgCl2, 10 mM CaCl2, 0.2 mM dithiothreitol, and 0.05% (v/v) Pluronic F-127 at 37°C	Homo sapiens	4-(4-acryloylamino-2-fluorobenzenesulfonyl)piperazine-1-carboxylic acid tert-butyl ester
0.00021	-	in 25 mM HEPES, pH 7.4, 250 mM NaCl, 2 mM MgCl2, 10 mM CaCl2, 0.2 mM dithiothreitol, and 0.05% (v/v) Pluronic F-127 at 37°C	Homo sapiens	[1-(4-acryloylaminobenzenesulfonyl)piperidin-4-ylmethyl]-carbamic acid benzyl ester
0.00022	-	in 25 mM HEPES, pH 7.4, 250 mM NaCl, 2 mM MgCl2, 10 mM CaCl2, 0.2 mM dithiothreitol, and 0.05% (v/v) Pluronic F-127 at 37°C	Homo sapiens	[1-(4-acryloylaminobenzenesulfonyl)piperidin-4-yl]-carbamic acid benzyl ester
0.00022	-	in 25 mM HEPES, pH 7.4, 250 mM NaCl, 2 mM MgCl2, 10 mM CaCl2, 0.2 mM dithiothreitol, and 0.05% (v/v) Pluronic F-127 at 37°C	Homo sapiens	4-(4-acryloylaminobenzenesulfonyl)piperazine-1-carboxylic acid naphthalen-2-ylmethyl ester
0.0003	-	in 25 mM HEPES, pH 7.4, 250 mM NaCl, 2 mM MgCl2, 10 mM CaCl2, 0.2 mM dithiothreitol, and 0.05% (v/v) Pluronic F-127 at 37°C	Homo sapiens	5-(4-acryloylaminobenzenesulfonyl)-2,5-diazabicyclo-[2.2.1]heptane-2-carboxylic acid tert-butyl ester
0.00031	-	in 25 mM HEPES, pH 7.4, 250 mM NaCl, 2 mM MgCl2, 10 mM CaCl2, 0.2 mM dithiothreitol, and 0.05% (v/v) Pluronic F-127 at 37°C	Homo sapiens	N-[4-[4-(4-phenylbutyl)piperazine-1-sulfonyl]phenyl]-acrylamide
0.00035	-	in 25 mM HEPES, pH 7.4, 250 mM NaCl, 2 mM MgCl2, 10 mM CaCl2, 0.2 mM dithiothreitol, and 0.05% (v/v) Pluronic F-127 at 37°C	Homo sapiens	4-(3-acryloylaminobenzenesulfonyl)piperazine-1-carboxylicacid benzyl ester
0.00038	-	in 25 mM HEPES, pH 7.4, 250 mM NaCl, 2 mM MgCl2, 10 mM CaCl2, 0.2 mM dithiothreitol, and 0.05% (v/v) Pluronic F-127 at 37°C	Homo sapiens	4-[(4-acryloylaminobenzenesulfonylamino)methyl]-piperidine-1-carboxylic acid benzyl ester
0.00038	-	in 25 mM HEPES, pH 7.4, 250 mM NaCl, 2 mM MgCl2, 10 mM CaCl2, 0.2 mM dithiothreitol, and 0.05% (v/v) Pluronic F-127 at 37°C	Homo sapiens	N-[4-[4-(3-phenylpropyl)piperazine-1-sulfonyl]phenyl]-acrylamide
0.00045	-	in 25 mM HEPES, pH 7.4, 250 mM NaCl, 2 mM MgCl2, 10 mM CaCl2, 0.2 mM dithiothreitol, and 0.05% (v/v) Pluronic F-127 at 37°C	Homo sapiens	4-(4-acryloylaminobenzenesulfonylamino)piperidine-1-carboxylic acid benzyl ester
0.00046	-	in 25 mM HEPES, pH 7.4, 250 mM NaCl, 2 mM MgCl2, 10 mM CaCl2, 0.2 mM dithiothreitol, and 0.05% (v/v) Pluronic F-127 at 37°C	Homo sapiens	4-(4-acryloylaminobenzenesulfonyl)[1,4]diazepane-1-carboxylicacid benzyl ester
0.0005	-	in 25 mM HEPES, pH 7.4, 250 mM NaCl, 2 mM MgCl2, 10 mM CaCl2, 0.2 mM dithiothreitol, and 0.05% (v/v) Pluronic F-127 at 37°C	Homo sapiens	3-(4-acryloylaminobenzenesulfonylamino)-(R)-pyrrolidine-1-carboxylic acid benzyl ester
0.00052	-	in 25 mM HEPES, pH 7.4, 250 mM NaCl, 2 mM MgCl2, 10 mM CaCl2, 0.2 mM dithiothreitol, and 0.05% (v/v) Pluronic F-127 at 37°C	Homo sapiens	3-(4-acryloylaminobenzenesulfonylamino)-(S)-pyrrolidine-1-carboxylic acid benzyl ester
0.00058	-	in 25 mM HEPES, pH 7.4, 250 mM NaCl, 2 mM MgCl2, 10 mM CaCl2, 0.2 mM dithiothreitol, and 0.05% (v/v) Pluronic F-127 at 37°C	Homo sapiens	3-(4-acryloylaminobenzenesulfonylamino)-(R)-pyrrolidine-1-carboxylic acid benzyl ester
0.00067	-	in 25 mM HEPES, pH 7.4, 250 mM NaCl, 2 mM MgCl2, 10 mM CaCl2, 0.2 mM dithiothreitol, and 0.05% (v/v) Pluronic F-127 at 37°C	Homo sapiens	N-[4-nitrophenyl]acrylamide
0.00091	-	in 25 mM HEPES, pH 7.4, 250 mM NaCl, 2 mM MgCl2, 10 mM CaCl2, 0.2 mM dithiothreitol, and 0.05% (v/v) Pluronic F-127 at 37°C	Homo sapiens	4-(4-acryloylamino-2-methylbenzenesulfonyl)piperazine-1-carboxylic acid tert-butyl ester
0.0012	-	in 25 mM HEPES, pH 7.4, 250 mM NaCl, 2 mM MgCl2, 10 mM CaCl2, 0.2 mM dithiothreitol, and 0.05% (v/v) Pluronic F-127 at 37°C	Homo sapiens	4-(4-acryloylaminobenzenesulfonyl)piperazine-1-carboxylic acid tert-butyl ester
0.0013	-	in 25 mM HEPES, pH 7.4, 250 mM NaCl, 2 mM MgCl2, 10 mM CaCl2, 0.2 mM dithiothreitol, and 0.05% (v/v) Pluronic F-127 at 37°C	Homo sapiens	N-[4-(piperazine-1-sulfonyl)phenyl]acrylamide
0.0014	-	in 25 mM HEPES, pH 7.4, 250 mM NaCl, 2 mM MgCl2, 10 mM CaCl2, 0.2 mM dithiothreitol, and 0.05% (v/v) Pluronic F-127 at 37°C	Homo sapiens	4-[4-(1-oxobut-2-ynylamino)benzenesulfonyl]piperazine-1-carboxylic acid tert-butyl ester
0.0015	-	in 25 mM HEPES, pH 7.4, 250 mM NaCl, 2 mM MgCl2, 10 mM CaCl2, 0.2 mM dithiothreitol, and 0.05% (v/v) Pluronic F-127 at 37°C	Homo sapiens	[2-[(4-acryloylaminobenzenesulfonyl)methylamino]ethyl]-methylcarbamic acid benzyl ester
0.0019	-	in 25 mM HEPES, pH 7.4, 250 mM NaCl, 2 mM MgCl2, 10 mM CaCl2, 0.2 mM dithiothreitol, and 0.05% (v/v) Pluronic F-127 at 37°C	Homo sapiens	N-[4-(pyrrolidine-1-sulfonyl)phenyl]acrylamide
0.0023	-	in 25 mM HEPES, pH 7.4, 250 mM NaCl, 2 mM MgCl2, 10 mM CaCl2, 0.2 mM dithiothreitol, and 0.05% (v/v) Pluronic F-127 at 37°C	Homo sapiens	4-[4-(2-fluoroacryloylamino)benzenesulfonyl]piperazine-1-carboxylic acid tert-butyl ester
0.0025	-	in 25 mM HEPES, pH 7.4, 250 mM NaCl, 2 mM MgCl2, 10 mM CaCl2, 0.2 mM dithiothreitol, and 0.05% (v/v) Pluronic F-127 at 37°C	Homo sapiens	4-(4-acryloylamino-2-methoxybenzenesulfonyl)piperazine-1-carboxylic acid tert-butyl ester
0.0028	-	in 25 mM HEPES, pH 7.4, 250 mM NaCl, 2 mM MgCl2, 10 mM CaCl2, 0.2 mM dithiothreitol, and 0.05% (v/v) Pluronic F-127 at 37°C	Homo sapiens	4-(4-but-2-enoylaminobenzenesulfonyl)piperazine-1-carboxylic acid tert-butyl ester
0.0029	-	in 25 mM HEPES, pH 7.4, 250 mM NaCl, 2 mM MgCl2, 10 mM CaCl2, 0.2 mM dithiothreitol, and 0.05% (v/v) Pluronic F-127 at 37°C	Homo sapiens	[4-(4-acryloylpiperazine-1-sulfonyl)phenyl]carbamic acid benzyl ester
0.003	-	in 25 mM HEPES, pH 7.4, 250 mM NaCl, 2 mM MgCl2, 10 mM CaCl2, 0.2 mM dithiothreitol, and 0.05% (v/v) Pluronic F-127 at 37°C	Homo sapiens	N-(3-bromophenyl)acrylamide
0.0033	-	in 25 mM HEPES, pH 7.4, 250 mM NaCl, 2 mM MgCl2, 10 mM CaCl2, 0.2 mM dithiothreitol, and 0.05% (v/v) Pluronic F-127 at 37°C	Homo sapiens	N-(4-bromophenyl)acrylamide
0.0038	-	in 25 mM HEPES, pH 7.4, 250 mM NaCl, 2 mM MgCl2, 10 mM CaCl2, 0.2 mM dithiothreitol, and 0.05% (v/v) Pluronic F-127 at 37°C	Homo sapiens	N-[4-trifluoromethylphenyl]acrylamide
0.004	-	25 mM HEPES, pH 7.4, 250 mM NaCl, 2 mM MgCl2, 10 mM CaCl2, 0.2 mM dithiothreitol, and 0.05% (v/v) Pluronic F-127 at 37°C	Homo sapiens	4-[4-(4-diazo-3-oxobutyl)benzenesulfonyl]piperazine-1-carboxylic acid benzyl ester
0.0045	-	in 25 mM HEPES, pH 7.4, 250 mM NaCl, 2 mM MgCl2, 10 mM CaCl2, 0.2 mM dithiothreitol, and 0.05% (v/v) Pluronic F-127 at 37°C	Homo sapiens	4-[4-(acryloylmethyl-amino)benzenesulfonyl]piperazine-1-carboxylic acid tert-butyl ester
0.005	-	in 25 mM HEPES, pH 7.4, 250 mM NaCl, 2 mM MgCl2, 10 mM CaCl2, 0.2 mM dithiothreitol, and 0.05% (v/v) Pluronic F-127 at 37°C	Homo sapiens	N-[4-methanesulfonylphenyl]acrylamide
0.0057	-	in 25 mM HEPES, pH 7.4, 250 mM NaCl, 2 mM MgCl2, 10 mM CaCl2, 0.2 mM dithiothreitol, and 0.05% (v/v) Pluronic F-127 at 37°C	Homo sapiens	N-[4-(aminomethyl)benzyl]-3-(5-[[[[(E)-2-phenylethenyl]sulfonyl](pyridin-2-ylmethyl)amino]methyl]-1,2,4-oxadiazol-3-yl)benzamide
0.0068	-	in 25 mM HEPES, pH 7.4, 250 mM NaCl, 2 mM MgCl2, 10 mM CaCl2, 0.2 mM dithiothreitol, and 0.05% (v/v) Pluronic F-127 at 37°C	Homo sapiens	4-[4-(3-(E)-chloroacryloylamino)benzenesulfonyl]-piperazine-1-carboxylic acid tert-butyl ester
0.0069	-	in 25 mM HEPES, pH 7.4, 250 mM NaCl, 2 mM MgCl2, 10 mM CaCl2, 0.2 mM dithiothreitol, and 0.05% (v/v) Pluronic F-127 at 37°C	Homo sapiens	(5-bromothiophen-2-yl)(4-methyl-1H-pyrazol-1-yl)methanone
0.01	-	IC50 above 0.01 mM, in 25 mM HEPES, pH 7.4, 250 mM NaCl, 2 mM MgCl2, 10 mM CaCl2, 0.2 mM dithiothreitol, and 0.05% (v/v) Pluronic F-127 at 37°C	Homo sapiens	4-[4-(4,4,4-trifluorobut-2-enoylamino)benzenesulfonyl]-piperazine-1-carboxylic acid tert-butyl ester
0.01	-	IC50 above 0.01 mM, in 25 mM HEPES, pH 7.4, 250 mM NaCl, 2 mM MgCl2, 10 mM CaCl2, 0.2 mM dithiothreitol, and 0.05% (v/v) Pluronic F-127 at 37°C	Homo sapiens	4-[4-(4,4,4-trifluoro-3-methylbut-2-enoylamino)-benzenesulfonyl]piperazine-1-carboxylic acid tert-butyl ester
0.013	-	in 25 mM HEPES, pH 7.4, 250 mM NaCl, 2 mM MgCl2, 10 mM CaCl2, 0.2 mM dithiothreitol, and 0.05% (v/v) Pluronic F-127 at 37°C	Homo sapiens	4-(4-acryloylamino-3-fluorobenzenesulfonyl)piperazine-1-carboxylic acid benzyl ester
0.016	-	in 25 mM HEPES, pH 7.4, 250 mM NaCl, 2 mM MgCl2, 10 mM CaCl2, 0.2 mM dithiothreitol, and 0.05% (v/v) Pluronic F-127 at 37°C	Homo sapiens	ethenesulfonic acid (4-bromophenyl)amide
0.016	-	in 25 mM HEPES, pH 7.4, 250 mM NaCl, 2 mM MgCl2, 10 mM CaCl2, 0.2 mM dithiothreitol, and 0.05% (v/v) Pluronic F-127 at 37°C	Homo sapiens	4-[4-(3-diazo-2-oxopropyl)benzenesulfonyl]piperazine-1-carboxylic acid benzyl ester
0.026	-	in 25 mM HEPES, pH 7.4, 250 mM NaCl, 2 mM MgCl2, 10 mM CaCl2, 0.2 mM dithiothreitol, and 0.05% (v/v) Pluronic F-127 at 37°C	Homo sapiens	N-[4-phenoxyphenyl]acrylamide
0.028	-	in 25 mM HEPES, pH 7.4, 250 mM NaCl, 2 mM MgCl2, 10 mM CaCl2, 0.2 mM dithiothreitol, and 0.05% (v/v) Pluronic F-127 at 37°C	Homo sapiens	4-[4-(cyanomethylcarbamoyl)benzenesulfonyl]piperazine-1-carboxylic acid tert-butyl ester
0.029	-	in 25 mM HEPES, pH 7.4, 250 mM NaCl, 2 mM MgCl2, 10 mM CaCl2, 0.2 mM dithiothreitol, and 0.05% (v/v) Pluronic F-127 at 37°C	Homo sapiens	N-(4-fluorophenyl)acrylamide
0.03	-	in 25 mM HEPES, pH 7.4, 250 mM NaCl, 2 mM MgCl2, 10 mM CaCl2, 0.2 mM dithiothreitol, and 0.05% (v/v) Pluronic F-127 at 37°C	Homo sapiens	pyrrolidine-1-carboxylic acid (4-acryloylaminophenyl)-amide
0.043	-	in 25 mM HEPES, pH 7.4, 250 mM NaCl, 2 mM MgCl2, 10 mM CaCl2, 0.2 mM dithiothreitol, and 0.05% (v/v) Pluronic F-127 at 37°C	Homo sapiens	N-(4-bromobenzyl)acrylamide
0.043	-	in 25 mM HEPES, pH 7.4, 250 mM NaCl, 2 mM MgCl2, 10 mM CaCl2, 0.2 mM dithiothreitol, and 0.05% (v/v) Pluronic F-127 at 37°C	Homo sapiens	N-phenylacrylamide
0.045	-	in 25 mM HEPES, pH 7.4, 250 mM NaCl, 2 mM MgCl2, 10 mM CaCl2, 0.2 mM dithiothreitol, and 0.05% (v/v) Pluronic F-127 at 37°C	Homo sapiens	N-[4-toluyl]acrylamide
0.058	-	in 25 mM HEPES, pH 7.4, 250 mM NaCl, 2 mM MgCl2, 10 mM CaCl2, 0.2 mM dithiothreitol, and 0.05% (v/v) Pluronic F-127 at 37°C	Homo sapiens	N-[4-methoxyphenyl]acrylamide
0.076	-	in 25 mM HEPES, pH 7.4, 250 mM NaCl, 2 mM MgCl2, 10 mM CaCl2, 0.2 mM dithiothreitol, and 0.05% (v/v) Pluronic F-127 at 37°C	Homo sapiens	4-[4-acryloylamino-3-(isobutylmethylamino)-benzenesulfonyl]piperazine-1-carboxylic acid benzyl ester
0.08	-	IC50 above 0.08 mM, in 25 mM HEPES, pH 7.4, 250 mM NaCl, 2 mM MgCl2, 10 mM CaCl2, 0.2 mM dithiothreitol, and 0.05% (v/v) Pluronic F-127 at 37°C	Homo sapiens	4-[4-(cyanomethylcarbamoyl)benzenesulfonyl]piperazine-1-carboxylic acid tert-butyl ester
0.08	-	IC50 above 0.08 mM, in 25 mM HEPES, pH 7.4, 250 mM NaCl, 2 mM MgCl2, 10 mM CaCl2, 0.2 mM dithiothreitol, and 0.05% (v/v) Pluronic F-127 at 37°C	Homo sapiens	N-(4-bromophenyl)propionamide
0.08	-	IC50 above 0.08 mM, in 25 mM HEPES, pH 7.4, 250 mM NaCl, 2 mM MgCl2, 10 mM CaCl2, 0.2 mM dithiothreitol, and 0.05% (v/v) Pluronic F-127 at 37°C	Homo sapiens	N-(2-bromophenyl)acrylamide
0.08	-	IC50 above 0.08 mM, in 25 mM HEPES, pH 7.4, 250 mM NaCl, 2 mM MgCl2, 10 mM CaCl2, 0.2 mM dithiothreitol, and 0.05% (v/v) Pluronic F-127 at 37°C	Homo sapiens	4-[4-(2-methylacryloylamino)benzenesulfonyl]piperazine-1-carboxylic acid tert-butyl ester
0.08	-	IC50 above 0.08 mM, in 25 mM HEPES, pH 7.4, 250 mM NaCl, 2 mM MgCl2, 10 mM CaCl2, 0.2 mM dithiothreitol, and 0.05% (v/v) Pluronic F-127 at 37°C	Homo sapiens	4-[4-(2-methylbut-2-enoylamino)benzenesulfonyl]-piperazine-1-carboxylic acid tert-butyl ester
0.08	-	IC50 above 0.08 mM, in 25 mM HEPES, pH 7.4, 250 mM NaCl, 2 mM MgCl2, 10 mM CaCl2, 0.2 mM dithiothreitol, and 0.05% (v/v) Pluronic F-127 at 37°C	Homo sapiens	4-[4-(3-cyanomethylureido)benzenesulfonyl]piperazine-1-carboxylic acid tert-butyl ester
0.08	-	IC50 above 0.08 mM, in 25 mM HEPES, pH 7.4, 250 mM NaCl, 2 mM MgCl2, 10 mM CaCl2, 0.2 mM dithiothreitol, and 0.05% (v/v) Pluronic F-127 at 37°C	Homo sapiens	4-[4-(ethoxycarbonylmethylamino)benzenesulfonyl]-piperazine-1-carboxylic acid tert-butyl ester
0.08	-	IC50 above 0.08 mM, in 25 mM HEPES, pH 7.4, 250 mM NaCl, 2 mM MgCl2, 10 mM CaCl2, 0.2 mM dithiothreitol, and 0.05% (v/v) Pluronic F-127 at 37°C	Homo sapiens	4-[4-(2-cyanoacetylamino)benzenesulfonyl]piperazine-1-carboxylic acid tert-butyl ester
0.08	-	IC50 above 0.08 mM, in 25 mM HEPES, pH 7.4, 250 mM NaCl, 2 mM MgCl2, 10 mM CaCl2, 0.2 mM dithiothreitol, and 0.05% (v/v) Pluronic F-127 at 37°C	Homo sapiens	4-[4-(2-oxopropionylamino)benzenesulfonyl]piperazine-1-carboxylic acid tert-butyl ester
0.08	-	IC50 above 0.08 mM, in 25 mM HEPES, pH 7.4, 250 mM NaCl, 2 mM MgCl2, 10 mM CaCl2, 0.2 mM dithiothreitol, and 0.05% (v/v) Pluronic F-127 at 37°C	Homo sapiens	4-(4-cyanobenzenesulfonyl)piperazine-1-carboxylic acid tert-butyl ester
0.08	-	IC50 above 0.08 mM, in 25 mM HEPES, pH 7.4, 250 mM NaCl, 2 mM MgCl2, 10 mM CaCl2, 0.2 mM dithiothreitol, and 0.05% (v/v) Pluronic F-127 at 37°C	Homo sapiens	4-[4-(2-ethoxycarbonylvinyl)benzenesulfonyl]piperazine-1-carboxylic acid benzyl ester
0.08	-	IC50 above 0.08 mM, in 25 mM HEPES, pH 7.4, 250 mM NaCl, 2 mM MgCl2, 10 mM CaCl2, 0.2 mM dithiothreitol, and 0.05% (v/v) Pluronic F-127 at 37°C	Homo sapiens	[4-[(4-aminophenyl)sulfonyl]piperazin-1-yl](cyclopropyl)methanone
0.091	-	in 25 mM HEPES, pH 7.4, 250 mM NaCl, 2 mM MgCl2, 10 mM CaCl2, 0.2 mM dithiothreitol, and 0.05% (v/v) Pluronic F-127 at 37°C	Homo sapiens	4-[4-(3-ethoxycarbonylallyl)benzenesulfonyl]piperazine-1-carboxylic acid benzyl ester

Expression

Organism	Comment	Expression
Homo sapiens	enzyme expression is up-regulated in the brains of Huntingtons disease patients	up