3.4.24.B12: ADAMTS5 endopeptidase
This is an abbreviated version!
For detailed information about ADAMTS5 endopeptidase, go to the full flat file.
Word Map on EC 3.4.24.B12
-
3.4.24.B12
-
cartilage
-
osteoarthritis
-
chondrocytes
-
articular
-
metalloproteinase
-
collagen
-
joint
-
disintegrin
-
degeneration
-
adamts-4
-
tnf
-
proteoglycans
-
knee
-
intervertebral
-
degener
-
synovial
-
cox-2
-
mmp-1
-
col2a1
-
pulposus
-
meniscus
-
interleukin-1
-
intra-articular
-
versican
-
disintegrin-like
-
timp-3
-
temporomandibular
-
subchondral
-
safranin
-
cruciate
-
matrix-degrading
-
neoepitope
-
chondroprotective
-
chondrogenic
-
brevican
-
medicine
-
mankin
-
surgically-induced
-
oa-like
-
collagen-ii
-
meniscectomy
-
anti-catabolic
-
cartilage-degrading
-
interglobular
-
dmm-induced
-
condylar
-
oa-related
-
oa-associated
-
osteophyte
-
motifs-4
-
osteoarthritis-like
- 3.4.24.B12
- cartilage
- osteoarthritis
- chondrocytes
-
articular
- metalloproteinase
- collagen
- joint
-
disintegrin
- degeneration
- adamts-4
- tnf
- proteoglycans
- knee
-
intervertebral
-
degener
- synovial
- cox-2
- mmp-1
-
col2a1
- pulposus
- meniscus
- interleukin-1
-
intra-articular
- versican
-
disintegrin-like
- timp-3
-
temporomandibular
-
subchondral
-
safranin
-
cruciate
-
matrix-degrading
-
neoepitope
-
chondroprotective
-
chondrogenic
- brevican
- medicine
-
mankin
-
surgically-induced
-
oa-like
-
collagen-ii
-
meniscectomy
-
anti-catabolic
-
cartilage-degrading
-
interglobular
-
dmm-induced
-
condylar
-
oa-related
-
oa-associated
- osteophyte
-
motifs-4
-
osteoarthritis-like
Reaction
proteolytic degradation of proteins =
Synonyms
a disintegrin and metalloprotease with thrombospondin motifs 5, a disintegrin and metalloproteinase with thrombospondin motifs 5, a disintegrin and metalloproteinase with thrombospondin motifs-5, a disintegrin and metalloproteinase with thrombospondin type 1 motifs, member 5, a disintegrin and metalloproteinase with thrombospondin type 1 motifs-5, a disintegrin and metalloproteinase with thrombospondin-1 motifs 5, a disintegrin-like and metalloproteinase with thrombospondin-1 motifs 5, ADAM-TS 5, ADAM-TS11, ADAM-TS5, adamalysin with thrombospondin type 1 motifs-5, ADAMTS-11, ADAMTS-5, ADAMTS-5(p45), ADAMTS-5(p60), ADAMTS-5(p85), ADAMTS-5-2, ADAMTS11, ADAMTS5, ADMP-2, Agg-2, aggrecanase 2, aggrecanase-, aggrecanase-2, implantin, M12.225
ECTree
3.4.24.B12 ADAMTS5 endopeptidaseAdvanced search results
results (
results (IC50 Value
IC50 Value on EC 3.4.24.B12 - ADAMTS5 endopeptidase
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IC50 VALUE [mM] 
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY 
LITERATURE
IMAGE
0.0008
(1R,2R,3S)-1-([[5-(4-chloro-1H-pyrazol-1-yl)thiophen-2-yl]sulfonyl]amino)-2,3-dimethylcyclopropanecarboxylate
Homo sapiens
-
pH and temperature not specified in the publication
0.000073
(1R,2S)-1-([(4'-chlorobiphenyl-4-yl)sulfonyl][2-[4-(methoxycarbonyl)-1H-imidazol-1-yl]ethyl]amino)-2-phenylcyclopropanecarboxylate
Homo sapiens
-
pH and temperature not specified in the publication
0.00007
(1R,2S)-1-([(4'-chlorobiphenyl-4-yl)sulfonyl][2-[4-(methoxycarbonyl)-1H-imidazol-1-yl]ethyl]amino)-2-phenylcyclopropanecarboxylic acid
Homo sapiens
-
0.0002
(1R,2S)-1-([(4'-chlorobiphenyl-4-yl)sulfonyl][2-[5-(methoxycarbonyl)-1H-imidazol-1-yl]ethyl]amino)-2-phenylcyclopropanecarboxylic acid
Homo sapiens
-
0.0045
(1R,2S)-1-([[4'-(acetylamino)biphenyl-4-yl]sulfonyl][2-(2-oxopyrrolidin-1-yl)ethyl]amino)-2-phenylcyclopropanecarboxylic acid
Homo sapiens
-
0.0066
(1R,2S)-1-([[4'-(dimethylamino)biphenyl-4-yl]sulfonyl][2-(2-oxopyrrolidin-1-yl)ethyl]amino)-2-phenylcyclopropanecarboxylic acid
Homo sapiens
-
0.00088
(1R,2S)-1-([[4-(4-chlorophenyl)-3,6-dihydropyridin-1(2H)-yl]sulfonyl][2-(2-oxopyrrolidin-1-yl)ethyl]amino)-2-phenylcyclopropanecarboxylic acid
Homo sapiens
-
0.0011
(1R,2S)-1-([[6-(4-chlorophenyl)pyridin-3-yl]sulfonyl][2-(2-oxopyrrolidin-1-yl)ethyl]amino)-2-phenylcyclopropanecarboxylic acid
Homo sapiens
-
0.00082
(1R,2S)-1-[[(4'-chlorobiphenyl-4-yl)sulfonyl](2-pyridin-2-ylethyl)amino]-2-phenylcyclopropanecarboxylic acid
Homo sapiens
-
0.00029
(1R,2S)-1-[[(4'-chlorobiphenyl-4-yl)sulfonyl](2-pyridin-3-ylethyl)amino]-2-phenylcyclopropanecarboxylate
Homo sapiens
-
0.00075
(1R,2S)-1-[[(4'-chlorobiphenyl-4-yl)sulfonyl](2-pyridin-4-ylethyl)amino]-2-phenylcyclopropanecarboxylic acid
Homo sapiens
-
0.00027
(1R,2S)-1-[[(4'-chlorobiphenyl-4-yl)sulfonyl][2-(1H-1,2,3-triazol-1-yl)ethyl]amino]-2-phenylcyclopropanecarboxylate
Homo sapiens
-
0.00018
(1R,2S)-1-[[(4'-chlorobiphenyl-4-yl)sulfonyl][2-(1H-1,2,4-triazol-1-yl)ethyl]amino]-2-phenylcyclopropanecarboxylic acid
Homo sapiens
-
0.0002
(1R,2S)-1-[[(4'-chlorobiphenyl-4-yl)sulfonyl][2-(1H-imidazol-1-yl)ethyl]amino]-2-phenylcyclopropanecarboxylic acid
Homo sapiens
-
0.00027
(1R,2S)-1-[[(4'-chlorobiphenyl-4-yl)sulfonyl][2-(1H-tetrazol-1-yl)ethyl]amino]-2-phenylcyclopropanecarboxylic acid
Homo sapiens
-
0.0001
(1R,2S)-1-[[(4'-chlorobiphenyl-4-yl)sulfonyl][2-(2,5-dioxopyrrolidin-1-yl)ethyl]amino]-2-phenylcyclopropanecarboxylic acid
Homo sapiens
-
0.00018
(1R,2S)-1-[[(4'-chlorobiphenyl-4-yl)sulfonyl][2-(2-oxo-1,3-oxazinan-3-yl)ethyl]amino]-2-phenylcyclopropanecarboxylate
Homo sapiens
-
0.00022
(1R,2S)-1-[[(4'-chlorobiphenyl-4-yl)sulfonyl][2-(2-oxo-1,3-oxazolidin-3-yl)ethyl]amino]-2-phenylcyclopropanecarboxylic acid
Homo sapiens
-
0.00021
(1R,2S)-1-[[(4'-chlorobiphenyl-4-yl)sulfonyl][2-(2-oxopiperidin-1-yl)ethyl]amino]-2-phenylcyclopropanecarboxylic acid
Homo sapiens
-
0.0002
(1R,2S)-1-[[(4'-chlorobiphenyl-4-yl)sulfonyl][2-(2-oxopyrrolidin-1-yl)ethyl]amino]-2-phenylcyclopropanecarboxylic acid
Homo sapiens
-
0.00026
(1R,2S)-1-[[(4'-chlorobiphenyl-4-yl)sulfonyl][2-(2H-1,2,3-triazol-2-yl)ethyl]amino]-2-phenylcyclopropanecarboxylate
Homo sapiens
-
0.00078
(1R,2S)-1-[[(4'-chlorobiphenyl-4-yl)sulfonyl][2-(3-methoxy-2-oxopyridin-1(2H)-yl)ethyl]amino]-2-phenylcyclopropanecarboxylate
Homo sapiens
-
0.00019
(1R,2S)-1-[[(4'-chlorobiphenyl-4-yl)sulfonyl][2-(4H-1,2,4-triazol-4-yl)ethyl]amino]-2-phenylcyclopropanecarboxylic acid
Homo sapiens
-
0.000071
(1R,2S)-1-[[(4'-chlorobiphenyl-4-yl)sulfonyl][2-(7H-purin-7-yl)ethyl]amino]-2-phenylcyclopropanecarboxylic acid
Homo sapiens
-
0.00017
(1R,2S)-1-[[(4'-chlorobiphenyl-4-yl)sulfonyl][2-(9H-purin-9-yl)ethyl]amino]-2-phenylcyclopropanecarboxylic acid
Homo sapiens
-
0.00021
(1S,2R)-1-([(4'-chlorobiphenyl-4-yl)sulfonyl][2-[4-(methoxycarbonyl)-1H-imidazol-1-yl]ethyl]amino)-2-phenylcyclopropanecarboxylate
Homo sapiens
-
pH and temperature not specified in the publication
0.000094
(1S,2R)-1-([[5-(3-chlorophenyl)thiophen-2-yl]sulfonyl]amino)-2-phenylcyclopropanecarboxylate
Homo sapiens
-
pH and temperature not specified in the publication
0.00077
(1S,2R)-1-([[5-(4-chloro-1H-pyrazol-1-yl)thiophen-2-yl]sulfonyl]amino)-2-(propan-2-yl)cyclopropanecarboxylate
Homo sapiens
-
pH and temperature not specified in the publication
0.00036
(1S,2R)-1-([[5-(4-chloro-1H-pyrazol-1-yl)thiophen-2-yl]sulfonyl]amino)-2-cyclohexylcyclopropanecarboxylate
Homo sapiens
-
pH and temperature not specified in the publication
0.000032
(1S,2R)-1-([[5-(4-chloro-1H-pyrazol-1-yl)thiophen-2-yl]sulfonyl]amino)-2-methyl-2-phenylcyclopropanecarboxylate
Homo sapiens
-
pH and temperature not specified in the publication
0.00008
(1S,2R)-1-([[5-(4-chloro-1H-pyrazol-1-yl)thiophen-2-yl]sulfonyl]amino)-2-phenylcyclopropanecarboxylate
Homo sapiens
-
pH and temperature not specified in the publication
0.00001
(1S,2R)-1-([[5-(4-chlorophenyl)thiophen-2-yl]sulfonyl]amino)-2-methyl-2-phenylcyclopropanecarboxylate
Homo sapiens
-
pH and temperature not specified in the publication
0.00006
(1S,2R)-1-([[5-(4-chlorophenyl)thiophen-2-yl]sulfonyl]amino)-2-phenylcyclopropanecarboxylate
Homo sapiens
-
pH and temperature not specified in the publication
0.0001
(1S,2R)-1-([[5-(5-chloropyridin-2-yl)thiophen-2-yl]sulfonyl]amino)-2-phenylcyclopropanecarboxylate
Homo sapiens
-
pH and temperature not specified in the publication
0.000084
(1S,2R)-1-[[(4'-chlorobiphenyl-4-yl)sulfonyl]amino]-2-phenylcyclopropanecarboxylate
Homo sapiens
-
pH and temperature not specified in the publication
0.0000074
(1S,2R,3R)-1-([[5-(4-chloro-1H-pyrazol-1-yl)thiophen-2-yl]sulfonyl]amino)-2-methyl-3-phenylcyclopropanecarboxylate
Homo sapiens
-
pH and temperature not specified in the publication
0.000021
(1S,2R,3R)-1-([[5-(4-chlorophenyl)thiophen-2-yl]sulfonyl]amino)-2-methyl-3-phenylcyclopropanecarboxylate
Homo sapiens
-
pH and temperature not specified in the publication
0.00012
(1S,2S,3R)-1-([[5-(4-chlorophenyl)thiophen-2-yl]sulfonyl]amino)-2-methyl-3-phenylcyclopropanecarboxylate
Homo sapiens
-
pH and temperature not specified in the publication
0.000129
(2R)-2-[4-(1,3-benzodioxol-5-yl)benzyl]-N4-hydroxy-N1-[(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]butanediamide
Homo sapiens
pH and temperature not specified in the publication
0.000093
(2R)-N4-hydroxy-2-(3-hydroxybenzyl)-N1-[(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]butanediamide
Homo sapiens
pH 7.5, 37°C
0.0000014
(2R,5R)-1-([4-[(2,4-dichlorobenzyl)oxy]phenyl]sulfonyl)-N,5-dihydroxy-3,3-dimethylpiperidine-2-carboxamide
Homo sapiens
-
37°C, pH and temperature not specified in the publication
0.000017
(3R)-N2-(cyclopropylmethyl)-N1-hydroxy-3-(3-hydroxybenzyl)-N4-[(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]-L-aspartamide
Homo sapiens
pH 7.5, 37°C
0.0053
(5E)-2-thioxo-5-([3-[3-(trifluoromethyl)phenoxy]phenyl]methylidene)-1,3-thiazolidin-4-one
Homo sapiens
-
-
0.067
(5E)-3-benzyl-5-[[3,4-bis(benzyloxy)phenyl]methylidene]-2-thioxo-1,3-thiazolidin-4-one
Homo sapiens
-
IC50 above 0.067 mM
0.0116
(5E)-5-([3-methoxy-4-[(4-methoxybenzyl)oxy]phenyl]methylidene)-2-thioxo-1,3-thiazolidin-4-one
Homo sapiens
-
-
0.0035
(5E)-5-([4-[(4-chlorobenzyl)oxy]-3-methoxyphenyl]methylidene)-2-thioxo-1,3-thiazolidin-4-one
Homo sapiens
-
-
0.022
(5E)-5-[(3-phenoxyphenyl)methylidene]-2-thioxo-1,3-thiazolidin-4-one
Homo sapiens
-
IC50 above 0.022 mM
0.0018
(5E)-5-[[3,4-bis(benzyloxy)phenyl]methylidene]-2-thioxo-1,3-thiazolidin-4-one
Homo sapiens
-
-
0.067
(5E)-5-[[3,4-bis(benzyloxy)phenyl]methylidene]-3-(2-phenylethyl)-2-thioxo-1,3-thiazolidin-4-one
Homo sapiens
-
IC50 above 0.067 mM
0.067
(5E)-5-[[3,4-bis(benzyloxy)phenyl]methylidene]-3-ethyl-2-thioxo-1,3-thiazolidin-4-one
Homo sapiens
-
IC50 above 0.067 mM
0.067
(5E)-5-[[3,4-bis(benzyloxy)phenyl]methylidene]-3-methyl-2-thioxo-1,3-thiazolidin-4-one
Homo sapiens
-
IC50 above 0.067 mM
0.067
(5E)-5-[[3,4-bis(benzyloxy)phenyl]methylidene]-3-phenyl-2-thioxo-1,3-thiazolidin-4-one
Homo sapiens
-
IC50 above 0.067 mM
0.0014
(5E)-5-[[3,5-bis(benzyloxy)phenyl]methylidene]-2-thioxo-1,3-thiazolidin-4-one
Homo sapiens
-
-
0.0032
(5E)-5-[[3-(3,4-dichlorophenoxy)phenyl]methylidene]-2-thioxo-1,3-thiazolidin-4-one
Homo sapiens
-
-
0.0025
(5E)-5-[[3-(3,5-dichlorophenoxy)phenyl]methylidene]-2-thioxo-1,3-thiazolidin-4-one
Homo sapiens
-
-
0.0049 - 0.022
(5E)-5-[[3-(4-chlorophenoxy)phenyl]methylidene]-2-thioxo-1,3-thiazolidin-4-one
0.0162
(5E)-5-[[3-(4-methoxyphenoxy)phenyl]methylidene]-2-thioxo-1,3-thiazolidin-4-one
Homo sapiens
-
-
0.0148
(5E)-5-[[3-(4-methylphenoxy)phenyl]methylidene]-2-thioxo-1,3-thiazolidin-4-one
Homo sapiens
-
-
0.0017
(5E)-5-[[3-(4-tert-butylphenoxy)phenyl]methylidene]-2-thioxo-1,3-thiazolidin-4-one
Homo sapiens
-
-
0.0201
(5E)-5-[[3-(benzyloxy)phenyl]methylidene]-2-thioxo-1,3-thiazolidin-4-one
Homo sapiens
-
-
0.022
(5E)-5-[[4-(benzyloxy)-3-methoxyphenyl]methylidene]-2-thioxo-1,3-thiazolidin-4-one
Homo sapiens
-
IC50 above 0.022 mM
0.01
(5Z)-5-[[3-(3,4-dichlorophenoxy)phenyl]methylidene]-2-thioxo-1,3-thiazolidin-4-one
Homo sapiens
-
-
0.0092
(5Z)-5-[[3-(3,5-dichlorophenoxy)phenyl]methylidene]-2-thioxo-1,3-thiazolidin-4-one
Homo sapiens
-
-
0.067
(5Z)-5-[[3-(3,5-dichlorophenoxy)phenyl]methylidene]-2-thioxoimidazolidin-4-one
Homo sapiens
-
IC50 above 0.067 mM
0.022
(5Z)-5-[[3-(4-chlorophenoxy)phenyl]methylidene]-1-methyl-2-thioxoimidazolidin-4-one
Homo sapiens
-
IC50 above 0.022 mM
0.067
(5Z)-5-[[3-(4-chlorophenoxy)phenyl]methylidene]-2-thioxoimidazolidin-4-one
Homo sapiens
-
IC50 above 0.067 mM
0.0068
(5Z)-5-[[3-(4-tert-butylphenoxy)phenyl]methylidene]-2-thioxo-1,3-thiazolidin-4-one
Homo sapiens
-
-
0.067
(5Z)-5-[[3-(4-tert-butylphenoxy)phenyl]methylidene]-2-thioxoimidazolidin-4-one
Homo sapiens
-
IC50 above 0.067 mM
0.0026
(R)-2-(4'-((4-(cyclohexanecarbonyl)phenoxy)methyl)biphenyl-4-ylsulfonamido)-3-methylbutanoic acid
Mus musculus
-
-
0.0084
(R)-2-(4'-((4-isobutyrylphenoxy)methyl)biphenyl-4-ylsulfonamido)-3-methylbutanoic acid
Mus musculus
-
-
0.0066
(R)-3-methyl-2-(4'-((5-oxo-5,6,7,8-tetrahydronaphthalen-2-yloxy)methyl)biphenyl-4-ylsulfonamido)butanoic acid
Mus musculus
-
-
0.00042
1-benzyl-4-((4-(4-chlorophenoxy) phenyl)-sulfonyl)-N-hydroxypiperidine-4-carboxamide
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.00233
2-(4-acetylphenoxy)-N-[(5-chloro-8-hydroxyquinolin-7-yl)(3-nitrophenyl)methyl]acetamide
Homo sapiens
-
0.00083
2-(benzyloxy)-N-[(5-chloro-8-hydroxyquinolin-7-yl)(3-fluorophenyl)methyl]acetamide
Homo sapiens
-
0.0007
2-(benzyloxy)-N-[(5-chloro-8-hydroxyquinolin-7-yl)(4-methylphenyl)methyl]acetamide
Homo sapiens
-
0.0011
2-[(5E)-5-[[3,4-bis(benzyloxy)phenyl]methylidene]-4-oxo-2-thioxo-1,3-thiazolidin-3-yl]-3-methylbutanoic acid
Homo sapiens
-
-
0.0013
2-[(5E)-5-[[3,4-bis(benzyloxy)phenyl]methylidene]-4-oxo-2-thioxo-1,3-thiazolidin-3-yl]-3-phenylpropanoic acid
Homo sapiens
-
-
0.0018
2-[(5Z)-5-[[3-(3,4-dichlorophenoxy)phenyl]methylidene]-4-oxo-2-thioxo-1,3-thiazolidin-3-yl]-3-methylbutanoic acid
Homo sapiens
-
-
0.0016
2-[(5Z)-5-[[3-(3,4-dichlorophenoxy)phenyl]methylidene]-4-oxo-2-thioxo-1,3-thiazolidin-3-yl]-3-phenylpropanoic acid
Homo sapiens
-
-
0.00234
2-[4-(acetylamino)phenoxy]-N-[(5-chloro-8-hydroxyquinolin-7-yl)(2-chlorophenyl)methyl]acetamide
Homo sapiens
-
0.00133
2-[4-(acetylamino)phenoxy]-N-[(5-chloro-8-hydroxyquinolin-7-yl)(3-fluorophenyl)methyl]acetamide
Homo sapiens
-
0.00339
2-[4-(acetylamino)phenoxy]-N-[(5-chloro-8-hydroxyquinolin-7-yl)(4-methoxyphenyl)methyl]acetamide
Homo sapiens
-
0.012
2-[4-(benzyloxy)phenyl]-2,3-dihydro-1-oxo-1H-pyrrolo[3,4-c]quinoline-4-carboxylate
Homo sapiens
-
37°C, pH and temperature not specified in the publication
0.00095
2-[4-(benzyloxy)phenyl]-2,3-dihydro-N-hydroxy-1-oxo-1Hpyrrolo[3,4-c]quinoline-4-carboxamide
Homo sapiens
-
37°C, pH and temperature not specified in the publication
0.0053
3-[(5E)-5-[[3,4-bis(benzyloxy)phenyl]methylidene]-4-oxo-2-thioxo-1,3-thiazolidin-3-yl]propanoic acid
Homo sapiens
-
-
0.00023 - 0.023
3-[2-[(Z)-(4-oxo-1,3-thiazolidin-2-ylidene)methyl]-4-(pyridin-2-yl)-1,3-thiazol-5-yl]propanoic acid
0.008
4-[(4-oxo-2-thioxo-1,3-thiazolidin-5-yl)methyl]-3-phenyl-5-(2-pyrimidin-1(6H)-ylpiperazin-1-yl)-1H-pyrazole-1-carbonitrile
Homo sapiens
-
-
0.0117
4-[(4-oxo-2-thioxo-1,3-thiazolidin-5-yl)methyl]-5-(2-pyrimidin-1(6H)-ylpiperazin-1-yl)-3-(trifluoromethyl)-1H-pyrazole-1-carbonitrile
Homo sapiens
-
-
0.0037
5-([1,3-diphenyl-5-[(thiophen-2-ylmethyl)sulfanyl]-1H-pyrazol-4-yl]methyl)-2-thioxo-1,3-thiazolidin-4-one
Homo sapiens
-
-
0.0083
5-([1-methyl-5-[(4-methylphenyl)sulfanyl]-3-phenyl-1H-pyrazol-4-yl]methyl)-2-thioxo-1,3-thiazolidin-4-one
Homo sapiens
-
-
0.0091
5-([1-phenyl-5-[2-(tetrahydrothiophen-2-yl)ethoxy]-3-(trifluoromethyl)-1H-pyrazol-4-yl]methyl)-2-thioxo-1,3-thiazolidin-4-one
Homo sapiens
-
-
0.0232
5-([5-[(2-chlorobenzyl)sulfanyl]-1-methyl-3-(2,2,2-trifluoroethyl)-1H-pyrazol-4-yl]methyl)-2-thioxo-1,3-thiazolidin-4-one
Homo sapiens
-
-
0.0011
5-([5-[(4-chlorobenzyl)sulfanyl]-1-methyl-3-(2,2,2-trifluoroethyl)-1H-pyrazol-4-yl]methyl)-2-thioxo-1,3-thiazolidin-4-one
Homo sapiens
-
-
0.0025
5-([5-[(4-chlorobenzyl)sulfanyl]-1-phenyl-3-(2,2,2-trifluoroethyl)-1H-pyrazol-4-yl]methyl)-2-thioxo-1,3-thiazolidin-4-one
Homo sapiens
-
-
0.0022
5-([5-[(4-tert-butylbenzyl)sulfanyl]-1-methyl-3-(2,2,2-trifluoroethyl)-1H-pyrazol-4-yl]methyl)-2-thioxo-1,3-thiazolidin-4-one
Homo sapiens
-
-
0.0067
5-([5-[(furan-2-ylmethyl)sulfanyl]-1,3-diphenyl-1H-pyrazol-4-yl]methyl)-2-thioxo-1,3-thiazolidin-4-one
Homo sapiens
-
-
0.0141
5-([5-[(furan-2-ylmethyl)sulfanyl]-1-methyl-3-phenyl-1H-pyrazol-4-yl]methyl)-2-thioxo-1,3-thiazolidin-4-one
Homo sapiens
-
-
0.0042
5-([5-[2-(4-chlorophenyl)ethoxy]-1-phenyl-3-(trifluoromethyl)-1H-pyrazol-4-yl]methyl)-2-thioxo-1,3-thiazolidin-4-one
Homo sapiens
-
-
0.0071
5-([5-[2-(4-fluorophenyl)ethoxy]-1-phenyl-3-(trifluoromethyl)-1H-pyrazol-4-yl]methyl)-2-thioxo-1,3-thiazolidin-4-one
Homo sapiens
-
-
0.009
5-([5-[4-(4-chlorophenyl)piperazin-1-yl]-1-methyl-3-(2,2,2-trifluoroethyl)-1H-pyrazol-4-yl]methyl)-2-thioxo-1,3-thiazolidin-4-one
Homo sapiens
-
-
0.0021
5-([5-[4-(4-chlorophenyl)piperazin-1-yl]-1-phenyl-3-(2,2,2-trifluoroethyl)-1H-pyrazol-4-yl]methyl)-2-thioxo-1,3-thiazolidin-4-one
Homo sapiens
-
-
0.0042
5-[(4-chlorobenzyl)sulfanyl]-4-[(4-oxo-2-thioxo-1,3-thiazolidin-5-yl)methyl]-3-(2,2,2-trifluoroethyl)-1H-pyrazole-1-carbonitrile
Homo sapiens
-
-
0.0046
5-[(furan-2-ylmethyl)sulfanyl]-4-[(4-oxo-2-thioxo-1,3-thiazolidin-5-yl)methyl]-3-phenyl-1H-pyrazole-1-carbonitrile
Homo sapiens
-
-
0.0046
5-[[5-(4-methylpiperazin-1-yl)-1,3-diphenyl-1H-pyrazol-4-yl]methyl]-2-thioxo-1,3-thiazolidin-4-one
Homo sapiens
-
-
0.0169
5-[[5-(benzylsulfanyl)-1-phenyl-3-(trifluoromethyl)-1H-pyrazol-4-yl]methyl]-2-thioxo-1,3-thiazolidin-4-one
Homo sapiens
-
-
0.129
N-hydroxy-4-(4-(4-(trifluoromethyl)-phenoxy)phenylsulfonyl)-tetrahydro-2H-pyran-4-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.00029
N-hydroxy-4-([4-[4-(trifluoromethyl)phenoxy]phenyl]sulfonyl)tetrahydro-2H-pyran-4-carboxamide
Homo sapiens
-
in 100 mM Tris-HCl, 100 mM NaCl, 0.01 mM CaCl2, 0.05% Brij, pH 7.5
0.00242
N-[(2-chlorophenyl)(8-hydroxy-5-methylquinolin-7-yl)methyl]-2-phenoxyacetamide
Homo sapiens
-
0.00094
N-[(2-chlorophenyl)(8-hydroxy-5-nitroquinolin-7-yl)methyl]-2-phenoxyacetamide
Homo sapiens
-
0.00083
N-[(5-bromo-8-hydroxyquinolin-7-yl)(2-chlorophenyl)methyl]-2-phenoxyacetamide
Homo sapiens
-
0.00062
N-[(5-bromo-8-hydroxyquinolin-7-yl)(3-nitrophenyl)methyl]-2-phenoxyacetamide
Homo sapiens
-
0.00035
N-[(5-chloro-8-hydroxyquinolin-7-yl)(2-chlorophenyl)methyl]-2-phenoxyacetamide
Homo sapiens
sub-micromol ADAMTS-5 potency and good selectivity over the related metalloproteases ADAMTS-4 (aggrecanase-1), MMP-13, and MMP-12
0.00172
N-[(5-chloro-8-hydroxyquinolin-7-yl)(2-chlorophenyl)methyl]-2-[3-(dimethylamino)phenoxy]acetamide
Homo sapiens
-
0.00148
N-[(5-chloro-8-hydroxyquinolin-7-yl)(2-chlorophenyl)methyl]-N2-(4-chloro-3-methylphenyl)glycinamide
Homo sapiens
-
0.00099
N-[(5-chloro-8-hydroxyquinolin-7-yl)(2-chlorophenyl)methyl]-N2-methyl-N2-phenylglycinamide
Homo sapiens
-
0.00232
N-[(5-chloro-8-hydroxyquinolin-7-yl)(2-cyanophenyl)methyl]-2-phenoxyacetamide
Homo sapiens
-
0.00122
N-[(5-chloro-8-hydroxyquinolin-7-yl)(2-fluorophenyl)methyl]-2-phenoxyacetamide
Homo sapiens
-
0.00185
N-[(5-chloro-8-hydroxyquinolin-7-yl)(2-methylphenyl)methyl]-2-phenoxyacetamide
Homo sapiens
-
0.00121
N-[(5-chloro-8-hydroxyquinolin-7-yl)(2-nitrophenyl)methyl]-2-phenoxyacetamide
Homo sapiens
-
0.00062
N-[(5-chloro-8-hydroxyquinolin-7-yl)(3-fluorophenyl)methyl]-2-phenoxyacetamide
Homo sapiens
-
0.00337
N-[(5-chloro-8-hydroxyquinolin-7-yl)(3-fluorophenyl)methyl]-2-[3-(dimethylamino)phenoxy]acetamide
Homo sapiens
-
0.00143
N-[(5-chloro-8-hydroxyquinolin-7-yl)(3-fluorophenyl)methyl]-N2-(4-chloro-3-methylphenyl)glycinamide
Homo sapiens
-
0.00125
N-[(5-chloro-8-hydroxyquinolin-7-yl)(3-fluorophenyl)methyl]-N2-methyl-N2-phenylglycinamide
Homo sapiens
-
0.00166
N-[(5-chloro-8-hydroxyquinolin-7-yl)(3-nitrophenyl)methyl]-2-(pyridin-3-yloxy)acetamide
Homo sapiens
-
0.00049
N-[(5-chloro-8-hydroxyquinolin-7-yl)(3-nitrophenyl)methyl]-2-phenoxyacetamide
Homo sapiens
sub-micromol ADAMTS-5 potency and good selectivity over the related metalloproteases ADAMTS-4 (aggrecanase-1), MMP-13, and MMP-12
0.00119
N-[(5-chloro-8-hydroxyquinolin-7-yl)(3-nitrophenyl)methyl]-N2-(4-chloro-3-methylphenyl)glycinamide
Homo sapiens
-
0.00056
N-[(5-chloro-8-hydroxyquinolin-7-yl)(3-nitrophenyl)methyl]-N2-methyl-N2-phenylglycinamide
Homo sapiens
sub-micromol ADAMTS-5 potency and good selectivity over the related metalloproteases ADAMTS-4 (aggrecanase-1), MMP-13, and MMP-12. Good balance of potent ADAMTS-5 inhibition, moderate CYP3A4 inhibition and good rat liver microsome stability
0.00083
N-[(5-chloro-8-hydroxyquinolin-7-yl)(4-chlorophenyl)methyl]-2-phenoxyacetamide
Homo sapiens
-
0.00094
N-[(5-chloro-8-hydroxyquinolin-7-yl)(4-methoxyphenyl)methyl]-2-(4-methoxyphenoxy)acetamide
Homo sapiens
sub-micromol ADAMTS-5 potency and good selectivity over the related metalloproteases ADAMTS-4 (aggrecanase-1), MMP-13, and MMP-12
0.00077
N-[(5-chloro-8-hydroxyquinolin-7-yl)(4-methoxyphenyl)methyl]-2-(4-methylphenoxy)acetamide
Homo sapiens
-
0.00298
N-[(5-chloro-8-hydroxyquinolin-7-yl)(4-methoxyphenyl)methyl]-2-(pyridin-3-yloxy)acetamide
Homo sapiens
-
0.00135
N-[(5-chloro-8-hydroxyquinolin-7-yl)(4-methoxyphenyl)methyl]-2-phenoxyacetamide
Homo sapiens
-
0.00167
N-[(5-chloro-8-hydroxyquinolin-7-yl)(4-methoxyphenyl)methyl]-2-[3-(dimethylamino)phenoxy]acetamide
Homo sapiens
-
0.00076
N-[(5-chloro-8-hydroxyquinolin-7-yl)(4-methylphenyl)methyl]-2-phenoxyacetamide
Homo sapiens
-
0.00158
N-[(5-chloro-8-hydroxyquinolin-7-yl)(4-methylphenyl)methyl]-N2-(4-chloro-3-methylphenyl)glycinamide
Homo sapiens
-
0.00101
N-[(5-chloro-8-hydroxyquinolin-7-yl)(4-methylphenyl)methyl]-N2-(4-cyanophenyl)glycinamide
Homo sapiens
-
0.00078
N-[(5-chloro-8-hydroxyquinolin-7-yl)(4-methylphenyl)methyl]-N2-methyl-N2-phenylglycinamide
Homo sapiens
-
0.00193
N-[(5-chloro-8-hydroxyquinolin-7-yl)(4-methylphenyl)methyl]-N2-[3-(dimethylamino)phenyl]glycinamide
Homo sapiens
-
0.00046
N-[(5-chloro-8-hydroxyquinolin-7-yl)(4-nitrophenyl)methyl]-2-phenoxyacetamide
Homo sapiens
-
0.00102
N-[(5-chloro-8-hydroxyquinolin-7-yl)(phenyl)methyl]-2-(4-chlorophenoxy)acetamide
Homo sapiens
-
0.0019
N-[(5-chloro-8-hydroxyquinolin-7-yl)(phenyl)methyl]-2-(4-methylphenoxy)acetamide
Homo sapiens
-
0.00078
N-[(5-chloro-8-hydroxyquinolin-7-yl)(phenyl)methyl]-2-phenoxyacetamide
Homo sapiens
-
0.00083
N-[(5-chloro-8-hydroxyquinolin-7-yl)[2-(trifluoromethyl)phenyl]methyl]-2-phenoxyacetamide
Homo sapiens
-
0.00484
N-[(5-fluoro-8-hydroxyquinolin-7-yl)(phenyl)methyl]-2-phenoxyacetamide
Homo sapiens
-
0.00132
N-[(8-hydroxy-5-methylquinolin-7-yl)(3-nitrophenyl)methyl]-2-phenoxyacetamide
Homo sapiens
-
0.00135
N-[(8-hydroxy-5-nitroquinolin-7-yl)(phenyl)methyl]-2-phenoxyacetamide
Homo sapiens
-
0.000004 - 0.000035
N-[[(4S)-4-(1-methylimidazol-2-yl)-2,5-dioxo-imidazolidin-4-yl]methyl]-5-(trifluoromethyl)benzofuran-2-carboxamide
0.00107
N2-(4-acetylphenyl)-N-[(5-chloro-8-hydroxyquinolin-7-yl)(3-nitrophenyl)methyl]glycinamide
Homo sapiens
-
0.00113
N2-(4-acetylphenyl)-N-[(5-chloro-8-hydroxyquinolin-7-yl)(4-methylphenyl)methyl]glycinamide
Homo sapiens
-
0.0011
N2-(biphenyl-4-ylcarbonyl)-N-(2-phenylpropan-2-yl)-L-alpha-glutamine
Homo sapiens
-
37°C, pH and temperature not specified in the publication
0.00131
N2-benzyl-N-[(5-chloro-8-hydroxyquinolin-7-yl)(2-chlorophenyl)methyl]-N2-methylglycinamide
Homo sapiens
-
0.00189
N2-benzyl-N-[(5-chloro-8-hydroxyquinolin-7-yl)(2-chlorophenyl)methyl]glycinamide
Homo sapiens
-
0.00144
N2-benzyl-N-[(5-chloro-8-hydroxyquinolin-7-yl)(3-fluorophenyl)methyl]-N2-methylglycinamide
Homo sapiens
-
0.00172
N2-benzyl-N-[(5-chloro-8-hydroxyquinolin-7-yl)(3-fluorophenyl)methyl]glycinamide
Homo sapiens
-
0.00082
N2-benzyl-N-[(5-chloro-8-hydroxyquinolin-7-yl)(3-nitrophenyl)methyl]-N2-methylglycinamide
Homo sapiens
-
0.00128
N2-benzyl-N-[(5-chloro-8-hydroxyquinolin-7-yl)(4-methylphenyl)methyl]-N2-methylglycinamide
Homo sapiens
-
0.00183
N2-benzyl-N-[(5-chloro-8-hydroxyquinolin-7-yl)(4-methylphenyl)methyl]glycinamide
Homo sapiens
-
0.00277
N2-[4-(acetylamino)phenyl]-N-[(5-chloro-8-hydroxyquinolin-7-yl)(3-nitrophenyl)methyl]glycinamide
Homo sapiens
-
0.0000038
TIMP-3
Homo sapiens
-
in 100 mM Tris-HCl, 100 mM NaCl, 0.01 mM CaCl2, 0.05% Brij, pH 7.5
-
0.0009
[(5E)-5-[[3,4-bis(benzyloxy)phenyl]methylidene]-4-oxo-2-thioxo-1,3-thiazolidin-3-yl](phenyl)acetic acid
Homo sapiens
-
-
0.0067
[(5E)-5-[[3,4-bis(benzyloxy)phenyl]methylidene]-4-oxo-2-thioxo-1,3-thiazolidin-3-yl]acetic acid
Homo sapiens
-
-
0.0013
[(5Z)-5-[[3-(3,4-dichlorophenoxy)phenyl]methylidene]-4-oxo-2-thioxo-1,3-thiazolidin-3-yl](phenyl)acetic acid
Homo sapiens
-
-
0.0111
[(5Z)-5-[[3-(3,4-dichlorophenoxy)phenyl]methylidene]-4-oxo-2-thioxo-1,3-thiazolidin-3-yl]acetic acid
Homo sapiens
-
-
0.0049
(5E)-5-[[3-(4-chlorophenoxy)phenyl]methylidene]-2-thioxo-1,3-thiazolidin-4-one
Homo sapiens
-
-
0.022
(5E)-5-[[3-(4-chlorophenoxy)phenyl]methylidene]-2-thioxo-1,3-thiazolidin-4-one
Homo sapiens
-
IC50 above 0.022 mM
0.00017
(E)-2-((1H-benzo[d]imidazol-2-yl)methylene)-5-propylthiazolidin-4-one
Homo sapiens
pH 7.5, 37°C
0.021
(E)-2-((1H-benzo[d]imidazol-2-yl)methylene)-5-propylthiazolidin-4-one
Homo sapiens
pH 7.5, 37°C
0.00023
3-[2-[(Z)-(4-oxo-1,3-thiazolidin-2-ylidene)methyl]-4-(pyridin-2-yl)-1,3-thiazol-5-yl]propanoic acid
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.023
3-[2-[(Z)-(4-oxo-1,3-thiazolidin-2-ylidene)methyl]-4-(pyridin-2-yl)-1,3-thiazol-5-yl]propanoic acid
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.000004
N-[[(4S)-4-(1-methylimidazol-2-yl)-2,5-dioxo-imidazolidin-4-yl]methyl]-5-(trifluoromethyl)benzofuran-2-carboxamide
Homo sapiens
-
pH 7.5, 22°C
0.000035
N-[[(4S)-4-(1-methylimidazol-2-yl)-2,5-dioxo-imidazolidin-4-yl]methyl]-5-(trifluoromethyl)benzofuran-2-carboxamide
Homo sapiens
-
pH 7.5, 22°C, presence of 50% rat plasma
additional information
2-[4-(benzyloxy)phenyl]-3-oxoisoindoline-4-carboxylic acid
Homo sapiens
-
IC25-value: 0.0075 mM, 37°C, pH and temperature not specified in the publication, plateau inhibition at about 50%
additional information
2-[4-(benzyloxy)phenyl]-N-hydroxy-3-oxoisoindoline-4-carboxamide
Homo sapiens
-
IC25-value: 0.0025 mM, 37°C, pH and temperature not specified in the publication, plateau inhibition at about 50%
