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Literature summary for 3.4.24.B12 extracted from

  • Shiozaki, M.; Imai, H.; Maeda, K.; Miura, T.; Yasue, K.; Suma, A.; Yokota, M.; Ogoshi, Y.; Haas, J.; Fryer, A.M.; Laird, E.R.; Littmann, N.M.; Andrews, S.W.; Josey, J.A.; Mimura, T.; Shinozaki, Y.; Yoshiuchi, H.; Inaba, T.
    Synthesis and SAR of 2-phenyl-1-sulfonylaminocyclopropane carboxylates as ADAMTS-5 (aggrecanase-2) inhibitors (2009), Bioorg. Med. Chem. Lett., 19, 6213-6217.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
(1R,2R,3S)-1-([[5-(4-chloro-1H-pyrazol-1-yl)thiophen-2-yl]sulfonyl]amino)-2,3-dimethylcyclopropanecarboxylate
-
Homo sapiens
(1R,2S)-1-([(4'-chlorobiphenyl-4-yl)sulfonyl][2-[4-(methoxycarbonyl)-1H-imidazol-1-yl]ethyl]amino)-2-phenylcyclopropanecarboxylate
-
Homo sapiens
(1R,2S)-1-[[(4'-chlorobiphenyl-4-yl)sulfonyl]amino]-2-phenylcyclopropanecarboxylate
-
Homo sapiens
(1S)-1-([[5-(4-chloro-1H-pyrazol-1-yl)thiophen-2-yl]sulfonyl]amino)-2,2-dimethylcyclopropanecarboxylate 0.001 mM, 19.6% inhibition Homo sapiens
(1S,2R)-1-([(4'-chlorobiphenyl-4-yl)sulfonyl][2-[4-(methoxycarbonyl)-1H-imidazol-1-yl]ethyl]amino)-2-phenylcyclopropanecarboxylate 0.0003 mM, 18% inhibition Homo sapiens
(1S,2R)-1-([[5-(2-chlorophenyl)thiophen-2-yl]sulfonyl]amino)-2-phenylcyclopropanecarboxylate 0.001 mM, 48% inhibition Homo sapiens
(1S,2R)-1-([[5-(3-chlorophenyl)thiophen-2-yl]sulfonyl]amino)-2-phenylcyclopropanecarboxylate
-
Homo sapiens
(1S,2R)-1-([[5-(4-chloro-1H-pyrazol-1-yl)thiophen-2-yl]sulfonyl]amino)-2-(propan-2-yl)cyclopropanecarboxylate
-
Homo sapiens
(1S,2R)-1-([[5-(4-chloro-1H-pyrazol-1-yl)thiophen-2-yl]sulfonyl]amino)-2-cyclohexylcyclopropanecarboxylate
-
Homo sapiens
(1S,2R)-1-([[5-(4-chloro-1H-pyrazol-1-yl)thiophen-2-yl]sulfonyl]amino)-2-methyl-2-phenylcyclopropanecarboxylate
-
Homo sapiens
(1S,2R)-1-([[5-(4-chloro-1H-pyrazol-1-yl)thiophen-2-yl]sulfonyl]amino)-2-phenylcyclopropanecarboxylate
-
Homo sapiens
(1S,2R)-1-([[5-(4-chlorophenyl)thiophen-2-yl]sulfonyl]amino)-2-methyl-2-phenylcyclopropanecarboxylate
-
Homo sapiens
(1S,2R)-1-([[5-(4-chlorophenyl)thiophen-2-yl]sulfonyl]amino)-2-phenylcyclopropanecarboxylate
-
Homo sapiens
(1S,2R)-1-([[5-(5-chloropyridin-2-yl)thiophen-2-yl]sulfonyl]amino)-2-phenylcyclopropanecarboxylate
-
Homo sapiens
(1S,2R)-1-[[(4'-chlorobiphenyl-4-yl)sulfonyl]amino]-2-phenylcyclopropanecarboxylate
-
Homo sapiens
(1S,2R,3R)-1-([[5-(4-chloro-1H-pyrazol-1-yl)thiophen-2-yl]sulfonyl]amino)-2-methyl-3-phenylcyclopropanecarboxylate
-
Homo sapiens
(1S,2R,3R)-1-([[5-(4-chlorophenyl)thiophen-2-yl]sulfonyl]amino)-2-methyl-3-phenylcyclopropanecarboxylate
-
Homo sapiens
(1S,2S)-1-([[5-(4-chloro-1H-pyrazol-1-yl)thiophen-2-yl]sulfonyl]amino)-2-methylcyclopropanecarboxylate 0.001 mM, 3.5% inhibition Homo sapiens
(1S,2S)-2-benzyl-1-([[5-(4-chloro-1H-pyrazol-1-yl)thiophen-2-yl]sulfonyl]amino)cyclopropanecarboxylate 0.001 mM, 25% inhibition Homo sapiens
(1S,2S,3R)-1-([[5-(4-chlorophenyl)thiophen-2-yl]sulfonyl]amino)-2-methyl-3-phenylcyclopropanecarboxylate
-
Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Synonyms

Synonyms Comment Organism
ADAMTS-5
-
Homo sapiens
aggrecanase-2
-
Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0000074
-
pH and temperature not specified in the publication Homo sapiens (1S,2R,3R)-1-([[5-(4-chloro-1H-pyrazol-1-yl)thiophen-2-yl]sulfonyl]amino)-2-methyl-3-phenylcyclopropanecarboxylate
0.00001
-
pH and temperature not specified in the publication Homo sapiens (1S,2R)-1-([[5-(4-chlorophenyl)thiophen-2-yl]sulfonyl]amino)-2-methyl-2-phenylcyclopropanecarboxylate
0.000021
-
pH and temperature not specified in the publication Homo sapiens (1S,2R,3R)-1-([[5-(4-chlorophenyl)thiophen-2-yl]sulfonyl]amino)-2-methyl-3-phenylcyclopropanecarboxylate
0.000032
-
pH and temperature not specified in the publication Homo sapiens (1S,2R)-1-([[5-(4-chloro-1H-pyrazol-1-yl)thiophen-2-yl]sulfonyl]amino)-2-methyl-2-phenylcyclopropanecarboxylate
0.00006
-
pH and temperature not specified in the publication Homo sapiens (1S,2R)-1-([[5-(4-chlorophenyl)thiophen-2-yl]sulfonyl]amino)-2-phenylcyclopropanecarboxylate
0.000073
-
pH and temperature not specified in the publication Homo sapiens (1R,2S)-1-([(4'-chlorobiphenyl-4-yl)sulfonyl][2-[4-(methoxycarbonyl)-1H-imidazol-1-yl]ethyl]amino)-2-phenylcyclopropanecarboxylate
0.00008
-
pH and temperature not specified in the publication Homo sapiens (1S,2R)-1-([[5-(4-chloro-1H-pyrazol-1-yl)thiophen-2-yl]sulfonyl]amino)-2-phenylcyclopropanecarboxylate
0.000084
-
pH and temperature not specified in the publication Homo sapiens (1S,2R)-1-[[(4'-chlorobiphenyl-4-yl)sulfonyl]amino]-2-phenylcyclopropanecarboxylate
0.000094
-
pH and temperature not specified in the publication Homo sapiens (1S,2R)-1-([[5-(3-chlorophenyl)thiophen-2-yl]sulfonyl]amino)-2-phenylcyclopropanecarboxylate
0.0001
-
pH and temperature not specified in the publication Homo sapiens (1S,2R)-1-([[5-(5-chloropyridin-2-yl)thiophen-2-yl]sulfonyl]amino)-2-phenylcyclopropanecarboxylate
0.00012
-
pH and temperature not specified in the publication Homo sapiens (1S,2S,3R)-1-([[5-(4-chlorophenyl)thiophen-2-yl]sulfonyl]amino)-2-methyl-3-phenylcyclopropanecarboxylate
0.00021
-
pH and temperature not specified in the publication Homo sapiens (1S,2R)-1-([(4'-chlorobiphenyl-4-yl)sulfonyl][2-[4-(methoxycarbonyl)-1H-imidazol-1-yl]ethyl]amino)-2-phenylcyclopropanecarboxylate
0.00036
-
pH and temperature not specified in the publication Homo sapiens (1S,2R)-1-([[5-(4-chloro-1H-pyrazol-1-yl)thiophen-2-yl]sulfonyl]amino)-2-cyclohexylcyclopropanecarboxylate
0.00077
-
pH and temperature not specified in the publication Homo sapiens (1S,2R)-1-([[5-(4-chloro-1H-pyrazol-1-yl)thiophen-2-yl]sulfonyl]amino)-2-(propan-2-yl)cyclopropanecarboxylate
0.0008
-
pH and temperature not specified in the publication Homo sapiens (1R,2R,3S)-1-([[5-(4-chloro-1H-pyrazol-1-yl)thiophen-2-yl]sulfonyl]amino)-2,3-dimethylcyclopropanecarboxylate