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Assay Detail

CHEMBL715839

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Binding
Inhibitory activity against human Matrix metalloprotease-2
19
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

72 kDa type IV collagenase (CHEMBL333)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

alpha-Alkyl-alpha-amino-beta-sulphone hydroxamates as potent MMP inhibitors that spare MMP-1.
Becker DP, DeCrescenzo G, Freskos J, Getman DP, Hockerman SL, Li M, Mehta P, Munie GE, Swearingen C.
Bioorg Med Chem Lett (2001) 11 : 2723 -2725
PubMed 11591510 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 19 8.55 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL94248 1 9.70
CHEMBL92899 3 9.70
CHEMBL93231 1 9.70
CHEMBL91124 1 9.70
CHEMBL92778 1 9.40
CHEMBL92923 1 9.30
CHEMBL91434 1 9.22
CHEMBL279785 MARIMASTAT 3.0 1 9.12
CHEMBL433171 1 8.89
CHEMBL90211 1 8.89
CHEMBL90762 1 8.49
CHEMBL514138 CGS-27023A 1 8.34
CHEMBL328346 1 8.30
CHEMBL92327 1 7.40
CHEMBL90487 1 7.10
CHEMBL419315 1 6.74
CHEMBL329659 1 6.27

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL94248 IC50 = 0.2 nM 9.70
CHEMBL93231 IC50 = 0.2 nM 9.70
CHEMBL92899 IC50 = 0.2 nM 9.70
CHEMBL91124 IC50 = 0.2 nM 9.70
CHEMBL92778 IC50 = 0.4 nM 9.40
CHEMBL92923 IC50 = 0.5 nM 9.30
CHEMBL91434 IC50 = 0.6 nM 9.22
CHEMBL279785 MARIMASTAT IC50 = 0.75 nM 9.12
CHEMBL90211 IC50 = 1.3 nM 8.89
CHEMBL433171 IC50 = 1.3 nM 8.89
CHEMBL90762 IC50 = 3.2 nM 8.49
CHEMBL514138 CGS-27023A IC50 = 4.6 nM 8.34
CHEMBL328346 IC50 = 5.0 nM 8.30
CHEMBL92899 IC50 = 19.3 nM 7.71
CHEMBL92327 IC50 = 40.0 nM 7.40
CHEMBL90487 IC50 = 80.0 nM 7.10
CHEMBL419315 IC50 = 184.0 nM 6.74
CHEMBL329659 IC50 = 540.0 nM 6.27
CHEMBL92899 IC50 < 0.1 nM -