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Assay Detail

CHEMBL710981

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Binding
Inhibition of matrix metalloprotease-2
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

Picking the S1, S1' and S2' pockets of matrix metalloproteinases. A niche for potent acyclic sulfonamide inhibitors.
Hanessian S, Bouzbouz S, Boudon A, Tucker GC, Peyroulan D.
Bioorg Med Chem Lett (1999) 9 : 1691 -1696
PubMed 10397503 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 8.19 9.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL296911 1 9.15
CHEMBL47728 1 9.15
CHEMBL279785 MARIMASTAT 3.0 1 8.70
CHEMBL296761 1 7.52
CHEMBL45162 1 7.31
CHEMBL45357 1 7.28

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL296911 IC50 = 0.7 nM 9.15
CHEMBL47728 IC50 = 0.7 nM 9.15
CHEMBL279785 MARIMASTAT IC50 = 2.0 nM 8.70
CHEMBL296761 IC50 = 30.0 nM 7.52
CHEMBL45162 IC50 = 49.0 nM 7.31
CHEMBL45357 IC50 = 53.0 nM 7.28