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Assay Detail

CHEMBL713990

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Binding
Inhibition of Matrix metalloprotease-1
12
Total Activities
12
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

Interstitial collagenase (CHEMBL332)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

General synthesis of alpha-substituted 3-bisaryloxy propionic acid derivatives as specific MMP inhibitors.
Chollet AM, Le Diguarher T, Murray L, Bertrand M, Tucker GC, Sabatini M, Pierré A, Atassi G, Bonnet J, Casara P.
Bioorg Med Chem Lett (2001) 11 : 295 -299
PubMed 11212095 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 6.80 8.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL279785 MARIMASTAT 3.0 1 8.82
CHEMBL323371 1 7.51
CHEMBL75094 PRINOMASTAT 3.0 1 7.32
CHEMBL317132 1 7.13
CHEMBL317508 1 6.94
CHEMBL101121 1 6.12
CHEMBL100805 1 5.54
CHEMBL100584 1 5.02
CHEMBL103442 1 -
CHEMBL318795 1 -
CHEMBL38851 1 -
CHEMBL102459 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL279785 MARIMASTAT IC50 = 1.5 nM 8.82
CHEMBL323371 IC50 = 31.0 nM 7.51
CHEMBL75094 PRINOMASTAT IC50 = 48.0 nM 7.32
CHEMBL317132 IC50 = 74.0 nM 7.13
CHEMBL317508 IC50 = 116.0 nM 6.94
CHEMBL101121 IC50 = 768.0 nM 6.12
CHEMBL100805 IC50 = 2850.0 nM 5.54
CHEMBL100584 IC50 = 9500.0 nM 5.02
CHEMBL103442 IC50 > 100000.0 nM -
CHEMBL318795 IC50 > 1000.0 nM -
CHEMBL38851 IC50 > 10.0 nM -
CHEMBL102459 IC50 > 10000.0 nM -