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Assay Detail

CHEMBL715380

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Inhibitory activity against MMP-1 (Matrix metalloprotease-1)
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Interstitial collagenase (CHEMBL332)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

New alpha-substituted succinate-based hydroxamic acids as TNFalpha convertase inhibitors.
Barlaam B, Bird TG, Lambert-Van Der Brempt C, Campbell D, Foster SJ, Maciewicz R.
J Med Chem (1999) 42 : 4890 -4908
PubMed 10579851 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 18 8.33 9.06

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL144611 1 9.06
CHEMBL144843 1 8.96
CHEMBL344759 1 8.92
CHEMBL342100 1 8.89
CHEMBL344060 1 8.82
CHEMBL439983 1 8.77
CHEMBL144525 1 8.66
CHEMBL144568 1 8.66
CHEMBL342732 1 8.62
CHEMBL144293 1 8.59
CHEMBL147051 1 8.55
CHEMBL29976 1 8.40
CHEMBL279785 MARIMASTAT 3.0 1 8.30
CHEMBL75094 PRINOMASTAT 3.0 1 8.09
CHEMBL16520 RO-319790 1 8.00
CHEMBL432079 1 8.00
CHEMBL358962 1 6.48
CHEMBL148331 1 6.14

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL144611 IC50 = 0.88 nM 9.06
CHEMBL144843 IC50 = 1.1 nM 8.96
CHEMBL344759 IC50 = 1.2 nM 8.92
CHEMBL342100 IC50 = 1.3 nM 8.89
CHEMBL344060 IC50 = 1.5 nM 8.82
CHEMBL439983 IC50 = 1.7 nM 8.77
CHEMBL144525 IC50 = 2.2 nM 8.66
CHEMBL144568 IC50 = 2.2 nM 8.66
CHEMBL342732 IC50 = 2.4 nM 8.62
CHEMBL144293 IC50 = 2.6 nM 8.59
CHEMBL147051 IC50 = 2.8 nM 8.55
CHEMBL29976 IC50 = 4.0 nM 8.40
CHEMBL279785 MARIMASTAT IC50 = 5.0 nM 8.30
CHEMBL75094 PRINOMASTAT IC50 = 8.2 nM 8.09
CHEMBL16520 RO-319790 IC50 = 10.0 nM 8.00
CHEMBL432079 IC50 = 10.0 nM 8.00
CHEMBL358962 IC50 = 330.0 nM 6.48
CHEMBL148331 IC50 = 730.0 nM 6.14