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Assay Detail

CHEMBL718136

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

Binding
50% inhibition of human recombinant Matrilysin
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Matrilysin (CHEMBL4073)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Inhibition of Matrix Metalloproteinases: An examination of the S1 pocket
Miller A, Askew M, Beckett R, Bellamy CL, Bone EA, Coates RE, Davidson AH, Drummond AH, Huxley P, Martin FM, Saroglou L, Thompson AJ, van Dijk SE, Whittaker M
Bioorg Med Chem Lett (1997) 7 : 193 -198
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 6.09 8.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL279786 BATIMASTAT 2.0 1 8.22
CHEMBL279785 MARIMASTAT 3.0 1 7.70
CHEMBL264495 1 7.70
CHEMBL291994 1 6.30
CHEMBL292313 1 6.30
CHEMBL294066 1 6.00
CHEMBL58945 1 5.70
CHEMBL60546 1 5.70
CHEMBL303756 1 5.70
CHEMBL62245 1 5.70
CHEMBL62056 1 5.52
CHEMBL59248 1 5.30
CHEMBL293382 1 5.00
CHEMBL418472 1 4.40

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL279786 BATIMASTAT IC50 = 6.0 nM 8.22
CHEMBL279785 MARIMASTAT IC50 = 20.0 nM 7.70
CHEMBL264495 IC50 = 20.0 nM 7.70
CHEMBL291994 IC50 = 500.0 nM 6.30
CHEMBL292313 IC50 = 500.0 nM 6.30
CHEMBL294066 IC50 = 1000.0 nM 6.00
CHEMBL58945 IC50 = 2000.0 nM 5.70
CHEMBL60546 IC50 = 2000.0 nM 5.70
CHEMBL303756 IC50 = 2000.0 nM 5.70
CHEMBL62245 IC50 = 2000.0 nM 5.70
CHEMBL62056 IC50 = 3000.0 nM 5.52
CHEMBL59248 IC50 = 5000.0 nM 5.30
CHEMBL293382 IC50 = 10000.0 nM 5.00
CHEMBL418472 IC50 = 40000.0 nM 4.40