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Assay Detail

CHEMBL715847

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

Binding
50 percent inhibition of human Matrix metalloprotease-2 by the cleavage of fluorogenic peptide MCA-Pro-Leu-Gly-Leu-Dpa-ala-Arg-NH2
13
Total Activities
13
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

Synthesis and activity of selective MMP inhibitors with an aryl backbone.
Barta TE, Becker DP, Bedell LJ, De Crescenzo GA, McDonald JJ, Munie GE, Rao S, Shieh HS, Stegeman R, Stevens AM, Villamil CI.
Bioorg Med Chem Lett (2000) 10 : 2815 -2817
PubMed 11133099 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 7.57 9.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL75094 PRINOMASTAT 3.0 1 9.52
CHEMBL440498 CTS-1027 2.0 1 9.40
CHEMBL279785 MARIMASTAT 3.0 1 9.12
CHEMBL83209 1 8.89
CHEMBL310008 1 8.70
CHEMBL309465 1 8.48
CHEMBL94467 1 7.46
CHEMBL94872 1 7.16
CHEMBL319055 1 6.83
CHEMBL433415 1 6.00
CHEMBL330078 1 5.75
CHEMBL97478 1 5.64
CHEMBL94324 1 5.46

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL75094 PRINOMASTAT IC50 = 0.3 nM 9.52
CHEMBL440498 CTS-1027 IC50 = 0.4 nM 9.40
CHEMBL279785 MARIMASTAT IC50 = 0.75 nM 9.12
CHEMBL83209 IC50 = 1.3 nM 8.89
CHEMBL310008 IC50 = 2.0 nM 8.70
CHEMBL309465 IC50 = 3.3 nM 8.48
CHEMBL94467 IC50 = 35.0 nM 7.46
CHEMBL94872 IC50 = 70.0 nM 7.16
CHEMBL319055 IC50 = 148.0 nM 6.83
CHEMBL433415 IC50 = 1000.0 nM 6.00
CHEMBL330078 IC50 = 1800.0 nM 5.75
CHEMBL97478 IC50 = 2300.0 nM 5.64
CHEMBL94324 IC50 = 3500.0 nM 5.46