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Assay Detail

CHEMBL714637

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

Binding
Inhibition of matrix metalloprotease-1 (MMP-1)
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

Interstitial collagenase (CHEMBL332)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

The synthesis and biological activity of a novel series of diazepine MMP inhibitors.
Levin JI, DiJoseph JF, Killar LM, Sung A, Walter T, Sharr MA, Roth CE, Skotnicki JS, Albright JD.
Bioorg Med Chem Lett (1998) 8 : 2657 -2662
PubMed 9873598 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 6.78 7.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL514138 CGS-27023A 1 7.82
CHEMBL90978 1 7.66
CHEMBL327621 1 7.35
CHEMBL539787 1 7.04
CHEMBL327442 1 6.94
CHEMBL329558 1 6.89
CHEMBL328255 1 6.60
CHEMBL310649 1 6.51
CHEMBL313168 1 6.51
CHEMBL419868 1 6.35
CHEMBL310655 1 6.21
CHEMBL88559 1 6.16
CHEMBL538028 1 6.15

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL514138 CGS-27023A IC50 = 15.0 nM 7.82
CHEMBL90978 IC50 = 22.0 nM 7.66
CHEMBL327621 IC50 = 45.0 nM 7.35
CHEMBL539787 IC50 = 91.0 nM 7.04
CHEMBL327442 IC50 = 116.0 nM 6.94
CHEMBL329558 IC50 = 128.0 nM 6.89
CHEMBL328255 IC50 = 251.0 nM 6.60
CHEMBL310649 IC50 = 312.0 nM 6.51
CHEMBL313168 IC50 = 309.0 nM 6.51
CHEMBL419868 IC50 = 445.0 nM 6.35
CHEMBL310655 IC50 = 618.0 nM 6.21
CHEMBL88559 IC50 = 690.0 nM 6.16
CHEMBL538028 IC50 = 703.0 nM 6.15