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Assay Detail

CHEMBL714722

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

Binding
In vitro inhibition of 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

The discovery of anthranilic acid-based MMP inhibitors. Part 2: SAR of the 5-position and P1(1) groups.
Levin JI, Chen J, Du M, Hogan M, Kincaid S, Nelson FC, Venkatesan AM, Wehr T, Zask A, DiJoseph J, Killar LM, Skala S, Sung A, Sharr M, Roth C, Jin G, Cowling R, Mohler KM, Black RA, March CJ, Skotnicki JS.
Bioorg Med Chem Lett (2001) 11 : 2189 -2192
PubMed 11514167 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 18 6.49 7.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL514138 CGS-27023A 1 7.82
CHEMBL69268 1 7.75
CHEMBL419995 1 7.13
CHEMBL68271 1 6.99
CHEMBL71725 1 6.91
CHEMBL307079 1 6.88
CHEMBL70176 1 6.84
CHEMBL303666 1 6.71
CHEMBL70957 1 6.54
CHEMBL68196 1 6.42
CHEMBL304730 1 6.27
CHEMBL71007 1 6.13
CHEMBL68542 1 6.13
CHEMBL71309 1 5.98
CHEMBL71686 1 5.88
CHEMBL71645 1 5.64
CHEMBL68212 1 5.49
CHEMBL71436 1 5.33

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL514138 CGS-27023A IC50 = 15.0 nM 7.82
CHEMBL69268 IC50 = 18.0 nM 7.75
CHEMBL419995 IC50 = 74.0 nM 7.13
CHEMBL68271 IC50 = 103.0 nM 6.99
CHEMBL71725 IC50 = 124.0 nM 6.91
CHEMBL307079 IC50 = 132.0 nM 6.88
CHEMBL70176 IC50 = 143.0 nM 6.84
CHEMBL303666 IC50 = 195.0 nM 6.71
CHEMBL70957 IC50 = 291.0 nM 6.54
CHEMBL68196 IC50 = 376.0 nM 6.42
CHEMBL304730 IC50 = 542.0 nM 6.27
CHEMBL71007 IC50 = 747.0 nM 6.13
CHEMBL68542 IC50 = 745.0 nM 6.13
CHEMBL71309 IC50 = 1050.0 nM 5.98
CHEMBL71686 IC50 = 1314.0 nM 5.88
CHEMBL71645 IC50 = 2268.0 nM 5.64
CHEMBL68212 IC50 = 3245.0 nM 5.49
CHEMBL71436 IC50 = 4640.0 nM 5.33