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Assay Detail

CHEMBL719138

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Binding
Inhibitory activity against Matrix metalloprotease-13
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

Collagenase 3 (CHEMBL280)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

The discovery of anthranilic acid-based MMP inhibitors. Part 1: SAR of the 3-position.
Levin JI, Du MT, DiJoseph JF, Killar LM, Sung A, Walter T, Sharr MA, Roth CE, Moy FJ, Powers R, Jin G, Cowling R, Skotnicki JS.
Bioorg Med Chem Lett (2001) 11 : 235 -238
PubMed 11206467 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 7.22 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL80272 1 9.00
CHEMBL76974 1 8.40
CHEMBL80300 1 8.22
CHEMBL514138 CGS-27023A 1 8.10
CHEMBL70176 1 8.10
CHEMBL311368 1 7.38
CHEMBL76606 1 7.30
CHEMBL308084 1 6.87
CHEMBL311509 1 6.86
CHEMBL80894 1 6.28
CHEMBL308305 1 6.26
CHEMBL77237 1 6.14
CHEMBL80322 1 6.14
CHEMBL311768 1 6.01

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL80272 IC50 = 1.0 nM 9.00
CHEMBL76974 IC50 = 4.0 nM 8.40
CHEMBL80300 IC50 = 6.0 nM 8.22
CHEMBL514138 CGS-27023A IC50 = 8.0 nM 8.10
CHEMBL70176 IC50 = 8.0 nM 8.10
CHEMBL311368 IC50 = 42.0 nM 7.38
CHEMBL76606 IC50 = 50.0 nM 7.30
CHEMBL308084 IC50 = 136.0 nM 6.87
CHEMBL311509 IC50 = 138.0 nM 6.86
CHEMBL80894 IC50 = 531.0 nM 6.28
CHEMBL308305 IC50 = 555.0 nM 6.26
CHEMBL77237 IC50 = 717.0 nM 6.14
CHEMBL80322 IC50 = 728.0 nM 6.14
CHEMBL311768 IC50 = 982.0 nM 6.01