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Assay Detail

CHEMBL3387083

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

Binding
Non-competitive inhibition of full-length recombinant human MMP-13 assessed as fTHP-15 substrate hydrolysis
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Collagenase 3 (CHEMBL280)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Characterization of selective exosite-binding inhibitors of matrix metalloproteinase 13 that prevent articular cartilage degradation in vitro.
Spicer TP, Jiang J, Taylor AB, Choi JY, Hart PJ, Roush WR, Fields GB, Hodder PS, Minond D.
J Med Chem (2014) 57 : 9598 -9611
PubMed 25330343 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 6.29 7.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL496942 1 7.85
CHEMBL514794 1 6.96
CHEMBL1371684 1 5.62
CHEMBL1515648 1 5.55
CHEMBL473326 1 5.47
CHEMBL734 ACETOHYDROXAMIC ACID 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL496942 IC50 = 14.0 nM 7.85
CHEMBL514794 IC50 = 110.0 nM 6.96
CHEMBL1371684 IC50 = 2400.0 nM 5.62
CHEMBL1515648 IC50 = 2800.0 nM 5.55
CHEMBL473326 IC50 = 3400.0 nM 5.47
CHEMBL734 ACETOHYDROXAMIC ACID IC50 - -