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Assay Detail

CHEMBL2050091

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

Binding
Inhibition of human recombinant MMP13 using MCA-Pro-Cha-Gly-Nva-His-Ala-Dpa-NH2 as substrate preincubated for 10 mins measured by fluorescence analysis
2
Total Activities
2
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

Discovery and evaluation of a non-Zn chelating, selective matrix metalloproteinase 13 (MMP-13) inhibitor for potential intra-articular treatment of osteoarthritis.
Gege C, Bao B, Bluhm H, Boer J, Gallagher BM, Korniski B, Powers TS, Steeneck C, Taveras AG, Baragi VM.
J Med Chem (2012) 55 : 709 -716
PubMed 22175799 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 9.71 10.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2047536 1 10.52
CHEMBL2047537 1 8.89

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2047536 IC50 = 0.03 nM 10.52
CHEMBL2047537 IC50 = 1.3 nM 8.89