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Assay Detail

CHEMBL816917

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

Binding
Inhibition of MMP13-mediated collagen degradation by SDS-PAGE
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Intermediate

Target

Collagenase 3 (CHEMBL280)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

N-O-isopropyl sulfonamido-based hydroxamates: design, synthesis and biological evaluation of selective matrix metalloproteinase-13 inhibitors as potential therapeutic agents for osteoarthritis.
Nuti E, Casalini F, Avramova SI, Santamaria S, Cercignani G, Marinelli L, La Pietra V, Novellino E, Orlandini E, Nencetti S, Tuccinardi T, Martinelli A, Lim NH, Visse R, Nagase H, Rossello A.
J Med Chem (2009) 52 : 4757 -4773
PubMed 19606871 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 8.28 8.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL550548 1 8.85
CHEMBL550148 1 8.62
CHEMBL561625 1 8.03
CHEMBL181244 1 7.60

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL550548 IC50 = 1.4 nM 8.85
CHEMBL550148 IC50 = 2.4 nM 8.62
CHEMBL561625 IC50 = 9.4 nM 8.03
CHEMBL181244 IC50 = 25.0 nM 7.60