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Assay Detail

CHEMBL4189737

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

Binding
Inhibition of recombinant human MMP-14 catalytic domain using Mca-Lys-Pro-Leu-Gly-Leu-Dap(Dnp)-Ala-Arg-NH2 as substrate preincubated for 3 hrs followed by substrate addition measured every 10 secs for 15 mins by fluorometric assay
4
Total Activities
4
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

Matrix metalloproteinase-14 (CHEMBL3869)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Development of Thioaryl-Based Matrix Metalloproteinase-12 Inhibitors with Alternative Zinc-Binding Groups: Synthesis, Potentiometric, NMR, and Crystallographic Studies.
Nuti E, Cuffaro D, Bernardini E, Camodeca C, Panelli L, Chaves S, Ciccone L, Tepshi L, Vera L, Orlandini E, Nencetti S, Stura EA, Santos MA, Dive V, Rossello A.
J Med Chem (2018) 61 : 4421 -4435
PubMed 29727184 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 5.41 6.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL584365 1 6.15
CHEMBL4210206 1 5.70
CHEMBL4214626 1 5.40
CHEMBL4203044 1 4.40

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL584365 IC50 = 710.0 nM 6.15
CHEMBL4210206 IC50 = 2000.0 nM 5.70
CHEMBL4214626 IC50 = 4000.0 nM 5.40
CHEMBL4203044 IC50 = 40000.0 nM 4.40