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Assay Detail

CHEMBL4013271

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

Binding
Inhibition of human MMP14 using Mca-PQGL-(3-[2, 4-dinitrophenyl]-L-2, 3-diaminopropionyl)-AR-OH as substrate after 2 to 4 hrs by fluorescence assay
8
Total Activities
8
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

A Highly Selective Hydantoin Inhibitor of Aggrecanase-1 and Aggrecanase-2 with a Low Projected Human Dose.
Durham TB, Marimuthu J, Toth JL, Liu C, Adams L, Mudra DR, Swearingen C, Lin C, Chambers MG, Thirunavukkarasu K, Wiley MR.
J Med Chem (2017) 60 : 5933 -5939
PubMed 28613895 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 5.39 6.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL187092 1 6.82
CHEMBL4094455 1 5.80
CHEMBL4102193 1 5.47
CHEMBL4066965 1 5.41
CHEMBL4072836 1 5.10
CHEMBL3972836 1 4.82
CHEMBL3980860 1 4.30
CHEMBL3955404 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL187092 IC50 = 150.0 nM 6.82
CHEMBL4094455 IC50 = 1600.0 nM 5.80
CHEMBL4102193 IC50 = 3400.0 nM 5.47
CHEMBL4066965 IC50 = 3900.0 nM 5.41
CHEMBL4072836 IC50 = 8000.0 nM 5.10
CHEMBL3972836 IC50 = 15000.0 nM 4.82
CHEMBL3980860 IC50 = 50000.0 nM 4.30
CHEMBL3955404 IC50 > 100000.0 nM -