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Assay Detail

CHEMBL4425565

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 measured after 2 to 4 hrs by fluorescence analysis
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

Use of Osmotic Pumps to Establish the Pharmacokinetic-Pharmacodynamic Relationship and Define Desirable Human Performance Characteristics for Aggrecanase Inhibitors.
Wiley MR, Durham TB, Adams LA, Chambers MG, Lin C, Liu C, Marimuthu J, Mitchell PG, Mudra DR, Swearingen CA, Toth JL, Weller JM, Thirunavukkarasu K.
J Med Chem (2016) 59 : 5810 -5822
PubMed 27194201 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 4.51 5.12

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4097165 1 5.12
CHEMBL3358155 1 5.06
CHEMBL4587825 1 4.58
CHEMBL4589438 1 4.47
CHEMBL3358156 1 4.43
CHEMBL4436740 1 4.24
CHEMBL4450729 1 4.11
CHEMBL3358158 1 4.07

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4097165 IC50 = 7600.0 nM 5.12
CHEMBL3358155 IC50 = 8700.0 nM 5.06
CHEMBL4587825 IC50 = 26000.0 nM 4.58
CHEMBL4589438 IC50 = 34000.0 nM 4.47
CHEMBL3358156 IC50 = 37000.0 nM 4.43
CHEMBL4436740 IC50 = 57000.0 nM 4.24
CHEMBL4450729 IC50 = 78000.0 nM 4.11
CHEMBL3358158 IC50 = 86000.0 nM 4.07