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Assay Detail

CHEMBL4000933

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

ADMET
Inhibition of APMA-activated recombinant human MMP-9 using Cy3-PLGLK(Cy5Q)AR-NH2 peptide as substrate measured after 40 mins by spectrofluorimetric method
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type ADMET
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Matrix metalloproteinase-9 (CHEMBL321)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of Novel, Highly Potent, and Selective Matrix Metalloproteinase (MMP)-13 Inhibitors with a 1,2,4-Triazol-3-yl Moiety as a Zinc Binding Group Using a Structure-Based Design Approach.
Nara H, Kaieda A, Sato K, Naito T, Mototani H, Oki H, Yamamoto Y, Kuno H, Santou T, Kanzaki N, Terauchi J, Uchikawa O, Kori M.
J Med Chem (2017) 60 : 608 -626
PubMed 27966948 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 7.81 9.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL440498 CTS-1027 2.0 1 9.96
CHEMBL1511860 1 5.66
CHEMBL3337869 1 -
CHEMBL4068176 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL440498 CTS-1027 IC50 = 0.11 nM 9.96
CHEMBL1511860 IC50 = 2200.0 nM 5.66
CHEMBL3337869 IC50 > 10000.0 nM -
CHEMBL4068176 IC50 > 10000.0 nM -