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Assay Detail

CHEMBL4372231

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

Binding
Inhibition of recombinant human proMMP9 using Mca-Lys-Pro-Leu-Gly-Leu-Dap(Dnp)-Ala-Arg-NH2 as substrate preincubated for 3 hrs followed by substrate addition and measured every 10 secs for 15 mins in presence of APMA by fluorometric assay
7
Total Activities
7
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-9 (CHEMBL321)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design, synthesis and biological evaluation of bifunctional inhibitors of membrane type 1 matrix metalloproteinase (MT1-MMP).
Cuffaro D, Nuti E, Gifford V, Ito N, Camodeca C, Tuccinardi T, Nencetti S, Orlandini E, Itoh Y, Rossello A.
Bioorg Med Chem (2019) 27 : 196 -207
PubMed 30522899 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 8.46 9.37

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3617407 1 9.37
CHEMBL4442617 1 8.90
CHEMBL4584813 1 8.68
CHEMBL267178 1 8.32
CHEMBL1090647 1 8.07
CHEMBL4466038 1 8.06
CHEMBL4518217 1 7.85

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3617407 IC50 = 0.43 nM 9.37
CHEMBL4442617 IC50 = 1.25 nM 8.90
CHEMBL4584813 IC50 = 2.1 nM 8.68
CHEMBL267178 IC50 = 4.8 nM 8.32
CHEMBL1090647 IC50 = 8.6 nM 8.07
CHEMBL4466038 IC50 = 8.7 nM 8.06
CHEMBL4518217 IC50 = 14.0 nM 7.85