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Assay Detail

CHEMBL3620107

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

Binding
Inhibition of recombinant human activated-MMP13 using Mca-Lys-Pro-Leu-Gly-Leu-Dap(Dnp)-Ala-Arg-NH2 as fluorogenic substrate incubated for 4 hrs followed by substrate addition measured every 10 secs for 20 mins by fluorometric 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

Collagenase 3 (CHEMBL280)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

N-O-Isopropyl Sulfonamido-Based Hydroxamates as Matrix Metalloproteinase Inhibitors: Hit Selection and in Vivo Antiangiogenic Activity.
Nuti E, Cantelmo AR, Gallo C, Bruno A, Bassani B, Camodeca C, Tuccinardi T, Vera L, Orlandini E, Nencetti S, Stura EA, Martinelli A, Dive V, Albini A, Rossello A.
J Med Chem (2015) 58 : 7224 -7240
PubMed 26263024 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 8.67 9.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3617407 1 9.72
CHEMBL3617405 1 9.60
CHEMBL3617404 1 9.24
CHEMBL3617402 1 9.17
CHEMBL3617403 1 8.85
CHEMBL3617401 1 8.66
CHEMBL3617400 1 8.34
CHEMBL3617406 1 5.75

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3617407 IC50 = 0.19 nM 9.72
CHEMBL3617405 IC50 = 0.25 nM 9.60
CHEMBL3617404 IC50 = 0.58 nM 9.24
CHEMBL3617402 IC50 = 0.68 nM 9.17
CHEMBL3617403 IC50 = 1.4 nM 8.85
CHEMBL3617401 IC50 = 2.2 nM 8.66
CHEMBL3617400 IC50 = 4.6 nM 8.34
CHEMBL3617406 IC50 = 1800.0 nM 5.75