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Assay Detail

CHEMBL829406

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

Binding
Inhibition of human matrix metalloprotease-3
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

Stromelysin-1 (CHEMBL283)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

N-i-Propoxy-N-biphenylsulfonylaminobutylhydroxamic acids as potent and selective inhibitors of MMP-2 and MT1-MMP.
Rossello A, Nuti E, Carelli P, Orlandini E, Macchia M, Nencetti S, Zandomeneghi M, Balzano F, Uccello Barretta G, Albini A, Benelli R, Cercignani G, Murphy G, Balsamo A.
Bioorg Med Chem Lett (2005) 15 : 1321 -1326
PubMed 15713379 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 7.37 9.64

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL75094 PRINOMASTAT 3.0 1 9.64
CHEMBL514138 CGS-27023A 1 7.66
CHEMBL179288 1 7.30
CHEMBL362651 1 6.89
CHEMBL181244 1 5.35

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL75094 PRINOMASTAT IC50 = 0.23 nM 9.64
CHEMBL514138 CGS-27023A IC50 = 22.0 nM 7.66
CHEMBL179288 IC50 = 50.0 nM 7.30
CHEMBL362651 IC50 = 130.0 nM 6.89
CHEMBL181244 IC50 = 4500.0 nM 5.35