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Assay Detail

CHEMBL1799651

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

Binding
Inhibition of human MMP9 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

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

Publication

Synthesis and biological evaluation in U87MG glioma cells of (ethynylthiophene)sulfonamido-based hydroxamates as matrix metalloproteinase inhibitors.
Nuti E, Casalini F, Santamaria S, Gabelloni P, Bendinelli S, Da Pozzo E, Costa B, Marinelli L, La Pietra V, Novellino E, Margarida Bernardo M, Fridman R, Da Settimo F, Martini C, Rossello A.
Eur J Med Chem (2011) 46 : 2617 -2629
PubMed 21514700 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 7.41 8.37

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1795862 1 8.37
CHEMBL514138 CGS-27023A 1 8.32
CHEMBL1795861 1 7.68
CHEMBL1795858 1 7.30
CHEMBL1795857 1 7.20
CHEMBL1795859 1 7.11
CHEMBL1795351 1 7.10
CHEMBL1795860 1 6.19

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1795862 IC50 = 4.3 nM 8.37
CHEMBL514138 CGS-27023A IC50 = 4.8 nM 8.32
CHEMBL1795861 IC50 = 21.0 nM 7.68
CHEMBL1795858 IC50 = 50.0 nM 7.30
CHEMBL1795857 IC50 = 63.0 nM 7.20
CHEMBL1795859 IC50 = 77.0 nM 7.11
CHEMBL1795351 IC50 = 79.0 nM 7.10
CHEMBL1795860 IC50 = 650.0 nM 6.19