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Assay Detail

CHEMBL710132

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

Binding
Inhibition of human matrix metalloprotease-3
13
Total Activities
13
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

Design and synthesis of phosphinamide-based hydroxamic acids as inhibitors of matrix metalloproteinases.
Pikul S, McDow Dunham KL, Almstead NG, De B, Natchus MG, Anastasio MV, McPhail SJ, Snider CE, Taiwo YO, Chen L, Dunaway CM, Gu F, Mieling GE.
J Med Chem (1999) 42 : 87 -94
PubMed 9888835 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 6.03 7.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL514138 CGS-27023A 1 7.77
CHEMBL176602 1 7.61
CHEMBL355752 1 7.17
CHEMBL172857 1 6.16
CHEMBL353479 1 6.16
CHEMBL367420 1 5.98
CHEMBL174037 1 5.80
CHEMBL173208 1 5.76
CHEMBL367675 1 5.59
CHEMBL368946 1 5.04
CHEMBL173207 1 4.99
CHEMBL366759 1 4.31
CHEMBL355754 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL514138 CGS-27023A IC50 = 16.9 nM 7.77
CHEMBL176602 IC50 = 24.4 nM 7.61
CHEMBL355752 IC50 = 67.9 nM 7.17
CHEMBL172857 IC50 = 700.0 nM 6.16
CHEMBL353479 IC50 = 700.0 nM 6.16
CHEMBL367420 IC50 = 1040.0 nM 5.98
CHEMBL174037 IC50 = 1600.0 nM 5.80
CHEMBL173208 IC50 = 1750.0 nM 5.76
CHEMBL367675 IC50 = 2550.0 nM 5.59
CHEMBL368946 IC50 = 9170.0 nM 5.04
CHEMBL173207 IC50 = 10300.0 nM 4.99
CHEMBL366759 IC50 = 49300.0 nM 4.31
CHEMBL355754 IC50 = 130500.0 nM -