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Assay Detail

CHEMBL715006

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

Binding
Inhibition of gelatinase-A (Matrix metalloprotease-2)
2
Total Activities
2
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

72 kDa type IV collagenase (CHEMBL333)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design, synthesis, and biological evaluation of potent thiazine- and thiazepine-based matrix metalloproteinase inhibitors.
Almstead NG, Bradley RS, Pikul S, De B, Natchus MG, Taiwo YO, Gu F, Williams LE, Hynd BA, Janusz MJ, Dunaway CM, Mieling GE.
J Med Chem (1999) 42 : 4547 -4562
PubMed 10579818 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 2 8.89 10.08

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL75094 PRINOMASTAT 3.0 1 10.08
CHEMBL514138 CGS-27023A 1 7.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL75094 PRINOMASTAT Ki = 0.083 nM 10.08
CHEMBL514138 CGS-27023A Ki = 20.0 nM 7.70