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Assay Detail

CHEMBL717023

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

Binding
Inhibition of Matrix metalloprotease-13 (MMP-13) in fluorimetric assay
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Collagenase 3 (CHEMBL280)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Phenoxyphenyl sulfone N-formylhydroxylamines (retrohydroxamates) as potent, selective, orally bioavailable matrix metalloproteinase inhibitors.
Wada CK, Holms JH, Curtin ML, Dai Y, Florjancic AS, Garland RB, Guo Y, Heyman HR, Stacey JR, Steinman DH, Albert DH, Bouska JJ, Elmore IN, Goodfellow CL, Marcotte PA, Tapang P, Morgan DW, Michaelides MR, Davidsen SK.
J Med Chem (2002) 45 : 219 -232
PubMed 11754593 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 9.03 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL75094 PRINOMASTAT 3.0 1 9.70
CHEMBL279785 MARIMASTAT 3.0 1 8.92
CHEMBL2115165 1 8.48

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL75094 PRINOMASTAT IC50 = 0.2 nM 9.70
CHEMBL279785 MARIMASTAT IC50 = 1.2 nM 8.92
CHEMBL2115165 IC50 = 3.3 nM 8.48