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Assay Detail

CHEMBL3428744

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

Binding
Inhibition of ovine COX-1 assessed as inhibition of PGH2 production using arachidonic acid as substrate by TMPD oxidation based colorimetric assay
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Ovis aries
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Prostaglandin G/H synthase 1 (CHEMBL2949)
Type SINGLE PROTEIN
Organism Ovis aries

Publication

General role of the amino and methylsulfamoyl groups in selective cyclooxygenase(COX)-1 inhibition by 1,4-diaryl-1,2,3-triazoles and validation of a predictive pharmacometric PLS model.
Perrone MG, Vitale P, Panella A, Fortuna CG, Scilimati A.
Eur J Med Chem (2015) 94 : 252 -264
PubMed 25768707 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 5.66 8.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL259972 MOFEZOLAC 4.0 1 8.85
CHEMBL26915 SC-560 1 8.15
CHEMBL3114664 1 5.96
CHEMBL3427198 1 5.52
CHEMBL3427204 1 5.47
CHEMBL3114671 1 5.40
CHEMBL3427197 1 4.82
CHEMBL3427202 1 4.64
CHEMBL3114659 1 4.57
CHEMBL3114661 1 4.52
CHEMBL363228 1 4.41

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL259972 MOFEZOLAC IC50 = 1.4 nM 8.85
CHEMBL26915 SC-560 IC50 = 7.0 nM 8.15
CHEMBL3114664 IC50 = 1100.0 nM 5.96
CHEMBL3427198 IC50 = 3000.0 nM 5.52
CHEMBL3427204 IC50 = 3400.0 nM 5.47
CHEMBL3114671 IC50 = 4000.0 nM 5.40
CHEMBL3427197 IC50 = 15000.0 nM 4.82
CHEMBL3427202 IC50 = 23000.0 nM 4.64
CHEMBL3114659 IC50 = 27000.0 nM 4.57
CHEMBL3114661 IC50 = 30000.0 nM 4.52
CHEMBL363228 IC50 = 39000.0 nM 4.41