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Assay Detail

CHEMBL664077

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Binding
In vivo ability to inhibit cyclooxygenase-2 enzyme in human whole blood was determined
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Blood
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Prostaglandin G/H synthase 2 (CHEMBL230)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and biological evaluation of 5,6-diarylimidazo[2.1-b]thiazole as selective COX-2 inhibitors
Therien M, Brideau C, Chan CC, Cromlish WA, Gauthier JY, Gordon R, Greig G, Kargman S, Lau CK, Leblanc Y, Li C, O'Neill GP, Riendeau D, Roy P, Wang Z, Xu L, Prasit P
Bioorg Med Chem Lett (1997) 7 : 47 -52
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 5.72 6.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL148976 1 6.40
CHEMBL146742 1 6.05
CHEMBL423576 1 5.66
CHEMBL358609 1 4.76

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL148976 IC50 = 400.0 nM 6.40
CHEMBL146742 IC50 = 900.0 nM 6.05
CHEMBL423576 IC50 = 2200.0 nM 5.66
CHEMBL358609 IC50 = 17500.0 nM 4.76