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Assay Detail

CHEMBL768833

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Binding
Inhibitory concentration was measured against Prostaglandin G/H synthase 1 in human whole blood
9
Total Activities
9
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 1 (CHEMBL221)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

3,4-Diaryl-5-hydroxyfuranones: highly selective inhibitors of cyclooxygenase-2 with aqueous solubility.
Black WC, Brideau C, Chan CC, Charleson S, Cromlish W, Gordon R, Grimm EL, Hughes G, Leger S, Li CS, Riendeau D, Thérien M, Wang Z, Xu LJ, Prasit P.
Bioorg Med Chem Lett (2003) 13 : 1195 -1198
PubMed 12643942 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 4.54 5.20

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL118 CELECOXIB 4.0 1 5.20
CHEMBL122 ROFECOXIB 4.0 1 4.72
CHEMBL277118 1 4.42
CHEMBL18498 1 4.24
CHEMBL18251 1 4.12
CHEMBL416363 1 -
CHEMBL18316 1 -
CHEMBL18867 1 -
CHEMBL273815 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL118 CELECOXIB IC50 = 6300.0 nM 5.20
CHEMBL122 ROFECOXIB IC50 = 19000.0 nM 4.72
CHEMBL277118 IC50 = 38000.0 nM 4.42
CHEMBL18498 IC50 = 57000.0 nM 4.24
CHEMBL18251 IC50 = 75000.0 nM 4.12
CHEMBL416363 IC50 > 90000.0 nM -
CHEMBL18316 IC50 > 90000.0 nM -
CHEMBL18867 IC50 > 100000.0 nM -
CHEMBL273815 IC50 > 100000.0 nM -