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Assay Detail

CHEMBL768834

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Binding
Inhibitory concentration was measured against Prostaglandin G/H synthase 1 in the sensitive U937 microsome assay
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

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 24 5.19 7.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL118 CELECOXIB 4.0 1 7.30
CHEMBL122 ROFECOXIB 4.0 1 5.77
CHEMBL18089 1 5.52
CHEMBL277118 1 5.16
CHEMBL278231 1 5.00
CHEMBL18498 1 4.85
CHEMBL18312 1 4.52
CHEMBL18251 1 4.46
CHEMBL279268 1 4.09
CHEMBL278738 1 -
CHEMBL19056 1 -
CHEMBL18377 1 -
CHEMBL277519 1 -
CHEMBL18790 1 -
CHEMBL416363 1 -
CHEMBL275664 1 -
CHEMBL273340 1 -
CHEMBL18316 1 -
CHEMBL18867 1 -
CHEMBL273815 1 -
CHEMBL18796 1 -
CHEMBL18254 1 -
CHEMBL275650 1 -
CHEMBL280009 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL118 CELECOXIB IC50 = 50.0 nM 7.30
CHEMBL122 ROFECOXIB IC50 = 1700.0 nM 5.77
CHEMBL18089 IC50 = 3000.0 nM 5.52
CHEMBL277118 IC50 = 7000.0 nM 5.16
CHEMBL278231 IC50 = 10000.0 nM 5.00
CHEMBL18498 IC50 = 14000.0 nM 4.85
CHEMBL18312 IC50 = 30000.0 nM 4.52
CHEMBL18251 IC50 = 35000.0 nM 4.46
CHEMBL279268 IC50 = 81000.0 nM 4.09
CHEMBL278738 IC50 > 10000.0 nM -
CHEMBL19056 IC50 > 100000.0 nM -
CHEMBL18377 IC50 > 10000.0 nM -
CHEMBL277519 IC50 > 100000.0 nM -
CHEMBL18790 IC50 > 10000.0 nM -
CHEMBL416363 IC50 > 100000.0 nM -
CHEMBL275664 IC50 = 105000.0 nM -
CHEMBL273340 IC50 > 100000.0 nM -
CHEMBL18316 IC50 > 100000.0 nM -
CHEMBL18867 IC50 > 300000.0 nM -
CHEMBL273815 IC50 = 101000.0 nM -
CHEMBL18796 IC50 > 10000.0 nM -
CHEMBL18254 IC50 > 100000.0 nM -
CHEMBL275650 IC50 > 100000.0 nM -
CHEMBL280009 IC50 > 300000.0 nM -