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Assay Detail

CHEMBL768837

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Binding
Inhibitory potency against Prostaglandin G/H synthase 1 in human whole blood assay
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

Evaluation of loxoprofen and its alcohol metabolites for potency and selectivity of inhibition of cyclooxygenase-2.
Riendeau D, Salem M, Styhler A, Ouellet M, Mancini JA, Li CS.
Bioorg Med Chem Lett (2004) 14 : 1201 -1203
PubMed 14980665 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 5.47 6.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL6 INDOMETHACIN 4.0 1 6.72
CHEMBL441414 LOXOPROFEN TRANS ALCOHOL -1.0 1 6.55
CHEMBL416542 1 5.72
CHEMBL19286 1 5.33
CHEMBL19299 LOXOPROFEN 4.0 1 5.19
CHEMBL18264 1 4.82
CHEMBL122 ROFECOXIB 4.0 1 4.73
CHEMBL417452 1 4.70
CHEMBL18883 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL6 INDOMETHACIN IC50 = 190.0 nM 6.72
CHEMBL441414 LOXOPROFEN TRANS ALCOHOL IC50 = 280.0 nM 6.55
CHEMBL416542 IC50 = 1900.0 nM 5.72
CHEMBL19286 IC50 = 4700.0 nM 5.33
CHEMBL19299 LOXOPROFEN IC50 = 6500.0 nM 5.19
CHEMBL18264 IC50 = 15300.0 nM 4.82
CHEMBL122 ROFECOXIB IC50 = 18800.0 nM 4.73
CHEMBL417452 IC50 = 20200.0 nM 4.70
CHEMBL18883 IC50 > 25000.0 nM -