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Assay Detail

CHEMBL2384262

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

Binding
Inhibition of COX-1 in human whole blood assessed as inhibition of serum TXB2 level after 1 hr by radioimmunoassay
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Tissue Blood
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Prostaglandin G/H synthase 1 (CHEMBL221)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis, pharmacological characterization, and docking analysis of a novel family of diarylisoxazoles as highly selective cyclooxygenase-1 (COX-1) inhibitors.
Vitale P, Tacconelli S, Perrone MG, Malerba P, Simone L, Scilimati A, Lavecchia A, Dovizio M, Marcantoni E, Bruno A, Patrignani P.
J Med Chem (2013) 56 : 4277 -4299
PubMed 23651359 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 22 5.62 6.57

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2380863 1 6.57
CHEMBL2380867 1 6.50
CHEMBL2380876 1 6.48
CHEMBL363228 1 6.30
CHEMBL2380864 1 6.09
CHEMBL2380862 1 5.89
CHEMBL2380865 1 5.72
CHEMBL2380866 1 5.72
CHEMBL2380874 1 5.66
CHEMBL2380870 1 5.38
CHEMBL2380871 1 5.30
CHEMBL1710350 1 4.76
CHEMBL2380877 1 4.76
CHEMBL2380869 1 4.72
CHEMBL2380861 1 4.43
CHEMBL2380868 1 -
CHEMBL2380872 1 -
CHEMBL2380873 1 -
CHEMBL2380875 1 -
CHEMBL2380878 1 -
CHEMBL2380879 1 -
CHEMBL2380880 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2380863 IC50 = 270.0 nM 6.57
CHEMBL2380867 IC50 = 320.0 nM 6.50
CHEMBL2380876 IC50 = 330.0 nM 6.48
CHEMBL363228 IC50 = 500.0 nM 6.30
CHEMBL2380864 IC50 = 810.0 nM 6.09
CHEMBL2380862 IC50 = 1300.0 nM 5.89
CHEMBL2380865 IC50 = 1900.0 nM 5.72
CHEMBL2380866 IC50 = 1900.0 nM 5.72
CHEMBL2380874 IC50 = 2200.0 nM 5.66
CHEMBL2380870 IC50 = 4200.0 nM 5.38
CHEMBL2380871 IC50 = 5000.0 nM 5.30
CHEMBL1710350 IC50 = 17280.0 nM 4.76
CHEMBL2380877 IC50 = 17400.0 nM 4.76
CHEMBL2380869 IC50 = 19200.0 nM 4.72
CHEMBL2380861 IC50 = 37000.0 nM 4.43
CHEMBL2380868 IC50 > 100000.0 nM -
CHEMBL2380872 IC50 > 100000.0 nM -
CHEMBL2380873 IC50 > 100000.0 nM -
CHEMBL2380875 IC50 > 100000.0 nM -
CHEMBL2380878 IC50 > 100000.0 nM -
CHEMBL2380879 IC50 > 100000.0 nM -
CHEMBL2380880 IC50 > 100000.0 nM -