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Assay Detail

CHEMBL764932

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

Binding
Inhibition of prostaglandin G/H synthase by measuring the reduction of prostaglandin F2-alpha in intact basophilic rat leukemia cells
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Cyclooxygenase (CHEMBL2095157)
Type PROTEIN FAMILY
Organism Rattus norvegicus

Publication

Design of 5-(3,5-di-tert-butyl-4-hydroxyphenyl)-1,3,4-thiadiazoles, -1,3,4-oxadiazoles, and -1,2,4-triazoles as orally-active, nonulcerogenic antiinflammatory agents.
Mullican MD, Wilson MW, Connor DT, Kostlan CR, Schrier DJ, Dyer RD.
J Med Chem (1993) 36 : 1090 -1099
PubMed 8478906 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 25 5.98 7.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL12594 E-5110 1 7.40
CHEMBL509 MECLOFENAMIC ACID 4.0 1 7.00
CHEMBL417073 1 6.89
CHEMBL8562 1 6.82
CHEMBL16828 1 6.46
CHEMBL12532 1 6.39
CHEMBL2079592 1 6.19
CHEMBL12483 1 6.11
CHEMBL122193 1 6.10
CHEMBL12302 1 5.82
CHEMBL12219 1 5.62
CHEMBL16977 1 5.60
CHEMBL276916 1 5.43
CHEMBL94851 1 5.28
CHEMBL12234 1 5.26
CHEMBL275909 1 5.17
CHEMBL12809 1 5.10
CHEMBL273941 1 5.03
CHEMBL12395 1 -
CHEMBL275445 1 -
CHEMBL12572 1 -
CHEMBL12154 1 -
CHEMBL273956 1 -
CHEMBL16827 1 -
CHEMBL12371 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL12594 E-5110 IC50 = 40.0 nM 7.40
CHEMBL509 MECLOFENAMIC ACID IC50 = 100.0 nM 7.00
CHEMBL417073 IC50 = 130.0 nM 6.89
CHEMBL8562 IC50 = 150.0 nM 6.82
CHEMBL16828 IC50 = 350.0 nM 6.46
CHEMBL12532 IC50 = 410.0 nM 6.39
CHEMBL2079592 IC50 = 650.0 nM 6.19
CHEMBL12483 IC50 = 780.0 nM 6.11
CHEMBL122193 IC50 = 800.0 nM 6.10
CHEMBL12302 IC50 = 1500.0 nM 5.82
CHEMBL12219 IC50 = 2400.0 nM 5.62
CHEMBL16977 IC50 = 2500.0 nM 5.60
CHEMBL276916 IC50 = 3700.0 nM 5.43
CHEMBL94851 IC50 = 5200.0 nM 5.28
CHEMBL12234 IC50 = 5500.0 nM 5.26
CHEMBL275909 IC50 = 6700.0 nM 5.17
CHEMBL12809 IC50 = 8000.0 nM 5.10
CHEMBL273941 IC50 = 9400.0 nM 5.03
CHEMBL12395 IC50 > 32000.0 nM -
CHEMBL275445 IC50 > 10000.0 nM -
CHEMBL12572 IC50 > 32000.0 nM -
CHEMBL12154 IC50 > 30000.0 nM -
CHEMBL273956 IC50 > 32000.0 nM -
CHEMBL16827 IC50 > 16000.0 nM -
CHEMBL12371 IC50 > 32000.0 nM -