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Assay Detail

CHEMBL4717168

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

ADMET
Inhibition of Ovine COX-1 assessed as decrease in prostaglandin production using arachidonic acid as substrate pretreated for 15 mins followed by substrate addition and measured after 2 mins by enzyme immunoassay
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type ADMET
Organism Ovis aries
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Prostaglandin G/H synthase 1 (CHEMBL2949)
Type SINGLE PROTEIN
Organism Ovis aries

Publication

Cyclooxygenase-2 and 15-lipoxygenase inhibition, synthesis, anti-inflammatory activity and ulcer liability of new celecoxib analogues: Determination of region-specific pyrazole ring formation by NOESY.
Abdelall EKA,Lamie PF,Ali WAM
Bioorg Med Chem Lett (2016) 26 : 2893 -2899
PubMed 27158139 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 5.26 6.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL25 ASPIRIN 4.0 1 6.52
CHEMBL4750876 1 5.41
CHEMBL4778023 1 5.24
CHEMBL4785437 1 5.19
CHEMBL4787167 1 5.19
CHEMBL4789752 1 5.17
CHEMBL4798825 1 5.17
CHEMBL4746534 1 5.14
CHEMBL4789069 1 5.12
CHEMBL118 CELECOXIB 4.0 1 5.12
CHEMBL4764063 1 5.08
CHEMBL4765087 1 5.07
CHEMBL4764950 1 4.99
CHEMBL1562610 MECLOFENAMATE SODIUM 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL25 ASPIRIN IC50 = 300.0 nM 6.52
CHEMBL4750876 IC50 = 3900.0 nM 5.41
CHEMBL4778023 IC50 = 5800.0 nM 5.24
CHEMBL4785437 IC50 = 6500.0 nM 5.19
CHEMBL4787167 IC50 = 6500.0 nM 5.19
CHEMBL4789752 IC50 = 6700.0 nM 5.17
CHEMBL4798825 IC50 = 6800.0 nM 5.17
CHEMBL4746534 IC50 = 7200.0 nM 5.14
CHEMBL4789069 IC50 = 7500.0 nM 5.12
CHEMBL118 CELECOXIB IC50 = 7600.0 nM 5.12
CHEMBL4764063 IC50 = 8400.0 nM 5.08
CHEMBL4765087 IC50 = 8600.0 nM 5.07
CHEMBL4764950 IC50 = 10200.0 nM 4.99
CHEMBL1562610 MECLOFENAMATE SODIUM IC50 - -