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Assay Detail

CHEMBL4153311

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

Binding
Inhibition of human recombinant COX2 using arachidonic acid as substrate preincubated for 5 mins followed by substrate addition and measured after 2 mins by ADPH probe-based fluorescence assay
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Prostaglandin G/H synthase 2 (CHEMBL230)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of novel Methylsulfonyl phenyl derivatives as potent human Cyclooxygenase-2 inhibitors with effective anticonvulsant action: Design, synthesis, in-silico, in-vitro and in-vivo evaluation.
Mishra CB, Kumari S, Prakash A, Yadav R, Tiwari AK, Pandey P, Tiwari M.
Eur J Med Chem (2018) 151 : 520 -532
PubMed 29655084 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 5.32 5.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL416146 ETORICOXIB 4.0 1 5.96
CHEMBL4170210 1 5.67
CHEMBL4162939 1 5.50
CHEMBL4169819 1 5.27
CHEMBL4177013 1 5.19
CHEMBL4173650 1 5.15
CHEMBL4166395 1 4.90
CHEMBL4159582 1 4.89
CHEMBL4161896 1 -
CHEMBL4173245 1 -
CHEMBL4165330 1 -
CHEMBL4163920 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL416146 ETORICOXIB IC50 = 1100.0 nM 5.96
CHEMBL4170210 IC50 = 2150.0 nM 5.67
CHEMBL4162939 IC50 = 3140.0 nM 5.50
CHEMBL4169819 IC50 = 5320.0 nM 5.27
CHEMBL4177013 IC50 = 6420.0 nM 5.19
CHEMBL4173650 IC50 = 7150.0 nM 5.15
CHEMBL4166395 IC50 = 12490.0 nM 4.90
CHEMBL4159582 IC50 = 12800.0 nM 4.89
CHEMBL4161896 IC50 - -
CHEMBL4173245 IC50 - -
CHEMBL4165330 IC50 - -
CHEMBL4163920 IC50 - -