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Assay Detail

CHEMBL4822089

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

Binding
Inhibition of human recombinant COX-2 using arachidonic acid as substrate preincubated with enzyme for 5 mins followed by substrate addition by colorimetric analysis
16
Total Activities
16
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

Novel 1,2,4-triazine-quinoline hybrids: The privileged scaffolds as potent multi-target inhibitors of LPS-induced inflammatory response via dual COX-2 and 15-LOX inhibition.
Ghanim AM, Rezq S, Ibrahim TS, Romero DG, Kothayer H.
Eur J Med Chem (2021) 219 : 113457 -113457
PubMed 33892270 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 6.98 7.35

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL118 CELECOXIB 4.0 1 7.35
CHEMBL4867950 1 7.33
CHEMBL4847404 1 7.27
CHEMBL4856646 1 7.22
CHEMBL4872636 1 7.19
CHEMBL4861765 1 7.17
CHEMBL4853361 1 7.14
CHEMBL4876293 1 7.10
CHEMBL4876862 1 7.07
CHEMBL4869763 1 7.01
CHEMBL4862389 1 6.96
CHEMBL4852008 1 6.92
CHEMBL4876637 1 6.80
CHEMBL4857790 1 6.55
CHEMBL4862415 1 6.50
CHEMBL1034 DICLOFENAC SODIUM 4.0 1 6.08

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL118 CELECOXIB IC50 = 45.0 nM 7.35
CHEMBL4867950 IC50 = 47.0 nM 7.33
CHEMBL4847404 IC50 = 54.0 nM 7.27
CHEMBL4856646 IC50 = 60.0 nM 7.22
CHEMBL4872636 IC50 = 65.0 nM 7.19
CHEMBL4861765 IC50 = 68.0 nM 7.17
CHEMBL4853361 IC50 = 73.0 nM 7.14
CHEMBL4876293 IC50 = 79.0 nM 7.10
CHEMBL4876862 IC50 = 85.0 nM 7.07
CHEMBL4869763 IC50 = 97.0 nM 7.01
CHEMBL4862389 IC50 = 110.0 nM 6.96
CHEMBL4852008 IC50 = 120.0 nM 6.92
CHEMBL4876637 IC50 = 160.0 nM 6.80
CHEMBL4857790 IC50 = 280.0 nM 6.55
CHEMBL4862415 IC50 = 320.0 nM 6.50
CHEMBL1034 DICLOFENAC SODIUM IC50 = 840.0 nM 6.08