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Assay Detail

CHEMBL4135370

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

Binding
Inhibition of human COX-2 using [14C]-arachidonic acid as substrate preincubated for 5 mins followed by substrate addition measured after 45 mins by thin layer chromatographic method
11
Total Activities
11
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 new indomethacin-based analogs with potentially selective cyclooxygenase-2 inhibition and observed diminishing to PGE2 activities.
Kassab SE, Khedr MA, Ali HI, Abdalla MM.
Eur J Med Chem (2017) 141 : 306 -321
PubMed 29031075 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 6.21 6.64

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4169347 1 6.64
CHEMBL4173526 1 6.55
CHEMBL118 CELECOXIB 4.0 1 6.52
CHEMBL4177185 1 6.47
CHEMBL4162061 1 6.24
CHEMBL4172740 1 6.10
CHEMBL4165597 1 6.09
CHEMBL4176892 1 6.06
CHEMBL4169030 1 6.04
CHEMBL4161755 1 6.01
CHEMBL6 INDOMETHACIN 4.0 1 5.58

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4169347 IC50 = 230.0 nM 6.64
CHEMBL4173526 IC50 = 280.0 nM 6.55
CHEMBL118 CELECOXIB IC50 = 300.0 nM 6.52
CHEMBL4177185 IC50 = 340.0 nM 6.47
CHEMBL4162061 IC50 = 580.0 nM 6.24
CHEMBL4172740 IC50 = 790.0 nM 6.10
CHEMBL4165597 IC50 = 810.0 nM 6.09
CHEMBL4176892 IC50 = 880.0 nM 6.06
CHEMBL4169030 IC50 = 910.0 nM 6.04
CHEMBL4161755 IC50 = 970.0 nM 6.01
CHEMBL6 INDOMETHACIN IC50 = 2630.0 nM 5.58