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Assay Detail

CHEMBL4714666

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

Binding
Inhibition of human recombinant COX-2 assessed as reduction in PGE2 production using 10 uM arachidonic acid as substrate preincubated with enzyme for 5 mins followed by substrate addition and measured after 20 mins by ELISA
13
Total Activities
13
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

Synthesis, Inhibitory Activity, and In Silico Modeling of Selective COX-1 Inhibitors with a Quinazoline Core.
Dvorakova M,Langhansova L,Temml V,Pavicic A,Vanek T,Landa P
ACS Med Chem Lett (2021) 12 : 610 -616
PubMed 33854702 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 5.05 5.99

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL26915 SC-560 1 5.99
CHEMBL521 IBUPROFEN 4.0 1 5.48
CHEMBL4763530 1 5.00
CHEMBL4792690 1 4.43
CHEMBL4789884 1 4.37
CHEMBL4787114 1 -
CHEMBL4751020 1 -
CHEMBL4763348 1 -
CHEMBL4795293 1 -
CHEMBL4760459 1 -
CHEMBL4753324 1 -
CHEMBL4796831 1 -
CHEMBL4755060 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL26915 SC-560 IC50 = 1030.0 nM 5.99
CHEMBL521 IBUPROFEN IC50 = 3300.0 nM 5.48
CHEMBL4763530 IC50 = 10100.0 nM 5.00
CHEMBL4792690 IC50 = 37300.0 nM 4.43
CHEMBL4789884 IC50 = 43000.0 nM 4.37
CHEMBL4787114 IC50 > 50000.0 nM -
CHEMBL4751020 IC50 > 50000.0 nM -
CHEMBL4763348 IC50 > 50000.0 nM -
CHEMBL4795293 IC50 > 50000.0 nM -
CHEMBL4760459 IC50 > 50000.0 nM -
CHEMBL4753324 IC50 > 50000.0 nM -
CHEMBL4796831 IC50 > 50000.0 nM -
CHEMBL4755060 IC50 > 50000.0 nM -