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Assay Detail

CHEMBL4407501

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

Binding
Inhibition of ovine COX1 using arachidonic acid as substrate pretreated for 5 mins followed by substrate addition and measured after 2 mins by fluorescence based enzyme immunoassay
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
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

Design of balanced COX inhibitors based on anti-inflammatory and/or COX-2 inhibitory ascidian metabolites.
Ju Z, Su M, Hong J, La Kim E, Moon HR, Chung HY, Kim S, Jung JH.
Eur J Med Chem (2019) 180 : 86 -98
PubMed 31301566 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 5.47 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL26915 SC-560 1 8.00
CHEMBL521 IBUPROFEN 4.0 1 5.38
CHEMBL25 ASPIRIN 4.0 1 5.21
CHEMBL704 MESALAMINE 4.0 1 5.11
CHEMBL139 DICLOFENAC 4.0 1 4.73
CHEMBL4448450 1 4.41
CHEMBL118 CELECOXIB 4.0 1 -
CHEMBL42485 DUP-697 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL26915 SC-560 IC50 = 10.0 nM 8.00
CHEMBL521 IBUPROFEN IC50 = 4120.0 nM 5.38
CHEMBL25 ASPIRIN IC50 = 6120.0 nM 5.21
CHEMBL704 MESALAMINE IC50 = 7730.0 nM 5.11
CHEMBL139 DICLOFENAC IC50 = 18790.0 nM 4.73
CHEMBL4448450 IC50 = 39200.0 nM 4.41
CHEMBL118 CELECOXIB IC50 > 100000.0 nM -
CHEMBL42485 DUP-697 IC50 > 3000.0 nM -