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Assay Detail

CHEMBL1003656

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

Binding
Inhibition of COX1 in bovine platelets assessed as formation of 12-hydroxyheptadecatrienoic acid by HPLC
26
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Bos taurus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Prostaglandin G/H synthase 1 (CHEMBL2860)
Type SINGLE PROTEIN
Organism Bos taurus

Publication

Diaryl-dithiolanes and -isothiazoles: COX-1/COX-2 and 5-LOX-inhibitory, *OH scavenging and anti-adhesive activities.
Scholz M, Ulbrich HK, Soehnlein O, Lindbom L, Mattern A, Dannhardt G.
Bioorg Med Chem (2009) 17 : 558 -568
PubMed 19097798 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 26 6.55 9.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL490292 1 9.52
CHEMBL139 DICLOFENAC 4.0 1 8.52
CHEMBL473946 1 8.52
CHEMBL522267 1 8.22
CHEMBL514950 1 8.00
CHEMBL504541 1 7.70
CHEMBL522624 1 7.70
CHEMBL489899 1 7.52
CHEMBL524133 1 7.40
CHEMBL491089 1 7.16
CHEMBL491088 1 7.00
CHEMBL490889 1 6.70
CHEMBL475545 1 6.70
CHEMBL300982 LICOFELONE 2.0 1 6.70
CHEMBL515547 1 6.22
CHEMBL491090 1 6.00
CHEMBL489898 1 5.70
CHEMBL491477 1 5.16
CHEMBL475347 1 5.10
CHEMBL118 CELECOXIB 4.0 1 5.10
CHEMBL491272 1 5.10
CHEMBL472722 1 4.70
CHEMBL472721 1 4.70
CHEMBL171646 1 4.30
CHEMBL52 NORDIHYDROGUAIARETIC ACID 1 4.30
CHEMBL489702 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL490292 IC50 = 0.3 nM 9.52
CHEMBL139 DICLOFENAC IC50 = 3.0 nM 8.52
CHEMBL473946 IC50 = 3.0 nM 8.52
CHEMBL522267 IC50 = 6.0 nM 8.22
CHEMBL514950 IC50 = 10.0 nM 8.00
CHEMBL504541 IC50 = 20.0 nM 7.70
CHEMBL522624 IC50 = 20.0 nM 7.70
CHEMBL489899 IC50 = 30.0 nM 7.52
CHEMBL524133 IC50 = 40.0 nM 7.40
CHEMBL491089 IC50 = 70.0 nM 7.16
CHEMBL491088 IC50 = 100.0 nM 7.00
CHEMBL490889 IC50 = 200.0 nM 6.70
CHEMBL475545 IC50 = 200.0 nM 6.70
CHEMBL300982 LICOFELONE IC50 = 200.0 nM 6.70
CHEMBL515547 IC50 = 600.0 nM 6.22
CHEMBL491090 IC50 = 1000.0 nM 6.00
CHEMBL489898 IC50 = 2000.0 nM 5.70
CHEMBL491477 IC50 = 7000.0 nM 5.16
CHEMBL475347 IC50 = 8000.0 nM 5.10
CHEMBL118 CELECOXIB IC50 = 8000.0 nM 5.10
CHEMBL491272 IC50 = 8000.0 nM 5.10
CHEMBL472722 IC50 = 20000.0 nM 4.70
CHEMBL472721 IC50 = 20000.0 nM 4.70
CHEMBL171646 IC50 = 50000.0 nM 4.30
CHEMBL52 NORDIHYDROGUAIARETIC ACID IC50 = 50000.0 nM 4.30
CHEMBL489702 IC50 > 50000.0 nM -