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Assay Detail

CHEMBL982355

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

Binding
Inhibition of cPLA2 in human platelets assessed as arachidonic acid release
9
Total Activities
9
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

Cytosolic phospholipase A2 (CHEMBL3816)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

1-(5-Carboxyindol-1-yl)propan-2-ones as inhibitors of human cytosolic phospholipase A2alpha: synthesis and properties of bioisosteric benzimidazole, benzotriazole and indazole analogues.
Bovens S, Kaptur M, Elfringhoff AS, Lehr M.
Bioorg Med Chem Lett (2009) 19 : 2107 -2111
PubMed 19327988 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 7.39 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL484413 1 8.30
CHEMBL30108 1 7.96
CHEMBL484954 1 7.80
CHEMBL484953 1 7.58
CHEMBL482775 1 7.58
CHEMBL205892 1 7.46
CHEMBL520836 1 7.07
CHEMBL482959 1 6.82
CHEMBL205941 1 5.96

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL484413 IC50 = 5.0 nM 8.30
CHEMBL30108 IC50 = 11.0 nM 7.96
CHEMBL484954 IC50 = 16.0 nM 7.80
CHEMBL484953 IC50 = 26.0 nM 7.58
CHEMBL482775 IC50 = 26.0 nM 7.58
CHEMBL205892 IC50 = 35.0 nM 7.46
CHEMBL520836 IC50 = 85.0 nM 7.07
CHEMBL482959 IC50 = 150.0 nM 6.82
CHEMBL205941 IC50 = 1100.0 nM 5.96