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Assay Detail

CHEMBL923246

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

Binding
Inhibition of cPLA2-alpha in TPA-stimulated intact human platelets assessed as liberation of arachidonic acid after 60 mins
5
Total Activities
5
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-(2-Carboxyindol-5-yloxy)propan-2-ones as inhibitors of human cytosolic phospholipase A2alpha: synthesis, biological activity, metabolic stability, and solubility.
Fritsche A, Elfringhoff AS, Fabian J, Lehr M.
Bioorg Med Chem (2008) 16 : 3489 -3500
PubMed 18321717 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 6.54 7.75

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL205892 1 7.75
CHEMBL260248 1 6.52
CHEMBL260708 1 6.30
CHEMBL260365 1 6.22
CHEMBL260247 1 5.89

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL205892 IC50 = 18.0 nM 7.75
CHEMBL260248 IC50 = 300.0 nM 6.52
CHEMBL260708 IC50 = 500.0 nM 6.30
CHEMBL260365 IC50 = 600.0 nM 6.22
CHEMBL260247 IC50 = 1300.0 nM 5.89