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Assay Detail

CHEMBL1805783

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

Binding
Inhibition of TPA-induced cPLA2alpha activity in human platelets assessed as inhibition of arachidonic acid production after 60 mins by UV-reverse phase HPLC analysis
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

1-(5-Carboxyindol-1-yl)propan-2-one inhibitors of human cytosolic phospholipase A2α: effect of substituents in position 3 of the indole scaffold on inhibitory potency, metabolic stability, solubility, and bioavailability.
Bovens S, Schulze Elfringhoff A, Kaptur M, Reinhardt D, Schäfers M, Lehr M.
J Med Chem (2010) 53 : 8298 -8308
PubMed 21067218 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 8.22 9.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1800085 1 9.22
CHEMBL30108 1 8.33
CHEMBL1801026 1 7.12

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1800085 IC50 = 0.6 nM 9.22
CHEMBL30108 IC50 = 4.7 nM 8.33
CHEMBL1801026 IC50 = 76.0 nM 7.12