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Assay Detail

CHEMBL665909

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

Functional
Inhibition of cPLA2 measuring Calcium ionophore A-23,187-induced arachidonic acid release from bovine platelets with HPLC/UV detection
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Confidence 8 — Homologous single protein target
Curated By Intermediate

Target

Cytosolic phospholipase A2 (CHEMBL2304401)
Type SINGLE PROTEIN
Organism Bos taurus

Publication

Structure-activity relationships of (4-acylpyrrol-2-yl)alkanoic acids as inhibitors of the cytosolic phospholipase A2: variation of the substituents in positions 1, 3, and 5.
Lehr M.
J Med Chem (1997) 40 : 3381 -3392
PubMed 9341913 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 5.26 5.48

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL115454 1 5.48
CHEMBL327129 1 5.47
CHEMBL114530 1 5.44
CHEMBL115274 1 5.43
CHEMBL111997 1 5.42
CHEMBL114466 1 5.41
CHEMBL326627 1 5.25
CHEMBL115014 1 5.10
CHEMBL325179 1 4.96
CHEMBL116169 1 4.96
CHEMBL442012 1 4.89

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL115454 IC50 = 3300.0 nM 5.48
CHEMBL327129 IC50 = 3400.0 nM 5.47
CHEMBL114530 IC50 = 3600.0 nM 5.44
CHEMBL115274 IC50 = 3700.0 nM 5.43
CHEMBL111997 IC50 = 3800.0 nM 5.42
CHEMBL114466 IC50 = 3900.0 nM 5.41
CHEMBL326627 IC50 = 5600.0 nM 5.25
CHEMBL115014 IC50 = 8000.0 nM 5.10
CHEMBL325179 IC50 = 11000.0 nM 4.96
CHEMBL116169 IC50 = 11000.0 nM 4.96
CHEMBL442012 IC50 = 13000.0 nM 4.89