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Assay Detail

CHEMBL665910

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.
18
Total Activities
18
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 18 4.97 5.16

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL112566 1 5.16
CHEMBL326138 1 5.10
CHEMBL326063 1 5.05
CHEMBL114371 1 5.05
CHEMBL114702 1 5.00
CHEMBL114650 1 5.00
CHEMBL114902 1 5.00
CHEMBL281211 ARACHIDONYL TRIFLUOROMETHYLKETONE 1 4.96
CHEMBL324279 1 4.96
CHEMBL115248 1 4.96
CHEMBL114214 1 4.92
CHEMBL324810 1 4.92
CHEMBL114709 1 4.89
CHEMBL112593 1 4.89
CHEMBL112571 1 4.85
CHEMBL115056 1 4.82
CHEMBL116561 1 -
CHEMBL114631 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL112566 IC50 = 7000.0 nM 5.16
CHEMBL326138 IC50 = 8000.0 nM 5.10
CHEMBL326063 IC50 = 9000.0 nM 5.05
CHEMBL114371 IC50 = 9000.0 nM 5.05
CHEMBL114702 IC50 = 10000.0 nM 5.00
CHEMBL114650 IC50 = 10000.0 nM 5.00
CHEMBL114902 IC50 = 10000.0 nM 5.00
CHEMBL281211 ARACHIDONYL TRIFLUOROMETHYLKETONE IC50 = 11000.0 nM 4.96
CHEMBL324279 IC50 = 11000.0 nM 4.96
CHEMBL115248 IC50 = 11000.0 nM 4.96
CHEMBL114214 IC50 = 12000.0 nM 4.92
CHEMBL324810 IC50 = 12000.0 nM 4.92
CHEMBL114709 IC50 = 13000.0 nM 4.89
CHEMBL112593 IC50 = 13000.0 nM 4.89
CHEMBL112571 IC50 = 14000.0 nM 4.85
CHEMBL115056 IC50 = 15000.0 nM 4.82
CHEMBL116561 IC50 > 10000.0 nM -
CHEMBL114631 IC50 - nM -