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Assay Detail

CHEMBL4000778

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

Binding
Inhibition of human platelet cytosolic phospholipase alpha-2 using 1-stearoyl-2-arachidonoyl-sn-glycero-3-phosphocholine/1,2-dioleoyl-sn-glycerol as substrate after 60 mins by UV-HPLC method
12
Total Activities
12
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

Structure-activity relationship studies on 1-(2-oxopropyl)indole-5-carboxylic acids acting as inhibitors of cytosolic phospholipase A2α: Effect of substituents at the indole 3-position on activity, solubility, and metabolic stability.
Arnsmann M, Hanekamp W, Elfringhoff AS, Lehr M.
Eur J Med Chem (2017) 125 : 1107 -1114
PubMed 27810597 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 7.59 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4097068 1 8.00
CHEMBL1800991 1 8.00
CHEMBL30108 1 7.96
CHEMBL1085637 1 7.92
CHEMBL4079052 1 7.82
CHEMBL1801026 1 7.66
CHEMBL4086908 1 7.64
CHEMBL4067166 1 7.51
CHEMBL205892 1 7.46
CHEMBL4100466 1 7.31
CHEMBL1800992 1 7.15
CHEMBL1801024 1 6.68

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4097068 IC50 = 10.0 nM 8.00
CHEMBL1800991 IC50 = 10.0 nM 8.00
CHEMBL30108 IC50 = 11.0 nM 7.96
CHEMBL1085637 IC50 = 12.0 nM 7.92
CHEMBL4079052 IC50 = 15.0 nM 7.82
CHEMBL1801026 IC50 = 22.0 nM 7.66
CHEMBL4086908 IC50 = 23.0 nM 7.64
CHEMBL4067166 IC50 = 31.0 nM 7.51
CHEMBL205892 IC50 = 35.0 nM 7.46
CHEMBL4100466 IC50 = 49.0 nM 7.31
CHEMBL1800992 IC50 = 71.0 nM 7.15
CHEMBL1801024 IC50 = 210.0 nM 6.68