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Assay Detail

CHEMBL863829

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

Binding
Inhibition of human isolated cPLA2-alpha by vesicle assay
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

Cytosolic phospholipase A2 (CHEMBL3816)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design and synthesis of 1-indol-1-yl-propan-2-ones as inhibitors of human cytosolic phospholipase A2alpha.
Ludwig J, Bovens S, Brauch C, Elfringhoff AS, Lehr M.
J Med Chem (2006) 49 : 2611 -2620
PubMed 16610804 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 7.21 8.37

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL443834 1 8.37
CHEMBL426665 1 8.31
CHEMBL30108 1 7.96
CHEMBL381294 1 7.82
CHEMBL207977 1 7.80
CHEMBL204618 1 7.80
CHEMBL208401 1 7.70
CHEMBL205892 1 7.46
CHEMBL205753 1 6.96
CHEMBL204302 1 6.92
CHEMBL206943 1 6.47
CHEMBL425596 1 6.05
CHEMBL205941 1 5.96
CHEMBL409321 1 5.37

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL443834 IC50 = 4.3 nM 8.37
CHEMBL426665 IC50 = 4.9 nM 8.31
CHEMBL30108 IC50 = 11.0 nM 7.96
CHEMBL381294 IC50 = 15.0 nM 7.82
CHEMBL207977 IC50 = 16.0 nM 7.80
CHEMBL204618 IC50 = 16.0 nM 7.80
CHEMBL208401 IC50 = 20.0 nM 7.70
CHEMBL205892 IC50 = 35.0 nM 7.46
CHEMBL205753 IC50 = 110.0 nM 6.96
CHEMBL204302 IC50 = 120.0 nM 6.92
CHEMBL206943 IC50 = 340.0 nM 6.47
CHEMBL425596 IC50 = 890.0 nM 6.05
CHEMBL205941 IC50 = 1100.0 nM 5.96
CHEMBL409321 IC50 = 4300.0 nM 5.37