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Assay Detail

CHEMBL4401978

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

Binding
Inhibition of human recombinant G4A cPLA2 using arachidonyl-1-14C PAPC , PAPC and PIP2 incubated for 30 mins by HPLC-MS analysis based radioactivity-based group specific mixed micelle assay
4
Total Activities
3
Compounds Tested
2
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

β-Lactones: A Novel Class of Ca<sup>2+</sup>-Independent Phospholipase A<sub>2</sub> (Group VIA iPLA<sub>2</sub>) Inhibitors with the Ability To Inhibit β-Cell Apoptosis.
Dedaki C, Kokotou MG, Mouchlis VD, Limnios D, Lei X, Mu CT, Ramanadham S, Magrioti V, Dennis EA, Kokotos G.
J Med Chem (2019) 62 : 2916 -2927
PubMed 30798607 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
XI50 3 - -
IC50 1 4.66 4.66

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4476476 2 4.66
CHEMBL4440212 1 -
CHEMBL4462080 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4476476 IC50 = 22000.0 nM 4.66
CHEMBL4440212 XI50 = 0.0019 mole fraction -
CHEMBL4462080 XI50 = 4e-05 mole fraction -
CHEMBL4476476 XI50 = 0.042 mole fraction -