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Assay Detail

CHEMBL4401976

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

Binding
Inhibition of human recombinant G6A iPLA2 using arachidonyl-1-14C PAPC and PAPC incubated for 30 mins by HPLC-MS analysis based radioactivity-based group specific mixed micelle assay
14
Total Activities
12
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

85/88 kDa calcium-independent phospholipase A2 (CHEMBL3213)
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 12 - -
IC50 2 7.23 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4476476 2 9.00
CHEMBL4439384 2 5.46
CHEMBL1095003 1 -
CHEMBL3818906 1 -
CHEMBL4543220 1 -
CHEMBL4440328 1 -
CHEMBL4581494 1 -
CHEMBL4462080 1 -
CHEMBL4530817 1 -
CHEMBL4460099 1 -
CHEMBL2420367 1 -
CHEMBL460312 FKGK11 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4476476 IC50 = 1.0 nM 9.00
CHEMBL4439384 IC50 = 3500.0 nM 5.46
CHEMBL1095003 XI50 = 0.0002 mole fraction -
CHEMBL3818906 XI50 = 0.0057 mole fraction -
CHEMBL4543220 XI50 = 0.00019 mole fraction -
CHEMBL4440328 XI50 = 0.0003 mole fraction -
CHEMBL4581494 XI50 = 0.00019 mole fraction -
CHEMBL4462080 XI50 = 0.038 mole fraction -
CHEMBL4530817 XI50 = 9e-05 mole fraction -
CHEMBL4460099 XI50 = 0.0021 mole fraction -
CHEMBL2420367 XI50 = 0.0001 mole fraction -
CHEMBL460312 FKGK11 XI50 = 0.0014 mole fraction -
CHEMBL4439384 XI50 = 0.007 mole fraction -
CHEMBL4476476 XI50 = 2.1e-05 mole fraction -