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Assay Detail

CHEMBL4413441

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

Binding
Inhibition of human recombinant calcium-independent PLA2 using PAPC as substrate assessed as reduction in free AA formation after 30 mins by HPLC-MS analysis
6
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

85/88 kDa calcium-independent phospholipase A2 (CHEMBL3213)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Substrate-Specific Inhibition Constants for Phospholipase A<sub>2</sub> Acting on Unique Phospholipid Substrates in Mixed Micelles and Membranes Using Lipidomics.
Mouchlis VD, Armando A, Dennis EA.
J Med Chem (2019) 62 : 1999 -2007
PubMed 30615445 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
XI50 3 - -
IC50 3 6.64 7.31

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL89506 2 7.31
CHEMBL148674 VARESPLADIB 2.0 2 6.88
CHEMBL4438490 2 5.73

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL89506 IC50 = 49.0 nM 7.31
CHEMBL148674 VARESPLADIB IC50 = 131.0 nM 6.88
CHEMBL4438490 IC50 = 1880.0 nM 5.73
CHEMBL148674 VARESPLADIB XI50 = 0.00018 uM -
CHEMBL89506 XI50 = 7e-05 uM -
CHEMBL4438490 XI50 = 0.0027 uM -