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Assay Detail

CHEMBL4151117

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

Binding
Inhibition of recombinant human sPLA2-5 expressed in Escherichia coli BL21(DE3) using 1-palmitoyl-2-oleoyl-sn-glycero-3-phosphocholine as substrate pretreated for 20 mins followed by substrate addition and measured after 60 mins
4
Total Activities
4
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

Phospholipase A2 group V (CHEMBL4323)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of a Series of Indole-2 Carboxamides as Selective Secreted Phospholipase A2 Type X (sPLA2-X) Inhibitors.
Knerr L, Giordanetto F, Nordberg P, Pettersen D, Selmi N, Beisel HG, de la Motte H, Olsson T, Perkins TDJ, Herslöf M, Månsson Å, Dahlström M, Starke I, Broddefalk J, Saarinen G, Klingegård F, Hurt-Camejo E, Rosengren B, Brengdahl J, Jansen F, Rohman M, Sandmark J, Hallberg K, Åkerud T, Roth RG, Ahlqvist M.
ACS Med Chem Lett (2018) 9 : 594 -599
PubMed 30034585 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 6.00 6.91

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL148674 VARESPLADIB 2.0 1 6.91
CHEMBL4171084 1 5.65
CHEMBL4176544 1 5.43
CHEMBL4173359 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL148674 VARESPLADIB IC50 = 124.0 nM 6.91
CHEMBL4171084 IC50 = 2230.0 nM 5.65
CHEMBL4176544 IC50 = 3700.0 nM 5.43
CHEMBL4173359 IC50 > 10000.0 nM -