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Assay Detail

CHEMBL4199510

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

Binding
Inhibition of sPLA2-2A (unknown origin) using 1-palmitoyl-2-oleoyl-sn-glycero-3-phosphocholine as substrate pretreated for 20 mins followed by substrate addition and measured after 60 mins by NEFA based assay
22
Total Activities
16
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, membrane associated (CHEMBL3474)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design of Selective sPLA2-X Inhibitor (-)-2-{2-[Carbamoyl-6-(trifluoromethoxy)-1H-indol-1-yl]pyridine-2-yl}propanoic Acid.
Giordanetto F, Knerr L, Nordberg P, Pettersen D, Selmi N, Beisel HG, de la Motte H, Månsson Å, Dahlström M, Broddefalk J, Saarinen G, Klingegård F, Hurt-Camejo E, Rosengren B, Wikström J, Wågberg M, Brengdahl J, Rohman M, Sandmark J, Åkerud T, Roth RG, Jansen F, Ahlqvist M.
ACS Med Chem Lett (2018) 9 : 600 -605
PubMed 30034586 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 22 6.17 7.36

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4205008 2 7.36
CHEMBL4214052 2 7.24
CHEMBL4205511 2 7.04
CHEMBL4204172 2 6.85
CHEMBL4203027 2 6.77
CHEMBL4213094 1 6.54
CHEMBL4171084 1 6.51
CHEMBL4217510 1 6.33
CHEMBL4215835 2 6.20
CHEMBL4210991 1 6.09
CHEMBL4206163 1 5.92
CHEMBL4207065 1 5.72
CHEMBL4204160 1 5.51
CHEMBL4207266 1 5.41
CHEMBL4213633 1 5.40
CHEMBL4204365 1 5.35

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4205008 IC50 = 44.0 nM 7.36
CHEMBL4214052 IC50 = 57.0 nM 7.24
CHEMBL4205511 IC50 = 92.0 nM 7.04
CHEMBL4204172 IC50 = 140.0 nM 6.85
CHEMBL4203027 IC50 = 170.0 nM 6.77
CHEMBL4213094 IC50 = 290.0 nM 6.54
CHEMBL4171084 IC50 = 310.0 nM 6.51
CHEMBL4205008 IC50 = 340.0 nM 6.47
CHEMBL4217510 IC50 = 470.0 nM 6.33
CHEMBL4215835 IC50 = 630.0 nM 6.20
CHEMBL4214052 IC50 = 810.0 nM 6.09
CHEMBL4210991 IC50 = 820.0 nM 6.09
CHEMBL4203027 IC50 = 840.0 nM 6.08
CHEMBL4206163 IC50 = 1200.0 nM 5.92
CHEMBL4205511 IC50 = 1700.0 nM 5.77
CHEMBL4207065 IC50 = 1900.0 nM 5.72
CHEMBL4204172 IC50 = 2700.0 nM 5.57
CHEMBL4204160 IC50 = 3100.0 nM 5.51
CHEMBL4215835 IC50 = 3800.0 nM 5.42
CHEMBL4207266 IC50 = 3900.0 nM 5.41
CHEMBL4213633 IC50 = 4000.0 nM 5.40
CHEMBL4204365 IC50 = 4500.0 nM 5.35