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Assay Detail

CHEMBL4199514

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

Binding
Inhibition of recombinant human sPLA2-10 using human HDL as substrate pretreated for 20 mins followed by substrate addition and measured after 60 mins by NEFA based assay
24
Total Activities
17
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

Group 10 secretory phospholipase A2 (CHEMBL4342)
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 23 6.38 7.38
IC90 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4215835 3 7.38
CHEMBL4210991 1 6.96
CHEMBL4204172 2 6.85
CHEMBL4217510 1 6.60
CHEMBL4205511 2 6.60
CHEMBL4171084 1 6.51
CHEMBL4203027 2 6.48
CHEMBL4214052 2 6.46
CHEMBL4213094 1 6.19
CHEMBL4205008 2 6.08
CHEMBL4206163 1 5.80
CHEMBL4204160 1 -
CHEMBL4207266 1 -
CHEMBL4207065 1 -
CHEMBL4213633 1 -
CHEMBL4204365 1 -
CHEMBL4209236 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4215835 IC50 = 42.0 nM 7.38
CHEMBL4210991 IC50 = 110.0 nM 6.96
CHEMBL4204172 IC50 = 140.0 nM 6.85
CHEMBL4205511 IC50 = 250.0 nM 6.60
CHEMBL4217510 IC50 = 250.0 nM 6.60
CHEMBL4171084 IC50 = 310.0 nM 6.51
CHEMBL4203027 IC50 = 330.0 nM 6.48
CHEMBL4214052 IC50 = 350.0 nM 6.46
CHEMBL4213094 IC50 = 640.0 nM 6.19
CHEMBL4205008 IC50 = 830.0 nM 6.08
CHEMBL4206163 IC50 = 1600.0 nM 5.80
CHEMBL4214052 IC50 = 2800.0 nM 5.55
CHEMBL4205008 IC50 = 3400.0 nM 5.47
CHEMBL4215835 IC90 = 362.0 nM -
CHEMBL4204160 IC50 - -
CHEMBL4203027 IC50 - -
CHEMBL4205511 IC50 - -
CHEMBL4215835 IC50 - -
CHEMBL4207266 IC50 - -
CHEMBL4204172 IC50 - -
CHEMBL4207065 IC50 - -
CHEMBL4213633 IC50 - -
CHEMBL4204365 IC50 - -
CHEMBL4209236 IC50 - -