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Assay Detail

CHEMBL4712751

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Binding
Inhibition of full length mouse NAPE-PLD expressed in HEK293T cell lysate using PED6 as substrate preincubated for 30 mins followed by substrate addition and measured at 2 mins interval for 1 hr by tecan-plate reader analysis
11
Total Activities
11
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Cell Type HEK293T
Subcellular Lysate
Confidence 9 — Direct single protein target
Curated By Autocuration

Publication

Structure-Activity Relationship Studies of Pyrimidine-4-Carboxamides as Inhibitors of N-Acylphosphatidylethanolamine Phospholipase D.
Mock ED,Kotsogianni I,Driever WPF,Fonseca CS,Vooijs JM,den Dulk H,van Boeckel CAA,van der Stelt M
J Med Chem (2021) 64 : 481 -515
PubMed 33382264 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 5.68 6.42
pIC50 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4761882 1 6.42
CHEMBL4782800 1 6.41
CHEMBL4794048 1 6.35
CHEMBL4754918 1 6.24
CHEMBL4750592 1 5.90
CHEMBL4760293 1 5.74
CHEMBL4790197 1 5.48
CHEMBL4780517 1 5.02
CHEMBL496 HEXACHLOROPHENE 4.0 1 4.96
CHEMBL4746648 1 4.27
CHEMBL4750134 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4761882 IC50 = 380.19 nM 6.42
CHEMBL4782800 IC50 = 389.05 nM 6.41
CHEMBL4794048 IC50 = 446.68 nM 6.35
CHEMBL4754918 IC50 = 575.44 nM 6.24
CHEMBL4750592 IC50 = 1258.93 nM 5.90
CHEMBL4760293 IC50 = 1819.7 nM 5.74
CHEMBL4790197 IC50 = 3311.31 nM 5.48
CHEMBL4780517 IC50 = 9549.93 nM 5.02
CHEMBL496 HEXACHLOROPHENE IC50 = 11000.0 nM 4.96
CHEMBL4746648 IC50 = 54000.0 nM 4.27
CHEMBL4750134 pIC50 - -