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Assay Detail

CHEMBL880414

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Binding
Inhibitory activity against Lysophosphatidic acid acyltransferase-beta enzyme over-expressed in Sf9 insect cell membrane
21
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Sf9
Confidence 9 — Direct single protein target
Curated By Expert

Target

1-acyl-sn-glycerol-3-phosphate acyltransferase beta (CHEMBL4772)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Diamino-C,N-diarylpyridine positional isomers as inhibitors of lysophosphatidic acid acyltransferase-beta.
Hong F, Hollenback D, Singer JW, Klein P.
Bioorg Med Chem Lett (2005) 15 : 4703 -4707
PubMed 16143520 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 21 6.35 7.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL308945 1 7.77
CHEMBL193874 1 7.40
CHEMBL195457 2 7.35
CHEMBL193911 1 7.30
CHEMBL194604 1 7.30
CHEMBL306107 1 7.27
CHEMBL193588 1 7.00
CHEMBL193589 2 6.85
CHEMBL193713 1 6.62
CHEMBL194603 1 6.58
CHEMBL193910 1 6.31
CHEMBL309753 2 5.70
CHEMBL372358 1 5.19
CHEMBL75561 1 5.16
CHEMBL193879 1 4.75
CHEMBL193878 1 4.54
CHEMBL194167 2 4.46

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL308945 IC50 = 17.0 nM 7.77
CHEMBL193874 IC50 = 40.0 nM 7.40
CHEMBL195457 IC50 = 45.0 nM 7.35
CHEMBL193911 IC50 = 50.0 nM 7.30
CHEMBL194604 IC50 = 50.0 nM 7.30
CHEMBL306107 IC50 = 54.0 nM 7.27
CHEMBL195457 IC50 = 70.0 nM 7.16
CHEMBL193588 IC50 = 99.0 nM 7.00
CHEMBL193589 IC50 = 140.0 nM 6.85
CHEMBL193713 IC50 = 240.0 nM 6.62
CHEMBL193589 IC50 = 260.0 nM 6.58
CHEMBL194603 IC50 = 260.0 nM 6.58
CHEMBL193910 IC50 = 490.0 nM 6.31
CHEMBL309753 IC50 = 2000.0 nM 5.70
CHEMBL309753 IC50 = 2050.0 nM 5.69
CHEMBL372358 IC50 = 6500.0 nM 5.19
CHEMBL75561 IC50 = 7000.0 nM 5.16
CHEMBL193879 IC50 = 18000.0 nM 4.75
CHEMBL193878 IC50 = 29000.0 nM 4.54
CHEMBL194167 IC50 = 35000.0 nM 4.46
CHEMBL194167 IC50 > 40000.0 nM -