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Assay Detail

CHEMBL710870

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Binding
Inhibitory activity against Lysophosphatidic acid acyltransferase-beta expressed in Sf9 insect cell membranes
44
Total Activities
44
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type Sf9
Confidence 8 — Homologous single protein target
Curated By Intermediate

Target

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

Publication

Synthesis, SAR, and antitumor properties of diamino-C,N-diarylpyrimidine positional isomers: inhibitors of lysophosphatidic acid acyltransferase-beta.
Gong B, Hong F, Kohm C, Jenkins S, Tulinsky J, Bhatt R, De Vries P, Singer JW, Klein P.
Bioorg Med Chem Lett (2004) 14 : 2303 -2308
PubMed 15081029 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 44 6.64 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL75167 1 8.00
CHEMBL310136 1 7.80
CHEMBL308945 1 7.77
CHEMBL77883 1 7.77
CHEMBL74548 1 7.75
CHEMBL307716 1 7.70
CHEMBL311379 1 7.66
CHEMBL74492 1 7.62
CHEMBL74708 1 7.55
CHEMBL424605 1 7.55
CHEMBL74549 1 7.51
CHEMBL73376 1 7.47
CHEMBL72618 1 7.47
CHEMBL306107 1 7.27
CHEMBL75522 1 7.12
CHEMBL76274 1 7.10
CHEMBL72992 1 7.08
CHEMBL73574 1 7.06
CHEMBL74932 1 7.04
CHEMBL309911 1 6.92
CHEMBL422414 1 6.85
CHEMBL73947 1 6.82
CHEMBL75714 1 6.68
CHEMBL75132 1 6.64
CHEMBL305915 1 6.40
CHEMBL308275 1 6.35
CHEMBL77790 1 6.24
CHEMBL305688 1 6.21
CHEMBL73912 1 6.19
CHEMBL74931 1 6.14

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL75167 IC50 = 10.0 nM 8.00
CHEMBL310136 IC50 = 16.0 nM 7.80
CHEMBL77883 IC50 = 17.0 nM 7.77
CHEMBL308945 IC50 = 17.0 nM 7.77
CHEMBL74548 IC50 = 18.0 nM 7.75
CHEMBL307716 IC50 = 20.0 nM 7.70
CHEMBL311379 IC50 = 22.0 nM 7.66
CHEMBL74492 IC50 = 24.0 nM 7.62
CHEMBL74708 IC50 = 28.0 nM 7.55
CHEMBL424605 IC50 = 28.0 nM 7.55
CHEMBL74549 IC50 = 31.0 nM 7.51
CHEMBL72618 IC50 = 34.0 nM 7.47
CHEMBL73376 IC50 = 34.0 nM 7.47
CHEMBL306107 IC50 = 54.0 nM 7.27
CHEMBL75522 IC50 = 75.0 nM 7.12
CHEMBL76274 IC50 = 80.0 nM 7.10
CHEMBL72992 IC50 = 84.0 nM 7.08
CHEMBL73574 IC50 = 88.0 nM 7.06
CHEMBL74932 IC50 = 91.0 nM 7.04
CHEMBL309911 IC50 = 120.0 nM 6.92
CHEMBL422414 IC50 = 140.0 nM 6.85
CHEMBL73947 IC50 = 150.0 nM 6.82
CHEMBL75714 IC50 = 210.0 nM 6.68
CHEMBL75132 IC50 = 230.0 nM 6.64
CHEMBL305915 IC50 = 400.0 nM 6.40
CHEMBL308275 IC50 = 450.0 nM 6.35
CHEMBL77790 IC50 = 580.0 nM 6.24
CHEMBL305688 IC50 = 610.0 nM 6.21
CHEMBL73912 IC50 = 640.0 nM 6.19
CHEMBL74931 IC50 = 720.0 nM 6.14
CHEMBL308100 IC50 = 750.0 nM 6.12
CHEMBL75170 IC50 = 800.0 nM 6.10
CHEMBL75467 IC50 = 970.0 nM 6.01
CHEMBL75791 IC50 = 1100.0 nM 5.96
CHEMBL72202 IC50 = 2100.0 nM 5.68
CHEMBL74188 IC50 = 2300.0 nM 5.64
CHEMBL77940 IC50 = 2700.0 nM 5.57
CHEMBL312087 IC50 = 4900.0 nM 5.31
CHEMBL75561 IC50 = 7000.0 nM 5.16
CHEMBL309753 IC50 = 7000.0 nM 5.16
CHEMBL75889 IC50 = 8000.0 nM 5.10
CHEMBL75203 IC50 = 8300.0 nM 5.08
CHEMBL451233 IC50 = 10000.0 nM 5.00
CHEMBL75551 IC50 > 5000.0 nM -