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Assay Detail

CHEMBL4187883

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Functional
Growth inhibition of human KG1a cells
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type KG-1a
Confidence 1 — Organism
Curated By Intermediate

Target

KG-1a (CHEMBL4296453)
Type CELL-LINE
Organism Homo sapiens

Publication

Design and synthesis of novel dasatinib derivatives as inhibitors of leukemia stem cells.
Li HY, He DD, Zhao XJ, Sun TY, Zhang Q, Bai CG, Chen Y.
Bioorg Med Chem Lett (2018) 28 : 700 -706
PubMed 29395973 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 15 5.96 7.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4218857 1 7.30
CHEMBL4212782 1 6.96
CHEMBL4216514 1 6.85
CHEMBL4203317 1 6.82
CHEMBL4216757 1 6.60
CHEMBL4203895 1 6.50
CHEMBL4213925 1 6.35
CHEMBL4203106 1 6.17
CHEMBL4207009 1 5.71
CHEMBL4209850 1 5.69
CHEMBL5416410 DASATINIB 4.0 1 5.05
CHEMBL4216010 1 5.01
CHEMBL4217670 1 4.89
CHEMBL4212055 1 4.87
CHEMBL4210740 1 4.59

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4218857 IC50 = 50.0 nM 7.30
CHEMBL4212782 IC50 = 110.0 nM 6.96
CHEMBL4216514 IC50 = 140.0 nM 6.85
CHEMBL4203317 IC50 = 150.0 nM 6.82
CHEMBL4216757 IC50 = 250.0 nM 6.60
CHEMBL4203895 IC50 = 320.0 nM 6.50
CHEMBL4213925 IC50 = 450.0 nM 6.35
CHEMBL4203106 IC50 = 680.0 nM 6.17
CHEMBL4207009 IC50 = 1960.0 nM 5.71
CHEMBL4209850 IC50 = 2060.0 nM 5.69
CHEMBL5416410 DASATINIB IC50 = 8980.0 nM 5.05
CHEMBL4216010 IC50 = 9750.0 nM 5.01
CHEMBL4217670 IC50 = 12880.0 nM 4.89
CHEMBL4212055 IC50 = 13560.0 nM 4.87
CHEMBL4210740 IC50 = 25390.0 nM 4.59