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Assay Detail

CHEMBL976275

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Binding
Inhibition of Abl kinase
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Tyrosine-protein kinase ABL1 (CHEMBL1862)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Novel N9-arenethenyl purines as potent dual Src/Abl tyrosine kinase inhibitors.
Wang Y, Shakespeare WC, Huang WS, Sundaramoorthi R, Lentini S, Das S, Liu S, Banda G, Wen D, Zhu X, Xu Q, Keats J, Wang F, Wardwell S, Ning Y, Snodgrass JT, Broudy MI, Russian K, Dalgarno D, Clackson T, Sawyer TK.
Bioorg Med Chem Lett (2008) 18 : 4907 -4912
PubMed 18691885 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 24 8.02 9.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL518166 1 9.30
CHEMBL461767 1 8.80
CHEMBL455384 1 8.79
CHEMBL509002 1 8.74
CHEMBL452563 1 8.63
CHEMBL454611 1 8.56
CHEMBL454358 1 8.52
CHEMBL488840 1 8.45
CHEMBL528330 1 8.23
CHEMBL509941 1 8.17
CHEMBL516498 1 8.13
CHEMBL459877 1 7.80
CHEMBL454868 1 7.78
CHEMBL454872 1 7.76
CHEMBL454873 1 7.75
CHEMBL451790 1 7.71
CHEMBL460074 1 7.49
CHEMBL520540 1 7.26
CHEMBL510891 1 7.16
CHEMBL488658 1 7.13
CHEMBL488659 1 6.20
CHEMBL510893 1 -
CHEMBL461768 1 -
CHEMBL517256 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL518166 IC50 = 0.5 nM 9.30
CHEMBL461767 IC50 = 1.57 nM 8.80
CHEMBL455384 IC50 = 1.63 nM 8.79
CHEMBL509002 IC50 = 1.8 nM 8.74
CHEMBL452563 IC50 = 2.36 nM 8.63
CHEMBL454611 IC50 = 2.77 nM 8.56
CHEMBL454358 IC50 = 3.02 nM 8.52
CHEMBL488840 IC50 = 3.58 nM 8.45
CHEMBL528330 IC50 = 5.93 nM 8.23
CHEMBL509941 IC50 = 6.8 nM 8.17
CHEMBL516498 IC50 = 7.32 nM 8.13
CHEMBL459877 IC50 = 15.8 nM 7.80
CHEMBL454868 IC50 = 16.7 nM 7.78
CHEMBL454872 IC50 = 17.3 nM 7.76
CHEMBL454873 IC50 = 17.6 nM 7.75
CHEMBL451790 IC50 = 19.5 nM 7.71
CHEMBL460074 IC50 = 32.3 nM 7.49
CHEMBL520540 IC50 = 54.3 nM 7.26
CHEMBL510891 IC50 = 69.4 nM 7.16
CHEMBL488658 IC50 = 73.3 nM 7.13
CHEMBL488659 IC50 = 626.0 nM 6.20
CHEMBL510893 IC50 < 0.46 nM -
CHEMBL461768 IC50 < 0.46 nM -
CHEMBL517256 IC50 < 0.46 nM -