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Assay Detail

CHEMBL846552

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Inhibition of v-Abl tyrosine kinase activity
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 4 — Cell-line / Tissue
Curated By Expert

Target

Tyrosine-protein kinase ABL (CHEMBL2111414)
Type PROTEIN FAMILY
Organism Homo sapiens

Publication

7-Alkyl- and 7-cycloalkyl-5-aryl-pyrrolo[2,3-d]pyrimidines--potent inhibitors of the tyrosine kinase c-Src.
Widler L, Green J, Missbach M, Susa M, Altmann E.
Bioorg Med Chem Lett (2001) 11 : 849 -852
PubMed 11277535 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 19 6.80 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL355330 1 8.30
CHEMBL169390 1 8.00
CHEMBL168285 1 7.40
CHEMBL352801 1 7.40
CHEMBL355191 1 7.30
CHEMBL166765 1 7.07
CHEMBL166766 1 7.05
CHEMBL169570 1 6.96
CHEMBL352954 1 6.85
CHEMBL168382 1 6.77
CHEMBL354310 1 6.64
CHEMBL170724 1 6.58
CHEMBL169467 1 6.47
CHEMBL168266 1 6.41
CHEMBL168550 1 6.38
CHEMBL168555 1 6.17
CHEMBL170438 1 5.66
CHEMBL171311 1 4.98
CHEMBL171256 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL355330 IC50 = 5.0 nM 8.30
CHEMBL169390 IC50 = 10.0 nM 8.00
CHEMBL168285 IC50 = 40.0 nM 7.40
CHEMBL352801 IC50 = 40.0 nM 7.40
CHEMBL355191 IC50 = 50.0 nM 7.30
CHEMBL166765 IC50 = 85.0 nM 7.07
CHEMBL166766 IC50 = 90.0 nM 7.05
CHEMBL169570 IC50 = 110.0 nM 6.96
CHEMBL352954 IC50 = 140.0 nM 6.85
CHEMBL168382 IC50 = 170.0 nM 6.77
CHEMBL354310 IC50 = 230.0 nM 6.64
CHEMBL170724 IC50 = 260.0 nM 6.58
CHEMBL169467 IC50 = 340.0 nM 6.47
CHEMBL168266 IC50 = 390.0 nM 6.41
CHEMBL168550 IC50 = 420.0 nM 6.38
CHEMBL168555 IC50 = 680.0 nM 6.17
CHEMBL170438 IC50 = 2200.0 nM 5.66
CHEMBL171311 IC50 = 10500.0 nM 4.98
CHEMBL171256 IC50 > 10000.0 nM -