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Assay Detail

CHEMBL846549

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

Binding
Inhibition of tyrosine kinase v-Abl
13
Total Activities
13
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

4-(Phenylamino)pyrrolopyrimidines: potent and selective, ATP site directed inhibitors of the EGF-receptor protein tyrosine kinase.
Traxler PM, Furet P, Mett H, Buchdunger E, Meyer T, Lydon N.
J Med Chem (1996) 39 : 2285 -2292
PubMed 8691423 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 4.86 5.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL75049 1 5.70
CHEMBL74722 1 5.64
CHEMBL307026 1 5.28
CHEMBL306315 1 4.52
CHEMBL72393 1 4.52
CHEMBL306081 1 4.39
CHEMBL308582 1 4.00
CHEMBL433305 1 -
CHEMBL307062 1 -
CHEMBL307209 1 -
CHEMBL308593 1 -
CHEMBL75177 1 -
CHEMBL311129 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL75049 IC50 = 2000.0 nM 5.70
CHEMBL74722 IC50 = 2300.0 nM 5.64
CHEMBL307026 IC50 = 5300.0 nM 5.28
CHEMBL306315 IC50 = 30000.0 nM 4.52
CHEMBL72393 IC50 = 30000.0 nM 4.52
CHEMBL306081 IC50 = 40500.0 nM 4.39
CHEMBL308582 IC50 = 99000.0 nM 4.00
CHEMBL433305 IC50 > 100000.0 nM -
CHEMBL307062 IC50 > 100000.0 nM -
CHEMBL307209 IC50 > 100000.0 nM -
CHEMBL308593 IC50 > 100000.0 nM -
CHEMBL75177 IC50 > 100000.0 nM -
CHEMBL311129 IC50 > 100000.0 nM -