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Assay Detail

CHEMBL1243979

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

Binding
Inhibition of ABL1 at 1 uM after 60 mins by FRET assay in presence of 10 uM ATP
10
Total Activities
10
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases.
Apsel B, Blair JA, Gonzalez B, Nazif TM, Feldman ME, Aizenstein B, Hoffman R, Williams RL, Shokat KM, Knight ZA.
Nat Chem Biol (2008) 4 : 691 -699
PubMed 18849971 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 7.30 9.00
Inhibition 2 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1241578 1 9.00
CHEMBL1081312 1 8.70
CHEMBL1233882 1 7.38
CHEMBL1241481 1 7.00
CHEMBL1233881 1 6.77
CHEMBL1241674 1 6.39
CHEMBL1241675 1 5.85
CHEMBL1241767 1 -
CHEMBL1230790 1 -
CHEMBL1234815 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1241578 IC50 = 1.0 nM 9.00
CHEMBL1081312 IC50 = 2.0 nM 8.70
CHEMBL1233882 IC50 = 42.0 nM 7.38
CHEMBL1241481 IC50 = 100.0 nM 7.00
CHEMBL1233881 IC50 = 170.0 nM 6.77
CHEMBL1241674 IC50 = 410.0 nM 6.39
CHEMBL1241675 IC50 = 1400.0 nM 5.85
CHEMBL1241767 IC50 > 50000.0 nM -
CHEMBL1230790 Inhibition = 99.0 % -
CHEMBL1234815 Inhibition = 78.0 % -