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Assay Detail

CHEMBL2378944

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

Binding
Inhibition of Bcr-Abl kinase (unknown origin) after 30 mins by HTRF assay
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 7 — Homologous single protein target
Curated By Autocuration

Target

Bcr/Abl fusion protein (CHEMBL2096618)
Type CHIMERIC PROTEIN
Organism Homo sapiens

Publication

Design, synthesis and biological activities of Nilotinib derivates as antitumor agents.
Pan X, Wang F, Zhang Y, Gao H, Hu Z, Wang S, Zhang J.
Bioorg Med Chem (2013) 21 : 2527 -2534
PubMed 23538233 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 21 7.66 9.48

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL255863 NILOTINIB 4.0 1 9.48
CHEMBL2375971 1 9.28
CHEMBL2375973 1 8.83
CHEMBL2375972 1 8.63
CHEMBL2375892 1 8.49
CHEMBL2375900 1 8.42
CHEMBL2375889 1 8.32
CHEMBL2375891 1 8.32
CHEMBL2375977 1 8.20
CHEMBL2375895 1 7.46
CHEMBL2375976 1 7.20
CHEMBL2375901 1 6.53
CHEMBL2375974 1 6.46
CHEMBL2375975 1 5.96
CHEMBL2375898 1 5.56
CHEMBL2375890 1 5.38
CHEMBL2375899 1 -
CHEMBL2375893 1 -
CHEMBL2375894 1 -
CHEMBL2375896 1 -
CHEMBL2375897 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL255863 NILOTINIB IC50 = 0.33 nM 9.48
CHEMBL2375971 IC50 = 0.52 nM 9.28
CHEMBL2375973 IC50 = 1.48 nM 8.83
CHEMBL2375972 IC50 = 2.34 nM 8.63
CHEMBL2375892 IC50 = 3.21 nM 8.49
CHEMBL2375900 IC50 = 3.78 nM 8.42
CHEMBL2375889 IC50 = 4.73 nM 8.32
CHEMBL2375891 IC50 = 4.79 nM 8.32
CHEMBL2375977 IC50 = 6.34 nM 8.20
CHEMBL2375895 IC50 = 34.77 nM 7.46
CHEMBL2375976 IC50 = 63.31 nM 7.20
CHEMBL2375901 IC50 = 294.34 nM 6.53
CHEMBL2375974 IC50 = 350.08 nM 6.46
CHEMBL2375975 IC50 = 1110.42 nM 5.96
CHEMBL2375898 IC50 = 2754.9 nM 5.56
CHEMBL2375890 IC50 = 4125.31 nM 5.38
CHEMBL2375899 IC50 - -
CHEMBL2375893 IC50 - -
CHEMBL2375894 IC50 - -
CHEMBL2375896 IC50 - -
CHEMBL2375897 IC50 - -