Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL1763239

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

Binding
Inhibition of Bcr/Abl by FRET-based Z-lyte assay
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 6 — Multiple protein complex / RNA
Curated By Autocuration

Target

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

Publication

Hybrid compounds as new Bcr/Abl inhibitors.
Wang D, Zhang Z, Lu X, Feng Y, Luo K, Gan J, Yingxue L, Wan J, Li X, Zhang F, Tu Z, Cai Q, Ren X, Ding K, Ding K.
Bioorg Med Chem Lett (2011) 21 : 1965 -1968
PubMed 21376587 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 15 6.36 7.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1760371 1 7.70
CHEMBL255863 NILOTINIB 4.0 1 7.41
CHEMBL1760370 1 6.75
CHEMBL1760367 1 6.56
CHEMBL941 IMATINIB 4.0 1 6.51
CHEMBL1760365 1 6.32
CHEMBL1760366 1 6.31
CHEMBL1760364 1 6.29
CHEMBL1760363 1 6.17
CHEMBL1760369 1 6.11
CHEMBL1760373 1 5.89
CHEMBL1760374 1 5.42
CHEMBL1760375 1 5.26
CHEMBL1760368 1 -
CHEMBL1760372 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1760371 IC50 = 20.1 nM 7.70
CHEMBL255863 NILOTINIB IC50 = 39.3 nM 7.41
CHEMBL1760370 IC50 = 177.0 nM 6.75
CHEMBL1760367 IC50 = 277.0 nM 6.56
CHEMBL941 IMATINIB IC50 = 309.0 nM 6.51
CHEMBL1760365 IC50 = 480.0 nM 6.32
CHEMBL1760366 IC50 = 491.0 nM 6.31
CHEMBL1760364 IC50 = 507.0 nM 6.29
CHEMBL1760363 IC50 = 671.0 nM 6.17
CHEMBL1760369 IC50 = 774.0 nM 6.11
CHEMBL1760373 IC50 = 1300.0 nM 5.89
CHEMBL1760374 IC50 = 3780.0 nM 5.42
CHEMBL1760375 IC50 = 5510.0 nM 5.26
CHEMBL1760368 IC50 > 10000.0 nM -
CHEMBL1760372 IC50 > 2000.0 nM -