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Assay Detail

CHEMBL4345302

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

Binding
Inhibition of human recombinant full length His-tagged Bcr-Abl expressed in baculovirus expression system using tyrosine-2 peptide as substrate after 1 hr in presence of 10 mM ATP by FRET based Z'-LYTE assay
25
Total Activities
25
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 and Optimization of 3'-(Imidazo[1,2-a]pyrazin-3-yl)-[1,1'-biphenyl]-3-carboxamides as Selective DDR1 Inhibitors.
Mo C, Zhang Z, Li Y, Huang M, Zou J, Luo J, Tu ZC, Xu Y, Ren X, Ding K, Lu X.
ACS Med Chem Lett (2020) 11 : 379 -384
PubMed 32184973 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 25 5.77 6.62

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4464080 1 6.62
CHEMBL2336015 1 6.45
CHEMBL4473475 1 6.36
CHEMBL4544048 1 6.00
CHEMBL4535081 1 5.84
CHEMBL4586565 1 5.74
CHEMBL4438475 1 5.65
CHEMBL4466438 1 5.43
CHEMBL4575992 1 5.30
CHEMBL4583808 1 5.29
CHEMBL4571430 1 5.27
CHEMBL4583783 1 5.25
CHEMBL4559959 1 -
CHEMBL4534464 1 -
CHEMBL4519510 1 -
CHEMBL4470983 1 -
CHEMBL4447486 1 -
CHEMBL4590224 1 -
CHEMBL4565522 1 -
CHEMBL4440007 1 -
CHEMBL4519003 1 -
CHEMBL4555024 1 -
CHEMBL4547295 1 -
CHEMBL4444612 1 -
CHEMBL4438214 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4464080 IC50 = 237.0 nM 6.62
CHEMBL2336015 IC50 = 355.0 nM 6.45
CHEMBL4473475 IC50 = 437.0 nM 6.36
CHEMBL4544048 IC50 = 989.3 nM 6.00
CHEMBL4535081 IC50 = 1452.0 nM 5.84
CHEMBL4586565 IC50 = 1813.0 nM 5.74
CHEMBL4438475 IC50 = 2220.0 nM 5.65
CHEMBL4466438 IC50 = 3696.0 nM 5.43
CHEMBL4575992 IC50 = 4992.0 nM 5.30
CHEMBL4583808 IC50 = 5120.0 nM 5.29
CHEMBL4571430 IC50 = 5345.0 nM 5.27
CHEMBL4583783 IC50 = 5637.0 nM 5.25
CHEMBL4559959 IC50 > 10000.0 nM -
CHEMBL4534464 IC50 > 10000.0 nM -
CHEMBL4519510 IC50 > 10000.0 nM -
CHEMBL4470983 IC50 > 10000.0 nM -
CHEMBL4447486 IC50 > 10000.0 nM -
CHEMBL4590224 IC50 > 10000.0 nM -
CHEMBL4565522 IC50 > 10000.0 nM -
CHEMBL4440007 IC50 > 10000.0 nM -
CHEMBL4519003 IC50 > 10000.0 nM -
CHEMBL4555024 IC50 > 10000.0 nM -
CHEMBL4547295 IC50 > 10000.0 nM -
CHEMBL4444612 IC50 > 10000.0 nM -
CHEMBL4438214 IC50 > 10000.0 nM -