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Assay Detail

CHEMBL5374124

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

Binding
Inhibition of human BCR-ABL1 T315I mutant using Tyr2 peptide as substrate incubated for 1 hrs by FRET based Z-LYTE assay
5
Total Activities
5
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

Expanding the Chemical Space: New Approach to Cell-Permeable Drugs.
Kargbo RB.
ACS Med Chem Lett (2023) 14 : 1329 -1330
PubMed 37849551 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 5 7.90 8.38

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1171837 PONATINIB 4.0 1 8.38
CHEMBL4208229 ASCIMINIB 4.0 1 8.19
CHEMBL5423801 1 8.14
CHEMBL5435926 1 7.62
CHEMBL5414962 1 7.19

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1171837 PONATINIB EC50 = 4.18 nM 8.38
CHEMBL4208229 ASCIMINIB EC50 = 6.45 nM 8.19
CHEMBL5423801 EC50 = 7.23 nM 8.14
CHEMBL5435926 EC50 = 23.8 nM 7.62
CHEMBL5414962 EC50 = 64.03 nM 7.19