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Assay Detail

CHEMBL4619595

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

Functional
Antiproliferative activity against human K562 cells incubated for 3 days by CCK8 assay
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type K562
Confidence 1 — Organism
Curated By Autocuration

Target

K562 (CHEMBL385)
Type CELL-LINE
Organism Homo sapiens

Publication

Global PROTAC Toolbox for Degrading BCR-ABL Overcomes Drug-Resistant Mutants and Adverse Effects.
Yang Y, Gao H, Sun X, Sun Y, Qiu Y, Weng Q, Rao Y.
J Med Chem (2020) 63 : 8567 -8583
PubMed 32657579 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 8.34 9.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5416410 DASATINIB 4.0 1 9.72
CHEMBL1171837 PONATINIB 4.0 1 9.52
CHEMBL4208229 ASCIMINIB 4.0 1 9.21
CHEMBL4640401 1 8.12
CHEMBL4642168 1 8.10
CHEMBL4639867 1 8.04
CHEMBL941 IMATINIB 4.0 1 7.12
CHEMBL4640733 1 6.92

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5416410 DASATINIB IC50 = 0.19 nM 9.72
CHEMBL1171837 PONATINIB IC50 = 0.3 nM 9.52
CHEMBL4208229 ASCIMINIB IC50 = 0.61 nM 9.21
CHEMBL4640401 IC50 = 7.5 nM 8.12
CHEMBL4642168 IC50 = 8.0 nM 8.10
CHEMBL4639867 IC50 = 9.2 nM 8.04
CHEMBL941 IMATINIB IC50 = 76.2 nM 7.12
CHEMBL4640733 IC50 = 121.0 nM 6.92