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Assay Detail

CHEMBL5554459

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

Functional
Cytotoxicity against human K562 cells incubated for 2 hrs followed by compound washout and measured after 72 hrs by Celltiter-blue viability assay
9
Total Activities
9
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

Novel <i>N,N</i>-Dimethyl-idarubicin Analogues Are Effective Cytotoxic Agents for ABCB1-Overexpressing, Doxorubicin-Resistant Cells.
van Gelder MA, Li Y, Wander DPA, Berlin I, Overkleeft HS, van der Zanden SY, Neefjes JJC.
J Med Chem (2024) 67 : 13802 -13812
PubMed 39088428 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 7.07 7.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5434379 1 7.72
CHEMBL1117 IDARUBICIN 4.0 1 7.57
CHEMBL3303266 1 7.42
CHEMBL457065 1 7.11
CHEMBL5407417 1 7.01
CHEMBL178 DAUNORUBICIN 4.0 1 6.85
CHEMBL5407496 1 6.85
CHEMBL417 EPIRUBICIN 4.0 1 6.62
CHEMBL53463 DOXORUBICIN 4.0 1 6.49

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5434379 IC50 = 19.0 nM 7.72
CHEMBL1117 IDARUBICIN IC50 = 27.0 nM 7.57
CHEMBL3303266 IC50 = 38.0 nM 7.42
CHEMBL457065 IC50 = 78.0 nM 7.11
CHEMBL5407417 IC50 = 98.0 nM 7.01
CHEMBL178 DAUNORUBICIN IC50 = 141.0 nM 6.85
CHEMBL5407496 IC50 = 141.0 nM 6.85
CHEMBL417 EPIRUBICIN IC50 = 239.0 nM 6.62
CHEMBL53463 DOXORUBICIN IC50 = 325.0 nM 6.49