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Assay Detail

CHEMBL4268714

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

Functional
Cytotoxicity against imatinib-sensitive human K562 cells assessed as decrease in cell viability after 24 hrs by XTT assay
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

K562 (CHEMBL385)
Type CELL-LINE
Organism Homo sapiens

Publication

Targeting heme Oxygenase-1 with hybrid compounds to overcome Imatinib resistance in chronic myeloid leukemia cell lines.
Sorrenti V, Pittalà V, Romeo G, Amata E, Dichiara M, Marrazzo A, Turnaturi R, Prezzavento O, Barbagallo I, Vanella L, Rescifina A, Floresta G, Tibullo D, Di Raimondo F, Intagliata S, Salerno L.
Eur J Med Chem (2018) 158 : 937 -950
PubMed 30261468 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 17 4.52 6.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL941 IMATINIB 4.0 1 6.00
CHEMBL4279418 1 5.19
CHEMBL4294145 1 5.00
CHEMBL4289670 1 4.92
CHEMBL4286253 1 4.60
CHEMBL4282448 1 4.53
CHEMBL4278991 1 4.49
CHEMBL4293078 1 4.32
CHEMBL4277944 1 4.30
CHEMBL4278359 1 4.24
CHEMBL4290101 1 4.23
CHEMBL4289687 1 4.23
CHEMBL4281817 1 4.18
CHEMBL4286268 1 4.18
CHEMBL482686 1 4.17
CHEMBL2414454 1 4.16
CHEMBL4288599 1 4.13

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL941 IMATINIB IC50 = 1000.0 nM 6.00
CHEMBL4279418 IC50 = 6500.0 nM 5.19
CHEMBL4294145 IC50 = 10110.0 nM 5.00
CHEMBL4289670 IC50 = 12000.0 nM 4.92
CHEMBL4286253 IC50 = 25020.0 nM 4.60
CHEMBL4282448 IC50 = 29510.0 nM 4.53
CHEMBL4278991 IC50 = 32470.0 nM 4.49
CHEMBL4293078 IC50 = 47500.0 nM 4.32
CHEMBL4277944 IC50 = 49890.0 nM 4.30
CHEMBL4278359 IC50 = 57410.0 nM 4.24
CHEMBL4290101 IC50 = 58870.0 nM 4.23
CHEMBL4289687 IC50 = 59480.0 nM 4.23
CHEMBL4281817 IC50 = 66090.0 nM 4.18
CHEMBL4286268 IC50 = 66500.0 nM 4.18
CHEMBL482686 IC50 = 68300.0 nM 4.17
CHEMBL2414454 IC50 = 69090.0 nM 4.16
CHEMBL4288599 IC50 = 74570.0 nM 4.13