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Assay Detail

CHEMBL3815852

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

Functional
Antiproliferative activity against human K562 cells assessed as inhibition of cell survival after 48 hrs by MTT assay
14
Total Activities
14
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

A combined ligand- and structure-based approach for the identification of rilmenidine-derived compounds which synergize the antitumor effects of doxorubicin.
Vucicevic J, Srdic-Rajic T, Pieroni M, Laurila JM, Perovic V, Tassini S, Azzali E, Costantino G, Glisic S, Agbaba D, Scheinin M, Nikolic K, Radi M, Veljkovic N.
Bioorg Med Chem (2016) 24 : 3174 -3183
PubMed 27265687 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 4.78 6.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL53463 DOXORUBICIN 4.0 1 6.00
CHEMBL289480 RILMENIDINE 4.0 1 4.19
CHEMBL3593723 1 4.16
CHEMBL3814535 1 -
CHEMBL3814593 1 -
CHEMBL3814220 1 -
CHEMBL3814521 1 -
CHEMBL3814626 1 -
CHEMBL3814276 1 -
CHEMBL3814259 1 -
CHEMBL3813724 1 -
CHEMBL3815157 1 -
CHEMBL3593725 1 -
CHEMBL57895 EFAROXAN 2.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL53463 DOXORUBICIN IC50 = 1000.0 nM 6.00
CHEMBL289480 RILMENIDINE IC50 = 65000.0 nM 4.19
CHEMBL3593723 IC50 = 70000.0 nM 4.16
CHEMBL3814535 IC50 = 222000.0 nM -
CHEMBL3814593 IC50 = 115000.0 nM -
CHEMBL3814220 IC50 > 300000.0 nM -
CHEMBL3814521 IC50 > 300000.0 nM -
CHEMBL3814626 IC50 = 128000.0 nM -
CHEMBL3814276 IC50 > 300000.0 nM -
CHEMBL3814259 IC50 = 224000.0 nM -
CHEMBL3813724 IC50 = 140000.0 nM -
CHEMBL3815157 IC50 > 300000.0 nM -
CHEMBL3593725 IC50 > 300000.0 nM -
CHEMBL57895 EFAROXAN IC50 > 300000.0 nM -