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Assay Detail

CHEMBL2405587

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

Functional
Cytotoxicity against adriamycin-resistant human HepG2 cells assessed as growth inhibition after 48 hrs by MTT assay
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type HepG2
Confidence 1 — Organism
Curated By Autocuration

Target

HepG2 (CHEMBL395)
Type CELL-LINE
Organism Homo sapiens

Publication

Discovery of bufadienolides as a novel class of ClC-3 chloride channel activators with antitumor activities.
Liu J, Zhang D, Li Y, Chen W, Ruan Z, Deng L, Wang L, Tian H, Yiu A, Fan C, Luo H, Liu S, Wang Y, Xiao G, Chen L, Ye W.
J Med Chem (2013) 56 : 5734 -5743
PubMed 23799775 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 5.86 6.46

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL399680 BUFALIN 1 6.46
CHEMBL250785 CINOBUFAGIN 1 5.77
CHEMBL2069023 1 5.62
CHEMBL463065 DESACETYLBUFOTALIN 1 5.59
CHEMBL2402164 1 -
CHEMBL2069030 1 -
CHEMBL2069056 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL399680 BUFALIN IC50 = 345.0 nM 6.46
CHEMBL250785 CINOBUFAGIN IC50 = 1706.0 nM 5.77
CHEMBL2069023 IC50 = 2375.0 nM 5.62
CHEMBL463065 DESACETYLBUFOTALIN IC50 = 2595.0 nM 5.59
CHEMBL2402164 IC50 > 100000.0 nM -
CHEMBL2069030 IC50 > 100000.0 nM -
CHEMBL2069056 IC50 > 100000.0 nM -