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Assay Detail

CHEMBL4345664

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Functional
Antiproliferative activity against bortezomib resistant human KM3/BTZ cells incubated for 48 hrs by MTT assay
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type KM3/BTZ
Confidence 1 — Organism
Curated By Autocuration

Target

KM3/BTZ (CHEMBL4483251)
Type CELL-LINE
Organism Homo sapiens

Publication

Discovery of Peptide Boronate Derivatives as Histone Deacetylase and Proteasome Dual Inhibitors for Overcoming Bortezomib Resistance of Multiple Myeloma.
Zhou Y, Liu X, Xue J, Liu L, Liang T, Li W, Yang X, Hou X, Fang H.
J Med Chem (2020) 63 : 4701 -4715
PubMed 32267687 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 6.68 8.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4456886 1 8.05
CHEMBL483254 PANOBINOSTAT 4.0 1 6.82
CHEMBL4576202 1 6.80
CHEMBL325041 BORTEZOMIB 3.0 1 6.65
CHEMBL98 VORINOSTAT 4.0 1 6.07
CHEMBL27759 ENTINOSTAT 3.0 1 5.69

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4456886 IC50 = 8.98 nM 8.05
CHEMBL483254 PANOBINOSTAT IC50 = 150.0 nM 6.82
CHEMBL4576202 IC50 = 157.0 nM 6.80
CHEMBL325041 BORTEZOMIB IC50 = 226.0 nM 6.65
CHEMBL98 VORINOSTAT IC50 = 860.0 nM 6.07
CHEMBL27759 ENTINOSTAT IC50 = 2040.0 nM 5.69