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Assay Detail

CHEMBL4394496

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

Functional
Cytotoxicity against human RPMI8226/Cfzr cells after 72 hrs by CellTiter 96 AQueous one solution cell proliferation assay
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Development of Novel Epoxyketone-Based Proteasome Inhibitors as a Strategy To Overcome Cancer Resistance to Carfilzomib and Bortezomib.
Lee MJ, Bhattarai D, Yoo J, Miller Z, Park JE, Lee S, Lee W, Driscoll JJ, Kim KB.
J Med Chem (2019) 62 : 4444 -4455
PubMed 30964987 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 6.24 6.97

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4451741 1 6.97
CHEMBL451887 CARFILZOMIB 4.0 1 6.57
CHEMBL4447840 1 6.51
CHEMBL207990 EPOXOMYCIN 1 6.27
CHEMBL3319605 1 5.67
CHEMBL4459808 1 5.47

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4451741 IC50 = 106.2 nM 6.97
CHEMBL451887 CARFILZOMIB IC50 = 269.0 nM 6.57
CHEMBL4447840 IC50 = 310.0 nM 6.51
CHEMBL207990 EPOXOMYCIN IC50 = 541.0 nM 6.27
CHEMBL3319605 IC50 = 2140.0 nM 5.67
CHEMBL4459808 IC50 = 3410.0 nM 5.47