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Assay Detail

CHEMBL4003673

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

Functional
Cytotoxicity against human RPMI8226 cells measured after 72 hrs by MTS assay
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type RPMI-8226
Confidence 1 — Organism
Curated By Autocuration

Target

RPMI-8226 (CHEMBL614882)
Type CELL-LINE
Organism Homo sapiens

Publication

Exploration of novel piperazine or piperidine constructed non-covalent peptidyl derivatives as proteasome inhibitors.
Zhuang R, Gao L, Lv X, Xi J, Sheng L, Zhao Y, He R, Hu X, Shao Y, Pan X, Liu S, Huang W, Zhou Y, Li J, Zhang J.
Eur J Med Chem (2017) 126 : 1056 -1070
PubMed 28027531 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 7.86 8.42

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4064404 1 8.42
CHEMBL4078693 1 8.08
CHEMBL4102324 1 7.99
CHEMBL451887 CARFILZOMIB 4.0 1 7.88
CHEMBL4094582 1 7.86
CHEMBL4099839 1 7.80
CHEMBL4061262 1 7.77
CHEMBL4072652 1 7.69
CHEMBL4104744 1 7.68
CHEMBL4078056 1 7.68
CHEMBL4082676 1 7.64

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4064404 IC50 = 3.8 nM 8.42
CHEMBL4078693 IC50 = 8.4 nM 8.08
CHEMBL4102324 IC50 = 10.2 nM 7.99
CHEMBL451887 CARFILZOMIB IC50 = 13.2 nM 7.88
CHEMBL4094582 IC50 = 13.9 nM 7.86
CHEMBL4099839 IC50 = 15.9 nM 7.80
CHEMBL4061262 IC50 = 17.1 nM 7.77
CHEMBL4072652 IC50 = 20.3 nM 7.69
CHEMBL4104744 IC50 = 20.8 nM 7.68
CHEMBL4078056 IC50 = 20.7 nM 7.68
CHEMBL4082676 IC50 = 22.7 nM 7.64