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Assay Detail

CHEMBL4375036

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Functional
Cytotoxicity against human PBMC cells assessed as reduction in cell viability by CellTiter Glo assay
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

PBMC (CHEMBL613107)
Type CELL-LINE
Organism Homo sapiens

Publication

Design and Evaluation of Highly Selective Human Immunoproteasome Inhibitors Reveal a Compensatory Process That Preserves Immune Cell Viability.
Ladi E, Everett C, Stivala CE, Daniels BE, Durk MR, Harris SF, Huestis MP, Purkey HE, Staben ST, Augustin M, Blaesse M, Steinbacher S, Eidenschenk C, Pappu R, Siu M.
J Med Chem (2019) 62 : 7032 -7041
PubMed 31283222 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 6.49 8.57

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL325041 BORTEZOMIB 3.0 1 8.57
CHEMBL4580854 1 7.00
CHEMBL4471761 1 5.24
CHEMBL4437785 1 5.14
CHEMBL4458214 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL325041 BORTEZOMIB IC50 = 2.7 nM 8.57
CHEMBL4580854 IC50 = 100.0 nM 7.00
CHEMBL4471761 IC50 = 5700.0 nM 5.24
CHEMBL4437785 IC50 = 7300.0 nM 5.14
CHEMBL4458214 IC50 > 10000.0 nM -