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Assay Detail

CHEMBL4375032

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

Binding
Inhibition of 20S proteasome beta 1c derived from human erythrocytes preincubated for 1 hr using Z-nLPnLD-Glo peptide as substrate by proteasome-glo caspase-like assay
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

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 22 5.95 7.50

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL325041 BORTEZOMIB 3.0 1 7.50
CHEMBL4468132 1 7.21
CHEMBL4445016 1 7.15
CHEMBL4437785 1 6.32
CHEMBL4516876 1 6.28
CHEMBL4580854 1 5.85
CHEMBL4460338 1 5.85
CHEMBL4558093 1 5.38
CHEMBL4542860 1 5.26
CHEMBL4576544 1 4.96
CHEMBL3237875 1 4.89
CHEMBL4435165 1 4.75
CHEMBL4573625 1 -
CHEMBL4470266 1 -
CHEMBL4465040 1 -
CHEMBL4519222 1 -
CHEMBL4471761 1 -
CHEMBL4565027 1 -
CHEMBL4452844 1 -
CHEMBL4543890 1 -
CHEMBL4542913 1 -
CHEMBL4458214 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL325041 BORTEZOMIB IC50 = 32.0 nM 7.50
CHEMBL4468132 IC50 = 61.0 nM 7.21
CHEMBL4445016 IC50 = 71.0 nM 7.15
CHEMBL4437785 IC50 = 480.0 nM 6.32
CHEMBL4516876 IC50 = 530.0 nM 6.28
CHEMBL4580854 IC50 = 1400.0 nM 5.85
CHEMBL4460338 IC50 = 1400.0 nM 5.85
CHEMBL4558093 IC50 = 4200.0 nM 5.38
CHEMBL4542860 IC50 = 5500.0 nM 5.26
CHEMBL4576544 IC50 = 11000.0 nM 4.96
CHEMBL3237875 IC50 = 13000.0 nM 4.89
CHEMBL4435165 IC50 = 18000.0 nM 4.75
CHEMBL4573625 IC50 > 20000.0 nM -
CHEMBL4470266 IC50 > 20000.0 nM -
CHEMBL4465040 IC50 > 20000.0 nM -
CHEMBL4519222 IC50 > 20000.0 nM -
CHEMBL4471761 IC50 > 20000.0 nM -
CHEMBL4565027 IC50 > 20000.0 nM -
CHEMBL4452844 IC50 > 20000.0 nM -
CHEMBL4543890 IC50 > 20000.0 nM -
CHEMBL4542913 IC50 > 20000.0 nM -
CHEMBL4458214 IC50 > 20000.0 nM -