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Assay Detail

CHEMBL4049702

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

Binding
Inhibition of 26S proteasome regulatory subunit RPN11 deubiquitinating activity in beta5 inhibitor MG132 pretreated human HeLa cells expressing UbG76V-GFP assessed as reduction in UbG76V-GFP degradation rate by fluorescence microscopic method
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HeLa
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

26S proteasome non-ATPase regulatory subunit 14 (CHEMBL2007629)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of an Inhibitor of the Proteasome Subunit Rpn11.
Perez C, Li J, Parlati F, Rouffet M, Ma Y, Mackinnon AL, Chou TF, Deshaies RJ, Cohen SM.
J Med Chem (2017) 60 : 1343 -1361
PubMed 28191850 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 27 5.76 6.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4073553 1 6.22
CHEMBL4091693 1 6.00
CHEMBL4095913 1 6.00
CHEMBL4070821 1 5.92
CHEMBL4078891 1 5.92
CHEMBL4099434 1 5.85
CHEMBL4103171 1 5.58
CHEMBL4093962 1 5.54
CHEMBL4105598 1 5.30
CHEMBL4100384 1 5.30
CHEMBL4083926 1 -
CHEMBL4062208 1 -
CHEMBL4065318 1 -
CHEMBL4086748 1 -
CHEMBL4104719 1 -
CHEMBL4080490 1 -
CHEMBL4069023 1 -
CHEMBL4096289 1 -
CHEMBL4085174 1 -
CHEMBL4103114 1 -
CHEMBL4095417 1 -
CHEMBL4091004 1 -
CHEMBL4080694 1 -
CHEMBL4059915 1 -
CHEMBL4088568 1 -
CHEMBL4060337 1 -
CHEMBL4070030 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4073553 IC50 = 600.0 nM 6.22
CHEMBL4091693 IC50 = 1000.0 nM 6.00
CHEMBL4095913 IC50 = 1000.0 nM 6.00
CHEMBL4070821 IC50 = 1200.0 nM 5.92
CHEMBL4078891 IC50 = 1200.0 nM 5.92
CHEMBL4099434 IC50 = 1400.0 nM 5.85
CHEMBL4103171 IC50 = 2600.0 nM 5.58
CHEMBL4093962 IC50 = 2900.0 nM 5.54
CHEMBL4105598 IC50 = 5000.0 nM 5.30
CHEMBL4100384 IC50 = 5000.0 nM 5.30
CHEMBL4083926 IC50 > 10000.0 nM -
CHEMBL4062208 IC50 > 10000.0 nM -
CHEMBL4065318 IC50 > 10000.0 nM -
CHEMBL4086748 IC50 > 300.0 nM -
CHEMBL4104719 IC50 > 10000.0 nM -
CHEMBL4080490 IC50 > 10000.0 nM -
CHEMBL4069023 IC50 > 10000.0 nM -
CHEMBL4096289 IC50 > 10000.0 nM -
CHEMBL4085174 IC50 > 100000.0 nM -
CHEMBL4103114 IC50 > 100000.0 nM -
CHEMBL4095417 IC50 > 10000.0 nM -
CHEMBL4091004 IC50 > 100000.0 nM -
CHEMBL4080694 IC50 > 10000.0 nM -
CHEMBL4059915 IC50 > 10000.0 nM -
CHEMBL4088568 IC50 > 10000.0 nM -
CHEMBL4060337 IC50 > 10000.0 nM -
CHEMBL4070030 IC50 > 100000.0 nM -