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Assay Detail

CHEMBL4049704

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 human erythrocytes using Ub4-pepOG protein substrate preincubated for 1 hr followed by substrate addition measured after 80 mins by fluorescence polarization assay
50
Total Activities
50
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
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 50 5.82 6.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4104719 1 6.70
CHEMBL4100384 1 6.52
CHEMBL4073553 1 6.41
CHEMBL4070821 1 6.40
CHEMBL4093962 1 6.30
CHEMBL4069023 1 6.10
CHEMBL4088568 1 6.10
CHEMBL4105598 1 6.10
CHEMBL4060337 1 6.05
CHEMBL4095913 1 6.05
CHEMBL4093473 1 6.05
CHEMBL4101230 1 6.05
CHEMBL4077883 1 6.00
CHEMBL4087722 1 6.00
CHEMBL4078891 1 6.00
CHEMBL4093484 1 5.96
CHEMBL4095417 1 5.96
CHEMBL4099434 1 5.92
CHEMBL4065865 1 5.89
CHEMBL4103171 1 5.80
CHEMBL4100994 1 5.80
CHEMBL4097864 1 5.66
CHEMBL4076575 1 5.60
CHEMBL4084782 1 5.60
CHEMBL4065318 1 5.58
CHEMBL4083926 1 5.50
CHEMBL4062208 1 5.40
CHEMBL4091693 1 5.34
CHEMBL4063134 1 5.24
CHEMBL4059915 1 5.19

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4104719 IC50 = 200.0 nM 6.70
CHEMBL4100384 IC50 = 300.0 nM 6.52
CHEMBL4073553 IC50 = 390.0 nM 6.41
CHEMBL4070821 IC50 = 400.0 nM 6.40
CHEMBL4093962 IC50 = 500.0 nM 6.30
CHEMBL4069023 IC50 = 800.0 nM 6.10
CHEMBL4088568 IC50 = 800.0 nM 6.10
CHEMBL4105598 IC50 = 800.0 nM 6.10
CHEMBL4060337 IC50 = 900.0 nM 6.05
CHEMBL4095913 IC50 = 900.0 nM 6.05
CHEMBL4093473 IC50 = 900.0 nM 6.05
CHEMBL4101230 IC50 = 900.0 nM 6.05
CHEMBL4078891 IC50 = 1000.0 nM 6.00
CHEMBL4087722 IC50 = 1000.0 nM 6.00
CHEMBL4077883 IC50 = 1000.0 nM 6.00
CHEMBL4093484 IC50 = 1100.0 nM 5.96
CHEMBL4095417 IC50 = 1100.0 nM 5.96
CHEMBL4099434 IC50 = 1200.0 nM 5.92
CHEMBL4065865 IC50 = 1300.0 nM 5.89
CHEMBL4103171 IC50 = 1600.0 nM 5.80
CHEMBL4100994 IC50 = 1600.0 nM 5.80
CHEMBL4097864 IC50 = 2200.0 nM 5.66
CHEMBL4076575 IC50 = 2500.0 nM 5.60
CHEMBL4084782 IC50 = 2500.0 nM 5.60
CHEMBL4065318 IC50 = 2600.0 nM 5.58
CHEMBL4083926 IC50 = 3200.0 nM 5.50
CHEMBL4062208 IC50 = 4000.0 nM 5.40
CHEMBL4091693 IC50 = 4600.0 nM 5.34
CHEMBL4063134 IC50 = 5700.0 nM 5.24
CHEMBL4059915 IC50 = 6400.0 nM 5.19
CHEMBL4069573 IC50 = 15000.0 nM 4.82
CHEMBL4085174 IC50 = 82000.0 nM 4.09
CHEMBL4083010 IC50 > 100000.0 nM -
CHEMBL4085742 IC50 > 50000.0 nM -
CHEMBL4075311 IC50 > 100000.0 nM -
CHEMBL4076981 IC50 > 100000.0 nM -
CHEMBL99932 8-AMINOQUINOLINE IC50 > 100000.0 nM -
CHEMBL310555 OXYQUINOLINE IC50 > 100000.0 nM -
CHEMBL1702610 IC50 > 100000.0 nM -
CHEMBL4094874 IC50 > 100000.0 nM -
CHEMBL4074496 IC50 > 20000.0 nM -
CHEMBL4068027 IC50 > 100000.0 nM -
CHEMBL4086748 IC50 > 2000.0 nM -
CHEMBL4080490 IC50 < 200.0 nM -
CHEMBL4080694 IC50 > 5000.0 nM -
CHEMBL4091004 IC50 > 40000.0 nM -
CHEMBL4070030 IC50 > 40000.0 nM -
CHEMBL4103114 IC50 > 100000.0 nM -
CHEMBL4096289 IC50 < 200.0 nM -
CHEMBL4079842 IC50 > 100000.0 nM -