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Assay Detail

CHEMBL4366978

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

Binding
Inhibition of MANT-uracil binding to wild-type Magnetospirillum gryphiswaldense CRBN isoform 4 by FRET assay
26
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Magnetospirillum gryphiswaldense
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Cereblon isoform 4 (CHEMBL3763007)
Type SINGLE PROTEIN
Organism Magnetospirillum gryphiswaldense

Publication

De-Novo Design of Cereblon (CRBN) Effectors Guided by Natural Hydrolysis Products of Thalidomide Derivatives.
Heim C, Pliatsika D, Mousavizadeh F, Bär K, Hernandez Alvarez B, Giannis A, Hartmann MD.
J Med Chem (2019) 62 : 6615 -6629
PubMed 31251063 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 26 5.02 6.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL43452 POMALIDOMIDE 4.0 1 6.10
CHEMBL848 LENALIDOMIDE 4.0 1 5.51
CHEMBL4464143 1 5.40
CHEMBL275661 SUCCINIMIDE -1.0 1 5.37
CHEMBL468 THALIDOMIDE 4.0 1 5.36
CHEMBL4454711 1 5.30
CHEMBL475232 1 5.05
CHEMBL4437349 1 5.05
CHEMBL4589257 1 5.00
CHEMBL4589159 1 4.96
CHEMBL4455877 1 4.92
CHEMBL4556836 1 4.92
CHEMBL4563318 1 4.92
CHEMBL4521923 1 4.70
CHEMBL4561295 1 4.70
CHEMBL4447985 1 4.70
CHEMBL3763941 1 4.55
CHEMBL4442722 1 4.44
CHEMBL4472234 1 4.35
CHEMBL4544710 1 -
CHEMBL4451173 1 -
CHEMBL4581801 1 -
CHEMBL4437150 1 -
CHEMBL4520346 1 -
CHEMBL370441 1 -
CHEMBL4454431 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL43452 POMALIDOMIDE Ki = 800.0 nM 6.10
CHEMBL848 LENALIDOMIDE Ki = 3100.0 nM 5.51
CHEMBL4464143 Ki = 4000.0 nM 5.40
CHEMBL275661 SUCCINIMIDE Ki = 4300.0 nM 5.37
CHEMBL468 THALIDOMIDE Ki = 4400.0 nM 5.36
CHEMBL4454711 Ki = 5000.0 nM 5.30
CHEMBL475232 Ki = 9000.0 nM 5.05
CHEMBL4437349 Ki = 9000.0 nM 5.05
CHEMBL4589257 Ki = 10000.0 nM 5.00
CHEMBL4589159 Ki = 11000.0 nM 4.96
CHEMBL4455877 Ki = 12000.0 nM 4.92
CHEMBL4556836 Ki = 12000.0 nM 4.92
CHEMBL4563318 Ki = 12000.0 nM 4.92
CHEMBL4521923 Ki = 20000.0 nM 4.70
CHEMBL4561295 Ki = 20000.0 nM 4.70
CHEMBL4447985 Ki = 20000.0 nM 4.70
CHEMBL3763941 Ki = 28000.0 nM 4.55
CHEMBL4442722 Ki = 36000.0 nM 4.44
CHEMBL4472234 Ki = 45000.0 nM 4.35
CHEMBL4544710 Ki > 40000.0 nM -
CHEMBL4451173 Ki > 99000.0 nM -
CHEMBL4581801 Ki > 40000.0 nM -
CHEMBL4437150 Ki > 40000.0 nM -
CHEMBL4520346 Ki > 40000.0 nM -
CHEMBL370441 Ki > 40000.0 nM -
CHEMBL4454431 Ki > 40000.0 nM -