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Assay Detail

CHEMBL5256274

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

Binding
Displacement of fluorescent tracer from NanoLuc-tagged CRBN (unknown origin) by NanoBRET assay
14
Total Activities
14
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

Protein cereblon (CHEMBL3763008)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Structural rationalization of GSPT1 and IKZF1 degradation by thalidomide molecular glue derivatives.
Nowak RP, Che J, Ferrao S, Kong NR, Liu H, Zerfas BL, Jones LH.
RSC Med Chem (2023) 14 : 501 -506
PubMed 36970148 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 6.17 6.63

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2324726 1 6.63
CHEMBL2324704 1 6.47
CHEMBL182442 1 6.42
CHEMBL40206 1 6.42
CHEMBL848 LENALIDOMIDE 4.0 1 6.41
CHEMBL43855 1 6.25
CHEMBL304572 1 6.22
CHEMBL2324714 1 6.20
CHEMBL297116 1 6.18
CHEMBL43452 POMALIDOMIDE 4.0 1 6.13
CHEMBL2324703 1 5.94
CHEMBL468 THALIDOMIDE 4.0 1 5.83
CHEMBL2324702 1 5.70
CHEMBL296118 1 5.54

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2324726 IC50 = 234.0 nM 6.63
CHEMBL2324704 IC50 = 337.0 nM 6.47
CHEMBL182442 IC50 = 376.0 nM 6.42
CHEMBL40206 IC50 = 382.0 nM 6.42
CHEMBL848 LENALIDOMIDE IC50 = 390.0 nM 6.41
CHEMBL43855 IC50 = 560.0 nM 6.25
CHEMBL304572 IC50 = 605.0 nM 6.22
CHEMBL2324714 IC50 = 630.0 nM 6.20
CHEMBL297116 IC50 = 658.0 nM 6.18
CHEMBL43452 POMALIDOMIDE IC50 = 739.0 nM 6.13
CHEMBL2324703 IC50 = 1140.0 nM 5.94
CHEMBL468 THALIDOMIDE IC50 = 1490.0 nM 5.83
CHEMBL2324702 IC50 = 2000.0 nM 5.70
CHEMBL296118 IC50 = 2900.0 nM 5.54