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Assay Detail

CHEMBL5380587

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

Binding
Inhibition of N-terminal fused Nano Luc CRBN in HEK293T cells by NanoBRET CRBN engagement assay
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293T
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Protein cereblon (CHEMBL3763008)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Development of sulfonyl fluoride chemical probes to advance the discovery of cereblon modulators.
Liu Y, Nowak RP, Che J, Donovan KA, Huerta F, Liu H, Metivier RJ, Fischer ES, Jones LH.
RSC Med Chem (2024) 15 : 607 -611
PubMed 38389883 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 17 6.09 8.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5279477 1 8.96
CHEMBL3989927 IBERDOMIDE 3.0 1 7.89
CHEMBL5431003 1 7.15
CHEMBL304572 1 6.26
CHEMBL5400126 1 6.09
CHEMBL5397713 1 5.44
CHEMBL5430028 1 5.07
CHEMBL5427622 1 4.80
CHEMBL5409036 1 4.64
CHEMBL5425793 1 4.64
CHEMBL5422831 1 -
CHEMBL5419662 1 -
CHEMBL5410477 1 -
CHEMBL5425952 1 -
CHEMBL5406424 1 -
CHEMBL4633140 1 -
CHEMBL5399582 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5279477 IC50 = 1.1 nM 8.96
CHEMBL3989927 IBERDOMIDE IC50 = 12.8 nM 7.89
CHEMBL5431003 IC50 = 71.0 nM 7.15
CHEMBL304572 IC50 = 550.0 nM 6.26
CHEMBL5400126 IC50 = 808.0 nM 6.09
CHEMBL5397713 IC50 = 3600.0 nM 5.44
CHEMBL5430028 IC50 = 8500.0 nM 5.07
CHEMBL5427622 IC50 = 16000.0 nM 4.80
CHEMBL5409036 IC50 = 23000.0 nM 4.64
CHEMBL5425793 IC50 = 23000.0 nM 4.64
CHEMBL5422831 IC50 > 100000.0 nM -
CHEMBL5419662 IC50 > 100000.0 nM -
CHEMBL5410477 IC50 > 100000.0 nM -
CHEMBL5425952 IC50 > 100000.0 nM -
CHEMBL5406424 IC50 > 100000.0 nM -
CHEMBL4633140 IC50 > 100000.0 nM -
CHEMBL5399582 IC50 > 50000.0 nM -