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Assay Detail

CHEMBL5226022

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

Binding
Displacement of Cy5-O-Len from 6His-tagged CRBN/DDB1 (unknown origin) incubated for 1 hr under dark condition by fluorescence polarization assay
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

Protein cereblon/DNA damage-binding protein 1 (CHEMBL4630734)
Type PROTEIN-PROTEIN INTERACTION
Organism Homo sapiens

Publication

Phenyl Dihydrouracil: An Alternative Cereblon Binder for PROTAC Design.
Jarusiewicz JA, Yoshimura S, Mayasundari A, Actis M, Aggarwal A, McGowan K, Yang L, Li Y, Fu X, Mishra V, Heath R, Narina S, Pruett-Miller SM, Nishiguchi G, Yang JJ, Rankovic Z.
ACS Med Chem Lett (2023) 14 : 141 -145
PubMed 36793425 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 7.39 8.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5270900 1 8.85
CHEMBL5276245 1 8.15
CHEMBL5268757 1 7.28
CHEMBL5283559 1 6.66
CHEMBL5271340 1 5.99

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5270900 IC50 = 1.4 nM 8.85
CHEMBL5276245 IC50 = 7.1 nM 8.15
CHEMBL5268757 IC50 = 52.0 nM 7.28
CHEMBL5283559 IC50 = 217.3 nM 6.66
CHEMBL5271340 IC50 = 1028.7 nM 5.99