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Assay Detail

CHEMBL5107170

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

Binding
Protac activity at His-tagged CRBN/FLAG-tagged DDB1 (unknown origin) in presence of Cy5-labeled thalidomide incubated for 60 min by TR-FRET assay
3
Total Activities
3
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

Linker-Dependent Folding Rationalizes PROTAC Cell Permeability.
Poongavanam V, Atilaw Y, Siegel S, Giese A, Lehmann L, Meibom D, Erdelyi M, Kihlberg J.
J Med Chem (2022) 65 : 13029 -13040
PubMed 36170570 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 9.21 9.61

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5178566 1 9.61
CHEMBL4848064 1 9.18
CHEMBL4854720 1 8.85

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5178566 IC50 = 0.244 nM 9.61
CHEMBL4848064 IC50 = 0.667 nM 9.18
CHEMBL4854720 IC50 = 1.41 nM 8.85