Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL5107168

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

Binding
Inhibition of His6-tagged recombinant human BRD4 BD1 using (SGRGK(Ac)GGK(Ac)GLGK(Ac)GGAK(Ac)RHGSGSK-biotin) as substrate 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 9 — Direct single protein target
Curated By Autocuration

Target

Bromodomain-containing protein 4 (CHEMBL1163125)
Type SINGLE PROTEIN
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 7.63 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4854720 1 8.00
CHEMBL4848064 1 7.47
CHEMBL5178566 1 7.42

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4854720 IC50 = 10.0 nM 8.00
CHEMBL4848064 IC50 = 34.0 nM 7.47
CHEMBL5178566 IC50 = 38.0 nM 7.42