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Assay Detail

CHEMBL3830592

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

Binding
Binding affinity to NanoLuc-tagged BRPF1 isoform 1 bromodomain (625 to 735 residues) (unknown origin) expressed in HEK293 cells co-transfected with histone H3.3-HaloTag using furimazine as substrate after 18 hrs by NanoBRET assay
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Peregrin (CHEMBL3132741)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

GSK6853, a Chemical Probe for Inhibition of the BRPF1 Bromodomain.
Bamborough P, Barnett HA, Becher I, Bird MJ, Chung CW, Craggs PD, Demont EH, Diallo H, Fallon DJ, Gordon LJ, Grandi P, Hobbs CI, Hooper-Greenhill E, Jones EJ, Law RP, Le Gall A, Lugo D, Michon AM, Mitchell DJ, Prinjha RK, Sheppard RJ, Watson AJ, Watson RJ.
ACS Med Chem Lett (2016) 7 : 552 -557
PubMed 27326325 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 6.55 7.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3828191 1 7.70
CHEMBL3827932 1 5.40

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3828191 IC50 = 19.95 nM 7.70
CHEMBL3827932 IC50 = 3981.07 nM 5.40