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Assay Detail

CHEMBL4351666

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

Binding
Inhibition of Halo-tagged histone H3.3 binding to N-terminal Nano luciferase-fused full-length PCAF (unknown origin) expressed in HEK293T cells co-expressing C-terminal Halo-tagged histone H3.3 measured after 18 hrs by 618 fluorescent ligand-based BRET assay
3
Total Activities
2
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

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

Target

Histone acetyltransferase KAT2B (CHEMBL5500)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of Pyrrolo[3,2- d]pyrimidin-4-one Derivatives as a New Class of Potent and Cell-Active Inhibitors of P300/CBP-Associated Factor Bromodomain.
Huang L, Li H, Li L, Niu L, Seupel R, Wu C, Cheng W, Chen C, Ding B, Brennan PE, Yang S.
J Med Chem (2019) 62 : 4526 -4542
PubMed 30998845 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Inhibition 2 - -
IC50 1 6.93 6.93

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4574669 2 6.93
CHEMBL4581184 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4574669 IC50 = 118.0 nM 6.93
CHEMBL4581184 Inhibition - % -
CHEMBL4574669 Inhibition - % -