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Assay Detail

CHEMBL5529786

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

Binding
Inhibition of p300/CBP (unknown origin) using histone H3 (1 to 21 residues) as substrate incubated for 90 mins by AlphaLISA 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

CREB-binding protein/Histone acetyltransferase p300 (CHEMBL3883300)
Type PROTEIN FAMILY
Organism Homo sapiens

Publication

Discovery of Novel PROTAC Degraders of p300/CBP as Potential Therapeutics for Hepatocellular Carcinoma.
Chang Q, Li J, Deng Y, Zhou R, Wang B, Wang Y, Zhang M, Huang X, Li Y.
J Med Chem (2024) 67 : 2466 -2486
PubMed 38316017 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 7.56 7.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5567101 1 7.60
CHEMBL5564786 1 7.58
CHEMBL4785363 INOBRODIB 1.0 1 7.50

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5567101 IC50 = 25.0 nM 7.60
CHEMBL5564786 IC50 = 26.0 nM 7.58
CHEMBL4785363 INOBRODIB IC50 = 32.0 nM 7.50