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Assay Detail

CHEMBL5545546

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Binding
Binding affinity to p300 (unknown origin) assessed as dissociation constant by ITC analysis
4
Total Activities
4
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

Histone acetyltransferase p300 (CHEMBL3784)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of CBPD-268 as an Exceptionally Potent and Orally Efficacious CBP/p300 PROTAC Degrader Capable of Achieving Tumor Regression.
Chen Z, Wang M, Wu D, Bai L, Xu T, Metwally H, Wang Y, McEachern D, Zhao L, Li R, Takyi-Williams J, Wang M, Wang L, Li Q, Wen B, Sun D, Wang S.
J Med Chem (2024) 67 : 5275 -5304
PubMed 38477974 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 4 8.02 8.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4097025 1 8.92
CHEMBL4076748 1 8.89
CHEMBL3622373 1 7.50
CHEMBL3774655 1 6.78

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4097025 Kd = 1.2 nM 8.92
CHEMBL4076748 Kd = 1.3 nM 8.89
CHEMBL3622373 Kd = 32.0 nM 7.50
CHEMBL3774655 Kd = 167.0 nM 6.78