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Assay Detail

CHEMBL5217995

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

Binding
Inhibition of full-length P300 (1 to 2414 residues) (unknown origin) using ARTKQTARKSTGGKAPRKQLAGG-K(Biotin)-amide as substrate preincubated for 60 mins followed by substrate addition and measured by scintillation proximity assay
2
Total Activities
2
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 Proline-Based p300/CBP Inhibitors Using DNA-Encoded Library Technology in Combination with High-Throughput Screening.
Tian X, Suarez D, Thomson D, Li W, King EA, LaFrance L, Boehm J, Barton L, Di Marco C, Martyr C, Thalji R, Medina J, Knight S, Heerding D, Gao E, Nartey E, Cecconie T, Nixon C, Zhang G, Berrodin TJ, Phelps C, Patel A, Bai X, Lind K, Prabhu N, Messer J, Zhu Z, Shewchuk L, Reid R, Graves AP, McHugh C, Mangatt B.
J Med Chem (2022) 65 : 14391 -14408
PubMed 36302181 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 9.10 9.20

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5220956 1 9.20
CHEMBL5219177 1 9.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5220956 IC50 = 0.631 nM 9.20
CHEMBL5219177 IC50 = 1.0 nM 9.00