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Assay Detail

CHEMBL3817162

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

Binding
Displacement of biotinylated ligand from recombinant His-tagged EP300 (unknown origin) incubated for 10 mins by TR-FRET assay
1
Total Activities
1
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

Fragment-Based Discovery of a Selective and Cell-Active Benzodiazepinone CBP/EP300 Bromodomain Inhibitor (CPI-637).
Taylor AM, Côté A, Hewitt MC, Pastor R, Leblanc Y, Nasveschuk CG, Romero FA, Crawford TD, Cantone N, Jayaram H, Setser J, Murray J, Beresini MH, de Leon Boenig G, Chen Z, Conery AR, Cummings RT, Dakin LA, Flynn EM, Huang OW, Kaufman S, Keller PJ, Kiefer JR, Lai T, Li Y, Liao J, Liu W, Lu H, Pardo E, Tsui V, Wang J, Wang Y, Xu Z, Yan F, Yu D, Zawadzke L, Zhu X, Zhu X, Sims RJ, Cochran AG, Bellon S, Audia JE, Magnuson S, Albrecht BK.
ACS Med Chem Lett (2016) 7 : 531 -536
PubMed 27190605 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 7.29 7.29

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3814752 1 7.29

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3814752 IC50 = 51.0 nM 7.29