Name:PLX51107
Synonyms:N/A
CAS Number:1627929-55-8
Formula:C26H22N4O3
M.w.:438.48
DMSO (mg/mL)Max Solubility:88
DMSO (mM)Max Solubility:200.69
Form:Free Base
SMILES:CC([N]1C=C(C2=CC=C(C=C2)C(O)=O)C3=NC=C(C=C13)C4=C(C)ON=C4C)C5=CC=CC=N5
ALogP:4.288
Target:Epigenetic Reader Domain
Pathway:Epigenetics
Information:PLX51107 is as a novel BET inhibitor with modest preference for bromodomain-1 (BD1) versus bromodomain-2 (BD2) within each BET protein (Kd = 1.6, 2.1, 1.7, and 5 nM for BD1 and 5.9, 6.2, 6.1 and 120 nM for BD2 of BRD2, BRD3, BRD4, and BRDT, respectively. Among non-BET proteins, PLX51107 shows significant interactions only with the bromodomains of CBP and EP300 (p300) (Kd in the 100 nM range).
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