Compound name
CPI-637
Protein family
Acetyltransferase
Target name
CREBBP@BRD
Affinity biochemical (nM)
30
Affinity on-target cellular (nM)
300
CG-Set
Epigenetic set
Recommended Concentration
1 µM
Compound EUbOPEN ID
EUB0000241b
SMILES
C[C@@H]1CC(O)=Nc2cccc(-c3ccc4c(c3)c(-c3cnn(C)c3)nn4C)c2N1
InChIKey
BFTKDWYIRJGJCA-CYBMUJFWSA-N
NCBI gene ID
1387
UniProt ID
Q92793
Synonyms
RTS, CBP, KAT3A
Mode of action
Inhibitor
Affinity biochemical definition
IC50
Affinity biochemical assay type
TR-FRET binding assay (CBP bromodomain)
Affinity Biochemical Source Knowledge
https://pubs.acs.org/doi/10.1021/acsmedchemlett.6b00075
Affinity biochemical relation
=
Affinity on-target cellular definition
IC50
Affinity on-target cellular assay type
NanoBRET assay (CBP, in HEK293T cells)
Affinity on-target cellular source knowledge
https://pubs.acs.org/doi/10.1021/acsmedchemlett.6b00075
Affinity on-target cellular relation
=
Selectivity platform
BET and bromodomain panel, literature
Selectivity platform number of targets
9
Selectivity remarks
>700-fold selective over the BET family of bromodomains; In-vitro potencies (enzymatic assay) of related targets: IC50(BRD9) = 0.73 μM, IC50(BRD4, BD1) = 11 µM, IC50(BRD4, BD2) = 13 µM, IC50(CECR2) = 7.7 µM, IC50(TAF1, BD2) = 17 µM, IC50(BAZ2B, BRG1, BRPF1, TAF1(BD1)) >20 µM;
Selectivity Source Knowledge
https://pubs.acs.org/doi/10.1021/acsmedchemlett.6b00075
Selectivity Number of Off-targets
1