Compound name
A-485
Protein family
HAT
Target name
CREBBP@Acetyltransferase
Affinity biochemical (nM)
3
CG-Set
Epigenetic set
Recommended Concentration
1 µM
Compound EUbOPEN ID
EUB0000328a
SMILES
C[C@H](N(C(CN1C([C@]2(OC1=O)CCC3=CC(NC(NC)=O)=CC=C23)=O)=O)CC4=CC=C(F)C=C4)C(F)(F)F
InChIKey
VRVJKILQRBSEAG-BSEYFRJRSA-N
NCBI gene ID
1387
UniProt ID
Q92793
Synonyms
RTS, CBP, KAT3A
Mode of action
Inhibitor
Negative control
A-486
Affinity biochemical definition
IC50
Affinity biochemical assay type
TR-FRET assay (BHC domains)
Affinity Biochemical Source Knowledge
https://doi.org/10.1038/nature24028
https://www.sgc-ffm.uni-frankfurt.de/#!specificprobeoverview/A-485
Affinity biochemical relation
=
Selectivity remarks
Selective against other available HATs (MYST3, MYST4, PCAF, HAT1, TIP60 and GCN5L2); Screened in KinomeScan (DiscoverX) against 468 targets at 10 µM, clostest targets as % of contr.: PRKCE (22%), LATS2 (47%), ABL1(H396P)-nonphosphorylated (49%); Screened against 45 GPCR targets, closest targets: Ki(SLC6A4) = 223.27 nM, Ki(GABA/PBR) = 1107.62 nM, Ki(HTR2B) = 1292.04 nM, Ki(SLC6A3) = 1817.04;Cerep ligand profiling against 83 targets, at 10 µM, closest targets as % inhibition: SLC6A4 (99%), SLC6A3 (94%);
Selectivity Source Knowledge
https://doi.org/10.1038/nature24028
https://www.sgc-ffm.uni-frankfurt.de/#!specificprobeoverview/A-485