Target
Histone acetyltransferase KAT5
Ligand
BDBM50346552
Substrate
n/a
Meas. Tech.
ChEMBL_2233605 (CHEMBL5147377)
IC50
37200±n/a nM
Citation
 Kanada, RKagoshima, YAsano, MSuzuki, TMurata, THaruta, MTakahashi, MUbukata, OHashimoto, KObata, KKihara, KKuroha, MBanjo, TTogashi, NSato, KYamamoto, YSuzuki, KIsoyama, TTominaga, YHiguchi, SNaito, H Discovery of EP300/CBP histone acetyltransferase inhibitors through scaffold hopping of 1,4-oxazepane ring. Bioorg Med Chem Lett 66:0 (2022) [PubMed] 
Target
Name:
Histone acetyltransferase KAT5
Synonyms:
HTATIP | KAT5 | KAT5_HUMAN | TIP60
Type:
PROTEIN
Mol. Mass.:
58595.98
Organism:
Homo sapiens (Human)
Description:
ChEMBL_796787
Residue:
513
Sequence:
MAEVGEIIEGCRLPVLRRNQDNEDEWPLAEILSVKDISGRKLFYVHYIDFNKRLDEWVTHERLDLKKIQFPKKEAKTPTKNGLPGSRPGSPEREVPASAQASGKTLPIPVQITLRFNLPKEREAIPGGEPDQPLSSSSCLQPNHRSTKRKVEVVSPATPVPSETAPASVFPQNGAARRAVAAQPGRKRKSNCLGTDEDSQDSSDGIPSAPRMTGSLVSDRSHDDIVTRMKNIECIELGRHRLKPWYFSPYPQELTTLPVLYLCEFCLKYGRSLKCLQRHLTKCDLRHPPGNEIYRKGTISFFEIDGRKNKSYSQNLCLLAKCFLDHKTLYYDTDPFLFYVMTEYDCKGFHIVGYFSKEKESTEDYNVACILTLPPYQRRGYGKLLIEFSYELSKVEGKTGTPEKPLSDLGLLSYRSYWSQTILEILMGLKSESGERPQITINEISEITSIKKEDVISTLQYLNLINYYKGQYILTLSEDIVDGHERAMLKRLLRIDSKCLHFTPKDWSKRGKW
  
Inhibitor
Name:
BDBM50346552
Synonyms:
CHEMBL1797936
Type:
Small organic molecule
Emp. Form.:
C24H19N3O6
Mol. Mass.:
445.4242
SMILES:
Cc1cc(-c2ccc(C=c3c(=C)[nH]n(-c4ccc(cc4)C(O)=O)c3=O)o2)c(cc1C)[N+]([O-])=O |w:8.7|
Structure:
Search PDB for entries with ligand similarity: