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Target
Histone acetyltransferase p300 [1287-1666]/Histone acetyltransferase type B catalytic subunit
Ligand
BDBM50542046
Substrate
n/a
Meas. Tech.
Scintillation Proximity Assay (SPA)
IC50
41.0±n/a nM
Citation
 Wilson, JE; Levell, JR P300/CBP hat inhibitors US Patent  US11414384 Publication Date 8/16/2022 
Target
Name:
Histone acetyltransferase p300 [1287-1666]/Histone acetyltransferase type B catalytic subunit
Synonyms:
P300/CBP-HAT
Type:
Protein
Mol. Mass.:
n/a
Description:
n/a
Components:
This complex has 2 components.
Component 1
Name:
Histone acetyltransferase type B catalytic subunit
Synonyms:
2.3.1.48 | HAT1 | HAT1_HUMAN | Histone acetyltransferase 1 | Histone acetyltransferase type B catalytic subunit | KAT1
Type:
PROTEIN
Mol. Mass.:
49505.96
Organism:
Homo sapiens
Description:
ChEMBL_118878
Residue:
419
Sequence:
MAGFGAMEKFLVEYKSAVEKKLAEYKCNTNTAIELKLVRFPEDLENDIRTFFPEYTHQLFGDDETAFGYKGLKILLYYIAGSLSTMFRVEYASKVDENFDCVEADDVEGKIRQIIPPGFCTNTNDFLSLLEKEVDFKPFGTLLHTYSVLSPTGGENFTFQIYKADMTCRGFREYHERLQTFLMWFIETASFIDVDDERWHYFLVFEKYNKDGATLFATVGYMTVYNYYVYPDKTRPRVSQMLILTPFQGQGHGAQLLETVHRYYTEFPTVLDITAEDPSKSYVKLRDFVLVKLCQDLPCFSREKLMQGFNEDMAIEAQQKFKINKQHARRVYEILRLLVTDMSDAEQYRSYRLDIKRRLISPYKKKQRDLAKMRKCLRPEELTNQMNQIEISMQHEQLEESFQELVEDYRRVIERLAQE
  
Component 2
Name:
Histone acetyltransferase p300 [1287-1666)
Synonyms:
EP300 | EP300_HUMAN | Histone acetyltransferase p300 (1287-1666) | P300
Type:
Enzyme Catalytic Domain
Mol. Mass.:
43958.57
Organism:
Homo sapiens (Human)
Description:
aa 1287-1666
Residue:
380
Sequence:
KFSAKRLPSTRLGTFLENRVNDFLRRQNHPESGEVTVRVVHASDKTVEVKPGMKARFVDSGEMAESFPYRTKALFAFEEIDGVDLCFFGMHVQEYGSDCPPPNQRRVYISYLDSVHFFRPKCLRTAVYHEILIGYLEYVKKLGYTTGHIWACPPSEGDDYIFHCHPPDQKIPKPKRLQEWYKKMLDKAVSERIVHDYKDIFKQATEDRLTSAKELPYFEGDFWPNVLEESIKELEQEEEERKREENTSNESTDVTKGDSKNAKKKNNKKTSKNKSSLSRGNKKKPGMPNVSNDLSQKLYATMEKHKEVFFVIRLIAGPAANSLPPIVDPDPLIPCDLMDGRDAFLTLARDKHLEFSSLRRAQWSTMCMLVELHTQSQDRF
  
Inhibitor
Name:
BDBM50542046
Synonyms:
CHEMBL4633516 | US11414384, Example 84 Isomer 2
Type:
Small organic molecule
Emp. Form.:
C29H25N5O
Mol. Mass.:
459.5417
SMILES:
Cn1cc(cn1)-c1ccc2c(c[nH]c2c1)C(=O)[C@H](NCCc1ccc(cc1)C#N)c1ccccc1 |r|
Structure:
Search PDB for entries with ligand similarity: