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Target
Bromodomain-containing protein 4 [44-168]/Histone H4
Ligand
BDBM209480
Substrate
n/a
Meas. Tech.
AlphaScreen Assay
IC50
8±n/a nM
Citation
 Engelhardt, H; Gianni, D; Smethurst, C Substituted [1,2,4]triazolo[4,3-A]pyrazines that are BRD4 inhibitors US Patent  US9266891 Publication Date 2/23/2016 
Target
Name:
Bromodomain-containing protein 4 [44-168]/Histone H4
Synonyms:
BRD4-BD1 and Histone H4
Type:
Protein
Mol. Mass.:
n/a
Description:
n/a
Components:
This complex has 2 components.
Component 1
Name:
Bromodomain-containing protein 4 [44-168]
Synonyms:
BET bromodomain 4(1) (BRD4(1)) | BRD4 | BRD4-BD1 protein (aa 44-168) | BRD4_HUMAN | Bromodomain protein 4 (BRD4-BD1) | Bromodomain-containing protein 4 (BRD4-BD1) | Bromodomain-containing protein 4 (BRD4) (aa 44-168) | Bromodomain-containing protein 4 (BRD4-BD1) | Bromodomain-containing protein 4 bromodomain 1 (BRD4-BD1) | HUNK1
Type:
Enzyme Catalytic Domain
Mol. Mass.:
14866.49
Organism:
Homo sapiens (Human)
Description:
aa (44-168)
Residue:
125
Sequence:
NPPPPETSNPNKPKRQTNQLQYLLRVVLKTLWKHQFAWPFQQPVDAVKLNLPDYYKIIKTPMDMGTIKKRLENNYYWNAQECIQDFNTMFTNCYIYNKPGDDIVLMAEALEKLFLQKINELPTEE
  
Component 2
Name:
Histone H4
Synonyms:
H4-16 | H4/A | H4/B | H4/C | H4/D | H4/E | H4/G | H4/H | H4/I | H4/J | H4/K | H4/M | H4/N | H4/O | H4C1 | H4F2 | H4FA | H4FB | H4FC | H4FD | H4FE | H4FG | H4FH | H4FI | H4FJ | H4FK | H4FM | H4FN | H4FO | H4_HUMAN | HIST1H4A | HIST1H4B | HIST1H4C | HIST1H4D | HIST1H4E | HIST1H4F | HIST1H4H | HIST1H4I | HIST1H4J | HIST1H4K | HIST1H4L | HIST2H4 | HIST2H4A | HIST2H4B | HIST4H4 | and | andH4/B | andH4/C | andH4/D | andH4/E | andH4/G | andH4/H | andH4/I | andH4/J | andH4/K | andH4/M | andH4/N | andH4/O
Type:
Protein
Mol. Mass.:
11386.36
Organism:
Homo sapiens (Human)
Description:
P62805
Residue:
103
Sequence:
MSGRGKGGKGLGKGGAKRHRKVLRDNIQGITKPAIRRLARRGGVKRISGLIYEETRGVLKVFLENVIRDAVTYTEHAKRKTVTAMDVVYALKRQGRTLYGFGG
  
Inhibitor
Name:
BDBM209480
Synonyms:
US10328074, Example III-21 | US11077107, Example III-21 | US9266891, III-21
Type:
Small organic molecule
Emp. Form.:
C25H28N10
Mol. Mass.:
468.5568
SMILES:
CNc1nc(cn2c(C)nnc12)-c1nc2ccc(cc2n1Cc1ccccn1)N1CCN(C)CC1
Structure:
Search PDB for entries with ligand similarity: