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Target
Histamine H4 receptor
Ligand
BDBM50133005
Substrate
n/a
Meas. Tech.
ChEMBL_325600 (CHEMBL860282)
Ki
8±n/a nM
Citation
 Venable, JD; Cai, H; Chai, W; Dvorak, CA; Grice, CA; Jablonowski, JA; Shah, CR; Kwok, AK; Ly, KS; Pio, B; Wei, J; Desai, PJ; Jiang, W; Nguyen, S; Ling, P; Wilson, SJ; Dunford, PJ; Thurmond, RL; Lovenberg, TW; Karlsson, L; Carruthers, NI; Edwards, JP Preparation and biological evaluation of indole, benzimidazole, and thienopyrrole piperazine carboxamides: potent human histamine h(4) antagonists. J Med Chem 48:8289-98 (2005) [PubMed]  Article 
Target
Name:
Histamine H4 receptor
Synonyms:
AXOR35 | G-protein coupled receptor 105 | GPCR105 | GPRv53 | HH4R | HISTAMINE H4 | HRH4 | HRH4_HUMAN | Histamine H4 receptor | Histamine H4 receptor (H4R) | Histamine receptor (H3 and H4) | Pfi-013 | SP9144
Type:
G Protein-Coupled Receptor (GPCR)
Mol. Mass.:
44517.02
Organism:
Homo sapiens (Human)
Description:
Binding assays were using CHO cells stably expressing hH4R receptors.
Residue:
390
Sequence:
MPDTNSTINLSLSTRVTLAFFMSLVAFAIMLGNALVILAFVVDKNLRHRSSYFFLNLAISDFFVGVISIPLYIPHTLFEWDFGKEICVFWLTTDYLLCTASVYNIVLISYDRYLSVSNAVSYRTQHTGVLKIVTLMVAVWVLAFLVNGPMILVSESWKDEGSECEPGFFSEWYILAITSFLEFVIPVILVAYFNMNIYWSLWKRDHLSRCQSHPGLTAVSSNICGHSFRGRLSSRRSLSASTEVPASFHSERQRRKSSLMFSSRTKMNSNTIASKMGSFSQSDSVALHQREHVELLRARRLAKSLAILLGVFAVCWAPYSLFTIVLSFYSSATGPKSVWYRIAFWLQWFNSFVNPLLYPLCHKRFQKAFLKIFCIKKQPLPSQHSRSVSS
  
Inhibitor
Name:
BDBM50133005
Synonyms:
(5-Bromo-1H-indol-2-yl)-(4-methyl-piperazin-1-yl)-methanone | (5-bromo-1H-indol-2-yl)(4-methylpiperazin-1-yl)methanone | CHEMBL128613
Type:
Small organic molecule
Emp. Form.:
C14H16BrN3O
Mol. Mass.:
322.2
SMILES:
CN1CCN(CC1)C(=O)c1cc2cc(Br)ccc2[nH]1
Structure:
Search PDB for entries with ligand similarity: