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Target
Histamine H4 receptor
Ligand
BDBM22566
Substrate
BDBM7966
Meas. Tech.
Radioligand Binding Assay
pH
7.4±n/a
Temperature
298.15±n/a K
Ki
12±7 nM
Citation
 Liu, H; Altenbach, RJ; Carr, TL; Chandran, P; Hsieh, GC; Lewis, LG; Manelli, AM; Milicic, I; Marsh, KC; Miller, TR; Strakhova, MI; Vortherms, TA; Wakefield, BD; Wetter, JM; Witte, DG; Honore, P; Esbenshade, TA; Brioni, JD; Cowart, MD cis-4-(Piperazin-1-yl)-5,6,7a,8,9,10,11,11a-octahydrobenzofuro[2,3-h]quinazolin-2-amine (A-987306), A New Histamine H4R Antagonist that Blocks Pain Responses against Carrageenan-Induced Hyperalgesia. J Med Chem 51:7094-8 (2008) [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:
BDBM22566
Synonyms:
5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-indole | CHEMBL129198 | JNJ 7777120
Type:
Small organic molecule
Emp. Form.:
C14H16ClN3O
Mol. Mass.:
277.749
SMILES:
CN1CCN(CC1)C(=O)c1cc2cc(Cl)ccc2[nH]1
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
BDBM7966
Synonyms:
2-(1H-imidazol-4-yl)ethan-1-amine | CHEMBL544208 | CHEMBL90 | Ceplene | Ergotidine | HISTAMINE DIHYDROCHLORIDE | Histamine | L-histamine | Peremin | [3H]histamine
Type:
Small organic molecule
Emp. Form.:
C5H9N3
Mol. Mass.:
111.1451
SMILES:
NCCc1cnc[nH]1
Structure:
Search PDB for entries with ligand similarity: