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Target
Histamine H4 receptor
Ligand
BDBM22885
Substrate
BDBM7966
Meas. Tech.
H4R Radioligand Binding Assay
pH
7.4±n/a
Temperature
310.15±n/a K
Ki
3162±650 nM
Comments
Analysis of the [3H]histamine saturation binding yielded a Kd value of 11 +/- 1 and a Bmax value of 1.8 +/- 0.4 pmol/mg protein.
Citation
 Lim, HD; van Rijn, RM; Ling, P; Bakker, RA; Thurmond, RL; Leurs, R Evaluation of histamine H1-, H2-, and H3-receptor ligands at the human histamine H4 receptor: identification of 4-methylhistamine as the first potent and selective H4 receptor agonist. J Pharmacol Exp Ther 314:1310-21 (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:
BDBM22885
Synonyms:
3-[(2S)-1-(1H-imidazol-5-yl)propan-2-yl]-2-(2-{[(5-methyl-1H-imidazol-4-yl)methyl]sulfanyl}ethyl)guanidine | CHEMBL417980 | N-[2-(1H-Imidazol-4-yl)-1-methyl-ethyl]-N'-[2-(5-methyl-1H-imidazol-4-ylmethylsulfanyl)-ethyl]-guanidine(S-sopromidine) | S-(+)-Sopromidine
Type:
Small organic molecule
Emp. Form.:
C14H23N7S
Mol. Mass.:
321.444
SMILES:
C[C@@H](Cc1cnc[nH]1)N=C(N)NCCSCc1[nH]cnc1C |w:9.10|
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: