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Target
Histamine H3 receptor
Ligand
BDBM22548
Substrate
BDBM22530
Meas. Tech.
Radioligand Binding Assay and Functional [35S]GTP-gamma-S Binding Assay
pH
7.4±n/a
Temperature
298.15±n/a K
Ki
1±0.15 nM
EC50
2±1 nM
Citation
 Wijtmans, M; Celanire, S; Snip, E; Gillard, MR; Gelens, E; Collart, PP; Venhuis, BJ; Christophe, B; Hulscher, S; van der Goot, H; Lebon, F; Timmerman, H; Bakker, RA; Lallemand, BI; Leurs, R; Talaga, PE; de Esch, IJ 4-benzyl-1H-imidazoles with oxazoline termini as histamine H3 receptor agonists. J Med Chem 51:2944-53 (2008) [PubMed]  Article 
Target
Name:
Histamine H3 receptor
Synonyms:
G-protein coupled receptor 97 | GPCR97 | HH3R | HISTAMINE H3 | HRH3 | HRH3_HUMAN | Histamine H3 receptor (H3) | Histamine H3L | Histamine receptor (H3 and H4)
Type:
G Protein-Coupled Receptor (GPCR)
Mol. Mass.:
48691.47
Organism:
Homo sapiens (Human)
Description:
Binding assays were using CHO cells stably expressing hH3R receptors.
Residue:
445
Sequence:
MERAPPDGPLNASGALAGEAAAAGGARGFSAAWTAVLAALMALLIVATVLGNALVMLAFVADSSLRTQNNFFLLNLAISDFLVGAFCIPLYVPYVLTGRWTFGRGLCKLWLVVDYLLCTSSAFNIVLISYDRFLSVTRAVSYRAQQGDTRRAVRKMLLVWVLAFLLYGPAILSWEYLSGGSSIPEGHCYAEFFYNWYFLITASTLEFFTPFLSVTFFNLSIYLNIQRRTRLRLDGAREAAGPEPPPEAQPSPPPPPGCWGCWQKGHGEAMPLHRYGVGEAAVGAEAGEATLGGGGGGGSVASPTSSSGSSSRGTERPRSLKRGSKPSASSASLEKRMKMVSQSFTQRFRLSRDRKVAKSLAVIVSIFGLCWAPYTLLMIIRAACHGHCVPDYWYETSFWLLWANSAVNPVLYPLCHHSFRRAFTKLLCPQKLKIQPHSSLEHCWK
  
Inhibitor
Name:
BDBM22548
Synonyms:
2-[3-(1H-imidazol-4-ylmethyl)phenyl]-4,4,6-trimethyl-5,6-dihydro-4H-1,3-oxazine | 4-Benzyl-1H-imidazole derivative, 26
Type:
Small organic molecule
Emp. Form.:
C17H21N3O
Mol. Mass.:
283.3681
SMILES:
CC1CC(C)(C)N=C(O1)c1cccc(Cc2cnc[nH]2)c1 |c:6|
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
BDBM22530
Synonyms:
N(alpha)-Methylhistamine | N-alpha-methylhistamine | N-methylhistamine | NAMH | [2-(1H-imidazol-5-yl)ethyl](methyl)amine | [3H]N-alpha-methyl histamine
Type:
radiolabeled ligand
Emp. Form.:
C6H11N3
Mol. Mass.:
125.1716
SMILES:
CNCCc1cnc[nH]1
Structure:
Search PDB for entries with ligand similarity: