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Target
Histamine H3 receptor
Ligand
BDBM26229
Substrate
BDBM22530
Meas. Tech.
Radioligand Binding Assay
pH
7.4±n/a
Temperature
298.15±n/a K
Ki
1288±118 nM
Citation
 Altenbach, RJ; Adair, RM; Bettencourt, BM; Black, LA; Fix-Stenzel, SR; Gopalakrishnan, SM; Hsieh, GC; Liu, H; Marsh, KC; McPherson, MJ; Milicic, I; Miller, TR; Vortherms, TA; Warrior, U; Wetter, JM; Wishart, N; Witte, DG; Honore, P; Esbenshade, TA; Hancock, AA; Brioni, JD; Cowart, MD Structure-activity studies on a series of a 2-aminopyrimidine-containing histamine H4 receptor ligands. J Med Chem 51:6571-80 (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:
BDBM26229
Synonyms:
2-Aminopyrimidine analog., 4 | 4-[2-amino-6-(4-methylpiperazin-1-yl)pyrimidin-4-yl]benzonitrile | JMC516547 Compound 2
Type:
Small organic molecule
Emp. Form.:
C16H18N6
Mol. Mass.:
294.3543
SMILES:
CN1CCN(CC1)c1cc(nc(N)n1)-c1ccc(cc1)C#N
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: