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Target
Histamine H3 receptor
Ligand
BDBM50200646
Substrate
n/a
Meas. Tech.
ChEMBL_453774 (CHEMBL885775)
Ki
0.22±n/a nM
Citation
 Black, LA; Nersesian, DL; Sharma, P; Ku, YY; Bennani, YL; Marsh, KC; Miller, TR; Esbenshade, TA; Hancock, AA; Cowart, M 4-[6-(2-Aminoethyl)naphthalen-2-yl]benzonitriles are potent histamine H3 receptor antagonists with high CNS penetration. Bioorg Med Chem Lett 17:1443-6 (2007) [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:
BDBM50200646
Synonyms:
4'-[3-((R)-2-methyl-pyrrolidin-1-yl)-propoxy]-biphenyl-4-carbonitrile | CHEMBL247953
Type:
Small organic molecule
Emp. Form.:
C21H24N2O
Mol. Mass.:
320.4281
SMILES:
C[C@@H]1CCCN1CCCOc1ccc(cc1)-c1ccc(cc1)C#N
Structure:
Search PDB for entries with ligand similarity: