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Target
Histamine H3 receptor
Ligand
BDBM50232355
Substrate
n/a
Meas. Tech.
ChEMBL_491620 (CHEMBL945391)
Ki
1±n/a nM
Citation
 Santora, VJ; Covel, JA; Hayashi, R; Hofilena, BJ; Ibarra, JB; Pulley, MD; Weinhouse, MI; Semple, G; Ren, A; Pereira, G; Edwards, JE; Suarez, M; Frazer, J; Thomsen, W; Hauser, E; Lorea, J; Grottick, AJ Novel H3 receptor antagonists with improved pharmacokinetic profiles. Bioorg Med Chem Lett 18:4133-6 (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:
BDBM50232355
Synonyms:
(3aR,6aR)-2-(cyclopropylmethyl)-6-(4-(2-(pyrrolidin-1-yl)ethyl)phenyl)-1,2,3,3a,4,6a-hexahydrocyclopenta[c]pyrrole | CHEMBL408934
Type:
Small organic molecule
Emp. Form.:
C23H32N2
Mol. Mass.:
336.5136
SMILES:
C(Cc1ccc(cc1)C1=CC[C@H]2CN(CC3CC3)C[C@@H]12)N1CCCC1 |r,t:9|
Structure:
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