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Target
Histamine H3 receptor
Ligand
BDBM50354216
Substrate
n/a
Meas. Tech.
ChEMBL_819069 (CHEMBL2034391)
Ki
0.4±n/a nM
Citation
 Zhou, D; Gross, JL; Adedoyin, AB; Aschmies, SB; Brennan, J; Bowlby, M; Di, L; Kubek, K; Platt, BJ; Wang, Z; Zhang, G; Brandon, N; Comery, TA; Robichaud, AJ 2-(Pyrrolidin-1-yl)ethyl-3,4-dihydroisoquinolin-1(2H)-one derivatives as potent and selective histamine-3 receptor antagonists. J Med Chem 55:2452-68 (2012) [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:
BDBM50354216
Synonyms:
CHEMBL1836004
Type:
Small organic molecule
Emp. Form.:
C23H26N4O
Mol. Mass.:
374.4787
SMILES:
Cc1nc2ccccc2n1-c1ccc(cc1)C(=O)N1CC[C@@H](C1)N1CCCC1 |r|
Structure:
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