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Target
Histamine H1 receptor
Ligand
BDBM50383163
Substrate
n/a
Meas. Tech.
ChEMBL_819073 (CHEMBL2034395)
Ki
8750±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 H1 receptor
Synonyms:
H1R | HH1R | HISTAMINE H1 | HRH1 | HRH1_HUMAN
Type:
G Protein-Coupled Receptor (GPCR)
Mol. Mass.:
55808.72
Organism:
Homo sapiens (Human)
Description:
Cell pellets from SK-N-MC cells transfected with human H1 receptor were used in binding assay.
Residue:
487
Sequence:
MSLPNSSCLLEDKMCEGNKTTMASPQLMPLVVVLSTICLVTVGLNLLVLYAVRSERKLHTVGNLYIVSLSVADLIVGAVVMPMNILYLLMSKWSLGRPLCLFWLSMDYVASTASIFSVFILCIDRYRSVQQPLRYLKYRTKTRASATILGAWFLSFLWVIPILGWNHFMQQTSVRREDKCETDFYDVTWFKVMTAIINFYLPTLLMLWFYAKIYKAVRQHCQHRELINRSLPSFSEIKLRPENPKGDAKKPGKESPWEVLKRKPKDAGGGSVLKSPSQTPKEMKSPVVFSQEDDREVDKLYCFPLDIVHMQAAAEGSSRDYVAVNRSHGQLKTDEQGLNTHGASEISEDQMLGDSQSFSRTDSDTTTETAPGKGKLRSGSNTGLDYIKFTWKRLRSHSRQYVSGLHMNRERKAAKQLGFIMAAFILCWIPYFIFFMVIAFCKNCCNEHLHMFTIWLGYINSTLNPLIYPLCNENFKKTFKRILHIRS
  
Inhibitor
Name:
BDBM50383163
Synonyms:
CHEMBL2031885
Type:
Small organic molecule
Emp. Form.:
C27H33N3O2
Mol. Mass.:
431.5698
SMILES:
C[C@@H]1CCCN1CCN1CCc2cc(ccc2C1=O)-c1ccc(cc1)C(=O)N1CCCC1 |r|
Structure:
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