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Target
Histamine H1 receptor
Ligand
BDBM50316938
Substrate
n/a
Meas. Tech.
ChEMBL_796225 (CHEMBL1938190)
Ki
0.5±n/a nM
Citation
 Ravula, SB; Yu, J; Tran, JA; Arellano, M; Tucci, FC; Moree, WJ; Li, BF; Petroski, RE; Wen, J; Malany, S; Hoare, SR; Madan, A; Crowe, PD; Beaton, G Lead optimization of 2-(piperidin-3-yl)-1H-benzimidazoles: identification of 2-morpholin- and 2-thiomorpholin-2-yl-1H-benzimidazoles as selective and CNS penetrating H¿?-antihistamines for insomnia. Bioorg Med Chem Lett 22:421-6 (2011) [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:
BDBM50316938
Synonyms:
1-(4-fluorobenzyl)-2-(1-methylpiperidin-3-yl)-1H-benzo[d]imidazole | CHEMBL1087089
Type:
Small organic molecule
Emp. Form.:
C20H22FN3
Mol. Mass.:
323.4072
SMILES:
CN1CCCC(C1)c1nc2ccccc2n1Cc1ccc(F)cc1
Structure:
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