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Target
Histamine H1 receptor
Ligand
BDBM50305270
Substrate
n/a
Meas. Tech.
ChEMBL_603320 (CHEMBL1038010)
IC50
98±n/a nM
Citation
 Ivachtchenko, AV; Frolov, EB; Mitkin, OD; Tkachenko, SE; Okun, IM; Khvat, AV Synthesis and biological activity of 5-styryl and 5-phenethyl-substituted 2,3,4,5-tetrahydro-1H-pyrido[4,3-b]indoles. Bioorg Med Chem Lett 20:78-82 (2010) [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:
BDBM50305270
Synonyms:
2,8-Dimethyl-5-[2-(4-trifluoromethylphenyl)ethyl]-2,3,4,5-tetrahydro-1H-pyrido[4,3-b]indole | CHEMBL606036
Type:
Small organic molecule
Emp. Form.:
C22H23F3N2
Mol. Mass.:
372.4266
SMILES:
CN1CCc2c(C1)c1cc(C)ccc1n2CCc1ccc(cc1)C(F)(F)F
Structure:
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