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Target
Histamine H1 receptor
Ligand
BDBM50397498
Substrate
n/a
Meas. Tech.
ChEMBL_862026 (CHEMBL2173976)
Ki
7.94±n/a nM
Citation
 Bahl, A; Barton, P; Bowers, K; Brough, S; Evans, R; Luckhurst, CA; Mochel, T; Perry, MW; Rigby, A; Riley, RJ; Sanganee, H; Sisson, A; Springthorpe, B The discovery of CCR3/H1 dual antagonists with reduced hERG risk. Bioorg Med Chem Lett 22:6688-93 (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:
BDBM50397498
Synonyms:
CHEMBL2171043
Type:
Small organic molecule
Emp. Form.:
C23H26Cl3N3O4S
Mol. Mass.:
546.894
SMILES:
Clc1cccc(c1)S(=O)(=O)NC(=O)N1CCC(CC1)N1CCC(CC1)Oc1ccc(Cl)c(Cl)c1
Structure:
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