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Target
Histamine H1 receptor
Ligand
BDBM50315348
Substrate
n/a
Meas. Tech.
ChEMBL_625973 (CHEMBL1103492)
IC50
>30000±n/a nM
Citation
 Cramp, S; Dyke, HJ; Higgs, C; Clark, DE; Gill, M; Savy, P; Jennings, N; Price, S; Lockey, PM; Norman, D; Porres, S; Wilson, F; Jones, A; Ramsden, N; Mangano, R; Leggate, D; Andersson, M; Hale, R Identification and hit-to-lead exploration of a novel series of histamine H4 receptor inverse agonists. Bioorg Med Chem Lett 20:2516-9 (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:
BDBM50315348
Synonyms:
(R)-8-chloro-4-(3-(methylamino)pyrrolidin-1-yl)benzofuro[3,2-d]pyrimidin-2-amine | CHEMBL1091874
Type:
Small organic molecule
Emp. Form.:
C15H16ClN5O
Mol. Mass.:
317.773
SMILES:
CN[C@@H]1CCN(C1)c1nc(N)nc2c3cc(Cl)ccc3oc12 |r|
Structure:
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