Target
Histamine H1 receptor
Ligand
BDBM50516710
Substrate
n/a
Meas. Tech.
ChEMBL_1866568 (CHEMBL4367543)
Ki
0.416869±n/a nM
Citation
 Bosma, RWang, ZKooistra, AJBushby, NKuhne, Svan den Bor, JWaring, MJde Graaf, Cde Esch, IJVischer, HFSheppard, RJWijtmans, MLeurs, R Route to Prolonged Residence Time at the Histamine H J Med Chem 62:6630-6644 (2019) [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:
BDBM50516710
Synonyms:
CHEMBL4469024
Type:
Small organic molecule
Emp. Form.:
C21H23ClN2
Mol. Mass.:
338.874
SMILES:
[#6]-[#6]-[#7]-1-[#6]-[#6]\[#6](-[#6]-[#6]-1)=[#6]-1\c2ccc(Cl)cc2-[#6]-[#6]-c2cccnc-12
Structure:
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