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Target
Histamine H1 receptor
Ligand
BDBM50018019
Substrate
n/a
Meas. Tech.
ChEMBL_1366831 (CHEMBL3297341)
Ki
69±n/a nM
Citation
 Kolaczkowski, M; Marcinkowska, M; Bucki, A; Pawlowski, M; Mitka, K; Jaskowska, J; Kowalski, P; Kazek, G; Siwek, A; Wasik, A; Wesolowska, A; Mierzejewski, P; Bienkowski, P Novel arylsulfonamide derivatives with 5-HT6/5-HT7 receptor antagonism targeting behavioral and psychological symptoms of dementia. J Med Chem 57:4543-57 (2014) [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:
BDBM50018019
Synonyms:
CHEMBL3290012
Type:
Small organic molecule
Emp. Form.:
C24H26FN3O3S2
Mol. Mass.:
487.61
SMILES:
Fc1ccc2c(noc2c1)C1CCN(CCCCNS(=O)(=O)c2cc3ccccc3s2)CC1
Structure:
Search PDB for entries with ligand similarity: