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Target
Histamine H1 receptor
Ligand
BDBM35255
Substrate
n/a
Meas. Tech.
ChEMBL_84427 (CHEMBL691615)
Ki
3.4±n/a nM
Citation
 Wermuth, CG Selective optimization of side activities: another way for drug discovery. J Med Chem 47:1303-14 (2004) [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:
BDBM35255
Synonyms:
2-Chlor-11-(2-dimethylaminoaethoxy)-dibenzo(b,f)-thiepin | 2-Chloro-11-(2-(dimethylamino)ethoxy)dibenzo(b,f)thiepin | 2-[(8-chlorodibenzo[b,f]thiepin-10-yl)oxy]-N,N-dimethylethanamine | CHEMBL285802 | Nipolept | Zoleptil | zotepine
Type:
Small organic molecule
Emp. Form.:
C18H18ClNOS
Mol. Mass.:
331.86
SMILES:
CN(C)CCOC1=Cc2ccccc2Sc2ccc(Cl)cc12 |t:6|
Structure:
Search PDB for entries with ligand similarity: