Target
Histamine H1 receptor
Ligand
BDBM78433
Substrate
n/a
Ki
21±n/a nM
Comments
PDSP_837
Citation
 Kroeze, WKHufeisen, SJPopadak, BARenock, SMSteinberg, SErnsberger, PJayathilake, KMeltzer, HYRoth, BL H1-histamine receptor affinity predicts short-term weight gain for typical and atypical antipsychotic drugs. Neuropsychopharmacology 28:519-26 (2003) [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:
BDBM78433
Synonyms:
2-[4-[3-[2-(trifluoromethyl)-10-phenothiazinyl]propyl]-1-piperazinyl]ethanol;hydrochloride | 2-[4-[3-[2-(trifluoromethyl)phenothiazin-10-yl]propyl]piperazin-1-yl]ethanol;hydrochloride | 2-[4-[3-[2-(trifluoromethyl)phenothiazin-10-yl]propyl]piperazino]ethanol;hydrochloride | FLUPHENAZINE | FLUPHENAZINE HYDROCHLORIDE | MLS001076508 | SMR000058411 | cid_3372 | cid_6602611 | med.21724, Compound 17
Type:
Small organic molecule
Emp. Form.:
C22H26F3N3OS
Mol. Mass.:
437.522
SMILES:
OCCN1CCN(CCCN2c3ccccc3Sc3ccc(cc23)C(F)(F)F)CC1
Structure:
Search PDB for entries with ligand similarity: