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Target
Histamine H1 receptor
Ligand
BDBM86187
Substrate
n/a
Ki
4±n/a nM
Comments
PDSP_1850
Citation
 Kroeze, WK; Hufeisen, SJ; Popadak, BA; Renock, SM; Steinberg, S; Ernsberger, P; Jayathilake, K; Meltzer, HY; Roth, 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:
BDBM86187
Synonyms:
CAS_22189-31-7 | NSC_5454 | THIOTHIXENE
Type:
Small organic molecule
Emp. Form.:
C23H29N3O2S2
Mol. Mass.:
443.625
SMILES:
CN(C)S(=O)(=O)c1ccc2Sc3ccccc3C(=CCCN3CCN(C)CC3)c2c1 |w:18.19|
Structure:
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