Target
Histamine H1 receptor
Ligand
BDBM27213
Substrate
n/a
Ki
>10000±n/a nM
Comments
PDSP_2989
Citation
 Esbenshade, TAFox, GBKrueger, KMMiller, TRKang, CHDenny, LIWitte, DGYao, BBPan, LWetter, JMarsh, KBennani, YLCowart, MDSullivan, JPHancock, AA Pharmacological properties of ABT-239 [4-(2-{2-[(2R)-2-Methylpyrrolidinyl]ethyl}-benzofuran-5-yl)benzonitrile]: I. Potent and selective histamine H3 receptor antagonist with drug-like properties. J Pharmacol Exp Ther 313:165-75 (2005) [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:
BDBM27213
Synonyms:
4-[3-(4-cyclopropanecarbonylphenoxy)propyl]-1H-imidazole | CHEMBL14638 | CHEMBL1795025 | Ciproxifan
Type:
Small organic molecule
Emp. Form.:
C16H18N2O2
Mol. Mass.:
270.3263
SMILES:
O=C(C1CC1)c1ccc(OCCCc2cnc[nH]2)cc1
Structure:
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