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Target
Histamine H1 receptor
Ligand
BDBM22914
Substrate
BDBM22567
Meas. Tech.
Radioligand Binding Assay
pH
7.4±n/a
Temperature
298.15±n/a K
Ki
>10000±n/a nM
Citation
 Zhao, C; Sun, M; Bennani, YL; Gopalakrishnan, SM; Witte, DG; Miller, TR; Krueger, KM; Browman, KE; Thiffault, C; Wetter, J; Marsh, KC; Hancock, AA; Esbenshade, TA; Cowart, MD The alkaloid conessine and analogues as potent histamine H3 receptor antagonists. J Med Chem 51:5423-30 (2008) [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:
BDBM22914
Synonyms:
CHEMBL260374 | N-cyclohexyl-4-(1H-imidazol-5-yl)piperidine-1-carbothioamide | Thioperamide | US11622967, Compound Thioperamide
Type:
Small organic molecule
Emp. Form.:
C15H24N4S
Mol. Mass.:
292.443
SMILES:
S=C(NC1CCCCC1)N1CCC(CC1)c1cnc[nH]1
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
BDBM22567
Synonyms:
3H]pyrilamine | CHEMBL511 | Dorantamin | Mepyramine | N-(4-methoxybenzyl)-N ,N -dimethyl-N-pyridin-2-ylethane-1,2-diamine | N-[2-(dimethylamino)ethyl]-N-[(4-methoxyphenyl)methyl]pyridin-2-amine | PYRILAMINE | Pyranisamine | [3H]mepyramine | [3H]pyrilamine
Type:
radiolabeled ligand
Emp. Form.:
C17H23N3O
Mol. Mass.:
285.384
SMILES:
COc1ccc(CN(CCN(C)C)c2ccccn2)cc1
Structure:
Search PDB for entries with ligand similarity: