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Target
Histamine H1 receptor
Ligand
BDBM22567
Substrate
n/a
Meas. Tech.
ChEMBL_1624854 (CHEMBL3867266)
Ki
1.3±n/a nM
Citation
Kuhne, S; Kooistra, AJ; Bosma, R; Bortolato, A; Wijtmans, M; Vischer, HF; Mason, JS; de Graaf, C; de Esch, IJ; Leurs, R Identification of Ligand Binding Hot Spots of the Histamine H J Med Chem 59:9047-9061 (2016) [PubMed] Article
More Info.:
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:
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