Reaction Details |
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Target | Histamine H1 receptor |
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Ligand | BDBM22567 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1651916 (CHEMBL4001171) |
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IC50 | 1.9±n/a nM |
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Citation | Odell, LR; Abdel-Hamid, MK; Hill, TA; Chau, N; Young, KA; Deane, FM; Sakoff, JA; Andersson, S; Daniel, JA; Robinson, PJ; McCluskey, A Pyrimidine-Based Inhibitors of Dynamin I GTPase Activity: Competitive Inhibition at the Pleckstrin Homology Domain. J Med Chem60:349-361 (2017) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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Histamine H1 receptor |
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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: | MSLPNSSCLLEDKMCEGNKTTMASPQLMPLVVVLSTICLVTVGLNLLVLYAVRSERKLHT
VGNLYIVSLSVADLIVGAVVMPMNILYLLMSKWSLGRPLCLFWLSMDYVASTASIFSVFI
LCIDRYRSVQQPLRYLKYRTKTRASATILGAWFLSFLWVIPILGWNHFMQQTSVRREDKC
ETDFYDVTWFKVMTAIINFYLPTLLMLWFYAKIYKAVRQHCQHRELINRSLPSFSEIKLR
PENPKGDAKKPGKESPWEVLKRKPKDAGGGSVLKSPSQTPKEMKSPVVFSQEDDREVDKL
YCFPLDIVHMQAAAEGSSRDYVAVNRSHGQLKTDEQGLNTHGASEISEDQMLGDSQSFSR
TDSDTTTETAPGKGKLRSGSNTGLDYIKFTWKRLRSHSRQYVSGLHMNRERKAAKQLGFI
MAAFILCWIPYFIFFMVIAFCKNCCNEHLHMFTIWLGYINSTLNPLIYPLCNENFKKTFK
RILHIRS
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BDBM22567 |
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n/a |
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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 |
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