Reaction Details |
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Target | Histamine H1 receptor |
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Ligand | BDBM50360996 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_796225 (CHEMBL1938190) |
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Ki | 4.9±n/a nM |
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Citation | Ravula, SB; Yu, J; Tran, JA; Arellano, M; Tucci, FC; Moree, WJ; Li, BF; Petroski, RE; Wen, J; Malany, S; Hoare, SR; Madan, A; Crowe, PD; Beaton, G Lead optimization of 2-(piperidin-3-yl)-1H-benzimidazoles: identification of 2-morpholin- and 2-thiomorpholin-2-yl-1H-benzimidazoles as selective and CNS penetrating H¿?-antihistamines for insomnia. Bioorg Med Chem Lett22:421-6 (2011) [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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BDBM50360996 |
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n/a |
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Name | BDBM50360996 |
Synonyms: | CHEMBL1935433 |
Type | Small organic molecule |
Emp. Form. | C26H31FN4O |
Mol. Mass. | 434.5489 |
SMILES | Fc1ccc(Cn2c(nc3ccccc23)C2CCCN(CC(=O)N3CCCCC3)C2)cc1 |
Structure |
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