Reaction Details |
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Target | Histamine H1 receptor |
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Ligand | BDBM50440737 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_986340 (CHEMBL2433831) |
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Ki | 1420±n/a nM |
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Citation | Peddibhotla, S; Hedrick, MP; Hershberger, P; Maloney, PR; Li, Y; Milewski, M; Gosalia, P; Gray, W; Mehta, A; Sugarman, E; Hood, B; Suyama, E; Nguyen, K; Heynen-Genel, S; Vasile, S; Salaniwal, S; Stonich, D; Su, Y; Mangravita-Novo, A; Vicchiarelli, M; Roth, GP; Smith, LH; Chung, TD; Hanson, GR; Thomas, JB; Caron, MG; Barak, LS; Pinkerton, AB Discovery of ML314, a Brain Penetrant Non-Peptidic?-Arrestin Biased Agonist of the Neurotensin NTR1 Receptor. ACS Med Chem Lett4:846-851 (2013) [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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BDBM50440737 |
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n/a |
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Name | BDBM50440737 |
Synonyms: | CHEMBL2431120 |
Type | Small organic molecule |
Emp. Form. | C24H28N4O3 |
Mol. Mass. | 420.5041 |
SMILES | COc1ccccc1N1CCN(CC1)c1nc(nc2cc(OC)c(OC)cc12)C1CC1 |
Structure |
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