Reaction Details |
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Target | Histamine H1 receptor |
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Ligand | BDBM50341448 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_848010 (CHEMBL2150561) |
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Ki | 1.2±n/a nM |
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Citation | Procopiou, PA; Browning, C; Gore, PM; Lynn, SM; Richards, SA; Slack, RJ; Sollis, SL Synthesis and pharmacological investigation of azaphthalazinone human histamine H(1) receptor antagonists. Bioorg Med Chem20:6097-108 (2012) [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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BDBM50341448 |
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n/a |
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Name | BDBM50341448 |
Synonyms: | 4-(4-Chloro-benzyl)-2-(1-methyl-azepan-4-yl)-2H-phthalazin-1-one | AZELASTINE | Astelin | Astepro | CHEMBL639 | Optilast | Optivar | Rhinolast | US20230414632, Compound II-a | rac-Azelastine |
Type | Small organic molecule |
Emp. Form. | C22H24ClN3O |
Mol. Mass. | 381.898 |
SMILES | CN1CCCC(CC1)n1nc(Cc2ccc(Cl)cc2)c2ccccc2c1=O |
Structure |
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