Reaction Details |
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Target | Histamine H1 receptor |
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Ligand | BDBM50394125 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_856370 (CHEMBL2160725) |
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Ki | 63.1±n/a nM |
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Citation | Bahl, A; Barton, P; Bowers, K; Caffrey, MV; Denton, R; Gilmour, P; Hawley, S; Linannen, T; Luckhurst, CA; Mochel, T; Perry, MW; Riley, RJ; Roe, E; Springthorpe, B; Stein, L; Webborn, P Scaffold-hopping with zwitterionic CCR3 antagonists: identification and optimisation of a series with good potency and pharmacokinetics leading to the discovery of AZ12436092. Bioorg Med Chem Lett22:6694-9 (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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BDBM50394125 |
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n/a |
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Name | BDBM50394125 |
Synonyms: | CHEMBL2158775 |
Type | Small organic molecule |
Emp. Form. | C27H34Cl2N2O4 |
Mol. Mass. | 521.476 |
SMILES | COc1ccccc1C[C@H](N1CCC(CN2CCC(CC2)Oc2ccc(Cl)c(Cl)c2)CC1)C(O)=O |r| |
Structure |
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