Activity Assay:Article Title: Benzo 2-azaspiro[4.4]nonane compound and use thereof
Article Snippet: .. Activity analysis of the compound was carried out by using CBIS data analysis kit (ChemInnovation, CAA); 2. calculation formula: % activity=100%×(average test sample RLU−average vehicle RLU)/(average maximum control ligand−average vehicle RLU) Experimental results are shown in Table 1: TABLE 1 S1PR1 agonistic activity test results Sample for test S1PR1 agonistic activity, Emax Compound 1 0.137 nM, 122% Compound 3 0.129 nM, 88.6% Compound 4 0.107 nM, 99.4% Compound 5 0.0688 nM, 85.1% Hydrochloride of compound 6 0.865 nM, 115% Compound 7 0.123 nM, 90.7% Compound 8 0.188 nM, 96.8% Compound 9 2.15 nM, 75.8% Compound 10 1.31 nM, 101% Compound 11 1.78 nM, 84.6% Compound 12 0.477 nM, 87.6% Compound 13 10.7 nM, 77.8% Compound 14 1.59 nM, 82.2% Compound 15 2.20 nM, 98.9% Compound 16 14.4 nM, 77.8% Compound 17 8.59 nM, 80.8% Compound 18 4.06 nM, 84.2% Compound 19 3.25 nM, 77.8% Compound 20 9.39 nM, 90.4% Compound 21 21.7 nM, 70.8% Hydrochloride of compound 22 0.0754 nM, 118% Hydrochloride of compound 23 0.0353 nM, 68.3% Hydrochloride of compound 24 4.99 nM, 87.1% Hydrochloride of compound 25 11.5 nM, 82.1% Hydrochloride of compound 26 4.47 nM, 73.8% Hydrochloride of compound 27 9.78 nM, 63.4% Hydrochloride of compound 28 1.32 nM, 77.7% Hydrochloride of compound 37 0.047 nM, 94.1% Hydrochloride of compound 38 0.041 nM, 100.3% Hydrochloride of compound 39 3.46 nM, 144.2% Compound 40 2.82 nM, 101.8% Hydrochloride of compound 43 0.10 nM, 107.7% Hydrochloride of compound 44 0.72 nM, 104.3% Compound 45 0.29 nM, 125.5% Hydrochloride of compound 46 5.76 nM, 104.8% Conclusion: the compounds of the present disclosure all have significant or even unexpected S1PR1 agonistic activity. ..
Control:Article Title: Benzo 2-azaspiro[4.4]nonane compound and use thereof
Article Snippet: .. Activity analysis of the compound was carried out by using CBIS data analysis kit (ChemInnovation, CAA); 2. calculation formula: % activity=100%×(average test sample RLU−average vehicle RLU)/(average maximum control ligand−average vehicle RLU) Experimental results are shown in Table 1: TABLE 1 S1PR1 agonistic activity test results Sample for test S1PR1 agonistic activity, Emax Compound 1 0.137 nM, 122% Compound 3 0.129 nM, 88.6% Compound 4 0.107 nM, 99.4% Compound 5 0.0688 nM, 85.1% Hydrochloride of compound 6 0.865 nM, 115% Compound 7 0.123 nM, 90.7% Compound 8 0.188 nM, 96.8% Compound 9 2.15 nM, 75.8% Compound 10 1.31 nM, 101% Compound 11 1.78 nM, 84.6% Compound 12 0.477 nM, 87.6% Compound 13 10.7 nM, 77.8% Compound 14 1.59 nM, 82.2% Compound 15 2.20 nM, 98.9% Compound 16 14.4 nM, 77.8% Compound 17 8.59 nM, 80.8% Compound 18 4.06 nM, 84.2% Compound 19 3.25 nM, 77.8% Compound 20 9.39 nM, 90.4% Compound 21 21.7 nM, 70.8% Hydrochloride of compound 22 0.0754 nM, 118% Hydrochloride of compound 23 0.0353 nM, 68.3% Hydrochloride of compound 24 4.99 nM, 87.1% Hydrochloride of compound 25 11.5 nM, 82.1% Hydrochloride of compound 26 4.47 nM, 73.8% Hydrochloride of compound 27 9.78 nM, 63.4% Hydrochloride of compound 28 1.32 nM, 77.7% Hydrochloride of compound 37 0.047 nM, 94.1% Hydrochloride of compound 38 0.041 nM, 100.3% Hydrochloride of compound 39 3.46 nM, 144.2% Compound 40 2.82 nM, 101.8% Hydrochloride of compound 43 0.10 nM, 107.7% Hydrochloride of compound 44 0.72 nM, 104.3% Compound 45 0.29 nM, 125.5% Hydrochloride of compound 46 5.76 nM, 104.8% Conclusion: the compounds of the present disclosure all have significant or even unexpected S1PR1 agonistic activity. ..
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