| Assay Method Information | |
| | GFP-NFAT translocation assay |
| Description: | Using the GFP-NFAT translocation assay method, the inhibitory activity of the selected compounds at 200 μM concentration was evaluated. As demonstrated in Table 2, several compounds showed good inhibition of CRAC channel, for example, Compounds 53, 62, 65, and 66. Then, IC50 values were calculated, with Compound 53 having the lowest IC50 at 8.14 μM. This IC50 value demonstrates an order of magnitude, e.g., about tenfold, improvement compared to the IC50 of the lead Compound 41 (shown in Table 1). Based on the result, a series of Compound 53 analogues was designed and synthesized de novo. |
| Affinity data for this assay | |
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