| Assay Method Information | |
| | SAR analysis counterscreen of small molecule antagonists of the CCR6 receptor using an APJ receptor luminescent beta-arrestin assay |
| Description: | Data Source: Sanford-Burnham Center for Chemical Genomics (SBCCG) Source Affiliation: Sanford-Burnham Medical Research Institute(SBMRI, San Diego, CA) Network: NIH Molecular Libraries Probe Production Centers Network (MLPCN) Grant Number: R21 NS064746-01A Assay Provider: Dr. Greg Roth, Sanford-Burnham Medical Research Institute This assay was developed and performed as a counter assay for the primary assay originally identified as "uHTS identification of small molecule antagonists of the CCR6 receptor via a luminescent beta-arrestin assay", AID 493098. Compounds are either acquired from commercial sources or synthesized internally. A probe that is selective against APJ (within equipotent range as defined by a >10-fold difference in IC50) is desired. In this description we utilize enzyme-fragment complementation to directly measure GPCR activation. Unlike imaging or other second messenger assays, the DiscoveRx b-Arrestin assay allows for a direct measure of GPCR activation by detect |
| Affinity data for this assay | |
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