Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
EC50 (functional) | > 20 uM | Agonist activity at rat GLP1R expressed in HEK293 cells assessed as stimulation of cAMP levels incubated for 6 hrs by multiple response element/cAMP response element (MRE/CRE)-driven reporter gene assay | ChEMBL. | 22103243 |
Efficacy (functional) | < 15 % | Agonist activity at rat GLP1R expressed in HEK293 cells assessed as stimulation of cAMP levels incubated for 6 hrs by multiple response element/cAMP response element (MRE/CRE)-driven reporter gene assay relative to 10 nM GLP1 | ChEMBL. | 22103243 |
IC50 (binding) | > 20 uM | Inhibition of [125I]GLP1 (7-36) amide binding to rat GLP1R expressed in HEK293 cells | ChEMBL. | 22103243 |
Inhibition (binding) | < 15 % | Inhibition of [125I]Exendin (9-39) binding to rat GLP1R expressed in HEK293 cells | ChEMBL. | 22103243 |
Inhibition (binding) | < 15 % | Inhibition of [125I]GLP1 (7-36) amide binding to rat GLP1R expressed in HEK293 cells relative to untreated control | ChEMBL. | 22103243 |
Many chemical entities in TDR Targets come from high-throughput screenings with whole cells or tissue samples, and not all assayed compounds have been tested against a single a single target protein, probably because they get ruled out during screening process. Even if these compounds may have not been of interest in the original screening, they may come as interesting leads for other screening assays. Furthermore, we may be able to propose drug-target associations using chemical similarities and network patterns.