Species | Target name | Source | Bibliographic reference |
---|---|---|---|
Homo sapiens | adrenoceptor beta 3 | Starlite/ChEMBL | References |
Homo sapiens | adrenoceptor beta 2, surface | Starlite/ChEMBL | References |
Homo sapiens | adrenoceptor beta 1 | Starlite/ChEMBL | References |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
Activity (functional) | = 4 % | Agonist activity at human beta3 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation at 10 uM after 5 hrs relative to isoprenaline | ChEMBL. | 23614528 |
Activity (functional) | = 15.3 % | Agonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as induction of 3H]cAMP accumulation at 10 uM after 5 hrs relative to isoprenaline | ChEMBL. | 23614528 |
Activity (functional) | = 28.3 % | Partial agonist activity at human beta1 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation measured after 5 hrs relative to isoprenaline | ChEMBL. | 23614528 |
EC50 (functional) | = 8.35 | Partial agonist activity at human beta1 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrs | ChEMBL. | 23614528 |
EC50 (functional) | = 10 uM | Agonist activity at human beta3 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrs | ChEMBL. | 23614528 |
EC50 (functional) | = 10 uM | Agonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrs | ChEMBL. | 23614528 |
Kd (binding) | = 5.58 | Displacement of [3H]-CGP12177 from human beta2 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysis | ChEMBL. | 23614528 |
Kd (functional) | = 5.92 | Antagonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as inhibition of cimaterol-induced [3H]cAMP accumulation incubated for 15 mins prior to cimaterol induction measured after 5 hrs | ChEMBL. | 23614528 |
Kd (binding) | = 7.91 | Displacement of [3H]-CGP12177 from human beta1 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysis | ChEMBL. | 23614528 |
Kd (functional) | = 8.46 | Antagonist activity at human beta1 adrenoceptor expressed in CHOK1 cells assessed as inhibition of cimaterol-induced [3H]cAMP accumulation incubated for 15 mins prior to cimaterol induction measured after 5 hrs | ChEMBL. | 23614528 |
Kd (functional) | > 10 uM | Antagonist activity at human beta3 adrenoceptor expressed in CHOK1 cells assessed as inhibition of cimaterol-induced [3H]cAMP accumulation incubated for 15 mins prior to cimaterol induction measured after 5 hrs | ChEMBL. | 23614528 |
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.
1 literature reference was collected for this gene.