# | Aladdin ID | Assay Type | Description | Organism | Compounds | Reference | BAO Format | Source | |
---|---|---|---|---|---|---|---|---|---|
1. | ALA4308446 | B | Inhibition of His-tagged recombinant human ATP-activated TRKA kinase domain (441 to 796 residues) expressed in baculovirus expression system at 10 uM preincubated with enzyme/ATP mixture for 20 mins followed by TK substrate-biotin addition followed by further incubation for 15 mins in presence of ATP by HTRF assay relative to control | Homo sapiens | 120 | ALA4304826 | assay format | Scientific Literature | |
2. | ALA4308447 | B | Inhibition of His-tagged recombinant human ATP-activated TRKA kinase domain (441 to 796 residues) expressed in baculovirus expression system at 1 uM preincubated with enzyme/ATP mixture for 20 mins followed by TK substrate-biotin addition followed by further incubation for 15 mins in presence of ATP by HTRF assay relative to control | Homo sapiens | 120 | ALA4304826 | assay format | Scientific Literature | |
3. | ALA4308448 | B | Inhibition of His-tagged recombinant human ATP-activated TRKA kinase domain (441 to 796 residues) expressed in baculovirus expression system preincubated with enzyme/ATP mixture for 20 mins followed by TK substrate-biotin addition followed by further incubation for 15 mins in presence of ATP by HTRF assay | Homo sapiens | 120 | ALA4304826 | assay format | Scientific Literature | |
4. | ALA4308449 | B | Inhibition of human full length TRKA expressed in CHO cells assessed as decrease in NGF-induced Ca2+ flux by Calcium 4 dye-based FLIPR TETRA assay | Homo sapiens | 113 | ALA4304826 | cell-based format | Scientific Literature | |
5. | ALA4308450 | B | Inhibition of human full length TRKB expressed in CHO cells assessed as decrease in NGF-induced Ca2+ flux by Calcium 4 dye-based FLIPR TETRA assay | Homo sapiens | 114 | ALA4304826 | cell-based format | Scientific Literature | |
6. | ALA4308451 | B | Binding affinity to wild type human biotinylated and N-terminal DYKDDDDK-tagged TrkA kinase domain (436 to 790 residues) expressed in Sf21 cells assessed as association rate constant by single cycle kinetics analysis | Homo sapiens | 2 | ALA4304826 | cell-based format | Scientific Literature | |
7. | ALA4308452 | B | Binding affinity to wild type human biotinylated and N-terminal DYKDDDDK-tagged TrkA kinase domain (436 to 790 residues) expressed in Sf21 cells assessed as dissociation rate constant by single cycle kinetics analysis | Homo sapiens | 2 | ALA4304826 | cell-based format | Scientific Literature | |
8. | ALA4308453 | B | Binding affinity to wild type human biotinylated and N-terminal DYKDDDDK-tagged TrkA kinase domain (436 to 790 residues) expressed in Sf21 cells assessed as equilibrium rate constant by single cycle kinetics analysis | Homo sapiens | 2 | ALA4304826 | cell-based format | Scientific Literature | |
9. | ALA4308454 | B | Binding affinity to wild type human biotinylated and N-terminal DYKDDDDK-tagged TrkA kinase domain (436 to 790 residues) expressed in Sf21 cells assessed as residence time by single cycle kinetics analysis | Homo sapiens | 2 | ALA4304826 | cell-based format | Scientific Literature | |
10. | ALA4308455 | B | Inhibition of human inactive TRKA assessed as decrease in substrate phosphorylation incubated for 2 hrs using CSKtide as substrate in presence of ATP measured every 5 minutes for 5 hrs by caliper method | Homo sapiens | 2 | ALA4304826 | single protein format | Scientific Literature | |
11. | ALA4308456 | B | Inhibition of human active TRKA assessed as decrease in substrate phosphorylation incubated for 2 hrs using CSKtide as substrate in presence of ATP measured every 5 minutes for 5 hrs by caliper method | Homo sapiens | 2 | ALA4304826 | single protein format | Scientific Literature | |
12. | ALA4308458 | B | Selectivity index, ratio of Ki for inhibition of human active TRKA to ratio of Ki for inhibition of inactive TRKA | Homo sapiens | 1 | ALA4304826 | single protein format | Scientific Literature | |
13. | ALA4308459 | A | Half life in Beagle dog plasma at 0.2 mg/kg, iv administered as bolus dose measured for 0.033 to 24 hrs post compound dose by protein precipitation based UPLC-MS/MS analysis | Canis lupus familiaris | 1 | ALA4304826 | organism-based format | Scientific Literature | |
14. | ALA4308460 | A | AUClast in Beagle dog plasma at 0.2 mg/kg, iv administered as bolus dose measured for 0.033 to 24 hrs post compound dose by protein precipitation based UPLC-MS/MS analysis | Canis lupus familiaris | 1 | ALA4304826 | organism-based format | Scientific Literature | |
15. | ALA4308461 | A | AUC (0 to infinity) in Beagle dog plasma at 0.2 mg/kg, iv administered as bolus dose measured for 0.033 to 24 hrs post compound dose by protein precipitation based UPLC-MS/MS analysis | Canis lupus familiaris | 1 | ALA4304826 | organism-based format | Scientific Literature | |
16. | ALA4308462 | A | Volume of distribution at steady state in Beagle dog plasma at 0.2 mg/kg, iv administered as bolus dose measured for 0.033 to 24 hrs post compound dose by protein precipitation based UPLC-MS/MS analysis | Canis lupus familiaris | 1 | ALA4304826 | organism-based format | Scientific Literature | |
17. | ALA4308463 | A | Clearance in Beagle dog plasma at 0.2 mg/kg, iv administered as bolus dose measured for 0.033 to 24 hrs post compound dose by protein precipitation based UPLC-MS/MS analysis | Canis lupus familiaris | 1 | ALA4304826 | organism-based format | Scientific Literature | |
18. | ALA4308464 | A | Cmax in Beagle dog plasma at 3 mg/kg, po measured for 0.033 to 24 hrs post compound dose by protein precipitation based UPLC-MS/MS analysis | Canis lupus familiaris | 1 | ALA4304826 | organism-based format | Scientific Literature | |
19. | ALA4308465 | A | Tmax in Beagle dog plasma at 3 mg/kg, po measured for 0.033 to 24 hrs post compound dose by protein precipitation based UPLC-MS/MS analysis | Canis lupus familiaris | 1 | ALA4304826 | organism-based format | Scientific Literature | |
20. | ALA4308466 | A | Half life in Beagle dog plasma at 3 mg/kg, po measured for 0.033 to 24 hrs post compound dose by protein precipitation based UPLC-MS/MS analysis | Canis lupus familiaris | 1 | ALA4304826 | organism-based format | Scientific Literature |