# | Aladdin ID | Assay Type | Description | Organism | Compounds | Reference | BAO Format | Source | |
---|---|---|---|---|---|---|---|---|---|
1. | ALA5167383 | B | Binding affinity to wild-type human partial length RIOK2 (M1 to D313 residues) expressed in mammalian expression system assessed as dissociation constant by KINOMEscan assay | Homo sapiens | 22 | ALA5154917 | assay format | Scientific Literature | |
2. | ALA5167384 | B | Binding affinity to wild-type human partial length RIOK2 (M1 to D313 residues) expressed in mammalian expression system assessed as residual activity at 1 uM by KINOMEscan assay relative to control | Homo sapiens | 1 | ALA5154917 | assay format | Scientific Literature | |
3. | ALA5167385 | B | Binding affinity to wild-type human full length RIOK1 (M1 to K568 residues) expressed in bacterial expression system assessed as residual activity at 1 uM by KINOMEscan assay relative to control | Homo sapiens | 1 | ALA5154917 | assay format | Scientific Literature | |
4. | ALA5167386 | B | Binding affinity to wild-type human full length RIOK3 (M1 to E519 residues) expressed in bacterial expression system assessed as residual activity at 1 uM by KINOMEscan assay relative to control | Homo sapiens | 1 | ALA5154917 | assay format | Scientific Literature | |
5. | ALA5167387 | B | Binding affinity to human partial length FLT3 ITD D835V mutant expressed in mammalian expression system assessed as residual activity at 1 uM by KINOMEscan assay relative to control | Homo sapiens | 1 | ALA5154917 | assay format | Scientific Literature | |
6. | ALA5167388 | B | Binding affinity to human partial length FLT3 ITD F691L mutant expressed in mammalian expression system assessed as residual activity at 1 uM by KINOMEscan assay relative to control | Homo sapiens | 1 | ALA5154917 | assay format | Scientific Literature | |
7. | ALA5167389 | B | Binding affinity to human partial length FLT3 D835V mutant (V592 to Y969 residues) expressed in mammalian expression system assessed as residual activity at 1 uM by KINOMEscan assay relative to control | Homo sapiens | 1 | ALA5154917 | assay format | Scientific Literature | |
8. | ALA5167390 | B | Inhibition of N-terminal hexahistidine-SUMO-tagged human full length RIOK2 (residues 1 to 321) expressed in Escherichia coli BL21 (DE3) incubated for 30 mins in presence of ATP by ADP-Glo assay | Homo sapiens | 1 | ALA5154917 | assay format | Scientific Literature | |
9. | ALA5167391 | B | Binding affinity to RIOK1 in human MKN-1 cells assessed as negative shift in melting temperature at 5 uM incubated for 3 hrs followed by heat treatment at 52 to 62 degC for 3 mins by CETSA | Homo sapiens | 1 | ALA5154917 | cell-based format | Scientific Literature | |
10. | ALA5167392 | B | Binding affinity to RIOK2 in human MKN-1 cells assessed as negative shift in melting temperature at 5 uM incubated for 3 hrs followed by heat treatment at 52 to 62 degC for 3 mins by CETSA | Homo sapiens | 1 | ALA5154917 | cell-based format | Scientific Literature | |
11. | ALA5167393 | B | Binding affinity to RIOK3 in human MKN-1 cells assessed as negative shift in melting temperature at 5 uM incubated for 3 hrs followed by heat treatment at 52 to 62 degC for 3 mins by CETSA | Homo sapiens | 1 | ALA5154917 | cell-based format | Scientific Literature | |
12. | ALA5167394 | B | Inhibition of RIOK2 in human MKN-1 cells assessed as reduction in mTOR phosphorylation >0.60 uM incubated for 4 hrs by Western blot analysis | Homo sapiens | 1 | ALA5154917 | cell-based format | Scientific Literature | |
13. | ALA5167395 | B | Inhibition of RIOK2 in human HT-29 cells assessed as reduction in mTOR phosphorylation >0.60 uM incubated for 4 hrs by Western blot analysis | Homo sapiens | 1 | ALA5154917 | cell-based format | Scientific Literature | |
14. | ALA5167396 | F | Antiproliferative activity against human HT-29 cells assessed as cell growth inhibition incubated for 72 hrs by CCK-8 assay | Homo sapiens | 3 | ALA5154917 | cell-based format | Scientific Literature | |
15. | ALA5167397 | F | Antiproliferative activity against human MKN-1 cells assessed as cell growth inhibition incubated for 72 hrs by CCK-8 assay | Homo sapiens | 3 | ALA5154917 | cell-based format | Scientific Literature | |
16. | ALA5167398 | P | Aqueous solubility of the compound | 1 | ALA5154917 | small-molecule physicochemical format | Scientific Literature | ||
17. | ALA5167399 | A | Oral bioavailability in Sprague-Dawley rat | Rattus norvegicus | 1 | ALA5154917 | organism-based format | Scientific Literature | |
18. | ALA5167400 | A | Cmax in Sprague-Dawley rat administered orally | Rattus norvegicus | 1 | ALA5154917 | assay format | Scientific Literature | |
19. | ALA5167401 | F | Antitumor activity against human MKN-1 cells xenografted in CB17-SCID mouse assessed as tumor growth inhibition at 25 mg/kg, ip qd for 18 consecutive days and measured once every 2 days relative to control | Homo sapiens | 1 | ALA5154917 | organism-based format | Scientific Literature | |
20. | ALA5167402 | T | Toxicity in CB17-SCID mouse xenografted with human MKN-1 cells assessed as mortality at 25 mg/kg, ip qd for 18 consecutive days | Mus musculus | 1 | ALA5154917 | organism-based format | Scientific Literature |