| # | Aladdin ID | Assay Type | Description | Organism | Compounds | Reference | BAO Format | Source | |
|---|---|---|---|---|---|---|---|---|---|
| 1. | ALA1926118 | B | Inhibition of CDK2/cyclin E | 36 | protein complex format | Scientific Literature | |||
| 2. | ALA1926135 | B | Inhibition of CDK9/cyclin T1 | 4 | protein complex format | Scientific Literature | |||
| 3. | ALA1926136 | P | Solubility of the compound in water | 5 | small-molecule physicochemical format | Scientific Literature | |||
| 4. | ALA1926137 | A | Cmax in BALB/c mouse plasma at 50 mg/kg, iv after 24 hrs by LC-MS analysis | Mus musculus | 5 | organism-based format | Scientific Literature | ||
| 5. | ALA1926138 | A | AUC in BALB/c mouse plasma at 50 mg/kg, iv after 24 hrs by LC-MS analysis | Mus musculus | 5 | organism-based format | Scientific Literature | ||
| 6. | ALA1926139 | A | Half life in BALB/c mouse plasma at 50 mg/kg, iv by LC-MS analysis | Mus musculus | 5 | organism-based format | Scientific Literature | ||
| 7. | ALA1926140 | A | Volume of distribution in BALB/c mouse plasma at 50 mg/kg, iv after 24 hrs by LC-MS analysis | Mus musculus | 5 | organism-based format | Scientific Literature | ||
| 8. | ALA1926141 | A | Clearance in BALB/c mouse plasma at 50 mg/kg, iv after 24 hrs by LC-MS analysis | Mus musculus | 5 | organism-based format | Scientific Literature | ||
| 9. | ALA1926142 | A | Ratio of Seliciclib clearance to compound clearance in BALB/c mouse plasma at 50 mg/kg, iv after 24 hrs by LC-MS analysis | Mus musculus | 4 | organism-based format | Scientific Literature | ||
| 10. | ALA1926143 | A | Oral bioavailability in BALB/c mouse at 50 mg/kg by LC-MS analysis | Mus musculus | 4 | organism-based format | Scientific Literature | ||
| 11. | ALA1926144 | F | Antitumor activity against human HCT116 cells xenografted in NCR athymic mouse assessed as reduction in tumor volume at 50 mg/kg, po twice daily at 12 to 14 hrs intervals measured after 12 days relative to vehicle treated control | Homo sapiens | 1 | organism-based format | Scientific Literature | ||
| 12. | ALA1926145 | F | Antitumor activity against human HCT116 cells xenografted in NCR athymic mouse assessed as growth delay at 50 mg/kg, po twice daily at 12 to 14 hrs intervals measured after 12 days relative to vehicle treated control | Homo sapiens | 1 | organism-based format | Scientific Literature | ||
| 13. | ALA1926146 | B | Inhibition of CDK-mediated RB phosphorylation at Ser-780 in human HT29 cells at 0.1 to 20 uM after 24 hrs by Western blotting relative to control | Homo sapiens | 1 | cell-based format | Scientific Literature | ||
| 14. | ALA1926147 | F | Reduction of RNA polymerase 2 expression in human HT-29 cells | Homo sapiens | 1 | cell-based format | Scientific Literature | ||
| 15. | ALA1926148 | B | Inhibition of CDK7 in human HT29 cells assessed as reduction in RNA polymerase 2 expression | Homo sapiens | 1 | cell-based format | Scientific Literature | ||
| 16. | ALA1926149 | B | Inhibition of CDK9 in human HT29 cells assessed as reduction in RNA polymerase 2 expression | Homo sapiens | 1 | cell-based format | Scientific Literature | ||
| 17. | ALA1926150 | F | Cell cycle arrest in human HT-29 cells assessed as reduction at S phase at 3.3 uM up to 16 hrs measuring distribution of bromodeoxyuridine incorporation by flow cytometry | Homo sapiens | 1 | cell-based format | Scientific Literature | ||
| 18. | ALA1926218 | F | Cell cycle arrest in human HT-29 cells assessed as accumulation at G2/M phase at 3.3 uM up to 16 hrs measuring distribution of bromodeoxyuridine incorporation by flow cytometry | Homo sapiens | 1 | cell-based format | Scientific Literature | ||
| 19. | ALA3705418 | B | Kinase Assay: The compounds from the examples below were investigated for their CDK2/cyclin E, CDK1/cyclin B, CDK4/cyclin D1 and CDK7/cyclin H, ERK-2, and PKA inhibitory activity. His6-tagged recombinant human cyclin-dependent kinases CDK1/cyclin B1, CDK2/cyclin E, CDK4 and CDK7/cyclin H were expressed in sf9 cells using a baculovirus expression system. Recombinant cyclin D1 was expressed in E. coli. Proteins were purified by metal chelate affinity chromatography to greater than 90% homogeneity. Kinase assays were performed in 96-well plates using recombinant CDK/cyclins, recombinant active ERK-2 (Upstate Biotechnology), or cyclic AMP-dependent kinase (PKA) catalytic subunit (Calbiochem Cat. 539487). Assays were performed in assay buffer (25 mM beta -glycerophosphate, 20 mM MOPS, 5 mM EGTA, 1 mM DTT, 1 mM Na3VO3, pH 7.4), into which were added 2-4 ug of active enzyme with appropriate substrates (purified histone H1 for CDK2, recombinant GST-retinoblastoma protein (residues 773-928) for CDK4. | Homo sapiens | 10 | cell-based format | BindingDB Database | ||
| 20. | ALA3707754 | B | Kinase Assay: The compounds from the examples below were investigated for their CDK2/cyclin E, CDK1/cyclin B, CDK4/cyclin D1 and CDK7/cyclin H, ERK-2, and PKA inhibitory activity. His6-tagged recombinant human cyclin-dependent kinases CDK1/cyclin B1, CDK2/cyclin E, CDK4 and CDK7/cyclin H were expressed in sf9 cells using a baculovirus expression system. Recombinant cyclin D1 was expressed in E. coli. Proteins were purified by metal chelate affinity chromatography to greater than 90% homogeneity. Kinase assays were performed in 96-well plates using recombinant CDK/cyclins, recombinant active ERK-2 (Upstate Biotechnology), or cyclic AMP-dependent kinase (PKA) catalytic subunit (Calbiochem Cat. 539487). Assays were performed in assay buffer (25 mM beta -glycerophosphate, 20 mM MOPS, 5 mM EGTA, 1 mM DTT, 1 mM Na3VO3, pH 7.4), into which were added 2-4 ug of active enzyme with appropriate substrates (purified histone H1 for CDK2, recombinant GST-retinoblastoma protein (residues 773-928) for CDK4. | Homo sapiens | 10 | cell-based format | BindingDB Database |
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