# | Aladdin ID | Assay Type | Description | Organism | Compounds | Reference | BAO Format | Source | |
---|---|---|---|---|---|---|---|---|---|
1. | ALA2089691 | Binding | Inhibition of human CDK4/cyclin D1 expressed in baculovirus infected Sf9 cells assessed as inhibition of pRb Ser780 phosphorylation after 60 mins by TR-FRET assay | Homo sapiens | 6 | ALA2086364 | cell-based format | Scientific Literature | |
2. | ALA2089692 | Binding | Inhibition of human CDK6/cyclin D3 assessed as inhibition of pRb Ser780 phosphorylation after 120 mins by TR-FRET assay | Homo sapiens | 4 | ALA2086364 | protein complex format | Scientific Literature | |
3. | ALA2089695 | Binding | Inhibition of human CDK1/cyclin B assessed as inhibition of Tamra-H1 phosphorylation by IMAP-FP assay | Homo sapiens | 6 | ALA2086364 | protein complex format | Scientific Literature | |
4. | ALA2089696 | Binding | Inhibition of human CDK2/cyclin A assessed as inhibition of Tamra-H1 phosphorylation by IMAP-FP assay | Homo sapiens | 6 | ALA2086364 | protein complex format | Scientific Literature | |
5. | ALA2089698 | Binding | Selectivity ratio of IC50 for human CDK4/cyclin D1 over IC50 for human CDK1/cyclin B | Homo sapiens | 2 | ALA2086364 | assay format | Scientific Literature | |
6. | ALA2089700 | Binding | Selectivity ratio of IC50 for human CDK4/cyclin D1 over IC50 for human CDK2/cyclin A | Homo sapiens | 2 | ALA2086364 | assay format | Scientific Literature | |
7. | ALA2089702 | ADME | AUC (0 to 8 hrs) in Sprague-Dawley rat at 5 mg/kg, po | Rattus norvegicus | 3 | ALA2086364 | organism-based format | Scientific Literature | |
8. | ALA2089703 | ADME | Oral bioavailability in Sprague-Dawley rat at 5 mg/kg | Rattus norvegicus | 1 | ALA2086364 | organism-based format | Scientific Literature | |
9. | ALA2089704 | ADME | Plasma clearance in Sprague-Dawley rat at 1 mg/kg, iv | Rattus norvegicus | 1 | ALA2086364 | organism-based format | Scientific Literature | |
10. | ALA2089705 | Binding | Inhibition of CDK4/CDK6 assessed as pRb phosphorylation in human JeKo1 cells by immunoblotting | Homo sapiens | 1 | ALA2086364 | cell-based format | Scientific Literature | |
11. | ALA2089706 | Functional | Cell cycle arrest in human JeKo1 cells assessed as accumulation at G1 phase by PI-based FACS analysis | Homo sapiens | 1 | ALA2086364 | cell-based format | Scientific Literature | |
12. | ALA2089796 | Functional | Cell cycle arrest in human JeKo1 cells assessed as accumulation at G1 phase at 0.625 to 2.5 uM by PI-based FACS analysis | Homo sapiens | 1 | ALA2086364 | cell-based format | Scientific Literature | |
13. | ALA2089797 | Functional | Cell cycle arrest in human JeKo1 cells assessed as accumulation at G2 phase at 10 uM by PI-based FACS analysis | Homo sapiens | 1 | ALA2086364 | cell-based format | Scientific Literature | |
14. | ALA2089798 | Functional | Cell cycle arrest in human JeKo1 cells assessed as accumulation at S phase at 10 uM by PI-based FACS analysis | Homo sapiens | 1 | ALA2086364 | cell-based format | Scientific Literature | |
15. | ALA2089799 | Functional | Inhibition of CDK4/6 in human JeKo1 cells xenografted po dosed SCID beige mouse assessed as reduction of pRb phosphorylation administered BID for 2.5 days by ELISA | Mus musculus | 1 | ALA2086364 | organism-based format | Scientific Literature | |
16. | ALA2089800 | Functional | Inhibition of CDK4/6 in human JeKo1 cells xenografted SCID beige mouse assessed as reduction of pRb phosphorylation at 250 mg/kg/day administered BID for 2.5 days post-last dose by ELISA relative to vehicle-treated control | Mus musculus | 1 | ALA2086364 | organism-based format | Scientific Literature | |
17. | ALA2089801 | Functional | Inhibition of CDK4/6 in human JeKo1 cells xenografted in SCID beige mouse assessed as reduction of pRb phosphorylation at 250 mg/kg/day administered BID for 2.5 days measured after 7 hrs post-last dose by ELISA relative to vehicle-treated control | Mus musculus | 1 | ALA2086364 | organism-based format | Scientific Literature | |
18. | ALA2089802 | Functional | Inhibition of CDK4/6 in human JeKo1 cells xenografted in SCID beige mouse assessed as reduction of pRb phosphorylation at 500 mg/kg/day administered BID for 2.5 days measured after 1 hr post-last dose by ELISA relative to vehicle-treated control | Mus musculus | 1 | ALA2086364 | organism-based format | Scientific Literature | |
19. | ALA2089803 | Functional | Inhibition of CDK4/6 in human JeKo1 cells xenografted in SCID beige mouse assessed as reduction of pRb phosphorylation at 500 mg/kg/day administered BID for 2.5 days measured after 7 hrs post-last dose by ELISA relative to vehicle-treated control | Mus musculus | 1 | ALA2086364 | organism-based format | Scientific Literature | |
20. | ALA2089804 | Toxicity | Toxicity in po dosed SCID beige mouse administered BID | Mus musculus | 1 | ALA2086364 | organism-based format | Scientific Literature |