# | Aladdin ID | Assay Type | Description | Organism | Compounds | Reference | BAO Format | Source | |
---|---|---|---|---|---|---|---|---|---|
1. | ALA4739796 | B | Inhibition of biotinylated-THZ1 binding to CDK12/CDK13 in human Jurkat cells assessed as reduction in cyclin K pull down at 1 uM preincubated for 6 hrs followed by biotinylated-THZ1 addition by Western blotting based pull-down assay | Homo sapiens | 2 | ALA4739714 | cell-based format | Patent Bioactivity Data | |
2. | ALA4739797 | B | Inhibition of biotinylated-THZ1 binding to CDK7 in human Jurkat cells assessed as reduction in cyclin H pull down at 1 uM preincubated for 6 hrs followed by biotinylated-THZ1 addition by Western blotting based pull-down assay | Homo sapiens | 4 | ALA4739714 | cell-based format | Patent Bioactivity Data | |
3. | ALA4739798 | B | Inhibition of biotinylated-THZ1 binding to CDK12 in human Jurkat cells assessed as reduction in cyclin K pull down at 1 uM preincubated for 6 hrs followed by biotinylated-THZ1 addition by Western blotting based pull-down assay | Homo sapiens | 6 | ALA4739714 | cell-based format | Patent Bioactivity Data | |
4. | ALA4739799 | F | Antiproliferative activity against human Jurkat cells measured after 72 hrs by Celltiter glo assay | Homo sapiens | 8 | ALA4739714 | cell-based format | Patent Bioactivity Data | |
5. | ALA4739800 | B | Inhibition of CDK2/cyclin A (unknown origin) | Homo sapiens | 13 | ALA4739714 | protein complex format | Patent Bioactivity Data | |
6. | ALA4739801 | B | Inhibition of CDK7/cyclin H/MNAT1 (unknown origin) | Homo sapiens | 13 | ALA4739714 | protein complex format | Patent Bioactivity Data | |
7. | ALA4739802 | B | Inhibition of CDK9/cyclin T1 (unknown origin) | Homo sapiens | 13 | ALA4739714 | protein complex format | Patent Bioactivity Data | |
8. | ALA4739803 | F | Antiproliferative activity against human HAP1 cells measured after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay | Homo sapiens | 1 | ALA4739714 | cell-based format | Patent Bioactivity Data | |
9. | ALA4739804 | F | Antiproliferative activity against human HAP1 cells harboring CDK12 C1039S/CDK13 C1017S double mutant measured after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay | Homo sapiens | 1 | ALA4739714 | cell-based format | Patent Bioactivity Data | |
10. | ALA4828797 | F | Antiproliferative activity against human TC71 cells assessed as reduction in cell viability | Homo sapiens | 2 | ALA4828703 | cell-based format | Scientific Literature | |
11. | ALA4828798 | B | Inhibition of CDK2/Cyclin A (unknown origin) | Homo sapiens | 20 | ALA4828703 | protein complex format | Scientific Literature | |
12. | ALA4828799 | B | Inhibition of CDK7/Cyclin H (unknown origin) | Homo sapiens | 20 | ALA4828703 | protein complex format | Scientific Literature | |
13. | ALA4828800 | B | Inhibition of CDK9/Cyclin T1 (unknown origin) | Homo sapiens | 20 | ALA4828703 | protein complex format | Scientific Literature | |
14. | ALA4828801 | B | Inhibition of human recombinant CDK12/CyclinK assessed as reduction in substrate phosphorylation using His-c-Myc as substrate preincubated with enzyme for 5 mins followed by substrate addition for 15 mins in presence of [gamma 32P-ATP] by radioactive kinase assay | Homo sapiens | 20 | ALA4828703 | protein complex format | Scientific Literature | |
15. | ALA4828802 | B | Inhibition of human recombinant CDK13/CyclinK assessed as reduction in substrate phosphorylation using His-c-Myc as substrate preincubated with enzyme for 5 mins followed by substrate addition for 15 mins in presence of [gamma 32P-ATP] by radioactive kinase assay | Homo sapiens | 20 | ALA4828703 | protein complex format | Scientific Literature | |
16. | ALA4828803 | A | Metabolic stability in mouse liver microsomes assessed as half life | Mus musculus | 7 | ALA4828703 | microsome format | Scientific Literature | |
17. | ALA4828804 | B | Binding affinity to CDK12 in CDK12/CyclinK complex (unknown origin) assessed as increase in CDK12 mass at 10-fold excess concentration incubated for 1 hr by LC-MS analysis | Homo sapiens | 1 | ALA4828703 | single protein format | Scientific Literature | |
18. | ALA4828805 | B | Inhibition of CDK12/13 in human jurkat cells assessed as reduction in RNA polymerase 2 CTD phosphorylation at Ser2 residue at 0.5 uM measured after 6 hrs by immunoblotting analysis | Homo sapiens | 1 | ALA4828703 | cell-based format | Scientific Literature | |
19. | ALA4828806 | B | Inhibition of CDK12/13 in human jurkat cells assessed as reduction in RNA polymerase 2 CTD phosphorylation at Ser2 residue at 1 uM measured after 6 hrs by immunoblotting analysis | Homo sapiens | 2 | ALA4828703 | cell-based format | Scientific Literature | |
20. | ALA4828807 | B | Inhibition of CDK12/13 in human Jurkat cells assessed as BRCA1 gene expression at 0.5 to 1 uM incubated for 4 hrs by RT-qPCR analysis | Homo sapiens | 1 | ALA4828703 | cell-based format | Scientific Literature |