# | Aladdin ID | Assay Type | Description | Organism | Compounds | Reference | BAO Format | Source | |
---|---|---|---|---|---|---|---|---|---|
1. | ALA5256396 | B | Covalent inhibition of CDK12 (unknown origin) using histone H1 as substrate incubated for 10 mins in presence of [gamma-32P]ATP by radioactivity based kinase assay | Homo sapiens | 4 | single protein format | Scientific Literature | ||
2. | ALA3991652 | B | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | Homo sapiens | 243 | subcellular format | Kuster lab chemical proteomics drug profiling | ||
3. | ALA4118328 | B | Inhibition of CRK7 in human SKCO1 cells at 1 uM after 4 hrs using biotin labeled DIKCSNILLNNSGQIK probe by mass-spectrometric analysis relative to control | Homo sapiens | 3 | cell-based format | Scientific Literature | ||
4. | ALA4151504 | B | Inhibition of CDK12 in human SK-BR-3 cells assessed as reduction in RNA polymerase 2 Ser2 phosphorylation incubated for 4 hrs by | Homo sapiens | 3 | cell-based format | Scientific Literature | ||
5. | ALA4151509 | B | Time dependent inhibition of human CDK12 incubated for 0 to 5 hrs using ULight-4E-BP1 (Thr37/Thr46) substrate by LANCE system based assay | Homo sapiens | 2 | single protein format | Scientific Literature | ||
6. | ALA4375312 | B | Binding affinity to wild-type human partial length CDK12 (P697 to E1077 residues) expressed in mammalian expression system measured after 1 hr by kinomescan method | Homo sapiens | 1 | assay format | Scientific Literature | ||
7. | ALA4611865 | B | Inhibition of CDK12 (unknown origin) | Homo sapiens | 4 | single protein format | Scientific Literature | ||
8. | ALA4612766 | B | Binding affinity to CDK12 (unknown origin) assessed as change in molecular weight at 10 fold excess of protein measured after 1 hr by LC-MS/MS analysis | Homo sapiens | 1 | single protein format | Scientific Literature | ||
9. | ALA4612768 | B | Binding affinity to CDK12 (1025 to 1041 residues) (unknown origin) assessed as Cys1039-adduct formation at 10 fold excess of protein measured after 1 hr by by capillary electrophoresis-MS/MS analysis | Homo sapiens | 1 | single protein format | Scientific Literature | ||
10. | ALA4612789 | B | Inhibition of CDK12 C1039S mutant in human HAP1 cells assessed as reduction in RNA Polymerase 2 CTD phosphorylation at Ser2 residues at 40 to 200 nM measured after 6 hrs by Western blot analysis | Homo sapiens | 1 | cell-based format | Scientific Literature | ||
11. | ALA4612790 | B | Inhibition of CDK12 C1039S mutant in human HAP1 cells assessed as reduction in RNA Polymerase 2 CTD phosphorylation at Ser5 residues at 40 to 200 nM measured after 6 hrs by Western blot analysis | Homo sapiens | 1 | cell-based format | Scientific Literature | ||
12. | ALA4612791 | B | Inhibition of CDK12 C1039S mutant in human HAP1 cells assessed as reduction in RNA Polymerase 2 CTD phosphorylation at Ser7 residues at 40 to 200 nM measured after 6 hrs by Western blot analysis | Homo sapiens | 1 | cell-based format | Scientific Literature | ||
13. | ALA4612792 | B | Inhibition of CDK12 C1039S mutant in human HAP1 cells assessed as reduction in RNA Polymerase 2 expression at 40 to 200 nM measured after 6 hrs by Western blot analysis | Homo sapiens | 1 | cell-based format | Scientific Literature | ||
14. | ALA4612805 | B | Inhibition of CDK12 C1039S mutant in human HAP1 cells assessed as reduction in RAD51 expression at 40 to 200 nM measured after 24 hrs by Western blot analysis | Homo sapiens | 1 | cell-based format | Scientific Literature | ||
15. | ALA4612807 | B | Inhibition of CDK12 C1039S mutant in human HAP1 cells assessed as reduction in RAD51C expression at 40 to 200 nM measured after 24 hrs by Western blot analysis | Homo sapiens | 1 | cell-based format | Scientific Literature | ||
16. | ALA4612809 | B | Inhibition of CDK12 C1039S mutant in human HAP1 cells assessed as reduction in RAD51 RNA expression at 40 to 200 nM measured after 24 hrs by RT-qPCR analysis | Homo sapiens | 1 | cell-based format | Scientific Literature | ||
17. | ALA4612811 | B | Inhibition of CDK12 C1039S mutant in human HAP1 cells assessed as reduction in RAD51C RNA expression at 40 to 200 nM measured after 24 hrs by RT-qPCR analysis | Homo sapiens | 1 | cell-based format | Scientific Literature | ||
18. | ALA4612813 | B | Inhibition of CDK12 in human HAP1 cells assessed as potentiation of olaparib-induced antiproliferative activity at 25 nM measured after 8 days by Celltiter glo assay | Homo sapiens | 1 | cell-based format | Scientific Literature | ||
19. | ALA4613418 | B | Inhibition of CDK12 (unknown origin) | Homo sapiens | 1 | single protein format | Scientific Literature | ||
20. | 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 | cell-based format | Patent Bioactivity Data |