Table 1.
Summary of libraries screened and number of hits. A total number of 107,600 small molecules were screened against recombinant JAK2 JH2 V617F by thermal shift assay (TSA) and/or fluorescence polarization (FP) in 384- or 1536-well plate formats, which resulted in identification of 55 hits.
| Library Type | Provider | No. of Compounds | Screening Method | Screening Format |
No. of Hits |
|---|---|---|---|---|---|
| Kinase-targeted | Uni Copenhagen Biomol SelleckChem Vitas-M |
4200 160 190 1000 |
TSA TSA, FP TSA, FP FP |
384- 384- 384- 1536- |
4 5 1 0 |
| Nucleotide/ nucleoside analogs |
Otava | 960 | TSA, FP | 384- | 22 |
| Clinical bioactives | NIH | 740 | TSA, FP | 384- | 2 |
| Known drugs | Prestwick | 1200 | FP | 1536- | 3 |
| Fragments | Org Pharm Chem | 500 | FP | 1536- | 1 |
| Natural derivatives | Timtec Analyticon |
3000 1000 |
FP FP |
1536- 1536- |
0 0 |
| Diverse | Enamine MayBridge Elite Synergy Specs ChemBridge |
28,200 14,400 2300 1900 30,300 17,500 |
FP FP FP FP FP FP |
1536- 1536- 1536- 1536- 1536- 1536- |
3 9 0 0 3 2 |
| SUM: | 107,600 | 55 |