Table 2. Lexicon azapurine HTS hits.
| Compound | CRK3:CYC6IC50 (µM) | CDK4:CYCD1IC50 (µM)a | IC50 against WT promastigote L. major (µM) | IC50 against WT amastigote L. major (µM) |
| 1 | 2.6 | 12.5 | >10 | >50 |
| 2 | 3.4 | 5.6 | >10 | 38.4 |
| 3 | 4.4 | 21.9 | >10 | >50 |
| 4 | 4.4 | 10.3 | >10 | >50 |
| 5 | 5.3 | 9.7 | 8.6 | >50 |
| 6 | 6.9 | 9.2 | >10 | >50 |
| 7 | 7.8 | 19.5 | ND | ND |
| 8 | 8.1 | 26.9 | ND | ND |
| 9 | 8.8 | 19.8 | ND | ND |
| 10 | 10.1 | 7.3 | ND | ND |
| 11 | 10.3 | 6.7 | ND | ND |
| 12 | 10.7 | 4.6 | ND | ND |
a
Also screened against CDK1:CYCB and CDK2:CYCA; IC50 values for all compounds in these screens were >50 µM. ND, not determined (See Table S2 in Supporting Information Text S1 for compound structures.).