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IC50 determinations for inhibiting EphB3 phosphorylation of BTK-peptide.
 | |||
|---|---|---|---|
| Cmpd | R | Method | IC50 (µM) |
| 60 | 3-indolyl | a | NA |
| 61 | N-methyl-3indolyl | A | NA |
| 62 | 4-quinolinyl | A | NA |
| 63 | 3-(1,2-benzisoxazolyl) | C | NA |
| 64 | 3-(1H-indazolyl) | Cb | > 20 |
| 65 | R1 | C | > 20 |
| 66 | R2 | Cb | NA |
| 67 | R3 | C | ~ 15 |
| 68 | R4 | C | NA |
| 69 | R5 | Cb | 0.46 |
Prepared by EDCI mediated coupling of indole-3-carboxylic acid with 2-chloroaniline
Method C, steps d and e; NA: Not active at 20µM.
