Table 1.
Literature CLK chemical probes and compounds in clinical trialsa.
| Compound | Name | Structure | CLK Activities (IC50 nM) |
Current Status |
|---|---|---|---|---|
| 1 | MU1210 |
|
CLK1 = 8 CLK2 = 20 CLK3 = 12 |
CLK Probe (Nemec et al., 2019) |
| 2 | T3-CLK |
|
CLK1 = 0.67 CLK2 = 15 CLK3 = 110 |
CLK Probe (Funnell et al., 2017) |
| 3 | Compound 25 |
|
CLK1 = 2.0 | CLK Probe (Sun et al., 2017) |
| 4 | SM08502 |
|
CLK2 = 2 CLK3 = 22 |
CLK Probe Phase I Clinical Trial for solid tumor (Tam et al., 2020; Bossard et al., 2020) |
| 5 | SM04690 Loricivivint |
|
CLK2 = 7.8 | CLK Probe Phase II Clinical trial for osteoarthritis (Hood et al., 2017; Kc Sunil, 2017) |
| 6 | SM04755 |
|
CLK2 = 0.82 | CLK Probe Phase I clinical trial for plaque psoriasis [ (Qin et al., 2021), terminated] |
| 7 | CTX-712 |
|
CLK2 = 1.4 | Phase I Clinical trial relapsed and refractory malignancies (Ogawa et al., 2019) |
a
For further information see the recent review on CLK inhibitors (Martin Moyano et al., 2020) and the SGC chemical portal [SGC-CLK1 (https://www.thesgc.org/chemical-probes/SGC-CLK-1); MU1210 (https://www.thesgc.org/chemical-probes/MU1210); T3-CLK (https://www.thesgc.org/chemical-probes/T3-CLK)].