SGC-CLK-1 |
SGC-CLK-1 : ATP Competitive inhibitor of CLK1, CLK2 and CLK4
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
Vendors
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Probe Summary
| Targets | Biochemical/Biophysical Potency | Cellular Potency |
|---|---|---|
| CLK1 |
|
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| CLK2 |
|
|
| CLK4 |
|
|
ATP competitive
up to 1 uM
Selectivity
In Vitro Selectivity Assessment
Potency Assay Off-Target:
KINOMEscan
Selectivity Assessment Description:
Only 6/403 kinases with PoC<35 when screened at 1 µM in KINOMEscan. (ERK8, NEK7, PIP5K2B, HIPK1 50 n ...
Potency Cellular
In Vitro
CLK1
Mode of Action: ATP competitive
Structure-Activity-Relationship data available? Yes
DOI Reference: 10.3390/ijms21207549
CLK2
Mode of Action: ATP competitive
Structure-Activity-Relationship data available? Yes
DOI Reference: 10.3390/ijms21207549
CLK4
Mode of Action: ATP competitive
Structure-Activity-Relationship data available? Yes
DOI Reference: 10.3390/ijms21207549
Negative Control Compounds
SGC-CLK-1
Notes: SGC-CLK-1N was tested in the Discoverx panel and no kinases had PoC<45. The negative control was sent to Eurofins for testing in enzyme assays for CLKs and typical CLK inhibitor off targets, showing no inhibition.
Chemical Information
| Molecular Formula | C19H15F3N6O2 |
| SMILEs | COc1cc(Nc2nccc(-c3cnn4nc(OC)ccc34)n2)cc(C(F)(F)F)c1 |
| InChI | InChI=1S/C19H15F3N6O2/c1-29-13-8-11(19(20,21)22)7-12(9-13)25-18-23-6-5-15(26-18)14-10-24-28-16(14)3-4-17(27-28)30-2/h3-10H,1-2H3,(H,23,25,26) |
| Molecular weight | 416.12 Da |
| AlogP | 3.965900000000002 |
| HBond acceptors | 8 |
| HBond donors | 1 |
| Atoms | 45 |