Table 1.
Summary of recombinant hNeks 1, 2, 6 and 7 thermal shift inhibitor screen showing only compounds withΔTm ≥ 2 °C. Names of compounds showing a significant thermal shift (ΔTm ≥ 4 °C) are depicted in bold.
| Nek | CAS Number | Compound Description | Δ Tm (°C) |
|---|---|---|---|
| Nek1(Δ262-1258)-(T162A) | 667463-62-9 | GSK-3 Inhibitor IX | 3.5 |
| Nek1(Δ262-1258)-(T162A) | 444723-13-1 | Cdk2 Inhibitor IV, NU6140 | 3.1 |
| Nek1(Δ262-1258)-(T162A) | 879127-16-9 | Aurora Kinase Inhibitor III | 3.6 |
| Nek1(Δ262-1258)-(T162A) | 443798-55-8 | Cdk1/2 Inhibitor III | 2.6 |
| Nek1(Δ262-1258)-(T162A) | 220792-57-4 | Aminopurvalanol A | 2.5 |
| Nek1(Δ262-1258)-(T162A) | 4129-56-6 | JNK Inhibitor II | 4.0 |
| Nek2(Δ272-445)-(T175A) | 220792-57-4 | Aminopurvalanol A | 4.0 |
| Nek2(Δ272-445)-(T175A) | 866405-64-3 | AMPK Inhibitor, Compound C | 2.5 |
| Nek2(Δ272-445)-(T175A) | 326914-10-7 | SU11652 | 9.6 |
| Nek2(Δ272-445)-(T175A) | 4129-56-6 | JNK Inhibitor II | 4.8 |
| Nek2(Δ272-445)-(T175A) | 97161-97-2 | K-252a, Nocardiopsis sp. | 5.4 |
| Nek2(Δ272-445)-(T175A) | 522629-08-9 | MNK1 Inhibitor | 2.1 |
| Nek2(Δ272-445)-(T175A) | 545380-34-5 | NF-kB Activation Inhibitor | 4.2 |
| Nek2(Δ272-445)-(T175A) | 601514-19-6 | GSK3b Inhibitor XII, TWS119 | 2.3 |
| Nek6(S206A) | 62996-74-1 | Staurosporine, Streptomyces sp. | 2.1 |
| Nek6(S206A) | 852527-97-0 | Alsterpaullone, 2-Cyanoethyl | 2.5 |
| Nek6(S206A) | 244148-46-7 | Isogranulatimide | 6.5 |
| Nek7wt | 345987-15-7 | JNK Inhibitor V | 4.9 |
| Nek7wt | 443798-55-8 | Cdk1/2 Inhibitor III | 4.2 |
| Nek7wt | 135897-06-2 | SB 218078 | 11.5 |
| Nek7wt | 152121-53-4 | PD 169316 | 4.4 |
| Nek7wt | 62996-74-1 | Staurosporine, Streptomyces sp. | 3.2 |
| Nek7wt | 97161-97-2 | K-252a, Nocardiopsis sp. | 8.8 |
| Nek7wt | 244148-46-7 | Isogranulatimide | 8.3 |
| Nek7wt | 404828-08-6 | GSK-3 Inhibitor XIII | 4.3 |
| Nek7wt | 220792-57-4 | Aminopurvalanol A | 3.0 |
| Nek7wt | 41179-33-3 | MK2a Inhibitor | 5.3 |
| Nek7wt | 854171-35-0 | Indirubin Derivative E804 | 9.7 |
| Nek7wt | 160807-49-8 | Indirubin-3'-monoxime | 7.9 |
| Nek7wt | 487021-52-3 | GSK-3b Inhibitor VIII | 3.3 |
| Nek7wt | 4129-56-6 | JNK Inhibitor II | 2.6 |