Table 1.
Chemotypes present along with the number of molecules GSK3β inhibitors
| Chemotype structure and name |
No. of molecules with various IC50 ranges |
Assay type | Assay method | ||||||
|---|---|---|---|---|---|---|---|---|---|
| <1 nM | 1 nM–10 nM | 10 nM–<100 nM | 100 nM–1 µM | 1 µM–10 µM | 10 µM–100 µM | >100 µM | |||
 Azaindole |
0 | 10 | 36 | 29 | 4 | 0 | 0 | In vitro | Scintillation counter |
 Benzimidazole |
2 | 16 | 42 | 61 | 2 | 17 | 0 | In vitro | Standard coupled enzyme assay, liquid scintillation counter |
 Benzthiazole |
0 | 0 | 0 | 1 | 0 | 9 | 0 | In vitro | Standard coupled enzyme assay, liquid scintillation counter |
 Imidazole |
1 | 11 | 17 | 299 | 101 | 47 | 1 | In vitro | Scintillation counter, HTRF assay |
 Indole |
1 | 24 | 80 | 614 | 366 | 21 | 3 | In vitro | Liquid scintillation counter |
 Oxazole |
0 | 0 | 1 | 1 | 2 | 5 | 0 | In vitro | Liquid scintillation counter, microtiterplate scintillation counter |
 Piperidine |
1 | 6 | 12 | 81 | 97 | 74 | 0 | In vitro | Scintillation counter |
 Pyrazole |
1 | 10 | 56 | 403 | 33 | 86 | 0 | In vitro | Scintillation counter |
 Pyrrole |
0 | 5 | 15 | 11 | 25 | 9 | 0 | In vitro | Liquid scintillation counter |
 Pyridine |
2 | 32 | 87 | 340 | 713 | 251 | 7 | In vitro | Liquid scintillation spectrometry, western blotting |
 Pyrimidine |
4 | 30 | 129 | 153 | 557 | 600 | 9 | In vitro | Spectrophotometric coupled enzyme assay, scintillation counter |
 Quinazoline |
0 | 0 | 0 | 1 | 1 | 1 | 0 | In vitro | Standard couple enzyme assay, trilux wallac scintillation counter, ELISA |
 Thiazole |
0 | 0 | 4 | 14 | 29 | 20 | 6 | In vitro | Scintillation counter |
 Thiophene |
0 | 4 | 16 | 30 | 11 | 7 | 0 | In vitro | Scintillation counter, wallac counter, standard coupled, microbeta microplate counter |
The in various IC50 range along with the assay methods and types are also indicated.
GSK3β, glycogen synthase kinase-3 beta.