Table 2. IC50 values for the PE24H inhibitors determined using the fluorescence ADPRT assay.
MsOH, mesylate salts.
| Code | Compound chemical name | IC50 (μM) |
|---|---|---|
| GP-D | 3-(Morpholin-4-ylmethyl)-1,5-dihydro-6H-[1,2]diazepino[4,5,6-cd]indol-6-one | 0.17±0.03 |
| PJ34 | N-(6-oxo-5,6-dihydro-phenanthridin-2-yl)-N,N-dimethylacetamide | 0.28±0.07 |
| GP-M | N-(6-oxo-5,6-dihydrobenzo[c][1,5]naphthyridin-2-yl)-2-(4-pyrrolidin-1-ylpiperidin-1-yl)acetamide-HCl | 0.29±0.04 |
| GP-P | 1,11b-Dihydro-[1]benzopyrano[4,3,2-de]isoquinolin-3(2H)-one-10-sulphonic acid | 0.45±0.02 |
| GP-F | 1-[4-(3-Dimethylamino-propoxy)-phenyl]-8,9-dihydro-7H-2,7,9a-triaza-benzo[cd]azulen-6-one-HCl | 0.48±0.04 |
| GP-L | 8-Fluoro-2-(3-piperidin-1-ylpropanoyl)-1,3,4,5-2H-tetrahydrobenzo[c]-1,6-naphthyridin-6-one-MsOH | 0.61±0.14 |
| GP-G | 2-(4-Methylpiperazin-1-yl)-5H-benzo[c][1,5]naphthyridin-6-one-MsOH | 0.69±0.13 |
| GP-H | 1-Dimethylaminomethyl-8,9-dihydro-7H-2,7,9a-triaza-benzo[cd]azulen-6-one-HCl | 0.96±0.05 |
| GP-N | 2-(4-Isopropylpiperazin-1-yl)-5H-benzo[c][1,5]naphthyridin-6-one-MsOH | 1.05±0.04 |
| GP-I | 1-[2-(4-Pyrrolidin-1-ylmethyl-phenyl)-ethyl]-8,9-dihydro-7H-2,7,9a-triaza-benzo[cd]azulen-6-one hydrochloride-HCl | 4.46±0.95 |
| 5-AIQ | 5-Amino-isoquinoline-HCl | 22.8±2.7 |