Table 1.
Biochemical Activities of p97 Inhibitorsa
| Entry | Compound ID | R1 Indole Substitution (R2) | ADPGlo IC50 [μM] | ADPGlo Std. Dev. |
|---|---|---|---|---|
| 1 | UPCDC30283 (1) | 5-CN (H) | 0.044 | 0.045 |
| 2 | UPCDC30287 (2) | 5-NO2 (H) | 0.047 | 0.040 |
| 3 | UPCDC30346 (3) | 5-F (Me) | 0.050 | 0.044 |
| 4 | UPCDC30245 (4) | 5-F (H) | 0.055 | 0.087 |
| 5 | UPCDC30361 (5) | 5-CN (Me) | 0.087 | 0.047 |
| 6 | UPCDC30310 (6) | 5-CONH2 (H) | 0.10 | 0.032 |
| 7 | UPCDC30256 (7) | 5-OH (H) | 0.12 | 0.073 |
| 8 | UPCDC30341 (8) | 5-CO2Me (H) | 0.13 | 0.076 |
| 9 | UPCDC30083 (9) | 5-H (H) | 0.16 | 0.10 |
| 10 | UPCDC30317 (10) | 5-Cl (H) | 0.19 | 0.14 |
| 11 | UPCDC30288 (11) | 5-N3 (H) | 0.23 | 0.18 |
| 12 | UPCDC30318 (12) | 5-CH3 (H) | 0.24 | 0.11 |
| 13 | UPCDC30206 (13) | benzo[α]carbazole | 0.39 | 0.069 |
| 14 | UPCDC30367 (14) | 5-CONHMe (H) | 0.45 | 0.12 |
| 15 | UPCDC30238 (15) | 5-OCH3 (H) | 0.71 | 0.22 |
| 16 | UPCDC30257 (16) | 5-OCF3 (H) | 3.8 | 0.8 |
| 17 | UPCDC30345 (17) | 5-azaindole (H) | 4.0 | 1.7 |
| 18 | UPCDC30297 (18) | 5-CF3 (H) | 4.67 | 2.0 |
| 19 | UPCDC30381 (19) | 5-F,7-azaindole (H) | 4.74 | 1.3 |
| 20 | UPCDC30222 (20) | naphthalene (H) | 5.2 | 1.1 |
| 21 | UPCDC30221 (21) | benzofuran (H) | 20.1 | 4.60 |
| 22 | UPCDC30277 (22) | 5-SF5 (H) | 21.5 | 0.40 |
| 23 | UPCDC30368 (23) | 5-CONMe2 (H) | 31.4 | 1.60 |
| 24 | UPCDC30250 (24) | benzimidazole (H) | 38.5 | 6.60 |
| 25 | UPCDC30201 (25) | N-Me indole (H) | >50 | - |