Table 2.
In vitro cell-free binding assays
| Compound | IC50 (nM)1 | Ki (nM)2 |
|---|---|---|
| SPEP-1 # | 500 | 115.5 |
| SPEP-2 | - | - |
| SPEP-3 | - | - |
| SPEP-4 # | 300 | 69 |
| SPEP-5*# | 70 | 16 |
| SPEP-6 # | 100 | 23 |
| SPEP-9 # | 100 | 23 |
| SPEP-10*# | 26 | 6 |
| SPEP-11 | 300 | 69 |
| SPEP-12 | 200 | 46 |
| SPEP-13 | 100 | 23 |
| SPEP-19 | 200 | 46 |
| SPEP-21 # | 500 | 115 |
| SPEP-22 # | 700 | 162 |
| SPEP-23 # | 20 | 4 |
| SPEP-24*# | 5 | 1 |
| SPEP-25 # | 200 | 46 |
| SPEP-26*# | 30 | 7 |
| SPEP-27* | 50 | 11 |
| SPEP-29 | 800 | 185 |
| SPEP-35 | 500 | 115 |
| SPEP-36* | 75 | 17 |
| SPEP-38 | 200 | 46 |
| SPEP-41* | 40 | 9 |
| SPEP-42* | 50 | 11 |
| SPEP-43* | 25 | 6 |
| HGSF-1*# | 5 | 1 |
| HGSF-2*# | 2 | 0.5 |
1IC50 calculated as the concentration required to compete 50% of [3H] MB binding. -, no competition
2Ki = IC50 of the compound/(1 + Conc. of MB in the assay/Kd of MB3)
3Kd of MB is 1.5 nM [49]
*Compounds that were selected for cell culture inhibition assay (see Table 3)
#Kinetic binding assays are provided in Supplemental Data 1, for selected compounds