Compound ID | Off target receptor profile | DNA Affinity & Selectivity (Measured by SPR) | Cancer cell activity | ”Normal” Cell activity | |||||
---|---|---|---|---|---|---|---|---|---|
Muscarinic (M2) % inh @1μM | β2 adrenergic %inh @1 μM | hERG % inh @10 μM | Quadruplex DNA affinity Kx106M-1 | Duplex DNA affinity Kx106M-1 | Quadruplex/duplex ratio | HT-29 (GI50/μm) | WI-38 (GI50/μM) | Ratio PMX WI38 /HT29 | |
1 | 98 | 100 | 100 | 9.0 | 0.6 | 16.3 | 0.62 | 7.2 | 11,6 |
2 | 98 | 11 | 41 | 4.2 | 0,2 | 21 | 0.10 | 3.11 | 31,1 |
3 | 98,0 | 13 | 74,0 | 22,0 | 0,1 | 244,4 | 0,70 | 13,04 | 18,5 |
4 | 65 | 1 | 15 | 7.4 | 1,1 | 6,7 | 1,63 | 17.3 | 10,6 |
5 | 93 | 10 | 16 | 23 | <0,1 | >230 | 1,83 | >30 | ND |
6 | 77 | 8 | 35 | 14,7 | 0,7 | 21 | 0,26 | 22,3 | 85,7 |
7 | 92 | 0 | 37 | 29,3 | 0,9 | 32,6 | 0,28 | 9.36 | 33,4 |
8 | 99 | 2 | 40 | 14,2 | 0,9 | 15,8 | 0,75 | 25,12 | 33,5 |
9 | 24 | NE | 86 | 1,5 | <0,1 | >15 | 0,21 | 5,11 | 24,3 |
10 | 49 | NE | 95 | 1,0 | <0,1 | >10 | 0,13 | 6,17 | 47,5 |