Table 2.
Binding affinities of compound 1 analogs reveal the importance of the triple-ring and imino group of compound 1
Compound | Structure | SMN | UHRF1 |
---|---|---|---|
Kd (µM) | |||
1 | ![]() |
2.6 ± 0.1 | 16 ± 1 |
2 | ![]() |
9.3 ± 0.6 | No binding |
3 | ![]() |
31 ± 2 | No binding |
4 | ![]() |
13 ± 1 | No binding |
5 | ![]() |
12 ± 1 | No binding |
6 | ![]() |
12 ± 2 | Weak binding |
7 | ![]() |
No binding | No binding |
8 | ![]() |
No binding | No binding |
9 | ![]() |
No binding | No binding |
10 | ![]() |
No binding | No binding |
11 | ![]() |
No binding | No binding |
12 | ![]() |
No binding | No binding |
13 | ![]() |
No binding | No binding |
14 | ![]() |
No binding | No binding |
15 | ![]() |
No binding | No binding |
16 | ![]() |
No binding | No binding |
17 | ![]() |
No binding | No binding |
18 | ![]() |
No binding | No binding |
19 | ![]() |
No binding | No binding |
20 | ![]() |
No binding | No binding |
ITC data shown are representative of two independent experiments. Source data are provided as a Source Data file. Kd: binding affinity.