Changes in Tm induced by inhibitor binding
ΔTm is calculated by subtracting the native Tm from the inhibitor-bound Tm. Data represent two to six separate experiments, each run in triplicate. All values listed are means ± S.D. The Tm values shown are for the indicated protein in buffer alone.
| GRK | Tma | ΔTm | |||
|---|---|---|---|---|---|
| 500 μM ATP | 10 μM balanol | 10 μM CMPD103A | 10 μM CMPD101 | ||
| °C | |||||
| GRK2 | 36.4 ± 0.8 | 5.0 ± 0.6 | 18.8 ± 0.7 | 15.5 ± 0.7 | 12.4 ± 0.5 |
| I197L | 37.1 ± 0.5 | 20.5 ± 0.6 | 14.6 ± 3.1 | 10.3 ± 2.5 | |
| Y206S | 30.0 ± 0.8 | 6.2 ± 1.0 | 24.3 ± 0.3 | 20.6 ± 0.1 | 16.7 ± 0.5 |
| L235G | 29.7 ± 2.0 | 7.0 ± 1.4 | 16.7 ± 0.9 | 15.7 ± 3.1 | 13.8 ± 2.9 |
| L271M | 31.1 ± 1.4 | 4.8 ± 2.3 | 21.5 ± 0.3 | 17.3 ± 0.6 | 13.8 ± 0.9 |
| GRK1 | 25.3 ± 1.8 | 16.5 ± 1.0 | 9.9 ± 0.6a | 6.2 ± 0.6a | 4.0 ± 0.5a |
| GRK5 | 29.2 ± 1.7 | 7.4 ± 0.7 | 5.8 ± 1.1a | 3.6 ± 0.4a | 2.3 ± 0.3a |
↵a 100 μM balanol, CMPD103A, and CMPD101 were used for GRK1 and GRK5.