Table 3. The potency of HC-070 on various human TRPC5 (hTRPC5) constructs.
| TRPC5 constructs | HC-070 | |||
|---|---|---|---|---|
| LogIC50* | Hill slope | IC50 (nM) | ||
| hTRPC5 WT | 2.31 ± 0.10 | −1.52 | 204.3 | |
| Mutations in HC-070-binding pocket | ||||
| C525A | 2.16 ± 0.15 | −1.03 | 145.8 | |
| R557A | 2.52 ± 0.07 | −1.45 | 329.7 | |
| F569A | 2.86 ± 0.15 | −1.21 | 727.4 | |
| L572A | 2.74 ± 0.17 | −1.58 | 552.7 | |
| Q573A | 3.10 ± 0.61 | −1.75 | >1000 | |
| F599A | 2.67 ± 0.29 | −1.09 | 467.9 | |
| F599N | 3.57 ± 1.55 | −0.86 | >1000 | |
| T603A | 2.68 ± 0.16 | −1.20 | 472.7 | |
| T607A | 2.43 ± 0.12 | −3.13 | 268.4 | |
* Data were expressed as logIC50 ± SEM, n = 3.