Clofilium | Quinidine | TBA | ||||
---|---|---|---|---|---|---|
Mutant | IC50 | ΔEbind fl. | ΔEbind ri. | IC50 | ΔEbind fl. | IC50 |
nM (n) | kcal/mol | kcal/mol | μM (n) | kcal/mol | μM (n) | |
hEAG1 | 0.79 ± 0.09 (5) | 0.0 | 0.0 | 2.08 ± 0.36 (5) | 0.0 | 1.15 ± 0.07 (4) |
S436T | 7.87 ± 0.76 (6) | 9.5 | −0.5 | 3.90 ± 0.80 (4) | 5.1 | 68.4 ± 4.6 (5) |
V437I | 3.04 ± 0.41 (4) | 1.5 | 0.6 | 5.77 ± 0.39 (6) | 4.5 | 5.96 ± 0.25 (5) |
S436T/V437I | 30.0 ± 4.4 (6) | 10.8 | −0.7 | 27.2 ± 4.7 (6) | 4.1 | 198 ± 23 (6) |
A453S | 4.67 ± 0.50 (5) | 0.6 | 0.2 | 4.60 ± 1.27 (7) | 0.1 | 1.97 ± 0.68 (5) |
E1-c2 | 77.3 ± 19.2 (5) | 55.6 ± 13.7 (7) | 198 ± 33 (5) | |||
E1-c2 TIS/SVA | 7.90 ± 0.95 (6) | 7.27 ± 0.41 (5) | 12.5 ± 1.3 (5) | |||
S433A | 1.48 ± 0.20 (6) | 0.31 ± 0.06 (5) | 0.089 ± 0.011 (5) | |||
S433C | 0.60 ± 0.08 (5) | 0.39 ± 0.01 (4) | 0.29 ± 0.09 (5) |