Construct | CGS21680 | LUF5834 | |||
---|---|---|---|---|---|
pKi High (Ki High) | pKi Low (Ki Low) | Change | pKi (Ki) | Change | |
nM | fold | nM | fold | ||
Wild-type | 6.8 ± 0.1 (159) | 5.4 ± 0.1 (3680) | 1.0 | 7.1 ± 0.2 (79.6) | 1.0 |
T883.36A | N.D. | N.D. | >1000 | 6.9 ± 0.1 (127) | 1.6 |
S2777.42A | N.D. | N.D. | >1000 | 7.8 ± 0.0 (17.7) | 0.2 |
N.D., not determined; the potency was too low to determine an accurate EC50 value.