Residue | LMD-584 | LMD-902 | LMD-268 | LMD-174 | ||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Position | Number | |||||||||||||||||
S | B-W | EC50 | EC50 | -Fold | n | EC50 | EC50 | -Fold | n | EC50 | EC50 | -Fold | n | EC50 | EC50 | -Fold | n | |
Log | nM | Log | nM | Log | nM | Log | nM | |||||||||||
wt | wt | −7.5 ± 0.07 | 29 | 1.0 | 15 | −7.8 ± 0.10 | 15 | 1.0 | 8 | −8.0 ± 0.05 | 9.0 | 1.0 | 4 | −7.5 ± 0.05 | 30 | 1.0 | 15 | |
I:07 | 1.39 | Y42A | −6.9 ± 0.04 | 131 | 4.6 | 3 | −6.7 ± 0.18 | 178 | 12 | 3 | −6.8 ± 0.22 | 172 | 19 | 3 | −6.7 ± 0.14 | 199 | 6.6 | 3 |
I:11 | 1.43 | F46A | −6.9 ± 0.05 | 126 | 4.4 | 3 | −7.3 ± 0.07 | 50 | 3.4 | 3 | −7.4 ± 0.06 | 43 | 4.8 | 2 | −7.3 ± 0.18 | 52 | 1.7 | 3 |
II:13 | 2.53 | F84A | −8.2 ± 0.25 | 7.0 | 0.24 | 4 | −7.9 ± 0.03 | 12 | 0.85 | 3 | −8.3 ± 0.06 | 4.8 | 0.54 | 4 | −6.9 ± 0.28 | 133 | 4.4 | 4 |
II:17 | 2.57 | F88A | −6.6 ± 0.19 | 251 | 8.8 | 3 | −6.7 ± 0.20 | 197 | 14 | 4 | −7.5 ± 0.23 | 31 | 3.5 | 3 | −7.0 ± 0.05 | 94 | 3.1 | 3 |
II:20 | 2.60 | Q91W | −6.4 ± 0.36 | 368 | 13 | 3 | −6.7 ± 0.13 | 180 | 12 | 3 | −6.8 ± 0.25 | 161 | 18 | 3 | −6.7 ± 0.17 | 201 | 6.7 | 3 |
III:04 | 3.28 | V109A | −7.5 ± 0.26 | 34 | 1.2 | 3 | −8.1 ± 0.05 | 8 | 0.52 | 3 | −8.6 ± 0.11 | 2.6 | 0.29 | 3 | −7.5 ± 0.18 | 33 | 1.1 | 3 |
III:05 | 3.29 | S110A | −8.2 ± 0.38 | 6.0 | 0.21 | 4 | −8.7 ± 0.34 | 2 | 0.15 | 3 | −8.8 ± 0.11 | 1.6 | 0.18 | 6 | −8.4 ± 0.15 | 3.6 | 0.12 | 4 |
III:05 | 3.29 | S110H | <−5 | >10,000 | >323 | 3 | <−5 ± 0.00 | >10,000 | >689 | 2 | <−5 | >10,000 | >1100 | 2 | <−5 | >10,000 | >323 | 3 |
III:05 | 3.29 | S110W | <−5 | >10,000 | >323 | 4 | <−5 ± 0.00 | >10,000 | >689 | 2 | <−5 | >10,000 | >1100 | 3 | <−5 | >10,000 | >323 | 3 |
III:07 | 3.31 | F112A | −7.3 ± 0.08 | 51 | 1.8 | 4 | −7.9 ± 0.09 | 13 | 0.88 | 4 | −8.1 ± 0.08 | 7.1 | 0.79 | 6 | −7.4 ± 0.08 | 37 | 1.2 | 4 |
III:08 | 3.32 | Y113A | <−5 ± 0.00 | >10,000 | >323 | 3 | >−5 | >10,000 | >689 | 3 | <−5 | >10,000 | >1100 | 3 | <−5 ± | >10,000 | >332 | 3 |
III:09 | 3.33 | Y114A | −6.4 ± 0.32 | 430 | 15 | 3 | −6.7 ± 0.11 | 191 | 13 | 3 | −6.2 ± 0.06 | 579 | 64 | 3 | −6.0 ± 0.11 | 945 | 31 | 3 |
III:18 | 3.42 | F123A | −7.7 ± 0.14 | 21 | 0.73 | 3 | −7.9 ± 0.02 | 12 | 0.85 | 3 | −8.3 ± 0.17 | 5.0 | 0.56 | 5 | −7.7 ± 0.07 | 19 | 0.63 | 3 |
IV:24 | 4.64 | Y172A | −7.3 ± 0.19 | 56 | 1.9 | 4 | −7.5 ± 0.15 | 31 | 2.1 | 3 | −7.6 ± 0.20 | 28 | 3.1 | 3 | −7.0 ± 0.04 | 93 | 3.1 | 5 |
V:−02 | 5.34 | K193A | −7.5 ± 0.18 | 31 | 1.1 | 4 | −7.8 ± 0.52 | 17 | 1.2 | 2 | −8.3 ± 0.17 | 4.7 | 0.52 | 3 | −7.5 ± 0.06 | 30 | 1.0 | 3 |
V:−01 | 5.33 | W194A | −7.9 ± 0.15 | 12 | 0.44 | 4 | −8.4 ± 0.40 | 4 | 0.29 | 3 | −8.2 ± 0.18 | 6 | 0.71 | 3 | −7.5 ± 0.11 | 32 | 1.1 | 3 |
V:01 | 5.35 | K195A | −7.7 ± 0.17 | 20 | 0.70 | 5 | −8.2 ± 0.25 | 7 | 0.48 | 3 | −9.7 ± 0.20 | 0.22 | 0.02 | 2 | −7.5 ± 0.05 | 30 | 1.0 | 4 |
V:12 | 5.46 | G206A | −7.3 ± 0.21 | 47 | 1.6 | 3 | −7.9 ± 0.04 | 12 | 0.83 | 3 | −8.8 0.10 | 2 | 0.19 | 2 | −7.20.5 | 62 | 2.1 | 3 |
V:12 | 5.46 | G206W | N.A. | 3 | N.A. | 3 | N.A. | 3 | 3 | |||||||||
VI:13 | 6.48 | W251A | −7.7 ± 0.38 | 20 | 0.70 | 3 | −8.30.14 | 4.7 | 0.32 | 2 | −7.4 ± 0.25 | 42 | 4.7 | 4 | −7.5 ± 0.41 | 29 | 0.97 | 3 |
VI:13 | 6.48 | W251Q | −7.7 ± 0.41 | 22 | 0.77 | 3 | −7.80.14 | 15 | 1.0 | 2 | −8.0 ± 0.39 | 10 | 1.1 | 3 | −7.5 ± 0.41 | 29 | 0.97 | 3 |
VI:16 | 6.51 | F254A | −6.6 ± 0.19 | 278 | 9.7 | 4 | −7.1 ± 0.04 | 80 | 5.5 | 3 | −8.0 ± 0.12 | 10 | 1.2 | 3 | −7.4 ± 0.13 | 42 | 1.4 | 3 |
VI:20 | 6.55 | L258A | −6.5 ± 0.29 | 329 | 12 | 3 | −7.5 ± 0.08 | 35 | 2.4 | 3 | −7.2 ± 0.05 | 65 | 7.2 | 5 | −7.2 ± 0.08 | 64 | 2.1 | 3 |
VI:24 | 6.59 | S262A | −7.2 ± 0.13 | 61 | 2.1 | 3 | −7.9 ± 0.10 | 13 | 0.86 | 3 | −8.1 ± 0.28 | 8.9 | 1.0 | 5 | −7.4 ± 0.02 | 39 | 1.3 | 3 |
VII:02 | 7.35 | T282A | −7.1 ± 0.07 | 77 | 2.7 | 3 | −7.5 ± 0.10 | 31 | 2.1 | 3 | −7.4 ± 0.08 | 40 | 4.4 | 3 | −7.0 ± 0.06 | 93 | 3.1 | 3 |
VII:03 | 7.36 | H283A | −7.5 ± 0.08 | 30 | 1.0 | 3 | −7.5 ± 0.06 | 34 | 2.4 | 3 | −7.8 ± 0.11 | 17 | 1.9 | 3 | −7.3 ± 0.09 | 46 | 1.5 | 3 |
VII:06 | 7.39 | E286A | <−5 | >10,000 | >323 | 3 | <−5 | >10,000 | >689 | 3 | <−5 | >10,000 | >1100 | 5 | <−5 | >10,000 | >332 | 3 |
VII:09 | 7.42 | S289A | −6.7 ± 0.27 | 211 | 7.4 | 3 | −7.5 ± 0.04 | 34 | 2.3 | 3 | −7.8 ± 0.08 | 17 | 1.9 | 3 | −7.4 ± 0.02 | 36 | 1.2 | 3 |
VII:10 | 7.43 | F290A | −7.4 ± 0.24 | 41 | 1.4 | 3 | −7.6 ± 0.31 | 26 | 1.8 | 3 | −7.7 ± 0.34 | 21 | 2.3 | 4 | −7.5 ± 0.46 | 29 | 1.0 | 3 |
N.A., no activation at all.