Residue | CCL1 | LMD-009 | |||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Potency | Potency | ||||||||||||
Position | Number | EC50 | EC50 | -Fold | n | Efficacy (Emax) | Basal Activity | EC50 | EC50 | -Fold | n | Efficacy (Emax) | |
S | B-W | ||||||||||||
Log | nM | cpm | cpm | Log | nM | cpm | |||||||
wt | wt | wt | −8.1 ± 0.03 | 8.7 | 1.0 | 65 | 4000 ± 314 | 712 ± 40 | −8.0 ± 0.17 | 11 | 1.0 | 11 | 3774 ± 448 |
I:07 | 1.39 | Y42A | −7.9 ± 0.13 | 11 | 1.3 | 9 | 2238 ± 370 | 786 ± 120 | −6.8 ± 0.09 | 158 | 15 | 3 | 1471 ± 302 |
I:11 | 1.43 | F46A | |||||||||||
II:13 | 2.53 | F84A | −8.4 ± 0.13 | 4.0 | 0.46 | 8 | 2098 ± 278 | 1009 ± 87 | −7.9 ± 0.09 | 14 | 1.3 | 3 | 1441 ± 158 |
II:17 | 2.57 | F88A | −8.0 ± 0.05 | 10 | 1.2 | 9 | 2445 ± 419 | 799 ± 118 | −7.0 ± 0.05 | 108 | 10 | 4 | 1107 ± 450 |
II:20 | 2.60 | Q91W | −7.2 ± 0.14 | 69 | 7.9 | 6 | 1232 ± 101 | 665 ± 58 | −7.0 ± 0.18 | 108 | 10 | 3 | 2916 ± 92 |
III:04 | 3.28 | V109A | −8.1 ± 0.07 | 8.2 | 0.95 | 3 | 2100 ± 356 | 940 ± 269 | −8.1 ± 0.21 | 7.7 | 0.73 | 3 | 2193 ± 297 |
III:05 | 3.29 | S110A | −8.8 ± 0.10 | 1.6 | 0.18 | 8 | 2804 ± 723 | 861 ± 214 | −8.8 ± 0.41 | 1.5 | 0.14 | 4 | 1066 ± 596 |
III:05 | 3.29 | S110H | <−6 | >1000 | >137 | 7 | N.E. | 556 ± 850 | <−5 | >10,000 | >950 | 2 | N.E. |
III:05 | 3.29 | S110W | <−6 | >1000 | >137 | 5 | N.E. | 400 ± 108 | <−5 | >10,000 | >950 | 2 | N.E. |
III:07 | 3.31 | F112A | −8.3 ± 0.07 | 4.6 | 0.53 | 9 | 3706 ± 552 | 651 ± 88 | −7.9 ± 0.04 | 11 | 1.1 | 4 | 2394 ± 702 |
III:08 | 3.32 | Y113A | −6.5 ± 0.12 | 323 | 37 | 10 | 1047 ± 185 | 570 ± 57 | <−5 ± 0.00 | >10,000 | >950 | 5 | N.E. |
III:09 | 3.33 | Y114A | −6.9 ± 0.13 | 131 | 15 | 4 | 2692 ± 784 | 927 ± 200 | −7.4 ± 0.09 | 42 | 3.9 | 6 | 3652 ± 710 |
III:18 | 3.42 | F123A | −8.4 ± 0.15 | 4.4 | 0.51 | 6 | 1466 ± 371 | 426 ± 64 | −8.2 ± 0.14 | 7.0 | 0.66 | 3 | 1430 |
IV:20 | 4.60 | L168D | −7.9 ± 0.18 | 12 | 1.4 | 11 | 3549 ± 537 | 948 ± 122 | −7.8 ± 0.17 | 18 | 1.7 | 2 | 4410 ± 1576 |
IV:24 | 4.64 | Y172A | −8.0 ± 0.11 | 11 | 1.3 | 8 | 2000 ± 155 | 1315 ± 110 | −7.7 ± 0.15 | 21 | 2.0 | 4 | 1557 ± 329 |
V:−02 | 5.33 | K193A | −7.7 ± 0.17 | 22 | 2.6 | 6 | 2956 ± 352 | 659 ± 89 | −8.1 ± 0.37 | 8.5 | 0.80 | 2 | 3414 ± 298 |
V:−01 | 5.34 | W194A | −6.9 ± 0.29 | 128 | 15 | 5 | 2500 ± 142 | 673 ± 44 | −8.1 ± 0.23 | 7.6 | 0.72 | 3 | 1273 ± 207 |
V:01 | 5.35 | K195A | −8.1 ± 0.09 | 7.5 | 0.87 | 7 | 1947 ± 314 | 666 ± 97 | −8.2 ± 0.30 | 6.2 | 0.59 | 3 | 2370 ± 485 |
V:12 | 5.46 | G206A | −7.2 ± 0.13 | 67 | 7.7 | 9 | 904 ± 63 | 508 ± 54 | −7.7 ± 0.08 | 19 | 1.4 | 3 | 744 ± 59 |
V:12 | 5.46 | G206W | N.A. | 8 | 501 ± 75 | N.A. | N.A. | 3 | |||||
VI:13 | 6.48 | W251Q | 8.5 ± 0.12 | 3.4 | 0.39 | 10 | 2245 ± 347 | 1146 ± 152 | −7.8 ± 0.34 | 44 | 4.1 | 3 | 1112 ± 468 |
VI:13 | 6.48 | W251Q | −8.2 ± 0.14 | 6.6 | 0.76 | 6 | 2528 ± 320 | 1097 ± 166 | −7.4 ± 0.34 | 44 | 4.1 | 3 | 1112 ± 468 |
VI:16 | 6.51 | F254A | −7.0 ± 0.09 | 109 | 13 | 10 | 3131 ± 609 | 835 ± 74 | −9.2 ± 0.24 | 0.57 | 0.05 | 5 | 6640 ± 1484 |
VI:20 | 6.55 | L258A | −7.6 ± 0.11 | 27 | 3.2 | 9 | 2699 ± 262 | 591 ± 54 | −7.9 ± 0.20 | 13 | 1.2 | 3 | 3162 ± 568 |
VI:24 | 6.59 | S262A | −8.3 ± 0.10 | 5.2 | 0.60 | 10 | 2949 ± 420 | 621 ± 67 | −7.7 ± 0.16 | 21 | 2.0 | 4 | 1854 ± 815 |
VII:03 | 7.36 | H283A | −7.9 ± 0.09 | 12 | 1.4 | 8 | 4003 ± 444 | 705 ± 58 | −7.6 ± 0.14 | 24 | 2.2 | 3 | 3644 ± 1595 |
VII:06 | 7.39 | E286A | −7.9 ± 0.11 | 12 | 1.4 | 11 | 3732 ± 578 | 930 ± 96 | <−5 | >10000 | >950 | 5 | N.E. |
VII:09 | 7.42 | S289A | −7.7 ± 0.14 | 18 | 2.1 | 3 | 9229 ± 3007 | 842 ± 293 | −7.8 ± 0.03 | 16 | 1.5 | 3 | 10833 ± 2827 |
VII:10 | 7.43 | F290A | −8.2 ± 0.20 | 6 | 0.68 | 5 | 4325 ± 940 | 2497 ± 517 | −7.7 ± 0.08 | 20 | 1.9 | 5 | 3700 ± 789 |
N.E., not estimated due to no plateau; N.A., no activation at all.