1mx1 A 2.4 BS01 SIA A 1 L1051 G1052 N1079 A1080 T1081 S1082 P1084 Y1118 L31 G32 N59 A60 T61 S62 P64 Y98 G1142 G1143 S1221 A1222 E1354 H1468 G122 G123 S201 A202 E334 H447 3.1.1.1,3.1.1.13,3.1.1.56 0004771,0005737,0005783,0005788,0005811,0005829,0006629,0006695,0008203,0009636,0010875,0010887,0016042,0030855,0042632,0043691,0047374,0051791,0052689,0070857,0071397,0071404,0090122,0090205,0106435,0120188 P23141 12725862 182 SSPPVVDTVHGKVLGKFVSLEGFAQPVAIFLGIPFAKPPLGPLRFTPPQPAEPWSFVKNATSYPPMCTQDPKAGQLLSELFTNRKENIPLKLSEDCLYLNIYTPADLTKKNRLPVMVWIHGGGLMVGAASTYDGLALAAHENVVVVTIQYRLGIWGFFSTGDEHSRGNWGHLDQVAALRWVQDNIASFGGNPGSVTIFGESAGGESVSVLVLSPLAKNLFHRAISESGVALTSVLVKKGDVKPLAEQIAITAGCKTTTSAVMVHCLRQKTEEELLETTLKMKFLSLDLQGDPRESQPLLGTVIDGMLLLKTPEELQAERNFHTVPYMVGINKQEFGWLIPMLMSYPLSEGQLDQKTAMSLLWKSYPLVCIAKELIPEATEKYLGGTDDTVKKKDLFLDLIADVMFGVPSVIVARNHRDAGAPTYMYEFQYRPSFSSDMKPKTVIGDHGDELFSVFGAPFLKEGASEEEIRLSKMVMKFWANFARNGNPNGEGLPHWPEYNQKEGYLQIGANTQAAQKLKDKEVAFWTNLFAK 1mx1 A 2.4 BS02 THA A 1 L1097 F1101 S1221 H1468 L77 F81 S201 H447 G1142 G1143 S1221 A1222 E1354 H1468 G122 G123 S201 A202 E334 H447 3.1.1.1,3.1.1.13,3.1.1.56 0004771,0005737,0005783,0005788,0005811,0005829,0006629,0006695,0008203,0009636,0010875,0010887,0016042,0030855,0042632,0043691,0047374,0051791,0052689,0070857,0071397,0071404,0090122,0090205,0106435,0120188 -logKd/Ki=4.00, Ki>100uM IC50=>100000nM, Ki=>100000nM P23141 12725862 1 SSPPVVDTVHGKVLGKFVSLEGFAQPVAIFLGIPFAKPPLGPLRFTPPQPAEPWSFVKNATSYPPMCTQDPKAGQLLSELFTNRKENIPLKLSEDCLYLNIYTPADLTKKNRLPVMVWIHGGGLMVGAASTYDGLALAAHENVVVVTIQYRLGIWGFFSTGDEHSRGNWGHLDQVAALRWVQDNIASFGGNPGSVTIFGESAGGESVSVLVLSPLAKNLFHRAISESGVALTSVLVKKGDVKPLAEQIAITAGCKTTTSAVMVHCLRQKTEEELLETTLKMKFLSLDLQGDPRESQPLLGTVIDGMLLLKTPEELQAERNFHTVPYMVGINKQEFGWLIPMLMSYPLSEGQLDQKTAMSLLWKSYPLVCIAKELIPEATEKYLGGTDDTVKKKDLFLDLIADVMFGVPSVIVARNHRDAGAPTYMYEFQYRPSFSSDMKPKTVIGDHGDELFSVFGAPFLKEGASEEEIRLSKMVMKFWANFARNGNPNGEGLPHWPEYNQKEGYLQIGANTQAAQKLKDKEVAFWTNLFAK 1mx1 B 2.4 BS01 SIA A 1 K2262 T2278 K241 T257 G2142 G2143 S2221 A2222 E2354 H2468 G121 G122 S200 A201 E333 H446 3.1.1.1,3.1.1.13,3.1.1.56 0004771,0005737,0005783,0005788,0005811,0005829,0006629,0006695,0008203,0009636,0010875,0010887,0016042,0030855,0042632,0043691,0047374,0051791,0052689,0070857,0071397,0071404,0090122,0090205,0106435,0120188 P23141 12725862 182 SPPVVDTVHGKVLGKFVSLEGFAQPVAIFLGIPFAKPPLGPLRFTPPQPAEPWSFVKNATSYPPMCTQDPKAGQLLSELFTNRKENIPLKLSEDCLYLNIYTPADLTKKNRLPVMVWIHGGGLMVGAASTYDGLALAAHENVVVVTIQYRLGIWGFFSTGDEHSRGNWGHLDQVAALRWVQDNIASFGGNPGSVTIFGESAGGESVSVLVLSPLAKNLFHRAISESGVALTSVLVKKGDVKPLAEQIAITAGCKTTTSAVMVHCLRQKTEEELLETTLKMKFLSLDLQGDPRESQPLLGTVIDGMLLLKTPEELQAERNFHTVPYMVGINKQEFGWLIPMLMSYPLSEGQLDQKTAMSLLWKSYPLVCIAKELIPEATEKYLGGTDDTVKKKDLFLDLIADVMFGVPSVIVARNHRDAGAPTYMYEFQYRPSFSSDMKPKTVIGDHGDELFSVFGAPFLKEGASEEEIRLSKMVMKFWANFARNGNPNGEGLPHWPEYNQKEGYLQIGANTQAAQKLKDKEVAFWTNLFAK 1mx1 B 2.4 BS02 SIA B 1 L2051 G2052 K2078 N2079 A2080 T2081 S2082 P2084 Y2118 L30 G31 K57 N58 A59 T60 S61 P63 Y97 G2142 G2143 S2221 A2222 E2354 H2468 G121 G122 S200 A201 E333 H446 3.1.1.1,3.1.1.13,3.1.1.56 0004771,0005737,0005783,0005788,0005811,0005829,0006629,0006695,0008203,0009636,0010875,0010887,0016042,0030855,0042632,0043691,0047374,0051791,0052689,0070857,0071397,0071404,0090122,0090205,0106435,0120188 P23141 12725862 282 SPPVVDTVHGKVLGKFVSLEGFAQPVAIFLGIPFAKPPLGPLRFTPPQPAEPWSFVKNATSYPPMCTQDPKAGQLLSELFTNRKENIPLKLSEDCLYLNIYTPADLTKKNRLPVMVWIHGGGLMVGAASTYDGLALAAHENVVVVTIQYRLGIWGFFSTGDEHSRGNWGHLDQVAALRWVQDNIASFGGNPGSVTIFGESAGGESVSVLVLSPLAKNLFHRAISESGVALTSVLVKKGDVKPLAEQIAITAGCKTTTSAVMVHCLRQKTEEELLETTLKMKFLSLDLQGDPRESQPLLGTVIDGMLLLKTPEELQAERNFHTVPYMVGINKQEFGWLIPMLMSYPLSEGQLDQKTAMSLLWKSYPLVCIAKELIPEATEKYLGGTDDTVKKKDLFLDLIADVMFGVPSVIVARNHRDAGAPTYMYEFQYRPSFSSDMKPKTVIGDHGDELFSVFGAPFLKEGASEEEIRLSKMVMKFWANFARNGNPNGEGLPHWPEYNQKEGYLQIGANTQAAQKLKDKEVAFWTNLFAK 1mx1 B 2.4 BS03 THA B 1 S2221 L2304 L2363 S200 L283 L341 G2142 G2143 S2221 A2222 E2354 H2468 G121 G122 S200 A201 E333 H446 3.1.1.1,3.1.1.13,3.1.1.56 0004771,0005737,0005783,0005788,0005811,0005829,0006629,0006695,0008203,0009636,0010875,0010887,0016042,0030855,0042632,0043691,0047374,0051791,0052689,0070857,0071397,0071404,0090122,0090205,0106435,0120188 IC50=>100000nM, Ki=>100000nM P23141 12725862 2 SPPVVDTVHGKVLGKFVSLEGFAQPVAIFLGIPFAKPPLGPLRFTPPQPAEPWSFVKNATSYPPMCTQDPKAGQLLSELFTNRKENIPLKLSEDCLYLNIYTPADLTKKNRLPVMVWIHGGGLMVGAASTYDGLALAAHENVVVVTIQYRLGIWGFFSTGDEHSRGNWGHLDQVAALRWVQDNIASFGGNPGSVTIFGESAGGESVSVLVLSPLAKNLFHRAISESGVALTSVLVKKGDVKPLAEQIAITAGCKTTTSAVMVHCLRQKTEEELLETTLKMKFLSLDLQGDPRESQPLLGTVIDGMLLLKTPEELQAERNFHTVPYMVGINKQEFGWLIPMLMSYPLSEGQLDQKTAMSLLWKSYPLVCIAKELIPEATEKYLGGTDDTVKKKDLFLDLIADVMFGVPSVIVARNHRDAGAPTYMYEFQYRPSFSSDMKPKTVIGDHGDELFSVFGAPFLKEGASEEEIRLSKMVMKFWANFARNGNPNGEGLPHWPEYNQKEGYLQIGANTQAAQKLKDKEVAFWTNLFAK 1mx1 C 2.4 BS01 THA C 1 S3221 V3254 L3255 S200 V233 L234 G3142 G3143 S3221 A3222 E3354 H3468 G121 G122 S200 A201 E333 H446 3.1.1.1,3.1.1.13,3.1.1.56 0004771,0005737,0005783,0005788,0005811,0005829,0006629,0006695,0008203,0009636,0010875,0010887,0016042,0030855,0042632,0043691,0047374,0051791,0052689,0070857,0071397,0071404,0090122,0090205,0106435,0120188 IC50=>100000nM, Ki=>100000nM P23141 12725862 3 SPPVVDTVHGKVLGKFVSLEGFAQPVAIFLGIPFAKPPLGPLRFTPPQPAEPWSFVKNATSYPPMCTQDPKAGQLLSELFTNRKENIPLKLSEDCLYLNIYTPADLTKKNRLPVMVWIHGGGLMVGAASTYDGLALAAHENVVVVTIQYRLGIWGFFSTGDEHSRGNWGHLDQVAALRWVQDNIASFGGNPGSVTIFGESAGGESVSVLVLSPLAKNLFHRAISESGVALTSVLVKKGDVKPLAEQIAITAGCKTTTSAVMVHCLRQKTEEELLETTLKMKFLSLDLQGDPRESQPLLGTVIDGMLLLKTPEELQAERNFHTVPYMVGINKQEFGWLIPMLMSYPLSEGQLDQKTAMSLLWKSYPLVCIAKELIPEATEKYLGGTDDTVKKKDLFLDLIADVMFGVPSVIVARNHRDAGAPTYMYEFQYRPSFSSDMKPKTVIGDHGDELFSVFGAPFLKEGASEEEIRLSKMVMKFWANFARNGNPNGEGLPHWPEYNQKEGYLQIGANTQAAQKLKDKEVAFWTNLFAK 1mx1 D 2.4 BS01 SIA D 1 G4052 K4078 N4079 P4085 Y4118 G31 K57 N58 P64 Y97 G4142 G4143 S4221 A4222 E4354 H4468 G121 G122 S200 A201 E333 H446 3.1.1.1,3.1.1.13,3.1.1.56 0004771,0005737,0005783,0005788,0005811,0005829,0006629,0006695,0008203,0009636,0010875,0010887,0016042,0030855,0042632,0043691,0047374,0051791,0052689,0070857,0071397,0071404,0090122,0090205,0106435,0120188 P23141 12725862 482 SPPVVDTVHGKVLGKFVSLEGFAQPVAIFLGIPFAKPPLGPLRFTPPQPAEPWSFVKNATSYPPMCTQDPKAGQLLSELFTNRKENIPLKLSEDCLYLNIYTPADLTKKNRLPVMVWIHGGGLMVGAASTYDGLALAAHENVVVVTIQYRLGIWGFFSTGDEHSRGNWGHLDQVAALRWVQDNIASFGGNPGSVTIFGESAGGESVSVLVLSPLAKNLFHRAISESGVALTSVLVKKGDVKPLAEQIAITAGCKTTTSAVMVHCLRQKTEEELLETTLKMKFLSLDLQGDPRESQPLLGTVIDGMLLLKTPEELQAERNFHTVPYMVGINKQEFGWLIPMLMSYPLSEGQLDQKTAMSLLWKSYPLVCIAKELIPEATEKYLGGTDDTVKKKDLFLDLIADVMFGVPSVIVARNHRDAGAPTYMYEFQYRPSFSSDMKPKTVIGDHGDELFSVFGAPFLKEGASEEEIRLSKMVMKFWANFARNGNPNGEGLPHWPEYNQKEGYLQIGANTQAAQKLKDKEVAFWTNLFAK 1mx1 D 2.4 BS02 THA D 1 S4221 L4304 L4363 H4468 S200 L283 L341 H446 G4142 G4143 S4221 A4222 E4354 H4468 G121 G122 S200 A201 E333 H446 3.1.1.1,3.1.1.13,3.1.1.56 0004771,0005737,0005783,0005788,0005811,0005829,0006629,0006695,0008203,0009636,0010875,0010887,0016042,0030855,0042632,0043691,0047374,0051791,0052689,0070857,0071397,0071404,0090122,0090205,0106435,0120188 IC50=>100000nM, Ki=>100000nM P23141 12725862 4 SPPVVDTVHGKVLGKFVSLEGFAQPVAIFLGIPFAKPPLGPLRFTPPQPAEPWSFVKNATSYPPMCTQDPKAGQLLSELFTNRKENIPLKLSEDCLYLNIYTPADLTKKNRLPVMVWIHGGGLMVGAASTYDGLALAAHENVVVVTIQYRLGIWGFFSTGDEHSRGNWGHLDQVAALRWVQDNIASFGGNPGSVTIFGESAGGESVSVLVLSPLAKNLFHRAISESGVALTSVLVKKGDVKPLAEQIAITAGCKTTTSAVMVHCLRQKTEEELLETTLKMKFLSLDLQGDPRESQPLLGTVIDGMLLLKTPEELQAERNFHTVPYMVGINKQEFGWLIPMLMSYPLSEGQLDQKTAMSLLWKSYPLVCIAKELIPEATEKYLGGTDDTVKKKDLFLDLIADVMFGVPSVIVARNHRDAGAPTYMYEFQYRPSFSSDMKPKTVIGDHGDELFSVFGAPFLKEGASEEEIRLSKMVMKFWANFARNGNPNGEGLPHWPEYNQKEGYLQIGANTQAAQKLKDKEVAFWTNLFAK 1mx1 E 2.4 BS01 SIA E 1 G5052 K5078 N5079 S5082 Y5083 P5084 Y5118 G31 K57 N58 S61 Y62 P63 Y97 G5142 G5143 S5221 A5222 E5354 H5468 G121 G122 S200 A201 E333 H446 3.1.1.1,3.1.1.13,3.1.1.56 0004771,0005737,0005783,0005788,0005811,0005829,0006629,0006695,0008203,0009636,0010875,0010887,0016042,0030855,0042632,0043691,0047374,0051791,0052689,0070857,0071397,0071404,0090122,0090205,0106435,0120188 P23141 12725862 582 SPPVVDTVHGKVLGKFVSLEGFAQPVAIFLGIPFAKPPLGPLRFTPPQPAEPWSFVKNATSYPPMCTQDPKAGQLLSELFTNRKENIPLKLSEDCLYLNIYTPADLTKKNRLPVMVWIHGGGLMVGAASTYDGLALAAHENVVVVTIQYRLGIWGFFSTGDEHSRGNWGHLDQVAALRWVQDNIASFGGNPGSVTIFGESAGGESVSVLVLSPLAKNLFHRAISESGVALTSVLVKKGDVKPLAEQIAITAGCKTTTSAVMVHCLRQKTEEELLETTLKMKFLSLDLQGDPRESQPLLGTVIDGMLLLKTPEELQAERNFHTVPYMVGINKQEFGWLIPMLMSYPLSEGQLDQKTAMSLLWKSYPLVCIAKELIPEATEKYLGGTDDTVKKKDLFLDLIADVMFGVPSVIVARNHRDAGAPTYMYEFQYRPSFSSDMKPKTVIGDHGDELFSVFGAPFLKEGASEEEIRLSKMVMKFWANFARNGNPNGEGLPHWPEYNQKEGYLQIGANTQAAQKLKDKEVAFWTNLFAK 1mx1 E 2.4 BS02 THA E 1 L5097 S5221 V5254 L5363 L76 S200 V233 L341 G5142 G5143 S5221 A5222 E5354 H5468 G121 G122 S200 A201 E333 H446 3.1.1.1,3.1.1.13,3.1.1.56 0004771,0005737,0005783,0005788,0005811,0005829,0006629,0006695,0008203,0009636,0010875,0010887,0016042,0030855,0042632,0043691,0047374,0051791,0052689,0070857,0071397,0071404,0090122,0090205,0106435,0120188 IC50=>100000nM, Ki=>100000nM P23141 12725862 5 SPPVVDTVHGKVLGKFVSLEGFAQPVAIFLGIPFAKPPLGPLRFTPPQPAEPWSFVKNATSYPPMCTQDPKAGQLLSELFTNRKENIPLKLSEDCLYLNIYTPADLTKKNRLPVMVWIHGGGLMVGAASTYDGLALAAHENVVVVTIQYRLGIWGFFSTGDEHSRGNWGHLDQVAALRWVQDNIASFGGNPGSVTIFGESAGGESVSVLVLSPLAKNLFHRAISESGVALTSVLVKKGDVKPLAEQIAITAGCKTTTSAVMVHCLRQKTEEELLETTLKMKFLSLDLQGDPRESQPLLGTVIDGMLLLKTPEELQAERNFHTVPYMVGINKQEFGWLIPMLMSYPLSEGQLDQKTAMSLLWKSYPLVCIAKELIPEATEKYLGGTDDTVKKKDLFLDLIADVMFGVPSVIVARNHRDAGAPTYMYEFQYRPSFSSDMKPKTVIGDHGDELFSVFGAPFLKEGASEEEIRLSKMVMKFWANFARNGNPNGEGLPHWPEYNQKEGYLQIGANTQAAQKLKDKEVAFWTNLFAK 1mx1 F 2.4 BS01 THA F 1 S6221 V6254 L6363 M6364 S200 V233 L341 M342 G6142 G6143 G6173 S6221 A6222 L6319 E6354 H6468 G121 G122 G152 S200 A201 L298 E333 H446 3.1.1.1,3.1.1.13,3.1.1.56 0004771,0005737,0005783,0005788,0005811,0005829,0006629,0006695,0008203,0009636,0010875,0010887,0016042,0030855,0042632,0043691,0047374,0051791,0052689,0070857,0071397,0071404,0090122,0090205,0106435,0120188 IC50=>100000nM, Ki=>100000nM P23141 12725862 6 SPPVVDTVHGKVLGKFVSLEGFAQPVAIFLGIPFAKPPLGPLRFTPPQPAEPWSFVKNATSYPPMCTQDPKAGQLLSELFTNRKENIPLKLSEDCLYLNIYTPADLTKKNRLPVMVWIHGGGLMVGAASTYDGLALAAHENVVVVTIQYRLGIWGFFSTGDEHSRGNWGHLDQVAALRWVQDNIASFGGNPGSVTIFGESAGGESVSVLVLSPLAKNLFHRAISESGVALTSVLVKKGDVKPLAEQIAITAGCKTTTSAVMVHCLRQKTEEELLETTLKMKFLSLDLQGDPRESQPLLGTVIDGMLLLKTPEELQAERNFHTVPYMVGINKQEFGWLIPMLMSYPLSEGQLDQKTAMSLLWKSYPLVCIAKELIPEATEKYLGGTDDTVKKKDLFLDLIADVMFGVPSVIVARNHRDAGAPTYMYEFQYRPSFSSDMKPKTVIGDHGDELFSVFGAPFLKEGASEEEIRLSKMVMKFWANFARNGNPNGEGLPHWPEYNQKEGYLQIGANTQAAQKLKDKEVAFWTNLFAK