3f5p A 2.9 BS01 741 A 1 L1005 A1031 K1033 F1047 E1050 M1079 M1082 T1083 M1142 L26 A52 K54 F68 E71 M100 M103 T104 M158 D1135 R1139 N1140 D1153 E1162 D151 R155 N156 D169 E178 2.7.10.1 0004672,0004713,0004714,0005524,0006468,0007169,0016020 -logKd/Ki=6.85, IC50=0.140uM IC50=140nM P08069 19041240 1 SFSAADVYVPDEWEVAREKITMSRELGQGSFGMVYEGVAKGVVKDEPETRVAIKTVNEAASMRERIEFLNEASVMKEFNCHHVVRLLGVVSQGQPTLVIMELMTRGDLKSYLRSLRPEMLAPPSLSKMIQMAGEIADGMAYLNANKFVHRDLAARNCMVAEDFTVKIGDFGMTRDIYETDYYRKGGKGLLPVRWMSPESLKDGVFTTYSDVWSFGVVLWEIATLAEQPYQGLSNEQVLRFVMEGGLLDKPDNCPDMLFELMRMCWQYNPKMRPSFLEIISSIKEEMEPGFREVSFYYSEENK 3f5p B 2.9 BS01 741 B 1 L1005 A1031 K1033 E1050 V1077 M1079 L1081 M1082 T1083 G1085 L26 A52 K54 E71 V98 M100 L102 M103 T104 G106 D1135 R1139 N1140 D1153 E1162 D150 R154 N155 D168 E177 2.7.10.1 0004672,0004713,0004714,0005524,0006468,0007169,0016020 IC50=140nM P08069 19041240 2 SFSAADVYVPDEWEVAREKITMSRELGQGSFGMVYEGVAKGVVKDEPETRVAIKTVNEAASMRERIEFLNEASVMKEFNCHHVVRLLGVVSQGQPTLVIMELMTRGDLKSYLRSLRPELAPPSLSKMIQMAGEIADGMAYLNANKFVHRDLAARNCMVAEDFTVKIGDFGMTRDIYETDYYRKGGKGLLPVRWMSPESLKDGVFTTYSDVWSFGVVLWEIATLAEQPYQGLSNEQVLRFVMEGGLLDKPDNCPDMLFELMRMCWQYNPKMRPSFLEIISSIKEEMEPGFREVSFYYSEENK 3f5p C 2.9 BS01 741 C 1 L1005 A1031 K1033 E1050 M1054 M1079 M1082 T1083 M1142 L26 A52 K54 E71 M75 M100 M103 T104 M160 D1135 R1139 N1140 D1153 E1162 D153 R157 N158 D171 E180 2.7.10.1 0004672,0004713,0004714,0005524,0006468,0007169,0016020 IC50=140nM P08069 19041240 3 SFSAADVYVPDEWEVAREKITMSRELGQGSFGMVYEGVAKGVVKDEPETRVAIKTVNEAASMRERIEFLNEASVMKEFNCHHVVRLLGVVSQGQPTLVIMELMTRGDLKSYLRSLRPEMPVLAPPSLSKMIQMAGEIADGMAYLNANKFVHRDLAARNCMVAEDFTVKIGDFGMTRDIYETDYYRKGGKGLLPVRWMSPESLKDGVFTTYSDVWSFGVVLWEIATLAEQPYQGLSNEQVLRFVMEGGLLDKPDNCPDMLFELMRMCWQYNPKMRPSFLEIISSIKEEMEPGFREVSFYYSEENK 3f5p D 2.9 BS01 741 D 1 L1005 S1009 A1031 K1033 F1047 M1079 M1082 T1083 M1142 L26 S30 A52 K54 F68 M100 M103 T104 M156 D1135 R1139 N1140 D1153 E1162 D149 R153 N154 D167 E176 2.7.10.1 0004672,0004713,0004714,0005524,0006468,0007169,0016020 IC50=140nM P08069 19041240 4 SFSAADVYVPDEWEVAREKITMSRELGQGSFGMVYEGVAKGVVKDEPETRVAIKTVNEAASMRERIEFLNEASVMKEFNCHHVVRLLGVVSQGQPTLVIMELMTRGDLKSYLRSLRPLAPPSLSKMIQMAGEIADGMAYLNANKFVHRDLAARNCMVAEDFTVKIGDFGMTRDIYETDYYRKGGKGLLPVRWMSPESLKDGVFTTYSDVWSFGVVLWEIATLAEQPYQGLSNEQVLRFVMEGGLLDKPDNCPDMLFELMRMCWQYNPKMRPSFLEIISSIKEEMEPGFREVSFYYSEENK 3f5p E 2.9 BS01 741 E 1 L1005 A1031 K1033 F1047 V1077 M1079 L1081 M1082 T1083 R1084 M1142 L26 A52 K54 F68 V98 M100 L102 M103 T104 R105 M159 D1135 R1139 N1140 D1153 E1162 D152 R156 N157 D170 E179 2.7.10.1 0004672,0004713,0004714,0005524,0006468,0007169,0016020 IC50=140nM P08069 19041240 5 SFSAADVYVPDEWEVAREKITMSRELGQGSFGMVYEGVAKGVVKDEPETRVAIKTVNEAASMRERIEFLNEASVMKEFNCHHVVRLLGVVSQGQPTLVIMELMTRGDLKSYLRSLRPEPVLAPPSLSKMIQMAGEIADGMAYLNANKFVHRDLAARNCMVAEDFTVKIGDFGMTRDIYETDYYRKGGKGLLPVRWMSPESLKDGVFTTYSDVWSFGVVLWEIATLAEQPYQGLSNEQVLRFVMEGGLLDKPDNCPDMLFELMRMCWQYNPKMRPSFLEIISSIKEEMEPGFREVSFYYSEEN 3f5p F 2.9 BS01 741 F 1 L1005 S1009 V1013 A1031 K1033 F1047 E1050 V1077 M1079 L1081 M1082 T1083 M1142 L26 S30 V34 A52 K54 F68 E71 V98 M100 L102 M103 T104 M159 D1135 R1139 N1140 D1153 E1162 D152 R156 N157 D170 E179 2.7.10.1 0004672,0004713,0004714,0005524,0006468,0007169,0016020 IC50=140nM P08069 19041240 6 SFSAADVYVPDEWEVAREKITMSRELGQGSFGMVYEGVAKGVVKDEPETRVAIKTVNEAASMRERIEFLNEASVMKEFNCHHVVRLLGVVSQGQPTLVIMELMTRGDLKSYLRSLRPEPVLAPPSLSKMIQMAGEIADGMAYLNANKFVHRDLAARNCMVAEDFTVKIGDFGMTRDIYETDYYRKGGKGLLPVRWMSPESLKDGVFTTYSDVWSFGVVLWEIATLAEQPYQGLSNEQVLRFVMEGGLLDKPDNCPDMLFELMRMCWQYNPKMRPSFLEIISSIKEEMEPGFREVSFYYSEEN 3f5p G 2.9 BS01 741 G 1 L1005 S1009 A1031 K1033 F1047 E1050 V1077 M1079 L1081 M1082 T1083 M1142 L26 S30 A52 K54 F68 E71 V98 M100 L102 M103 T104 M159 D1135 R1139 N1140 D1153 E1162 D152 R156 N157 D170 E179 2.7.10.1 0004672,0004713,0004714,0005524,0006468,0007169,0016020 IC50=140nM P08069 19041240 7 SFSAADVYVPDEWEVAREKITMSRELGQGSFGMVYEGVAKGVVKDEPETRVAIKTVNEAASMRERIEFLNEASVMKEFNCHHVVRLLGVVSQGQPTLVIMELMTRGDLKSYLRSLRPEPVLAPPSLSKMIQMAGEIADGMAYLNANKFVHRDLAARNCMVAEDFTVKIGDFGMTRDIYETDYYRKGGKGLLPVRWMSPESLKDGVFTTYSDVWSFGVVLWEIATLAEQPYQGLSNEQVLRFVMEGGLLDKPDNCPDMLFELMRMCWQYNPKMRPSFLEIISSIKEEMEPGFREVSFYYSEEN 3f5p H 2.9 BS01 741 H 1 L1005 S1009 F1010 A1031 K1033 M1079 L1081 M1082 T1083 M1142 L26 S30 F31 A52 K54 M100 L102 M103 T104 M158 D1135 R1139 N1140 D1153 E1162 D151 R155 N156 D169 E178 2.7.10.1 0004672,0004713,0004714,0005524,0006468,0007169,0016020 IC50=140nM P08069 19041240 8 SFSAADVYVPDEWEVAREKITMSRELGQGSFGMVYEGVAKGVVKDEPETRVAIKTVNEAASMRERIEFLNEASVMKEFNCHHVVRLLGVVSQGQPTLVIMELMTRGDLKSYLRSLRPEMLAPPSLSKMIQMAGEIADGMAYLNANKFVHRDLAARNCMVAEDFTVKIGDFGMTRDIYETDYYRKGGKGLLPVRWMSPESLKDGVFTTYSDVWSFGVVLWEIATLAEQPYQGLSNEQVLRFVMEGGLLDKPDNCPDMLFELMRMCWQYNPKMRPSFLEIISSIKEEMEPGFREVSFYYSEENK 3f5p I 2.9 BS01 741 I 1 L1005 A1031 K1033 F1047 E1050 V1077 M1079 M1082 T1083 M1142 L26 A52 K54 F68 E71 V98 M100 M103 T104 M154 D1135 R1139 N1140 D1153 E1162 D147 R151 N152 D165 E174 2.7.10.1 0004672,0004713,0004714,0005524,0006468,0007169,0016020 IC50=140nM P08069 19041240 9 SFSAADVYVPDEWEVAREKITMSRELGQGSFGMVYEGVAKGVVKDEPETRVAIKTVNEAASMRERIEFLNEASVMKEFNCHHVVRLLGVVSQGQPTLVIMELMTRGDLKSYLRSLRPPPSLSKMIQMAGEIADGMAYLNANKFVHRDLAARNCMVAEDFTVKIGDFGMTRDIYETDYYRKGGKGLLPVRWMSPESLKDGVFTTYSDVWSFGVVLWEIATLAEQPYQGLSNEQVLRFVMEGGLLDKPDNCPDMLFELMRMCWQYNPKMRPSFLEIISSIKEEMEPGFREVSFYYSEEN 3f5p J 2.9 BS01 741 J 1 L1005 A1031 K1033 F1047 E1050 V1077 M1079 L1081 M1082 T1083 M1142 L26 A52 K54 F68 E71 V98 M100 L102 M103 T104 M153 D1135 R1139 N1140 D1153 E1162 D146 R150 N151 D164 E173 2.7.10.1 0004672,0004713,0004714,0005524,0006468,0007169,0016020 IC50=140nM P08069 19041240 10 SFSAADVYVPDEWEVAREKITMSRELGQGSFGMVYEGVAKGVVKDEPETRVAIKTVNEAASMRERIEFLNEASVMKEFNCHHVVRLLGVVSQGQPTLVIMELMTRGDLKSYLRSLRPPSLSKMIQMAGEIADGMAYLNANKFVHRDLAARNCMVAEDFTVKIGDFGMTRDIYETDYYRKGGKGLLPVRWMSPESLKDGVFTTYSDVWSFGVVLWEIATLAEQPYQGLSNEQVLRFVMEGGLLDKPDNCPDMLFELMRMCWQYNPKMRPSFLEIISSIKEEMEPGFREVSFYYSEEN 3f5p K 2.9 BS01 741 K 1 A1031 K1033 F1047 E1050 M1079 M1082 T1083 M1142 A52 K54 F68 E71 M100 M103 T104 M153 D1135 R1139 N1140 D1153 E1162 D146 R150 N151 D164 E173 2.7.10.1 0004672,0004713,0004714,0005524,0006468,0007169,0016020 IC50=140nM P08069 19041240 11 SFSAADVYVPDEWEVAREKITMSRELGQGSFGMVYEGVAKGVVKDEPETRVAIKTVNEAASMRERIEFLNEASVMKEFNCHHVVRLLGVVSQGQPTLVIMELMTRGDLKSYLRSLRPPSLSKMIQMAGEIADGMAYLNANKFVHRDLAARNCMVAEDFTVKIGDFGMTRDIYETDYYRKGGKGLLPVRWMSPESLKDGVFTTYSDVWSFGVVLWEIATLAEQPYQGLSNEQVLRFVMEGGLLDKPDNCPDMLFELMRMCWQYNPKMRPSFLEIISSIKEEMEPGFREVSFYYSEEN 3f5p L 2.9 BS01 741 L 1 L1005 A1031 K1033 F1047 M1079 L1081 M1082 T1083 M1142 L26 A52 K54 F68 M100 L102 M103 T104 M153 D1135 R1139 N1140 D1153 E1162 D146 R150 N151 D164 E173 2.7.10.1 0004672,0004713,0004714,0005524,0006468,0007169,0016020 IC50=140nM P08069 19041240 13 SFSAADVYVPDEWEVAREKITMSRELGQGSFGMVYEGVAKGVVKDEPETRVAIKTVNEAASMRERIEFLNEASVMKEFNCHHVVRLLGVVSQGQPTLVIMELMTRGDLKSYLRSLRPPSLSKMIQMAGEIADGMAYLNANKFVHRDLAARNCMVAEDFTVKIGDFGMTRDIYETDYYRKGGKGLLPVRWMSPESLKDGVFTTYSDVWSFGVVLWEIATLAEQPYQGLSNEQVLRFVMEGGLLDKPDNCPDMLFELMRMCWQYNPKMRPSFLEIISSIKEEMEPGFREVSFYYSEEN 3f5p M 2.9 BS01 741 M 1 L1005 V1013 A1031 K1033 F1047 E1050 V1077 M1079 L1081 M1082 T1083 M1142 L26 V34 A52 K54 F68 E71 V98 M100 L102 M103 T104 M155 D1135 R1139 N1140 D1153 E1162 D148 R152 N153 D166 E175 2.7.10.1 0004672,0004713,0004714,0005524,0006468,0007169,0016020 IC50=140nM P08069 19041240 12 SFSAADVYVPDEWEVAREKITMSRELGQGSFGMVYEGVAKGVVKDEPETRVAIKTVNEAASMRERIEFLNEASVMKEFNCHHVVRLLGVVSQGQPTLVIMELMTRGDLKSYLRSLRPAPPSLSKMIQMAGEIADGMAYLNANKFVHRDLAARNCMVAEDFTVKIGDFGMTRDIYETDYYRKGGKGLLPVRWMSPESLKDGVFTTYSDVWSFGVVLWEIATLAEQPYQGLSNEQVLRFVMEGGLLDKPDNCPDMLFELMRMCWQYNPKMRPSFLEIISSIKEEMEPGFREVSFYYSEEN 3f5p R 2.9 BS01 741 R 1 L1005 S1009 V1013 A1031 K1033 F1047 E1050 V1077 M1079 M1082 T1083 M1142 L26 S30 V34 A52 K54 F68 E71 V98 M100 M103 T104 M154 N1140 D1153 N152 D165 2.7.10.1 0004672,0004713,0004714,0005524,0006468,0007169,0016020 IC50=140nM P08069 19041240 14 SFSAADVYVPDEWEVAREKITMSRELGQGSFGMVYEGVAKGVVKDEPETRVAIKTVNEAASMRERIEFLNEASVMKEFNCHHVVRLLGVVSQGQPTLVIMELMTRGDLKSYLRSLRPPPSLSKMIQMAGEIADGMAYLNANKFVHRDLAARNCMVAEDFTVKIGDFGMTRDIYETDYYRKGGKGLLPVRWMSPESLKDGVFTTYSDVWSFGVVLWEIATLAEQPYQGLSNEQVLRFVMEGGLLDKPDNCPDMLFELMRMCWQYNPKMRPSFLEIISSIKEEMEPGFREVSFYYSEEN 3f5p S 2.9 BS01 741 S 1 L1005 A1031 K1033 F1047 E1050 V1077 M1079 M1082 M1142 L26 A52 K54 F68 E71 V98 M100 M103 M154 N1140 D1153 N152 D165 2.7.10.1 0004672,0004713,0004714,0005524,0006468,0007169,0016020 IC50=140nM P08069 19041240 15 SFSAADVYVPDEWEVAREKITMSRELGQGSFGMVYEGVAKGVVKDEPETRVAIKTVNEAASMRERIEFLNEASVMKEFNCHHVVRLLGVVSQGQPTLVIMELMTRGDLKSYLRSLRPPPSLSKMIQMAGEIADGMAYLNANKFVHRDLAARNCMVAEDFTVKIGDFGMTRDIYETDYYRKGGKGLLPVRWMSPESLKDGVFTTYSDVWSFGVVLWEIATLAEQPYQGLSNEQVLRFVMEGGLLDKPDNCPDMLFELMRMCWQYNPKMRPSFLEIISSIKEEMEPGFREVSFYYSEENK 3f5p T 2.9 BS01 741 T 1 L1005 A1031 K1033 M1079 M1082 T1083 M1142 L26 A52 K54 M100 M103 T104 M154 N1140 D1153 N152 D165 2.7.10.1 0004672,0004713,0004714,0005524,0006468,0007169,0016020 IC50=140nM P08069 19041240 16 SFSAADVYVPDEWEVAREKITMSRELGQGSFGMVYEGVAKGVVKDEPETRVAIKTVNEAASMRERIEFLNEASVMKEFNCHHVVRLLGVVSQGQPTLVIMELMTRGDLKSYLRSLRPPPSLSKMIQMAGEIADGMAYLNANKFVHRDLAARNCMVAEDFTVKIGDFGMTRDIYETDYYRKGGKGLLPVRWMSPESLKDGVFTTYSDVWSFGVVLWEIATLAEQPYQGLSNEQVLRFVMEGGLLDKPDNCPDMLFELMRMCWQYNPKMRPSFLEIISSIKEEMEPGFREVSFYYSEENK