3a2c A 2.9 BS01 PDY A 1 V78 Q80 C140 L141 E190 N191 L193 D207 V32 Q34 C94 L95 E144 N145 L147 D161 D186 K188 E190 N191 D207 S216 D140 K142 E144 N145 D161 S170 2.7.11.1 0004672,0005524,0006468 -logKd/Ki=6.90, Ki=0.126uM IC50=130nM P49137 20057052 1 HVKSGLQIKKNAIIDDYKVTSQVLGLGINGKVLQIFNKRTQEKFALKMLQDCPKARREVELHWRASQCPHIVRIVDVYENLYAGRKCLLIVMECLDGGELFSRIQDRGDQAFTEREASEIMKSIGEAIQYLHSINIAHRDVKPENLLYTSKRPNAILKLTDFGFAKETTSVAPEVLYDKSCDMWSLGVIMYILLCGYPPFYSPGMKTRIRMGQYEFPNPEWSEVSEEVKMLIRNLLKTEPTQRMTITEFMNHPWIMQSTKVPQTPLHTSRVLKE 3a2c A 2.9 BS02 PDY A 2 Y260 P261 Y264 Y197 P198 Y201 D186 K188 E190 N191 D207 S216 D140 K142 E144 N145 D161 S170 2.7.11.1 0004672,0005524,0006468 -logKd/Ki=6.90, Ki=0.126uM IC50=130nM P49137 20057052 2 HVKSGLQIKKNAIIDDYKVTSQVLGLGINGKVLQIFNKRTQEKFALKMLQDCPKARREVELHWRASQCPHIVRIVDVYENLYAGRKCLLIVMECLDGGELFSRIQDRGDQAFTEREASEIMKSIGEAIQYLHSINIAHRDVKPENLLYTSKRPNAILKLTDFGFAKETTSVAPEVLYDKSCDMWSLGVIMYILLCGYPPFYSPGMKTRIRMGQYEFPNPEWSEVSEEVKMLIRNLLKTEPTQRMTITEFMNHPWIMQSTKVPQTPLHTSRVLKE 3a2c B 2.9 BS01 PDY B 1 V78 Q80 A91 C140 L141 E190 N191 L193 D207 V32 Q34 A45 C94 L95 E144 N145 L147 D161 D186 K188 E190 N191 D207 S216 D140 K142 E144 N145 D161 S170 2.7.11.1 0004672,0005524,0006468 IC50=130nM P49137 20057052 1 HVKSGLQIKKNAIIDDYKVTSQVLGLGINGKVLQIFNKRTQEKFALKMLQDCPKARREVELHWRASQCPHIVRIVDVYENLYAGRKCLLIVMECLDGGELFSRIQDRGDQAFTEREASEIMKSIGEAIQYLHSINIAHRDVKPENLLYTSKRPNAILKLTDFGFAKETTSVAPEVLYDKSCDMWSLGVIMYILLCGYPPFYSNSPGMKTRIRMGQYEFPNPEWSEVSEEVKMLIRNLLKTEPTQRMTITEFMNHPWIMQSTKVPQTPLHTSRVLKED 3a2c B 2.9 BS02 PDY B 2 Y260 P261 Y264 Y197 P198 Y201 D186 K188 E190 N191 D207 S216 D140 K142 E144 N145 D161 S170 2.7.11.1 0004672,0005524,0006468 IC50=130nM P49137 20057052 2 HVKSGLQIKKNAIIDDYKVTSQVLGLGINGKVLQIFNKRTQEKFALKMLQDCPKARREVELHWRASQCPHIVRIVDVYENLYAGRKCLLIVMECLDGGELFSRIQDRGDQAFTEREASEIMKSIGEAIQYLHSINIAHRDVKPENLLYTSKRPNAILKLTDFGFAKETTSVAPEVLYDKSCDMWSLGVIMYILLCGYPPFYSNSPGMKTRIRMGQYEFPNPEWSEVSEEVKMLIRNLLKTEPTQRMTITEFMNHPWIMQSTKVPQTPLHTSRVLKED 3a2c C 2.9 BS01 PDY C 1 V78 Q80 A91 M138 E139 C140 L141 E190 N191 L193 D207 V30 Q32 A43 M90 E91 C92 L93 E142 N143 L145 D159 D186 K188 E190 N191 D207 S216 D138 K140 E142 N143 D159 S168 2.7.11.1 0004672,0005524,0006468 IC50=130nM P49137 20057052 1 VKSGLQIKKNAIIDDYKVTSVLGLGINGKVLQIFNKRTQEKFALKMLQDCPKARREVELHWRASQCPHIVRIVDVYENLYAGRKCLLIVMECLDGGELFSRIQDRGDQAFTEREASEIMKSIGEAIQYLHSINIAHRDVKPENLLYTSKRPNAILKLTDFGFAKETTSYVAPEVLYDKSCDMWSLGVIMYILLCGYPPFYSNSPGMKTRIRMGQYEFPNPEWSEVSEEVKMLIRNLLKTEPTQRMTITEFMNHPWIMQSTKVPQTPLHTSRVL 3a2c C 2.9 BS02 PDY C 2 P261 Y264 S265 P197 Y200 S201 D186 K188 E190 N191 D207 S216 D138 K140 E142 N143 D159 S168 2.7.11.1 0004672,0005524,0006468 IC50=130nM P49137 20057052 2 VKSGLQIKKNAIIDDYKVTSVLGLGINGKVLQIFNKRTQEKFALKMLQDCPKARREVELHWRASQCPHIVRIVDVYENLYAGRKCLLIVMECLDGGELFSRIQDRGDQAFTEREASEIMKSIGEAIQYLHSINIAHRDVKPENLLYTSKRPNAILKLTDFGFAKETTSYVAPEVLYDKSCDMWSLGVIMYILLCGYPPFYSNSPGMKTRIRMGQYEFPNPEWSEVSEEVKMLIRNLLKTEPTQRMTITEFMNHPWIMQSTKVPQTPLHTSRVL 3a2c D 2.9 BS01 PDY D 1 V78 Q80 A91 C140 L141 E190 N191 L193 D207 V31 Q33 A44 C93 L94 E143 N144 L146 D160 D186 K188 E190 N191 D207 S216 D139 K141 E143 N144 D160 S169 2.7.11.1 0004672,0005524,0006468 IC50=130nM P49137 20057052 1 VKSGLQIKKNAIIDDYKVTSQVLGLGINGKVLQIFNKRTQEKFALKMLQDCPKARREVELHWRASQCPHIVRIVDVYENLYAGRKCLLIVMECLDGGELFSRIQDRGDQAFTEREASEIMKSIGEAIQYLHSINIAHRDVKPENLLYTSKRPNAILKLTDFGFAKETTSVAPEVLEKYDKSCDMWSLGVIMYILLCGYPPFYSNHPGMKTRIRMGQYEFPNPEWSEVSEEVKMLIRNLLKTEPTQRMTITEFMNHPWIMQSTKVPQTPLHTSRVLKE 3a2c D 2.9 BS02 PDY D 2 F147 Y264 F100 Y202 D186 K188 E190 N191 D207 S216 D139 K141 E143 N144 D160 S169 2.7.11.1 0004672,0005524,0006468 IC50=130nM P49137 20057052 2 VKSGLQIKKNAIIDDYKVTSQVLGLGINGKVLQIFNKRTQEKFALKMLQDCPKARREVELHWRASQCPHIVRIVDVYENLYAGRKCLLIVMECLDGGELFSRIQDRGDQAFTEREASEIMKSIGEAIQYLHSINIAHRDVKPENLLYTSKRPNAILKLTDFGFAKETTSVAPEVLEKYDKSCDMWSLGVIMYILLCGYPPFYSNHPGMKTRIRMGQYEFPNPEWSEVSEEVKMLIRNLLKTEPTQRMTITEFMNHPWIMQSTKVPQTPLHTSRVLKE 3a2c E 2.9 BS01 PDY E 1 V78 Q80 A91 C140 L141 E190 N191 L193 D207 V31 Q33 A44 C93 L94 E143 N144 L146 D160 D186 K188 E190 N191 D207 S216 D139 K141 E143 N144 D160 S169 2.7.11.1 0004672,0005524,0006468 IC50=130nM P49137 20057052 1 VKSGLQIKKNAIIDDYKVTSQVLGLGINGKVLQIFNKRTQEKFALKMLQDCPKARREVELHWRASQCPHIVRIVDVYENLYAGRKCLLIVMECLDGGELFSRIQDRGDQAFTEREASEIMKSIGEAIQYLHSINIAHRDVKPENLLYTSKRPNAILKLTDFGFAKETTSYVAPEVLYDKSCDMWSLGVIMYILLCGYPPFYSNSPGMKTRIRMGQYEFPNPEWSEVSEEVKMLIRNLLKTEPTQRMTITEFMNHPWIMQSTKVPQTPLHTSRVLKE 3a2c E 2.9 BS02 PDY E 2 Y260 P261 Y264 Y197 P198 Y201 D186 K188 E190 N191 D207 S216 D139 K141 E143 N144 D160 S169 2.7.11.1 0004672,0005524,0006468 IC50=130nM P49137 20057052 2 VKSGLQIKKNAIIDDYKVTSQVLGLGINGKVLQIFNKRTQEKFALKMLQDCPKARREVELHWRASQCPHIVRIVDVYENLYAGRKCLLIVMECLDGGELFSRIQDRGDQAFTEREASEIMKSIGEAIQYLHSINIAHRDVKPENLLYTSKRPNAILKLTDFGFAKETTSYVAPEVLYDKSCDMWSLGVIMYILLCGYPPFYSNSPGMKTRIRMGQYEFPNPEWSEVSEEVKMLIRNLLKTEPTQRMTITEFMNHPWIMQSTKVPQTPLHTSRVLKE 3a2c F 2.9 BS01 PDY F 1 V78 Q80 A91 C140 L141 E190 N191 L193 D207 V32 Q34 A45 C94 L95 E144 N145 L147 D161 D186 K188 E190 N191 D207 S216 D140 K142 E144 N145 D161 S170 2.7.11.1 0004672,0005524,0006468 IC50=130nM P49137 20057052 1 HVKSGLQIKKNAIIDDYKVTSQVLGLGINGKVLQIFNKRTQEKFALKMLQDCPKARREVELHWRASQCPHIVRIVDVYENLYAGRKCLLIVMECLDGGELFSRIQDRGDQAFTEREASEIMKSIGEAIQYLHSINIAHRDVKPENLLYTSKRPNAILKLTDFGFAKETTSYVAPEVLGPEKYDKSCDMWSLGVIMYILLCGYPPFYSNHGLAISPGMKTRIRMGQYEFPNPEWSEVSEEVKMLIRNLLKTEPTQRMTITEFMNHPWIMQSTKVPQTPLHTSRVLKED 3a2c F 2.9 BS02 PDY F 2 Y260 P261 Y264 S265 L269 Y202 P203 Y206 S207 L211 D186 K188 E190 N191 D207 S216 D140 K142 E144 N145 D161 S170 2.7.11.1 0004672,0005524,0006468 IC50=130nM P49137 20057052 2 HVKSGLQIKKNAIIDDYKVTSQVLGLGINGKVLQIFNKRTQEKFALKMLQDCPKARREVELHWRASQCPHIVRIVDVYENLYAGRKCLLIVMECLDGGELFSRIQDRGDQAFTEREASEIMKSIGEAIQYLHSINIAHRDVKPENLLYTSKRPNAILKLTDFGFAKETTSYVAPEVLGPEKYDKSCDMWSLGVIMYILLCGYPPFYSNHGLAISPGMKTRIRMGQYEFPNPEWSEVSEEVKMLIRNLLKTEPTQRMTITEFMNHPWIMQSTKVPQTPLHTSRVLKED 3a2c G 2.9 BS01 PDY G 1 V78 Q80 C140 L141 D142 E190 N191 L193 D207 V31 Q33 C93 L94 D95 E143 N144 L146 D160 D186 K188 E190 N191 D207 S216 D139 K141 E143 N144 D160 S169 2.7.11.1 0004672,0005524,0006468 IC50=130nM P49137 20057052 1 VKSGLQIKKNAIIDDYKVTSQVLGLGINGKVLQIFNKRTQEKFALKMLQDCPKARREVELHWRASQCPHIVRIVDVYENLYAGRKCLLIVMECLDGGELFSRIQDRGDQAFTEREASEIMKSIGEAIQYLHSINIAHRDVKPENLLYTSKRPNAILKLTDFGFAKETTSYVAPEVLYDKSCDMWSLGVIMYILLCGYPPFYSNPGMKTRIRMGQYEFPNPEWSEVSEEVKMLIRNLLKTEPTQRMTITEFMNHPWIMQSTKVPQTPLHTSRVL 3a2c G 2.9 BS02 PDY G 2 Y260 P261 Y264 S265 Y197 P198 Y201 S202 D186 K188 E190 N191 D207 S216 D139 K141 E143 N144 D160 S169 2.7.11.1 0004672,0005524,0006468 IC50=130nM P49137 20057052 2 VKSGLQIKKNAIIDDYKVTSQVLGLGINGKVLQIFNKRTQEKFALKMLQDCPKARREVELHWRASQCPHIVRIVDVYENLYAGRKCLLIVMECLDGGELFSRIQDRGDQAFTEREASEIMKSIGEAIQYLHSINIAHRDVKPENLLYTSKRPNAILKLTDFGFAKETTSYVAPEVLYDKSCDMWSLGVIMYILLCGYPPFYSNPGMKTRIRMGQYEFPNPEWSEVSEEVKMLIRNLLKTEPTQRMTITEFMNHPWIMQSTKVPQTPLHTSRVL 3a2c H 2.9 BS01 PDY H 1 V78 Q80 M138 C140 L141 E190 N191 L193 D207 V31 Q33 M91 C93 L94 E143 N144 L146 D160 D186 K188 E190 N191 D207 S216 D139 K141 E143 N144 D160 S169 2.7.11.1 0004672,0005524,0006468 IC50=130nM P49137 20057052 1 HVKSGLQIKKNAIIDDYKVTSVLGLGINGKVLQIFNKRTQEKFALKMLQDCPKARREVELHWRASQCPHIVRIVDVYENLYAGRKCLLIVMECLDGGELFSRIQDRGDQAFTEREASEIMKSIGEAIQYLHSINIAHRDVKPENLLYTSKRPNAILKLTDFGFAKETTSYVAPEVLYDKSCDMWSLGVIMYILLCGYPPFYSNSPGMKTRIRMGQYEFPNPEWSEVSEEVKMLIRNLLKTEPTQRMTITEFMNHPWIMQSTKVPQTPLHTSRVLK 3a2c H 2.9 BS02 PDY H 2 P261 Y264 S265 P198 Y201 S202 D186 K188 E190 N191 D207 S216 D139 K141 E143 N144 D160 S169 2.7.11.1 0004672,0005524,0006468 IC50=130nM P49137 20057052 2 HVKSGLQIKKNAIIDDYKVTSVLGLGINGKVLQIFNKRTQEKFALKMLQDCPKARREVELHWRASQCPHIVRIVDVYENLYAGRKCLLIVMECLDGGELFSRIQDRGDQAFTEREASEIMKSIGEAIQYLHSINIAHRDVKPENLLYTSKRPNAILKLTDFGFAKETTSYVAPEVLYDKSCDMWSLGVIMYILLCGYPPFYSNSPGMKTRIRMGQYEFPNPEWSEVSEEVKMLIRNLLKTEPTQRMTITEFMNHPWIMQSTKVPQTPLHTSRVLK 3a2c I 2.9 BS01 PDY I 1 V78 C140 L141 E190 N191 L193 D207 V31 C93 L94 E143 N144 L146 D160 D186 K188 E190 N191 D207 S216 D139 K141 E143 N144 D160 S169 2.7.11.1 0004672,0005524,0006468 IC50=130nM P49137 20057052 1 VKSGLQIKKNAIIDDYKVTSQVLGLGINGKVLQIFNKRTQEKFALKMLQDCPKARREVELHWRASQCPHIVRIVDVYENLYAGRKCLLIVMECLDGGELFSRIQDRGDQAFTEREASEIMKSIGEAIQYLHSINIAHRDVKPENLLYTSKRPNAILKLTDFGFAKETTSYVAPEVLYDKSCDMWSLGVIMYILLCGYPPFYSNSPGMKTRIRMGQYEFPNPEWSEVSEEVKMLIRNLLKTEPTQRMTITEFMNHPWIMQSTKVPQTPLHTSRVLK 3a2c I 2.9 BS02 PDY I 2 P261 Y264 P198 Y201 D186 K188 E190 N191 D207 S216 D139 K141 E143 N144 D160 S169 2.7.11.1 0004672,0005524,0006468 IC50=130nM P49137 20057052 2 VKSGLQIKKNAIIDDYKVTSQVLGLGINGKVLQIFNKRTQEKFALKMLQDCPKARREVELHWRASQCPHIVRIVDVYENLYAGRKCLLIVMECLDGGELFSRIQDRGDQAFTEREASEIMKSIGEAIQYLHSINIAHRDVKPENLLYTSKRPNAILKLTDFGFAKETTSYVAPEVLYDKSCDMWSLGVIMYILLCGYPPFYSNSPGMKTRIRMGQYEFPNPEWSEVSEEVKMLIRNLLKTEPTQRMTITEFMNHPWIMQSTKVPQTPLHTSRVLK 3a2c J 2.9 BS01 PDY J 1 V78 Q80 A91 M138 C140 L141 E190 N191 L193 D207 V31 Q33 A44 M91 C93 L94 E143 N144 L146 D160 D186 K188 E190 N191 D207 S216 D139 K141 E143 N144 D160 S169 2.7.11.1 0004672,0005524,0006468 IC50=130nM P49137 20057052 1 VKSGLQIKKNAIIDDYKVTSQVLGLGINGKVLQIFNKRTQEKFALKMLQDCPKARREVELHWRASQCPHIVRIVDVYENLYAGRKCLLIVMECLDGGELFSRIQDRGDQAFTEREASEIMKSIGEAIQYLHSINIAHRDVKPENLLYTSKRPNAILKLTDFGFAKETTSYVAPEVLYDKSCDMWSLGVIMYILLCGYPPFYSNSPGMKTRIRMGQYEFPNPEWSEVSEEVKMLIRNLLKTEPTQRMTITEFMNHPWIMQSTKVPQTPLHTSRVLK 3a2c J 2.9 BS02 PDY J 2 F147 Y260 P261 Y264 S265 F100 Y197 P198 Y201 S202 D186 K188 E190 N191 D207 S216 D139 K141 E143 N144 D160 S169 2.7.11.1 0004672,0005524,0006468 IC50=130nM P49137 20057052 2 VKSGLQIKKNAIIDDYKVTSQVLGLGINGKVLQIFNKRTQEKFALKMLQDCPKARREVELHWRASQCPHIVRIVDVYENLYAGRKCLLIVMECLDGGELFSRIQDRGDQAFTEREASEIMKSIGEAIQYLHSINIAHRDVKPENLLYTSKRPNAILKLTDFGFAKETTSYVAPEVLYDKSCDMWSLGVIMYILLCGYPPFYSNSPGMKTRIRMGQYEFPNPEWSEVSEEVKMLIRNLLKTEPTQRMTITEFMNHPWIMQSTKVPQTPLHTSRVLK 3a2c K 2.9 BS01 PDY K 1 V78 Q80 A91 E139 C140 L141 E190 N191 D207 V31 Q33 A44 E92 C93 L94 E143 N144 D160 D186 K188 E190 N191 D207 S216 D139 K141 E143 N144 D160 S169 2.7.11.1 0004672,0005524,0006468 IC50=130nM P49137 20057052 1 VKSGLQIKKNAIIDDYKVTSQVLGLGINGKVLQIFNKRTQEKFALKMLQDCPKARREVELHWRASQCPHIVRIVDVYENLYAGRKCLLIVMECLDGGELFSRIQDRGDQAFTEREASEIMKSIGEAIQYLHSINIAHRDVKPENLLYTSKRPNAILKLTDFGFAKETTSVAPEVLYDKSCDMWSLGVIMYILLCGYPPFYSPGMKTRIRMGQYEFPNPEWSEVSEEVKMLIRNLLKTEPTQRMTITEFMNHPWIMQSTKVPQTPLHTSRVLKE 3a2c K 2.9 BS02 PDY K 2 F147 P261 Y264 F100 P197 Y200 D186 K188 E190 N191 D207 S216 D139 K141 E143 N144 D160 S169 2.7.11.1 0004672,0005524,0006468 IC50=130nM P49137 20057052 2 VKSGLQIKKNAIIDDYKVTSQVLGLGINGKVLQIFNKRTQEKFALKMLQDCPKARREVELHWRASQCPHIVRIVDVYENLYAGRKCLLIVMECLDGGELFSRIQDRGDQAFTEREASEIMKSIGEAIQYLHSINIAHRDVKPENLLYTSKRPNAILKLTDFGFAKETTSVAPEVLYDKSCDMWSLGVIMYILLCGYPPFYSPGMKTRIRMGQYEFPNPEWSEVSEEVKMLIRNLLKTEPTQRMTITEFMNHPWIMQSTKVPQTPLHTSRVLKE 3a2c L 2.9 BS01 PDY L 1 V78 Q80 C140 L141 E190 N191 L193 D207 V31 Q33 C93 L94 E143 N144 L146 D160 D186 K188 E190 N191 D207 S216 D139 K141 E143 N144 D160 S169 2.7.11.1 0004672,0005524,0006468 IC50=130nM P49137 20057052 1 VKSGLQIKKNAIIDDYKVTSQVLGLGINGKVLQIFNKRTQEKFALKMLQDCPKARREVELHWRASQCPHIVRIVDVYENLYAGRKCLLIVMECLDGGELFSRIQDRGDQAFTEREASEIMKSIGEAIQYLHSINIAHRDVKPENLLYTSKRPNAILKLTDFGFAKETTSYVAPEVLYDKSCDMWSLGVIMYILLCGYPPFYSNSPGMKTRIRMGQYEFPNPEWSEVSEEVKMLIRNLLKTEPTQRMTITEFMNHPWIMQSTKVPQTPLHTSRVLKE 3a2c L 2.9 BS02 PDY L 2 Y260 P261 Y264 Y197 P198 Y201 D186 K188 E190 N191 D207 S216 D139 K141 E143 N144 D160 S169 2.7.11.1 0004672,0005524,0006468 IC50=130nM P49137 20057052 2 VKSGLQIKKNAIIDDYKVTSQVLGLGINGKVLQIFNKRTQEKFALKMLQDCPKARREVELHWRASQCPHIVRIVDVYENLYAGRKCLLIVMECLDGGELFSRIQDRGDQAFTEREASEIMKSIGEAIQYLHSINIAHRDVKPENLLYTSKRPNAILKLTDFGFAKETTSYVAPEVLYDKSCDMWSLGVIMYILLCGYPPFYSNSPGMKTRIRMGQYEFPNPEWSEVSEEVKMLIRNLLKTEPTQRMTITEFMNHPWIMQSTKVPQTPLHTSRVLKE