| MET | Met | TK | 7v3r | A | B | ~{n}1'-[3-fluoranyl-4-(2-phenylazanylpyrimidin-4-yl)oxy-phenyl]-~{n}1-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide | Human | 14330 | 0.48 | |
| MET | Met | TK | 7v3s | A | A | ~{n}1'-[3-fluoranyl-4-(10~{h}-pyrido[3,2-b][1,4]benzoxazin-4-yloxy)phenyl]-~{n}1-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide | Human | 14329 | 0.50 | |
| MET | Met | TK | 7v3s | A | B | ~{n}1'-[3-fluoranyl-4-(10~{h}-pyrido[3,2-b][1,4]benzoxazin-4-yloxy)phenyl]-~{n}1-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide | Human | 14327 | 0.50 | |
| MET | Met | TK | 7v3r | A | A | ~{n}1'-[3-fluoranyl-4-(2-phenylazanylpyrimidin-4-yl)oxy-phenyl]-~{n}1-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide | Human | 14328 | 0.48 | |
| EPHA2 (EphA2) | Eph | TK | 5ia4 | A | B | n-(3-fluoro-4-{[6-methoxy-7-(3-morpholin-4-ylpropoxy)quinolin-4-yl]oxy}phenyl)-n'-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide | Human | 7168 | 1.00 | |
| MET | Met | TK | 6sdc | A | A | n-(3-fluoro-4-{[6-methoxy-7-(3-morpholin-4-ylpropoxy)quinolin-4-yl]oxy}phenyl)-n'-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide | Human | 11532 | 1.00 | |
| EPHA2 (EphA2) | Eph | TK | 5ia4 | A | A | n-(3-fluoro-4-{[6-methoxy-7-(3-morpholin-4-ylpropoxy)quinolin-4-yl]oxy}phenyl)-n'-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide | Human | 7189 | 1.00 | |
| EGFR | EGFR | TK | 3ug2 | A | A | gefitinib | Human | 898 | 0.51 | |
| EGFR | EGFR | TK | 2ity | A | | gefitinib | Human | 790 | 0.51 | |
| GAK | NAK | Other | 5y80 | A | A | gefitinib | Human | 10329 | 0.51 | |
| GAK | NAK | Other | 5y7z | A | | gefitinib | Human | 10332 | 0.51 | |
| STK10 (LOK) | STE20 | STE | 6i2y | B | | n-(3-fluoro-4-{[6-methoxy-7-(3-morpholin-4-ylpropoxy)quinolin-4-yl]oxy}phenyl)-n'-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide | Human | 10788 | 1.00 | |
| MET | Met | TK | 5dg5 | B | B | n-(2,5-difluoro-4-{[2-(1-methyl-1h-pyrazol-4-yl)pyridin-4-yl]oxy}phenyl)-n'-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide | Human | 7036 | 0.42 | |
| GAK | NAK | Other | 5y80 | A | B | gefitinib | Human | 10330 | 0.51 | |
| STK10 (LOK) | STE20 | STE | 6i2y | A | | n-(3-fluoro-4-{[6-methoxy-7-(3-morpholin-4-ylpropoxy)quinolin-4-yl]oxy}phenyl)-n'-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide | Human | 10787 | 1.00 | |
| MET | Met | TK | 3ctj | A | A | 2-(4-fluorophenyl)-n-{[3-fluoro-4-(1h-pyrrolo[2,3-b]pyridin-4-yloxy)phenyl]carbamoyl}acetamide | Human | 6767 | 0.41 | |
| MET | Met | TK | 4mxc | A | B | n-(3-fluoro-4-{[2-({3-[(methylsulfonyl)methyl]phenyl}amino)pyrimidin-4-yl]oxy}phenyl)-n'-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide | Human | 3025 | 0.48 | |
| KDR | VEGFR | TK | 3b8q | B | | n-(4-chlorophenyl)-6-[(6,7-dimethoxyquinolin-4-yl)oxy]naphthalene-1-carboxamide | Human | 5319 | 0.41 | |
| KDR | VEGFR | TK | 2rl5 | A | | n-(4-chlorophenyl)-7-[(6,7-dimethoxyquinolin-4-yl)oxy]-2,3-dihydro-1,4-benzoxazine-4-carboxamide | Human | 5348 | 0.45 | |
| GAK | NAK | Other | 5y7z | B | | gefitinib | Human | 10331 | 0.51 | |
| MERTK (MER) | Axl | TK | 7aax | A | A | ~{n}-[4-(6,7-dimethoxyquinolin-4-yl)oxy-3-fluoranyl-phenyl]-4-ethoxy-1-(4-fluoranyl-2-methyl-phenyl)pyrazole-3-carboxamide | Human | 12938 | 0.49 | |
| MERTK (MER) | Axl | TK | 7aax | A | B | ~{n}-[4-(6,7-dimethoxyquinolin-4-yl)oxy-3-fluoranyl-phenyl]-4-ethoxy-1-(4-fluoranyl-2-methyl-phenyl)pyrazole-3-carboxamide | Human | 12941 | 0.49 | |
| EGFR | EGFR | TK | 4i22 | A | | gefitinib | Human | 823 | 0.51 | |
| EGFR | EGFR | TK | 4wkq | A | A | gefitinib | Human | 889 | 0.51 | |
| MAPK14 (p38a) | MAPK | CMGC | 4a9y | A | | n-(3-{[7-methoxy-6-(2-pyrrolidin-1-ylethoxy)quinazolin-4-yl]amino}-4-methylphenyl)-2-morpholin-4-ylisonicotinamide | Human | 5073 | 0.43 | |
| EGFR | EGFR | TK | 3ug2 | A | B | gefitinib | Human | 819 | 0.51 | |
| EGFR | EGFR | TK | 2ito | A | | gefitinib | Human | 783 | 0.51 | |
| MAPK14 (p38a) | MAPK | CMGC | 2bak | A | | n-(3-{[7-methoxy-6-(2-pyrrolidin-1-ylethoxy)quinazolin-4-yl]amino}-4-methylphenyl)-2-morpholin-4-ylisonicotinamide | Human | 5114 | 0.43 | |
| EGFR | EGFR | TK | 2itz | A | | gefitinib | Human | 789 | 0.51 | |
| KDR | VEGFR | TK | 3b8q | A | | n-(4-chlorophenyl)-6-[(6,7-dimethoxyquinolin-4-yl)oxy]naphthalene-1-carboxamide | Human | 5332 | 0.41 | |
| FGFR1 | FGFR | TK | 4rwl | B | | 6-({7-[(1-aminocyclopropyl)methoxy]-6-methoxyquinolin-4-yl}oxy)-n-methylnaphthalene-1-carboxamide | Human | 3596 | 0.41 | |
| KDR | VEGFR | TK | 3u6j | A | | n-{4-[(6,7-dimethoxyquinolin-4-yl)oxy]-3-fluorophenyl}-1,5-dimethyl-3-oxo-2-phenyl-2,3-dihydro-1h-pyrazole-4-carboxamide | Human | 5318 | 0.50 | |
| MET | Met | TK | 3u6h | A | B | n-{4-[(6,7-dimethoxyquinolin-4-yl)oxy]-3-fluorophenyl}-1,5-dimethyl-3-oxo-2-phenyl-2,3-dihydro-1h-pyrazole-4-carboxamide | Human | 2965 | 0.50 | |
| EGFR | EGFR | TK | 4wkq | A | B | gefitinib | Human | 837 | 0.51 | |
| EGFR | EGFR | TK | 5y25 | A | | (2r)-n-[4-[(3-chloranyl-4-fluoranyl-phenyl)amino]-7-(3-morpholin-4-ylpropoxy)quinazolin-6-yl]-1-(2-fluoranylethanoyl)pyrrolidine-2-carboxamide | Human | 10373 | 0.41 | |
| MET | Met | TK | 3lq8 | A | B | n-(3-fluoro-4-{[6-methoxy-7-(3-morpholin-4-ylpropoxy)quinolin-4-yl]oxy}phenyl)-n'-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide | Human | 2964 | 1.00 | |
| MET | Met | TK | 2rfn | B | | 2-benzyl-5-(3-fluoro-4-{[6-methoxy-7-(3-morpholin-4-ylpropoxy)quinolin-4-yl]oxy}phenyl)-3-methylpyrimidin-4(3h)-one | Human | 2961 | 0.57 | |
| MET | Met | TK | 3u6h | A | A | n-{4-[(6,7-dimethoxyquinolin-4-yl)oxy]-3-fluorophenyl}-1,5-dimethyl-3-oxo-2-phenyl-2,3-dihydro-1h-pyrazole-4-carboxamide | Human | 2996 | 0.50 | |
| MET | Met | TK | 3lq8 | A | A | n-(3-fluoro-4-{[6-methoxy-7-(3-morpholin-4-ylpropoxy)quinolin-4-yl]oxy}phenyl)-n'-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide | Human | 2998 | 1.00 | |
| MET | Met | TK | 5dg5 | B | A | n-(2,5-difluoro-4-{[2-(1-methyl-1h-pyrazol-4-yl)pyridin-4-yl]oxy}phenyl)-n'-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide | Human | 7035 | 0.42 | |
| MET | Met | TK | 5hti | A | B | n-[3-fluoro-4-({7-[2-(morpholin-4-yl)ethoxy]-1,6-naphthyridin-4-yl}oxy)phenyl]-n'-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide | Human | 8009 | 0.72 | |
| MET | Met | TK | 5hti | A | A | n-[3-fluoro-4-({7-[2-(morpholin-4-yl)ethoxy]-1,6-naphthyridin-4-yl}oxy)phenyl]-n'-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide | Human | 8010 | 0.72 | |
| MET | Met | TK | 3vw8 | A | | n-({4-[(6,7-dimethoxyquinolin-4-yl)oxy]phenyl}carbamothioyl)-2-phenylacetamide | Human | 2985 | 0.43 | |
| MET | Met | TK | 5dg5 | A | A | n-(2,5-difluoro-4-{[2-(1-methyl-1h-pyrazol-4-yl)pyridin-4-yl]oxy}phenyl)-n'-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide | Human | 7037 | 0.42 | |
| MET | Met | TK | 6sd9 | A | | n-(3-fluoro-4-{[6-methoxy-7-(3-morpholin-4-ylpropoxy)quinolin-4-yl]oxy}phenyl)-n'-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide | Human | 11531 | 1.00 | |
| MET | Met | TK | 4mxc | A | A | n-(3-fluoro-4-{[2-({3-[(methylsulfonyl)methyl]phenyl}amino)pyrimidin-4-yl]oxy}phenyl)-n'-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide | Human | 3033 | 0.48 | |
| MET | Met | TK | 5t3q | A | | n-{3-fluoro-4-[(7-methoxyquinolin-4-yl)oxy]phenyl}-1-(2-hydroxy-2-methylpropyl)-5-methyl-3-oxo-2-phenyl-2,3-dihydro-1h-pyrazole-4-carboxamide | Human | 7413 | 0.40 | |
| MET | Met | TK | 3u6i | A | | n-{3-fluoro-4-[(7-methoxyquinolin-4-yl)oxy]phenyl}-1-[(2r)-2-hydroxypropyl]-5-methyl-3-oxo-2-phenyl-2,3-dihydro-1h-pyrazole-4-carboxamide | Human | 2967 | 0.41 | |
| MET | Met | TK | 2rfn | A | | 2-benzyl-5-(3-fluoro-4-{[6-methoxy-7-(3-morpholin-4-ylpropoxy)quinolin-4-yl]oxy}phenyl)-3-methylpyrimidin-4(3h)-one | Human | 3022 | 0.57 | |
| MET | Met | TK | 3efj | A | | 2-benzyl-5-{4-[(6,7-dimethoxyquinolin-4-yl)oxy]-3-fluorophenyl}-3-methylpyrimidin-4(3h)-one | Human | 3015 | 0.40 | |
| MET | Met | TK | 3efk | A | | 5-{4-[(6,7-dimethoxyquinolin-4-yl)oxy]-3-fluorophenyl}-2-[(4-fluorophenyl)amino]-3-methylpyrimidin-4(3h)-one | Human | 3018 | 0.47 | |
| MET | Met | TK | 5dg5 | A | B | n-(2,5-difluoro-4-{[2-(1-methyl-1h-pyrazol-4-yl)pyridin-4-yl]oxy}phenyl)-n'-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide | Human | 7034 | 0.42 | |
| MET | Met | TK | 6sdc | A | B | n-(3-fluoro-4-{[6-methoxy-7-(3-morpholin-4-ylpropoxy)quinolin-4-yl]oxy}phenyl)-n'-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide | Human | 11534 | 1.00 | |
| MET | Met | TK | 3ctj | A | B | 2-(4-fluorophenyl)-n-{[3-fluoro-4-(1h-pyrrolo[2,3-b]pyridin-4-yloxy)phenyl]carbamoyl}acetamide | Human | 6766 | 0.41 | |
| MET | Met | TK | 3efj | B | | 2-benzyl-5-{4-[(6,7-dimethoxyquinolin-4-yl)oxy]-3-fluorophenyl}-3-methylpyrimidin-4(3h)-one | Human | 2957 | 0.40 | |
| MET | Met | TK | 3efk | B | | 5-{4-[(6,7-dimethoxyquinolin-4-yl)oxy]-3-fluorophenyl}-2-[(4-fluorophenyl)amino]-3-methylpyrimidin-4(3h)-one | Human | 2988 | 0.47 | |
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