| 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 | 0.44 | |
| 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 | 0.44 | |
| KIT | PDGFR | TK | 6xva | B | | ~{n}-[[3-[2-[3-methoxy-5-(7-methoxyquinolin-4-yl)oxy-pyridin-2-yl]ethanoylamino]-5-methyl-phenyl]methyl]propanamide | Human | 12281 | 0.41 | |
| KIT | PDGFR | TK | 6gql | A | | ~{n}-[4-(6,7-dimethoxyquinazolin-4-yl)oxyphenyl]-2-(4-propan-2-yl-1,2,3-triazol-1-yl)ethanamide | Human | 10362 | 0.40 | |
| KIT | PDGFR | TK | 6gqk | A | B | ~{n}-[4-(6,7-dimethoxyquinazolin-4-yl)oxyphenyl]-2-(1-ethylpyrazol-4-yl)ethanamide | Human | 10353 | 0.41 | |
| KIT | PDGFR | TK | 6gqk | A | A | ~{n}-[4-(6,7-dimethoxyquinazolin-4-yl)oxyphenyl]-2-(1-ethylpyrazol-4-yl)ethanamide | Human | 10355 | 0.41 | |
| KIT | PDGFR | TK | 6gqk | B | B | ~{n}-[4-(6,7-dimethoxyquinazolin-4-yl)oxyphenyl]-2-(1-ethylpyrazol-4-yl)ethanamide | Human | 10360 | 0.41 | |
| 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 | 0.44 | |
| 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 | 0.44 | |
| 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 | 0.63 | |
| 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 | 0.63 | |
| 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 | 0.49 | |
| 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 | 0.63 | |
| 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 | 0.42 | |
| SLK | STE20 | STE | 8bem | A | B | tivozanib | Human | 14486 | 0.46 | |
| KDR | VEGFR | TK | 3wzd | A | B | 4-{3-chloro-4-[(cyclopropylcarbamoyl)amino]phenoxy}-7-methoxyquinoline-6-carboxamide | Human | 5350 | 0.45 | |
| 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 | 0.44 | |
| 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 | 0.44 | |
| 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 | 0.45 | |
| 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 | 0.47 | |
| 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 | 0.45 | |
| 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 | 0.49 | |
| 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 | 0.63 | |
| EPHA2 (EphA2) | Eph | TK | 5ia5 | A | B | golvatinib | Human | 7183 | 0.43 | |
| SLK | STE20 | STE | 8bem | A | A | tivozanib | Human | 14487 | 0.46 | |
| EPHA2 (EphA2) | Eph | TK | 5ia5 | A | A | golvatinib | Human | 7192 | 0.43 | |
| KDR | VEGFR | TK | 3b8q | A | | n-(4-chlorophenyl)-6-[(6,7-dimethoxyquinolin-4-yl)oxy]naphthalene-1-carboxamide | Human | 5332 | 0.52 | |
| KDR | VEGFR | TK | 3b8q | B | | n-(4-chlorophenyl)-6-[(6,7-dimethoxyquinolin-4-yl)oxy]naphthalene-1-carboxamide | Human | 5319 | 0.52 | |
| 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 | 0.51 | |
| KDR | VEGFR | TK | 3b8r | B | | n-cyclopropyl-6-[(6,7-dimethoxyquinolin-4-yl)oxy]naphthalene-1-carboxamide | Human | 5341 | 0.47 | |
| KDR | VEGFR | TK | 3b8r | A | | n-cyclopropyl-6-[(6,7-dimethoxyquinolin-4-yl)oxy]naphthalene-1-carboxamide | Human | 5327 | 0.47 | |
| 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 | 0.45 | |
| KDR | VEGFR | TK | 6gqp | A | B | ~{n}-[4-(6,7-dimethoxyquinazolin-4-yl)oxyphenyl]-2-(1-ethylpyrazol-4-yl)ethanamide | Human | 10584 | 0.41 | |
| KDR | VEGFR | TK | 3wzd | A | A | 4-{3-chloro-4-[(cyclopropylcarbamoyl)amino]phenoxy}-7-methoxyquinoline-6-carboxamide | Human | 5325 | 0.45 | |
| KDR | VEGFR | TK | 6gqq | A | A | ~{n}-[4-(6,7-dimethoxyquinazolin-4-yl)oxyphenyl]-2-(4-propan-2-yl-1,2,3-triazol-1-yl)ethanamide | Human | 10581 | 0.40 | |
| KDR | VEGFR | TK | 6gqq | A | B | ~{n}-[4-(6,7-dimethoxyquinazolin-4-yl)oxyphenyl]-2-(4-propan-2-yl-1,2,3-triazol-1-yl)ethanamide | Human | 10585 | 0.40 | |
| KDR | VEGFR | TK | 4ase | A | | tivozanib | Human | 5349 | 0.46 | |
| KDR | VEGFR | TK | 6gqp | A | A | ~{n}-[4-(6,7-dimethoxyquinazolin-4-yl)oxyphenyl]-2-(1-ethylpyrazol-4-yl)ethanamide | Human | 10582 | 0.41 | |
| SYK | Syk | TK | 3tuc | A | | 1-benzyl-n-{5-[(6,7-dimethoxyquinolin-4-yl)oxy]pyridin-2-yl}-2-oxo-1,2-dihydropyridine-3-carboxamide | Human | 1195 | 0.47 | |
| SYK | Syk | TK | 3tub | A | | 1-{5-[(6,7-dimethoxyquinolin-4-yl)oxy]pyridin-2-yl}-3-[(1r,2s)-2-phenylcyclopropyl]urea | Human | 1179 | 0.50 | |
| FGFR1 | FGFR | TK | 4rwl | B | | 6-({7-[(1-aminocyclopropyl)methoxy]-6-methoxyquinolin-4-yl}oxy)-n-methylnaphthalene-1-carboxamide | Human | 3596 | 0.47 | |
| FGFR1 | FGFR | TK | 5zv2 | A | | 4-{3-chloro-4-[(cyclopropylcarbamoyl)amino]phenoxy}-7-methoxyquinoline-6-carboxamide | Human | 10055 | 0.45 | |
| FGFR1 | FGFR | TK | 5zv2 | B | | 4-{3-chloro-4-[(cyclopropylcarbamoyl)amino]phenoxy}-7-methoxyquinoline-6-carboxamide | Human | 10054 | 0.45 | |
| EIF2AK3 (PEK) | PEK | Other | 4x7h | A | B | n-{5-[(6,7-dimethoxyquinolin-4-yl)oxy]pyridin-2-yl}-1-methyl-3-oxo-2-phenyl-5-(pyridin-4-yl)-2,3-dihydro-1h-pyrazole-4-carboxamide | Human | 7240 | 0.43 | |
| EIF2AK3 (PEK) | PEK | Other | 4x7h | A | A | n-{5-[(6,7-dimethoxyquinolin-4-yl)oxy]pyridin-2-yl}-1-methyl-3-oxo-2-phenyl-5-(pyridin-4-yl)-2,3-dihydro-1h-pyrazole-4-carboxamide | Human | 7247 | 0.43 | |
| KIT | PDGFR | TK | 6gql | B | | ~{n}-[4-(6,7-dimethoxyquinazolin-4-yl)oxyphenyl]-2-(4-propan-2-yl-1,2,3-triazol-1-yl)ethanamide | Human | 10357 | 0.40 | |
| KIT | PDGFR | TK | 6xva | A | | ~{n}-[[3-[2-[3-methoxy-5-(7-methoxyquinolin-4-yl)oxy-pyridin-2-yl]ethanoylamino]-5-methyl-phenyl]methyl]propanamide | Human | 12284 | 0.41 | |
| ALK | ALK | TK | 4fny | A | | n-(4-chlorophenyl)-5-[(6,7-dimethoxyquinolin-4-yl)oxy]-1,3-benzoxazol-2-amine | Human | 5367 | 0.44 | |
| 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 | 0.63 | |
| 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 | 0.63 | |
| 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 | 0.49 | |
| 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 | 0.63 | |
| 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 | 0.63 | |
| 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 | 0.47 | |
| MET | Met | TK | 3vw8 | A | | n-({4-[(6,7-dimethoxyquinolin-4-yl)oxy]phenyl}carbamothioyl)-2-phenylacetamide | Human | 2985 | 0.60 | |
| 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 | 0.42 | |
| 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 | |
| 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 | 0.49 | |
| 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 | 0.63 | |
| KIT | PDGFR | TK | 6gqk | B | A | ~{n}-[4-(6,7-dimethoxyquinazolin-4-yl)oxyphenyl]-2-(1-ethylpyrazol-4-yl)ethanamide | Human | 10363 | 0.41 | |
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