Proteins > Hepatocyte growth factor receptor
Page last updated: 2024-08-07 15:47:21
Hepatocyte growth factor receptor
A hepatocyte growth factor receptor that is encoded in the genome of human. [PRO:DNx, UniProtKB:P08581]
Synonyms
HGF receptor;
EC 2.7.10.1;
HGF/SF receptor;
Proto-oncogene c-Met;
Scatter factor receptor;
SF receptor;
Tyrosine-protein kinase Met
Research
Bioassay Publications (186)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 30 (16.13) | 29.6817 |
| 2010's | 131 (70.43) | 24.3611 |
| 2020's | 25 (13.44) | 2.80 |
Compounds (268)
Drugs with Inhibition Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| imatinib | Homo sapiens (human) | IC50 | 0.0216 | 1 | 1 |
| 4-hydroxyphenylethanol | Homo sapiens (human) | IC50 | 20.0000 | 1 | 1 |
| staurosporine | Homo sapiens (human) | IC50 | 0.1917 | 17 | 17 |
| epigallocatechin gallate | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| epigallocatechin gallate | Homo sapiens (human) | Ki | 3.3000 | 1 | 1 |
| epicatechin gallate | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| vatalanib | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| birb 796 | Homo sapiens (human) | IC50 | 30.0000 | 1 | 1 |
| erlotinib | Homo sapiens (human) | IC50 | 12.5000 | 1 | 1 |
| (-)-gallocatechin gallate | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| sorafenib | Homo sapiens (human) | IC50 | 5.7500 | 1 | 1 |
| hematoxylin | Homo sapiens (human) | IC50 | 0.4000 | 1 | 1 |
| hydroxyphenethylferulate | Homo sapiens (human) | IC50 | 12.9000 | 1 | 1 |
| n-(indol-3-ylglyoxylyl)benzylamine | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
| quercetin | Homo sapiens (human) | IC50 | 0.5800 | 1 | 1 |
| norlichexanthone | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
| ellagic acid | Homo sapiens (human) | IC50 | 0.5800 | 1 | 1 |
| astrogorgiadiol | Homo sapiens (human) | IC50 | 78.0000 | 1 | 1 |
| su 11248 | Homo sapiens (human) | IC50 | 7.0001 | 6 | 6 |
| coniferyl ferulate | Homo sapiens (human) | IC50 | 20.0000 | 1 | 1 |
| a 419259 | Homo sapiens (human) | IC50 | 20.0000 | 1 | 1 |
| gdp 366 | Homo sapiens (human) | IC50 | 50.0000 | 1 | 1 |
| ((3z)-n-(3-chlorophenyl)-3-((3,5-dimethyl-4-((4-methylpiperazin-1-yl)carbonyl)-1h-pyrrol-2-yl)methylene)-n-methyl-2-oxo-2,3-dihydro-1h-indole-5-sulfonamide) | Homo sapiens (human) | IC50 | 0.2864 | 7 | 7 |
| ki23057 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| oblongifolin c | Homo sapiens (human) | IC50 | 7.7700 | 1 | 1 |
| sotrastaurin | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| pha 665752 | Homo sapiens (human) | IC50 | 0.0187 | 6 | 6 |
| l 783277 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| cembra-2,7,11-triene-4,6-diol | Homo sapiens (human) | IC50 | 22.6000 | 1 | 1 |
| ki 8751 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| danusertib | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| nvp-aew541 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| arq 197 | Homo sapiens (human) | IC50 | 0.3600 | 1 | 1 |
| arq 197 | Homo sapiens (human) | Ki | 0.3550 | 2 | 2 |
| 3-[1-(2,6-dichloro-3-fluorophenyl)ethoxy]-5-[1-(piperidin-4-yl)pyrazol-4-yl]pyridin-2-amine | Homo sapiens (human) | IC50 | 0.0164 | 2 | 2 |
| 3-[1-(2,6-dichloro-3-fluorophenyl)ethoxy]-5-[1-(piperidin-4-yl)pyrazol-4-yl]pyridin-2-amine | Homo sapiens (human) | Ki | 0.0193 | 1 | 1 |
| tak 285 | Homo sapiens (human) | IC50 | 4.2000 | 1 | 1 |
| crizotinib | Homo sapiens (human) | IC50 | 0.0057 | 33 | 33 |
| crizotinib | Homo sapiens (human) | Ki | 0.0027 | 3 | 3 |
| 4-[2-(2-chloro-4-fluoroanilino)-5-methyl-4-pyrimidinyl]-N-[(1S)-1-(3-chlorophenyl)-2-hydroxyethyl]-1H-pyrrole-2-carboxamide | Homo sapiens (human) | Ki | 4.0000 | 1 | 1 |
| osi 906 | Homo sapiens (human) | IC50 | 12.5000 | 1 | 1 |
| 2,4,3',5'-tetrahydroxystilbene | Homo sapiens (human) | IC50 | 5.1500 | 2 | 2 |
| pha 767491 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| N-(2,4-dimethoxyphenyl)-N-[2-[4-(4-methyl-1-piperazinyl)anilino]-4-pyrimidinyl]carbamic acid (2,6-dimethylphenyl) ester | Homo sapiens (human) | IC50 | 0.4870 | 1 | 4 |
| nvp-tae684 | Homo sapiens (human) | IC50 | 1.6670 | 1 | 1 |
| e 7050 | Homo sapiens (human) | IC50 | 0.0160 | 3 | 3 |
| pha 848125 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| amg 1 | Homo sapiens (human) | IC50 | 0.0344 | 3 | 3 |
| amg 1 | Homo sapiens (human) | Ki | 0.2920 | 3 | 4 |
| pf 04217903 | Homo sapiens (human) | IC50 | 0.0136 | 5 | 4 |
| pf 04217903 | Homo sapiens (human) | Ki | 3.3274 | 4 | 3 |
| meleagrin | Homo sapiens (human) | IC50 | 3.1500 | 2 | 2 |
| amg 458 | Homo sapiens (human) | IC50 | 0.0434 | 3 | 3 |
| amg 458 | Homo sapiens (human) | Ki | 0.2754 | 8 | 15 |
| sgx 523 | Homo sapiens (human) | IC50 | 0.0038 | 4 | 4 |
| bms 777607 | Homo sapiens (human) | IC50 | 0.0343 | 21 | 19 |
| ponatinib | Homo sapiens (human) | IC50 | 0.0017 | 1 | 1 |
| AMG-208 | Homo sapiens (human) | IC50 | 0.0342 | 9 | 11 |
| N-[[3-fluoro-4-[[2-(1-methyl-4-imidazolyl)-7-thieno[3,2-b]pyridinyl]oxy]anilino]-sulfanylidenemethyl]-2-phenylacetamide | Homo sapiens (human) | IC50 | 0.0721 | 9 | 10 |
| cabozantinib | Homo sapiens (human) | IC50 | 0.0791 | 27 | 28 |
| entrectinib | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| pexidartinib | Homo sapiens (human) | IC50 | 3.3000 | 1 | 1 |
| emd1214063 | Homo sapiens (human) | IC50 | 0.0048 | 4 | 4 |
| N-trans-sinapoyltyramine | Homo sapiens (human) | IC50 | 20.0000 | 1 | 1 |
| gsk 1363089 | Homo sapiens (human) | IC50 | 0.0560 | 58 | 65 |
| mk 2461 | Homo sapiens (human) | IC50 | 0.4413 | 18 | 18 |
| nvp bvu972 | Homo sapiens (human) | IC50 | 0.0140 | 1 | 1 |
| 4-[6-[4-(methoxycarbonylamino)phenyl]-4-(4-morpholinyl)-1-pyrazolo[3,4-d]pyrimidinyl]-1-piperidinecarboxylic acid methyl ester | Homo sapiens (human) | IC50 | 50.0000 | 1 | 1 |
| tas-115 | Homo sapiens (human) | IC50 | 0.0320 | 1 | 1 |
| n-(3-fluoro-4-((1-methyl-6-(1h-pyrazol-4-yl)-1h-indazol-5 yl)oxy)phenyl)-1-(4-fluorophenyl)-6-methyl-2-oxo-1,2-dihydropyridine-3-carboxamide | Homo sapiens (human) | IC50 | 0.0047 | 1 | 1 |
| mk-8033 | Homo sapiens (human) | IC50 | 1.0629 | 10 | 10 |
| pha 793887 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| nps-1034 | Homo sapiens (human) | IC50 | 0.0480 | 2 | 2 |
| tak-632 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| jnj38877605 | Homo sapiens (human) | IC50 | 0.0042 | 5 | 5 |
| nms p937 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| alectinib | Homo sapiens (human) | IC50 | 5.0000 | 1 | 1 |
| nms-p118 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| dcc-2701 | Homo sapiens (human) | IC50 | 0.0027 | 3 | 3 |
| lfm a13 | Homo sapiens (human) | IC50 | 215.0000 | 1 | 1 |
| urmc-099 | Homo sapiens (human) | IC50 | 0.1770 | 1 | 1 |
| ent-crizotinib | Homo sapiens (human) | Ki | 0.1610 | 1 | 1 |
| ceritinib | Homo sapiens (human) | IC50 | 1.2967 | 6 | 6 |
| volitinib | Homo sapiens (human) | IC50 | 5.3852 | 6 | 6 |
| osimertinib | Homo sapiens (human) | IC50 | 1.0000 | 1 | 1 |
| unc2025 | Homo sapiens (human) | IC50 | 0.3640 | 1 | 1 |
| chir 258 | Homo sapiens (human) | IC50 | 0.0011 | 1 | 1 |
| bms 536924 | Homo sapiens (human) | IC50 | 4.8700 | 1 | 1 |
| nms-e973 | Homo sapiens (human) | IC50 | 0.0100 | 1 | 1 |
Drugs with Activation Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| fasudil | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| 4-(4'-hydroxyphenyl)-amino-6,7-dimethoxyquinazoline | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| sb 202190 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| imatinib | Homo sapiens (human) | Kd | 14.0000 | 5 | 5 |
| triciribine phosphate | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| staurosporine | Homo sapiens (human) | Kd | 0.1625 | 4 | 4 |
| picropodophyllin | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| gefitinib | Homo sapiens (human) | Kd | 7.5744 | 5 | 5 |
| lestaurtinib | Homo sapiens (human) | Kd | 4.4859 | 7 | 7 |
| vatalanib | Homo sapiens (human) | Kd | 14.0000 | 5 | 5 |
| ruboxistaurin | Homo sapiens (human) | Kd | 14.0000 | 5 | 5 |
| canertinib | Homo sapiens (human) | Kd | 8.7460 | 5 | 5 |
| birb 796 | Homo sapiens (human) | Kd | 10.0000 | 4 | 4 |
| cyc 202 | Homo sapiens (human) | Kd | 20.0000 | 2 | 2 |
| sb 203580 | Homo sapiens (human) | Kd | 9.4750 | 4 | 4 |
| enzastaurin | Homo sapiens (human) | Kd | 12.8000 | 4 | 4 |
| erlotinib | Homo sapiens (human) | Kd | 8.3000 | 5 | 5 |
| lapatinib | Homo sapiens (human) | Kd | 14.0000 | 5 | 5 |
| sorafenib | Homo sapiens (human) | Kd | 10.0000 | 7 | 7 |
| pd 173955 | Homo sapiens (human) | Kd | 0.9700 | 4 | 4 |
| s 1033 | Homo sapiens (human) | Kd | 15.0000 | 4 | 4 |
| bms 387032 | Homo sapiens (human) | Kd | 8.3326 | 5 | 5 |
| sf 2370 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| tandutinib | Homo sapiens (human) | Kd | 12.5000 | 8 | 8 |
| vx-745 | Homo sapiens (human) | Kd | 10.0000 | 4 | 4 |
| dasatinib | Homo sapiens (human) | Kd | 14.0000 | 5 | 5 |
| ha 1100 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| 7-epi-hydroxystaurosporine | Homo sapiens (human) | Kd | 0.9370 | 1 | 1 |
| zd 6474 | Homo sapiens (human) | Kd | 11.1000 | 5 | 5 |
| 4-(5-benzo(1,3)dioxol-5-yl-4-pyridin-2-yl-1h-imidazol-2-yl)benzamide | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| imd 0354 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| sirolimus | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| alvocidib | Homo sapiens (human) | Kd | 14.0000 | 5 | 5 |
| bosutinib | Homo sapiens (human) | Kd | 10.5250 | 4 | 4 |
| orantinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| su 11248 | Homo sapiens (human) | Kd | 8.6250 | 8 | 8 |
| palbociclib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| jnj-7706621 | Homo sapiens (human) | Kd | 0.6500 | 1 | 1 |
| vx680 | Homo sapiens (human) | Kd | 0.6350 | 5 | 5 |
| cyc 116 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| everolimus | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| ekb 569 | Homo sapiens (human) | Kd | 6.2000 | 1 | 1 |
| axitinib | Homo sapiens (human) | Kd | 8.2275 | 4 | 4 |
| temsirolimus | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| pd 184352 | Homo sapiens (human) | Kd | 10.0000 | 3 | 3 |
| on 01910 | Homo sapiens (human) | Kd | 0.9400 | 1 | 1 |
| av 412 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| telatinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| y-39983 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| cp 547632 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| bms345541 | Homo sapiens (human) | Kd | 10.0000 | 3 | 3 |
| lenvatinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| pd 0325901 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| midostaurin | Homo sapiens (human) | Kd | 4.6738 | 8 | 8 |
| px-866 | Homo sapiens (human) | Kd | 30.0000 | 1 | 2 |
| ripasudil | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| osi 930 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| ki 20227 | Homo sapiens (human) | Kd | 0.9767 | 3 | 3 |
| scio-469 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| cp 724714 | Homo sapiens (human) | Kd | 20.0000 | 2 | 2 |
| pi103 | Homo sapiens (human) | Kd | 10.0000 | 4 | 4 |
| hmn-214 | Homo sapiens (human) | Kd | 1.3930 | 1 | 1 |
| tivozanib | Homo sapiens (human) | Kd | 5.4030 | 1 | 1 |
| hki 272 | Homo sapiens (human) | Kd | 11.2250 | 4 | 4 |
| tofacitinib | Homo sapiens (human) | Kd | 14.0000 | 5 | 5 |
| n-(6-chloro-7-methoxy-9h-beta-carbolin-8-yl)-2-methylnicotinamide | Homo sapiens (human) | Kd | 10.0000 | 3 | 3 |
| cediranib | Homo sapiens (human) | Kd | 1.6065 | 4 | 4 |
| masitinib | Homo sapiens (human) | Kd | 15.0000 | 4 | 4 |
| ly-2157299 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| pazopanib | Homo sapiens (human) | Kd | 9.5000 | 5 | 5 |
| azd 6244 | Homo sapiens (human) | Kd | 15.0000 | 4 | 4 |
| su 14813 | Homo sapiens (human) | Kd | 12.6400 | 5 | 5 |
| bibw 2992 | Homo sapiens (human) | Kd | 2.7393 | 4 | 4 |
| binimetinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| sotrastaurin | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| aee 788 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| saracatinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| vx 702 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| crenolanib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| tg100-115 | Homo sapiens (human) | Kd | 15.0000 | 4 | 4 |
| cc 401 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| bms 599626 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| exel-7647 | Homo sapiens (human) | Kd | 30.0000 | 1 | 2 |
| volasertib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| pha 665752 | Homo sapiens (human) | EC50 | 0.0420 | 1 | 1 |
| pha 665752 | Homo sapiens (human) | Kd | 0.0006 | 3 | 3 |
| azd 7762 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| regorafenib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| 6-[[5-fluoro-2-(3,4,5-trimethoxyanilino)-4-pyrimidinyl]amino]-2,2-dimethyl-4H-pyrido[3,2-b][1,4]oxazin-3-one | Homo sapiens (human) | Kd | 7.8175 | 4 | 4 |
| brivanib | Homo sapiens (human) | Kd | 15.0000 | 4 | 4 |
| mp470 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| rgb 286638 | Homo sapiens (human) | Kd | 30.0000 | 1 | 2 |
| at 7519 | Homo sapiens (human) | Kd | 15.0000 | 4 | 4 |
| bi 2536 | Homo sapiens (human) | Kd | 13.1000 | 4 | 4 |
| inno-406 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| nvp-ast487 | Homo sapiens (human) | Kd | 2.4083 | 4 | 4 |
| kw 2449 | Homo sapiens (human) | Kd | 7.7375 | 4 | 4 |
| danusertib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| abt 869 | Homo sapiens (human) | Kd | 6.0967 | 6 | 6 |
| azd 8931 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| arq 197 | Homo sapiens (human) | Kd | 0.5110 | 1 | 1 |
| azd 1152 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| pf 00299804 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| ridaforolimus | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| ch 4987655 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| 6-(5-((cyclopropylamino)carbonyl)-3-fluoro-2-methylphenyl)-n-(2,2-dimethylprpyl)-3-pyridinecarboxamide | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| cc-930 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| gw 2580 | Homo sapiens (human) | Kd | 10.0000 | 4 | 4 |
| tak 285 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| idelalisib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| crizotinib | Homo sapiens (human) | Kd | 0.0024 | 6 | 6 |
| osi 906 | Homo sapiens (human) | Kd | 0.3950 | 1 | 1 |
| chir-265 | Homo sapiens (human) | Kd | 11.5200 | 5 | 5 |
| motesanib | Homo sapiens (human) | Kd | 14.0000 | 5 | 5 |
| fostamatinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| trametinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 2 |
| mln8054 | Homo sapiens (human) | Kd | 14.0000 | 5 | 5 |
| pf-562,271 | Homo sapiens (human) | Kd | 2.0180 | 1 | 1 |
| GDC-0879 | Homo sapiens (human) | Kd | 10.0000 | 3 | 3 |
| jnj-26483327 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| ly2603618 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| tg100801 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| dactolisib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| bgt226 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| gsk 461364 | Homo sapiens (human) | Kd | 15.0000 | 4 | 4 |
| azd 1152-hqpa | Homo sapiens (human) | Kd | 13.1400 | 5 | 5 |
| nvp-tae684 | Homo sapiens (human) | Kd | 0.1380 | 3 | 3 |
| enmd 2076 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| e 7050 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| tak-901 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| gdc-0973 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| azd 1480 | Homo sapiens (human) | Kd | 30.0000 | 1 | 2 |
| pha 848125 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| ro5126766 | Homo sapiens (human) | Kd | 30.0000 | 1 | 2 |
| fedratinib | Homo sapiens (human) | Kd | 13.2250 | 4 | 4 |
| gsk690693 | Homo sapiens (human) | Kd | 15.0000 | 4 | 4 |
| 14-methyl-20-oxa-5,7,14,26-tetraazatetracyclo(19.3.1.1(2,6).1(8,12))heptacosa-1(25),2(26),3,5,8(27),9,11,16,21,23-decaene | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| azd5438 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| pf 04217903 | Homo sapiens (human) | EC50 | 0.0003 | 1 | 1 |
| pf 04217903 | Homo sapiens (human) | Kd | 0.0032 | 2 | 1 |
| gdc 0941 | Homo sapiens (human) | Kd | 15.0000 | 4 | 4 |
| icotinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| ph 797804 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| kx-01 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| plx 4720 | Homo sapiens (human) | Kd | 10.0000 | 3 | 3 |
| mk 5108 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| cx 4945 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| cudc 101 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| arry-614 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| tak 593 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| mln 8237 | Homo sapiens (human) | Kd | 30.0000 | 1 | 2 |
| sgx 523 | Homo sapiens (human) | Kd | 7.5012 | 4 | 4 |
| bms 754807 | Homo sapiens (human) | Kd | 0.0140 | 1 | 1 |
| bms 777607 | Homo sapiens (human) | Kd | 0.0110 | 1 | 1 |
| sgi 1776 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| pci 32765 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| ponatinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| amg 900 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| mk-1775 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| AMG-208 | Homo sapiens (human) | Kd | 0.0280 | 1 | 1 |
| quizartinib | Homo sapiens (human) | Kd | 12.8571 | 7 | 7 |
| at13148 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| tak 733 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| mk 2206 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| sns 314 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| lucitanib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| n-(cyanomethyl)-4-(2-((4-(4-morpholinyl)phenyl)amino)-4-pyrimidinyl)benzamide | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| dcc-2036 | Homo sapiens (human) | Kd | 0.1260 | 1 | 1 |
| cabozantinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| defactinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| ly2584702 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| incb-018424 | Homo sapiens (human) | Kd | 15.0000 | 4 | 4 |
| poziotinib | Homo sapiens (human) | Kd | 0.7940 | 1 | 1 |
| asp3026 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| entrectinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| pexidartinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| TAK-580 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| emd1214063 | Homo sapiens (human) | Kd | 0.0010 | 1 | 1 |
| gsk 1838705a | Homo sapiens (human) | Kd | 10.0000 | 3 | 3 |
| pf 3758309 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| gdc 0980 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| azd2014 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| (5-(2,4-bis((3s)-3-methylmorpholin-4-yl)pyrido(2,3-d)pyrimidin-7-yl)-2-methoxyphenyl)methanol | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| plx4032 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| gsk 1363089 | Homo sapiens (human) | Kd | 0.0243 | 4 | 4 |
| arry-334543 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| kin-193 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| mk 2461 | Homo sapiens (human) | Kd | 6.0121 | 5 | 5 |
| bay 869766 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| as 703026 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| baricitinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 2 |
| dabrafenib | Homo sapiens (human) | Kd | 1.6340 | 1 | 1 |
| pki 587 | Homo sapiens (human) | Kd | 30.0000 | 1 | 2 |
| n-(3-fluoro-4-((1-methyl-6-(1h-pyrazol-4-yl)-1h-indazol-5 yl)oxy)phenyl)-1-(4-fluorophenyl)-6-methyl-2-oxo-1,2-dihydropyridine-3-carboxamide | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| ribociclib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| mk-8033 | Homo sapiens (human) | Kd | 0.0582 | 3 | 3 |
| pha 793887 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| sb 1518 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| abemaciclib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| mk-8776 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| afuresertib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| gsk 1070916 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| jnj38877605 | Homo sapiens (human) | Kd | 0.0020 | 1 | 1 |
| dinaciclib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| gilteritinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| alectinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| glpg0634 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| encorafenib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| bms-911543 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| gsk2141795 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| azd8186 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| byl719 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| ent-crizotinib | Homo sapiens (human) | Kd | 0.0375 | 1 | 1 |
| cep-32496 | Homo sapiens (human) | Kd | 15.2565 | 2 | 2 |
| ceritinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| azd1208 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| vx-509 | Homo sapiens (human) | Kd | 0.0940 | 1 | 1 |
| debio 1347 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| at 9283 | Homo sapiens (human) | Kd | 0.0070 | 1 | 1 |
| otssp167 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| chir 258 | Homo sapiens (human) | Kd | 14.0000 | 5 | 5 |
| nintedanib | Homo sapiens (human) | Kd | 7.7500 | 4 | 4 |
| bay 80-6946 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| pp242 | Homo sapiens (human) | Kd | 10.0000 | 3 | 3 |
Drugs with Other Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| bms 777607 | Homo sapiens (human) | INH | 0.0039 | 1 | 1 |
| cabozantinib | Homo sapiens (human) | INH | 0.0210 | 1 | 1 |
| gsk 1363089 | Homo sapiens (human) | INH | 0.0004 | 1 | 1 |
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Targeting gain of function and resistance mutations in Abl and KIT by hybrid compound design.Journal of medicinal chemistry, , Jul-25, Volume: 56, Issue:14, 2013
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
Isoxazole derivatives as anticancer agent: A review on synthetic strategies, mechanism of action and SAR studies.European journal of medicinal chemistry, , Oct-05, Volume: 221, 2021
Design, synthesis and biological evaluation of novel 4-(pyrrolo[2,3-d]pyrimidine-4-yloxy)benzamide derivatives as potential antitumor agents.Bioorganic & medicinal chemistry letters, , 02-01, Volume: 33, 2021
Design, synthesis and biological evaluation of 4-(pyridin-4-yloxy)benzamide derivatives bearing a 5-methylpyridazin-3(2H)-one fragment.Bioorganic & medicinal chemistry letters, , 05-01, Volume: 30, Issue:9, 2020
ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells.European journal of medicinal chemistry, , Jan-01, Volume: 161, 2019
Challenging clinically unresponsive medullary thyroid cancer: Discovery and pharmacological activity of novel RET inhibitors.European journal of medicinal chemistry, , Apr-25, Volume: 150, 2018
Identification of novel NEuropean journal of medicinal chemistry, , Feb-25, Volume: 146, 2018
Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors.Bioorganic & medicinal chemistry, , 05-01, Volume: 26, Issue:8, 2018
Synthesis and evaluation of a series of pyridine and pyrimidine derivatives as type II c-Met inhibitors.Bioorganic & medicinal chemistry, , 06-15, Volume: 25, Issue:12, 2017
Novel LCK/FMS inhibitors based on phenoxypyrimidine scaffold as potential treatment for inflammatory disorders.European journal of medicinal chemistry, , Dec-01, Volume: 141, 2017
Synthesis, antitumor evaluation and molecular docking studies of [1,2,4]triazolo[4,3-b][1,2,4,5]tetrazine derivatives.Bioorganic & medicinal chemistry letters, , 07-01, Volume: 26, Issue:13, 2016
Synthesis and biological evaluation of new [1,2,4]triazolo[4,3-a]pyridine derivatives as potential c-Met inhibitors.Bioorganic & medicinal chemistry, , 08-15, Volume: 24, Issue:16, 2016
Discovery of 4-arylamido 3-methyl isoxazole derivatives as novel FMS kinase inhibitors.European journal of medicinal chemistry, , Sep-18, Volume: 102, 2015
Protein kinase and HDAC inhibitors from the endophytic fungus Epicoccum nigrum.Journal of natural products, , Jan-24, Volume: 77, Issue:1, 2014
Syntheses of phenylpyrazolodiazepin-7-ones as conformationally rigid analogs of aminopyrazole amide scaffold and their antiproliferative effects on cancer cells.Bioorganic & medicinal chemistry, , Nov-15, Volume: 19, Issue:22, 2011
Imidazo[2,1-b]thiazole guanylhydrazones as RSK2 inhibitors.European journal of medicinal chemistry, , Volume: 46, Issue:9, 2011
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
Synthesis, activity, and pharmacophore development for isatin-beta-thiosemicarbazones with selective activity toward multidrug-resistant cells.Journal of medicinal chemistry, , May-28, Volume: 52, Issue:10, 2009
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
Discovery of 2-pyrimidyl-5-amidothiophenes as potent inhibitors for AKT: synthesis and SAR studies.Bioorganic & medicinal chemistry letters, , Aug-15, Volume: 16, Issue:16, 2006
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).Blood, , Oct-01, Volume: 114, Issue:14, 2009
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
Identification of a new chemical class of potent angiogenesis inhibitors based on conformational considerations and database searching.Bioorganic & medicinal chemistry letters, , Sep-15, Volume: 13, Issue:18, 2003
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD).Bioorganic & medicinal chemistry letters, , Dec-01, Volume: 21, Issue:23, 2011
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Discovery and Biological Evaluation of Novel Dual EGFR/c-Met Inhibitors.ACS medicinal chemistry letters, , Apr-10, Volume: 5, Issue:4, 2014
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
Design, synthesis and docking study of novel picolinamide derivatives as anticancer agents and VEGFR-2 inhibitors.European journal of medicinal chemistry, , Apr-15, Volume: 168, 2019
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).Blood, , Oct-01, Volume: 114, Issue:14, 2009
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
Dual MET and SMO Negative Modulators Overcome Resistance to EGFR Inhibitors in Human Nonsmall Cell Lung Cancer.Journal of medicinal chemistry, , 09-14, Volume: 60, Issue:17, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).Blood, , Oct-01, Volume: 114, Issue:14, 2009
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Targeting gain of function and resistance mutations in Abl and KIT by hybrid compound design.Journal of medicinal chemistry, , Jul-25, Volume: 56, Issue:14, 2013
Imidazo[2,1-b]thiazole guanylhydrazones as RSK2 inhibitors.European journal of medicinal chemistry, , Volume: 46, Issue:9, 2011
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
N-(3-fluoro-4-(2-arylthieno[3,2-b]pyridin-7-yloxy)phenyl)-2-oxo-3-phenylimidazolidine-1-carboxamides: a novel series of dual c-Met/VEGFR2 receptor tyrosine kinase inhibitors.Bioorganic & medicinal chemistry letters, , Mar-01, Volume: 19, Issue:5, 2009
N-(4-(6,7-Disubstituted-quinolin-4-yloxy)-3-fluorophenyl)-2-oxo-3-phenylimidazolidine-1-carboxamides: a novel series of dual c-Met/VEGFR2 receptor tyrosine kinase inhibitors.Bioorganic & medicinal chemistry letters, , Dec-01, Volume: 19, Issue:23, 2009
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).Blood, , Oct-01, Volume: 114, Issue:14, 2009
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
Discovery of a novel and potent series of thieno[3,2-b]pyridine-based inhibitors of c-Met and VEGFR2 tyrosine kinases.Bioorganic & medicinal chemistry letters, , May-01, Volume: 18, Issue:9, 2008
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
Identification of new aminoacid amides containing the imidazo[2,1-b]benzothiazol-2-ylphenyl moiety as inhibitors of tumorigenesis by oncogenic Met signaling.European journal of medicinal chemistry, , Volume: 47, Issue:1, 2012
Synthesis and c-Met kinase inhibition of 3,5-disubstituted and 3,5,7-trisubstituted quinolines: identification of 3-(4-acetylpiperazin-1-yl)-5-(3-nitrobenzylamino)-7- (trifluoromethyl)quinoline as a novel anticancer agent.Journal of medicinal chemistry, , Apr-14, Volume: 54, Issue:7, 2011
Structure based drug design of crizotinib (PF-02341066), a potent and selective dual inhibitor of mesenchymal-epithelial transition factor (c-MET) kinase and anaplastic lymphoma kinase (ALK).Journal of medicinal chemistry, , Sep-22, Volume: 54, Issue:18, 2011
Combined SVM-based and docking-based virtual screening for retrieving novel inhibitors of c-Met.European journal of medicinal chemistry, , Volume: 46, Issue:9, 2011
A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases.Proceedings of the National Academy of Sciences of the United States of America, , Dec-18, Volume: 104, Issue:51, 2007
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).Blood, , Oct-01, Volume: 114, Issue:14, 2009
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Discovery of 3-(1H-indol-3-yl)-4-[2-(4-methylpiperazin-1-yl)quinazolin-4-yl]pyrrole-2,5-dione (AEB071), a potent and selective inhibitor of protein kinase C isotypes.Journal of medicinal chemistry, , Oct-22, Volume: 52, Issue:20, 2009
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
Recent advances in the development of dual VEGFR and c-Met small molecule inhibitors as anticancer drugs.European journal of medicinal chemistry, , Jan-27, Volume: 108, 2016
Structure based drug design of crizotinib (PF-02341066), a potent and selective dual inhibitor of mesenchymal-epithelial transition factor (c-MET) kinase and anaplastic lymphoma kinase (ALK).Journal of medicinal chemistry, , Sep-22, Volume: 54, Issue:18, 2011
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
N-(3-fluoro-4-(2-arylthieno[3,2-b]pyridin-7-yloxy)phenyl)-2-oxo-3-phenylimidazolidine-1-carboxamides: a novel series of dual c-Met/VEGFR2 receptor tyrosine kinase inhibitors.Bioorganic & medicinal chemistry letters, , Mar-01, Volume: 19, Issue:5, 2009
N-(4-(6,7-Disubstituted-quinolin-4-yloxy)-3-fluorophenyl)-2-oxo-3-phenylimidazolidine-1-carboxamides: a novel series of dual c-Met/VEGFR2 receptor tyrosine kinase inhibitors.Bioorganic & medicinal chemistry letters, , Dec-01, Volume: 19, Issue:23, 2009
Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling.Proceedings of the National Academy of Sciences of the United States of America, , Dec-11, Volume: 104, Issue:50, 2007
(1S,2E,4S,7E,11E)-2,7,11-Cembratriene-4,6-diol semisynthetic analogs as novel c-Met inhibitors for the control of c-Met-dependent breast malignancies.Bioorganic & medicinal chemistry, , 11-15, Volume: 24, Issue:22, 2016
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazoles: identification of a potent Aurora kinase inhibitor with a favorable antitumor kinase inhibition profile.Journal of medicinal chemistry, , Nov-30, Volume: 49, Issue:24, 2006
Dual MET and SMO Negative Modulators Overcome Resistance to EGFR Inhibitors in Human Nonsmall Cell Lung Cancer.Journal of medicinal chemistry, , 09-14, Volume: 60, Issue:17, 2017
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
Principles of Kinase Allosteric Inhibition and Pocket Validation.Journal of medicinal chemistry, , 04-14, Volume: 65, Issue:7, 2022
Non-kinase targets of protein kinase inhibitors.Nature reviews. Drug discovery, , Volume: 16, Issue:6, 2017
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Recent advances in the development of dual VEGFR and c-Met small molecule inhibitors as anticancer drugs.European journal of medicinal chemistry, , Jan-27, Volume: 108, 2016
Design, synthesis and biological evaluation of 1H-pyrrolo[2,3-b]pyridine and 1H-pyrazolo[3,4-b]pyridine derivatives as c-Met inhibitors.Bioorganic chemistry, , Volume: 65, 2016
Structure based drug design of crizotinib (PF-02341066), a potent and selective dual inhibitor of mesenchymal-epithelial transition factor (c-MET) kinase and anaplastic lymphoma kinase (ALK).Journal of medicinal chemistry, , Sep-22, Volume: 54, Issue:18, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Design and synthesis of novel human epidermal growth factor receptor 2 (HER2)/epidermal growth factor receptor (EGFR) dual inhibitors bearing a pyrrolo[3,2-d]pyrimidine scaffold.Journal of medicinal chemistry, , Dec-08, Volume: 54, Issue:23, 2011
Discovery of pyrrolo[2,3-d]pyrimidine derivatives as potent Axl inhibitors: Design, synthesis and biological evaluation.European journal of medicinal chemistry, , Aug-05, Volume: 220, 2021
Promiscuity of in Vitro Secondary Pharmacology Assays and Implications for Lead Optimization Strategies.Journal of medicinal chemistry, , 06-25, Volume: 63, Issue:12, 2020
Fragment-based modification of 2,4-diarylaminopyrimidine derivatives as ALK and ROS1 dual inhibitors to overcome secondary mutants.Bioorganic & medicinal chemistry, , 10-15, Volume: 28, Issue:20, 2020
Synthesis and biological evaluation of quinoxaline derivatives as specific c-Met kinase inhibitors.Bioorganic & medicinal chemistry letters, , 07-01, Volume: 30, Issue:13, 2020
[no title available]Journal of medicinal chemistry, , 12-26, Volume: 62, Issue:24, 2019
Structural and Molecular Insight into Resistance Mechanisms of First Generation cMET Inhibitors.ACS medicinal chemistry letters, , Sep-12, Volume: 10, Issue:9, 2019
Discovery of novel 2,4-diarylaminopyrimidine analogues as ALK and ROS1 dual inhibitors to overcome crizotinib-resistant mutants including G1202R.European journal of medicinal chemistry, , Jan-01, Volume: 143, 2018
Discovery, optimization and biological evaluation for novel c-Met kinase inhibitors.European journal of medicinal chemistry, , Jan-01, Volume: 143, 2018
Discovery of [1,2,4]triazolo[3,4-b][1,3,4]thiadiazole derivatives as novel, potent and selective c-Met kinase inhibitors: Synthesis, SAR study, and biological activity.European journal of medicinal chemistry, , Apr-25, Volume: 150, 2018
Structure-based design, synthesis, and evaluation of 4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine derivatives as novel c-Met inhibitors.European journal of medicinal chemistry, , Sep-29, Volume: 138, 2017
The discovery of novel benzothiazinones as highly selective non-ATP competitive glycogen synthase kinase 3β inhibitors for the treatment of ovarian cancer.European journal of medicinal chemistry, , Jul-28, Volume: 135, 2017
Non-kinase targets of protein kinase inhibitors.Nature reviews. Drug discovery, , Volume: 16, Issue:6, 2017
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Design, synthesis and biological evaluation of 1H-pyrrolo[2,3-b]pyridine and 1H-pyrazolo[3,4-b]pyridine derivatives as c-Met inhibitors.Bioorganic chemistry, , Volume: 65, 2016
Design and synthesis of novel benzo[d]oxazol-2(3H)-one derivatives bearing 7-substituted-4-enthoxyquinoline moieties as c-Met kinase inhibitors.European journal of medicinal chemistry, , Jun-10, Volume: 115, 2016
Recent advances in the development of dual VEGFR and c-Met small molecule inhibitors as anticancer drugs.European journal of medicinal chemistry, , Jan-27, Volume: 108, 2016
Pyridazinone derivatives displaying highly potent and selective inhibitory activities against c-Met tyrosine kinase.European journal of medicinal chemistry, , Jan-27, Volume: 108, 2016
Discovery and Pharmacokinetic and Pharmacological Properties of the Potent and Selective MET Kinase Inhibitor 1-{6-[6-(4-Fluorophenyl)-[1,2,4]triazolo[4,3-b]pyridazin-3-ylsulfanyl]benzothiazol-2-yl}-3-(2-morpholin-4-ylethyl)urea (SAR125844).Journal of medicinal chemistry, , 08-11, Volume: 59, Issue:15, 2016
Design, synthesis and biological evaluation of c-Met kinase inhibitors bearing 2-oxo-1,2-dihydroquinoline scaffold.Bioorganic & medicinal chemistry letters, , 09-15, Volume: 26, Issue:18, 2016
Design, synthesis and biological evaluation of novel 4-arylaminopyrimidine derivatives possessing a hydrazone moiety as dual inhibitors of L1196M ALK and ROS1.European journal of medicinal chemistry, , Nov-10, Volume: 123, 2016
Synthesis and biological evaluation of new pyrazol-4-ylpyrimidine derivatives as potential ROS1 kinase inhibitors.European journal of medicinal chemistry, , Jan-27, Volume: 90, 2015
Discovery of novel 2,4-diarylaminopyrimidine analogues (DAAPalogues) showing potent inhibitory activities against both wild-type and mutant ALK kinases.Journal of medicinal chemistry, , Jan-08, Volume: 58, Issue:1, 2015
Enhancing the cellular anti-proliferation activity of pyridazinones as c-met inhibitors using docking analysis.European journal of medicinal chemistry, , May-05, Volume: 95, 2015
Design, Synthesis, and Biological Evaluation of Novel Imidazo[1,2-a]pyridine Derivatives as Potent c-Met Inhibitors.ACS medicinal chemistry letters, , May-14, Volume: 6, Issue:5, 2015
Novel 2,4-Diarylaminopyrimidine Analogues (DAAPalogues) Showing Potent c-Met/ALK Multikinase Inhibitory Activities.ACS medicinal chemistry letters, , Apr-10, Volume: 5, Issue:4, 2014
Aminopyridyl/Pyrazinyl Spiro[indoline-3,4'-piperidine]-2-ones As Highly Selective and Efficacious c-Met/ALK Inhibitors.ACS medicinal chemistry letters, , Aug-08, Volume: 4, Issue:8, 2013
Synthesis and biological evaluation of 2-amino-5-aryl-3-benzylthiopyridine scaffold based potent c-Met inhibitors.Bioorganic & medicinal chemistry, , Nov-01, Volume: 21, Issue:21, 2013
Discovery of novel 2-aminopyridine-3-carboxamides as c-Met kinase inhibitors.Bioorganic & medicinal chemistry, , Sep-01, Volume: 20, Issue:17, 2012
Synthesis of an aryloxy oxo pyrimidinone library that displays ALK-selective inhibition.Bioorganic & medicinal chemistry letters, , Aug-01, Volume: 21, Issue:15, 2011
Combined SVM-based and docking-based virtual screening for retrieving novel inhibitors of c-Met.European journal of medicinal chemistry, , Volume: 46, Issue:9, 2011
Structure based drug design of crizotinib (PF-02341066), a potent and selective dual inhibitor of mesenchymal-epithelial transition factor (c-MET) kinase and anaplastic lymphoma kinase (ALK).Journal of medicinal chemistry, , Sep-22, Volume: 54, Issue:18, 2011
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
Discovery of 6-benzyloxyquinolines as c-Met selective kinase inhibitors.Bioorganic & medicinal chemistry letters, , Feb-15, Volume: 20, Issue:4, 2010
Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling.Proceedings of the National Academy of Sciences of the United States of America, , Dec-11, Volume: 104, Issue:50, 2007
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Discovery and Biological Evaluation of Novel Dual EGFR/c-Met Inhibitors.ACS medicinal chemistry letters, , Apr-10, Volume: 5, Issue:4, 2014
The indole alkaloid meleagrin, from the olive tree endophytic fungus Penicillium chrysogenum, as a novel lead for the control of c-Met-dependent breast cancer proliferation, migration and invasion.Bioorganic & medicinal chemistry, , Jan-15, Volume: 24, Issue:2, 2016
Olive secoiridoids and semisynthetic bioisostere analogues for the control of metastatic breast cancer.Bioorganic & medicinal chemistry, , Apr-01, Volume: 21, Issue:7, 2013
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
Identification of NVP-TAE684, a potent, selective, and efficacious inhibitor of NPM-ALK.Proceedings of the National Academy of Sciences of the United States of America, , Jan-02, Volume: 104, Issue:1, 2007
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
The "Cyclopropyl Fragment" is a Versatile Player that Frequently Appears in Preclinical/Clinical Drug Molecules.Journal of medicinal chemistry, , 10-13, Volume: 59, Issue:19, 2016
Recent advances in the development of dual VEGFR and c-Met small molecule inhibitors as anticancer drugs.European journal of medicinal chemistry, , Jan-27, Volume: 108, 2016
Discovery of quinazolin-4-amines bearing benzimidazole fragments as dual inhibitors of c-Met and VEGFR-2.Bioorganic & medicinal chemistry, , Sep-01, Volume: 22, Issue:17, 2014
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Identification of N,1,4,4-tetramethyl-8-{[4-(4-methylpiperazin-1-yl)phenyl]amino}-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide (PHA-848125), a potent, orally available cyclin dependent kinase inhibitor.Journal of medicinal chemistry, , Aug-27, Volume: 52, Issue:16, 2009
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
Structure-based design of novel class II c-Met inhibitors: 2. SAR and kinase selectivity profiles of the pyrazolone series.Journal of medicinal chemistry, , Mar-08, Volume: 55, Issue:5, 2012
Combined SVM-based and docking-based virtual screening for retrieving novel inhibitors of c-Met.European journal of medicinal chemistry, , Volume: 46, Issue:9, 2011
Discovery of a potent, selective, and orally bioavailable c-Met inhibitor: 1-(2-hydroxy-2-methylpropyl)-N-(5-(7-methoxyquinolin-4-yloxy)pyridin-2-yl)-5-methyl-3-oxo-2-phenyl-2,3-dihydro-1H-pyrazole-4-carboxamide (AMG 458).Journal of medicinal chemistry, , Jul-10, Volume: 51, Issue:13, 2008
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Discovery and optimization of a series of imidazo[4,5-b]pyrazine derivatives as highly potent and exquisitely selective inhibitors of the mesenchymal-epithelial transition factor (c-Met) protein kinase.Bioorganic & medicinal chemistry, , 09-15, Volume: 24, Issue:18, 2016
Recent advances in the development of dual VEGFR and c-Met small molecule inhibitors as anticancer drugs.European journal of medicinal chemistry, , Jan-27, Volume: 108, 2016
Design, Synthesis, and Biological Evaluation of Novel Imidazo[1,2-a]pyridine Derivatives as Potent c-Met Inhibitors.ACS medicinal chemistry letters, , May-14, Volume: 6, Issue:5, 2015
Selectivity data: assessment, predictions, concordance, and implications.Journal of medicinal chemistry, , Sep-12, Volume: 56, Issue:17, 2013
Discovery of a novel class of exquisitely selective mesenchymal-epithelial transition factor (c-MET) protein kinase inhibitors and identification of the clinical candidate 2-(4-(1-(quinolin-6-ylmethyl)-1H-[1,2,3]triazolo[4,5-b]pyrazin-6-yl)-1H-pyrazol-1-yJournal of medicinal chemistry, , Sep-27, Volume: 55, Issue:18, 2012
[no title available],
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
Recent advances in the development of dual VEGFR and c-Met small molecule inhibitors as anticancer drugs.European journal of medicinal chemistry, , Jan-27, Volume: 108, 2016
Structure-based design of novel class II c-Met inhibitors: 2. SAR and kinase selectivity profiles of the pyrazolone series.Journal of medicinal chemistry, , Mar-08, Volume: 55, Issue:5, 2012
Discovery of a potent, selective, and orally bioavailable c-Met inhibitor: 1-(2-hydroxy-2-methylpropyl)-N-(5-(7-methoxyquinolin-4-yloxy)pyridin-2-yl)-5-methyl-3-oxo-2-phenyl-2,3-dihydro-1H-pyrazole-4-carboxamide (AMG 458).Journal of medicinal chemistry, , Jul-10, Volume: 51, Issue:13, 2008
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Design, synthesis and biological evaluation of 1H-pyrrolo[2,3-b]pyridine and 1H-pyrazolo[3,4-b]pyridine derivatives as c-Met inhibitors.Bioorganic chemistry, , Volume: 65, 2016
Recent advances in the development of dual VEGFR and c-Met small molecule inhibitors as anticancer drugs.European journal of medicinal chemistry, , Jan-27, Volume: 108, 2016
Synthesis and biological evaluation of new [1,2,4]triazolo[4,3-a]pyridine derivatives as potential c-Met inhibitors.Bioorganic & medicinal chemistry, , 08-15, Volume: 24, Issue:16, 2016
Design, Synthesis, and Biological Evaluation of Novel Imidazo[1,2-a]pyridine Derivatives as Potent c-Met Inhibitors.ACS medicinal chemistry letters, , May-14, Volume: 6, Issue:5, 2015
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
Development of Dual Inhibitors Targeting Epidermal Growth Factor Receptor in Cancer Therapy.Journal of medicinal chemistry, , 04-14, Volume: 65, Issue:7, 2022
Synthesis and biological evaluation of new MET inhibitors with 1,6-naphthyridinone scaffold.European journal of medicinal chemistry, , Jan-01, Volume: 185, 2020
2,7-naphthyridinone-based MET kinase inhibitors: A promising novel scaffold for antitumor drug development.European journal of medicinal chemistry, , Sep-15, Volume: 178, 2019
Structural and Molecular Insight into Resistance Mechanisms of First Generation cMET Inhibitors.ACS medicinal chemistry letters, , Sep-12, Volume: 10, Issue:9, 2019
Synthesis and evaluation of a series of pyridine and pyrimidine derivatives as type II c-Met inhibitors.Bioorganic & medicinal chemistry, , 06-15, Volume: 25, Issue:12, 2017
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Recent advances in the development of dual VEGFR and c-Met small molecule inhibitors as anticancer drugs.European journal of medicinal chemistry, , Jan-27, Volume: 108, 2016
Design, synthesis and biological evaluation of c-Met kinase inhibitors bearing 2-oxo-1,2-dihydroquinoline scaffold.Bioorganic & medicinal chemistry letters, , 09-15, Volume: 26, Issue:18, 2016
Design and biological evaluation of novel 4-(2-fluorophenoxy)quinoline derivatives bearing an imidazolone moiety as c-Met kinase inhibitors.Bioorganic & medicinal chemistry, , Aug-01, Volume: 23, Issue:15, 2015
Discovery of novel type II c-Met inhibitors based on BMS-777607.European journal of medicinal chemistry, , Jun-10, Volume: 80, 2014
Discovery and Biological Evaluation of Novel Dual EGFR/c-Met Inhibitors.ACS medicinal chemistry letters, , Apr-10, Volume: 5, Issue:4, 2014
Combined SVM-based and docking-based virtual screening for retrieving novel inhibitors of c-Met.European journal of medicinal chemistry, , Volume: 46, Issue:9, 2011
Discovery of N-(4-(2-amino-3-chloropyridin-4-yloxy)-3-fluorophenyl)-4-ethoxy-1-(4-fluorophenyl)-2-oxo-1,2-dihydropyridine-3-carboxamide (BMS-777607), a selective and orally efficacious inhibitor of the Met kinase superfamily.Journal of medicinal chemistry, , Mar-12, Volume: 52, Issue:5, 2009
[no title available],
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Targeting gain of function and resistance mutations in Abl and KIT by hybrid compound design.Journal of medicinal chemistry, , Jul-25, Volume: 56, Issue:14, 2013
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Discovery of imidazopyridine derivatives as novel c-Met kinase inhibitors: Synthesis, SAR study, and biological activity.Bioorganic chemistry, , Volume: 70, 2017
Recent advances in the development of dual VEGFR and c-Met small molecule inhibitors as anticancer drugs.European journal of medicinal chemistry, , Jan-27, Volume: 108, 2016
Discovery of potent and selective 8-fluorotriazolopyridine c-Met inhibitors.Journal of medicinal chemistry, , Mar-12, Volume: 58, Issue:5, 2015
Combined SVM-based and docking-based virtual screening for retrieving novel inhibitors of c-Met.European journal of medicinal chemistry, , Volume: 46, Issue:9, 2011
Discovery and optimization of potent and selective triazolopyridazine series of c-Met inhibitors.Bioorganic & medicinal chemistry letters, , Nov-15, Volume: 19, Issue:22, 2009
Discovery and optimization of triazolopyridazines as potent and selective inhibitors of the c-Met kinase.Journal of medicinal chemistry, , May-22, Volume: 51, Issue:10, 2008
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).Blood, , Oct-01, Volume: 114, Issue:14, 2009
Combined SVM-based and docking-based virtual screening for retrieving novel inhibitors of c-Met.European journal of medicinal chemistry, , Volume: 46, Issue:9, 2011
N-(3-fluoro-4-(2-arylthieno[3,2-b]pyridin-7-yloxy)phenyl)-2-oxo-3-phenylimidazolidine-1-carboxamides: a novel series of dual c-Met/VEGFR2 receptor tyrosine kinase inhibitors.Bioorganic & medicinal chemistry letters, , Mar-01, Volume: 19, Issue:5, 2009
N-(4-(6,7-Disubstituted-quinolin-4-yloxy)-3-fluorophenyl)-2-oxo-3-phenylimidazolidine-1-carboxamides: a novel series of dual c-Met/VEGFR2 receptor tyrosine kinase inhibitors.Bioorganic & medicinal chemistry letters, , Dec-01, Volume: 19, Issue:23, 2009
Discovery of a novel and potent series of thieno[3,2-b]pyridine-based inhibitors of c-Met and VEGFR2 tyrosine kinases.Bioorganic & medicinal chemistry letters, , May-01, Volume: 18, Issue:9, 2008
[no title available]Journal of medicinal chemistry, , 11-24, Volume: 65, Issue:22, 2022
Design, synthesis and biological evaluation of novel 2,4-diaryl pyrimidine derivatives as selective EGFREuropean journal of medicinal chemistry, , Feb-15, Volume: 212, 2021
Structure-guided design and development of novel N-phenylpyrimidin-2-amine derivatives as potential c-Met inhibitors.European journal of medicinal chemistry, , Nov-05, Volume: 223, 2021
Discovery of Novel c-Mesenchymal-Epithelia transition factor and histone deacetylase dual inhibitors.European journal of medicinal chemistry, , Oct-15, Volume: 204, 2020
Design, synthesis and biological evaluation of novel c-Met/HDAC dual inhibitors.Bioorganic & medicinal chemistry letters, , 12-01, Volume: 30, Issue:23, 2020
Discovery of novel pyrrolo[2,3-b]pyridine derivatives bearing 4-oxoquinoline moiety as potential antitumor inhibitor.Bioorganic & medicinal chemistry letters, , 01-15, Volume: 30, Issue:2, 2020
Structure-activity relationship study of novel quinazoline-based 1,6-naphthyridinones as MET inhibitors with potent antitumor efficacy.European journal of medicinal chemistry, , Dec-15, Volume: 208, 2020
Discovery of 1,6-naphthyridinone-based MET kinase inhibitor bearing quinoline moiety as promising antitumor drug candidate.European journal of medicinal chemistry, , Apr-15, Volume: 192, 2020
Structure based designing of triazolopyrimidone-based reversible inhibitors for kinases involved in NSCLC.Bioorganic & medicinal chemistry letters, , 07-01, Volume: 29, Issue:13, 2019
Identification of novel NEuropean journal of medicinal chemistry, , Feb-25, Volume: 146, 2018
Exploration of novel pyrrolo[2,1-f][1,2,4]triazine derivatives with improved anticancer efficacy as dual inhibitors of c-Met/VEGFR-2.European journal of medicinal chemistry, , Oct-05, Volume: 158, 2018
Discovery of novel 2-substituted-4-(2-fluorophenoxy) pyridine derivatives possessing pyrazolone and triazole moieties as dual c-Met/VEGFR-2 receptor tyrosine kinase inhibitors.Bioorganic chemistry, , Volume: 72, 2017
Synthesis and evaluation of a series of pyridine and pyrimidine derivatives as type II c-Met inhibitors.Bioorganic & medicinal chemistry, , 06-15, Volume: 25, Issue:12, 2017
Design, synthesis, and biological evaluation of thieno[2,3-d]pyrimidine derivatives as novel dual c-Met and VEGFR-2 kinase inhibitors.Bioorganic & medicinal chemistry, , 12-15, Volume: 25, Issue:24, 2017
Structure-based design, synthesis, and evaluation of 4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine derivatives as novel c-Met inhibitors.European journal of medicinal chemistry, , Sep-29, Volume: 138, 2017
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Design, synthesis and biological evaluation of 4-aminopyrimidine-5-cabaldehyde oximes as dual inhibitors of c-Met and VEGFR-2.Bioorganic & medicinal chemistry, , 08-15, Volume: 24, Issue:16, 2016
The "Cyclopropyl Fragment" is a Versatile Player that Frequently Appears in Preclinical/Clinical Drug Molecules.Journal of medicinal chemistry, , 10-13, Volume: 59, Issue:19, 2016
Recent advances in the development of dual VEGFR and c-Met small molecule inhibitors as anticancer drugs.European journal of medicinal chemistry, , Jan-27, Volume: 108, 2016
Discovery and SAR study of c-Met kinase inhibitors bearing an 3-amino-benzo[d]isoxazole or 3-aminoindazole scaffold.Bioorganic & medicinal chemistry, , Feb-01, Volume: 23, Issue:3, 2015
Design and biological evaluation of novel 4-(2-fluorophenoxy)quinoline derivatives bearing an imidazolone moiety as c-Met kinase inhibitors.Bioorganic & medicinal chemistry, , Aug-01, Volume: 23, Issue:15, 2015
Design, synthesis and evaluation of highly selective pyridone-based class II MET inhibitors.Bioorganic & medicinal chemistry letters, , Aug-01, Volume: 24, Issue:15, 2014
Design, synthesis and structure-activity relationships of novel 4-phenoxyquinoline derivatives containing pyridazinone moiety as potential antitumor agents.European journal of medicinal chemistry, , Aug-18, Volume: 83, 2014
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Discovery of Entrectinib: A New 3-Aminoindazole As a Potent Anaplastic Lymphoma Kinase (ALK), c-ros Oncogene 1 Kinase (ROS1), and Pan-Tropomyosin Receptor Kinases (Pan-TRKs) inhibitor.Journal of medicinal chemistry, , Apr-14, Volume: 59, Issue:7, 2016
Discovery of acyl ureas as highly selective small molecule CSF1R kinase inhibitors.Bioorganic & medicinal chemistry letters, , 10-15, Volume: 74, 2022
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
[no title available]Journal of medicinal chemistry, , 11-24, Volume: 65, Issue:22, 2022
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Recent advances in the development of dual VEGFR and c-Met small molecule inhibitors as anticancer drugs.European journal of medicinal chemistry, , Jan-27, Volume: 108, 2016
Identification and optimization of pyridazinones as potent and selective c-Met kinase inhibitors.Bioorganic & medicinal chemistry letters, , Apr-01, Volume: 25, Issue:7, 2015
Medulloblastoma drugs in development: Current leads, trials and drawbacks.European journal of medicinal chemistry, , Apr-05, Volume: 215, 2021
Design, synthesis and biological evaluation of novel N-sulfonylamidine-based derivatives as c-Met inhibitors via Cu-catalyzed three-component reaction.European journal of medicinal chemistry, , Aug-15, Volume: 200, 2020
Design, synthesis and biological evaluation of novel c-Met/HDAC dual inhibitors.Bioorganic & medicinal chemistry letters, , 12-01, Volume: 30, Issue:23, 2020
Structure-based discovery of novel 4-(2-fluorophenoxy)quinoline derivatives as c-Met inhibitors using isocyanide-involved multicomponent reactions.European journal of medicinal chemistry, , May-01, Volume: 193, 2020
Design, synthesis and biological evaluation of novel N-[4-(2-fluorophenoxy)pyridin-2-yl]cyclopropanecarboxamide derivatives as potential c-Met kinase inhibitors.European journal of medicinal chemistry, , May-15, Volume: 194, 2020
Design, synthesis, and biological evaluation of 4-phenoxyquinoline derivatives as potent c-Met kinase inhibitor.Bioorganic & medicinal chemistry letters, , 12-01, Volume: 29, Issue:23, 2019
1,2,3-Triazole-containing hybrids as potential anticancer agents: Current developments, action mechanisms and structure-activity relationships.European journal of medicinal chemistry, , Dec-01, Volume: 183, 2019
1,2,3-Triazole-containing hybrids as leads in medicinal chemistry: A recent overview.Bioorganic & medicinal chemistry, , 08-15, Volume: 27, Issue:16, 2019
Design, synthesis and evaluation of sulfonylurea-containing 4-phenoxyquinolines as highly selective c-Met kinase inhibitors.Bioorganic & medicinal chemistry, , 07-01, Volume: 27, Issue:13, 2019
Structural and Molecular Insight into Resistance Mechanisms of First Generation cMET Inhibitors.ACS medicinal chemistry letters, , Sep-12, Volume: 10, Issue:9, 2019
Synthesis and antiproliferative activity of 6,7-disubstituted-4-phenoxyquinoline derivatives bearing the 1,8-naphthyridin-2-one moiety.European journal of medicinal chemistry, , Oct-05, Volume: 158, 2018
Synthesis and bioevaluation study of novel N-methylpicolinamide and thienopyrimidine derivatives as selectivity c-Met kinase inhibitors.Bioorganic & medicinal chemistry, , 01-01, Volume: 26, Issue:1, 2018
[no title available]Bioorganic & medicinal chemistry letters, , 02-01, Volume: 28, Issue:3, 2018
Synthesis and bioevaluation and doking study of 1H-pyrrolo[2,3-b]pyridine derivatives bearing aromatic hydrazone moiety as c-Met inhibitors.European journal of medicinal chemistry, , Feb-10, Volume: 145, 2018
[no title available]European journal of medicinal chemistry, , Jan-01, Volume: 143, 2018
Exploration of novel pyrrolo[2,1-f][1,2,4]triazine derivatives with improved anticancer efficacy as dual inhibitors of c-Met/VEGFR-2.European journal of medicinal chemistry, , Oct-05, Volume: 158, 2018
Discovery of novel 7-azaindole derivatives bearing dihydropyridazine moiety as c-Met kinase inhibitors.European journal of medicinal chemistry, , Jun-16, Volume: 133, 2017
Discovery of novel pyrrolo-pyridine/pyrimidine derivatives bearing pyridazinone moiety as c-Met kinase inhibitors.European journal of medicinal chemistry, , Dec-01, Volume: 141, 2017
Dual MET and SMO Negative Modulators Overcome Resistance to EGFR Inhibitors in Human Nonsmall Cell Lung Cancer.Journal of medicinal chemistry, , 09-14, Volume: 60, Issue:17, 2017
Design, synthesis and biological evaluation of novel 4-(2-fluorophenoxy)quinoline derivatives as selective c-Met inhibitors.Bioorganic & medicinal chemistry, , 02-01, Volume: 25, Issue:3, 2017
Design, synthesis and biological evaluation of novel 4-phenoxyquinoline derivatives containing 3-oxo-3,4-dihydroquinoxaline moiety as c-Met kinase inhibitors.Bioorganic & medicinal chemistry, , 08-15, Volume: 25, Issue:16, 2017
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Recent advances in the development of dual VEGFR and c-Met small molecule inhibitors as anticancer drugs.European journal of medicinal chemistry, , Jan-27, Volume: 108, 2016
Discovery of a novel 6,7-disubstituted-4-(2-fluorophenoxy)quinolines bearing 1,2,3-triazole-4-carboxamide moiety as potent c-Met kinase inhibitors.European journal of medicinal chemistry, , Aug-25, Volume: 119, 2016
The "Cyclopropyl Fragment" is a Versatile Player that Frequently Appears in Preclinical/Clinical Drug Molecules.Journal of medicinal chemistry, , 10-13, Volume: 59, Issue:19, 2016
AXL Inhibitors in Cancer: A Medicinal Chemistry Perspective.Journal of medicinal chemistry, , 04-28, Volume: 59, Issue:8, 2016
Design, synthesis and structure-activity relationships of novel 4-phenoxyquinoline derivatives containing 1,2,4-triazolone moiety as c-Met kinase inhibitors.European journal of medicinal chemistry, , Nov-10, Volume: 123, 2016
Design, synthesis and biological evaluation of 4-aminopyrimidine-5-cabaldehyde oximes as dual inhibitors of c-Met and VEGFR-2.Bioorganic & medicinal chemistry, , 08-15, Volume: 24, Issue:16, 2016
Synthesis, and docking studies of phenylpyrimidine-carboxamide derivatives bearing 1H-pyrrolo[2,3-b]pyridine moiety as c-Met inhibitors.Bioorganic & medicinal chemistry, , Apr-15, Volume: 24, Issue:8, 2016
Design, synthesis, and docking studies of phenylpicolinamide derivatives bearing 1H-pyrrolo[2,3-b]pyridine moiety as c-Met inhibitors.Bioorganic & medicinal chemistry, , Feb-15, Volume: 24, Issue:4, 2016
Design, synthesis and biological evaluation of c-Met kinase inhibitors bearing 2-oxo-1,2-dihydroquinoline scaffold.Bioorganic & medicinal chemistry letters, , 09-15, Volume: 26, Issue:18, 2016
Synthesis and antiproliferative activity of 6,7-disubstituted-4-phenoxyquinoline derivatives bearing the 2-oxo-4-chloro-1,2-dihydroquinoline-3-carboxamide moiety.Bioorganic & medicinal chemistry letters, , Apr-01, Volume: 26, Issue:7, 2016
Discovery of novel pyrrolo[2,3-b]pyridine derivatives bearing 1,2,3-triazole moiety as c-Met kinase inhibitors.Bioorganic & medicinal chemistry letters, , Apr-01, Volume: 26, Issue:7, 2016
Design, synthesis and biological evaluation of novel 4-phenoxy-6,7-disubstituted quinolines possessing (thio)semicarbazones as c-Met kinase inhibitors.Bioorganic & medicinal chemistry, , Mar-15, Volume: 24, Issue:6, 2016
Synthesis and biological evaluation of 4-(2-fluorophenoxy)-3,3'-bipyridine derivatives as potential c-met inhibitors.European journal of medicinal chemistry, , Sep-14, Volume: 120, 2016
Synthesis and biological evaluation of new pyrazol-4-ylpyrimidine derivatives as potential ROS1 kinase inhibitors.European journal of medicinal chemistry, , Jan-27, Volume: 90, 2015
Design and biological evaluation of novel 4-(2-fluorophenoxy)quinoline derivatives bearing an imidazolone moiety as c-Met kinase inhibitors.Bioorganic & medicinal chemistry, , Aug-01, Volume: 23, Issue:15, 2015
Design, synthesis and pharmacological evaluation of 6,7-disubstituted-4-phenoxyquinoline derivatives as potential antitumor agents.Bioorganic chemistry, , Volume: 57, 2014
Design and optimization of novel 4-(2-fluorophenoxy)quinoline derivatives bearing a hydrazone moiety as c-Met kinase inhibitors.European journal of medicinal chemistry, , Nov-24, Volume: 87, 2014
Design, synthesis and biological evaluation of novel 6,7-disubstituted-4-phenoxyquinoline derivatives bearing 4-oxo-3,4-dihydrophthalazine-1-carboxamide moieties as c-Met kinase inhibitors.Bioorganic & medicinal chemistry, , Jul-15, Volume: 22, Issue:14, 2014
Discovery of novel type II c-Met inhibitors based on BMS-777607.European journal of medicinal chemistry, , Jun-10, Volume: 80, 2014
Discovery andw biological evaluation of novel 6,7-disubstituted-4-(2-fluorophenoxy)quinoline derivatives possessing 1,2,3-triazole-4-carboxamide moiety as c-Met kinase inhibitors.Bioorganic & medicinal chemistry, , Nov-15, Volume: 22, Issue:22, 2014
Design, synthesis and structure-activity relationships of novel 4-phenoxyquinoline derivatives containing pyridazinone moiety as potential antitumor agents.European journal of medicinal chemistry, , Aug-18, Volume: 83, 2014
Discovery of novel 6,7-disubstituted-4-phenoxyquinoline derivatives bearing 5-(aminomethylene)pyrimidine-2,4,6-trione moiety as c-Met kinase inhibitors.Bioorganic & medicinal chemistry, , Feb-15, Volume: 22, Issue:4, 2014
Discovery and optimization of novel 4-phenoxy-6,7-disubstituted quinolines possessing semicarbazones as c-Met kinase inhibitors.Bioorganic & medicinal chemistry, , Sep-01, Volume: 21, Issue:17, 2013
Discovery of novel 4-(2-fluorophenoxy)quinoline derivatives bearing 4-oxo-1,4-dihydrocinnoline-3-carboxamide moiety as c-Met kinase inhibitors.Bioorganic & medicinal chemistry, , Jun-01, Volume: 21, Issue:11, 2013
Design, synthesis and antitumour activity of bisquinoline derivatives connected by 4-oxy-3-fluoroaniline moiety.European journal of medicinal chemistry, , Volume: 64, 2013
Design, synthesis, and structure-activity relationships of novel 6,7-disubstituted-4-phenoxyquinoline derivatives as potential antitumor agents.European journal of medicinal chemistry, , Volume: 69, 2013
Vascular endothelial growth factor (VEGF) receptors: drugs and new inhibitors.Journal of medicinal chemistry, , Dec-27, Volume: 55, Issue:24, 2012
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Recent advances in the development of dual VEGFR and c-Met small molecule inhibitors as anticancer drugs.European journal of medicinal chemistry, , Jan-27, Volume: 108, 2016
Discovery of 1-[3-(1-methyl-1H-pyrazol-4-yl)-5-oxo-5H-benzo[4,5]cyclohepta[1,2-b]pyridin-7-yl]-N-(pyridin-2-ylmethyl)methanesulfonamide (MK-8033): A Specific c-Met/Ron dual kinase inhibitor with preferential affinity for the activated state of c-Met.Journal of medicinal chemistry, , Mar-28, Volume: 56, Issue:6, 2013
Combined SVM-based and docking-based virtual screening for retrieving novel inhibitors of c-Met.European journal of medicinal chemistry, , Volume: 46, Issue:9, 2011
Discovery, synthesis, and investigation of the antitumor activity of novel piperazinylpyrimidine derivatives.European journal of medicinal chemistry, , Volume: 46, Issue:6, 2011
Discovery of a 5H-benzo[4,5]cyclohepta[1,2-b]pyridin-5-one (MK-2461) inhibitor of c-Met kinase for the treatment of cancer.Journal of medicinal chemistry, , Jun-23, Volume: 54, Issue:12, 2011
Insights into Current Tropomyosin Receptor Kinase (TRK) Inhibitors: Development and Clinical Application.Journal of medicinal chemistry, , 02-28, Volume: 62, Issue:4, 2019
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Discovery of 1-[3-(1-methyl-1H-pyrazol-4-yl)-5-oxo-5H-benzo[4,5]cyclohepta[1,2-b]pyridin-7-yl]-N-(pyridin-2-ylmethyl)methanesulfonamide (MK-8033): A Specific c-Met/Ron dual kinase inhibitor with preferential affinity for the activated state of c-Met.Journal of medicinal chemistry, , Mar-28, Volume: 56, Issue:6, 2013
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Optimization of 6,6-dimethyl pyrrolo[3,4-c]pyrazoles: Identification of PHA-793887, a potent CDK inhibitor suitable for intravenous dosing.Bioorganic & medicinal chemistry, , Mar-01, Volume: 18, Issue:5, 2010
AXL Inhibitors in Cancer: A Medicinal Chemistry Perspective.Journal of medicinal chemistry, , 04-28, Volume: 59, Issue:8, 2016
4-Oxo-1,4-dihydroquinoline-3-carboxamide Derivatives as New Axl Kinase Inhibitors.Journal of medicinal chemistry, , 07-28, Volume: 59, Issue:14, 2016
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Recent advances in the development of dual VEGFR and c-Met small molecule inhibitors as anticancer drugs.European journal of medicinal chemistry, , Jan-27, Volume: 108, 2016
Discovery of 6-(difluoro(6-(4-fluorophenyl)-[1,2,4]triazolo[4,3-b][1,2,4]triazin-3-yl)methyl)quinoline as a highly potent and selective c-Met inhibitor.European journal of medicinal chemistry, , Jun-30, Volume: 116, 2016
Design, Synthesis, and Biological Evaluation of Novel Imidazo[1,2-a]pyridine Derivatives as Potent c-Met Inhibitors.ACS medicinal chemistry letters, , May-14, Volume: 6, Issue:5, 2015
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Design and synthesis of a highly selective, orally active and potent anaplastic lymphoma kinase inhibitor (CH5424802).Bioorganic & medicinal chemistry, , Feb-01, Volume: 20, Issue:3, 2012
Insights into Current Tropomyosin Receptor Kinase (TRK) Inhibitors: Development and Clinical Application.Journal of medicinal chemistry, , 02-28, Volume: 62, Issue:4, 2019
Exploration of novel pyrrolo[2,1-f][1,2,4]triazine derivatives with improved anticancer efficacy as dual inhibitors of c-Met/VEGFR-2.European journal of medicinal chemistry, , Oct-05, Volume: 158, 2018
The "Cyclopropyl Fragment" is a Versatile Player that Frequently Appears in Preclinical/Clinical Drug Molecules.Journal of medicinal chemistry, , 10-13, Volume: 59, Issue:19, 2016
Non-kinase targets of protein kinase inhibitors.Nature reviews. Drug discovery, , Volume: 16, Issue:6, 2017
Structure based drug design of crizotinib (PF-02341066), a potent and selective dual inhibitor of mesenchymal-epithelial transition factor (c-MET) kinase and anaplastic lymphoma kinase (ALK).Journal of medicinal chemistry, , Sep-22, Volume: 54, Issue:18, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Identification of 1-(3-(6,7-dimethoxyquinazolin-4-yloxy)phenyl)-3-(5-(1,1,1-trifluoro-2-methylpropan-2-yl)isoxazol-3-yl)urea hydrochloride (CEP-32496), a highly potent and orally efficacious inhibitor of V-RAF murine sarcoma viral oncogene homologue B1 (BJournal of medicinal chemistry, , Feb-09, Volume: 55, Issue:3, 2012
Fragment-based modification of 2,4-diarylaminopyrimidine derivatives as ALK and ROS1 dual inhibitors to overcome secondary mutants.Bioorganic & medicinal chemistry, , 10-15, Volume: 28, Issue:20, 2020
An exploration of solvent-front region high affinity moiety leading to novel potent ALK & ROS1 dual inhibitors with mutant-combating effects.Bioorganic & medicinal chemistry, , 10-15, Volume: 27, Issue:20, 2019
Discovery of novel 2,4-diarylaminopyrimidine analogues as ALK and ROS1 dual inhibitors to overcome crizotinib-resistant mutants including G1202R.European journal of medicinal chemistry, , Jan-01, Volume: 143, 2018
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Design, synthesis and biological evaluation of novel 4-arylaminopyrimidine derivatives possessing a hydrazone moiety as dual inhibitors of L1196M ALK and ROS1.European journal of medicinal chemistry, , Nov-10, Volume: 123, 2016
Synthesis, structure-activity relationships, and in vivo efficacy of the novel potent and selective anaplastic lymphoma kinase (ALK) inhibitor 5-chloro-N2-(2-isopropoxy-5-methyl-4-(piperidin-4-yl)phenyl)-N4-(2-(isopropylsulfonyl)phenyl)pyrimidine-2,4-diamJournal of medicinal chemistry, , Jul-25, Volume: 56, Issue:14, 2013
Structural and Molecular Insight into Resistance Mechanisms of First Generation cMET Inhibitors.ACS medicinal chemistry letters, , Sep-12, Volume: 10, Issue:9, 2019
Discovery of (S)-1-(1-(Imidazo[1,2-a]pyridin-6-yl)ethyl)-6-(1-methyl-1H-pyrazol-4-yl)-1H-[1,2,3]triazolo[4,5-b]pyrazine (volitinib) as a highly potent and selective mesenchymal-epithelial transition factor (c-Met) inhibitor in clinical development for treJournal of medicinal chemistry, , Sep-25, Volume: 57, Issue:18, 2014
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Targeting gain of function and resistance mutations in Abl and KIT by hybrid compound design.Journal of medicinal chemistry, , Jul-25, Volume: 56, Issue:14, 2013
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
Enables
This protein enables 8 target(s):
| Target | Category | Definition |
|---|
| protein tyrosine kinase activity | molecular function | Catalysis of the reaction: ATP + a protein tyrosine = ADP + protein tyrosine phosphate. [RHEA:10596] |
| protein binding | molecular function | Binding to a protein. [GOC:go_curators] |
| ATP binding | molecular function | Binding to ATP, adenosine 5'-triphosphate, a universally important coenzyme and enzyme regulator. [ISBN:0198506732] |
| semaphorin receptor activity | molecular function | Combining with a semaphorin, and transmitting the signal from one side of the membrane to the other to initiate a change in cell activity. [GOC:mah, GOC:signaling, PMID:15239958] |
| protein phosphatase binding | molecular function | Binding to a protein phosphatase. [GOC:jl] |
| identical protein binding | molecular function | Binding to an identical protein or proteins. [GOC:jl] |
| molecular function activator activity | molecular function | A molecular function regulator that activates or increases the activity of its target via non-covalent binding that does not result in covalent modification to the target. [GOC:curators] |
| hepatocyte growth factor receptor activity | molecular function | Combining with hepatocyte growth factor receptor ligand and transmitting the signal across the plasma membrane to initiate a change in cell activity. [GOC:mah] |
Located In
This protein is located in 6 target(s):
| Target | Category | Definition |
|---|
| extracellular region | cellular component | The space external to the outermost structure of a cell. For cells without external protective or external encapsulating structures this refers to space outside of the plasma membrane. This term covers the host cell environment outside an intracellular parasite. [GOC:go_curators] |
| plasma membrane | cellular component | The membrane surrounding a cell that separates the cell from its external environment. It consists of a phospholipid bilayer and associated proteins. [ISBN:0716731363] |
| basal plasma membrane | cellular component | The region of the plasma membrane located at the basal end of the cell. Often used in reference to animal polarized epithelial membranes, where the basal membrane is the part attached to the extracellular matrix, or in plant cells, where the basal membrane is defined with respect to the zygotic axis. [GOC:go_curators] |
| cell surface | cellular component | The external part of the cell wall and/or plasma membrane. [GOC:jl, GOC:mtg_sensu, GOC:sm] |
| membrane | cellular component | A lipid bilayer along with all the proteins and protein complexes embedded in it and attached to it. [GOC:dos, GOC:mah, ISBN:0815316194] |
| postsynapse | cellular component | The part of a synapse that is part of the post-synaptic cell. [GOC:dos] |
Active In
This protein is active in 2 target(s):
| Target | Category | Definition |
|---|
| basal plasma membrane | cellular component | The region of the plasma membrane located at the basal end of the cell. Often used in reference to animal polarized epithelial membranes, where the basal membrane is the part attached to the extracellular matrix, or in plant cells, where the basal membrane is defined with respect to the zygotic axis. [GOC:go_curators] |
| plasma membrane | cellular component | The membrane surrounding a cell that separates the cell from its external environment. It consists of a phospholipid bilayer and associated proteins. [ISBN:0716731363] |
Part Of
This protein is part of 1 target(s):
| Target | Category | Definition |
|---|
| receptor complex | cellular component | Any protein complex that undergoes combination with a hormone, neurotransmitter, drug or intracellular messenger to initiate a change in cell function. [GOC:go_curators] |
Involved In
This protein is involved in 27 target(s):
| Target | Category | Definition |
|---|
| endothelial cell morphogenesis | biological process | The change in form (cell shape and size) that occurs during the differentiation of an endothelial cell. [GOC:ascb_2009, GOC:dph, GOC:tb] |
| signal transduction | biological process | The cellular process in which a signal is conveyed to trigger a change in the activity or state of a cell. Signal transduction begins with reception of a signal (e.g. a ligand binding to a receptor or receptor activation by a stimulus such as light), or for signal transduction in the absence of ligand, signal-withdrawal or the activity of a constitutively active receptor. Signal transduction ends with regulation of a downstream cellular process, e.g. regulation of transcription or regulation of a metabolic process. Signal transduction covers signaling from receptors located on the surface of the cell and signaling via molecules located within the cell. For signaling between cells, signal transduction is restricted to events at and within the receiving cell. [GOC:go_curators, GOC:mtg_signaling_feb11] |
| cell surface receptor signaling pathway | biological process | The series of molecular signals initiated by an extracellular ligand binding to a receptor located on the cell surface. The pathway ends with regulation of a downstream cellular process, e.g. transcription. [GOC:signaling] |
| negative regulation of autophagy | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of autophagy. Autophagy is the process in which cells digest parts of their own cytoplasm. [GOC:dph, GOC:tb] |
| positive regulation of microtubule polymerization | biological process | Any process that activates or increases the frequency, rate or extent of microtubule polymerization. [GOC:mah] |
| negative regulation of Rho protein signal transduction | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of Rho protein signal transduction. [GOC:bf] |
| positive regulation of transcription by RNA polymerase II | biological process | Any process that activates or increases the frequency, rate or extent of transcription from an RNA polymerase II promoter. [GOC:go_curators, GOC:txnOH] |
| hepatocyte growth factor receptor signaling pathway | biological process | The series of molecular signals initiated by a ligand binding to a hepatocyte growth factor receptor, and ending with the regulation of a downstream cellular process, e.g. transcription. [GOC:ceb] |
| branching morphogenesis of an epithelial tube | biological process | The process in which the anatomical structures of branches in an epithelial tube are generated and organized. A tube is a long hollow cylinder. [GOC:dgh, GOC:dph, GOC:jid] |
| positive chemotaxis | biological process | The directed movement of a motile cell or organism towards a higher concentration of a chemical. [GOC:ai, GOC:bf, GOC:isa_complete] |
| negative regulation of stress fiber assembly | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of the assembly a stress fiber, a bundle of microfilaments and other proteins found in fibroblasts. [GOC:ai] |
| excitatory postsynaptic potential | biological process | A process that leads to a temporary increase in postsynaptic potential due to the flow of positively charged ions into the postsynaptic cell. The flow of ions that causes an EPSP is an excitatory postsynaptic current (EPSC) and makes it easier for the neuron to fire an action potential. [GOC:dph, GOC:ef] |
| establishment of skin barrier | biological process | Establishment of the epithelial barrier, the functional barrier in the skin that limits its permeability. [GOC:dph] |
| negative regulation of thrombin-activated receptor signaling pathway | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of thrombin-activated receptor protein signaling pathway activity. A thrombin receptor signaling pathway is the series of molecular signals generated as a consequence of a thrombin-activated receptor binding to one of its physiological ligands. [GOC:mah] |
| semaphorin-plexin signaling pathway | biological process | The series of molecular signals generated as a consequence of a semaphorin receptor (composed of a plexin and a neurophilin) binding to a semaphorin ligand. [GOC:BHF, GOC:mah, GOC:vk, PMID:15239959] |
| negative regulation of hydrogen peroxide-mediated programmed cell death | biological process | Any process that stops, prevents or reduces the frequency, rate or extent of hydrogen peroxide-mediated programmed cell death. [GOC:BHF, GOC:TermGenie] |
| negative regulation of guanyl-nucleotide exchange factor activity | biological process | Any process that stops, prevents or reduces the frequency, rate or extent of guanyl-nucleotide exchange factor activity. [GO_REF:0000059, GOC:TermGenie, PMID:20484009] |
| positive regulation of endothelial cell chemotaxis | biological process | Any process that activates or increases the frequency, rate or extent of endothelial cell chemotaxis. [GOC:BHF] |
| liver development | biological process | The process whose specific outcome is the progression of the liver over time, from its formation to the mature structure. The liver is an exocrine gland which secretes bile and functions in metabolism of protein and carbohydrate and fat, synthesizes substances involved in the clotting of the blood, synthesizes vitamin A, detoxifies poisonous substances, stores glycogen, and breaks down worn-out erythrocytes. [GOC:add, ISBN:068340007X] |
| cell surface receptor protein tyrosine kinase signaling pathway | biological process | The series of molecular signals initiated by an extracellular ligand binding to a receptor on the surface of the target cell where the receptor possesses tyrosine kinase activity, and ending with the regulation of a downstream cellular process, e.g. transcription. [GOC:ceb, GOC:signaling] |
| phagocytosis | biological process | A vesicle-mediated transport process that results in the engulfment of external particulate material by phagocytes and their delivery to the lysosome. The particles are initially contained within phagocytic vacuoles (phagosomes), which then fuse with primary lysosomes to effect digestion of the particles. [ISBN:0198506732] |
| multicellular organism development | biological process | The biological process whose specific outcome is the progression of a multicellular organism over time from an initial condition (e.g. a zygote or a young adult) to a later condition (e.g. a multicellular animal or an aged adult). [GOC:dph, GOC:ems, GOC:isa_complete, GOC:tb] |
| neuron differentiation | biological process | The process in which a relatively unspecialized cell acquires specialized features of a neuron. [GOC:mah] |
| positive regulation of kinase activity | biological process | Any process that activates or increases the frequency, rate or extent of kinase activity, the catalysis of the transfer of a phosphate group, usually from ATP, to a substrate molecule. [GOC:mah] |
| cell migration | biological process | The controlled self-propelled movement of a cell from one site to a destination guided by molecular cues. [GOC:cjm, GOC:dph, GOC:ems, GOC:pf, Wikipedia:Cell_migration] |
| pancreas development | biological process | The process whose specific outcome is the progression of the pancreas over time, from its formation to the mature structure. The pancreas is an endoderm derived structure that produces precursors of digestive enzymes and blood glucose regulating hormones. [GOC:cvs] |
| nervous system development | biological process | The process whose specific outcome is the progression of nervous tissue over time, from its formation to its mature state. [GOC:dgh] |