Proteins > Vascular endothelial growth factor receptor 2
Page last updated: 2024-08-07 16:35:10
Vascular endothelial growth factor receptor 2
A vascular endothelial growth factor receptor 2 that is encoded in the genome of human. [PRO:WCB, UniProtKB:P35968]
Synonyms
VEGFR-2;
EC 2.7.10.1;
Fetal liver kinase 1;
FLK-1;
Kinase insert domain receptor;
KDR;
Protein-tyrosine kinase receptor flk-1
Research
Bioassay Publications (409)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 2 (0.49) | 18.2507 |
| 2000's | 115 (28.12) | 29.6817 |
| 2010's | 243 (59.41) | 24.3611 |
| 2020's | 49 (11.98) | 2.80 |
Compounds (220)
Drugs with Inhibition Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| pd 173074 | Homo sapiens (human) | IC50 | 0.1325 | 4 | 4 |
| ag 1295 | Homo sapiens (human) | IC50 | 6.2000 | 2 | 2 |
| indirubin-5-sulfonate | Homo sapiens (human) | IC50 | 6.8000 | 1 | 6 |
| 4-(4'-hydroxyphenyl)-amino-6,7-dimethoxyquinazoline | Homo sapiens (human) | IC50 | 2.8000 | 1 | 1 |
| nsc 664704 | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
| mebendazole | Homo sapiens (human) | IC50 | 5.5667 | 3 | 3 |
| niclosamide | Homo sapiens (human) | IC50 | 23.1000 | 1 | 1 |
| olomoucine | Homo sapiens (human) | IC50 | 7.0000 | 1 | 1 |
| papaverine | Homo sapiens (human) | IC50 | 24.3300 | 1 | 1 |
| pd 153035 | Homo sapiens (human) | IC50 | 3.8963 | 3 | 3 |
| imatinib | Homo sapiens (human) | GI50 | 10.0000 | 3 | 3 |
| imatinib | Homo sapiens (human) | IC50 | 25.7465 | 4 | 4 |
| vorinostat | Homo sapiens (human) | IC50 | 10.0000 | 3 | 3 |
| whi p180 | Homo sapiens (human) | IC50 | 1.3811 | 7 | 9 |
| galantamine | Homo sapiens (human) | IC50 | 0.5900 | 1 | 1 |
| indirubin | Homo sapiens (human) | IC50 | 2.0000 | 1 | 1 |
| staurosporine | Homo sapiens (human) | IC50 | 0.9925 | 32 | 36 |
| staurosporine | Homo sapiens (human) | Ki | 0.0017 | 1 | 1 |
| delphinidin | Homo sapiens (human) | IC50 | 0.0051 | 1 | 1 |
| gefitinib | Homo sapiens (human) | IC50 | 7.9248 | 6 | 6 |
| ptk 787 | Homo sapiens (human) | IC50 | 0.0330 | 4 | 4 |
| vatalanib | Homo sapiens (human) | IC50 | 0.3780 | 38 | 41 |
| birb 796 | Homo sapiens (human) | IC50 | 0.3400 | 1 | 1 |
| Serotonin hydrochloride | Homo sapiens (human) | IC50 | 50.0000 | 1 | 1 |
| erlotinib | Homo sapiens (human) | IC50 | 53.9199 | 14 | 14 |
| lapatinib | Homo sapiens (human) | IC50 | 105.0000 | 2 | 2 |
| sorafenib | Homo sapiens (human) | IC50 | 0.1000 | 79 | 85 |
| sorafenib | Homo sapiens (human) | Ki | 0.0074 | 3 | 3 |
| papaverinol | Homo sapiens (human) | IC50 | 10.7300 | 1 | 1 |
| nexavar | Homo sapiens (human) | IC50 | 0.0143 | 3 | 3 |
| hematoxylin | Homo sapiens (human) | IC50 | 2.1000 | 1 | 1 |
| purvalanol b | Homo sapiens (human) | IC50 | 0.0060 | 1 | 1 |
| N-(3-cyano-4,5,6,7-tetrahydro-1-benzothiophen-2-yl)-1-naphthalenecarboxamide | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| 3,3-dimethyl-5-oxo-5-[(3-phenyl-1H-pyrazol-5-yl)amino]pentanoic acid | Homo sapiens (human) | IC50 | 47.0000 | 1 | 1 |
| sf 2370 | Homo sapiens (human) | IC50 | 0.0430 | 2 | 2 |
| tandutinib | Homo sapiens (human) | IC50 | 16.0350 | 2 | 2 |
| vx-745 | Homo sapiens (human) | IC50 | 5.0000 | 1 | 1 |
| dasatinib | Homo sapiens (human) | IC50 | 18.1200 | 3 | 3 |
| zd 6474 | Homo sapiens (human) | IC50 | 0.5425 | 49 | 53 |
| gtp 14564 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| quercetin | Homo sapiens (human) | IC50 | 0.9700 | 2 | 2 |
| norlichexanthone | Homo sapiens (human) | IC50 | 11.7000 | 1 | 1 |
| ellagic acid | Homo sapiens (human) | IC50 | 0.7900 | 1 | 1 |
| astrogorgiadiol | Homo sapiens (human) | IC50 | 4.3500 | 1 | 1 |
| alvocidib | Homo sapiens (human) | IC50 | 0.4000 | 1 | 1 |
| su 5402 | Homo sapiens (human) | IC50 | 15.1321 | 7 | 14 |
| su 9516 | Homo sapiens (human) | IC50 | 5.8740 | 2 | 5 |
| ag 183 | Homo sapiens (human) | IC50 | 4.3000 | 1 | 1 |
| cb676475 | Homo sapiens (human) | IC50 | 1.9500 | 4 | 6 |
| semaxinib | Homo sapiens (human) | IC50 | 13.4181 | 37 | 44 |
| orantinib | Homo sapiens (human) | IC50 | 10.8373 | 8 | 13 |
| su 11248 | Homo sapiens (human) | GI50 | 0.0330 | 1 | 1 |
| su 11248 | Homo sapiens (human) | IC50 | 3.7676 | 57 | 59 |
| su 11248 | Homo sapiens (human) | Ki | 0.0075 | 4 | 4 |
| su 11652 | Homo sapiens (human) | IC50 | 3.8752 | 4 | 6 |
| palladia | Homo sapiens (human) | IC50 | 6.0050 | 2 | 4 |
| su9518 | Homo sapiens (human) | IC50 | 17.6067 | 3 | 6 |
| n,n'-dimethyl-n,n'-bis(mercaptoacetyl)hydrazine | Homo sapiens (human) | IC50 | 1.4810 | 6 | 8 |
| 6-(4-methoxyphenyl)-3-(3-thiophenyl)pyrazolo[1,5-a]pyrimidine | Homo sapiens (human) | IC50 | 0.1479 | 7 | 7 |
| m475271 | Homo sapiens (human) | IC50 | 0.4060 | 4 | 5 |
| jnj-7706621 | Homo sapiens (human) | IC50 | 0.1300 | 1 | 1 |
| 2-tert-butyl-9-fluoro-3,6-dihydro-7h-benz(h)imidazo(4,5-f)isoquinoline-7-one | Homo sapiens (human) | IC50 | 1.4000 | 1 | 1 |
| 4,5-diphenyl-2,3-dihydro-1H-pyrazolo[3,4-c]pyridazin-3-one | Homo sapiens (human) | IC50 | 50.0000 | 1 | 1 |
| su 1498 | Homo sapiens (human) | IC50 | 0.7000 | 1 | 1 |
| 2-((4-pyridyl)methyl)amino-n-(3-(trifluoromethyl)phenyl)benzamide | Homo sapiens (human) | IC50 | 0.0506 | 25 | 26 |
| cyc 116 | Homo sapiens (human) | IC50 | 0.0690 | 1 | 1 |
| cyc 116 | Homo sapiens (human) | Ki | 0.0440 | 1 | 1 |
| ekb 569 | Homo sapiens (human) | IC50 | 6.5655 | 2 | 2 |
| axitinib | Homo sapiens (human) | IC50 | 0.0079 | 5 | 5 |
| axitinib | Homo sapiens (human) | Ki | 0.0038 | 1 | 0 |
| a 419259 | Homo sapiens (human) | IC50 | 2.0881 | 3 | 7 |
| gdp 366 | Homo sapiens (human) | IC50 | 0.0746 | 7 | 10 |
| b 43 | Homo sapiens (human) | IC50 | 2.5267 | 3 | 3 |
| a 770041 | Homo sapiens (human) | IC50 | 50.0000 | 1 | 1 |
| krn 633 | Homo sapiens (human) | IC50 | 0.0805 | 2 | 2 |
| jnj 10198409 | Homo sapiens (human) | IC50 | 3.1000 | 1 | 1 |
| telatinib | Homo sapiens (human) | IC50 | 0.0060 | 3 | 3 |
| cp 547632 | Homo sapiens (human) | IC50 | 0.0093 | 3 | 3 |
| lenvatinib | Homo sapiens (human) | IC50 | 0.0035 | 7 | 7 |
| gw843682x | Homo sapiens (human) | IC50 | 0.3600 | 2 | 1 |
| midostaurin | Homo sapiens (human) | IC50 | 0.2500 | 1 | 1 |
| ki23057 | Homo sapiens (human) | IC50 | 0.0760 | 2 | 2 |
| sb-505124 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| osi 930 | Homo sapiens (human) | IC50 | 0.0070 | 2 | 2 |
| 3,5-bis(2-fluorobenzylidene)piperidin-4-one | Homo sapiens (human) | IC50 | 0.7700 | 1 | 1 |
| ct52923 | Homo sapiens (human) | IC50 | 17.3000 | 1 | 1 |
| tivozanib | Homo sapiens (human) | IC50 | 0.0782 | 5 | 8 |
| hki 272 | Homo sapiens (human) | IC50 | 5.4291 | 2 | 2 |
| 3,9-bis((ethylthio)methyl)-k-252a | Homo sapiens (human) | IC50 | 0.0430 | 1 | 1 |
| cediranib | Homo sapiens (human) | IC50 | 0.0016 | 4 | 4 |
| chir 99021 | Homo sapiens (human) | IC50 | 5.0000 | 1 | 1 |
| ly2090314 | Homo sapiens (human) | IC50 | 20.0000 | 1 | 1 |
| ly-2157299 | Homo sapiens (human) | IC50 | 0.4420 | 1 | 1 |
| pazopanib | Homo sapiens (human) | IC50 | 0.4929 | 12 | 14 |
| bibw 2992 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| sotrastaurin | Homo sapiens (human) | IC50 | 3.9000 | 1 | 1 |
| aee 788 | Homo sapiens (human) | IC50 | 0.0770 | 1 | 1 |
| saracatinib | Homo sapiens (human) | IC50 | 15.7007 | 3 | 4 |
| exel-7647 | Homo sapiens (human) | IC50 | 0.0500 | 1 | 0 |
| pha 665752 | Homo sapiens (human) | IC50 | 0.5315 | 2 | 2 |
| l 783277 | Homo sapiens (human) | GI50 | 0.1400 | 1 | 1 |
| l 783277 | Homo sapiens (human) | IC50 | 0.0171 | 4 | 4 |
| regorafenib | Homo sapiens (human) | GI50 | 0.1140 | 1 | 1 |
| regorafenib | Homo sapiens (human) | IC50 | 0.0043 | 5 | 5 |
| calpain inhibitor iii | Homo sapiens (human) | IC50 | 0.1000 | 1 | 1 |
| brivanib | Homo sapiens (human) | IC50 | 0.0255 | 4 | 4 |
| brivanib | Homo sapiens (human) | Ki | 0.0260 | 1 | 1 |
| ki 8751 | Homo sapiens (human) | IC50 | 0.8016 | 3 | 3 |
| verubulin | Homo sapiens (human) | IC50 | 0.0084 | 1 | 1 |
| danusertib | Homo sapiens (human) | IC50 | 0.4320 | 1 | 1 |
| nvp-aew541 | Homo sapiens (human) | IC50 | 7.1000 | 2 | 2 |
| abt 869 | Homo sapiens (human) | IC50 | 0.0312 | 15 | 20 |
| azd2932 | Homo sapiens (human) | GI50 | 0.0930 | 1 | 1 |
| azd2932 | Homo sapiens (human) | IC50 | 0.0080 | 1 | 1 |
| dorsomorphin | Homo sapiens (human) | IC50 | 1.6305 | 4 | 7 |
| gw 2580 | Homo sapiens (human) | IC50 | 20.0000 | 1 | 1 |
| tak 285 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| crizotinib | Homo sapiens (human) | IC50 | 7.7500 | 4 | 4 |
| 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 |
| chir-265 | Homo sapiens (human) | IC50 | 0.6600 | 2 | 2 |
| motesanib | Homo sapiens (human) | IC50 | 0.7987 | 5 | 15 |
| in 1130 | Homo sapiens (human) | IC50 | 2.4400 | 1 | 1 |
| 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 | 0.5176 | 2 | 5 |
| tg100801 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| azd 1152-hqpa | Homo sapiens (human) | Ki | 1.8000 | 1 | 1 |
| nvp-tae684 | Homo sapiens (human) | IC50 | 2.1230 | 1 | 1 |
| enmd 2076 | Homo sapiens (human) | IC50 | 0.0230 | 2 | 2 |
| 4-methyl-3-(2-(2-morpholinoethylamino)quinazolin-6-yl)-n-(3-(trifluoromethyl)phenyl)benzamide | Homo sapiens (human) | IC50 | 0.0010 | 1 | 1 |
| e 7050 | Homo sapiens (human) | IC50 | 0.0240 | 3 | 3 |
| famitinib | Homo sapiens (human) | IC50 | 0.0035 | 2 | 2 |
| pha 848125 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| amg 1 | Homo sapiens (human) | IC50 | 0.9210 | 1 | 1 |
| amg 1 | Homo sapiens (human) | Ki | 0.8707 | 3 | 4 |
| zm323881 | Homo sapiens (human) | IC50 | 0.0020 | 1 | 1 |
| plx 4720 | Homo sapiens (human) | IC50 | 1.3575 | 1 | 4 |
| cudc 101 | Homo sapiens (human) | IC50 | 0.8490 | 1 | 1 |
| amg 458 | Homo sapiens (human) | IC50 | 0.8450 | 2 | 2 |
| amg 458 | Homo sapiens (human) | Ki | 1.0646 | 3 | 10 |
| tak 593 | Homo sapiens (human) | IC50 | 0.0008 | 4 | 4 |
| bms 777607 | Homo sapiens (human) | IC50 | 0.1635 | 5 | 4 |
| ponatinib | Homo sapiens (human) | IC50 | 0.0053 | 8 | 8 |
| N-cyclopropyl-3-{4-[(cyclopropylmethyl)carbamoyl]phenyl}-4-methylbenzamide | Homo sapiens (human) | IC50 | 20.0000 | 1 | 1 |
| quizartinib | Homo sapiens (human) | IC50 | 3.6200 | 3 | 3 |
| N-[[3-fluoro-4-[[2-(1-methyl-4-imidazolyl)-7-thieno[3,2-b]pyridinyl]oxy]anilino]-sulfanylidenemethyl]-2-phenylacetamide | Homo sapiens (human) | IC50 | 0.0185 | 5 | 6 |
| PP121 | Homo sapiens (human) | IC50 | 0.0217 | 3 | 3 |
| lucitanib | Homo sapiens (human) | IC50 | 0.0250 | 3 | 3 |
| cabozantinib | Homo sapiens (human) | GI50 | 0.0030 | 1 | 1 |
| cabozantinib | Homo sapiens (human) | IC50 | 0.3151 | 24 | 25 |
| defactinib | Homo sapiens (human) | IC50 | 0.2732 | 1 | 1 |
| entrectinib | Homo sapiens (human) | IC50 | 1.0000 | 1 | 1 |
| sch 1473759 | Homo sapiens (human) | IC50 | 0.0010 | 1 | 1 |
| pexidartinib | Homo sapiens (human) | IC50 | 1.5000 | 2 | 2 |
| ldn 193189 | Homo sapiens (human) | IC50 | 0.4314 | 2 | 5 |
| n-methyl-4-(4-(3-(trifluoromethyl)benzamido)phenoxy)picolinamide | Homo sapiens (human) | IC50 | 0.4600 | 1 | 1 |
| plx4032 | Homo sapiens (human) | IC50 | 0.3600 | 1 | 1 |
| gsk 1363089 | Homo sapiens (human) | IC50 | 0.1234 | 18 | 25 |
| mk 2461 | Homo sapiens (human) | IC50 | 0.0440 | 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 | 0.0300 | 1 | 1 |
| ml347 | Homo sapiens (human) | IC50 | 19.7000 | 1 | 1 |
| apatinib | Homo sapiens (human) | IC50 | 0.0010 | 1 | 1 |
| bay 1000394 | Homo sapiens (human) | IC50 | 0.1630 | 2 | 2 |
| pha 793887 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| abt-348 | Homo sapiens (human) | IC50 | 0.0028 | 4 | 4 |
| tak-632 | Homo sapiens (human) | IC50 | 0.1600 | 1 | 1 |
| gsk 2334470 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| 3-((4-(6-methylpyridin-2-yl)-5-(quinolin-6-yl)-1h-imidazol-2-yl)methyl)benzamide | Homo sapiens (human) | IC50 | 2.2000 | 1 | 1 |
| ly2874455 | Homo sapiens (human) | IC50 | 0.0064 | 2 | 2 |
| nms p937 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| alectinib | Homo sapiens (human) | IC50 | 1.4000 | 2 | 2 |
| nms-p118 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| DMH1 | Homo sapiens (human) | IC50 | 0.1079 | 1 | 1 |
| azd4547 | Homo sapiens (human) | IC50 | 0.0383 | 6 | 6 |
| chir 98014 | Homo sapiens (human) | IC50 | 2.0000 | 1 | 1 |
| dcc-2701 | Homo sapiens (human) | IC50 | 0.0092 | 2 | 2 |
| ew-7197 | Homo sapiens (human) | IC50 | 0.0970 | 1 | 1 |
| cep-32496 | Homo sapiens (human) | IC50 | 0.0300 | 2 | 2 |
| ceritinib | Homo sapiens (human) | IC50 | 4.2100 | 1 | 1 |
| ldn-212854 | Homo sapiens (human) | IC50 | 2.0400 | 1 | 1 |
| debio 1347 | Homo sapiens (human) | IC50 | 2.1000 | 2 | 2 |
| pf-543 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| erdafitinib | Homo sapiens (human) | IC50 | 2.2405 | 6 | 3 |
| sar131675 | Homo sapiens (human) | GI50 | 4.6000 | 1 | 1 |
| sar131675 | Homo sapiens (human) | IC50 | 0.0670 | 1 | 1 |
| sklb1002 | Homo sapiens (human) | IC50 | 0.0320 | 1 | 1 |
| ly3009120 | Homo sapiens (human) | IC50 | 3.9000 | 1 | 1 |
| azd3759 | Homo sapiens (human) | IC50 | 0.1560 | 1 | 1 |
| at 9283 | Homo sapiens (human) | IC50 | 0.0100 | 1 | 1 |
| chir 258 | Homo sapiens (human) | IC50 | 0.0303 | 3 | 3 |
| r 1530 | Homo sapiens (human) | IC50 | 0.0100 | 2 | 2 |
| nintedanib | Homo sapiens (human) | IC50 | 0.0090 | 9 | 9 |
| bms 536924 | Homo sapiens (human) | IC50 | 1.4000 | 1 | 1 |
| pf-477736 | Homo sapiens (human) | IC50 | 0.0080 | 1 | 0 |
| pp242 | Homo sapiens (human) | IC50 | 2.5011 | 2 | 9 |
| nms-e973 | Homo sapiens (human) | IC50 | 0.0100 | 1 | 1 |
Drugs with Activation Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| pd 173074 | Homo sapiens (human) | EC50 | 0.2500 | 1 | 1 |
| sb 202190 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| imatinib | Homo sapiens (human) | Kd | 10.0000 | 2 | 2 |
| staurosporine | Homo sapiens (human) | Kd | 0.2367 | 3 | 3 |
| gefitinib | Homo sapiens (human) | Kd | 10.0000 | 2 | 2 |
| lestaurtinib | Homo sapiens (human) | Kd | 0.2200 | 2 | 2 |
| vatalanib | Homo sapiens (human) | Kd | 0.0647 | 3 | 3 |
| ruboxistaurin | Homo sapiens (human) | Kd | 10.0000 | 2 | 2 |
| canertinib | Homo sapiens (human) | Kd | 10.0000 | 2 | 2 |
| birb 796 | Homo sapiens (human) | Kd | 3.6667 | 3 | 3 |
| cyc 202 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| sb 203580 | Homo sapiens (human) | Kd | 10.0000 | 2 | 2 |
| enzastaurin | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| erlotinib | Homo sapiens (human) | Kd | 7.8500 | 2 | 2 |
| lapatinib | Homo sapiens (human) | Kd | 10.0000 | 2 | 2 |
| sorafenib | Homo sapiens (human) | EC50 | 0.5000 | 1 | 1 |
| sorafenib | Homo sapiens (human) | Kd | 0.0660 | 6 | 6 |
| pd 173955 | Homo sapiens (human) | Kd | 0.6900 | 1 | 1 |
| s 1033 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| bms 387032 | Homo sapiens (human) | Kd | 10.0000 | 2 | 2 |
| tandutinib | Homo sapiens (human) | Kd | 10.0000 | 3 | 3 |
| vx-745 | Homo sapiens (human) | Kd | 10.0000 | 2 | 2 |
| dasatinib | Homo sapiens (human) | Kd | 6.4500 | 2 | 2 |
| zd 6474 | Homo sapiens (human) | Kd | 0.7033 | 3 | 3 |
| 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 |
| alvocidib | Homo sapiens (human) | Kd | 10.0000 | 2 | 2 |
| bosutinib | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| su 11248 | Homo sapiens (human) | Kd | 0.0058 | 6 | 6 |
| jnj-7706621 | Homo sapiens (human) | Kd | 3.7000 | 1 | 1 |
| vx680 | Homo sapiens (human) | Kd | 2.0000 | 2 | 2 |
| ekb 569 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| axitinib | Homo sapiens (human) | Kd | 0.0059 | 1 | 1 |
| pd 184352 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| bms345541 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| lenvatinib | Homo sapiens (human) | Kd | 0.0021 | 1 | 1 |
| midostaurin | Homo sapiens (human) | Kd | 3.2000 | 3 | 3 |
| ki 20227 | Homo sapiens (human) | Kd | 0.0180 | 1 | 1 |
| cp 724714 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| pi103 | Homo sapiens (human) | Kd | 10.0000 | 2 | 2 |
| hki 272 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| tofacitinib | Homo sapiens (human) | Kd | 10.0000 | 2 | 2 |
| n-(6-chloro-7-methoxy-9h-beta-carbolin-8-yl)-2-methylnicotinamide | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| cediranib | Homo sapiens (human) | Kd | 0.0011 | 1 | 1 |
| masitinib | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| pazopanib | Homo sapiens (human) | Kd | 0.0140 | 2 | 2 |
| azd 6244 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| su 14813 | Homo sapiens (human) | Kd | 0.0023 | 2 | 2 |
| bibw 2992 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| tg100-115 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| pha 665752 | Homo sapiens (human) | EC50 | 2.5000 | 1 | 1 |
| pha 665752 | Homo sapiens (human) | Kd | 10.0000 | 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) | EC50 | 0.0360 | 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 | 0.0400 | 1 | 1 |
| brivanib | Homo sapiens (human) | Kd | 0.0050 | 1 | 1 |
| at 7519 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| bi 2536 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| nvp-ast487 | Homo sapiens (human) | Kd | 0.2000 | 2 | 2 |
| kw 2449 | Homo sapiens (human) | Kd | 0.1200 | 1 | 1 |
| abt 869 | Homo sapiens (human) | Kd | 0.0081 | 2 | 2 |
| gw 2580 | Homo sapiens (human) | Kd | 10.0000 | 2 | 2 |
| crizotinib | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| chir-265 | Homo sapiens (human) | Kd | 1.3000 | 2 | 2 |
| motesanib | Homo sapiens (human) | Kd | 0.0260 | 2 | 2 |
| mln8054 | Homo sapiens (human) | Kd | 10.0000 | 2 | 2 |
| GDC-0879 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| gsk 461364 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| azd 1152-hqpa | Homo sapiens (human) | Kd | 0.5000 | 2 | 2 |
| nvp-tae684 | Homo sapiens (human) | EC50 | 1.0000 | 1 | 1 |
| nvp-tae684 | Homo sapiens (human) | Kd | 0.9400 | 1 | 1 |
| fedratinib | Homo sapiens (human) | Kd | 5.2000 | 1 | 1 |
| gsk690693 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| gdc 0941 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| plx 4720 | Homo sapiens (human) | Kd | 2.1000 | 1 | 1 |
| sgx 523 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| quizartinib | Homo sapiens (human) | Kd | 0.0870 | 3 | 3 |
| incb-018424 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| gsk 1838705a | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| gsk 1363089 | Homo sapiens (human) | Kd | 0.0120 | 1 | 1 |
| cep-32496 | Homo sapiens (human) | Kd | 0.0080 | 2 | 2 |
| gs-9973 | Homo sapiens (human) | EC50 | 1.0000 | 1 | 1 |
| chir 258 | Homo sapiens (human) | EC50 | 0.0460 | 1 | 1 |
| chir 258 | Homo sapiens (human) | Kd | 0.0680 | 2 | 2 |
| nintedanib | Homo sapiens (human) | Kd | 0.0029 | 1 | 1 |
| pp242 | Homo sapiens (human) | Kd | 1.2000 | 1 | 1 |
Drugs with Other Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| ptk 787 | Homo sapiens (human) | ED50 | 0.0340 | 1 | 1 |
| sorafenib | Homo sapiens (human) | INH | 100.0000 | 1 | 1 |
| semaxinib | Homo sapiens (human) | ED50 | 0.9300 | 1 | 1 |
| brivanib | Homo sapiens (human) | Activity | 0.0400 | 1 | 1 |
| ponatinib | Homo sapiens (human) | INH | 0.0017 | 1 | 1 |
| cabozantinib | Homo sapiens (human) | INH | 0.0070 | 1 | 1 |
| gsk 1363089 | Homo sapiens (human) | INH | 0.0008 | 1 | 1 |
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Functionalized quinoxalinones as privileged structures with broad-ranging pharmacological activities.European journal of medicinal chemistry, , Feb-05, Volume: 229, 2022
Targeting Rearranged during Transfection in Cancer: A Perspective on Small-Molecule Inhibitors and Their Clinical Development.Journal of medicinal chemistry, , 08-26, Volume: 64, Issue:16, 2021
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[no title available]Journal of medicinal chemistry, , 11-11, Volume: 64, Issue:21, 2021
[no title available]Journal of medicinal chemistry, , 08-26, Volume: 64, Issue:16, 2021
Novel 4-(piperazin-1-yl)quinolin-2(1H)-one bearing thiazoles with antiproliferative activity through VEGFR-2-TK inhibition.Bioorganic & medicinal chemistry, , 06-15, Volume: 40, 2021
Design, synthesis and biological evaluation of novel 2-(4-(1H-indazol-6-yl)-1H-pyrazol-1-yl)acetamide derivatives as potent VEGFR-2 inhibitors.European journal of medicinal chemistry, , Mar-05, Volume: 213, 2021
Discovery of novel VEGFR-2 inhibitors embedding 6,7-dimethoxyquinazoline and diarylamide fragments.Bioorganic & medicinal chemistry letters, , 03-15, Volume: 36, 2021
Design, synthesis, biological evaluation, and modeling studies of novel conformationally-restricted analogues of sorafenib as selective kinase-inhibitory antiproliferative agents against hepatocellular carcinoma cells.European journal of medicinal chemistry, , Jan-15, Volume: 210, 2021
Pyridazine as a privileged structure: An updated review on anticancer activity of pyridazine containing bioactive molecules.European journal of medicinal chemistry, , Jan-01, Volume: 209, 2021
Effect of phenylurea hydroxamic acids on histone deacetylase and VEGFR-2.Bioorganic & medicinal chemistry, , 11-15, Volume: 50, 2021
Exploration of carbamide derived pyrimidine-thioindole conjugates as potential VEGFR-2 inhibitors with anti-angiogenesis effect.European journal of medicinal chemistry, , Aug-15, Volume: 200, 2020
1,2,3-Triazole-Chalcone hybrids: Synthesis, in vitro cytotoxic activity and mechanistic investigation of apoptosis induction in multiple myeloma RPMI-8226.European journal of medicinal chemistry, , Mar-01, Volume: 189, 2020
New series of isoxazole derivatives targeting EGFR-TK: Synthesis, molecular modeling and antitumor evaluation.Bioorganic & medicinal chemistry, , 11-01, Volume: 28, Issue:21, 2020
Discovery of novel anti-angiogenesis agents. Part 9: Multiplex inhibitors suppressing compensatory activations of RTKs.European journal of medicinal chemistry, , Feb-15, Volume: 164, 2019
Design, synthesis and in vitro evaluation of 6-amide-2-aryl benzoxazole/benzimidazole derivatives against tumor cells by inhibiting VEGFR-2 kinase.European journal of medicinal chemistry, , Oct-01, Volume: 179, 2019
Enhancement of the tail hydrophobic interactions within the carbonic anhydrase IX active site via structural extension: Design and synthesis of novel N-substituted isatins-SLC-0111 hybrids as carbonic anhydrase inhibitors and antitumor agents.European journal of medicinal chemistry, , Jan-15, Volume: 162, 2019
Discovery of arylamide-5-anilinoquinazoline-8-nitro derivatives as VEGFR-2 kinase inhibitors: Synthesis, in vitro biological evaluation and molecular docking.Bioorganic & medicinal chemistry letters, , 12-01, Volume: 29, Issue:23, 2019
The association between anti-tumor potency and structure-activity of protein-kinases inhibitors based on quinazoline molecular skeleton.Bioorganic & medicinal chemistry, , 02-01, Volume: 27, Issue:3, 2019
Novel promising 4-anilinoquinazoline-based derivatives as multi-target RTKs inhibitors: Design, molecular docking, synthesis, and antitumor activities in vitro and vivo.Bioorganic & medicinal chemistry, , 10-15, Volume: 27, Issue:20, 2019
Coumarin-containing hybrids and their anticancer activities.European journal of medicinal chemistry, , Nov-01, Volume: 181, 2019
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
Type IIA - Type IIB protein tyrosine kinase inhibitors hybridization as an efficient approach for potent multikinase inhibitor development: Design, synthesis, anti-proliferative activity, multikinase inhibitory activity and molecular modeling of novel indEuropean journal of medicinal chemistry, , Feb-01, Volume: 163, 2019
Novel potent substituted 4-amino-2-thiopyrimidines as dual VEGFR-2 and BRAF kinase inhibitors.European journal of medicinal chemistry, , Oct-01, Volume: 179, 2019
Discovery of novel anti-angiogenesis agents. Part 10: Multi-target inhibitors of VEGFR-2, Tie-2 and EphB4 incorporated with 1,2,3-triazol.European journal of medicinal chemistry, , Feb-01, Volume: 163, 2019
Discovery of novel picolinamide-based derivatives as novel VEGFR-2 kinase inhibitors: synthesis, MedChemComm, , Jun-01, Volume: 9, Issue:6, 2018
Novel thioureido-benzenesulfonamide derivatives with enaminone linker as potent anticancer, radiosensitizers and VEGFR2 inhibitors.Bioorganic & medicinal chemistry letters, , 05-15, Volume: 28, Issue:9, 2018
[no title available]European journal of medicinal chemistry, , Jul-15, Volume: 155, 2018
Design and discovery of thioether and nicotinamide containing sorafenib analogues as multikinase inhibitors targeting B-Raf, B-RafBioorganic & medicinal chemistry, , 05-15, Volume: 26, Issue:9, 2018
[no title available]European journal of medicinal chemistry, , Jan-01, Volume: 143, 2018
Synthesis and anticancer activity of new dihydropyrimidinone derivatives.European journal of medicinal chemistry, , Aug-05, Volume: 156, 2018
Cyclin-Dependent Kinase 8: A New Hope in Targeted Cancer Therapy?Journal of medicinal chemistry, , 06-28, Volume: 61, Issue:12, 2018
Discovery of Novel Potent VEGFR-2 Inhibitors Exerting Significant Antiproliferative Activity against Cancer Cell Lines.Journal of medicinal chemistry, , 01-11, Volume: 61, Issue:1, 2018
Discovery of novel anti-angiogenesis agents. Part 6: Multi-targeted RTK inhibitors.European journal of medicinal chemistry, , Feb-15, Volume: 127, 2017
Design, synthesis, molecular docking and cytotoxic evaluation of novel 2-furybenzimidazoles as VEGFR-2 inhibitors.European journal of medicinal chemistry, , Aug-18, Volume: 136, 2017
Discovery of novel anti-angiogenesis agents. Part 8: Diaryl thiourea bearing 1H-indazole-3-amine as multi-target RTKs inhibitors.European journal of medicinal chemistry, , Dec-01, Volume: 141, 2017
Discovery of novel anti-angiogenesis agents. Part 7: Multitarget inhibitors of VEGFR-2, TIE-2 and EphB4.European journal of medicinal chemistry, , Dec-01, Volume: 141, 2017
Design, synthesis and antitumor activity of Novel Sorafenib derivatives bearing pyrazole scaffold.Bioorganic & medicinal chemistry, , 10-15, Volume: 25, Issue:20, 2017
[no title available]Bioorganic & medicinal chemistry, , 12-01, Volume: 24, Issue:23, 2016
[no title available]Bioorganic & medicinal chemistry letters, , 11-15, Volume: 26, Issue:22, 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
Expanding the structural diversity of diarylureas as multi-target tyrosine kinase inhibitors.Bioorganic & medicinal chemistry, , Feb-15, Volume: 24, Issue:4, 2016
Increasing the binding affinity of VEGFR-2 inhibitors by extending their hydrophobic interaction with the active site: Design, synthesis and biological evaluation of 1-substituted-4-(4-methoxybenzyl)phthalazine derivatives.European journal of medicinal chemistry, , May-04, Volume: 113, 2016
Design and discovery of 4-anilinoquinazoline-acylamino derivatives as EGFR and VEGFR-2 dual TK inhibitors.European journal of medicinal chemistry, , Feb-15, Volume: 109, 2016
1-Piperazinylphthalazines as potential VEGFR-2 inhibitors and anticancer agents: Synthesis and in vitro biological evaluation.European journal of medicinal chemistry, , Jan-01, Volume: 107, 2016
Combination of 4-anilinoquinazoline, arylurea and tertiary amine moiety to discover novel anticancer agents.Bioorganic & medicinal chemistry, , Jan-15, Volume: 24, Issue:2, 2016
5-Benzylidene-2,4-thiazolidenedione derivatives: Design, synthesis and evaluation as inhibitors of angiogenesis targeting VEGR-2.Bioorganic chemistry, , Volume: 67, 2016
LEADOPT: an automatic tool for structure-based lead optimization, and its application in structural optimizations of VEGFR2 and SYK inhibitors.European journal of medicinal chemistry, , Mar-26, Volume: 93, 2015
Distinct binding mode of multikinase inhibitor lenvatinib revealed by biochemical characterization.ACS medicinal chemistry letters, , Jan-08, Volume: 6, Issue:1, 2015
Design, synthesis and evaluation of novel 2-(1H-imidazol-2-yl) pyridine Sorafenib derivatives as potential BRAF inhibitors and anti-tumor agents.European journal of medicinal chemistry, , Jan-27, Volume: 90, 2015
Synthesis, antiangiogenesis evaluation and molecular docking studies of 1-aryl-3-[(thieno[3,2-b]pyridin-7-ylthio)phenyl]ureas: Discovery of a new substitution pattern for type II VEGFR-2 Tyr kinase inhibitors.Bioorganic & medicinal chemistry, , Oct-01, Volume: 23, Issue:19, 2015
Identification of a potent 5-phenyl-thiazol-2-ylamine-based inhibitor of FLT3 with activity against drug resistance-conferring point mutations.European journal of medicinal chemistry, , Jul-15, Volume: 100, 2015
Discovery of biphenyl-based VEGFR-2 inhibitors. Part 3: design, synthesis and 3D-QSAR studies.Bioorganic & medicinal chemistry, , Mar-01, Volume: 23, Issue:5, 2015
Indoline ureas as potential anti-hepatocellular carcinoma agents targeting VEGFR-2: Synthesis, in vitro biological evaluation and molecular docking.European journal of medicinal chemistry, , Jul-15, Volume: 100, 2015
Discovery of biphenyl-aryl ureas as novel VEGFR-2 inhibitors. Part 4: exploration of diverse hinge-binding fragments.Bioorganic & medicinal chemistry, , Jul-01, Volume: 23, Issue:13, 2015
Discovery of novel VEGFR-2 inhibitors. Part 5: Exploration of diverse hinge-binding fragments via core-refining approach.European journal of medicinal chemistry, , Oct-20, Volume: 103, 2015
Biphenyl derivatives incorporating urea unit as novel VEGFR-2 inhibitors: design, synthesis and biological evaluation.Bioorganic & medicinal chemistry, , Jan-01, Volume: 22, Issue:1, 2014
Discovery of 3-phenyl-1H-5-pyrazolylamine derivatives containing a urea pharmacophore as potent and efficacious inhibitors of FMS-like tyrosine kinase-3 (FLT3).Bioorganic & medicinal chemistry, , Jun-01, Volume: 21, Issue:11, 2013
Structure-activity relationship studies of pyrazolo[3,4-d]pyrimidine derivatives leading to the discovery of a novel multikinase inhibitor that potently inhibits FLT3 and VEGFR2 and evaluation of its activity against acute myeloid leukemia in vitro and inJournal of medicinal chemistry, , Feb-28, Volume: 56, Issue:4, 2013
A new target for an old drug: identifying mitoxantrone as a nanomolar inhibitor of PIM1 kinase via kinome-wide selectivity modeling.Journal of medicinal chemistry, , Mar-28, Volume: 56, Issue:6, 2013
Novel VEGFR-2 kinase inhibitors identified by the back-to-front approach.Bioorganic & medicinal chemistry letters, , May-15, Volume: 23, Issue:10, 2013
3-Phenyl-1H-5-pyrazolylamine-based derivatives as potent and efficacious inhibitors of FMS-like tyrosine kinase-3 (FLT3).Bioorganic & medicinal chemistry letters, , Jul-15, Volume: 22, Issue:14, 2012
Life beyond kinases: structure-based discovery of sorafenib as nanomolar antagonist of 5-HT receptors.Journal of medicinal chemistry, , Jun-28, Volume: 55, Issue:12, 2012
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
Discovery and evaluation of 3-phenyl-1H-5-pyrazolylamine-based derivatives as potent, selective and efficacious inhibitors of FMS-like tyrosine kinase-3 (FLT3).Bioorganic & medicinal chemistry, , Jul-15, Volume: 19, Issue:14, 2011
Biochemical characterization of a novel type-II VEGFR2 kinase inhibitor: comparison of binding to non-phosphorylated and phosphorylated VEGFR2.Bioorganic & medicinal chemistry, , Sep-15, Volume: 19, Issue:18, 2011
Selectively nonselective kinase inhibition: striking the right balance.Journal of medicinal chemistry, , Feb-25, Volume: 53, Issue:4, 2010
Synthesis and structure-activity relationship of 6-arylureido-3-pyrrol-2-ylmethylideneindolin-2-one derivatives as potent receptor tyrosine kinase inhibitors.Bioorganic & medicinal chemistry, , Jul-01, Volume: 18, Issue:13, 2010
Pharmacophore modeling and virtual screening studies for new VEGFR-2 kinase inhibitors.European journal of medicinal chemistry, , Volume: 45, Issue:11, 2010
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
Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases.Nature chemical biology, , Volume: 4, Issue:11, 2008
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
Rational design of inhibitors that bind to inactive kinase conformations.Nature chemical biology, , Volume: 2, Issue:7, 2006
A small molecule-kinase interaction map for clinical kinase inhibitors.Nature biotechnology, , Volume: 23, Issue:3, 2005
BAY 43-9006 exhibits broad spectrum oral antitumor activity and targets the RAF/MEK/ERK pathway and receptor tyrosine kinases involved in tumor progression and angiogenesis.Cancer research, , Oct-01, Volume: 64, Issue:19, 2004
Quinoides and VEGFR2 TKIs influence the fate of hepatocellular carcinoma and its cancer stem cells.MedChemComm, , Jan-01, Volume: 8, Issue:1, 2017
A development of chimeric VEGFR2 TK inhibitor based on two ligand conformers from PDB: 1Y6A complex--medicinal chemistry consequences of a TKs analysis.European journal of medicinal chemistry, , Jan-24, Volume: 72, 2014
2-Anilino-4-(benzimidazol-2-yl)pyrimidines--a multikinase inhibitor scaffold with antiproliferative activity toward cancer cell lines.European journal of medicinal chemistry, , Volume: 53, 2012
N-(3-Cyano-4,5,6,7-tetrahydro-1-benzothien-2-yl)amides as potent, selective, inhibitors of JNK2 and JNK3.Bioorganic & medicinal chemistry letters, , Mar-01, Volume: 17, Issue:5, 2007
Synthesis, modeling, and in vitro activity of (3'S)-epi-K-252a analogues. Elucidating the stereochemical requirements of the 3'-sugar alcohol on trkA tyrosine kinase activity.Journal of medicinal chemistry, , Jun-02, Volume: 48, Issue:11, 2005
Synthesis and kinase inhibitory activity of 3'-(S)-epi-K-252a.Bioorganic & medicinal chemistry letters, , Oct-21, Volume: 12, Issue:20, 2002
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
Synthesis and structure-activity relationship of 6-arylureido-3-pyrrol-2-ylmethylideneindolin-2-one derivatives as potent receptor tyrosine kinase inhibitors.Bioorganic & medicinal chemistry, , Jul-01, Volume: 18, Issue:13, 2010
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
Identification of orally active, potent, and selective 4-piperazinylquinazolines as antagonists of the platelet-derived growth factor receptor tyrosine kinase family.Journal of medicinal chemistry, , Aug-15, Volume: 45, Issue:17, 2002
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The Discovery of VX-745: A Novel and Selective p38α Kinase Inhibitor.ACS medicinal chemistry letters, , Oct-13, Volume: 2, Issue:10, 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
Structure-based virtual screening of Src kinase inhibitors.Bioorganic & medicinal chemistry, , Apr-15, Volume: 17, Issue:8, 2009
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases.Nature chemical biology, , Volume: 4, Issue:11, 2008
Discovery of N-(2-chloro-6-methyl- phenyl)-2-(6-(4-(2-hydroxyethyl)- piperazin-1-yl)-2-methylpyrimidin-4- ylamino)thiazole-5-carboxamide (BMS-354825), a dual Src/Abl kinase inhibitor with potent antitumor activity in preclinical assays.Journal of medicinal chemistry, , Dec-30, Volume: 47, Issue:27, 2004
Comprehensive review for anticancer hybridized multitargeting HDAC inhibitors.European journal of medicinal chemistry, , Jan-01, Volume: 209, 2021
Angiokinase inhibition of VEGFR-2, PDGFR and FGFR and cell growth inhibition in lung cancer: Design, synthesis, biological evaluation and molecular docking of novel azaheterocyclic coumarin derivatives.Bioorganic & medicinal chemistry letters, , 09-15, Volume: 48, 2021
[no title available]Journal of medicinal chemistry, , 08-26, Volume: 64, Issue:16, 2021
Targeting Rearranged during Transfection in Cancer: A Perspective on Small-Molecule Inhibitors and Their Clinical Development.Journal of medicinal chemistry, , 08-26, Volume: 64, Issue:16, 2021
FDA-approved pyrimidine-fused bicyclic heterocycles for cancer therapy: Synthesis and clinical application.European journal of medicinal chemistry, , Mar-15, Volume: 214, 2021
Recent advancements of 4-aminoquinazoline derivatives as kinase inhibitors and their applications in medicinal chemistry.European journal of medicinal chemistry, , May-15, Volume: 170, 2019
Design, synthesis and biological evaluation of novel 4-anilinoquinazoline derivatives as hypoxia-selective EGFR and VEGFR-2 dual inhibitors.European journal of medicinal chemistry, , Nov-01, Volume: 181, 2019
Evolution in medicinal chemistry of sorafenib derivatives for hepatocellular carcinoma.European journal of medicinal chemistry, , Oct-01, Volume: 179, 2019
Design, synthesis, biological evaluation of benzoyl amide derivatives containing nitrogen heterocyclic ring as potential VEGFR-2 inhibitors.Bioorganic & medicinal chemistry, , 09-01, Volume: 27, Issue:17, 2019
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
Novel promising 4-anilinoquinazoline-based derivatives as multi-target RTKs inhibitors: Design, molecular docking, synthesis, and antitumor activities in vitro and vivo.Bioorganic & medicinal chemistry, , 10-15, Volume: 27, Issue:20, 2019
Discovery of Novel Potent VEGFR-2 Inhibitors Exerting Significant Antiproliferative Activity against Cancer Cell Lines.Journal of medicinal chemistry, , 01-11, Volume: 61, Issue:1, 2018
Design and discovery of 4-anilinoquinazoline-urea derivatives as dual TK inhibitors of EGFR and VEGFR-2.European journal of medicinal chemistry, , Jan-05, Volume: 125, 2017
1-Piperazinylphthalazines as potential VEGFR-2 inhibitors and anticancer agents: Synthesis and in vitro biological evaluation.European journal of medicinal chemistry, , Jan-01, Volume: 107, 2016
The discovery of 2-substituted phenol quinazolines as potent RET kinase inhibitors with improved KDR selectivity.European journal of medicinal chemistry, , Apr-13, Volume: 112, 2016
Design, synthesis and biological evaluation of N-phenylquinazolin-4-amine hybrids as dual inhibitors of VEGFR-2 and HDAC.European journal of medicinal chemistry, , Feb-15, Volume: 109, 2016
Hybrids from 4-anilinoquinazoline and hydroxamic acid as dual inhibitors of vascular endothelial growth factor receptor-2 and histone deacetylase.Bioorganic & medicinal chemistry letters, , Nov-15, Volume: 25, Issue:22, 2015
Design, synthesis and antitumor activity of 4-aminoquinazoline derivatives targeting VEGFR-2 tyrosine kinase.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 22, Issue:1, 2012
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
Impact of aryloxy-linked quinazolines: a novel series of selective VEGFR-2 receptor tyrosine kinase inhibitors.Bioorganic & medicinal chemistry letters, , Apr-01, Volume: 21, Issue:7, 2011
Pharmacophore modeling and virtual screening studies for new VEGFR-2 kinase inhibitors.European journal of medicinal chemistry, , Volume: 45, Issue:11, 2010
Arylphthalazines as potent, and orally bioavailable inhibitors of VEGFR-2.Bioorganic & medicinal chemistry, , Jan-15, Volume: 17, Issue:2, 2009
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
Synthesis and evaluation of heteroaryl-ketone derivatives as a novel class of VEGFR-2 inhibitors.Bioorganic & medicinal chemistry letters, , Aug-01, Volume: 18, Issue:15, 2008
Dual irreversible kinase inhibitors: quinazoline-based inhibitors incorporating two independent reactive centers with each targeting different cysteine residues in the kinase domains of EGFR and VEGFR-2.Bioorganic & medicinal chemistry, , Jun-01, Volume: 15, Issue:11, 2007
ortho-Substituted azoles as selective and dual inhibitors of VEGF receptors 1 and 2.Bioorganic & medicinal chemistry letters, , Mar-01, Volume: 17, Issue:5, 2007
2-((1H-Azol-1-yl)methyl)-N-arylbenzamides: novel dual inhibitors of VEGFR-1/2 kinases.Bioorganic & medicinal chemistry letters, , Mar-15, Volume: 16, Issue:6, 2006
N-(Aryl)-4-(azolylethyl)thiazole-5-carboxamides: novel potent inhibitors of VEGF receptors I and II.Bioorganic & medicinal chemistry letters, , Volume: 16, Issue:3, 2006
Hetaryl imidazoles: a novel dual inhibitors of VEGF receptors I and II.Bioorganic & medicinal chemistry letters, , Mar-01, Volume: 16, Issue:5, 2006
Inhibitors of VEGF receptors-1 and -2 based on the 2-((pyridin-4-yl)ethyl)pyridine template.Bioorganic & medicinal chemistry letters, , Apr-01, Volume: 16, Issue:7, 2006
A small molecule-kinase interaction map for clinical kinase inhibitors.Nature biotechnology, , Volume: 23, Issue:3, 2005
2-(Quinazolin-4-ylamino)-[1,4]benzoquinones as covalent-binding, irreversible inhibitors of the kinase domain of vascular endothelial growth factor receptor-2.Journal of medicinal chemistry, , Dec-01, Volume: 48, Issue:24, 2005
Discovery and evaluation of 2-anilino-5-aryloxazoles as a novel class of VEGFR2 kinase inhibitors.Journal of medicinal chemistry, , Mar-10, Volume: 48, Issue:5, 2005
Anthranilic acid amides: a novel class of antiangiogenic VEGF receptor kinase inhibitors.Journal of medicinal chemistry, , Dec-19, Volume: 45, Issue:26, 2002
Novel 4-anilinoquinazolines with C-7 basic side chains: design and structure activity relationship of a series of potent, orally active, VEGF receptor tyrosine kinase inhibitors.Journal of medicinal chemistry, , Mar-14, Volume: 45, Issue:6, 2002
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
Pyrazolo[3,4-c]pyridazines as novel and selective inhibitors of cyclin-dependent kinases.Journal of medicinal chemistry, , Nov-03, Volume: 48, Issue:22, 2005
The discovery of novel vascular endothelial growth factor receptor tyrosine kinases inhibitors: pharmacophore modeling, virtual screening and docking studies.Chemical biology & drug design, , Volume: 69, Issue:3, 2007
Pharmacophore modeling and in silico screening for new KDR kinase inhibitors.Bioorganic & medicinal chemistry letters, , Apr-15, Volume: 17, Issue:8, 2007
Identification of substituted 3-[(4,5,6, 7-tetrahydro-1H-indol-2-yl)methylene]-1,3-dihydroindol-2-ones as growth factor receptor inhibitors for VEGF-R2 (Flk-1/KDR), FGF-R1, and PDGF-Rbeta tyrosine kinases.Journal of medicinal chemistry, , Jul-13, Volume: 43, Issue:14, 2000
Design, synthesis, and evaluations of substituted 3-[(3- or 4-carboxyethylpyrrol-2-yl)methylidenyl]indolin-2-ones as inhibitors of VEGF, FGF, and PDGF receptor tyrosine kinases.Journal of medicinal chemistry, , Dec-16, Volume: 42, Issue:25, 1999
Synthesis of a novel biotin-tagged photoaffinity probe for VEGF receptor tyrosine kinases.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 16, Issue:1, 2006
Design and structure-activity relationship of a new class of potent VEGF receptor tyrosine kinase inhibitors.Journal of medicinal chemistry, , Dec-30, Volume: 42, Issue:26, 1999
Discovery of Pyrido[3',2':5,6]thiopyrano[4,3-ACS medicinal chemistry letters, , Apr-11, Volume: 10, Issue:4, 2019
Design, synthesis and preclinical evaluation of 5-methyl-NBioorganic & medicinal chemistry letters, , 10-01, Volume: 28, Issue:18, 2018
Discovery and preclinical evaluation of 7-benzyl-N-(substituted)-pyrrolo[3,2-d]pyrimidin-4-amines as single agents with microtubule targeting effects along with triple-acting angiokinase inhibition as antitumor agents.Bioorganic & medicinal chemistry, , 01-15, Volume: 25, Issue:2, 2017
Synthesis and evaluation of 5-(arylthio)-9H-pyrimido[4,5-b]indole-2,4-diamines as receptor tyrosine kinase and thymidylate synthase inhibitors and as antitumor agents.Bioorganic & medicinal chemistry letters, , 04-01, Volume: 27, Issue:7, 2017
The design, synthesis and biological evaluation of conformationally restricted 4-substituted-2,6-dimethylfuro[2,3-d]pyrimidines as multi-targeted receptor tyrosine kinase and microtubule inhibitors as potential antitumor agents.Bioorganic & medicinal chemistry, , May-15, Volume: 23, Issue:10, 2015
Investigation of new 2-aryl substituted Benzothiopyrano[4,3-d]pyrimidines as kinase inhibitors targeting vascular endothelial growth factor receptor 2.European journal of medicinal chemistry, , Oct-20, Volume: 103, 2015
Discovery of antitubulin agents with antiangiogenic activity as single entities with multitarget chemotherapy potential.ACS medicinal chemistry letters, , May-08, Volume: 5, Issue:5, 2014
The design and discovery of water soluble 4-substituted-2,6-dimethylfuro[2,3-d]pyrimidines as multitargeted receptor tyrosine kinase inhibitors and microtubule targeting antitumor agents.Bioorganic & medicinal chemistry, , Jul-15, Volume: 22, Issue:14, 2014
N2-Trimethylacetyl substituted and unsubstituted-N4-phenylsubstituted-6-(2-pyridin-2-ylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamines: design, cellular receptor tyrosine kinase inhibitory activities and in vivo evaluation as antiangiogenic, antimetastatiBioorganic & medicinal chemistry, , Mar-01, Volume: 21, Issue:5, 2013
Vegfrecine, an inhibitor of VEGF receptor tyrosine kinases isolated from the culture broth of Streptomyces sp.Journal of natural products, , Apr-26, Volume: 76, Issue:4, 2013
Synthesis and biological activity of 5-chloro-N⁴-substituted phenyl-9H-pyrimido[4,5-b]indole-2,4-diamines as vascular endothelial growth factor receptor-2 inhibitors and antiangiogenic agents.Bioorganic & medicinal chemistry, , Apr-01, Volume: 21, Issue:7, 2013
N⁴-(3-Bromophenyl)-7-(substituted benzyl) pyrrolo[2,3-d]pyrimidines as potent multiple receptor tyrosine kinase inhibitors: design, synthesis, and in vivo evaluation.Bioorganic & medicinal chemistry, , Apr-01, Volume: 20, Issue:7, 2012
Novel tricyclic indeno[2,1-d]pyrimidines with dual antiangiogenic and cytotoxic activities as potent antitumor agents.Bioorganic & medicinal chemistry, , Jul-15, Volume: 20, Issue:14, 2012
N⁴-Aryl-6-substitutedphenylmethyl-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamines as receptor tyrosine kinase inhibitors.Bioorganic & medicinal chemistry, , Jan-15, Volume: 20, Issue:2, 2012
Quinazoline-urea, new protein kinase inhibitors in treatment of prostate cancer.Journal of enzyme inhibition and medicinal chemistry, , Volume: 25, Issue:2, 2010
Synthesis and biological activity of N(4)-phenylsubstituted-6-(2,4-dichloro phenylmethyl)-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamines as vascular endothelial growth factor receptor-2 inhibitors and antiangiogenic and antitumor agents.Bioorganic & medicinal chemistry, , May-15, Volume: 18, Issue:10, 2010
The contribution of a 2-amino group on receptor tyrosine kinase inhibition and antiangiogenic activity in 4-anilinosubstituted pyrrolo[2,3-d]pyrimidines.Bioorganic & medicinal chemistry letters, , May-15, Volume: 20, Issue:10, 2010
Single agents with designed combination chemotherapy potential: synthesis and evaluation of substituted pyrimido[4,5-b]indoles as receptor tyrosine kinase and thymidylate synthase inhibitors and as antitumor agents.Journal of medicinal chemistry, , Feb-25, Volume: 53, Issue:4, 2010
Design, synthesis and evaluation of 2-amino-4-m-bromoanilino-6-arylmethyl-7H-pyrrolo[2,3-d]pyrimidines as tyrosine kinase inhibitors and antiangiogenic agents.Bioorganic & medicinal chemistry, , Jul-15, Volume: 18, Issue:14, 2010
Synthesis and radiopharmacological investigation of 3-[4'-[(18)F]fluorobenzylidene]indolin-2-one as possible tyrosine kinase inhibitor.Bioorganic & medicinal chemistry, , Nov-15, Volume: 17, Issue:22, 2009
Design, synthesis, and X-ray crystal structures of 2,4-diaminofuro[2,3-d]pyrimidines as multireceptor tyrosine kinase and dihydrofolate reductase inhibitors.Bioorganic & medicinal chemistry, , Oct-15, Volume: 17, Issue:20, 2009
Design, synthesis and biological evaluation of substituted pyrrolo[2,3-d]pyrimidines as multiple receptor tyrosine kinase inhibitors and antiangiogenic agents.Bioorganic & medicinal chemistry, , May-15, Volume: 16, Issue:10, 2008
Pharmacophore modeling and in silico screening for new KDR kinase inhibitors.Bioorganic & medicinal chemistry letters, , Apr-15, Volume: 17, Issue:8, 2007
Chemical modulation of receptor signaling inhibits regenerative angiogenesis in adult zebrafish.Nature chemical biology, , Volume: 2, Issue:5, 2006
Indolin-2-ones with high in vivo efficacy in a model for multiple sclerosis.Journal of medicinal chemistry, , Aug-25, Volume: 48, Issue:17, 2005
Discovery of 5-[5-fluoro-2-oxo-1,2- dihydroindol-(3Z)-ylidenemethyl]-2,4- dimethyl-1H-pyrrole-3-carboxylic acid (2-diethylaminoethyl)amide, a novel tyrosine kinase inhibitor targeting vascular endothelial and platelet-derived growth factor receptor tyrosiJournal of medicinal chemistry, , Mar-27, Volume: 46, Issue:7, 2003
Anthranilic acid amides: a novel class of antiangiogenic VEGF receptor kinase inhibitors.Journal of medicinal chemistry, , Dec-19, Volume: 45, Issue:26, 2002
Identification of substituted 3-[(4,5,6, 7-tetrahydro-1H-indol-2-yl)methylene]-1,3-dihydroindol-2-ones as growth factor receptor inhibitors for VEGF-R2 (Flk-1/KDR), FGF-R1, and PDGF-Rbeta tyrosine kinases.Journal of medicinal chemistry, , Jul-13, Volume: 43, Issue:14, 2000
New anilinophthalazines as potent and orally well absorbed inhibitors of the VEGF receptor tyrosine kinases useful as antagonists of tumor-driven angiogenesis.Journal of medicinal chemistry, , Jun-15, Volume: 43, Issue:12, 2000
Design, synthesis, and evaluations of substituted 3-[(3- or 4-carboxyethylpyrrol-2-yl)methylidenyl]indolin-2-ones as inhibitors of VEGF, FGF, and PDGF receptor tyrosine kinases.Journal of medicinal chemistry, , Dec-16, Volume: 42, Issue:25, 1999
The design, synthesis, and biological evaluation of potent receptor tyrosine kinase inhibitors.Bioorganic & medicinal chemistry letters, , Aug-01, Volume: 22, Issue:15, 2012
Synthesis and biological activity of N(4)-phenylsubstituted-6-(2,4-dichloro phenylmethyl)-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamines as vascular endothelial growth factor receptor-2 inhibitors and antiangiogenic and antitumor agents.Bioorganic & medicinal chemistry, , May-15, Volume: 18, Issue:10, 2010
5-Substituted pyrido[2,3-d]pyrimidine, an inhibitor against three receptor tyrosine kinases.Bioorganic & medicinal chemistry letters, , Feb-01, Volume: 19, Issue:3, 2009
Discovery of 5-[5-fluoro-2-oxo-1,2- dihydroindol-(3Z)-ylidenemethyl]-2,4- dimethyl-1H-pyrrole-3-carboxylic acid (2-diethylaminoethyl)amide, a novel tyrosine kinase inhibitor targeting vascular endothelial and platelet-derived growth factor receptor tyrosiJournal of medicinal chemistry, , Mar-27, Volume: 46, Issue:7, 2003
Design, synthesis, and evaluations of substituted 3-[(3- or 4-carboxyethylpyrrol-2-yl)methylidenyl]indolin-2-ones as inhibitors of VEGF, FGF, and PDGF receptor tyrosine kinases.Journal of medicinal chemistry, , Dec-16, Volume: 42, Issue:25, 1999
Targeting Rearranged during Transfection in Cancer: A Perspective on Small-Molecule Inhibitors and Their Clinical Development.Journal of medicinal chemistry, , 08-26, Volume: 64, Issue:16, 2021
Design, synthesis, and in vitro and in vivo anti-angiogenesis study of a novel vascular endothelial growth factor receptor-2 (VEGFR-2) inhibitor based on 1,2,3-triazole scaffold.European journal of medicinal chemistry, , Feb-05, Volume: 211, 2021
Potential of substituted quinazolines to interact with multiple targets in the treatment of cancer.Bioorganic & medicinal chemistry, , 04-01, Volume: 35, 2021
[no title available]Journal of medicinal chemistry, , 04-22, Volume: 64, Issue:8, 2021
Novel 2-indolinone thiazole hybrids as sunitinib analogues: Design, synthesis, and potent VEGFR-2 inhibition with potential anti-renal cancer activity.European journal of medicinal chemistry, , Dec-15, Volume: 208, 2020
Substituted oxindol-3-ylidenes as AMP-activated protein kinase (AMPK) inhibitors.European journal of medicinal chemistry, , Jul-01, Volume: 197, 2020
Design, synthesis and in vitro evaluation of 6-amide-2-aryl benzoxazole/benzimidazole derivatives against tumor cells by inhibiting VEGFR-2 kinase.European journal of medicinal chemistry, , Oct-01, Volume: 179, 2019
Evolution in medicinal chemistry of sorafenib derivatives for hepatocellular carcinoma.European journal of medicinal chemistry, , Oct-01, Volume: 179, 2019
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
Synthesis and biological evaluation of 3-aryl-quinolin derivatives as anti-breast cancer agents targeting ERα and VEGFR-2.European journal of medicinal chemistry, , Jan-01, Volume: 161, 2019
Design, synthesis and preclinical evaluation of 5-methyl-NBioorganic & medicinal chemistry letters, , 10-01, Volume: 28, Issue:18, 2018
Structure-activity relationships of 2, 4-disubstituted pyrimidines as dual ERα/VEGFR-2 ligands with anti-breast cancer activity.European journal of medicinal chemistry, , Apr-25, Volume: 150, 2018
Discovery of Novel Potent VEGFR-2 Inhibitors Exerting Significant Antiproliferative Activity against Cancer Cell Lines.Journal of medicinal chemistry, , 01-11, Volume: 61, Issue:1, 2018
Discovery of N-(4-{[5-Fluoro-7-(2-methoxyethoxy)quinazolin-4-yl]amino}phenyl)-2-[4-(propan-2-yl)-1 H-1,2,3-triazol-1-yl]acetamide (AZD3229), a Potent Pan-KIT Mutant Inhibitor for the Treatment of Gastrointestinal Stromal Tumors.Journal of medicinal chemistry, , 10-11, Volume: 61, Issue:19, 2018
Pyrazolo[4,3-b]pyrimido[4,5-e][1,4]diazepine derivatives as new multi-targeted inhibitors of Aurora A/B and KDR.European journal of medicinal chemistry, , Oct-05, Volume: 158, 2018
Discovery and preclinical evaluation of 7-benzyl-N-(substituted)-pyrrolo[3,2-d]pyrimidin-4-amines as single agents with microtubule targeting effects along with triple-acting angiokinase inhibition as antitumor agents.Bioorganic & medicinal chemistry, , 01-15, Volume: 25, Issue:2, 2017
Synthesis of Novel c(AmpRGD)-Sunitinib Dual Conjugates as Molecular Tools Targeting the αJournal of medicinal chemistry, , 01-12, Volume: 60, Issue:1, 2017
Discovery of 1,3-Diaryl-pyridones as Potent VEGFR-2 Inhibitors: Design, Synthesis, and Biological Evaluation.Chemical biology & drug design, , Volume: 87, Issue:5, 2016
1-Piperazinylphthalazines as potential VEGFR-2 inhibitors and anticancer agents: Synthesis and in vitro biological evaluation.European journal of medicinal chemistry, , Jan-01, Volume: 107, 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 evaluation of 6-aryl-indenoisoquinolone derivatives dual targeting ERα and VEGFR-2 as anti-breast cancer agents.European journal of medicinal chemistry, , Aug-08, Volume: 118, 2016
Distinct binding mode of multikinase inhibitor lenvatinib revealed by biochemical characterization.ACS medicinal chemistry letters, , Jan-08, Volume: 6, Issue:1, 2015
The design, synthesis and biological evaluation of conformationally restricted 4-substituted-2,6-dimethylfuro[2,3-d]pyrimidines as multi-targeted receptor tyrosine kinase and microtubule inhibitors as potential antitumor agents.Bioorganic & medicinal chemistry, , May-15, Volume: 23, Issue:10, 2015
Ynamide Click chemistry in development of triazole VEGFR2 TK modulators.European journal of medicinal chemistry, , Oct-20, Volume: 103, 2015
Discovery of N-(2-phenyl-1H-benzo[d]imidazol-5-yl)quinolin-4-amine derivatives as novel VEGFR-2 kinase inhibitors.European journal of medicinal chemistry, , Sep-12, Volume: 84, 2014
Discovery of antitubulin agents with antiangiogenic activity as single entities with multitarget chemotherapy potential.ACS medicinal chemistry letters, , May-08, Volume: 5, Issue:5, 2014
The design and discovery of water soluble 4-substituted-2,6-dimethylfuro[2,3-d]pyrimidines as multitargeted receptor tyrosine kinase inhibitors and microtubule targeting antitumor agents.Bioorganic & medicinal chemistry, , Jul-15, Volume: 22, Issue:14, 2014
Synthesis and in vivo SAR study of indolin-2-one-based multi-targeted inhibitors as potential anticancer agents.European journal of medicinal chemistry, , Jul-23, Volume: 82, 2014
Design, synthesis, and biological evaluation of novel 3-pyrrolo[b]cyclohexylene-2-dihydroindolinone derivatives as potent receptor tyrosine kinase inhibitors.Bioorganic & medicinal chemistry letters, , Oct-15, Volume: 23, Issue:20, 2013
N2-Trimethylacetyl substituted and unsubstituted-N4-phenylsubstituted-6-(2-pyridin-2-ylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamines: design, cellular receptor tyrosine kinase inhibitory activities and in vivo evaluation as antiangiogenic, antimetastatiBioorganic & medicinal chemistry, , Mar-01, Volume: 21, Issue:5, 2013
Synthesis and biological activity of 5-chloro-N⁴-substituted phenyl-9H-pyrimido[4,5-b]indole-2,4-diamines as vascular endothelial growth factor receptor-2 inhibitors and antiangiogenic agents.Bioorganic & medicinal chemistry, , Apr-01, Volume: 21, Issue:7, 2013
Radioiodinated sunitinib as a potential radiotracer for imaging angiogenesis-radiosynthesis and first radiopharmacological evaluation of 5-[125I]Iodo-sunitinib.Bioorganic & medicinal chemistry letters, , Apr-15, Volume: 22, Issue:8, 2012
Novel tricyclic indeno[2,1-d]pyrimidines with dual antiangiogenic and cytotoxic activities as potent antitumor agents.Bioorganic & medicinal chemistry, , Jul-15, Volume: 20, Issue:14, 2012
VX-322: a novel dual receptor tyrosine kinase inhibitor for the treatment of acute myelogenous leukemia.Journal of medicinal chemistry, , Jan-26, Volume: 55, Issue:2, 2012
N⁴-Aryl-6-substitutedphenylmethyl-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamines as receptor tyrosine kinase inhibitors.Bioorganic & medicinal chemistry, , Jan-15, Volume: 20, Issue:2, 2012
Synthesis, in silico, in vitro, and in vivo investigation of 5-[¹¹C]methoxy-substituted sunitinib, a tyrosine kinase inhibitor of VEGFR-2.European journal of medicinal chemistry, , Volume: 58, 2012
The design, synthesis, and biological evaluation of potent receptor tyrosine kinase inhibitors.Bioorganic & medicinal chemistry letters, , Aug-01, Volume: 22, Issue:15, 2012
2-Anilino-4-(benzimidazol-2-yl)pyrimidines--a multikinase inhibitor scaffold with antiproliferative activity toward cancer cell lines.European journal of medicinal chemistry, , Volume: 53, 2012
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
Biochemical characterization of a novel type-II VEGFR2 kinase inhibitor: comparison of binding to non-phosphorylated and phosphorylated VEGFR2.Bioorganic & medicinal chemistry, , Sep-15, Volume: 19, Issue:18, 2011
Synthesis and biological evaluation of 2-indolinone derivatives as potential antitumor agents.European journal of medicinal chemistry, , Volume: 46, Issue:12, 2011
Synthesis and biological activity of N(4)-phenylsubstituted-6-(2,4-dichloro phenylmethyl)-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamines as vascular endothelial growth factor receptor-2 inhibitors and antiangiogenic and antitumor agents.Bioorganic & medicinal chemistry, , May-15, Volume: 18, Issue:10, 2010
Selectively nonselective kinase inhibition: striking the right balance.Journal of medicinal chemistry, , Feb-25, Volume: 53, Issue:4, 2010
Novel potent orally active multitargeted receptor tyrosine kinase inhibitors: synthesis, structure-activity relationships, and antitumor activities of 2-indolinone derivatives.Journal of medicinal chemistry, , Nov-25, Volume: 53, Issue:22, 2010
Synthesis and structure-activity relationship of 6-arylureido-3-pyrrol-2-ylmethylideneindolin-2-one derivatives as potent receptor tyrosine kinase inhibitors.Bioorganic & medicinal chemistry, , Jul-01, Volume: 18, Issue:13, 2010
Pharmacophore modeling and virtual screening studies for new VEGFR-2 kinase inhibitors.European journal of medicinal chemistry, , Volume: 45, Issue:11, 2010
Novel azulene-based derivatives as potent multi-receptor tyrosine kinase inhibitors.Bioorganic & medicinal chemistry letters, , Oct-15, Volume: 20, Issue:20, 2010
Design, synthesis and evaluation of 2-amino-4-m-bromoanilino-6-arylmethyl-7H-pyrrolo[2,3-d]pyrimidines as tyrosine kinase inhibitors and antiangiogenic agents.Bioorganic & medicinal chemistry, , Jul-15, Volume: 18, Issue:14, 2010
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
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
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
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases.Nature chemical biology, , Volume: 4, Issue:11, 2008
Pharmacophore modeling and in silico screening for new KDR kinase inhibitors.Bioorganic & medicinal chemistry letters, , Apr-15, Volume: 17, Issue:8, 2007
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
A small molecule-kinase interaction map for clinical kinase inhibitors.Nature biotechnology, , Volume: 23, Issue:3, 2005
Thienopyrimidine ureas as novel and potent multitargeted receptor tyrosine kinase inhibitors.Journal of medicinal chemistry, , Sep-22, Volume: 48, Issue:19, 2005
Discovery of 5-[5-fluoro-2-oxo-1,2- dihydroindol-(3Z)-ylidenemethyl]-2,4- dimethyl-1H-pyrrole-3-carboxylic acid (2-diethylaminoethyl)amide, a novel tyrosine kinase inhibitor targeting vascular endothelial and platelet-derived growth factor receptor tyrosiJournal of medicinal chemistry, , Mar-27, Volume: 46, Issue:7, 2003
Structure and regulation of the human Nek2 centrosomal kinase.The Journal of biological chemistry, , Mar-02, Volume: 282, Issue:9, 2007
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
Discovery of 5-[5-fluoro-2-oxo-1,2- dihydroindol-(3Z)-ylidenemethyl]-2,4- dimethyl-1H-pyrrole-3-carboxylic acid (2-diethylaminoethyl)amide, a novel tyrosine kinase inhibitor targeting vascular endothelial and platelet-derived growth factor receptor tyrosiJournal of medicinal chemistry, , Mar-27, Volume: 46, Issue:7, 2003
An insight on synthetic and medicinal aspects of pyrazolo[1,5-a]pyrimidine scaffold.European journal of medicinal chemistry, , Jan-27, Volume: 126, 2017
In vivo structure-activity relationship study of dorsomorphin analogues identifies selective VEGF and BMP inhibitors.ACS chemical biology, , Feb-19, Volume: 5, Issue:2, 2010
Optimization of a pyrazolo[1,5-a]pyrimidine class of KDR kinase inhibitors: improvements in physical properties enhance cellular activity and pharmacokinetics.Bioorganic & medicinal chemistry letters, , Dec-16, Volume: 12, Issue:24, 2002
Investigation of a novel molecular descriptor for the lead optimization of 4-aminoquinazolines as vascular endothelial growth factor receptor-2 inhibitors: application for quantitative structure-activity relationship analysis in lead optimization.Bioorganic & medicinal chemistry letters, , Mar-01, Volume: 21, Issue:5, 2011
7-Aminopyrazolo[1,5-a]pyrimidines as potent multitargeted receptor tyrosine kinase inhibitors.Journal of medicinal chemistry, , Jul-10, Volume: 51, Issue:13, 2008
Synthesis and initial SAR studies of 3,6-disubstituted pyrazolo[1,5-a]pyrimidines: a new class of KDR kinase inhibitors.Bioorganic & medicinal chemistry letters, , Oct-07, Volume: 12, Issue:19, 2002
Optimization of a pyrazolo[1,5-a]pyrimidine class of KDR kinase inhibitors: improvements in physical properties enhance cellular activity and pharmacokinetics.Bioorganic & medicinal chemistry letters, , Dec-16, Volume: 12, Issue:24, 2002
N-(5-chloro-1,3-benzodioxol-4-yl)-7-[2-(4-methylpiperazin-1-yl)ethoxy]-5- (tetrahydro-2H-pyran-4-yloxy)quinazolin-4-amine, a novel, highly selective, orally available, dual-specific c-Src/Abl kinase inhibitor.Journal of medicinal chemistry, , Nov-02, Volume: 49, Issue:22, 2006
Discovery of a new class of anilinoquinazoline inhibitors with high affinity and specificity for the tyrosine kinase domain of c-Src.Journal of medicinal chemistry, , Feb-12, Volume: 47, Issue:4, 2004
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
1-Acyl-1H-[1,2,4]triazole-3,5-diamine analogues as novel and potent anticancer cyclin-dependent kinase inhibitors: synthesis and evaluation of biological activities.Journal of medicinal chemistry, , Jun-30, Volume: 48, Issue:13, 2005
Pharmacophore modeling and virtual screening studies for new VEGFR-2 kinase inhibitors.European journal of medicinal chemistry, , Volume: 45, Issue:11, 2010
3,4-Disubstituted isothiazoles: novel potent inhibitors of VEGF receptors 1 and 2.Bioorganic & medicinal chemistry letters, , Feb-15, Volume: 19, Issue:4, 2009
(1,2,3-Triazol-4-yl)benzenamines: synthesis and activity against VEGF receptors 1 and 2.Bioorganic & medicinal chemistry letters, , Mar-01, Volume: 19, Issue:5, 2009
Conformation-activity relationship on novel 4-pyridylmethylthio derivatives with antiangiogenic activity.Bioorganic & medicinal chemistry letters, , May-01, Volume: 18, Issue:9, 2008
Discovery of indenopyrazoles as EGFR and VEGFR-2 tyrosine kinase inhibitors by in silico high-throughput screening.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 18, Issue:1, 2008
ortho-Substituted azoles as selective and dual inhibitors of VEGF receptors 1 and 2.Bioorganic & medicinal chemistry letters, , Mar-01, Volume: 17, Issue:5, 2007
2-((1H-Azol-1-yl)methyl)-N-arylbenzamides: novel dual inhibitors of VEGFR-1/2 kinases.Bioorganic & medicinal chemistry letters, , Mar-15, Volume: 16, Issue:6, 2006
N-(Aryl)-4-(azolylethyl)thiazole-5-carboxamides: novel potent inhibitors of VEGF receptors I and II.Bioorganic & medicinal chemistry letters, , Volume: 16, Issue:3, 2006
Synthesis and biological evaluation of benzamides and benzamidines as selective inhibitors of VEGFR tyrosine kinases.Bioorganic & medicinal chemistry letters, , Oct-01, Volume: 16, Issue:19, 2006
Hetaryl imidazoles: a novel dual inhibitors of VEGF receptors I and II.Bioorganic & medicinal chemistry letters, , Mar-01, Volume: 16, Issue:5, 2006
Rational design of inhibitors that bind to inactive kinase conformations.Nature chemical biology, , Volume: 2, Issue:7, 2006
Inhibitors of VEGF receptors-1 and -2 based on the 2-((pyridin-4-yl)ethyl)pyridine template.Bioorganic & medicinal chemistry letters, , Apr-01, Volume: 16, Issue:7, 2006
Anthranilic acid amides: a novel class of antiangiogenic VEGF receptor kinase inhibitors.Journal of medicinal chemistry, , Dec-19, Volume: 45, Issue:26, 2002
Discovery of N-phenyl-4-(thiazol-5-yl)pyrimidin-2-amine aurora kinase inhibitors.Journal of medicinal chemistry, , Jun-10, Volume: 53, Issue:11, 2010
Discovery and development of aurora kinase inhibitors as anticancer agents.Journal of medicinal chemistry, , May-14, Volume: 52, Issue:9, 2009
Pyrazolo-benzothiazole hybrids: Synthesis, anticancer properties and evaluation of antiangiogenic activity using in vitro VEGFR-2 kinase and in vivo transgenic zebrafish model.European journal of medicinal chemistry, , Nov-15, Volume: 182, 2019
Evolution in medicinal chemistry of sorafenib derivatives for hepatocellular carcinoma.European journal of medicinal chemistry, , Oct-01, Volume: 179, 2019
Discovery of Novel Potent VEGFR-2 Inhibitors Exerting Significant Antiproliferative Activity against Cancer Cell Lines.Journal of medicinal chemistry, , 01-11, Volume: 61, Issue:1, 2018
Recent developments in small molecule therapies for renal cell carcinoma.European journal of medicinal chemistry, , Dec-15, Volume: 142, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
Pharmacophore modeling and virtual screening studies for new VEGFR-2 kinase inhibitors.European journal of medicinal chemistry, , Volume: 45, Issue:11, 2010
[no title available],
Pyrazolo[3,4-d]pyrimidines containing an extended 3-substituent as potent inhibitors of Lck -- a selectivity insight.Bioorganic & medicinal chemistry letters, , Jun-17, Volume: 12, Issue:12, 2002
Pyrrolo[2,3-d]pyrimidines containing diverse N-7 substituents as potent inhibitors of Lck.Bioorganic & medicinal chemistry letters, , Jun-17, Volume: 12, Issue:12, 2002
The discovery of novel vascular endothelial growth factor receptor tyrosine kinases inhibitors: pharmacophore modeling, virtual screening and docking studies.Chemical biology & drug design, , Volume: 69, Issue:3, 2007
3D QSAR studies on a series of potent and high selective inhibitors for three kinases of RTK family.Journal of molecular graphics & modelling, , Volume: 26, Issue:1, 2007
Isothiazolopyrimidines and isoxazolopyrimidines as novel multi-targeted inhibitors of receptor tyrosine kinases.Bioorganic & medicinal chemistry letters, , Aug-15, Volume: 16, Issue:16, 2006
Thienopyrimidine ureas as novel and potent multitargeted receptor tyrosine kinase inhibitors.Journal of medicinal chemistry, , Sep-22, Volume: 48, Issue:19, 2005
Pyrrolo[2,3-d]pyrimidines containing diverse N-7 substituents as potent inhibitors of Lck.Bioorganic & medicinal chemistry letters, , Jun-17, Volume: 12, Issue:12, 2002
Pyrrolo[2,3-d]pyrimidines containing an extended 5-substituent as potent and selective inhibitors of lck I.Bioorganic & medicinal chemistry letters, , Oct-02, Volume: 10, Issue:19, 2000
[no title available]Journal of medicinal chemistry, , 08-26, Volume: 64, Issue:16, 2021
Vascular endothelial growth factor (VEGF) receptors: drugs and new inhibitors.Journal of medicinal chemistry, , Dec-27, Volume: 55, Issue:24, 2012
Pharmacophore modeling and virtual screening studies for new VEGFR-2 kinase inhibitors.European journal of medicinal chemistry, , Volume: 45, Issue:11, 2010
Vascular endothelial growth factor (VEGF) receptors: drugs and new inhibitors.Journal of medicinal chemistry, , Dec-27, Volume: 55, Issue:24, 2012
Design and synthesis of dihydroindazolo[5,4-a]pyrrolo[3,4-c]carbazole oximes as potent dual inhibitors of TIE-2 and VEGF-R2 receptor tyrosine kinases.Bioorganic & medicinal chemistry letters, , Mar-15, Volume: 18, Issue:6, 2008
Design, synthesis and biological evaluation of novel 2,4-diaryl pyrimidine derivatives as selective EGFREuropean journal of medicinal chemistry, , Feb-15, Volume: 212, 2021
[no title available]Journal of medicinal chemistry, , 08-26, Volume: 64, Issue:16, 2021
Evolution in medicinal chemistry of sorafenib derivatives for hepatocellular carcinoma.European journal of medicinal chemistry, , Oct-01, Volume: 179, 2019
Discovery of Dioxino[2,3-f]quinazoline derivative VEGFR-2 inhibitors exerting significant antipro-liferative activity in HUVECs and mice.European journal of medicinal chemistry, , Aug-01, Volume: 175, 2019
Discovery of Novel Potent VEGFR-2 Inhibitors Exerting Significant Antiproliferative Activity against Cancer Cell Lines.Journal of medicinal chemistry, , 01-11, Volume: 61, Issue:1, 2018
Distinct binding mode of multikinase inhibitor lenvatinib revealed by biochemical characterization.ACS medicinal chemistry letters, , Jan-08, Volume: 6, Issue:1, 2015
Vascular endothelial growth factor (VEGF) receptors: drugs and new inhibitors.Journal of medicinal chemistry, , Dec-27, Volume: 55, Issue:24, 2012
Pharmacophore modeling and virtual screening studies for new VEGFR-2 kinase inhibitors.European journal of medicinal chemistry, , Volume: 45, Issue:11, 2010
Identification of a potent 5-phenyl-thiazol-2-ylamine-based inhibitor of FLT3 with activity against drug resistance-conferring point mutations.European journal of medicinal chemistry, , Jul-15, Volume: 100, 2015
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
Vascular endothelial growth factor (VEGF) receptors: drugs and new inhibitors.Journal of medicinal chemistry, , Dec-27, Volume: 55, Issue:24, 2012
Orally active anti-proliferation agents: novel diphenylamine derivatives as FGF-R2 autophosphorylation inhibitors.Bioorganic & medicinal chemistry letters, , Feb-23, Volume: 14, Issue:4, 2004
Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/Journal of medicinal chemistry, , May-22, Volume: 57, Issue:10, 2014
Vascular endothelial growth factor (VEGF) receptors: drugs and new inhibitors.Journal of medicinal chemistry, , Dec-27, Volume: 55, Issue:24, 2012
Inhibition of c-Kit, VEGFR-2 (KDR), and ABCG2 by analogues of OSI-930.Bioorganic & medicinal chemistry letters, , Nov-01, Volume: 21, Issue:21, 2011
Design, synthesis and biological evaluation of deuterated Tivozanib for improving pharmacokinetic properties.Bioorganic & medicinal chemistry letters, , Jun-01, Volume: 25, Issue:11, 2015
Discovery of new 4-alkoxyquinazoline-based derivatives as potent VEGFR2 inhibitors.Chemical biology & drug design, , Volume: 86, Issue:5, 2015
Recent advances in the structural library of functionalized quinazoline and quinazolinone scaffolds: synthetic approaches and multifarious applications.European journal of medicinal chemistry, , Apr-09, Volume: 76, 2014
Vascular endothelial growth factor (VEGF) receptors: drugs and new inhibitors.Journal of medicinal chemistry, , Dec-27, Volume: 55, Issue:24, 2012
Pharmacophore modeling and virtual screening studies for new VEGFR-2 kinase inhibitors.European journal of medicinal chemistry, , Volume: 45, Issue:11, 2010
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
Dual irreversible kinase inhibitors: quinazoline-based inhibitors incorporating two independent reactive centers with each targeting different cysteine residues in the kinase domains of EGFR and VEGFR-2.Bioorganic & medicinal chemistry, , Jun-01, Volume: 15, Issue:11, 2007
[no title available]Journal of medicinal chemistry, , 08-26, Volume: 64, Issue:16, 2021
The association between anti-tumor potency and structure-activity of protein-kinases inhibitors based on quinazoline molecular skeleton.Bioorganic & medicinal chemistry, , 02-01, Volume: 27, Issue:3, 2019
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
Pharmacophore modeling and virtual screening studies for new VEGFR-2 kinase inhibitors.European journal of medicinal chemistry, , Volume: 45, Issue:11, 2010
Substituted 3-imidazo[1,2-a]pyridin-3-yl- 4-(1,2,3,4-tetrahydro-[1,4]diazepino-[6,7,1-hi]indol-7-yl)pyrrole-2,5-diones as highly selective and potent inhibitors of glycogen synthase kinase-3.Journal of medicinal chemistry, , Jul-29, Volume: 47, Issue:16, 2004
Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/Journal of medicinal chemistry, , May-22, Volume: 57, Issue:10, 2014
[no title available]Journal of medicinal chemistry, , 08-26, Volume: 64, Issue:16, 2021
Evolution in medicinal chemistry of sorafenib derivatives for hepatocellular carcinoma.European journal of medicinal chemistry, , Oct-01, Volume: 179, 2019
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
Discovery of Novel Pazopanib-Based HDAC and VEGFR Dual Inhibitors Targeting Cancer Epigenetics and Angiogenesis Simultaneously.Journal of medicinal chemistry, , 06-28, Volume: 61, Issue:12, 2018
Recent developments in small molecule therapies for renal cell carcinoma.European journal of medicinal chemistry, , Dec-15, Volume: 142, 2017
Design, synthesis and biological evaluation of pazopanib derivatives as antitumor agents.Chemical biology & drug design, , Volume: 83, Issue:3, 2014
Synthesis and biological evaluation of novel pazopanib derivatives as antitumor agents.Bioorganic & medicinal chemistry letters, , Feb-15, Volume: 24, Issue:4, 2014
Selectivity data: assessment, predictions, concordance, and implications.Journal of medicinal chemistry, , Sep-12, Volume: 56, Issue:17, 2013
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
Pharmacophore modeling and virtual screening studies for new VEGFR-2 kinase inhibitors.European journal of medicinal chemistry, , Volume: 45, Issue:11, 2010
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
Discovery of 5-[[4-[(2,3-dimethyl-2H-indazol-6-yl)methylamino]-2-pyrimidinyl]amino]-2-methyl-benzenesulfonamide (Pazopanib), a novel and potent vascular endothelial growth factor receptor inhibitor.Journal of medicinal chemistry, , Aug-14, Volume: 51, Issue:15, 2008
Structure-based virtual screening of Src kinase inhibitors.Bioorganic & medicinal chemistry, , Apr-15, Volume: 17, Issue:8, 2009
N-(5-chloro-1,3-benzodioxol-4-yl)-7-[2-(4-methylpiperazin-1-yl)ethoxy]-5- (tetrahydro-2H-pyran-4-yloxy)quinazolin-4-amine, a novel, highly selective, orally available, dual-specific c-Src/Abl kinase inhibitor.Journal of medicinal chemistry, , Nov-02, Volume: 49, Issue:22, 2006
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
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
Identification of a Unique Resorcylic Acid Lactone Derivative That Targets Both Lymphangiogenesis and Angiogenesis.Journal of medicinal chemistry, , 10-24, Volume: 62, Issue:20, 2019
Identification of the First Selective Activin Receptor-Like Kinase 1 Inhibitor, a Reversible Version of L-783277.Journal of medicinal chemistry, , 02-23, Volume: 60, Issue:4, 2017
Kinase inhibition by deoxy analogues of the resorcylic lactone L-783277.ACS medicinal chemistry letters, , Jan-13, Volume: 2, Issue:1, 2011
Recent Developments in the Use of Kinase Inhibitors for Management of Viral Infections.Journal of medicinal chemistry, , 01-27, Volume: 65, Issue:2, 2022
Targeting Rearranged during Transfection in Cancer: A Perspective on Small-Molecule Inhibitors and Their Clinical Development.Journal of medicinal chemistry, , 08-26, Volume: 64, Issue:16, 2021
Evolution in medicinal chemistry of sorafenib derivatives for hepatocellular carcinoma.European journal of medicinal chemistry, , Oct-01, Volume: 179, 2019
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
Novel potent substituted 4-amino-2-thiopyrimidines as dual VEGFR-2 and BRAF kinase inhibitors.European journal of medicinal chemistry, , Oct-01, Volume: 179, 2019
Discovery of N-(4-{[5-Fluoro-7-(2-methoxyethoxy)quinazolin-4-yl]amino}phenyl)-2-[4-(propan-2-yl)-1 H-1,2,3-triazol-1-yl]acetamide (AZD3229), a Potent Pan-KIT Mutant Inhibitor for the Treatment of Gastrointestinal Stromal Tumors.Journal of medicinal chemistry, , 10-11, Volume: 61, Issue:19, 2018
Discovery of GS-9973, a selective and orally efficacious inhibitor of spleen tyrosine kinase.Journal of medicinal chemistry, , May-08, Volume: 57, Issue:9, 2014
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
Metabolic chiral inversion of brivanib and its relevance to safety and pharmacology.Drug metabolism and disposition: the biological fate of chemicals, , Volume: 40, Issue:12, 2012
Metabolism and disposition of [14C]brivanib alaninate after oral administration to rats, monkeys, and humans.Drug metabolism and disposition: the biological fate of chemicals, , Volume: 39, Issue:5, 2011
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
Discovery and preclinical studies of 5-isopropyl-6-(5-methyl-1,3,4-oxadiazol-2-yl)-N-(2-methyl-1H-pyrrolo[2,3-b]pyridin-5-yl)pyrrolo[2,1-f][1,2,4]triazin-4-amine (BMS-645737), an in vivo active potent VEGFR-2 inhibitor.Bioorganic & medicinal chemistry letters, , May-01, Volume: 18, Issue:9, 2008
Discovery and preclinical studies of (R)-1-(4-(4-fluoro-2-methyl-1H-indol-5-yloxy)-5- methylpyrrolo[2,1-f][1,2,4]triazin-6-yloxy)propan- 2-ol (BMS-540215), an in vivo active potent VEGFR-2 inhibitor.Journal of medicinal chemistry, , Apr-06, Volume: 49, Issue:7, 2006
Potential anti-angiogenesis effects of p-terphenyl compounds from Polyozellus multiplex.Journal of natural products, , Apr-25, Volume: 77, Issue:4, 2014
Novel potent orally active selective VEGFR-2 tyrosine kinase inhibitors: synthesis, structure-activity relationships, and antitumor activities of N-phenyl-N'-{4-(4-quinolyloxy)phenyl}ureas.Journal of medicinal chemistry, , Mar-10, Volume: 48, Issue:5, 2005
Identification of a 5-[3-phenyl-(2-cyclic-ether)-methylether]-4-aminopyrrolo[2,3-d]pyrimidine series of IGF-1R inhibitors.Bioorganic & medicinal chemistry letters, , Apr-15, Volume: 26, Issue:8, 2016
Optimisation of a 5-[3-phenyl-(2-cyclic-ether)-methyl-ether]-4-aminopyrrolopyrimidine series of IGF-1R inhibitors.Bioorganic & medicinal chemistry letters, , Apr-15, Volume: 26, Issue:8, 2016
Discovery of novel anti-angiogenesis agents. Part 11: Development of PROTACs based on active molecules with potency of promoting vascular normalization.European journal of medicinal chemistry, , Nov-01, Volume: 205, 2020
Design, synthesis and structure-activity relationship of diaryl-ureas with novel isoxazol[3,4-b]pyridine-3-amino-structure as multi-target inhibitors against receptor tyrosine kinase.Bioorganic & medicinal chemistry, , 09-01, Volume: 26, Issue:16, 2018
Cyclin-Dependent Kinase 8: A New Hope in Targeted Cancer Therapy?Journal of medicinal chemistry, , 06-28, Volume: 61, Issue:12, 2018
Discovery of Potent, Selective Stem Cell Factor Receptor/Platelet Derived Growth Factor Receptor Alpha (c-KIT/PDGFRα) Dual Inhibitor for the Treatment of Imatinib-Resistant Gastrointestinal Stromal Tumors (GISTs).Journal of medicinal chemistry, , 06-22, Volume: 60, Issue:12, 2017
Discovery of a New Series of Naphthamides as Potent VEGFR-2 Kinase Inhibitors.ACS medicinal chemistry letters, , May-08, Volume: 5, Issue:5, 2014
Discovery of 3-phenyl-1H-5-pyrazolylamine derivatives containing a urea pharmacophore as potent and efficacious inhibitors of FMS-like tyrosine kinase-3 (FLT3).Bioorganic & medicinal chemistry, , Jun-01, Volume: 21, Issue:11, 2013
3-Phenyl-1H-5-pyrazolylamine-based derivatives as potent and efficacious inhibitors of FMS-like tyrosine kinase-3 (FLT3).Bioorganic & medicinal chemistry letters, , Jul-15, Volume: 22, Issue:14, 2012
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
Discovery and evaluation of 3-phenyl-1H-5-pyrazolylamine-based derivatives as potent, selective and efficacious inhibitors of FMS-like tyrosine kinase-3 (FLT3).Bioorganic & medicinal chemistry, , Jul-15, Volume: 19, Issue:14, 2011
7-Aminopyrazolo[1,5-a]pyrimidines as potent multitargeted receptor tyrosine kinase inhibitors.Journal of medicinal chemistry, , Jul-10, Volume: 51, Issue:13, 2008
3-amino-benzo[d]isoxazoles as novel multitargeted inhibitors of receptor tyrosine kinases.Journal of medicinal chemistry, , Mar-13, Volume: 51, Issue:5, 2008
Identification of aminopyrazolopyridine ureas as potent VEGFR/PDGFR multitargeted kinase inhibitors.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 18, Issue:1, 2008
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
Discovery of N-(4-(3-amino-1H-indazol-4-yl)phenyl)-N'-(2-fluoro-5-methylphenyl)urea (ABT-869), a 3-aminoindazole-based orally active multitargeted receptor tyrosine kinase inhibitor.Journal of medicinal chemistry, , Apr-05, Volume: 50, Issue:7, 2007
Discovery of N-(4-{[5-Fluoro-7-(2-methoxyethoxy)quinazolin-4-yl]amino}phenyl)-2-[4-(propan-2-yl)-1 H-1,2,3-triazol-1-yl]acetamide (AZD3229), a Potent Pan-KIT Mutant Inhibitor for the Treatment of Gastrointestinal Stromal Tumors.Journal of medicinal chemistry, , 10-11, Volume: 61, Issue:19, 2018
Discovery of new quinoline ether inhibitors with high affinity and selectivity for PDGFR tyrosine kinases.Bioorganic & medicinal chemistry letters, , May-01, Volume: 22, Issue:9, 2012
Medicinal Chemistry Approaches to Heart Regeneration.Journal of medicinal chemistry, , Dec-24, Volume: 58, Issue:24, 2015
Synthesis and structure-activity relationships of a novel and selective bone morphogenetic protein receptor (BMP) inhibitor derived from the pyrazolo[1.5-a]pyrimidine scaffold of dorsomorphin: the discovery of ML347 as an ALK2 versus ALK3 selective MLPCN Bioorganic & medicinal chemistry letters, , Jun-01, Volume: 23, Issue:11, 2013
In vivo structure-activity relationship study of dorsomorphin analogues identifies selective VEGF and BMP inhibitors.ACS chemical biology, , Feb-19, Volume: 5, Issue:2, 2010
The rational design of a novel potent analogue of the 5'-AMP-activated protein kinase inhibitor compound C with improved selectivity and cellular activity.Bioorganic & medicinal chemistry letters, , Nov-15, Volume: 20, Issue:22, 2010
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
Inhibition of colony-stimulating-factor-1 signaling in vivo with the orally bioavailable cFMS kinase inhibitor GW2580.Proceedings of the National Academy of Sciences of the United States of America, , Nov-01, Volume: 102, Issue:44, 2005
Pyridazinone derivatives displaying highly potent and selective inhibitory activities against c-Met tyrosine kinase.European journal of medicinal chemistry, , Jan-27, Volume: 108, 2016
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 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
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
Discovery of RAF265: A Potent mut-B-RAF Inhibitor for the Treatment of Metastatic Melanoma.ACS medicinal chemistry letters, , Sep-10, Volume: 6, Issue:9, 2015
Exploration of acridine scaffold as a potentially interesting scaffold for discovering novel multi-target VEGFR-2 and Src kinase inhibitors.Bioorganic & medicinal chemistry, , Jun-01, Volume: 19, Issue:11, 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
[no title available]Journal of medicinal chemistry, , 08-26, Volume: 64, Issue:16, 2021
De Novo Design at the Edge of Chaos.Journal of medicinal chemistry, , 05-12, Volume: 59, Issue:9, 2016
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
Pharmacophore modeling and virtual screening studies for new VEGFR-2 kinase inhibitors.European journal of medicinal chemistry, , Volume: 45, Issue:11, 2010
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
AMG 706, an oral, multikinase inhibitor that selectively targets vascular endothelial growth factor, platelet-derived growth factor, and kit receptors, potently inhibits angiogenesis and induces regression in tumor xenografts.Cancer research, , Sep-01, Volume: 66, Issue:17, 2006
Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/Journal of medicinal chemistry, , May-22, Volume: 57, Issue:10, 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
Discovery, synthesis, and in vivo activity of a new class of pyrazoloquinazolines as selective inhibitors of aurora B kinase.Journal of medicinal chemistry, , May-03, Volume: 50, Issue:9, 2007
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
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
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 "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
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
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
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
Discovery of a selective inhibitor of oncogenic B-Raf kinase with potent antimelanoma activity.Proceedings of the National Academy of Sciences of the United States of America, , Feb-26, Volume: 105, Issue:8, 2008
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
Discovery of N-[5-({2-[(cyclopropylcarbonyl)amino]imidazo[1,2-b]pyridazin-6-yl}oxy)-2-methylphenyl]-1,3-dimethyl-1H-pyrazole-5-carboxamide (TAK-593), a highly potent VEGFR2 kinase inhibitor.Bioorganic & medicinal chemistry, , Apr-15, Volume: 21, Issue:8, 2013
Vascular endothelial growth factor (VEGF) receptors: drugs and new inhibitors.Journal of medicinal chemistry, , Dec-27, Volume: 55, Issue:24, 2012
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
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
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 progress of small-molecules and degraders against BCR-ABL for the treatment of CML.European journal of medicinal chemistry, , Aug-05, Volume: 238, 2022
Discovery of Novel Benzothiazepinones as Irreversible Covalent Glycogen Synthase Kinase 3β Inhibitors for the Treatment of Acute Promyelocytic Leukemia.Journal of medicinal chemistry, , 06-10, Volume: 64, Issue:11, 2021
Global PROTAC Toolbox for Degrading BCR-ABL Overcomes Drug-Resistant Mutants and Adverse Effects.Journal of medicinal chemistry, , 08-13, Volume: 63, Issue:15, 2020
Discovery and anti-inflammatory evaluation of benzothiazepinones (BTZs) as novel non-ATP competitive inhibitors of glycogen synthase kinase-3β (GSK-3β).Bioorganic & medicinal chemistry, , 11-01, Volume: 26, Issue:20, 2018
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
Discovery of novel Ponatinib analogues for reducing KDR activity as potent FGFRs inhibitors.European journal of medicinal chemistry, , Jan-27, Volume: 126, 2017
An overview of the binding models of FGFR tyrosine kinases in complex with small molecule inhibitors.European journal of medicinal chemistry, , Jan-27, Volume: 126, 2017
Novel benzothiazinones (BTOs) as allosteric modulator or substrate competitive inhibitor of glycogen synthase kinase 3β (GSK-3β) with cellular activity of promoting glucose uptake.Bioorganic & medicinal chemistry letters, , Dec-15, Volume: 24, Issue:24, 2014
Discovery of Anilinopyrimidines as Dual Inhibitors of c-Met and VEGFR-2: Synthesis, SAR, and Cellular Activity.ACS medicinal chemistry letters, , Jun-12, Volume: 5, Issue:6, 2014
Identification of a Unique Resorcylic Acid Lactone Derivative That Targets Both Lymphangiogenesis and Angiogenesis.Journal of medicinal chemistry, , 10-24, Volume: 62, Issue:20, 2019
Identification of a potent 5-phenyl-thiazol-2-ylamine-based inhibitor of FLT3 with activity against drug resistance-conferring point mutations.European journal of medicinal chemistry, , Jul-15, Volume: 100, 2015
3-Phenyl-1H-5-pyrazolylamine-based derivatives as potent and efficacious inhibitors of FMS-like tyrosine kinase-3 (FLT3).Bioorganic & medicinal chemistry letters, , Jul-15, Volume: 22, Issue:14, 2012
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
Identification of N-(5-tert-butyl-isoxazol-3-yl)-N'-{4-[7-(2-morpholin-4-yl-ethoxy)imidazo[2,1-b][1,3]benzothiazol-2-yl]phenyl}urea dihydrochloride (AC220), a uniquely potent, selective, and efficacious FMS-like tyrosine kinase-3 (FLT3) inhibitor.Journal of medicinal chemistry, , Dec-10, Volume: 52, Issue:23, 2009
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
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, , 08-26, Volume: 64, Issue:16, 2021
Design, synthesis and biological evaluation of a series of novel 2-benzamide-4-(6-oxy-N-methyl-1-naphthamide)-pyridine derivatives as potent fibroblast growth factor receptor (FGFR) inhibitors.European journal of medicinal chemistry, , Jun-25, Volume: 154, 2018
An overview of the binding models of FGFR tyrosine kinases in complex with small molecule inhibitors.European journal of medicinal chemistry, , Jan-27, Volume: 126, 2017
[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
Targeting Rearranged during Transfection in Cancer: A Perspective on Small-Molecule Inhibitors and Their Clinical Development.Journal of medicinal chemistry, , 08-26, Volume: 64, Issue:16, 2021
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
Evolution in medicinal chemistry of sorafenib derivatives for hepatocellular carcinoma.European journal of medicinal chemistry, , Oct-01, Volume: 179, 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
Identification of novel NEuropean journal of medicinal chemistry, , Feb-25, Volume: 146, 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
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
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
Discovery of a highly potent, selective and novel CDK9 inhibitor as an anticancer drug candidate.Bioorganic & medicinal chemistry letters, , 08-01, Volume: 27, Issue:15, 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
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
The discovery of 2-substituted phenol quinazolines as potent RET kinase inhibitors with improved KDR selectivity.European journal of medicinal chemistry, , Apr-13, Volume: 112, 2016
A Pyrazolo[3,4-d]pyrimidin-4-amine Derivative Containing an Isoxazole Moiety Is a Selective and Potent Inhibitor of RET Gatekeeper Mutants.Journal of medicinal chemistry, , Jan-14, Volume: 59, Issue:1, 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
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 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 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
Design, synthesis and evaluation of highly selective pyridone-based class II MET inhibitors.Bioorganic & medicinal chemistry letters, , Aug-01, Volume: 24, Issue:15, 2014
Discovery of acyl ureas as highly selective small molecule CSF1R kinase inhibitors.Bioorganic & medicinal chemistry letters, , 10-15, Volume: 74, 2022
Discovery of vimseltinib (DCC-3014), a highly selective CSF1R switch-control kinase inhibitor, in clinical development for the treatment of Tenosynovial Giant Cell Tumor (TGCT).Bioorganic & medicinal chemistry letters, , 10-15, Volume: 74, 2022
Synthesis and structure-activity relationships of a novel and selective bone morphogenetic protein receptor (BMP) inhibitor derived from the pyrazolo[1.5-a]pyrimidine scaffold of dorsomorphin: the discovery of ML347 as an ALK2 versus ALK3 selective MLPCN Bioorganic & medicinal chemistry letters, , Jun-01, Volume: 23, Issue:11, 2013
In vivo structure-activity relationship study of dorsomorphin analogues identifies selective VEGF and BMP inhibitors.ACS chemical biology, , Feb-19, Volume: 5, Issue:2, 2010
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-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 evaluation of sulfonylurea-containing 4-phenoxyquinolines as highly selective c-Met kinase inhibitors.Bioorganic & medicinal chemistry, , 07-01, Volume: 27, Issue:13, 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
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
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
AXL Inhibitors in Cancer: A Medicinal Chemistry Perspective.Journal of medicinal chemistry, , 04-28, Volume: 59, Issue:8, 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
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
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 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, 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
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 antitumour activity of bisquinoline derivatives connected by 4-oxy-3-fluoroaniline moiety.European journal of medicinal chemistry, , Volume: 64, 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
From Structure Modification to Drug Launch: A Systematic Review of the Ongoing Development of Cyclin-Dependent Kinase Inhibitors for Multiple Cancer Therapy.Journal of medicinal chemistry, , 05-12, Volume: 65, Issue:9, 2022
Cyclin dependent kinase (CDK) inhibitors as anticancer drugs.Bioorganic & medicinal chemistry letters, , Sep-01, Volume: 25, Issue:17, 2015
Thienopyridine ureas as dual inhibitors of the VEGF and Aurora kinase families.Bioorganic & medicinal chemistry letters, , May-01, Volume: 22, Issue:9, 2012
Pyrazole diaminopyrimidines as dual inhibitors of KDR and Aurora B kinases.Bioorganic & medicinal chemistry letters, , Jul-15, Volume: 22, Issue:14, 2012
Discovery of 1,6-Naphthyridin-2(1Journal of medicinal chemistry, , 06-09, Volume: 65, Issue:11, 2022
Discovery of 3-(5'-Substituted)-Benzimidazole-5-(1-(3,5-dichloropyridin-4-yl)ethoxy)-1H-indazoles as Potent Fibroblast Growth Factor Receptor Inhibitors: Design, Synthesis, and Biological Evaluation.Journal of medicinal chemistry, , 07-28, Volume: 59, Issue:14, 2016
[no title available]Journal of medicinal chemistry, , 12-26, Volume: 62, Issue:24, 2019
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
Discovery and optimization of novel pyrazole-benzimidazole CPL304110, as a potent and selective inhibitor of fibroblast growth factor receptors FGFR (1-3).European journal of medicinal chemistry, , Jan-15, Volume: 210, 2021
Discovery and Development of a Series of Pyrazolo[3,4-Journal of medicinal chemistry, , 08-22, Volume: 62, Issue:16, 2019
Design, synthesis and biological evaluation of pyrazolylaminoquinazoline derivatives as highly potent pan-fibroblast growth factor receptor inhibitors.Bioorganic & medicinal chemistry letters, , 06-01, Volume: 26, Issue:11, 2016
Discovery of 3-(5'-Substituted)-Benzimidazole-5-(1-(3,5-dichloropyridin-4-yl)ethoxy)-1H-indazoles as Potent Fibroblast Growth Factor Receptor Inhibitors: Design, Synthesis, and Biological Evaluation.Journal of medicinal chemistry, , 07-28, Volume: 59, Issue:14, 2016
Discovery of Substituted 1H-Pyrazolo[3,4-b]pyridine Derivatives as Potent and Selective FGFR Kinase Inhibitors.ACS medicinal chemistry letters, , Jun-09, Volume: 7, Issue:6, 2016
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
Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/Journal of medicinal chemistry, , May-22, Volume: 57, Issue:10, 2014
Targeting Rearranged during Transfection in Cancer: A Perspective on Small-Molecule Inhibitors and Their Clinical Development.Journal of medicinal chemistry, , 08-26, Volume: 64, Issue:16, 2021
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
An overview of the binding models of FGFR tyrosine kinases in complex with small molecule inhibitors.European journal of medicinal chemistry, , Jan-27, Volume: 126, 2017
Discovery of [5-Amino-1-(2-methyl-3H-benzimidazol-5-yl)pyrazol-4-yl]-(1H-indol-2-yl)methanone (CH5183284/Debio 1347), An Orally Available and Selective Fibroblast Growth Factor Receptor (FGFR) Inhibitor.Journal of medicinal chemistry, , 12-08, Volume: 59, Issue:23, 2016
Discovery of 1,6-Naphthyridin-2(1Journal of medicinal chemistry, , 06-09, Volume: 65, Issue:11, 2022
Structure-based drug design of 1,3,5-triazine and pyrimidine derivatives as novel FGFR3 inhibitors with high selectivity over VEGFR2.Bioorganic & medicinal chemistry, , 05-15, Volume: 28, Issue:10, 2020
Fibroblast Growth Factor Receptor 4 (FGFR4) Selective Inhibitors as Hepatocellular Carcinoma Therapy: Advances and Prospects.Journal of medicinal chemistry, , 03-28, Volume: 62, Issue:6, 2019
[no title available],
Structure-based drug design of 1,3,5-triazine and pyrimidine derivatives as novel FGFR3 inhibitors with high selectivity over VEGFR2.Bioorganic & medicinal chemistry, , 05-15, Volume: 28, Issue:10, 2020
An overview of the binding models of FGFR tyrosine kinases in complex with small molecule inhibitors.European journal of medicinal chemistry, , Jan-27, Volume: 126, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
Design, structure-activity relationships and in vivo characterization of 4-amino-3-benzimidazol-2-ylhydroquinolin-2-ones: a novel class of receptor tyrosine kinase inhibitors.Journal of medicinal chemistry, , Jan-22, Volume: 52, Issue:2, 2009
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
Design, synthesis, and biological evaluation of novel pyrazolo [3,4-d]pyrimidine derivatives as potent PLK4 inhibitors for the treatment of TRIM37-amplified breast cancer.European journal of medicinal chemistry, , Aug-05, Volume: 238, 2022
Discovery of a highly potent, orally active mitosis/angiogenesis inhibitor r1530 for the treatment of solid tumors.ACS medicinal chemistry letters, , Feb-14, Volume: 4, Issue:2, 2013
Structural modifications of indolinones bearing a pyrrole moiety and discovery of a multi-kinase inhibitor with potent antitumor activity.Bioorganic & medicinal chemistry, , 06-01, Volume: 28, Issue:11, 2020
Evolution in medicinal chemistry of sorafenib derivatives for hepatocellular carcinoma.European journal of medicinal chemistry, , Oct-01, Volume: 179, 2019
Discovery of Novel Potent VEGFR-2 Inhibitors Exerting Significant Antiproliferative Activity against Cancer Cell Lines.Journal of medicinal chemistry, , 01-11, Volume: 61, Issue:1, 2018
Discovery of Indolinone-Based Multikinase Inhibitors as Potential Therapeutics for Idiopathic Pulmonary Fibrosis.ACS medicinal chemistry letters, , Nov-09, Volume: 8, Issue:11, 2017
Novel 6-methoxycarbonyl indolinones bearing a pyrrole Mannich base moiety as angiokinase inhibitors.Bioorganic & medicinal chemistry, , 03-15, Volume: 25, Issue:6, 2017
Novel methyl indolinone-6-carboxylates containing an indole moiety as angiokinase inhibitors.European journal of medicinal chemistry, , Oct-20, Volume: 139, 2017
Naphthalimides exhibit in vitro antiproliferative and antiangiogenic activities by inhibiting both topoisomerase II (topo II) and receptor tyrosine kinases (RTKs).European journal of medicinal chemistry, , Volume: 65, 2013
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
Design, synthesis, and evaluation of indolinones as triple angiokinase inhibitors and the discovery of a highly specific 6-methoxycarbonyl-substituted indolinone (BIBF 1120).Journal of medicinal chemistry, , Jul-23, Volume: 52, Issue:14, 2009
BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy.Cancer research, , Jun-15, Volume: 68, Issue:12, 2008
Enables
This protein enables 12 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] |
| transmembrane receptor protein tyrosine kinase activity | molecular function | Combining with a signal and transmitting the signal from one side of the membrane to the other to initiate a change in cell activity by catalysis of the reaction: ATP + a protein-L-tyrosine = ADP + a protein-L-tyrosine phosphate. [EC:2.7.10.1, GOC:mah] |
| vascular endothelial growth factor receptor activity | molecular function | Combining with a vascular endothelial growth factor (VEGF) receptor ligand and transmitting the signal across the plasma membrane to initiate a change in cell activity. [GOC:mah, GOC:signaling, PMID:19909239] |
| integrin binding | molecular function | Binding to an integrin. [GOC:ceb] |
| 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] |
| coreceptor activity | molecular function | Combining with an extracellular or intracellular messenger, and in cooperation with a nearby primary receptor, initiating a change in cell activity. [GOC:go_curators] |
| growth factor binding | molecular function | Binding to a growth factor, proteins or polypeptides that stimulate a cell or organism to grow or proliferate. [GOC:curators] |
| vascular endothelial growth factor binding | molecular function | Binding to a vascular endothelial growth factor. [PMID:17470632] |
| identical protein binding | molecular function | Binding to an identical protein or proteins. [GOC:jl] |
| cadherin binding | molecular function | Binding to cadherin, a type I membrane protein involved in cell adhesion. [GOC:bf] |
| Hsp90 protein binding | molecular function | Binding to Hsp90 proteins, any of a group of heat shock proteins around 90kDa in size. [GOC:ai] |
Located In
This protein is located in 12 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] |
| nucleus | cellular component | A membrane-bounded organelle of eukaryotic cells in which chromosomes are housed and replicated. In most cells, the nucleus contains all of the cell's chromosomes except the organellar chromosomes, and is the site of RNA synthesis and processing. In some species, or in specialized cell types, RNA metabolism or DNA replication may be absent. [GOC:go_curators] |
| endosome | cellular component | A vacuole to which materials ingested by endocytosis are delivered. [ISBN:0198506732, PMID:19696797] |
| early endosome | cellular component | A membrane-bounded organelle that receives incoming material from primary endocytic vesicles that have been generated by clathrin-dependent and clathrin-independent endocytosis; vesicles fuse with the early endosome to deliver cargo for sorting into recycling or degradation pathways. [GOC:mah, NIF_Subcellular:nlx_subcell_20090701, PMID:19696797] |
| endoplasmic reticulum | cellular component | The irregular network of unit membranes, visible only by electron microscopy, that occurs in the cytoplasm of many eukaryotic cells. The membranes form a complex meshwork of tubular channels, which are often expanded into slitlike cavities called cisternae. The ER takes two forms, rough (or granular), with ribosomes adhering to the outer surface, and smooth (with no ribosomes attached). [ISBN:0198506732] |
| Golgi apparatus | cellular component | A membrane-bound cytoplasmic organelle of the endomembrane system that further processes the core oligosaccharides (e.g. N-glycans) added to proteins in the endoplasmic reticulum and packages them into membrane-bound vesicles. The Golgi apparatus operates at the intersection of the secretory, lysosomal, and endocytic pathways. [ISBN:0198506732] |
| 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] |
| external side of plasma membrane | cellular component | The leaflet of the plasma membrane that faces away from the cytoplasm and any proteins embedded or anchored in it or attached to its surface. [GOC:dos, GOC:tb] |
| cell junction | cellular component | A cellular component that forms a specialized region of connection between two or more cells, or between a cell and the extracellular matrix, or between two membrane-bound components of a cell, such as flagella. [GOC:aruk, GOC:bc, GOC:mah, http://www.vivo.colostate.edu/hbooks/cmb/cells/pmemb/junctions_a.html, ISBN:0198506732, PMID:26820516, PMID:28096264] |
| membrane raft | cellular component | Any of the small (10-200 nm), heterogeneous, highly dynamic, sterol- and sphingolipid-enriched membrane domains that compartmentalize cellular processes. Small rafts can sometimes be stabilized to form larger platforms through protein-protein and protein-lipid interactions. [PMID:16645198, PMID:20044567] |
| anchoring junction | cellular component | A cell junction that mechanically attaches a cell (and its cytoskeleton) to neighboring cells or to the extracellular matrix. [ISBN:0815332181] |
| sorting endosome | cellular component | A multivesicular body surrounded by and connected with multiple tubular compartments with associated vesicles. [NIF_Subcellular:sao1028571114] |
Active In
This protein is active in 1 target(s):
| Target | Category | Definition |
|---|
| 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 59 target(s):
| Target | Category | Definition |
|---|
| angiogenesis | biological process | Blood vessel formation when new vessels emerge from the proliferation of pre-existing blood vessels. [ISBN:0878932453] |
| ovarian follicle development | biological process | The process whose specific outcome is the progression of the ovarian follicle over time, from its formation to the mature structure. [https://www.ncbi.nlm.nih.gov/books/NBK279054/] |
| vasculogenesis | biological process | The differentiation of endothelial cells from progenitor cells during blood vessel development, and the de novo formation of blood vessels and tubes. [PMID:8999798] |
| positive regulation of protein phosphorylation | biological process | Any process that activates or increases the frequency, rate or extent of addition of phosphate groups to amino acids within a protein. [GOC:hjd] |
| positive regulation of endothelial cell proliferation | biological process | Any process that activates or increases the rate or extent of endothelial cell proliferation. [GOC:add] |
| lymph vessel development | biological process | The process whose specific outcome is the progression of a lymph vessel over time, from its formation to the mature structure. [GOC:dph, UBERON:0001473] |
| cell migration involved in sprouting angiogenesis | biological process | The orderly movement of endothelial cells into the extracellular matrix in order to form new blood vessels involved in sprouting angiogenesis. [PMID:16391003] |
| positive regulation of mesenchymal cell proliferation | biological process | The process of activating or increasing the rate or extent of mesenchymal cell proliferation. Mesenchymal cells are loosely organized embryonic cells. [GOC:dph] |
| epithelial cell maturation | biological process | The developmental process, independent of morphogenetic (shape) change, that is required for an epithelial cell to attain its fully functional state. An epithelial cell is a cell usually found in a two-dimensional sheet with a free surface. [GOC:dph] |
| endocardium development | biological process | The process whose specific outcome is the progression of the endocardium over time, from its formation to the mature structure. The endocardium is an anatomical structure comprised of an endothelium and an extracellular matrix that forms the innermost layer of tissue of the heart, and lines the heart chambers. [GOC:mtg_heart] |
| endothelium development | biological process | The process whose specific outcome is the progression of an endothelium over time, from its formation to the mature structure. Endothelium refers to the layer of cells lining blood vessels, lymphatics, the heart, and serous cavities, and is derived from bone marrow or mesoderm. Corneal endothelium is a special case, derived from neural crest cells. [GOC:mtg_heart] |
| 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] |
| positive regulation of cell population proliferation | biological process | Any process that activates or increases the rate or extent of cell proliferation. [GOC:go_curators] |
| regulation of cell shape | biological process | Any process that modulates the surface configuration of a cell. [GOC:dph, GOC:go_curators, GOC:tb] |
| mesenchymal cell proliferation | biological process | The multiplication or reproduction of cells, resulting in the expansion of a mesenchymal cell population. A mesenchymal cell is a cell that normally gives rise to other cells that are organized as three-dimensional masses, rather than sheets. [GOC:dph, GOC:tb] |
| positive regulation of endothelial cell migration | biological process | Any process that increases the rate, frequency, or extent of the orderly movement of an endothelial cell into the extracellular matrix to form an endothelium. [GOC:BHF, GOC:dph, GOC:tb] |
| negative regulation of gene expression | biological process | Any process that decreases the frequency, rate or extent of gene expression. Gene expression is the process in which a gene's coding sequence is converted into a mature gene product (protein or RNA). [GOC:txnOH-2018] |
| peptidyl-tyrosine phosphorylation | biological process | The phosphorylation of peptidyl-tyrosine to form peptidyl-O4'-phospho-L-tyrosine. [RESID:AA0039] |
| positive regulation of cell migration | biological process | Any process that activates or increases the frequency, rate or extent of cell migration. [GOC:go_curators] |
| positive regulation of BMP signaling pathway | biological process | Any process that activates or increases the frequency, rate or extent of BMP signaling pathway activity. [GOC:go_curators] |
| embryonic hemopoiesis | biological process | The stages of blood cell formation that take place within the embryo. [GOC:bf] |
| cellular response to vascular endothelial growth factor stimulus | biological process | Any process that results in a change in state or activity of a cell (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a vascular endothelial growth factor stimulus. [GOC:BHF, GOC:rl, PMID:18440775] |
| vascular endothelial growth factor receptor-2 signaling pathway | biological process | The series of molecular signals initiated by a ligand binding to a vascular endothelial growth factor receptor-2 (VEGFR-2) on the surface of a target cell, and ending with the regulation of a downstream cellular process, e.g. transcription. [GOC:bf, GOC:uh, PMID:12967471, Wikipedia:Kinase_insert_domain_receptor, Wikipedia:VEGF_receptors] |
| peptidyl-tyrosine autophosphorylation | biological process | The phosphorylation by a protein of one or more of its own tyrosine amino acid residues, or a tyrosine residue on an identical protein. [PMID:10037737, PMID:10068444, PMID:10940390] |
| vascular endothelial growth factor signaling pathway | biological process | The series of molecular signals initiated by vascular endothelial growth factor (VEGF) binding its receptor on the surface of the target cell, and ending with the regulation of a downstream cellular process, e.g. transcription. [GOC:signaling, PMID:17470632] |
| surfactant homeostasis | biological process | Any process involved in the maintenance of a steady-state level of a surface-active agent that maintains the surface tension of a liquid. [PMID:23708874, PMID:9751757] |
| positive regulation of MAPK cascade | biological process | Any process that activates or increases the frequency, rate or extent of signal transduction mediated by the MAPK cascade. [GOC:go_curators] |
| negative regulation of neuron apoptotic process | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of cell death by apoptotic process in neurons. [GOC:go_curators, GOC:mtg_apoptosis] |
| positive regulation of blood vessel endothelial cell migration | biological process | Any process that activates or increases the frequency, rate or extent of the migration of the endothelial cells of blood vessels. [GOC:go_curators] |
| cell fate commitment | biological process | The cellular developmental process by which a cell establishes the intrinsic character of a cell or tissue region irreversibly committing it to a particular fate. [ISBN:0716731185] |
| positive regulation of angiogenesis | biological process | Any process that activates or increases angiogenesis. [GOC:go_curators] |
| protein autophosphorylation | biological process | The phosphorylation by a protein of one or more of its own amino acid residues (cis-autophosphorylation), or residues on an identical protein (trans-autophosphorylation). [ISBN:0198506732] |
| vascular endothelial growth factor receptor signaling pathway | biological process | The series of molecular signals initiated by a ligand binding to a vascular endothelial growth factor receptor (VEGFR) on the surface of the target cell, and ending with the regulation of a downstream cellular process, e.g. transcription. [GOC:ceb, GOC:signaling] |
| lung alveolus development | biological process | The process whose specific outcome is the progression of the alveolus over time, from its formation to the mature structure. The alveolus is a sac for holding air in the lungs; formed by the terminal dilation of air passageways. [GOC:mtg_lung, PMID:9751757] |
| post-embryonic camera-type eye morphogenesis | biological process | The process in which the anatomical structures of the eye are generated and organized during post-embryonic development. [GOC:jid, GOC:mtg_transport, ISBN:0815340729] |
| epithelial cell proliferation | biological process | The multiplication or reproduction of epithelial cells, resulting in the expansion of a cell population. Epithelial cells make up the epithelium, the covering of internal and external surfaces of the body, including the lining of vessels and other small cavities. It consists of cells joined by small amounts of cementing substances. [ISBN:0721662544] |
| positive regulation of positive chemotaxis | biological process | Any process that activates or increases the frequency, rate or extent of the directed movement of a motile cell or organism towards a higher concentration in a concentration gradient of a specific chemical. [GOC:ai] |
| positive regulation of nitric-oxide synthase biosynthetic process | biological process | Any process that activates or increases the frequency, rate or extent of the chemical reactions and pathways resulting in the formation of a nitric oxide synthase enzyme. [GOC:ai] |
| positive regulation of focal adhesion assembly | biological process | Any process that activates or increases the frequency, rate or extent of focal adhesion assembly, the establishment and maturation of focal adhesions. [GOC:ai] |
| positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transduction | biological process | Any process that activates or increases the frequency, rate or extent of phosphatidylinositol 3-kinase/protein kinase B signal transduction. [GOC:ai] |
| calcium ion homeostasis | biological process | Any process involved in the maintenance of an internal steady state of calcium ions within an organism or cell. [GOC:ceb, GOC:jid, GOC:mah] |
| blood vessel endothelial cell differentiation | biological process | The process in which a relatively unspecialized cell acquires specialized features of a blood vessel endothelial cell, a thin flattened cell that lines the inside surfaces of blood vessels. [GOC:dph, GOC:sdb_2009, GOC:tb] |
| vascular wound healing | biological process | Blood vessel formation when new vessels emerge from the proliferation of pre-existing blood vessels and contribute to the series of events that restore integrity to damaged vasculature. [GOC:BHF, GOC:dph] |
| positive regulation of ERK1 and ERK2 cascade | biological process | Any process that activates or increases the frequency, rate or extent of signal transduction mediated by the ERK1 and ERK2 cascade. [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] |
| stem cell proliferation | biological process | The multiplication or reproduction of stem cells, resulting in the expansion of a stem cell population. A stem cell is a cell that retains the ability to divide and proliferate throughout life to provide progenitor cells that can differentiate into specialized cells. [GOC:mtg_kidney_jan10] |
| positive regulation of cell migration involved in sprouting angiogenesis | biological process | Any process that increases the frequency, rate or extent of cell migration involved in sprouting angiogenesis. Cell migration involved in sprouting angiogenesis is the orderly movement of endothelial cells into the extracellular matrix in order to form new blood vessels contributing to the process of sprouting angiogenesis. [GOC:BHF, GOC:dph, GOC:rl, GOC:tb] |
| regulation of hematopoietic progenitor cell differentiation | biological process | Any process that modulates the frequency, rate or extent of hematopoietic progenitor cell differentiation. [GOC:BHF, GOC:rl, GOC:TermGenie] |
| regulation of bone development | biological process | Any process that modulates the frequency, rate or extent of bone development. [GO_REF:0000058, GOC:mr, GOC:TermGenie, PMID:22510437] |
| cellular response to hydrogen sulfide | biological process | Any process that results in a change in state or activity of a cell (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a hydrogen sulfide stimulus. [GO_REF:0000071, GOC:TermGenie, PMID:24012591] |
| negative regulation of endothelial cell apoptotic process | biological process | Any process that stops, prevents or reduces the frequency, rate or extent of endothelial cell apoptotic process. [GOC:BHF, GOC:mah, GOC:mtg_apoptosis] |
| positive regulation of stem cell proliferation | biological process | Any process that activates or increases the frequency, rate or extent of stem cell proliferation. [GOC:dph] |
| 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] |
| positive regulation of vasculogenesis | biological process | Any process that activates or increases the frequency, rate or extent of vasculogenesis. [GOC:obol] |
| regulation of MAPK cascade | biological process | Any process that modulates the frequency, rate or extent of signal transduction mediated by the MAP kinase (MAPK) cascade. [GOC:go_curators] |
| 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] |
| 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] |
| endothelial cell differentiation | biological process | The process in which a mesodermal, bone marrow or neural crest cell acquires specialized features of an endothelial cell, a thin flattened cell. A layer of such cells lines the inside surfaces of body cavities, blood vessels, and lymph vessels, making up the endothelium. [CL:0000115, GOC:go_curators] |
| 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] |