Proteins > Epidermal growth factor receptor
Page last updated: 2024-08-07 15:31:23
Epidermal growth factor receptor
An epidermal growth factor receptor that is encoded in the genome of human. [PRO:DNx, UniProtKB:P00533]
Synonyms
EC 2.7.10.1;
Proto-oncogene c-ErbB-1;
Receptor tyrosine-protein kinase erbB-1
Research
Bioassay Publications (564)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 1 (0.18) | 18.7374 |
| 1990's | 37 (6.56) | 18.2507 |
| 2000's | 117 (20.74) | 29.6817 |
| 2010's | 298 (52.84) | 24.3611 |
| 2020's | 111 (19.68) | 2.80 |
Compounds (428)
Drugs with Inhibition Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| catechol | Homo sapiens (human) | IC50 | 26.0430 | 1 | 0 |
| dihydroxyphenylalanine | Homo sapiens (human) | IC50 | 900.0000 | 1 | 1 |
| pyrogallol | Homo sapiens (human) | IC50 | 1.2300 | 1 | 0 |
| 2-(6-methoxy-2-naphthalenyl)propanoic acid | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| pd 173074 | Homo sapiens (human) | IC50 | 50.0000 | 1 | 1 |
| cgp 52411 | Homo sapiens (human) | IC50 | 1.7000 | 3 | 3 |
| cgp 52411 | Homo sapiens (human) | Ki | 0.1600 | 1 | 1 |
| ag 127 | Homo sapiens (human) | IC50 | 450.0000 | 1 | 1 |
| ag 127 | Homo sapiens (human) | Ki | 150.0000 | 2 | 2 |
| ag 1295 | Homo sapiens (human) | IC50 | 6.2000 | 1 | 1 |
| rtki cpd | Homo sapiens (human) | IC50 | 0.1152 | 9 | 9 |
| tyrphostin a23 | Homo sapiens (human) | IC50 | 36.6667 | 3 | 3 |
| tyrphostin a23 | Homo sapiens (human) | Ki | 11.0000 | 2 | 2 |
| tyrphostin 25 | Homo sapiens (human) | IC50 | 3.0000 | 1 | 1 |
| tyrphostin 25 | Homo sapiens (human) | Ki | 1.0000 | 2 | 2 |
| tyrphostin a1 | Homo sapiens (human) | IC50 | 1,250.0000 | 1 | 1 |
| tyrphostin a1 | Homo sapiens (human) | Ki | 400.0000 | 2 | 2 |
| aspirin | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| astemizole | Homo sapiens (human) | IC50 | 6.0570 | 1 | 0 |
| bisindolylmaleimide iv | Homo sapiens (human) | IC50 | 50.0000 | 1 | 1 |
| bithionol | Homo sapiens (human) | IC50 | 0.6140 | 1 | 0 |
| candesartan | Homo sapiens (human) | IC50 | 3.2769 | 1 | 0 |
| chlorpromazine | Homo sapiens (human) | IC50 | 28.8680 | 1 | 0 |
| ciglitazone | Homo sapiens (human) | IC50 | 4.6550 | 1 | 0 |
| cl 387785 | Homo sapiens (human) | IC50 | 0.0456 | 8 | 9 |
| clotrimazole | Homo sapiens (human) | IC50 | 69.4210 | 1 | 0 |
| ebastine | Homo sapiens (human) | IC50 | 0.5591 | 1 | 0 |
| econazole | Homo sapiens (human) | IC50 | 32.4040 | 1 | 0 |
| fluphenazine | Homo sapiens (human) | IC50 | 40.1070 | 1 | 0 |
| fluorouracil | Homo sapiens (human) | IC50 | 0.3200 | 1 | 1 |
| hexachlorophene | Homo sapiens (human) | IC50 | 0.7486 | 1 | 0 |
| ibuprofen | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| indirubin-5-sulfonate | Homo sapiens (human) | IC50 | 6.8000 | 1 | 6 |
| indomethacin | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| iodoquinol | Homo sapiens (human) | IC50 | 1.8890 | 1 | 0 |
| 1-(2-naphthalenyl)-2-propen-1-one | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| ketoprofen | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| lavendustin a | Homo sapiens (human) | IC50 | 4.1000 | 1 | 1 |
| 2-hydroxy-5-(2,5-dihydrobenzyl)aminobenzoic acid | Homo sapiens (human) | IC50 | 37.4160 | 5 | 5 |
| miconazole | Homo sapiens (human) | IC50 | 29.2560 | 1 | 0 |
| mitoxantrone | Homo sapiens (human) | IC50 | 5.3859 | 1 | 0 |
| niclosamide | Homo sapiens (human) | IC50 | 10.5000 | 1 | 1 |
| olomoucine | Homo sapiens (human) | IC50 | 440.0000 | 1 | 1 |
| pd 153035 | Homo sapiens (human) | IC50 | 3.9091 | 49 | 53 |
| pd 153035 | Homo sapiens (human) | Ki | 0.0000 | 1 | 1 |
| pd 158780 | Homo sapiens (human) | IC50 | 1.1857 | 11 | 11 |
| pd168393 | Homo sapiens (human) | IC50 | 0.0143 | 26 | 28 |
| perhexiline | Homo sapiens (human) | IC50 | 1.4852 | 1 | 0 |
| phloretin | Homo sapiens (human) | IC50 | 25,000.0000 | 1 | 1 |
| ag 1879 | Homo sapiens (human) | IC50 | 0.4800 | 1 | 1 |
| ag 1879 | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| 1-phenyl-4-pyrazolo[3,4-d]pyrimidinamine | Homo sapiens (human) | IC50 | 2.7000 | 1 | 1 |
| sb 239063 | Homo sapiens (human) | IC50 | 0.0830 | 1 | 1 |
| imatinib | Homo sapiens (human) | IC50 | 0.0001 | 1 | 1 |
| vorinostat | Homo sapiens (human) | IC50 | 0.4560 | 2 | 2 |
| sulforaphane | Homo sapiens (human) | IC50 | 9.0000 | 1 | 1 |
| terfenadine | Homo sapiens (human) | IC50 | 3.5660 | 1 | 0 |
| thioridazine | Homo sapiens (human) | IC50 | 2.9470 | 1 | 0 |
| tyrphostin a9 | Homo sapiens (human) | IC50 | 460.0000 | 1 | 1 |
| tyrphostin a9 | Homo sapiens (human) | Ki | 155.0000 | 2 | 2 |
| ici 204,219 | Homo sapiens (human) | IC50 | 5.7510 | 1 | 0 |
| levodopa | Homo sapiens (human) | IC50 | 451.4400 | 2 | 1 |
| salicylanilide | Homo sapiens (human) | IC50 | 50.0000 | 1 | 1 |
| sterogenol | Homo sapiens (human) | IC50 | 3.4720 | 1 | 0 |
| quinazolines | Homo sapiens (human) | IC50 | 0.0270 | 2 | 2 |
| indirubin | Homo sapiens (human) | IC50 | 2.0000 | 1 | 1 |
| oleanolic acid | Homo sapiens (human) | IC50 | 20.0000 | 3 | 3 |
| gentian violet | Homo sapiens (human) | IC50 | 0.4730 | 1 | 0 |
| tribromsalan | Homo sapiens (human) | IC50 | 15.7585 | 2 | 1 |
| 4-octylphenol | Homo sapiens (human) | IC50 | 16.2190 | 1 | 0 |
| proquazone | Homo sapiens (human) | IC50 | 0.0020 | 1 | 1 |
| paclitaxel | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| dobutamine | Homo sapiens (human) | IC50 | 5.5510 | 1 | 0 |
| methyldopa | Homo sapiens (human) | IC50 | 5.2280 | 1 | 0 |
| closantel | Homo sapiens (human) | IC50 | 0.5640 | 1 | 0 |
| staurosporine | Homo sapiens (human) | IC50 | 5.4744 | 33 | 33 |
| adenosine | Homo sapiens (human) | IC50 | 195.0000 | 1 | 1 |
| nelfinavir | Homo sapiens (human) | IC50 | 55.6290 | 1 | 0 |
| delphinidin | Homo sapiens (human) | IC50 | 0.0063 | 1 | 1 |
| hederagenin | Homo sapiens (human) | IC50 | 20.0000 | 3 | 3 |
| 4'-bromosalicylanilide | Homo sapiens (human) | IC50 | 50.0000 | 1 | 1 |
| tyrphostin 8 | Homo sapiens (human) | IC50 | 560.0000 | 1 | 1 |
| tyrphostin 8 | Homo sapiens (human) | Ki | 160.0000 | 2 | 2 |
| u 74006f | Homo sapiens (human) | IC50 | 20.3970 | 1 | 0 |
| gefitinib | Homo sapiens (human) | IC50 | 1.3292 | 195 | 194 |
| gefitinib | Homo sapiens (human) | Ki | 0.0004 | 1 | 1 |
| 4-(3-chloroanilino)quinazoline | Homo sapiens (human) | IC50 | 0.5402 | 8 | 8 |
| (hydroxy-2-naphthalenylmethyl)phosphonic acid | Homo sapiens (human) | IC50 | 225.0000 | 2 | 2 |
| ptk 787 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| vatalanib | Homo sapiens (human) | IC50 | 6.8192 | 3 | 3 |
| canertinib dihydrochloride | Homo sapiens (human) | IC50 | 0.0036 | 7 | 7 |
| canertinib | Homo sapiens (human) | IC50 | 0.0068 | 24 | 24 |
| canertinib | Homo sapiens (human) | Ki | 0.0001 | 1 | 1 |
| birb 796 | Homo sapiens (human) | IC50 | 11.9000 | 2 | 2 |
| Serotonin hydrochloride | Homo sapiens (human) | IC50 | 50.0000 | 1 | 1 |
| sb 203580 | Homo sapiens (human) | IC50 | 64.5000 | 2 | 2 |
| erlotinib | Homo sapiens (human) | IC50 | 3.9784 | 146 | 148 |
| erlotinib | Homo sapiens (human) | Ki | 0.0475 | 13 | 13 |
| erlotinib hydrochloride | Homo sapiens (human) | IC50 | 0.1683 | 3 | 3 |
| lapatinib | Homo sapiens (human) | IC50 | 6.5561 | 67 | 70 |
| lapatinib | Homo sapiens (human) | Ki | 0.0030 | 1 | 1 |
| sorafenib | Homo sapiens (human) | IC50 | 6.4377 | 8 | 8 |
| hematoxylin | Homo sapiens (human) | IC50 | 3.4000 | 1 | 1 |
| pd 166326 | Homo sapiens (human) | IC50 | 0.0930 | 3 | 6 |
| shikonin | Homo sapiens (human) | IC50 | 0.1392 | 1 | 1 |
| 2-chloro-N-(5-methyl-3-isoxazolyl)acetamide | Homo sapiens (human) | IC50 | 0.1060 | 1 | 1 |
| N-benzylquinazolin-4-amine | Homo sapiens (human) | IC50 | 0.3200 | 2 | 2 |
| trans-4-coumaric acid | Homo sapiens (human) | IC50 | 3,000.0000 | 1 | 1 |
| trans-4-coumaric acid | Homo sapiens (human) | Ki | 1,000.0000 | 2 | 2 |
| alpha-cyanocinnamate | Homo sapiens (human) | IC50 | 850.0000 | 1 | 1 |
| alpha-cyanocinnamate | Homo sapiens (human) | Ki | 1,675.0000 | 2 | 2 |
| N-[3-(trifluoromethyl)phenyl]-4-quinazolinamine | Homo sapiens (human) | IC50 | 0.5794 | 5 | 5 |
| (1S,2R)-2-(octylamino)-1-[4-(propan-2-ylthio)phenyl]-1-propanol | Homo sapiens (human) | IC50 | 0.7944 | 1 | 0 |
| ag-213 | Homo sapiens (human) | IC50 | 3.2220 | 5 | 5 |
| ag-213 | Homo sapiens (human) | Ki | 0.8500 | 2 | 2 |
| caffeic acid | Homo sapiens (human) | IC50 | 1,100.0000 | 2 | 2 |
| caffeic acid | Homo sapiens (human) | Ki | 400.0000 | 2 | 2 |
| N-(3-cyano-4,5,6,7-tetrahydro-1-benzothiophen-2-yl)-1-naphthalenecarboxamide | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| sulindac | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| enclomiphene | Homo sapiens (human) | IC50 | 1.0500 | 1 | 0 |
| tamoxifen | Homo sapiens (human) | IC50 | 3.5530 | 1 | 0 |
| cgp 74514a | Homo sapiens (human) | IC50 | 3.5500 | 1 | 2 |
| bms 387032 | Homo sapiens (human) | IC50 | 25.0000 | 1 | 1 |
| rtki cpd | Homo sapiens (human) | IC50 | 0.0584 | 3 | 3 |
| tandutinib | Homo sapiens (human) | IC50 | 30.0000 | 1 | 1 |
| dasatinib | Homo sapiens (human) | IC50 | 0.7144 | 5 | 5 |
| zd 6474 | Homo sapiens (human) | IC50 | 0.9316 | 21 | 24 |
| gtp 14564 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| quercetin | Homo sapiens (human) | IC50 | 68.6000 | 3 | 3 |
| daphnetin | Homo sapiens (human) | IC50 | 7.6700 | 1 | 1 |
| genistein | Homo sapiens (human) | IC50 | 29.7169 | 7 | 13 |
| montelukast | Homo sapiens (human) | IC50 | 3.1970 | 1 | 0 |
| butein | Homo sapiens (human) | IC50 | 12.0000 | 2 | 2 |
| caffeic acid phenethyl ester | Homo sapiens (human) | IC50 | 1.0050 | 1 | 0 |
| tectorigenin | Homo sapiens (human) | IC50 | 3.3000 | 1 | 1 |
| ellagic acid | Homo sapiens (human) | IC50 | 0.6900 | 1 | 1 |
| alvocidib | Homo sapiens (human) | IC50 | 16.8667 | 3 | 3 |
| as 605240 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| su 5402 | Homo sapiens (human) | IC50 | 43.2092 | 6 | 13 |
| su 9516 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| pd 180970 | Homo sapiens (human) | IC50 | 0.3900 | 1 | 1 |
| pd 166285 | Homo sapiens (human) | IC50 | 6.3750 | 4 | 7 |
| arcyriaflavin a | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
| pd 089828 | Homo sapiens (human) | IC50 | 0.4500 | 1 | 1 |
| pd 166866 | Homo sapiens (human) | IC50 | 50.0000 | 2 | 2 |
| pd 161570 | Homo sapiens (human) | IC50 | 0.3400 | 3 | 3 |
| erbstatin | Homo sapiens (human) | IC50 | 8.0000 | 4 | 4 |
| AG-370 | Homo sapiens (human) | IC50 | 566.6667 | 3 | 3 |
| ag 538 | Homo sapiens (human) | IC50 | 3.0652 | 8 | 8 |
| ag 99 | Homo sapiens (human) | IC50 | 8.7185 | 9 | 9 |
| ag 99 | Homo sapiens (human) | Ki | 3.5000 | 2 | 2 |
| tyrphostin ag 555 | Homo sapiens (human) | IC50 | 0.9583 | 7 | 7 |
| tyrphostin ag-494 | Homo sapiens (human) | IC50 | 4.5399 | 8 | 9 |
| tyrphostin b44 | Homo sapiens (human) | IC50 | 0.4000 | 1 | 1 |
| ag 556 | Homo sapiens (human) | IC50 | 3.3686 | 6 | 6 |
| ag-490 | Homo sapiens (human) | IC50 | 1.9224 | 9 | 9 |
| ag 127 | Homo sapiens (human) | IC50 | 125.0000 | 1 | 1 |
| ag 127 | Homo sapiens (human) | Ki | 49.0000 | 2 | 2 |
| alpha-cyano-4-hydroxycinnamic acid | Homo sapiens (human) | IC50 | 182.5000 | 2 | 2 |
| alpha-cyano-4-hydroxycinnamic acid | Homo sapiens (human) | Ki | 236.5000 | 2 | 2 |
| ag 30 | Homo sapiens (human) | IC50 | 27.5000 | 2 | 2 |
| ag 30 | Homo sapiens (human) | Ki | 47.5000 | 2 | 2 |
| ag 112 | Homo sapiens (human) | IC50 | 0.1125 | 2 | 2 |
| ag 183 | Homo sapiens (human) | IC50 | 1.6250 | 4 | 4 |
| bosutinib | Homo sapiens (human) | IC50 | 0.2720 | 2 | 2 |
| semaxinib | Homo sapiens (human) | IC50 | 49.0295 | 12 | 19 |
| orantinib | Homo sapiens (human) | IC50 | 36.4482 | 6 | 11 |
| su 11248 | Homo sapiens (human) | IC50 | 64.3788 | 15 | 17 |
| su 11652 | Homo sapiens (human) | IC50 | 10.5328 | 4 | 6 |
| palladia | Homo sapiens (human) | IC50 | 10.9900 | 2 | 4 |
| su9518 | Homo sapiens (human) | IC50 | 42.3067 | 3 | 6 |
| d-64406 | Homo sapiens (human) | IC50 | 30.0000 | 1 | 1 |
| jnj-7706621 | Homo sapiens (human) | IC50 | 38.7792 | 2 | 14 |
| fosbretabulin | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| sulindac sulfide | Homo sapiens (human) | IC50 | 23.9810 | 1 | 0 |
| st 638 | Homo sapiens (human) | IC50 | 0.4000 | 1 | 1 |
| su 4984 | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
| tyrphostin ag825 | Homo sapiens (human) | IC50 | 18.4009 | 5 | 5 |
| 2-((4-pyridyl)methyl)amino-n-(3-(trifluoromethyl)phenyl)benzamide | Homo sapiens (human) | IC50 | 10.4000 | 1 | 1 |
| st 271 | Homo sapiens (human) | IC50 | 1.0000 | 1 | 1 |
| 1,2-dihydroxy-4-(nitroethenyl)benzene | Homo sapiens (human) | IC50 | 8.9000 | 2 | 2 |
| marein | Homo sapiens (human) | IC50 | 19,000.0000 | 1 | 1 |
| ekb 569 | Homo sapiens (human) | IC50 | 0.0489 | 17 | 17 |
| su 4312 | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
| gw 1929 | Homo sapiens (human) | IC50 | 10.8960 | 1 | 0 |
| gdp 366 | Homo sapiens (human) | IC50 | 50.0000 | 1 | 1 |
| b 43 | Homo sapiens (human) | IC50 | 1.6885 | 2 | 2 |
| gw2974 | Homo sapiens (human) | IC50 | 0.0727 | 3 | 3 |
| cgp 53353 | Homo sapiens (human) | IC50 | 1.4500 | 2 | 2 |
| bibx 1382bs | Homo sapiens (human) | IC50 | 0.0030 | 3 | 3 |
| c 1368 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| jnj 10198409 | Homo sapiens (human) | IC50 | 100.0000 | 2 | 2 |
| av 412 | Homo sapiens (human) | IC50 | 0.0012 | 4 | 4 |
| edotecarin | Homo sapiens (human) | IC50 | 200.0000 | 1 | 1 |
| gw843682x | Homo sapiens (human) | IC50 | 48.0000 | 1 | 1 |
| ki23057 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| sb 242235 | Homo sapiens (human) | IC50 | 0.0100 | 1 | 1 |
| cp 724714 | Homo sapiens (human) | IC50 | 6.4000 | 2 | 2 |
| ct52923 | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
| tivozanib | Homo sapiens (human) | IC50 | 0.0709 | 1 | 4 |
| zm 447439 | Homo sapiens (human) | IC50 | 0.1100 | 1 | 1 |
| hki 272 | Homo sapiens (human) | IC50 | 0.4614 | 24 | 24 |
| tofacitinib | Homo sapiens (human) | IC50 | 1.1835 | 2 | 9 |
| tae226 | Homo sapiens (human) | IC50 | 0.5500 | 1 | 1 |
| bibw 2992 | Homo sapiens (human) | IC50 | 0.0361 | 67 | 66 |
| sotrastaurin | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| aee 788 | Homo sapiens (human) | IC50 | 0.0020 | 3 | 3 |
| saracatinib | Homo sapiens (human) | IC50 | 1.9615 | 4 | 4 |
| bms 599626 | Homo sapiens (human) | IC50 | 0.0280 | 3 | 3 |
| exel-7647 | Homo sapiens (human) | IC50 | 0.0252 | 2 | 1 |
| pha 665752 | Homo sapiens (human) | IC50 | 3.8000 | 1 | 1 |
| PDGF receptor tyrosine kinase inhibitor III | Homo sapiens (human) | IC50 | 30.0000 | 1 | 1 |
| baci-im | Homo sapiens (human) | IC50 | 5.3770 | 1 | 0 |
| brivanib | Homo sapiens (human) | IC50 | 1.9000 | 1 | 1 |
| zm 252868 | Homo sapiens (human) | IC50 | 0.0714 | 3 | 3 |
| ki 8751 | Homo sapiens (human) | IC50 | 10.0000 | 2 | 2 |
| verubulin | Homo sapiens (human) | IC50 | 0.0028 | 1 | 1 |
| danusertib | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| N-[5-[[5-[(4-acetyl-1-piperazinyl)-oxomethyl]-4-methoxy-2-methylphenyl]thio]-2-thiazolyl]-4-[(3,3-dimethylbutan-2-ylamino)methyl]benzamide | Homo sapiens (human) | IC50 | 50.0000 | 1 | 1 |
| nvp-aew541 | Homo sapiens (human) | IC50 | 8.4000 | 3 | 3 |
| azd 8931 | Homo sapiens (human) | IC50 | 0.0072 | 5 | 5 |
| pf 00299804 | Homo sapiens (human) | IC50 | 0.0370 | 15 | 15 |
| lapatinib ditosylate | Homo sapiens (human) | IC50 | 0.0302 | 7 | 7 |
| cc-930 | Homo sapiens (human) | IC50 | 0.3800 | 1 | 1 |
| gw 2580 | Homo sapiens (human) | IC50 | 24.0000 | 1 | 1 |
| tak 285 | Homo sapiens (human) | IC50 | 1.6902 | 5 | 5 |
| crizotinib | Homo sapiens (human) | IC50 | 146.9544 | 7 | 7 |
| 5-(5,6-dimethoxy-1-benzimidazolyl)-3-[(2-methylsulfonylphenyl)methoxy]-2-thiophenecarbonitrile | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| osi 906 | Homo sapiens (human) | IC50 | 11.6667 | 3 | 3 |
| motesanib | Homo sapiens (human) | IC50 | 1.0880 | 1 | 11 |
| 4-(3-cyclohexyl-5-(4-fluoro-phenyl)-3h-imidazol-4-yl)pyrimidin-2-ylamine | Homo sapiens (human) | IC50 | 0.1500 | 1 | 1 |
| pha 767491 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| jnj-26483327 | Homo sapiens (human) | IC50 | 0.0100 | 1 | 1 |
| azd 1152-hqpa | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| nvp-tae684 | Homo sapiens (human) | GI50 | 0.4402 | 3 | 3 |
| N-(3-ethynylphenyl)-6,7-dimethoxy-4-quinazolinamine | Homo sapiens (human) | IC50 | 0.0380 | 5 | 5 |
| pha 848125 | Homo sapiens (human) | IC50 | 3.0690 | 1 | 1 |
| icotinib | Homo sapiens (human) | IC50 | 0.0173 | 3 | 3 |
| cudc 101 | Homo sapiens (human) | IC50 | 0.0046 | 7 | 5 |
| bms 777607 | Homo sapiens (human) | IC50 | 7.0000 | 4 | 4 |
| pci 32765 | Homo sapiens (human) | GI50 | 2.0493 | 7 | 7 |
| pci 32765 | Homo sapiens (human) | IC50 | 0.0402 | 28 | 28 |
| ponatinib | Homo sapiens (human) | IC50 | 1.0000 | 1 | 1 |
| N-cyclopropyl-3-{4-[(cyclopropylmethyl)carbamoyl]phenyl}-4-methylbenzamide | Homo sapiens (human) | IC50 | 25.0000 | 1 | 1 |
| AMG-208 | Homo sapiens (human) | IC50 | 0.0767 | 1 | 3 |
| PP121 | Homo sapiens (human) | IC50 | 0.2600 | 1 | 1 |
| cabozantinib | Homo sapiens (human) | IC50 | 1.1180 | 3 | 3 |
| N-(2,6-difluorophenyl)-5-[3-[2-[5-ethyl-2-methoxy-4-[4-(4-methylsulfonyl-1-piperazinyl)-1-piperidinyl]anilino]-4-pyrimidinyl]-2-imidazo[1,2-a]pyridinyl]-2-methoxybenzamide | Homo sapiens (human) | IC50 | 5.5000 | 2 | 1 |
| poziotinib | Homo sapiens (human) | IC50 | 0.0020 | 8 | 6 |
| asp3026 | Homo sapiens (human) | GI50 | 1.5080 | 1 | 1 |
| entrectinib | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| pexidartinib | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| plx4032 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| gsk 1363089 | Homo sapiens (human) | IC50 | 1.5147 | 7 | 14 |
| arry-334543 | Homo sapiens (human) | IC50 | 0.0070 | 2 | 2 |
| 8-chloro-4-(3-chloro-4-fluoroanilino)-6-[[1-(1-ethyl-4-piperidinyl)-4-triazolyl]methylamino]-3-quinolinecarbonitrile | Homo sapiens (human) | IC50 | 11.0000 | 1 | 1 |
| thiopental sodium | Homo sapiens (human) | GI50 | 0.6276 | 7 | 7 |
| thiopental sodium | Homo sapiens (human) | IC50 | 0.5510 | 57 | 57 |
| pha 793887 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| tak-632 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| gsk 2334470 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| nms p937 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| nms-p118 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| butyrolactone i | Homo sapiens (human) | IC50 | 590.0000 | 1 | 1 |
| AZD3463 | Homo sapiens (human) | GI50 | 0.1315 | 1 | 1 |
| rociletinib | Homo sapiens (human) | IC50 | 0.3545 | 42 | 42 |
| rociletinib | Homo sapiens (human) | Ki | 0.0578 | 7 | 7 |
| ceritinib | Homo sapiens (human) | GI50 | 0.7805 | 1 | 1 |
| ceritinib | Homo sapiens (human) | IC50 | 77.7772 | 13 | 13 |
| ap26113 | Homo sapiens (human) | GI50 | 0.0591 | 1 | 1 |
| cc-292 | Homo sapiens (human) | IC50 | 0.4420 | 1 | 1 |
| pf-543 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| acp-196 | Homo sapiens (human) | IC50 | 1.8782 | 4 | 4 |
| osimertinib | Homo sapiens (human) | GI50 | 0.6719 | 20 | 20 |
| osimertinib | Homo sapiens (human) | IC50 | 3.2863 | 169 | 170 |
| osimertinib | Homo sapiens (human) | Ki | 0.0666 | 11 | 11 |
| pf-06463922 | Homo sapiens (human) | Ki | 0.1875 | 2 | 0 |
| 9-(1-methyl-4-pyrazolyl)-1-[1-(1-oxoprop-2-enyl)-2,3-dihydroindol-6-yl]-2-benzo[h][1,6]naphthyridinone | Homo sapiens (human) | IC50 | 0.8740 | 1 | 1 |
| azd3759 | Homo sapiens (human) | IC50 | 0.0192 | 10 | 10 |
| tyrphostin ag 1112 | Homo sapiens (human) | IC50 | 100.0000 | 1 | 2 |
| nintedanib | Homo sapiens (human) | IC50 | 30.0000 | 2 | 2 |
| bms 536924 | Homo sapiens (human) | IC50 | 1.6000 | 1 | 1 |
| pp242 | Homo sapiens (human) | IC50 | 4.4000 | 1 | 1 |
| nms-e973 | Homo sapiens (human) | IC50 | 0.0100 | 1 | 1 |
Drugs with Activation Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| cl 387785 | Homo sapiens (human) | EC50 | 0.4500 | 3 | 3 |
| fasudil | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| 4-(4'-hydroxyphenyl)-amino-6,7-dimethoxyquinazoline | Homo sapiens (human) | Kd | 1.1630 | 1 | 1 |
| sb 202190 | Homo sapiens (human) | Kd | 1.8745 | 11 | 11 |
| imatinib | Homo sapiens (human) | Kd | 10.6609 | 23 | 23 |
| triciribine phosphate | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| staurosporine | Homo sapiens (human) | Kd | 0.3906 | 23 | 23 |
| picropodophyllin | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| gefitinib | Homo sapiens (human) | EC50 | 6.4475 | 2 | 2 |
| gefitinib | Homo sapiens (human) | Kd | 0.0360 | 33 | 38 |
| lestaurtinib | Homo sapiens (human) | Kd | 2.3291 | 19 | 19 |
| docetaxel | Homo sapiens (human) | Kd | 0.0008 | 1 | 1 |
| perifosine | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| vatalanib | Homo sapiens (human) | Kd | 10.8696 | 23 | 23 |
| ruboxistaurin | Homo sapiens (human) | Kd | 10.5435 | 23 | 23 |
| canertinib | Homo sapiens (human) | Kd | 0.0006 | 25 | 25 |
| birb 796 | Homo sapiens (human) | Kd | 8.1091 | 22 | 22 |
| cyc 202 | Homo sapiens (human) | Kd | 11.8182 | 11 | 11 |
| sb 203580 | Homo sapiens (human) | Kd | 1.6783 | 23 | 23 |
| enzastaurin | Homo sapiens (human) | Kd | 11.5385 | 13 | 13 |
| erlotinib | Homo sapiens (human) | Kd | 0.0931 | 27 | 27 |
| lapatinib | Homo sapiens (human) | Kd | 0.4228 | 26 | 26 |
| sorafenib | Homo sapiens (human) | Kd | 10.6897 | 29 | 29 |
| pd 173955 | Homo sapiens (human) | Kd | 2.5833 | 12 | 12 |
| s 1033 | Homo sapiens (human) | Kd | 11.5385 | 13 | 13 |
| xl147 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| bms 387032 | Homo sapiens (human) | Kd | 10.8696 | 23 | 23 |
| sf 2370 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| tandutinib | Homo sapiens (human) | Kd | 3.3333 | 29 | 30 |
| vx-745 | Homo sapiens (human) | Kd | 10.0000 | 22 | 22 |
| dasatinib | Homo sapiens (human) | Kd | 0.4208 | 23 | 23 |
| ha 1100 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| 7-epi-hydroxystaurosporine | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| zd 6474 | Homo sapiens (human) | Kd | 0.1711 | 25 | 25 |
| ml106 | Homo sapiens (human) | Kd | 0.2300 | 1 | 1 |
| 4-(5-benzo(1,3)dioxol-5-yl-4-pyridin-2-yl-1h-imidazol-2-yl)benzamide | Homo sapiens (human) | Kd | 10.0000 | 10 | 10 |
| imd 0354 | Homo sapiens (human) | Kd | 30.0000 | 1 | 2 |
| sirolimus | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| alvocidib | Homo sapiens (human) | Kd | 5.9683 | 23 | 23 |
| bosutinib | Homo sapiens (human) | Kd | 2.2316 | 14 | 14 |
| orantinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| su 11248 | Homo sapiens (human) | Kd | 8.9810 | 29 | 29 |
| palbociclib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| jnj-7706621 | Homo sapiens (human) | Kd | 10.0000 | 10 | 10 |
| vx680 | Homo sapiens (human) | Kd | 10.8696 | 23 | 23 |
| cyc 116 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| everolimus | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| ekb 569 | Homo sapiens (human) | Kd | 0.0014 | 12 | 12 |
| axitinib | Homo sapiens (human) | Kd | 10.6538 | 13 | 13 |
| temsirolimus | Homo sapiens (human) | Kd | 30.0000 | 1 | 2 |
| pd 184352 | Homo sapiens (human) | Kd | 10.0000 | 12 | 12 |
| on 01910 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| av 412 | Homo sapiens (human) | Kd | 0.0100 | 1 | 1 |
| telatinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| y-39983 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| cp 547632 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| bms345541 | Homo sapiens (human) | Kd | 10.0000 | 12 | 12 |
| lenvatinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| pd 0325901 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| midostaurin | Homo sapiens (human) | Kd | 3.1402 | 29 | 29 |
| px-866 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| ripasudil | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| osi 930 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| ki 20227 | Homo sapiens (human) | Kd | 8.1667 | 12 | 12 |
| scio-469 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| cp 724714 | Homo sapiens (human) | Kd | 0.5787 | 11 | 11 |
| pi103 | Homo sapiens (human) | Kd | 10.0000 | 22 | 22 |
| hmn-214 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| tivozanib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| hki 272 | Homo sapiens (human) | EC50 | 0.0515 | 2 | 2 |
| hki 272 | Homo sapiens (human) | Kd | 0.0052 | 14 | 14 |
| tofacitinib | Homo sapiens (human) | Kd | 10.8696 | 23 | 23 |
| n-(6-chloro-7-methoxy-9h-beta-carbolin-8-yl)-2-methylnicotinamide | Homo sapiens (human) | Kd | 10.0000 | 12 | 12 |
| cediranib | Homo sapiens (human) | Kd | 1.2690 | 13 | 13 |
| masitinib | Homo sapiens (human) | Kd | 9.7538 | 13 | 13 |
| ly-2157299 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| pazopanib | Homo sapiens (human) | Kd | 10.8696 | 23 | 23 |
| azd 6244 | Homo sapiens (human) | Kd | 7.6923 | 13 | 13 |
| su 14813 | Homo sapiens (human) | Kd | 10.4913 | 23 | 23 |
| bibw 2992 | Homo sapiens (human) | EC50 | 0.0216 | 4 | 4 |
| bibw 2992 | Homo sapiens (human) | Kd | 0.0004 | 14 | 14 |
| binimetinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| sotrastaurin | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| aee 788 | Homo sapiens (human) | Kd | 0.0599 | 3 | 8 |
| saracatinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| vx 702 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| crenolanib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| tg100-115 | Homo sapiens (human) | Kd | 5.2077 | 13 | 13 |
| cc 401 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| bms 599626 | Homo sapiens (human) | Kd | 0.0030 | 1 | 1 |
| exel-7647 | Homo sapiens (human) | Kd | 0.0380 | 1 | 1 |
| volasertib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| pha 665752 | Homo sapiens (human) | Kd | 10.0000 | 12 | 12 |
| azd 7762 | Homo sapiens (human) | Kd | 0.8080 | 1 | 1 |
| regorafenib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| 6-[[5-fluoro-2-(3,4,5-trimethoxyanilino)-4-pyrimidinyl]amino]-2,2-dimethyl-4H-pyrido[3,2-b][1,4]oxazin-3-one | Homo sapiens (human) | Kd | 4.1218 | 13 | 13 |
| brivanib | Homo sapiens (human) | Kd | 9.6923 | 13 | 13 |
| mp470 | Homo sapiens (human) | Kd | 30.0000 | 1 | 2 |
| rgb 286638 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| np 031112 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| at 7519 | Homo sapiens (human) | Kd | 11.5385 | 13 | 13 |
| bms-690514 | Homo sapiens (human) | Kd | 0.2225 | 2 | 2 |
| bi 2536 | Homo sapiens (human) | Kd | 4.4715 | 13 | 13 |
| inno-406 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| nvp-ast487 | Homo sapiens (human) | Kd | 1.8073 | 22 | 22 |
| kw 2449 | Homo sapiens (human) | Kd | 8.8923 | 13 | 13 |
| danusertib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| abt 869 | Homo sapiens (human) | Kd | 10.5652 | 23 | 23 |
| azd 8931 | Homo sapiens (human) | Kd | 0.0010 | 1 | 1 |
| arq 197 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| azd 1152 | Homo sapiens (human) | Kd | 1.7340 | 1 | 1 |
| pf 00299804 | Homo sapiens (human) | EC50 | 0.0310 | 2 | 2 |
| pf 00299804 | Homo sapiens (human) | Kd | 0.0050 | 1 | 1 |
| ridaforolimus | Homo sapiens (human) | Kd | 30.0000 | 1 | 2 |
| ch 4987655 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| 6-(5-((cyclopropylamino)carbonyl)-3-fluoro-2-methylphenyl)-n-(2,2-dimethylprpyl)-3-pyridinecarboxamide | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| cc-930 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| gw 2580 | Homo sapiens (human) | Kd | 10.0000 | 22 | 22 |
| tak 285 | Homo sapiens (human) | Kd | 0.6770 | 1 | 1 |
| idelalisib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| crizotinib | Homo sapiens (human) | Kd | 10.4154 | 13 | 13 |
| osi 906 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| chir-265 | Homo sapiens (human) | Kd | 10.8696 | 23 | 23 |
| motesanib | Homo sapiens (human) | Kd | 5.7902 | 23 | 23 |
| fostamatinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| trametinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| mln8054 | Homo sapiens (human) | Kd | 9.9652 | 23 | 23 |
| pf-562,271 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| GDC-0879 | Homo sapiens (human) | Kd | 10.0000 | 12 | 12 |
| jnj-26483327 | Homo sapiens (human) | Kd | 0.6020 | 1 | 1 |
| ly2603618 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| tg100801 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| dactolisib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| bgt226 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| gsk 461364 | Homo sapiens (human) | Kd | 11.5385 | 13 | 13 |
| azd 1152-hqpa | Homo sapiens (human) | Kd | 3.4354 | 23 | 23 |
| nvp-tae684 | Homo sapiens (human) | Kd | 0.3897 | 12 | 12 |
| enmd 2076 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| N-(3-ethynylphenyl)-6,7-dimethoxy-4-quinazolinamine | Homo sapiens (human) | Kd | 0.0006 | 1 | 1 |
| e 7050 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| 2-amino-8-ethyl-4-methyl-6-(1H-pyrazol-5-yl)-7-pyrido[2,3-d]pyrimidinone | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| tak-901 | Homo sapiens (human) | Kd | 1.4680 | 1 | 1 |
| gdc-0973 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| buparlisib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| azd 1480 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| azd8330 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| pha 848125 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| ro5126766 | Homo sapiens (human) | Kd | 30.0000 | 1 | 2 |
| fedratinib | Homo sapiens (human) | Kd | 6.9808 | 13 | 13 |
| gsk690693 | Homo sapiens (human) | Kd | 11.5385 | 13 | 13 |
| 14-methyl-20-oxa-5,7,14,26-tetraazatetracyclo(19.3.1.1(2,6).1(8,12))heptacosa-1(25),2(26),3,5,8(27),9,11,16,21,23-decaene | Homo sapiens (human) | Kd | 79.9330 | 1 | 1 |
| azd5438 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| pf 04217903 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| gdc 0941 | Homo sapiens (human) | Kd | 11.5385 | 13 | 13 |
| icotinib | Homo sapiens (human) | Kd | 10.1280 | 1 | 1 |
| ph 797804 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| kx-01 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| plx 4720 | Homo sapiens (human) | Kd | 10.0000 | 12 | 12 |
| mk 5108 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| cx 4945 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| cudc 101 | Homo sapiens (human) | Kd | 0.7390 | 1 | 1 |
| arry-614 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| tak 593 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| mln 8237 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| sgx 523 | Homo sapiens (human) | Kd | 11.5385 | 13 | 13 |
| bms 754807 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| bms 777607 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| sgi 1776 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| pci 32765 | Homo sapiens (human) | EC50 | 0.0595 | 2 | 2 |
| pci 32765 | Homo sapiens (human) | Kd | 0.0179 | 3 | 3 |
| ponatinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| amg 900 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| mk-1775 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| AMG-208 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| quizartinib | Homo sapiens (human) | Kd | 11.0526 | 19 | 19 |
| at13148 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| tak 733 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| mk 2206 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| sns 314 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| lucitanib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| pf-04691502 | Homo sapiens (human) | Kd | 30.0000 | 1 | 2 |
| n-(cyanomethyl)-4-(2-((4-(4-morpholinyl)phenyl)amino)-4-pyrimidinyl)benzamide | Homo sapiens (human) | Kd | 30.0000 | 1 | 2 |
| dcc-2036 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| cabozantinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| defactinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| ly2584702 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| incb-018424 | Homo sapiens (human) | Kd | 11.5385 | 13 | 13 |
| poziotinib | Homo sapiens (human) | Kd | 0.0020 | 1 | 1 |
| asp3026 | Homo sapiens (human) | Kd | 20.8270 | 1 | 1 |
| entrectinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| pexidartinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| TAK-580 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| gsk 2126458 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| emd1214063 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| gsk 1838705a | Homo sapiens (human) | Kd | 3.5353 | 12 | 12 |
| pf 3758309 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| gdc 0980 | Homo sapiens (human) | Kd | 4.8740 | 1 | 1 |
| azd2014 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| (5-(2,4-bis((3s)-3-methylmorpholin-4-yl)pyrido(2,3-d)pyrimidin-7-yl)-2-methoxyphenyl)methanol | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| plx4032 | Homo sapiens (human) | Kd | 30.0000 | 1 | 2 |
| gsk 1363089 | Homo sapiens (human) | Kd | 2.7243 | 13 | 13 |
| arry-334543 | Homo sapiens (human) | Kd | 0.0050 | 1 | 1 |
| kin-193 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| mk 2461 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| bay 869766 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| as 703026 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| baricitinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| dabrafenib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| pki 587 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| n-(3-fluoro-4-((1-methyl-6-(1h-pyrazol-4-yl)-1h-indazol-5 yl)oxy)phenyl)-1-(4-fluorophenyl)-6-methyl-2-oxo-1,2-dihydropyridine-3-carboxamide | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| thiopental sodium | Homo sapiens (human) | EC50 | 0.2282 | 5 | 5 |
| thiopental sodium | Homo sapiens (human) | Kd | 0.0413 | 5 | 5 |
| ribociclib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| mk-8033 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| pha 793887 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| sb 1518 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| abemaciclib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| mk-8776 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| afuresertib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| gsk 1070916 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| jnj38877605 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| dinaciclib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| gilteritinib | Homo sapiens (human) | Kd | 3.5020 | 1 | 1 |
| alectinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| glpg0634 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| encorafenib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| bms-911543 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| gsk2141795 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| azd8186 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| byl719 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| cep-32496 | Homo sapiens (human) | Kd | 15.0110 | 2 | 2 |
| rociletinib | Homo sapiens (human) | EC50 | 0.8865 | 2 | 2 |
| rociletinib | Homo sapiens (human) | Kd | 0.4980 | 1 | 1 |
| ceritinib | Homo sapiens (human) | EC50 | 2.7320 | 5 | 5 |
| ceritinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| azd1208 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| vx-509 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| debio 1347 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| volitinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| acp-196 | Homo sapiens (human) | EC50 | 2.8500 | 2 | 2 |
| acp-196 | Homo sapiens (human) | Kd | 2.8850 | 2 | 2 |
| osimertinib | Homo sapiens (human) | EC50 | 1.1610 | 20 | 21 |
| osimertinib | Homo sapiens (human) | Kd | 0.1550 | 1 | 1 |
| at 9283 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| otssp167 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| chir 258 | Homo sapiens (human) | Kd | 10.1017 | 23 | 23 |
| osi 027 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| nintedanib | Homo sapiens (human) | Kd | 11.5385 | 13 | 13 |
| bay 80-6946 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| pp242 | Homo sapiens (human) | Kd | 1.9767 | 12 | 12 |
Drugs with Other Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| osimertinib | Homo sapiens (human) | DC50 | 2.0000 | 2 | 2 |
| protac-3 | Homo sapiens (human) | DC50 | 0.0139 | 5 | 5 |
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FDA-approved pyrimidine-fused bicyclic heterocycles for cancer therapy: Synthesis and clinical application.European journal of medicinal chemistry, , Mar-15, Volume: 214, 2021
Rational Design and Synthesis of Novel Dual PROTACs for Simultaneous Degradation of EGFR and PARP.Journal of medicinal chemistry, , 06-10, Volume: 64, Issue:11, 2021
[no title available]European journal of medicinal chemistry, , Dec-05, Volume: 225, 2021
Design, synthesis and assessment of new series of quinazolinone derivatives as EGFR inhibitors along with their cytotoxic evaluation against MCF7 and A549 cancer cell lines.Bioorganic & medicinal chemistry letters, , 06-01, Volume: 41, 2021
[no title available]Bioorganic & medicinal chemistry, , 03-15, Volume: 34, 2021
Design, synthesis and biological evaluation of novel 2,4-diaryl pyrimidine derivatives as selective EGFREuropean journal of medicinal chemistry, , Feb-15, Volume: 212, 2021
Synthesis and biological evaluation of selenogefitinib for reducing bleomycin-induced pulmonary fibrosis.Bioorganic & medicinal chemistry letters, , 09-15, Volume: 48, 2021
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Design, synthesis, biological evaluation, QSAR analysis and molecular modelling of new thiazol-benzimidazoles as EGFR inhibitors.Bioorganic & medicinal chemistry, , 09-15, Volume: 28, Issue:18, 2020
Design and synthesis of a novel class EGFR/HER2 dual inhibitors containing tricyclic oxazine fused quinazolines scaffold.Bioorganic & medicinal chemistry letters, , 05-01, Volume: 30, Issue:9, 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
Acetylene Group, Friend or Foe in Medicinal Chemistry.Journal of medicinal chemistry, , 06-11, Volume: 63, Issue:11, 2020
Design, synthesis and biological evaluation of 2-amino-4-(1,2,4-triazol)pyridine derivatives as potent EGFR inhibitors to overcome TKI-resistance.European journal of medicinal chemistry, , Feb-01, Volume: 187, 2020
Synthesis, biological evaluation and molecular modeling study of [1,2,4]-Triazolo[4,3-c]quinazolines: New class of EGFR-TK inhibitors.Bioorganic & medicinal chemistry, , 04-01, Volume: 28, Issue:7, 2020
Comparative analysis of the dual EGFR-DNA targeting and growth inhibitory properties of 6-mono-alkylamino- and 6,6-dialkylaminoquinazoline-based type II combi-molecules.European journal of medicinal chemistry, , Apr-15, Volume: 192, 2020
Discovery of Potent and Selective Epidermal Growth Factor Receptor (EGFR) Bifunctional Small-Molecule Degraders.Journal of medicinal chemistry, , 02-13, Volume: 63, Issue:3, 2020
Lead generation of 1,2-dithiolanes as exon 19 and exon 21 mutant EGFR tyrosine kinase inhibitors.Bioorganic & medicinal chemistry letters, , 06-15, Volume: 29, Issue:12, 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
Acrylamide Functional Group Incorporation Improves Drug-like Properties: An Example with EGFR Inhibitors.ACS medicinal chemistry letters, , Jan-10, Volume: 10, Issue:1, 2019
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
Balancing reactivity and antitumor activity: heteroarylthioacetamide derivatives as potent and time-dependent inhibitors of EGFR.European journal of medicinal chemistry, , Jan-15, Volume: 162, 2019
Click chemistry for improvement in selectivity of quinazoline-based kinase inhibitors for mutant epidermal growth factor receptors.Bioorganic & medicinal chemistry letters, , 02-01, Volume: 29, Issue:3, 2019
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Utilizing comprehensive and mini-kinome panels to optimize the selectivity of quinoline inhibitors for cyclin G associated kinase (GAK).Bioorganic & medicinal chemistry letters, , 07-15, Volume: 29, Issue:14, 2019
Discovery of an Oleanolic Acid/Hederagenin-Nitric Oxide Donor Hybrid as an EGFR Tyrosine Kinase Inhibitor for Non-Small-Cell Lung Cancer.Journal of natural products, , 11-22, Volume: 82, Issue:11, 2019
Design of a Cyclin G Associated Kinase (GAK)/Epidermal Growth Factor Receptor (EGFR) Inhibitor Set to Interrogate the Relationship of EGFR and GAK in Chordoma.Journal of medicinal chemistry, , 05-09, Volume: 62, Issue:9, 2019
Discovery of a Furanopyrimidine-Based Epidermal Growth Factor Receptor Inhibitor (DBPR112) as a Clinical Candidate for the Treatment of Non-Small Cell Lung Cancer.Journal of medicinal chemistry, , 11-27, Volume: 62, Issue:22, 2019
Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors.Bioorganic & medicinal chemistry, , 05-01, Volume: 26, Issue:8, 2018
Design, synthesis and biological evaluation of novel 4-aminoquinazolines as dual target inhibitors of EGFR-PI3Kα.European journal of medicinal chemistry, , Feb-25, Volume: 146, 2018
The synthesis of 4-arylamido-2-arylaminoprimidines as potent EGFR T790M/L858R inhibitors for NSCLC.Bioorganic & medicinal chemistry, , 12-15, Volume: 26, Issue:23-24, 2018
Design and Evaluation of Potent EGFR Inhibitors through the Incorporation of Macrocyclic Polyamine Moieties into the 4-Anilinoquinazoline Scaffold.Journal of medicinal chemistry, , 12-27, Volume: 61, Issue:24, 2018
ROCK inhibitors 2. Improving potency, selectivity and solubility through the application of rationally designed solubilizing groups.Bioorganic & medicinal chemistry letters, , 08-15, Volume: 28, Issue:15, 2018
[no title available]Bioorganic & medicinal chemistry, , 05-01, Volume: 26, Issue:8, 2018
Design, synthesis, antiproliferative activity and docking studies of quinazoline derivatives bearing 2,3-dihydro-indole or 1,2,3,4-tetrahydroquinoline as potential EGFR inhibitors.European journal of medicinal chemistry, , Jun-25, Volume: 154, 2018
6,7-Dimorpholinoalkoxy quinazoline derivatives as potent EGFR inhibitors with enhanced antiproliferative activities against tumor cells.European journal of medicinal chemistry, , Mar-10, Volume: 147, 2018
Design, synthesis, antiproliferative activity, molecular docking and cell cycle analysis of some novel (morpholinosulfonyl) isatins with potential EGFR inhibitory activity.European journal of medicinal chemistry, , Aug-05, Volume: 156, 2018
Discovery of anilino-furo[2,3-d]pyrimidine derivatives as dual inhibitors of EGFR/HER2 tyrosine kinase and their anticancer activity.European journal of medicinal chemistry, , Jan-20, Volume: 144, 2018
Quinazoline-1-deoxynojirimycin hybrids as high active dual inhibitors of EGFR and α-glucosidase.Bioorganic & medicinal chemistry letters, , 09-15, Volume: 27, Issue:18, 2017
[no title available]European journal of medicinal chemistry, , Sep-29, Volume: 138, 2017
Development of a series of novel 4-anlinoquinazoline derivatives possessing quinazoline skeleton: Design, synthesis, EGFR kinase inhibitory efficacy, and evaluation of anticancer activities in vitro.European journal of medicinal chemistry, , Sep-29, Volume: 138, 2017
Trisubstituted Pyridinylimidazoles as Potent Inhibitors of the Clinically Resistant L858R/T790M/C797S EGFR Mutant: Targeting of Both Hydrophobic Regions and the Phosphate Binding Site.Journal of medicinal chemistry, , 07-13, Volume: 60, Issue:13, 2017
Novel conjugates of endoperoxide and 4-anilinoquinazoline as potential anticancer agents.Bioorganic & medicinal chemistry letters, , 03-15, Volume: 27, Issue:6, 2017
Design, synthesis, docking and QSAR study of substituted benzimidazole linked oxadiazole as cytotoxic agents, EGFR and erbB2 receptor inhibitors.European journal of medicinal chemistry, , Jan-27, Volume: 126, 2017
Synthesis and biological evaluation of morpholine-substituted diphenylpyrimidine derivatives (Mor-DPPYs) as potent EGFR T790M inhibitors with improved activity toward the gefitinib-resistant non-small cell lung cancers (NSCLC).European journal of medicinal chemistry, , Jun-16, Volume: 133, 2017
C-2 (E)-4-(Styryl)aniline substituted diphenylpyrimidine derivatives (Sty-DPPYs) as specific kinase inhibitors targeting clinical resistance related EGFRBioorganic & medicinal chemistry, , 05-15, Volume: 25, Issue:10, 2017
Indazole-Based Covalent Inhibitors To Target Drug-Resistant Epidermal Growth Factor Receptor.Journal of medicinal chemistry, , 03-23, Volume: 60, Issue:6, 2017
Synthesis and in vitro biological evaluation of novel quinazoline derivatives.Bioorganic & medicinal chemistry letters, , 04-01, Volume: 27, Issue:7, 2017
Design, synthesis, and evaluation of A-ring-modified lamellarin N analogues as noncovalent inhibitors of the EGFR T790M/L858R mutant.Bioorganic & medicinal chemistry, , 12-15, Volume: 25, Issue:24, 2017
Design, synthesis and biological evaluation of WZ4002 analogues as EGFR inhibitors.Bioorganic & medicinal chemistry letters, , 11-01, Volume: 27, Issue:21, 2017
Synthesis and investigation of novel 6-(1,2,3-triazol-4-yl)-4-aminoquinazolin derivatives possessing hydroxamic acid moiety for cancer therapy.Bioorganic & medicinal chemistry, , 01-01, Volume: 25, Issue:1, 2017
Design and synthesis of quinazolinones as EGFR inhibitors to overcome EGFR resistance obstacle.Bioorganic & medicinal chemistry, , 05-15, Volume: 25, Issue:10, 2017
Structure-Guided Development of Covalent and Mutant-Selective Pyrazolopyrimidines to Target T790M Drug Resistance in Epidermal Growth Factor Receptor.Journal of medicinal chemistry, , 09-28, Volume: 60, Issue:18, 2017
First Bispecific Inhibitors of the Epidermal Growth Factor Receptor Kinase and the NF-κB Activity As Novel Anticancer Agents.Journal of medicinal chemistry, , 04-13, Volume: 60, Issue:7, 2017
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Synthesis and biological evaluation of novel tricyclic oxazine and oxazepine fused quinazolines. Part 2: Gefitinib analogs.Bioorganic & medicinal chemistry letters, , 10-01, Volume: 26, Issue:19, 2016
Novel 4-anilinoquinazoline derivatives featuring an 1-adamantyl moiety as potent EGFR inhibitors with enhanced activity against NSCLC cell lines.European journal of medicinal chemistry, , Mar-03, Volume: 110, 2016
Design, synthesis, anti-tumor activity, and molecular modeling of quinazoline and pyrido[2,3-d]pyrimidine derivatives targeting epidermal growth factor receptor.European journal of medicinal chemistry, , Aug-08, Volume: 118, 2016
Discovery of new [1,4]dioxino[2,3-f]quinazoline-based inhibitors of EGFR including the T790M/L858R mutant.Bioorganic & medicinal chemistry, , 07-01, Volume: 24, Issue:13, 2016
Novel morpholin-3-one fused quinazoline derivatives as EGFR tyrosine kinase inhibitors.Bioorganic & medicinal chemistry letters, , Mar-15, Volume: 26, Issue:6, 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
Tyrosine Kinase Inhibitors. 20. Optimization of Substituted Quinazoline and Pyrido[3,4-d]pyrimidine Derivatives as Orally Active, Irreversible Inhibitors of the Epidermal Growth Factor Receptor Family.Journal of medicinal chemistry, , 09-08, Volume: 59, Issue:17, 2016
6-Oxooxazolidine-quinazolines as noncovalent inhibitors with the potential to target mutant forms of EGFR.Bioorganic & medicinal chemistry, , 08-15, Volume: 24, Issue:16, 2016
Toward discovery of mutant EGFR inhibitors; Design, synthesis and in vitro biological evaluation of potent 4-arylamino-6-ureido and thioureido-quinazoline derivatives.Bioorganic & medicinal chemistry, , 08-15, Volume: 24, Issue:16, 2016
Synthesis and evaluation of salicylanilide derivatives as potential epidermal growth factor receptor inhibitors.Chemical biology & drug design, , Volume: 85, Issue:3, 2015
Molecular design and synthesis of certain new quinoline derivatives having potential anticancer activity.European journal of medicinal chemistry, , Sep-18, Volume: 102, 2015
Design, synthesis and biological evaluation of 6-(nitroimidazole-1H-alkyloxyl)-4-anilinoquinazolines as efficient EGFR inhibitors exerting cytotoxic effects both under normoxia and hypoxia.European journal of medicinal chemistry, , Jan-07, Volume: 89, 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 and Evaluation of Clinical Candidate AZD3759, a Potent, Oral Active, Central Nervous System-Penetrant, Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor.Journal of medicinal chemistry, , Oct-22, Volume: 58, Issue:20, 2015
Targeting Drug Resistance in EGFR with Covalent Inhibitors: A Structure-Based Design Approach.Journal of medicinal chemistry, , Sep-10, Volume: 58, Issue:17, 2015
Novel hydrazone moiety-bearing aminopyrimidines as selective inhibitors of epidermal growth factor receptor T790M mutant.European journal of medicinal chemistry, , Nov-02, Volume: 104, 2015
Truncated structures used in search for new lead compounds and in a retrospective analysis of thienopyrimidine-based EGFR inhibitors.European journal of medicinal chemistry, , Apr-13, Volume: 94, 2015
Identification and optimization of new dual inhibitors of B-Raf and epidermal growth factor receptor kinases for overcoming resistance against vemurafenib.Journal of medicinal chemistry, , Mar-27, Volume: 57, Issue:6, 2014
Identification of novel 4-anilinoquinazoline derivatives as potent EGFR inhibitors both under normoxia and hypoxia.Bioorganic & medicinal chemistry, , Dec-15, Volume: 22, Issue:24, 2014
A chemical tuned strategy to develop novel irreversible EGFR-TK inhibitors with improved safety and pharmacokinetic profiles.Journal of medicinal chemistry, , Dec-11, Volume: 57, Issue:23, 2014
Synthesis and evaluation of 2-anilinopyrimidines bearing 3-aminopropamides as potential epidermal growth factor receptor inhibitors.European journal of medicinal chemistry, , Apr-22, Volume: 77, 2014
Synthesis and biological evaluation of compounds which contain pyrazole, thiazole and naphthalene ring as antitumor agents.Bioorganic & medicinal chemistry letters, , May-15, Volume: 24, Issue:10, 2014
Synthesis and biological evaluation of novel tricyclic oxazine and oxazepine fused quinazolines. Part 1: erlotinib analogs.Bioorganic & medicinal chemistry letters, , Feb-01, Volume: 24, Issue:3, 2014
Design, synthesis and in vitro anti-proliferative activity of 4,6-quinazolinediamines as potent EGFR-TK inhibitors.European journal of medicinal chemistry, , Volume: 61, 2013
Protein kinase inhibitor design by targeting the Asp-Phe-Gly (DFG) motif: the role of the DFG motif in the design of epidermal growth factor receptor inhibitors.Journal of medicinal chemistry, , May-23, Volume: 56, Issue:10, 2013
Design, Synthesis, and Biological Evaluation of Novel Conformationally Constrained Inhibitors Targeting EGFR.ACS medicinal chemistry letters, , Oct-10, Volume: 4, Issue:10, 2013
Four-membered heterocycles-containing 4-anilino-quinazoline derivatives as epidermal growth factor receptor (EGFR) kinase inhibitors.Bioorganic & medicinal chemistry letters, , Oct-01, Volume: 23, Issue:19, 2013
Discovery of 2-aryl-8-hydroxy (or methoxy)-isoquinolin-1(2H)-ones as novel EGFR inhibitor by scaffold hopping.Bioorganic & medicinal chemistry, , Nov-15, Volume: 21, Issue:22, 2013
Long-lasting inhibition of EGFR autophosphorylation in A549 tumor cells by intracellular accumulation of non-covalent inhibitors.Bioorganic & medicinal chemistry letters, , Oct-01, Volume: 23, Issue:19, 2013
Structure- and reactivity-based development of covalent inhibitors of the activating and gatekeeper mutant forms of the epidermal growth factor receptor (EGFR).Journal of medicinal chemistry, , Sep-12, Volume: 56, Issue:17, 2013
Nitric oxide donating anilinopyrimidines: synthesis and biological evaluation as EGFR inhibitors.European journal of medicinal chemistry, , Volume: 66, 2013
Novel hybrids of (phenylsulfonyl)furoxan and anilinopyrimidine as potent and selective epidermal growth factor receptor inhibitors for intervention of non-small-cell lung cancer.Journal of medicinal chemistry, , Jun-13, Volume: 56, Issue:11, 2013
Synthesis and biological evaluation of quinazoline and quinoline bearing 2,2,6,6-tetramethylpiperidine-N-oxyl as potential epidermal growth factor receptor(EGFR) tyrosine kinase inhibitors and EPR bio-probe agents.European journal of medicinal chemistry, , Volume: 49, 2012
Synthesis and biological evaluation of N-aryl salicylamides with a hydroxamic acid moiety at 5-position as novel HDAC-EGFR dual inhibitors.Bioorganic & medicinal chemistry, , Jul-15, Volume: 20, Issue:14, 2012
Discovery of novel 5-alkynyl-4-anilinopyrimidines as potent, orally active dual inhibitors of EGFR and Her-2 tyrosine kinases.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 22, Issue:1, 2012
Synthesis, molecular modeling and biological evaluation of 2-(benzylthio)-5-aryloxadiazole derivatives as anti-tumor agents.European journal of medicinal chemistry, , Volume: 47, Issue:1, 2012
Novel oxazolo[4,5-g]quinazolin-2(1H)-ones: dual inhibitors of EGFR and Src protein tyrosine kinases.European journal of medicinal chemistry, , Volume: 55, 2012
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
Discovery of benzimidazole derivatives as novel multi-target EGFR, VEGFR-2 and PDGFR kinase inhibitors.Bioorganic & medicinal chemistry, , Aug-01, Volume: 19, Issue:15, 2011
Synthesis and evaluation of novel pyrimidine-based dual EGFR/Her-2 inhibitors.Bioorganic & medicinal chemistry letters, , Mar-15, Volume: 21, Issue:6, 2011
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
Enhancement of EGFR tyrosine kinase inhibition by C-C multiple bonds-containing anilinoquinazolines.Bioorganic & medicinal chemistry, , Jan-15, Volume: 18, Issue:2, 2010
Design, synthesis and biological evaluation of chrysin long-chain derivatives as potential anticancer agents.Bioorganic & medicinal chemistry, , Volume: 18, Issue:3, 2010
Synthesis and antiproliferative activity of indolizine derivatives incorporating a cyclopropylcarbonyl group against Hep-G2 cancer cell line.European journal of medicinal chemistry, , Volume: 45, Issue:7, 2010
Selectively nonselective kinase inhibition: striking the right balance.Journal of medicinal chemistry, , Feb-25, Volume: 53, Issue:4, 2010
Design and synthesis of tetrahydropyridothieno[2,3-d]pyrimidine scaffold based epidermal growth factor receptor (EGFR) kinase inhibitors: the role of side chain chirality and Michael acceptor group for maximal potency.Journal of medicinal chemistry, , Oct-28, Volume: 53, Issue:20, 2010
Fast-forwarding hit to lead: aurora and epidermal growth factor receptor kinase inhibitor lead identification.Journal of medicinal chemistry, , Jul-08, Volume: 53, Issue:13, 2010
Quinazoline-urea, new protein kinase inhibitors in treatment of prostate cancer.Journal of enzyme inhibition and medicinal chemistry, , Volume: 25, Issue:2, 2010
Design and synthesis of new stabilized combi-triazenes for targeting solid tumors expressing the epidermal growth factor receptor (EGFR) or its closest homologue HER2.Bioorganic & medicinal chemistry letters, , Sep-15, Volume: 19, Issue:18, 2009
Synthesis and stereochemical effects of pyrrolidinyl-acetylenic thieno[3,2-d]pyrimidines as EGFR and ErbB-2 inhibitors.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 19, Issue:1, 2009
Computational studies of epidermal growth factor receptor: docking reliability, three-dimensional quantitative structure-activity relationship analysis, and virtual screening studies.Journal of medicinal chemistry, , Feb-26, Volume: 52, Issue:4, 2009
Kinase domain mutations in cancer: implications for small molecule drug design strategies.Journal of medicinal chemistry, , Mar-26, Volume: 52, Issue:6, 2009
Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases.Nature chemical biology, , Volume: 4, Issue:11, 2008
The T790M mutation in EGFR kinase causes drug resistance by increasing the affinity for ATP.Proceedings of the National Academy of Sciences of the United States of America, , Feb-12, Volume: 105, Issue:6, 2008
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
Syntheses of 4-(indole-3-yl)quinazolines: a new class of epidermal growth factor receptor tyrosine kinase inhibitors.European journal of medicinal chemistry, , Volume: 43, Issue:7, 2008
Structures of lung cancer-derived EGFR mutants and inhibitor complexes: mechanism of activation and insights into differential inhibitor sensitivity.Cancer cell, , Volume: 11, Issue:3, 2007
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
Synthesis and biological evaluation of substituted 6-alkynyl-4-anilinoquinazoline derivatives as potent EGFR inhibitors.Bioorganic & medicinal chemistry letters, , Nov-15, Volume: 17, Issue:22, 2007
Novel 4-anilinoquinazolines with C-6 carbon-linked side chains: synthesis and structure-activity relationship of a series of potent, orally active, EGF receptor tyrosine kinase inhibitors.Bioorganic & medicinal chemistry letters, , May-15, Volume: 16, Issue:10, 2006
Inhibitors of epidermal growth factor receptor tyrosine kinase: optimisation of potency and in vivo pharmacokinetics.Bioorganic & medicinal chemistry letters, , Sep-15, Volume: 16, Issue:18, 2006
Tyrosine kinase inhibitors. 19. 6-Alkynamides of 4-anilinoquinazolines and 4-anilinopyrido[3,4-d]pyrimidines as irreversible inhibitors of the erbB family of tyrosine kinase receptors.Journal of medicinal chemistry, , Feb-23, Volume: 49, Issue:4, 2006
Features of selective kinase inhibitors.Chemistry & biology, , Volume: 12, Issue:6, 2005
A small molecule-kinase interaction map for clinical kinase inhibitors.Nature biotechnology, , Volume: 23, Issue:3, 2005
Synthesis and SAR of potent EGFR/erbB2 dual inhibitors.Bioorganic & medicinal chemistry letters, , Jan-05, Volume: 14, Issue:1, 2004
Syntheses and EGFR and HER-2 kinase inhibitory activities of 4-anilinoquinoline-3-carbonitriles: analogues of three important 4-anilinoquinazolines currently undergoing clinical evaluation as therapeutic antitumor agents.Bioorganic & medicinal chemistry letters, , Oct-21, Volume: 12, Issue:20, 2002
Studies leading to the identification of ZD1839 (IRESSA): an orally active, selective epidermal growth factor receptor tyrosine kinase inhibitor targeted to the treatment of cancer.Bioorganic & medicinal chemistry letters, , Jul-23, Volume: 11, Issue:14, 2001
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The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).Blood, , Oct-01, Volume: 114, Issue:14, 2009
Discovery of kinase inhibitors by high-throughput docking and scoring based on a transferable linear interaction energy model.Journal of medicinal chemistry, , Mar-13, Volume: 51, Issue:5, 2008
Tyrosine kinase inhibitors. 16. 6,5,6-tricyclic benzothieno[3, 2-d]pyrimidines and pyrimido[5,4-b-] and -[4,5-b]ĭndoles as potent inhibitors of the epidermal growth factor receptor tyrosine kinase.Journal of medicinal chemistry, , Dec-30, Volume: 42, Issue:26, 1999
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Tyrphostins IV--highly potent inhibitors of EGF receptor kinase. Structure-activity relationship study of 4-anilidoquinazolines.Bioorganic & medicinal chemistry, , Volume: 4, Issue:8, 1996
Tyrosine kinase inhibitors. 5. Synthesis and structure-activity relationships for 4-[(phenylmethyl)amino]- and 4-(phenylamino)quinazolines as potent adenosine 5'-triphosphate binding site inhibitors of the tyrosine kinase domain of the epidermal growth faJournal of medicinal chemistry, , Sep-01, Volume: 38, Issue:18, 1995
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
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
Identification of a new chemical class of potent angiogenesis inhibitors based on conformational considerations and database searching.Bioorganic & medicinal chemistry letters, , Sep-15, Volume: 13, Issue:18, 2003
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
Tyrosine Kinase Inhibitors. 20. Optimization of Substituted Quinazoline and Pyrido[3,4-d]pyrimidine Derivatives as Orally Active, Irreversible Inhibitors of the Epidermal Growth Factor Receptor Family.Journal of medicinal chemistry, , 09-08, Volume: 59, Issue:17, 2016
Tyrosine kinase inhibitors. 19. 6-Alkynamides of 4-anilinoquinazolines and 4-anilinopyrido[3,4-d]pyrimidines as irreversible inhibitors of the erbB family of tyrosine kinase receptors.Journal of medicinal chemistry, , Feb-23, Volume: 49, Issue:4, 2006
Tyrosine kinase inhibitors. 18. 6-Substituted 4-anilinoquinazolines and 4-anilinopyrido[3,4-d]pyrimidines as soluble, irreversible inhibitors of the epidermal growth factor receptor.Journal of medicinal chemistry, , Feb-01, Volume: 44, Issue:3, 2001
Recent Developments in the Use of Kinase Inhibitors for Management of Viral Infections.Journal of medicinal chemistry, , 01-27, Volume: 65, Issue:2, 2022
Development of Dual Inhibitors Targeting Epidermal Growth Factor Receptor in Cancer Therapy.Journal of medicinal chemistry, , 04-14, Volume: 65, Issue:7, 2022
Therapeutic progression of quinazolines as targeted chemotherapeutic agents.European journal of medicinal chemistry, , Feb-05, Volume: 211, 2021
Lead generation of 1,2-dithiolanes as exon 19 and exon 21 mutant EGFR tyrosine kinase inhibitors.Bioorganic & medicinal chemistry letters, , 06-15, Volume: 29, Issue:12, 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
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 of a Cyclin G Associated Kinase (GAK)/Epidermal Growth Factor Receptor (EGFR) Inhibitor Set to Interrogate the Relationship of EGFR and GAK in Chordoma.Journal of medicinal chemistry, , 05-09, Volume: 62, Issue:9, 2019
Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors.Bioorganic & medicinal chemistry, , 05-01, Volume: 26, Issue:8, 2018
Design, synthesis, antiproliferative activity and docking studies of quinazoline derivatives bearing 2,3-dihydro-indole or 1,2,3,4-tetrahydroquinoline as potential EGFR inhibitors.European journal of medicinal chemistry, , Jun-25, Volume: 154, 2018
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
How to train your inhibitor: Design strategies to overcome resistance to Epidermal Growth Factor Receptor inhibitors.European journal of medicinal chemistry, , Dec-15, Volume: 142, 2017
Discovery of 1-{(3R,4R)-3-[({5-Chloro-2-[(1-methyl-1H-pyrazol-4-yl)amino]-7H-pyrrolo[2,3-d]pyrimidin-4-yl}oxy)methyl]-4-methoxypyrrolidin-1-yl}prop-2-en-1-one (PF-06459988), a Potent, WT Sparing, Irreversible Inhibitor of T790M-Containing EGFR Mutants.Journal of medicinal chemistry, , Mar-10, Volume: 59, Issue:5, 2016
Molecular design and synthesis of certain new quinoline derivatives having potential anticancer activity.European journal of medicinal chemistry, , Sep-18, Volume: 102, 2015
Irreversible protein kinase inhibitors: balancing the benefits and risks.Journal of medicinal chemistry, , Jul-26, Volume: 55, Issue:14, 2012
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
Synthesis and stereochemical effects of pyrrolidinyl-acetylenic thieno[3,2-d]pyrimidines as EGFR and ErbB-2 inhibitors.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 19, Issue:1, 2009
Clinical stage EGFR inhibitors irreversibly alkylate Bmx kinase.Bioorganic & medicinal chemistry letters, , Nov-15, Volume: 18, Issue:22, 2008
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
A small molecule-kinase interaction map for clinical kinase inhibitors.Nature biotechnology, , Volume: 23, Issue:3, 2005
Syntheses and EGFR and HER-2 kinase inhibitory activities of 4-anilinoquinoline-3-carbonitriles: analogues of three important 4-anilinoquinazolines currently undergoing clinical evaluation as therapeutic antitumor agents.Bioorganic & medicinal chemistry letters, , Oct-21, Volume: 12, Issue:20, 2002
Tyrosine kinase inhibitors. 18. 6-Substituted 4-anilinoquinazolines and 4-anilinopyrido[3,4-d]pyrimidines as soluble, irreversible inhibitors of the epidermal growth factor receptor.Journal of medicinal chemistry, , Feb-01, Volume: 44, Issue:3, 2001
Tyrosine kinase inhibitors. 17. Irreversible inhibitors of the epidermal growth factor receptor: 4-(phenylamino)quinazoline- and 4-(phenylamino)pyrido[3,2-d]pyrimidine-6-acrylamides bearing additional solubilizing functions.Journal of medicinal chemistry, , Apr-06, Volume: 43, Issue:7, 2000
Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD).Bioorganic & medicinal chemistry letters, , Dec-01, Volume: 21, Issue:23, 2011
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
Pyrazole urea-based inhibitors of p38 MAP kinase: from lead compound to clinical candidate.Journal of medicinal chemistry, , Jul-04, Volume: 45, Issue:14, 2002
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
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
A small molecule-kinase interaction map for clinical kinase inhibitors.Nature biotechnology, , Volume: 23, Issue:3, 2005
Novel, potent and selective anilinoquinazoline and anilinopyrimidine inhibitors of p38 MAP kinase.Bioorganic & medicinal chemistry letters, , Nov-01, Volume: 14, Issue:21, 2004
Design and synthesis of potent, selective, and orally bioavailable tetrasubstituted imidazole inhibitors of p38 mitogen-activated protein kinase.Journal of medicinal chemistry, , Jun-17, Volume: 42, Issue:12, 1999
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
Recent applications of vinyl sulfone motif in drug design and discovery.European journal of medicinal chemistry, , Apr-15, Volume: 234, 2022
Exploration of novel phthalazinone derivatives as potential efflux transporter inhibitors for reversing multidrug resistance and improving the oral absorption of paclitaxel.European journal of medicinal chemistry, , Apr-05, Volume: 233, 2022
Discovery of potent antiproliferative agents from selected oxygen heterocycles as EGFR tyrosine kinase inhibitors from the U.S. National Cancer Institute database by in silico screening and bioactivity evaluation.Bioorganic & medicinal chemistry letters, , 02-15, Volume: 58, 2022
Novel benzothiazole-based dual VEGFR-2/EGFR inhibitors targeting breast and liver cancers: Synthesis, cytotoxic activity, QSAR and molecular docking studies.Bioorganic & medicinal chemistry letters, , 02-15, Volume: 58, 2022
Kinase Inhibitors as Underexplored Antiviral Agents.Journal of medicinal chemistry, , 01-27, Volume: 65, Issue:2, 2022
Discovery of Novel Allosteric EGFR L858R Inhibitors for the Treatment of Non-Small-Cell Lung Cancer as a Single Agent or in Combination with Osimertinib.Journal of medicinal chemistry, , 10-13, Volume: 65, Issue:19, 2022
Comprehensive review for anticancer hybridized multitargeting HDAC inhibitors.European journal of medicinal chemistry, , Jan-01, Volume: 209, 2021
FDA-approved pyrimidine-fused bicyclic heterocycles for cancer therapy: Synthesis and clinical application.European journal of medicinal chemistry, , Mar-15, Volume: 214, 2021
Design, synthesis and evaluation of new quinazolin-4-one derivatives as apoptotic enhancers and autophagy inhibitors with potent antitumor activity.European journal of medicinal chemistry, , Oct-15, Volume: 222, 2021
[no title available]Bioorganic & medicinal chemistry letters, , 10-01, Volume: 49, 2021
Design, synthesis and assessment of new series of quinazolinone derivatives as EGFR inhibitors along with their cytotoxic evaluation against MCF7 and A549 cancer cell lines.Bioorganic & medicinal chemistry letters, , 06-01, Volume: 41, 2021
Discovery of novel JAK2 and EGFR inhibitors from a series of thiazole-based chalcone derivatives.RSC medicinal chemistry, , Mar-01, Volume: 12, Issue:3, 2021
Potential of substituted quinazolines to interact with multiple targets in the treatment of cancer.Bioorganic & medicinal chemistry, , 04-01, Volume: 35, 2021
Design, synthesis and biological evaluation of novel 2,4-diaryl pyrimidine derivatives as selective EGFREuropean journal of medicinal chemistry, , Feb-15, Volume: 212, 2021
Discovery of a novel series of substituted quinolines acting as anticancer agents and selective EGFR blocker: Molecular docking study.Bioorganic & medicinal chemistry letters, , 07-15, Volume: 44, 2021
Pyrimidine-based EGFR TK inhibitors in targeted cancer therapy.European journal of medicinal chemistry, , Oct-05, Volume: 221, 2021
Anticancer potential of some imidazole and fused imidazole derivatives: exploring the mechanism RSC medicinal chemistry, , Aug-01, Volume: 11, Issue:8, 2020
[no title available]Journal of medicinal chemistry, , 11-25, Volume: 63, Issue:22, 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
Design, synthesis and biological evaluation of novel heptamethine cyanine dye-erlotinib conjugates as antitumor agents.Bioorganic & medicinal chemistry letters, , 12-01, Volume: 30, Issue:23, 2020
Design, synthesis, biological evaluation, QSAR analysis and molecular modelling of new thiazol-benzimidazoles as EGFR inhibitors.Bioorganic & medicinal chemistry, , 09-15, Volume: 28, Issue:18, 2020
Design and synthesis of a novel class EGFR/HER2 dual inhibitors containing tricyclic oxazine fused quinazolines scaffold.Bioorganic & medicinal chemistry letters, , 05-01, Volume: 30, Issue:9, 2020
Development of a Potent Brain-Penetrant EGFR Tyrosine Kinase Inhibitor against Malignant Brain Tumors.ACS medicinal chemistry letters, , Oct-08, Volume: 11, Issue:10, 2020
Acetylene Group, Friend or Foe in Medicinal Chemistry.Journal of medicinal chemistry, , 06-11, Volume: 63, Issue:11, 2020
Design, synthesis and biological evaluation of 2-amino-4-(1,2,4-triazol)pyridine derivatives as potent EGFR inhibitors to overcome TKI-resistance.European journal of medicinal chemistry, , Feb-01, Volume: 187, 2020
Synthesis and anticancer activity of thiourea derivatives bearing a benzodioxole moiety with EGFR inhibitory activity, apoptosis assay and molecular docking study.European journal of medicinal chemistry, , Jul-15, Volume: 198, 2020
Synthesis and biological evaluation of novel xanthine derivatives as potential apoptotic antitumor agents.European journal of medicinal chemistry, , Aug-15, Volume: 176, 2019
Lead generation of 1,2-dithiolanes as exon 19 and exon 21 mutant EGFR tyrosine kinase inhibitors.Bioorganic & medicinal chemistry letters, , 06-15, Volume: 29, Issue:12, 2019
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 a new series of thiazolyl-pyrazolines as dual EGFR and HER2 inhibitors.European journal of medicinal chemistry, , Nov-15, Volume: 182, 2019
Design, Synthesis and Anticancer Evaluation of New Substituted Thiophene-Quinoline Derivatives.Bioorganic & medicinal chemistry, , 10-01, Volume: 27, Issue:19, 2019
Utilizing comprehensive and mini-kinome panels to optimize the selectivity of quinoline inhibitors for cyclin G associated kinase (GAK).Bioorganic & medicinal chemistry letters, , 07-15, Volume: 29, Issue:14, 2019
Design of a Cyclin G Associated Kinase (GAK)/Epidermal Growth Factor Receptor (EGFR) Inhibitor Set to Interrogate the Relationship of EGFR and GAK in Chordoma.Journal of medicinal chemistry, , 05-09, Volume: 62, Issue:9, 2019
Design, Synthesis, and Biological Evaluation of 6-Substituted Thieno[3,2- d]pyrimidine Analogues as Dual Epidermal Growth Factor Receptor Kinase and Microtubule Inhibitors.Journal of medicinal chemistry, , 02-14, Volume: 62, Issue:3, 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
Discovery of novel thienoquinoline-2-carboxamide chalcone derivatives as antiproliferative EGFR tyrosine kinase inhibitors.Bioorganic & medicinal chemistry, , 03-15, Volume: 27, Issue:6, 2019
Structure based designing of triazolopyrimidone-based reversible inhibitors for kinases involved in NSCLC.Bioorganic & medicinal chemistry letters, , 07-01, Volume: 29, Issue:13, 2019
New oxadiazoles with selective-COX-2 and EGFR dual inhibitory activity: Design, synthesis, cytotoxicity evaluation and in silico studies.European journal of medicinal chemistry, , Dec-01, Volume: 183, 2019
Design, synthesis, mechanistic and histopathological studies of small-molecules of novel indole-2-carboxamides and pyrazino[1,2-a]indol-1(2H)-ones as potential anticancer agents effecting the reactive oxygen species production.European journal of medicinal chemistry, , Feb-25, Volume: 146, 2018
Novel series of 6-(2-substitutedacetamido)-4-anilinoquinazolines as EGFR-ERK signal transduction inhibitors in MCF-7 breast cancer cells.European journal of medicinal chemistry, , Jul-15, Volume: 155, 2018
Design, synthesis and preclinical evaluation of 5-methyl-NBioorganic & medicinal chemistry letters, , 10-01, Volume: 28, Issue:18, 2018
Design, synthesis and anticancer evaluation of novel spirobenzo[h]chromene and spirochromane derivatives with dual EGFR and B-RAF inhibitory activities.European journal of medicinal chemistry, , Apr-25, Volume: 150, 2018
Discovery of novel substituted benzo-anellated 4-benzylamino pyrrolopyrimidines as dual EGFR and VEGFR2 inhibitors.Bioorganic & medicinal chemistry letters, , 06-15, Volume: 27, Issue:12, 2017
Design, synthesis and biological evaluation of WZ4002 analogues as EGFR inhibitors.Bioorganic & medicinal chemistry letters, , 11-01, Volume: 27, Issue:21, 2017
Discovery of N-((3R,4R)-4-Fluoro-1-(6-((3-methoxy-1-methyl-1H-pyrazol-4-yl)amino)-9-methyl-9H-purin-2-yl)pyrrolidine-3-yl)acrylamide (PF-06747775) through Structure-Based Drug Design: A High Affinity Irreversible Inhibitor Targeting Oncogenic EGFR MutantsJournal of medicinal chemistry, , 04-13, Volume: 60, Issue:7, 2017
[no title available]European journal of medicinal chemistry, , Dec-01, Volume: 141, 2017
Discovery of potential anticancer multi-targeted ligustrazine based cyclohexanone and oxime analogs overcoming the cancer multidrug resistance.European journal of medicinal chemistry, , Jul-28, Volume: 135, 2017
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
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
[no title available]European journal of medicinal chemistry, , Nov-29, Volume: 124, 2016
Synthesis and biological evaluation of novel tricyclic oxazine and oxazepine fused quinazolines. Part 2: Gefitinib analogs.Bioorganic & medicinal chemistry letters, , 10-01, Volume: 26, Issue:19, 2016
Novel morpholin-3-one fused quinazoline derivatives as EGFR tyrosine kinase inhibitors.Bioorganic & medicinal chemistry letters, , Mar-15, Volume: 26, Issue:6, 2016
Chiral 6-aryl-furo[2,3-d]pyrimidin-4-amines as EGFR inhibitors.European journal of medicinal chemistry, , Aug-25, Volume: 119, 2016
Discovery of 1-{(3R,4R)-3-[({5-Chloro-2-[(1-methyl-1H-pyrazol-4-yl)amino]-7H-pyrrolo[2,3-d]pyrimidin-4-yl}oxy)methyl]-4-methoxypyrrolidin-1-yl}prop-2-en-1-one (PF-06459988), a Potent, WT Sparing, Irreversible Inhibitor of T790M-Containing EGFR Mutants.Journal of medicinal chemistry, , Mar-10, Volume: 59, Issue:5, 2016
4-Aminoindazolyl-dihydrofuro[3,4-d]pyrimidines as non-covalent inhibitors of mutant epidermal growth factor receptor tyrosine kinase.Bioorganic & medicinal chemistry letters, , Jan-15, Volume: 26, Issue:2, 2016
Design, synthesis and biological evaluation of pyrazolyl-nitroimidazole derivatives as potential EGFR/HER-2 kinase inhibitors.Bioorganic & medicinal chemistry letters, , Jan-15, Volume: 26, Issue:2, 2016
Pyridones as Highly Selective, Noncovalent Inhibitors of T790M Double Mutants of EGFR.ACS medicinal chemistry letters, , Jan-14, Volume: 7, Issue:1, 2016
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
Molecular design and synthesis of certain new quinoline derivatives having potential anticancer activity.European journal of medicinal chemistry, , Sep-18, Volume: 102, 2015
Synthetic approaches, functionalization and therapeutic potential of quinazoline and quinazolinone skeletons: the advances continue.European journal of medicinal chemistry, , Jan-27, Volume: 90, 2015
Noncovalent Mutant Selective Epidermal Growth Factor Receptor Inhibitors: A Lead Optimization Case Study.Journal of medicinal chemistry, , Nov-25, Volume: 58, Issue:22, 2015
Synthesis and Evaluation of Novel Erlotinib-NSAID Conjugates as More Comprehensive Anticancer Agents.ACS medicinal chemistry letters, , Oct-08, Volume: 6, Issue:10, 2015
Design, synthesis and biological activities of novel oxazolo[4,5-g]quinazolin-2(1H)-one derivatives as EGFR inhibitors.European journal of medicinal chemistry, , Aug-28, Volume: 101, 2015
Selective Inhibitors of Cyclin G Associated Kinase (GAK) as Anti-Hepatitis C Agents.Journal of medicinal chemistry, , Apr-23, Volume: 58, Issue:8, 2015
Design, synthesis and molecular modeling of biquinoline-pyridine hybrids as a new class of potential EGFR and HER-2 kinase inhibitors.Bioorganic & medicinal chemistry letters, , Sep-15, Volume: 24, Issue:18, 2014
Design, synthesis and molecular modeling of pyrazole-quinoline-pyridine hybrids as a new class of antimicrobial and anticancer agents.European journal of medicinal chemistry, , Apr-09, Volume: 76, 2014
Discovery of selective and noncovalent diaminopyrimidine-based inhibitors of epidermal growth factor receptor containing the T790M resistance mutation.Journal of medicinal chemistry, , Dec-11, Volume: 57, Issue:23, 2014
Schiff's base derivatives bearing nitroimidazole and quinoline nuclei: new class of anticancer agents and potential EGFR tyrosine kinase inhibitors.Bioorganic & medicinal chemistry letters, , Apr-01, Volume: 24, Issue:7, 2014
Design, synthesis and biological evaluation of novel 6-alkenylamides substituted of 4-anilinothieno[2,3-d]pyrimidines as irreversible epidermal growth factor receptor inhibitors.Bioorganic & medicinal chemistry, , Apr-01, Volume: 22, Issue:7, 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
Discovery and Biological Evaluation of Novel Dual EGFR/c-Met Inhibitors.ACS medicinal chemistry letters, , Apr-10, Volume: 5, Issue:4, 2014
Synthesis and biological evaluation of novel tricyclic oxazine and oxazepine fused quinazolines. Part 1: erlotinib analogs.Bioorganic & medicinal chemistry letters, , Feb-01, Volume: 24, Issue:3, 2014
Schiff's base derivatives bearing nitroimidazole moiety: new class of antibacterial, anticancer agents and potential EGFR tyrosine kinase inhibitors.Bioorganic & medicinal chemistry letters, , Dec-01, Volume: 23, Issue:23, 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
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
Design, modification and 3D QSAR studies of novel naphthalin-containing pyrazoline derivatives with/without thiourea skeleton as anticancer agents.Bioorganic & medicinal chemistry, , Mar-01, Volume: 21, Issue:5, 2013
Discovery of novel 4-anilinoquinazoline derivatives as potent inhibitors of epidermal growth factor receptor with antitumor activity.Bioorganic & medicinal chemistry, , Oct-01, Volume: 21, Issue:19, 2013
Design, synthesis and molecular docking of α,β-unsaturated cyclohexanone analogous of curcumin as potent EGFR inhibitors with antiproliferative activity.Bioorganic & medicinal chemistry, , Jan-15, Volume: 21, Issue:2, 2013
Design, synthesis and biological evaluation of novel 4-anilinoquinazolines with C-6 urea-linked side chains as inhibitors of the epidermal growth factor receptor.Bioorganic & medicinal chemistry, , Dec-15, Volume: 21, Issue:24, 2013
Structure- and reactivity-based development of covalent inhibitors of the activating and gatekeeper mutant forms of the epidermal growth factor receptor (EGFR).Journal of medicinal chemistry, , Sep-12, Volume: 56, Issue:17, 2013
Development of erlotinib derivatives as CIP2A-ablating agents independent of EGFR activity.Bioorganic & medicinal chemistry, , Oct-15, Volume: 20, Issue:20, 2012
Design and synthesis of 4,6-substituted-(diaphenylamino)quinazolines as potent EGFR inhibitors with antitumor activity.Bioorganic & medicinal chemistry, , Jan-01, Volume: 20, Issue:1, 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
Design, synthesis and biological evaluation of pyrazolyl-thiazolinone derivatives as potential EGFR and HER-2 kinase inhibitors.Bioorganic & medicinal chemistry, , Mar-15, Volume: 20, Issue:6, 2012
Discovery of novel 5-alkynyl-4-anilinopyrimidines as potent, orally active dual inhibitors of EGFR and Her-2 tyrosine kinases.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 22, Issue:1, 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
Design, synthesis and biological evaluation of N-phenylsulfonylnicotinamide derivatives as novel antitumor inhibitors.Bioorganic & medicinal chemistry, , Feb-15, Volume: 20, Issue:4, 2012
Novel inhibitors of epidermal growth factor receptor: (4-(Arylamino)-7H-pyrrolo[2,3-d]pyrimidin-6-yl)(1H-indol-2-yl)methanones and (1H-indol-2-yl)(4-(phenylamino)thieno[2,3-d]pyrimidin-6-yl)methanones.Bioorganic & medicinal chemistry, , Jan-01, Volume: 20, Issue:1, 2012
The combination of 4-anilinoquinazoline and cinnamic acid: a novel mode of binding to the epidermal growth factor receptor tyrosine kinase.Bioorganic & medicinal chemistry, , Aug-15, Volume: 19, Issue:16, 2011
Synthesis, molecular modeling and biological evaluation of chalcone thiosemicarbazide derivatives as novel anticancer agents.European journal of medicinal chemistry, , Volume: 46, Issue:9, 2011
Synthesis, molecular docking and evaluation of thiazolyl-pyrazoline derivatives as EGFR TK inhibitors and potential anticancer agents.Bioorganic & medicinal chemistry letters, , Sep-15, Volume: 21, Issue:18, 2011
Structural analysis of the mechanism of inhibition and allosteric activation of the kinase domain of HER2 protein.The Journal of biological chemistry, , May-27, Volume: 286, Issue:21, 2011
Synthesis and evaluation of novel pyrimidine-based dual EGFR/Her-2 inhibitors.Bioorganic & medicinal chemistry letters, , Mar-15, Volume: 21, Issue:6, 2011
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
Metronidazole acid acyl sulfonamide: a novel class of anticancer agents and potential EGFR tyrosine kinase inhibitors.Bioorganic & medicinal chemistry, , Oct-15, Volume: 19, Issue:20, 2011
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, molecular modeling, and biological evaluation of cinnamic acid metronidazole ester derivatives as novel anticancer agents.Bioorganic & medicinal chemistry, , Jul-15, Volume: 18, Issue:14, 2010
Discovery of 7-(4-(3-ethynylphenylamino)-7-methoxyquinazolin-6-yloxy)-N-hydroxyheptanamide (CUDc-101) as a potent multi-acting HDAC, EGFR, and HER2 inhibitor for the treatment of cancer.Journal of medicinal chemistry, , Mar-11, Volume: 53, Issue:5, 2010
Enhancement of EGFR tyrosine kinase inhibition by C-C multiple bonds-containing anilinoquinazolines.Bioorganic & medicinal chemistry, , Jan-15, Volume: 18, Issue:2, 2010
Design, synthesis and biological evaluation of thiazolidinone derivatives as potential EGFR and HER-2 kinase inhibitors.Bioorganic & medicinal chemistry, , Jan-01, Volume: 18, Issue:1, 2010
Substituted 4-amino-1H-pyrazolo[3,4-d]pyrimidines as multi-targeted inhibitors of insulin-like growth factor-1 receptor (IGF1R) and members of ErbB-family receptor kinases.Bioorganic & medicinal chemistry letters, , Oct-15, Volume: 20, Issue:20, 2010
Synthesis and biological evaluation of pyrazole derivatives containing thiourea skeleton as anticancer agents.Bioorganic & medicinal chemistry, , Jul-01, Volume: 18, Issue:13, 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
Synthesis and structure-activity relationships of N-benzyl-N-(X-2-hydroxybenzyl)-N'-phenylureas and thioureas as antitumor agents.Bioorganic & medicinal chemistry, , Jan-01, Volume: 18, Issue:1, 2010
Selectively nonselective kinase inhibition: striking the right balance.Journal of medicinal chemistry, , Feb-25, Volume: 53, Issue:4, 2010
Synthesis, biological evaluation and molecular docking studies of amide-coupled benzoic nitrogen mustard derivatives as potential antitumor agents.Bioorganic & medicinal chemistry, , Jan-15, Volume: 18, Issue:2, 2010
Imidazo[2,1-b]thiazoles: multitargeted inhibitors of both the insulin-like growth factor receptor and members of the epidermal growth factor family of receptor tyrosine kinases.Bioorganic & medicinal chemistry letters, , Apr-15, Volume: 20, Issue:8, 2010
Synthesis and biological evaluation of 4-anilinoquinolines as potent inhibitors of epidermal growth factor receptor.Journal of medicinal chemistry, , Apr-08, Volume: 53, Issue:7, 2010
Synthesis and stereochemical effects of pyrrolidinyl-acetylenic thieno[3,2-d]pyrimidines as EGFR and ErbB-2 inhibitors.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 19, Issue:1, 2009
Discovery of a novel Her-1/Her-2 dual tyrosine kinase inhibitor for the treatment of Her-1 selective inhibitor-resistant non-small cell lung cancer.Journal of medicinal chemistry, , Nov-12, Volume: 52, Issue:21, 2009
Structural insights into how irreversible inhibitors can overcome drug resistance in EGFR.Bioorganic & medicinal chemistry, , Apr-01, Volume: 16, Issue:7, 2008
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
Syntheses of 4-(indole-3-yl)quinazolines: a new class of epidermal growth factor receptor tyrosine kinase inhibitors.European journal of medicinal chemistry, , Volume: 43, Issue:7, 2008
Synthesis and biological evaluation of substituted 6-alkynyl-4-anilinoquinazoline derivatives as potent EGFR inhibitors.Bioorganic & medicinal chemistry letters, , Nov-15, Volume: 17, Issue:22, 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
Tyrosine kinase inhibitors. 19. 6-Alkynamides of 4-anilinoquinazolines and 4-anilinopyrido[3,4-d]pyrimidines as irreversible inhibitors of the erbB family of tyrosine kinase receptors.Journal of medicinal chemistry, , Feb-23, Volume: 49, Issue:4, 2006
A small molecule-kinase interaction map for clinical kinase inhibitors.Nature biotechnology, , Volume: 23, Issue:3, 2005
Synthesis and SAR of potent EGFR/erbB2 dual inhibitors.Bioorganic & medicinal chemistry letters, , Jan-05, Volume: 14, Issue:1, 2004
Syntheses and EGFR and HER-2 kinase inhibitory activities of 4-anilinoquinoline-3-carbonitriles: analogues of three important 4-anilinoquinazolines currently undergoing clinical evaluation as therapeutic antitumor agents.Bioorganic & medicinal chemistry letters, , Oct-21, Volume: 12, Issue:20, 2002
[no title available],
Synthesis, anticancer activity and molecular modeling studies of 1,2,4-triazole derivatives as EGFR inhibitors.European journal of medicinal chemistry, , Aug-05, Volume: 156, 2018
Synthesis and biological evaluation of pyrrolopyridazine derivatives as novel HER-2 tyrosine kinase inhibitors.Bioorganic & medicinal chemistry letters, , Nov-15, Volume: 19, Issue:22, 2009
Exploration of novel phthalazinone derivatives as potential efflux transporter inhibitors for reversing multidrug resistance and improving the oral absorption of paclitaxel.European journal of medicinal chemistry, , Apr-05, Volume: 233, 2022
Development of Dual Inhibitors Targeting Epidermal Growth Factor Receptor in Cancer Therapy.Journal of medicinal chemistry, , 04-14, Volume: 65, Issue:7, 2022
Therapeutic progression of quinazolines as targeted chemotherapeutic agents.European journal of medicinal chemistry, , Feb-05, Volume: 211, 2021
FDA-approved pyrimidine-fused bicyclic heterocycles for cancer therapy: Synthesis and clinical application.European journal of medicinal chemistry, , Mar-15, Volume: 214, 2021
[no title available]Journal of medicinal chemistry, , 09-09, Volume: 64, Issue:17, 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
Design, synthesis, biological evaluation, QSAR analysis and molecular modelling of new thiazol-benzimidazoles as EGFR inhibitors.Bioorganic & medicinal chemistry, , 09-15, Volume: 28, Issue:18, 2020
Design and synthesis of a novel class EGFR/HER2 dual inhibitors containing tricyclic oxazine fused quinazolines scaffold.Bioorganic & medicinal chemistry letters, , 05-01, Volume: 30, Issue:9, 2020
Targeting Her2-insYVMA with Covalent Inhibitors-A Focused Compound Screening and Structure-Based Design Approach.Journal of medicinal chemistry, , 10-22, Volume: 63, Issue:20, 2020
[no title available]Bioorganic & medicinal chemistry letters, , 08-15, Volume: 30, Issue:16, 2020
Synthesis and anticancer activity of thiourea derivatives bearing a benzodioxole moiety with EGFR inhibitory activity, apoptosis assay and molecular docking study.European journal of medicinal chemistry, , Jul-15, Volume: 198, 2020
Lead generation of 1,2-dithiolanes as exon 19 and exon 21 mutant EGFR tyrosine kinase inhibitors.Bioorganic & medicinal chemistry letters, , 06-15, Volume: 29, Issue:12, 2019
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
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
Why Some Targets Benefit from beyond Rule of Five Drugs.Journal of medicinal chemistry, , 11-27, Volume: 62, Issue:22, 2019
Design of a Cyclin G Associated Kinase (GAK)/Epidermal Growth Factor Receptor (EGFR) Inhibitor Set to Interrogate the Relationship of EGFR and GAK in Chordoma.Journal of medicinal chemistry, , 05-09, Volume: 62, Issue:9, 2019
6,7-Dimorpholinoalkoxy quinazoline derivatives as potent EGFR inhibitors with enhanced antiproliferative activities against tumor cells.European journal of medicinal chemistry, , Mar-10, Volume: 147, 2018
Design and Evaluation of Potent EGFR Inhibitors through the Incorporation of Macrocyclic Polyamine Moieties into the 4-Anilinoquinazoline Scaffold.Journal of medicinal chemistry, , 12-27, Volume: 61, Issue:24, 2018
Design, synthesis, antiproliferative activity, molecular docking and cell cycle analysis of some novel (morpholinosulfonyl) isatins with potential EGFR inhibitory activity.European journal of medicinal chemistry, , Aug-05, Volume: 156, 2018
Discovery of anilino-furo[2,3-d]pyrimidine derivatives as dual inhibitors of EGFR/HER2 tyrosine kinase and their anticancer activity.European journal of medicinal chemistry, , Jan-20, Volume: 144, 2018
Quinazoline-1-deoxynojirimycin hybrids as high active dual inhibitors of EGFR and α-glucosidase.Bioorganic & medicinal chemistry letters, , 09-15, Volume: 27, Issue:18, 2017
Synthesis and investigation of novel 6-(1,2,3-triazol-4-yl)-4-aminoquinazolin derivatives possessing hydroxamic acid moiety for cancer therapy.Bioorganic & medicinal chemistry, , 01-01, Volume: 25, Issue:1, 2017
[no title available]European journal of medicinal chemistry, , Sep-29, Volume: 138, 2017
How to train your inhibitor: Design strategies to overcome resistance to Epidermal Growth Factor Receptor inhibitors.European journal of medicinal chemistry, , Dec-15, Volume: 142, 2017
Synthesis and in vitro biological evaluation of novel quinazoline derivatives.Bioorganic & medicinal chemistry letters, , 04-01, Volume: 27, Issue:7, 2017
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Design, synthesis and biological evaluation of novel EGFR/HER2 dual inhibitors bearing a oxazolo[4,5-g]quinazolin-2(1H)-one scaffold.European journal of medicinal chemistry, , Sep-14, Volume: 120, 2016
Design, synthesis and biological evaluation of pyrazolyl-nitroimidazole derivatives as potential EGFR/HER-2 kinase inhibitors.Bioorganic & medicinal chemistry letters, , Jan-15, Volume: 26, Issue:2, 2016
Molecular design and synthesis of certain new quinoline derivatives having potential anticancer activity.European journal of medicinal chemistry, , Sep-18, Volume: 102, 2015
Targeting EGFR/HER2 tyrosine kinases with a new potent series of 6-substituted 4-anilinoquinazoline hybrids: Design, synthesis, kinase assay, cell-based assay, and molecular docking.Bioorganic & medicinal chemistry letters, , Nov-15, Volume: 25, Issue:22, 2015
Truncated structures used in search for new lead compounds and in a retrospective analysis of thienopyrimidine-based EGFR inhibitors.European journal of medicinal chemistry, , Apr-13, Volume: 94, 2015
Design and synthesis of Lapatinib derivatives containing a branched side chain as HER1/HER2 targeting antitumor drug candidates.European journal of medicinal chemistry, , Nov-24, Volume: 87, 2014
Discovery of novel selective inhibitors for EGFR-T790M/L858R.Bioorganic & medicinal chemistry letters, , Feb-01, Volume: 22, Issue:3, 2012
Discovery of novel 5-alkynyl-4-anilinopyrimidines as potent, orally active dual inhibitors of EGFR and Her-2 tyrosine kinases.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 22, Issue:1, 2012
Synthesis and biological evaluation of 4-[3-chloro-4-(3-fluorobenzyloxy)anilino]-6-(3-substituted-phenoxy)pyrimidines as dual EGFR/ErbB-2 kinase inhibitors.Bioorganic & medicinal chemistry, , Jan-15, Volume: 20, Issue:2, 2012
Synthesis and biological evaluation of pyrimidine-based dual inhibitors of human epidermal growth factor receptor 1 (HER-1) and HER-2 tyrosine kinases.Journal of medicinal chemistry, , Mar-22, Volume: 55, Issue:6, 2012
Discovery of novel EGFR tyrosine kinase inhibitors by structure-based virtual screening.Bioorganic & medicinal chemistry letters, , Jun-15, Volume: 22, Issue:12, 2012
Novel inhibitors of epidermal growth factor receptor: (4-(Arylamino)-7H-pyrrolo[2,3-d]pyrimidin-6-yl)(1H-indol-2-yl)methanones and (1H-indol-2-yl)(4-(phenylamino)thieno[2,3-d]pyrimidin-6-yl)methanones.Bioorganic & medicinal chemistry, , Jan-01, Volume: 20, Issue:1, 2012
Structural analysis of the mechanism of inhibition and allosteric activation of the kinase domain of HER2 protein.The Journal of biological chemistry, , May-27, Volume: 286, Issue:21, 2011
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
Discovery of 7-(4-(3-ethynylphenylamino)-7-methoxyquinazolin-6-yloxy)-N-hydroxyheptanamide (CUDc-101) as a potent multi-acting HDAC, EGFR, and HER2 inhibitor for the treatment of cancer.Journal of medicinal chemistry, , Mar-11, Volume: 53, Issue:5, 2010
Substituted 4-amino-1H-pyrazolo[3,4-d]pyrimidines as multi-targeted inhibitors of insulin-like growth factor-1 receptor (IGF1R) and members of ErbB-family receptor kinases.Bioorganic & medicinal chemistry letters, , Oct-15, Volume: 20, Issue:20, 2010
Selectively nonselective kinase inhibition: striking the right balance.Journal of medicinal chemistry, , Feb-25, Volume: 53, Issue:4, 2010
Novel chimeric histone deacetylase inhibitors: a series of lapatinib hybrides as potent inhibitors of epidermal growth factor receptor (EGFR), human epidermal growth factor receptor 2 (HER2), and histone deacetylase activity.Journal of medicinal chemistry, , Dec-23, Volume: 53, Issue:24, 2010
Imidazo[2,1-b]thiazoles: multitargeted inhibitors of both the insulin-like growth factor receptor and members of the epidermal growth factor family of receptor tyrosine kinases.Bioorganic & medicinal chemistry letters, , Apr-15, Volume: 20, Issue:8, 2010
Computational studies of epidermal growth factor receptor: docking reliability, three-dimensional quantitative structure-activity relationship analysis, and virtual screening studies.Journal of medicinal chemistry, , Feb-26, Volume: 52, Issue:4, 2009
Discovery of a novel Her-1/Her-2 dual tyrosine kinase inhibitor for the treatment of Her-1 selective inhibitor-resistant non-small cell lung cancer.Journal of medicinal chemistry, , Nov-12, Volume: 52, Issue:21, 2009
6-Ethynylthieno[3,2-d]- and 6-ethynylthieno[2,3-d]pyrimidin-4-anilines as tunable covalent modifiers of ErbB kinases.Proceedings of the National Academy of Sciences of the United States of America, , Feb-26, Volume: 105, Issue:8, 2008
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
Alkynyl pyrimidines as dual EGFR/ErbB2 kinase inhibitors.Bioorganic & medicinal chemistry letters, , May-01, Volume: 16, Issue:9, 2006
Optimization and SAR for dual ErbB-1/ErbB-2 tyrosine kinase inhibition in the 6-furanylquinazoline series.Bioorganic & medicinal chemistry letters, , Sep-01, Volume: 16, Issue:17, 2006
A small molecule-kinase interaction map for clinical kinase inhibitors.Nature biotechnology, , Volume: 23, Issue:3, 2005
Synthesis and SAR of potent EGFR/erbB2 dual inhibitors.Bioorganic & medicinal chemistry letters, , Jan-05, Volume: 14, Issue:1, 2004
[no title available],
New thiazole-based derivatives as EGFR/HER2 and DHFR inhibitors: Synthesis, molecular modeling simulations and anticancer activity.European journal of medicinal chemistry, , Nov-05, Volume: 241, 2022
Discovery of a novel series of substituted quinolines acting as anticancer agents and selective EGFR blocker: Molecular docking study.Bioorganic & medicinal chemistry letters, , 07-15, Volume: 44, 2021
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 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
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
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
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
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Discovery of Evobrutinib: An Oral, Potent, and Highly Selective, Covalent Bruton's Tyrosine Kinase (BTK) Inhibitor for the Treatment of Immunological Diseases.Journal of medicinal chemistry, , 09-12, Volume: 62, Issue:17, 2019
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
Recent Developments in the Use of Kinase Inhibitors for Management of Viral Infections.Journal of medicinal chemistry, , 01-27, Volume: 65, Issue:2, 2022
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
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
(6,7-Dimethoxy-2,4-dihydroindeno[1,2-c]pyrazol-3-yl)phenylamines: platelet-derived growth factor receptor tyrosine kinase inhibitors with broad antiproliferative activity against tumor cells.Journal of medicinal chemistry, , Dec-29, Volume: 48, Issue:26, 2005
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
How to train your inhibitor: Design strategies to overcome resistance to Epidermal Growth Factor Receptor inhibitors.European journal of medicinal chemistry, , Dec-15, Volume: 142, 2017
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
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
[no title available]Journal of medicinal chemistry, , 12-24, Volume: 63, Issue:24, 2020
Synthesis and investigation of novel 6-(1,2,3-triazol-4-yl)-4-aminoquinazolin derivatives possessing hydroxamic acid moiety for cancer therapy.Bioorganic & medicinal chemistry, , 01-01, Volume: 25, Issue:1, 2017
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Discovery of new 4-alkoxyquinazoline-based derivatives as potent VEGFR2 inhibitors.Chemical biology & drug design, , Volume: 86, Issue:5, 2015
Discovery of SPH5030, a Selective, Potent, and Irreversible Tyrosine Kinase Inhibitor for HER2-Amplified and HER2-Mutant Cancer Treatment.Journal of medicinal chemistry, , 04-14, Volume: 65, Issue:7, 2022
The Ascension of Targeted Covalent Inhibitors.Journal of medicinal chemistry, , 04-28, Volume: 65, Issue:8, 2022
Discovery of a novel series of substituted quinolines acting as anticancer agents and selective EGFR blocker: Molecular docking study.Bioorganic & medicinal chemistry letters, , 07-15, Volume: 44, 2021
[no title available]Journal of medicinal chemistry, , 12-24, Volume: 63, Issue:24, 2020
The Exploration of Chirality for Improved Druggability within the Human Kinome.Journal of medicinal chemistry, , 01-23, Volume: 63, Issue:2, 2020
Targeting Her2-insYVMA with Covalent Inhibitors-A Focused Compound Screening and Structure-Based Design Approach.Journal of medicinal chemistry, , 10-22, Volume: 63, Issue:20, 2020
Lead generation of 1,2-dithiolanes as exon 19 and exon 21 mutant EGFR tyrosine kinase inhibitors.Bioorganic & medicinal chemistry letters, , 06-15, Volume: 29, Issue:12, 2019
Design of a Cyclin G Associated Kinase (GAK)/Epidermal Growth Factor Receptor (EGFR) Inhibitor Set to Interrogate the Relationship of EGFR and GAK in Chordoma.Journal of medicinal chemistry, , 05-09, Volume: 62, Issue:9, 2019
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Molecular design and synthesis of certain new quinoline derivatives having potential anticancer activity.European journal of medicinal chemistry, , Sep-18, Volume: 102, 2015
Targeting EGFR/HER2 tyrosine kinases with a new potent series of 6-substituted 4-anilinoquinazoline hybrids: Design, synthesis, kinase assay, cell-based assay, and molecular docking.Bioorganic & medicinal chemistry letters, , Nov-15, Volume: 25, Issue:22, 2015
Therapeutic melting pot of never in mitosis gene a related kinase 2 (Nek2): a perspective on Nek2 as an oncology target and recent advancements in Nek2 small molecule inhibition.Journal of medicinal chemistry, , Jul-24, Volume: 57, Issue:14, 2014
Design, synthesis and biological evaluation of novel pyrimidine, 3-cyanopyridine and m-amino-N-phenylbenzamide based monocyclic EGFR tyrosine kinase inhibitors.Bioorganic & medicinal chemistry, , Jun-01, Volume: 21, Issue:11, 2013
Structure-Based Approach for the Discovery of Pyrrolo[3,2-d]pyrimidine-Based EGFR T790M/L858R Mutant Inhibitors.ACS medicinal chemistry letters, , Feb-14, Volume: 4, Issue:2, 2013
Discovery of novel selective inhibitors for EGFR-T790M/L858R.Bioorganic & medicinal chemistry letters, , Feb-01, Volume: 22, Issue:3, 2012
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
Synthesis and stereochemical effects of pyrrolidinyl-acetylenic thieno[3,2-d]pyrimidines as EGFR and ErbB-2 inhibitors.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 19, Issue:1, 2009
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
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
Optimization of 6,7-disubstituted-4-(arylamino)quinoline-3-carbonitriles as orally active, irreversible inhibitors of human epidermal growth factor receptor-2 kinase activity.Journal of medicinal chemistry, , Feb-24, Volume: 48, Issue:4, 2005
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Discovery of a JAK3-Selective Inhibitor: Functional Differentiation of JAK3-Selective Inhibition over pan-JAK or JAK1-Selective Inhibition.ACS chemical biology, , 12-16, Volume: 11, Issue:12, 2016
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
Prevention of organ allograft rejection by a specific Janus kinase 3 inhibitor.Science (New York, N.Y.), , Oct-31, Volume: 302, Issue:5646, 2003
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
Discovery of N-(3-bromo-1H-indol-5-yl)-quinazolin-4-amine as an effective molecular skeleton to develop reversible/irreversible pan-HER inhibitors.European journal of medicinal chemistry, , Apr-05, Volume: 233, 2022
Synthesis and biological evaluation of new series of quinazoline derivatives as EGFR/HER2 dual-target inhibitors.Bioorganic & medicinal chemistry letters, , 07-01, Volume: 67, 2022
The Ascension of Targeted Covalent Inhibitors.Journal of medicinal chemistry, , 04-28, Volume: 65, Issue:8, 2022
[no title available]Journal of medicinal chemistry, , 02-10, Volume: 65, Issue:3, 2022
Design, synthesis and assessment of new series of quinazolinone derivatives as EGFR inhibitors along with their cytotoxic evaluation against MCF7 and A549 cancer cell lines.Bioorganic & medicinal chemistry letters, , 06-01, Volume: 41, 2021
[no title available]Bioorganic & medicinal chemistry, , 03-15, Volume: 34, 2021
FDA-approved pyrimidine-fused bicyclic heterocycles for cancer therapy: Synthesis and clinical application.European journal of medicinal chemistry, , Mar-15, Volume: 214, 2021
Discovery and optimization of covalent EGFR T790M/L858R mutant inhibitors.Bioorganic & medicinal chemistry letters, , 11-15, Volume: 52, 2021
The Exploration of Chirality for Improved Druggability within the Human Kinome.Journal of medicinal chemistry, , 01-23, Volume: 63, Issue:2, 2020
Design, synthesis, biological evaluation, QSAR analysis and molecular modelling of new thiazol-benzimidazoles as EGFR inhibitors.Bioorganic & medicinal chemistry, , 09-15, Volume: 28, Issue:18, 2020
Discovery of new thieno[3,2-d]pyrimidine derivatives targeting EGFREuropean journal of medicinal chemistry, , Aug-01, Volume: 199, 2020
Design, synthesis and SAR study of 2-aminopyrimidines with diverse Michael addition acceptors for chemically tuning the potency against EGFRBioorganic & medicinal chemistry, , 10-01, Volume: 28, Issue:19, 2020
Discovery of 4,6-pyrimidinediamine derivatives as novel dual EGFR/FGFR inhibitors aimed EGFR/FGFR1-positive NSCLC.European journal of medicinal chemistry, , Feb-01, Volume: 187, 2020
Targeting Her2-insYVMA with Covalent Inhibitors-A Focused Compound Screening and Structure-Based Design Approach.Journal of medicinal chemistry, , 10-22, Volume: 63, Issue:20, 2020
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
Design, synthesis and biological evaluation of benzoylacrylic acid shikonin ester derivatives as irreversible dual inhibitors of tubulin and EGFR.Bioorganic & medicinal chemistry, , 12-01, Volume: 27, Issue:23, 2019
Lead generation of 1,2-dithiolanes as exon 19 and exon 21 mutant EGFR tyrosine kinase inhibitors.Bioorganic & medicinal chemistry letters, , 06-15, Volume: 29, Issue:12, 2019
Click chemistry for improvement in selectivity of quinazoline-based kinase inhibitors for mutant epidermal growth factor receptors.Bioorganic & medicinal chemistry letters, , 02-01, Volume: 29, Issue:3, 2019
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 of a Cyclin G Associated Kinase (GAK)/Epidermal Growth Factor Receptor (EGFR) Inhibitor Set to Interrogate the Relationship of EGFR and GAK in Chordoma.Journal of medicinal chemistry, , 05-09, Volume: 62, Issue:9, 2019
Discovery of new quinazoline derivatives as irreversible dual EGFR/HER2 inhibitors and their anticancer activities - Part 1.Bioorganic & medicinal chemistry letters, , 02-15, Volume: 29, Issue:4, 2019
Discovery of a Furanopyrimidine-Based Epidermal Growth Factor Receptor Inhibitor (DBPR112) as a Clinical Candidate for the Treatment of Non-Small Cell Lung Cancer.Journal of medicinal chemistry, , 11-27, Volume: 62, Issue:22, 2019
Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors.Bioorganic & medicinal chemistry, , 05-01, Volume: 26, Issue:8, 2018
Trisubstituted Pyridinylimidazoles as Potent Inhibitors of the Clinically Resistant L858R/T790M/C797S EGFR Mutant: Targeting of Both Hydrophobic Regions and the Phosphate Binding Site.Journal of medicinal chemistry, , 07-13, Volume: 60, Issue:13, 2017
Design, synthesis, and docking studies of quinazoline analogues bearing aryl semicarbazone scaffolds as potent EGFR inhibitors.Bioorganic & medicinal chemistry, , 06-15, Volume: 25, Issue:12, 2017
Design, synthesis, and evaluation of A-ring-modified lamellarin N analogues as noncovalent inhibitors of the EGFR T790M/L858R mutant.Bioorganic & medicinal chemistry, , 12-15, Volume: 25, Issue:24, 2017
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Design, synthesis and biological evaluation of WZ4002 analogues as EGFR inhibitors.Bioorganic & medicinal chemistry letters, , 11-01, Volume: 27, Issue:21, 2017
Challenges and Perspectives on the Development of Small-Molecule EGFR Inhibitors against T790M-Mediated Resistance in Non-Small-Cell Lung Cancer.Journal of medicinal chemistry, , 07-28, Volume: 59, Issue:14, 2016
Design, synthesis, and docking studies of afatinib analogs bearing cinnamamide moiety as potent EGFR inhibitors.Bioorganic & medicinal chemistry, , Apr-01, Volume: 24, Issue:7, 2016
Structure-activity study of quinazoline derivatives leading to the discovery of potent EGFR-T790M inhibitors.European journal of medicinal chemistry, , Sep-18, Volume: 102, 2015
Design, synthesis and biological evaluation of novel 6-alkenylamides substituted of 4-anilinothieno[2,3-d]pyrimidines as irreversible epidermal growth factor receptor inhibitors.Bioorganic & medicinal chemistry, , Apr-01, Volume: 22, Issue:7, 2014
A chemical tuned strategy to develop novel irreversible EGFR-TK inhibitors with improved safety and pharmacokinetic profiles.Journal of medicinal chemistry, , Dec-11, Volume: 57, Issue:23, 2014
Design, synthesis and biological evaluation of novel 4-anilinoquinazolines with C-6 urea-linked side chains as inhibitors of the epidermal growth factor receptor.Bioorganic & medicinal chemistry, , Dec-15, Volume: 21, Issue:24, 2013
Structure- and reactivity-based development of covalent inhibitors of the activating and gatekeeper mutant forms of the epidermal growth factor receptor (EGFR).Journal of medicinal chemistry, , Sep-12, Volume: 56, Issue:17, 2013
Irreversible protein kinase inhibitors: balancing the benefits and risks.Journal of medicinal chemistry, , Jul-26, Volume: 55, Issue:14, 2012
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
Fast-forwarding hit to lead: aurora and epidermal growth factor receptor kinase inhibitor lead identification.Journal of medicinal chemistry, , Jul-08, Volume: 53, Issue:13, 2010
Synthesis and stereochemical effects of pyrrolidinyl-acetylenic thieno[3,2-d]pyrimidines as EGFR and ErbB-2 inhibitors.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 19, Issue:1, 2009
[no title available],
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Discovery of 3-(1H-indol-3-yl)-4-[2-(4-methylpiperazin-1-yl)quinazolin-4-yl]pyrrole-2,5-dione (AEB071), a potent and selective inhibitor of protein kinase C isotypes.Journal of medicinal chemistry, , Oct-22, Volume: 52, Issue:20, 2009
Development of Dual Inhibitors Targeting Epidermal Growth Factor Receptor in Cancer Therapy.Journal of medicinal chemistry, , 04-14, Volume: 65, Issue:7, 2022
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Vascular endothelial growth factor (VEGF) receptors: drugs and new inhibitors.Journal of medicinal chemistry, , Dec-27, Volume: 55, Issue:24, 2012
Synthesis and in vitro EGFR (ErbB1) tyrosine kinase inhibitory activity of 4-N-substituted 6-aryl-7H-pyrrolo[2,3-d]pyrimidine-4-amines.European journal of medicinal chemistry, , Volume: 46, Issue:12, 2011
The T790M mutation in EGFR kinase causes drug resistance by increasing the affinity for ATP.Proceedings of the National Academy of Sciences of the United States of America, , Feb-12, Volume: 105, Issue:6, 2008
Structures of lung cancer-derived EGFR mutants and inhibitor complexes: mechanism of activation and insights into differential inhibitor sensitivity.Cancer cell, , Volume: 11, Issue:3, 2007
Design of a Cyclin G Associated Kinase (GAK)/Epidermal Growth Factor Receptor (EGFR) Inhibitor Set to Interrogate the Relationship of EGFR and GAK in Chordoma.Journal of medicinal chemistry, , 05-09, Volume: 62, Issue:9, 2019
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Structure-based virtual screening of Src kinase inhibitors.Bioorganic & medicinal chemistry, , Apr-15, Volume: 17, Issue:8, 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
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
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
Development of Dual Inhibitors Targeting Epidermal Growth Factor Receptor in Cancer Therapy.Journal of medicinal chemistry, , 04-14, Volume: 65, Issue:7, 2022
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Novel pyrrolo[2,1-f][1,2,4]triazin-4-amines: Dual inhibitors of EGFR and HER2 protein tyrosine kinases.Bioorganic & medicinal chemistry letters, , Jan-15, Volume: 21, Issue:2, 2011
Discovery and preclinical evaluation of [4-[[1-(3-fluorophenyl)methyl]-1H-indazol-5-ylamino]-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yl]carbamic acid, (3S)-3-morpholinylmethyl ester (BMS-599626), a selective and orally efficacious inhibitor of human epiderJournal of medicinal chemistry, , Nov-12, Volume: 52, Issue:21, 2009
Design of a Cyclin G Associated Kinase (GAK)/Epidermal Growth Factor Receptor (EGFR) Inhibitor Set to Interrogate the Relationship of EGFR and GAK in Chordoma.Journal of medicinal chemistry, , 05-09, Volume: 62, Issue:9, 2019
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
[no title available],
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
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
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
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
Design of a Cyclin G Associated Kinase (GAK)/Epidermal Growth Factor Receptor (EGFR) Inhibitor Set to Interrogate the Relationship of EGFR and GAK in Chordoma.Journal of medicinal chemistry, , 05-09, Volume: 62, Issue:9, 2019
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazoles: identification of a potent Aurora kinase inhibitor with a favorable antitumor kinase inhibition profile.Journal of medicinal chemistry, , Nov-30, Volume: 49, Issue:24, 2006
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
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
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
Design of a Cyclin G Associated Kinase (GAK)/Epidermal Growth Factor Receptor (EGFR) Inhibitor Set to Interrogate the Relationship of EGFR and GAK in Chordoma.Journal of medicinal chemistry, , 05-09, Volume: 62, Issue:9, 2019
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
Synthesis and investigation of novel 6-(1,2,3-triazol-4-yl)-4-aminoquinazolin derivatives possessing hydroxamic acid moiety for cancer therapy.Bioorganic & medicinal chemistry, , 01-01, Volume: 25, Issue:1, 2017
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Discovery of AZD8931, an Equipotent, Reversible Inhibitor of Signaling by EGFR, HER2, and HER3 Receptors.ACS medicinal chemistry letters, , Aug-08, Volume: 4, Issue:8, 2013
The Ascension of Targeted Covalent Inhibitors.Journal of medicinal chemistry, , 04-28, Volume: 65, Issue:8, 2022
Advanced approaches of developing targeted covalent drugs.RSC medicinal chemistry, , Dec-14, Volume: 13, Issue:12, 2022
FDA-approved pyrimidine-fused bicyclic heterocycles for cancer therapy: Synthesis and clinical application.European journal of medicinal chemistry, , Mar-15, Volume: 214, 2021
Design, synthesis and assessment of new series of quinazolinone derivatives as EGFR inhibitors along with their cytotoxic evaluation against MCF7 and A549 cancer cell lines.Bioorganic & medicinal chemistry letters, , 06-01, Volume: 41, 2021
Design, synthesis, biological evaluation, QSAR analysis and molecular modelling of new thiazol-benzimidazoles as EGFR inhibitors.Bioorganic & medicinal chemistry, , 09-15, Volume: 28, Issue:18, 2020
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
Design of a Cyclin G Associated Kinase (GAK)/Epidermal Growth Factor Receptor (EGFR) Inhibitor Set to Interrogate the Relationship of EGFR and GAK in Chordoma.Journal of medicinal chemistry, , 05-09, Volume: 62, Issue:9, 2019
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
How to train your inhibitor: Design strategies to overcome resistance to Epidermal Growth Factor Receptor inhibitors.European journal of medicinal chemistry, , Dec-15, Volume: 142, 2017
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Tyrosine Kinase Inhibitors. 20. Optimization of Substituted Quinazoline and Pyrido[3,4-d]pyrimidine Derivatives as Orally Active, Irreversible Inhibitors of the Epidermal Growth Factor Receptor Family.Journal of medicinal chemistry, , 09-08, Volume: 59, Issue:17, 2016
Structure-activity study of quinazoline derivatives leading to the discovery of potent EGFR-T790M inhibitors.European journal of medicinal chemistry, , Sep-18, Volume: 102, 2015
Structure- and reactivity-based development of covalent inhibitors of the activating and gatekeeper mutant forms of the epidermal growth factor receptor (EGFR).Journal of medicinal chemistry, , Sep-12, Volume: 56, Issue:17, 2013
Discovery of a potent dual EGFR/HER-2 inhibitor L-2 (selatinib) for the treatment of cancer.European journal of medicinal chemistry, , Volume: 69, 2013
Discovery of novel 5-alkynyl-4-anilinopyrimidines as potent, orally active dual inhibitors of EGFR and Her-2 tyrosine kinases.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 22, Issue:1, 2012
Synthesis and evaluation of novel pyrimidine-based dual EGFR/Her-2 inhibitors.Bioorganic & medicinal chemistry letters, , Mar-15, Volume: 21, Issue:6, 2011
Thienopyrimidine-based dual EGFR/ErbB-2 inhibitors.Bioorganic & medicinal chemistry letters, , Feb-01, Volume: 19, Issue:3, 2009
Synthesis and stereochemical effects of pyrrolidinyl-acetylenic thieno[3,2-d]pyrimidines as EGFR and ErbB-2 inhibitors.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 19, Issue:1, 2009
Synthesis and biological evaluation of pyrrolopyridazine derivatives as novel HER-2 tyrosine kinase inhibitors.Bioorganic & medicinal chemistry letters, , Nov-15, Volume: 19, Issue:22, 2009
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Discovery of CC-930, an orally active anti-fibrotic JNK inhibitor.Bioorganic & medicinal chemistry letters, , Feb-01, Volume: 22, Issue:3, 2012
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
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Targeting EGFR/HER2 tyrosine kinases with a new potent series of 6-substituted 4-anilinoquinazoline hybrids: Design, synthesis, kinase assay, cell-based assay, and molecular docking.Bioorganic & medicinal chemistry letters, , Nov-15, Volume: 25, Issue:22, 2015
Design and synthesis of novel pyrimido[4,5-b]azepine derivatives as HER2/EGFR dual inhibitors.Bioorganic & medicinal chemistry, , Apr-15, Volume: 21, Issue:8, 2013
Structure-Based Approach for the Discovery of Pyrrolo[3,2-d]pyrimidine-Based EGFR T790M/L858R Mutant Inhibitors.ACS medicinal chemistry letters, , Feb-14, Volume: 4, Issue:2, 2013
Design and synthesis of novel human epidermal growth factor receptor 2 (HER2)/epidermal growth factor receptor (EGFR) dual inhibitors bearing a pyrrolo[3,2-d]pyrimidine scaffold.Journal of medicinal chemistry, , Dec-08, Volume: 54, Issue:23, 2011
Discovery of novel mutant-combating ALK and ROS1 dual inhibitors bearing imidazolidin-2-one moiety with reasonable PK properties.European journal of medicinal chemistry, , Jun-01, Volume: 171, 2019
Discovery of novel 2,4-diarylaminopyrimidine analogues as ALK and ROS1 dual inhibitors to overcome crizotinib-resistant mutants including G1202R.European journal of medicinal chemistry, , Jan-01, Volume: 143, 2018
[no title available]European journal of medicinal chemistry, , Oct-05, Volume: 158, 2018
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Pyridazinone derivatives displaying highly potent and selective inhibitory activities against c-Met tyrosine kinase.European journal of medicinal chemistry, , Jan-27, Volume: 108, 2016
Design, synthesis and biological evaluation of novel 4-arylaminopyrimidine derivatives possessing a hydrazone moiety as dual inhibitors of L1196M ALK and ROS1.European journal of medicinal chemistry, , Nov-10, Volume: 123, 2016
Discovery and Biological Evaluation of Novel Dual EGFR/c-Met Inhibitors.ACS medicinal chemistry letters, , Apr-10, Volume: 5, Issue:4, 2014
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Discovery and Biological Evaluation of Novel Dual EGFR/c-Met Inhibitors.ACS medicinal chemistry letters, , Apr-10, Volume: 5, Issue:4, 2014
Imidazo[2,1-b]thiazoles: multitargeted inhibitors of both the insulin-like growth factor receptor and members of the epidermal growth factor family of receptor tyrosine kinases.Bioorganic & medicinal chemistry letters, , Apr-15, Volume: 20, Issue:8, 2010
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
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The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
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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
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
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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
Recent Progress of Small-Molecule Epidermal Growth Factor Receptor (EGFR) Inhibitors against C797S Resistance in Non-Small-Cell Lung Cancer.Journal of medicinal chemistry, , 05-24, Volume: 61, Issue:10, 2018
Discovery of N-(5-((5-chloro-4-((2-(isopropylsulfonyl)phenyl)amino)pyrimidin-2-yl)amino)-4-methoxy-2-(4-methyl-1,4-diazepan-1-yl)phenyl)acrylamide (CHMFL-ALK/EGFR-050) as a potent ALK/EGFR dual kinase inhibitor capable of overcoming a variety of ALK/EGFR European journal of medicinal chemistry, , Oct-20, Volume: 139, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
Design of a Cyclin G Associated Kinase (GAK)/Epidermal Growth Factor Receptor (EGFR) Inhibitor Set to Interrogate the Relationship of EGFR and GAK in Chordoma.Journal of medicinal chemistry, , 05-09, Volume: 62, Issue:9, 2019
Synthesis and biological evaluation of 4-anilinoquinolines as potent inhibitors of epidermal growth factor receptor.Journal of medicinal chemistry, , Apr-08, Volume: 53, Issue:7, 2010
Synthesis and biological evaluation of substituted 6-alkynyl-4-anilinoquinazoline derivatives as potent EGFR inhibitors.Bioorganic & medicinal chemistry letters, , Nov-15, Volume: 17, Issue:22, 2007
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Identification of N,1,4,4-tetramethyl-8-{[4-(4-methylpiperazin-1-yl)phenyl]amino}-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide (PHA-848125), a potent, orally available cyclin dependent kinase inhibitor.Journal of medicinal chemistry, , Aug-27, Volume: 52, Issue:16, 2009
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
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The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
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
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Synthesis and biological evaluation of crown ether fused quinazoline analogues as potent EGFR inhibitors.Bioorganic & medicinal chemistry letters, , Oct-01, Volume: 22, Issue:19, 2012
Comprehensive review for anticancer hybridized multitargeting HDAC inhibitors.European journal of medicinal chemistry, , Jan-01, Volume: 209, 2021
Kinase and Histone Deacetylase Hybrid Inhibitors for Cancer Therapy.Journal of medicinal chemistry, , 04-11, Volume: 62, Issue:7, 2019
Synthesis and investigation of novel 6-(1,2,3-triazol-4-yl)-4-aminoquinazolin derivatives possessing hydroxamic acid moiety for cancer therapy.Bioorganic & medicinal chemistry, , 01-01, Volume: 25, Issue:1, 2017
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Discovery of 7-(4-(3-ethynylphenylamino)-7-methoxyquinazolin-6-yloxy)-N-hydroxyheptanamide (CUDc-101) as a potent multi-acting HDAC, EGFR, and HER2 inhibitor for the treatment of cancer.Journal of medicinal chemistry, , Mar-11, Volume: 53, Issue:5, 2010
Selectively nonselective kinase inhibition: striking the right balance.Journal of medicinal chemistry, , Feb-25, Volume: 53, Issue:4, 2010
[no title available],
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Synthesis and evaluation of a series of pyridine and pyrimidine derivatives as type II c-Met inhibitors.Bioorganic & medicinal chemistry, , 06-15, Volume: 25, Issue:12, 2017
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Discovery and Biological Evaluation of Novel Dual EGFR/c-Met Inhibitors.ACS medicinal chemistry letters, , Apr-10, Volume: 5, Issue:4, 2014
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
Review of the development of BTK inhibitors in overcoming the clinical limitations of ibrutinib.European journal of medicinal chemistry, , Feb-05, Volume: 229, 2022
The Ascension of Targeted Covalent Inhibitors.Journal of medicinal chemistry, , 04-28, Volume: 65, Issue:8, 2022
Ophiorrhines F and G, Key Biogenetic Intermediates of Ophiorrhine Alkaloids from Journal of natural products, , 02-25, Volume: 85, Issue:2, 2022
Optimization of a novel piperazinone series as potent selective peripheral covalent BTK inhibitors.Bioorganic & medicinal chemistry letters, , 03-15, Volume: 60, 2022
[no title available]Journal of medicinal chemistry, , 02-10, Volume: 65, Issue:3, 2022
Discovery of 1-Amino-1Journal of medicinal chemistry, , 11-11, Volume: 64, Issue:21, 2021
Characterization of ibrutinib as a non-covalent inhibitor of SRC-family kinases.Bioorganic & medicinal chemistry letters, , 02-15, Volume: 34, 2021
Discovery of LOU064 (Remibrutinib), a Potent and Highly Selective Covalent Inhibitor of Bruton's Tyrosine Kinase.Journal of medicinal chemistry, , 05-28, Volume: 63, Issue:10, 2020
Discovery of potent and highly selective covalent inhibitors of Bruton's tyrosine kinase bearing triazine scaffold.European journal of medicinal chemistry, , Aug-01, Volume: 199, 2020
Discovery of quinoline-based irreversible BTK inhibitors.Bioorganic & medicinal chemistry letters, , 07-15, Volume: 30, Issue:14, 2020
Discovery and Biological evaluation of pyrimido[4,5-d]pyrimidine-2,4(1H,3H)-dione derivatives as potent Bruton's tyrosine kinase inhibitors.Bioorganic & medicinal chemistry, , 08-01, Volume: 27, Issue:15, 2019
Design, synthesis and evaluation of novel 7H-pyrrolo[2,3-d]pyrimidin-4-amine derivatives as potent, selective and reversible Bruton's tyrosine kinase (BTK) inhibitors for the treatment of rheumatoid arthritis.European journal of medicinal chemistry, , May-01, Volume: 169, 2019
Discovery of Branebrutinib (BMS-986195): A Strategy for Identifying a Highly Potent and Selective Covalent Inhibitor Providing Rapid in Vivo Inactivation of Bruton's Tyrosine Kinase (BTK).Journal of medicinal chemistry, , 04-11, Volume: 62, Issue:7, 2019
Design of Potent and Selective Covalent Inhibitors of Bruton's Tyrosine Kinase Targeting an Inactive Conformation.ACS medicinal chemistry letters, , Oct-10, Volume: 10, Issue:10, 2019
Aminopyrazole Carboxamide Bruton's Tyrosine Kinase Inhibitors. Irreversible to Reversible Covalent Reactive Group Tuning.ACS medicinal chemistry letters, , Jan-10, Volume: 10, Issue:1, 2019
Discovery of Zanubrutinib (BGB-3111), a Novel, Potent, and Selective Covalent Inhibitor of Bruton's Tyrosine Kinase.Journal of medicinal chemistry, , 09-12, Volume: 62, Issue:17, 2019
Targeting the MKK7-JNK (Mitogen-Activated Protein Kinase Kinase 7-c-Jun N-Terminal Kinase) Pathway with Covalent Inhibitors.Journal of medicinal chemistry, , 03-14, Volume: 62, Issue:5, 2019
Discovery of 4,7-Diamino-5-(4-phenoxyphenyl)-6-methylene-pyrimido[5,4- b]pyrrolizines as Novel Bruton's Tyrosine Kinase Inhibitors.Journal of medicinal chemistry, , 05-24, Volume: 61, Issue:10, 2018
[no title available]European journal of medicinal chemistry, , Feb-10, Volume: 145, 2018
[no title available]European journal of medicinal chemistry, , May-05, Volume: 131, 2017
Discovery of (R)-5-(benzo[d][1,3]dioxol-5-yl)-7-((1-(vinylsulfonyl)pyrrolidin-2-yl)methyl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine (B6) as a potent Bmx inhibitor for the treatment of NSCLC.Bioorganic & medicinal chemistry letters, , 09-01, Volume: 27, Issue:17, 2017
[no title available]European journal of medicinal chemistry, , Sep-08, Volume: 137, 2017
Discovery of (R)-1-(3-(4-Amino-3-(3-chloro-4-(pyridin-2-ylmethoxy)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)prop-2-en-1-one (CHMFL-EGFR-202) as a Novel Irreversible EGFR Mutant Kinase Inhibitor with a Distinct Binding Mode.Journal of medicinal chemistry, , 04-13, Volume: 60, Issue:7, 2017
Structure-Guided Development of Covalent and Mutant-Selective Pyrazolopyrimidines to Target T790M Drug Resistance in Epidermal Growth Factor Receptor.Journal of medicinal chemistry, , 09-28, Volume: 60, Issue:18, 2017
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Imidazo[1,5-a]quinoxalines as irreversible BTK inhibitors for the treatment of rheumatoid arthritis.Bioorganic & medicinal chemistry letters, , Nov-01, Volume: 21, Issue:21, 2011
Discovery of novel Ponatinib analogues for reducing KDR activity as potent FGFRs inhibitors.European journal of medicinal chemistry, , Jan-27, Volume: 126, 2017
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Discovery of imidazopyridine derivatives as novel c-Met kinase inhibitors: Synthesis, SAR study, and biological activity.Bioorganic chemistry, , Volume: 70, 2017
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
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 thiazolidin-4-one urea analogues as novel multikinase inhibitors that potently inhibit FLT3 and VEGFR2.Bioorganic & medicinal chemistry, , 05-15, Volume: 27, Issue:10, 2019
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Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
Synthesis and biological evaluation of new series of quinazoline derivatives as EGFR/HER2 dual-target inhibitors.Bioorganic & medicinal chemistry letters, , 07-01, Volume: 67, 2022
Discovery of a Furanopyrimidine-Based Epidermal Growth Factor Receptor Inhibitor (DBPR112) as a Clinical Candidate for the Treatment of Non-Small Cell Lung Cancer.Journal of medicinal chemistry, , 11-27, Volume: 62, Issue:22, 2019
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
How to train your inhibitor: Design strategies to overcome resistance to Epidermal Growth Factor Receptor inhibitors.European journal of medicinal chemistry, , Dec-15, Volume: 142, 2017
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Recent Progress of Small-Molecule Epidermal Growth Factor Receptor (EGFR) Inhibitors against C797S Resistance in Non-Small-Cell Lung Cancer.Journal of medicinal chemistry, , 05-24, Volume: 61, Issue:10, 2018
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The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Discovery of Entrectinib: A New 3-Aminoindazole As a Potent Anaplastic Lymphoma Kinase (ALK), c-ros Oncogene 1 Kinase (ROS1), and Pan-Tropomyosin Receptor Kinases (Pan-TRKs) inhibitor.Journal of medicinal chemistry, , Apr-14, Volume: 59, Issue:7, 2016
Design, Synthesis, and Structure-Activity Relationship Study of 2-Oxo-3,4-dihydropyrimido[4,5- d]pyrimidines as New Colony Stimulating Factor 1 Receptor (CSF1R) Kinase Inhibitors.Journal of medicinal chemistry, , 03-22, Volume: 61, Issue:6, 2018
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Identification and optimization of new dual inhibitors of B-Raf and epidermal growth factor receptor kinases for overcoming resistance against vemurafenib.Journal of medicinal chemistry, , Mar-27, Volume: 57, Issue:6, 2014
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
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 evaluation of sulfonylurea-containing 4-phenoxyquinolines as highly selective c-Met kinase inhibitors.Bioorganic & medicinal chemistry, , 07-01, Volume: 27, Issue:13, 2019
Design, synthesis and biological evaluation of novel 4-phenoxyquinoline derivatives containing 3-oxo-3,4-dihydroquinoxaline moiety as c-Met kinase inhibitors.Bioorganic & medicinal chemistry, , 08-15, Volume: 25, Issue:16, 2017
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Design and biological evaluation of novel 4-(2-fluorophenoxy)quinoline derivatives bearing an imidazolone moiety as c-Met kinase inhibitors.Bioorganic & medicinal chemistry, , Aug-01, Volume: 23, Issue:15, 2015
Design, synthesis and pharmacological evaluation of 6,7-disubstituted-4-phenoxyquinoline derivatives as potential antitumor agents.Bioorganic chemistry, , Volume: 57, 2014
Design and optimization of novel 4-(2-fluorophenoxy)quinoline derivatives bearing a hydrazone moiety as c-Met kinase inhibitors.European journal of medicinal chemistry, , Nov-24, Volume: 87, 2014
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
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
Synthesis and investigation of novel 6-(1,2,3-triazol-4-yl)-4-aminoquinazolin derivatives possessing hydroxamic acid moiety for cancer therapy.Bioorganic & medicinal chemistry, , 01-01, Volume: 25, Issue:1, 2017
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Dual nicotinamide phosphoribosyltransferase and epidermal growth factor receptor inhibitors for the treatment of cancer.European journal of medicinal chemistry, , Feb-05, Volume: 211, 2021
Identification and Optimization of Novel Cathepsin C Inhibitors Derived from EGFR Inhibitors.Journal of medicinal chemistry, , 06-27, Volume: 62, Issue:12, 2019
[no title available]Bioorganic & medicinal chemistry letters, , 04-15, Volume: 28, Issue:7, 2018
Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors.Bioorganic & medicinal chemistry, , 05-01, Volume: 26, Issue:8, 2018
Trisubstituted Pyridinylimidazoles as Potent Inhibitors of the Clinically Resistant L858R/T790M/C797S EGFR Mutant: Targeting of Both Hydrophobic Regions and the Phosphate Binding Site.Journal of medicinal chemistry, , 07-13, Volume: 60, Issue:13, 2017
Design, synthesis and biological evaluation of WZ4002 analogues as EGFR inhibitors.Bioorganic & medicinal chemistry letters, , 11-01, Volume: 27, Issue:21, 2017
Discovery of N-(5-((5-chloro-4-((2-(isopropylsulfonyl)phenyl)amino)pyrimidin-2-yl)amino)-4-methoxy-2-(4-methyl-1,4-diazepan-1-yl)phenyl)acrylamide (CHMFL-ALK/EGFR-050) as a potent ALK/EGFR dual kinase inhibitor capable of overcoming a variety of ALK/EGFR European journal of medicinal chemistry, , Oct-20, Volume: 139, 2017
Discovery of a potent dual ALK and EGFR T790M inhibitor.European journal of medicinal chemistry, , Aug-18, Volume: 136, 2017
Trisubstituted Imidazoles with a Rigidized Hinge Binding Motif Act As Single Digit nM Inhibitors of Clinically Relevant EGFR L858R/T790M and L858R/T790M/C797S Mutants: An Example of Target Hopping.Journal of medicinal chemistry, , 06-08, Volume: 60, Issue:11, 2017
Structure-Guided Development of Covalent and Mutant-Selective Pyrazolopyrimidines to Target T790M Drug Resistance in Epidermal Growth Factor Receptor.Journal of medicinal chemistry, , 09-28, Volume: 60, Issue:18, 2017
Discovery of 5-(methylthio)pyrimidine derivatives as L858R/T790M mutant selective epidermal growth factor receptor (EGFR) inhibitors.Bioorganic & medicinal chemistry, , 06-15, Volume: 24, Issue:12, 2016
Challenges and Perspectives on the Development of Small-Molecule EGFR Inhibitors against T790M-Mediated Resistance in Non-Small-Cell Lung Cancer.Journal of medicinal chemistry, , 07-28, Volume: 59, Issue:14, 2016
Targeting Drug Resistance in EGFR with Covalent Inhibitors: A Structure-Based Design Approach.Journal of medicinal chemistry, , Sep-10, Volume: 58, Issue:17, 2015
Novel hydrazone moiety-bearing aminopyrimidines as selective inhibitors of epidermal growth factor receptor T790M mutant.European journal of medicinal chemistry, , Nov-02, Volume: 104, 2015
Structure-based design and synthesis of covalent-reversible inhibitors to overcome drug resistance in EGFR.Bioorganic & medicinal chemistry, , Jun-15, Volume: 23, Issue:12, 2015
Synthesis and evaluation of 2-anilinopyrimidines bearing 3-aminopropamides as potential epidermal growth factor receptor inhibitors.European journal of medicinal chemistry, , Apr-22, Volume: 77, 2014
Discovery of pteridin-7(8H)-one-based irreversible inhibitors targeting the epidermal growth factor receptor (EGFR) kinase T790M/L858R mutant.Journal of medicinal chemistry, , Oct-24, Volume: 56, Issue:20, 2013
Structure- and reactivity-based development of covalent inhibitors of the activating and gatekeeper mutant forms of the epidermal growth factor receptor (EGFR).Journal of medicinal chemistry, , Sep-12, Volume: 56, Issue:17, 2013
Nitric oxide donating anilinopyrimidines: synthesis and biological evaluation as EGFR inhibitors.European journal of medicinal chemistry, , Volume: 66, 2013
Novel hybrids of (phenylsulfonyl)furoxan and anilinopyrimidine as potent and selective epidermal growth factor receptor inhibitors for intervention of non-small-cell lung cancer.Journal of medicinal chemistry, , Jun-13, Volume: 56, Issue:11, 2013
Irreversible protein kinase inhibitors: balancing the benefits and risks.Journal of medicinal chemistry, , Jul-26, Volume: 55, Issue:14, 2012
Design, synthesis, and biological evaluation of novel conformationally constrained inhibitors targeting epidermal growth factor receptor threonine⁷⁹⁰ → methionine⁷⁹⁰ mutant.Journal of medicinal chemistry, , Mar-22, Volume: 55, Issue:6, 2012
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Optimization of 6,6-dimethyl pyrrolo[3,4-c]pyrazoles: Identification of PHA-793887, a potent CDK inhibitor suitable for intravenous dosing.Bioorganic & medicinal chemistry, , Mar-01, Volume: 18, Issue:5, 2010
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Identification of 1-(3-(6,7-dimethoxyquinazolin-4-yloxy)phenyl)-3-(5-(1,1,1-trifluoro-2-methylpropan-2-yl)isoxazol-3-yl)urea hydrochloride (CEP-32496), a highly potent and orally efficacious inhibitor of V-RAF murine sarcoma viral oncogene homologue B1 (BJournal of medicinal chemistry, , Feb-09, Volume: 55, Issue:3, 2012
[no title available]European journal of medicinal chemistry, , Aug-05, Volume: 238, 2022
Design, synthesis and SAR study of 2-aminopyrimidines with diverse Michael addition acceptors for chemically tuning the potency against EGFRBioorganic & medicinal chemistry, , 10-01, Volume: 28, Issue:19, 2020
Design, Synthesis, and Biological Evaluation of Pyrimido[4,5- d]pyrimidine-2,4(1 H,3 H)-diones as Potent and Selective Epidermal Growth Factor Receptor (EGFR) Inhibitors against L858R/T790M Resistance Mutation.Journal of medicinal chemistry, , 07-12, Volume: 61, Issue:13, 2018
A structure-guided optimization of pyrido[2,3-d]pyrimidin-7-ones as selective inhibitors of EGFREuropean journal of medicinal chemistry, , Jan-27, Volume: 126, 2017
Synthesis and biological evaluation of morpholine-substituted diphenylpyrimidine derivatives (Mor-DPPYs) as potent EGFR T790M inhibitors with improved activity toward the gefitinib-resistant non-small cell lung cancers (NSCLC).European journal of medicinal chemistry, , Jun-16, Volume: 133, 2017
Discovery of N-((3R,4R)-4-Fluoro-1-(6-((3-methoxy-1-methyl-1H-pyrazol-4-yl)amino)-9-methyl-9H-purin-2-yl)pyrrolidine-3-yl)acrylamide (PF-06747775) through Structure-Based Drug Design: A High Affinity Irreversible Inhibitor Targeting Oncogenic EGFR MutantsJournal of medicinal chemistry, , 04-13, Volume: 60, Issue:7, 2017
C-2 (E)-4-(Styryl)aniline substituted diphenylpyrimidine derivatives (Sty-DPPYs) as specific kinase inhibitors targeting clinical resistance related EGFRBioorganic & medicinal chemistry, , 05-15, Volume: 25, Issue:10, 2017
Covalent Modifiers: A Chemical Perspective on the Reactivity of α,β-Unsaturated Carbonyls with Thiols via Hetero-Michael Addition Reactions.Journal of medicinal chemistry, , 02-09, Volume: 60, Issue:3, 2017
Structure-Guided Development of Covalent and Mutant-Selective Pyrazolopyrimidines to Target T790M Drug Resistance in Epidermal Growth Factor Receptor.Journal of medicinal chemistry, , 09-28, Volume: 60, Issue:18, 2017
Indazole-Based Covalent Inhibitors To Target Drug-Resistant Epidermal Growth Factor Receptor.Journal of medicinal chemistry, , 03-23, Volume: 60, Issue:6, 2017
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Synthesis and biological evaluation of azole-diphenylpyrimidine derivatives (AzDPPYs) as potent T790M mutant form of epidermal growth factor receptor inhibitors.Bioorganic & medicinal chemistry, , 11-01, Volume: 24, Issue:21, 2016
Discovery of (R,E)-N-(7-Chloro-1-(1-[4-(dimethylamino)but-2-enoyl]azepan-3-yl)-1H-benzo[d]imidazol-2-yl)-2-methylisonicotinamide (EGF816), a Novel, Potent, and WT Sparing Covalent Inhibitor of Oncogenic (L858R, ex19del) and Resistant (T790M) EGFR Mutants Journal of medicinal chemistry, , 07-28, Volume: 59, Issue:14, 2016
Recent progress on third generation covalent EGFR inhibitors.Bioorganic & medicinal chemistry letters, , Apr-15, Volume: 26, Issue:8, 2016
Discovery of 1-{(3R,4R)-3-[({5-Chloro-2-[(1-methyl-1H-pyrazol-4-yl)amino]-7H-pyrrolo[2,3-d]pyrimidin-4-yl}oxy)methyl]-4-methoxypyrrolidin-1-yl}prop-2-en-1-one (PF-06459988), a Potent, WT Sparing, Irreversible Inhibitor of T790M-Containing EGFR Mutants.Journal of medicinal chemistry, , Mar-10, Volume: 59, Issue:5, 2016
Targeting Drug Resistance in EGFR with Covalent Inhibitors: A Structure-Based Design Approach.Journal of medicinal chemistry, , Sep-10, Volume: 58, Issue:17, 2015
Identification and anti-tumor evaluation of 3-acyl-indol-based 2,4-diarylaminopyrimidine analogues as potent ALK inhibitors capable of overcoming drug-resistant mutants.European journal of medicinal chemistry, , Aug-05, Volume: 238, 2022
[no title available]European journal of medicinal chemistry, , Nov-05, Volume: 241, 2022
[no title available]European journal of medicinal chemistry, , Mar-15, Volume: 214, 2021
Discovery and antitumor activity of Benzo[d]imidazol-containing 2,4-diarylaminopyrimidine analogues as ALK inhibitors with mutation-combating effects.Bioorganic & medicinal chemistry, , 05-01, Volume: 37, 2021
An exploration of solvent-front region high affinity moiety leading to novel potent ALK & ROS1 dual inhibitors with mutant-combating effects.Bioorganic & medicinal chemistry, , 10-15, Volume: 27, Issue:20, 2019
Discovery of novel mutant-combating ALK and ROS1 dual inhibitors bearing imidazolidin-2-one moiety with reasonable PK properties.European journal of medicinal chemistry, , Jun-01, Volume: 171, 2019
Discovery of novel 2,4-diarylaminopyrimidine analogues as ALK and ROS1 dual inhibitors to overcome crizotinib-resistant mutants including G1202R.European journal of medicinal chemistry, , Jan-01, Volume: 143, 2018
Recent Progress of Small-Molecule Epidermal Growth Factor Receptor (EGFR) Inhibitors against C797S Resistance in Non-Small-Cell Lung Cancer.Journal of medicinal chemistry, , 05-24, Volume: 61, Issue:10, 2018
[no title available]European journal of medicinal chemistry, , Oct-05, Volume: 158, 2018
Discovery of a potent dual ALK and EGFR T790M inhibitor.European journal of medicinal chemistry, , Aug-18, Volume: 136, 2017
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Design, synthesis and biological evaluation of novel 4-arylaminopyrimidine derivatives possessing a hydrazone moiety as dual inhibitors of L1196M ALK and ROS1.European journal of medicinal chemistry, , Nov-10, Volume: 123, 2016
Synthesis, structure-activity relationships, and in vivo efficacy of the novel potent and selective anaplastic lymphoma kinase (ALK) inhibitor 5-chloro-N2-(2-isopropoxy-5-methyl-4-(piperidin-4-yl)phenyl)-N4-(2-(isopropylsulfonyl)phenyl)pyrimidine-2,4-diamJournal of medicinal chemistry, , Jul-25, Volume: 56, Issue:14, 2013
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Optimization of a novel piperazinone series as potent selective peripheral covalent BTK inhibitors.Bioorganic & medicinal chemistry letters, , 03-15, Volume: 60, 2022
Discovery of 1-Amino-1Journal of medicinal chemistry, , 11-11, Volume: 64, Issue:21, 2021
Discovery of LOU064 (Remibrutinib), a Potent and Highly Selective Covalent Inhibitor of Bruton's Tyrosine Kinase.Journal of medicinal chemistry, , 05-28, Volume: 63, Issue:10, 2020
Discovery of quinoline-based irreversible BTK inhibitors.Bioorganic & medicinal chemistry letters, , 07-15, Volume: 30, Issue:14, 2020
Discovery of 4-Aminoquinoline-3-carboxamide Derivatives as Potent Reversible Bruton's Tyrosine Kinase Inhibitors for the Treatment of Rheumatoid Arthritis.Journal of medicinal chemistry, , 07-25, Volume: 62, Issue:14, 2019
Discovery and structural optimization of potent epidermal growth factor receptor (EGFR) inhibitors against L858R/T790M/C797S resistance mutation for lung cancer treatment.European journal of medicinal chemistry, , Jul-05, Volume: 237, 2022
[no title available]Journal of medicinal chemistry, , 05-12, Volume: 65, Issue:9, 2022
Discovery of Potent PROTACs Targeting EGFR Mutants through the Optimization of Covalent EGFR Ligands.Journal of medicinal chemistry, , 03-24, Volume: 65, Issue:6, 2022
Design of a "Two-in-One" Mutant-Selective Epidermal Growth Factor Receptor Inhibitor That Spans the Orthosteric and Allosteric Sites.Journal of medicinal chemistry, , 01-27, Volume: 65, Issue:2, 2022
Macrocyclization of Quinazoline-Based EGFR Inhibitors Leads to Exclusive Mutant Selectivity for EGFR L858R and Del19.Journal of medicinal chemistry, , 12-08, Volume: 65, Issue:23, 2022
[no title available]European journal of medicinal chemistry, , Aug-05, Volume: 238, 2022
Development of Dual Inhibitors Targeting Epidermal Growth Factor Receptor in Cancer Therapy.Journal of medicinal chemistry, , 04-14, Volume: 65, Issue:7, 2022
The Ascension of Targeted Covalent Inhibitors.Journal of medicinal chemistry, , 04-28, Volume: 65, Issue:8, 2022
Structural Basis for Inhibition of Mutant EGFR with Lazertinib (YH25448).ACS medicinal chemistry letters, , Dec-08, Volume: 13, Issue:12, 2022
Discovery of Novel Allosteric EGFR L858R Inhibitors for the Treatment of Non-Small-Cell Lung Cancer as a Single Agent or in Combination with Osimertinib.Journal of medicinal chemistry, , 10-13, Volume: 65, Issue:19, 2022
Advanced approaches of developing targeted covalent drugs.RSC medicinal chemistry, , Dec-14, Volume: 13, Issue:12, 2022
[no title available]Bioorganic & medicinal chemistry, , Nov-15, Volume: 74, 2022
[no title available]European journal of medicinal chemistry, , Jan-15, Volume: 228, 2022
Optimization of Brigatinib as New Wild-Type Sparing Inhibitors of EGFRACS medicinal chemistry letters, , Feb-10, Volume: 13, Issue:2, 2022
Design, synthesis and evaluation of novel ErbB/HDAC multitargeted inhibitors with selectivity in EGFREuropean journal of medicinal chemistry, , Mar-05, Volume: 213, 2021
Discovery of Dosimertinib, a Highly Potent, Selective, and Orally Efficacious Deuterated EGFR Targeting Clinical Candidate for the Treatment of Non-Small-Cell Lung Cancer.Journal of medicinal chemistry, , 01-28, Volume: 64, Issue:2, 2021
Structural modifications on indole and pyrimidine rings of osimertinib lead to high selectivity towards L858R/T790M double mutant enzyme and potent antitumor activity.Bioorganic & medicinal chemistry, , 04-15, Volume: 36, 2021
[no title available]European journal of medicinal chemistry, , Dec-05, Volume: 225, 2021
Design, synthesis and assessment of new series of quinazolinone derivatives as EGFR inhibitors along with their cytotoxic evaluation against MCF7 and A549 cancer cell lines.Bioorganic & medicinal chemistry letters, , 06-01, Volume: 41, 2021
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]European journal of medicinal chemistry, , Nov-05, Volume: 223, 2021
Design, synthesis and biological evaluation of sulfamoylphenyl-quinazoline derivatives as potential EGFR/CAIX dual inhibitors.European journal of medicinal chemistry, , Apr-15, Volume: 216, 2021
Comprehensive review for anticancer hybridized multitargeting HDAC inhibitors.European journal of medicinal chemistry, , Jan-01, Volume: 209, 2021
Design, synthesis and biological evaluation of aminopyrimidine derivatives bearing a 4,5,6,7-tetrahydrothieno [3,2-c]pyridine as potent EGFR inhibitors.European journal of medicinal chemistry, , Dec-15, Volume: 226, 2021
Discovery and optimization of covalent EGFR T790M/L858R mutant inhibitors.Bioorganic & medicinal chemistry letters, , 11-15, Volume: 52, 2021
Medicinal Chemistry Strategies for the Development of Kinase Inhibitors Targeting Point Mutations.Journal of medicinal chemistry, , 10-08, Volume: 63, Issue:19, 2020
Discovery of new thieno[3,2-d]pyrimidine derivatives targeting EGFREuropean journal of medicinal chemistry, , Aug-01, Volume: 199, 2020
Design, synthesis, biological evaluation, QSAR analysis and molecular modelling of new thiazol-benzimidazoles as EGFR inhibitors.Bioorganic & medicinal chemistry, , 09-15, Volume: 28, Issue:18, 2020
Design and synthesis of selective degraders of EGFREuropean journal of medicinal chemistry, , Apr-15, Volume: 192, 2020
Synthesis and cytotoxic evaluation of halogenated α-exo-methylene-lactones.Bioorganic & medicinal chemistry, , 02-01, Volume: 28, Issue:3, 2020
[no title available]Bioorganic & medicinal chemistry letters, , 08-15, Volume: 30, Issue:16, 2020
Design, synthesis and biological evaluation of 2-amino-4-(1,2,4-triazol)pyridine derivatives as potent EGFR inhibitors to overcome TKI-resistance.European journal of medicinal chemistry, , Feb-01, Volume: 187, 2020
Design, synthesis and biological evaluation of 4-aniline quinazoline derivatives conjugated with hydrogen sulfide (HEuropean journal of medicinal chemistry, , Sep-15, Volume: 202, 2020
Targeting Her2-insYVMA with Covalent Inhibitors-A Focused Compound Screening and Structure-Based Design Approach.Journal of medicinal chemistry, , 10-22, Volume: 63, Issue:20, 2020
Design, synthesis and 3D-QSAR analysis of novel thiopyranopyrimidine derivatives as potential antitumor agents inhibiting A549 and Hela cancer cells.European journal of medicinal chemistry, , Jan-01, Volume: 185, 2020
[no title available]European journal of medicinal chemistry, , Jan-15, Volume: 186, 2020
Lead generation of 1,2-dithiolanes as exon 19 and exon 21 mutant EGFR tyrosine kinase inhibitors.Bioorganic & medicinal chemistry letters, , 06-15, Volume: 29, Issue:12, 2019
Design, synthesis and biological evaluation of AZD9291 derivatives as selective and potent EGFREuropean journal of medicinal chemistry, , Feb-01, Volume: 163, 2019
[no title available]European journal of medicinal chemistry, , Dec-01, Volume: 183, 2019
Discovery of an Oleanolic Acid/Hederagenin-Nitric Oxide Donor Hybrid as an EGFR Tyrosine Kinase Inhibitor for Non-Small-Cell Lung Cancer.Journal of natural products, , 11-22, Volume: 82, Issue:11, 2019
Discovery of a Furanopyrimidine-Based Epidermal Growth Factor Receptor Inhibitor (DBPR112) as a Clinical Candidate for the Treatment of Non-Small Cell Lung Cancer.Journal of medicinal chemistry, , 11-27, Volume: 62, Issue:22, 2019
Discovery of selective EGFR modulator to inhibit L858R/T790M double mutants bearing a N-9-Diphenyl-9H-purin-2-amine scaffold.Bioorganic & medicinal chemistry, , 05-01, Volume: 26, Issue:8, 2018
[no title available]Bioorganic & medicinal chemistry letters, , 04-15, Volume: 28, Issue:7, 2018
[no title available]European journal of medicinal chemistry, , May-25, Volume: 152, 2018
Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors.Bioorganic & medicinal chemistry, , 05-01, Volume: 26, Issue:8, 2018
The synthesis of 4-arylamido-2-arylaminoprimidines as potent EGFR T790M/L858R inhibitors for NSCLC.Bioorganic & medicinal chemistry, , 12-15, Volume: 26, Issue:23-24, 2018
Synthesis and biological evaluation of irreversible EGFR tyrosine kinase inhibitors containing pyrido[3,4-d]pyrimidine scaffold.Bioorganic & medicinal chemistry, , 07-23, Volume: 26, Issue:12, 2018
[no title available]ACS medicinal chemistry letters, , Nov-08, Volume: 9, Issue:11, 2018
[no title available]MedChemComm, , Feb-01, Volume: 9, Issue:2, 2018
Discovery of 2,4,6-trisubstitued pyrido[3,4-d]pyrimidine derivatives as new EGFR-TKIs.European journal of medicinal chemistry, , Mar-25, Volume: 148, 2018
Design, synthesis and evaluation of the osimertinib analogue (C-005) as potent EGFR inhibitor against NSCLC.Bioorganic & medicinal chemistry, , 12-15, Volume: 26, Issue:23-24, 2018
Synthesis and evaluation of 2,9-disubstituted 8-phenylthio/phenylsulfinyl-9H-purine as new EGFR inhibitors.Bioorganic & medicinal chemistry, , 05-01, Volume: 26, Issue:8, 2018
Covalent Modifiers: A Chemical Perspective on the Reactivity of α,β-Unsaturated Carbonyls with Thiols via Hetero-Michael Addition Reactions.Journal of medicinal chemistry, , 02-09, Volume: 60, Issue:3, 2017
A structure-guided optimization of pyrido[2,3-d]pyrimidin-7-ones as selective inhibitors of EGFREuropean journal of medicinal chemistry, , Jan-27, Volume: 126, 2017
Design, synthesis and biological evaluation of WZ4002 analogues as EGFR inhibitors.Bioorganic & medicinal chemistry letters, , 11-01, Volume: 27, Issue:21, 2017
Synthesis and evaluation of osimertinib derivatives as potent EGFR inhibitors.Bioorganic & medicinal chemistry, , 09-01, Volume: 25, Issue:17, 2017
Discovery of a potent dual ALK and EGFR T790M inhibitor.European journal of medicinal chemistry, , Aug-18, Volume: 136, 2017
Design, synthesis, SAR discussion, in vitro and in vivo evaluation of novel selective EGFR modulator to inhibit L858R/T790M double mutants.European journal of medicinal chemistry, , Jul-28, Volume: 135, 2017
Trisubstituted Imidazoles with a Rigidized Hinge Binding Motif Act As Single Digit nM Inhibitors of Clinically Relevant EGFR L858R/T790M and L858R/T790M/C797S Mutants: An Example of Target Hopping.Journal of medicinal chemistry, , 06-08, Volume: 60, Issue:11, 2017
Discovery of (R)-1-(3-(4-Amino-3-(3-chloro-4-(pyridin-2-ylmethoxy)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)prop-2-en-1-one (CHMFL-EGFR-202) as a Novel Irreversible EGFR Mutant Kinase Inhibitor with a Distinct Binding Mode.Journal of medicinal chemistry, , 04-13, Volume: 60, Issue:7, 2017
Structure-Guided Development of Covalent and Mutant-Selective Pyrazolopyrimidines to Target T790M Drug Resistance in Epidermal Growth Factor Receptor.Journal of medicinal chemistry, , 09-28, Volume: 60, Issue:18, 2017
Trisubstituted Pyridinylimidazoles as Potent Inhibitors of the Clinically Resistant L858R/T790M/C797S EGFR Mutant: Targeting of Both Hydrophobic Regions and the Phosphate Binding Site.Journal of medicinal chemistry, , 07-13, Volume: 60, Issue:13, 2017
Indazole-Based Covalent Inhibitors To Target Drug-Resistant Epidermal Growth Factor Receptor.Journal of medicinal chemistry, , 03-23, Volume: 60, Issue:6, 2017
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Discovery of 5-(methylthio)pyrimidine derivatives as L858R/T790M mutant selective epidermal growth factor receptor (EGFR) inhibitors.Bioorganic & medicinal chemistry, , 06-15, Volume: 24, Issue:12, 2016
Discovery of (R,E)-N-(7-Chloro-1-(1-[4-(dimethylamino)but-2-enoyl]azepan-3-yl)-1H-benzo[d]imidazol-2-yl)-2-methylisonicotinamide (EGF816), a Novel, Potent, and WT Sparing Covalent Inhibitor of Oncogenic (L858R, ex19del) and Resistant (T790M) EGFR Mutants Journal of medicinal chemistry, , 07-28, Volume: 59, Issue:14, 2016
Recent progress on third generation covalent EGFR inhibitors.Bioorganic & medicinal chemistry letters, , Apr-15, Volume: 26, Issue:8, 2016
Discovery of 1-{(3R,4R)-3-[({5-Chloro-2-[(1-methyl-1H-pyrazol-4-yl)amino]-7H-pyrrolo[2,3-d]pyrimidin-4-yl}oxy)methyl]-4-methoxypyrrolidin-1-yl}prop-2-en-1-one (PF-06459988), a Potent, WT Sparing, Irreversible Inhibitor of T790M-Containing EGFR Mutants.Journal of medicinal chemistry, , Mar-10, Volume: 59, Issue:5, 2016
4-Aminoindazolyl-dihydrofuro[3,4-d]pyrimidines as non-covalent inhibitors of mutant epidermal growth factor receptor tyrosine kinase.Bioorganic & medicinal chemistry letters, , Jan-15, Volume: 26, Issue:2, 2016
Discovery of a potent and selective EGFR inhibitor (AZD9291) of both sensitizing and T790M resistance mutations that spares the wild type form of the receptor.Journal of medicinal chemistry, , Oct-23, Volume: 57, Issue:20, 2014
Acrylamide Functional Group Incorporation Improves Drug-like Properties: An Example with EGFR Inhibitors.ACS medicinal chemistry letters, , Jan-10, Volume: 10, Issue:1, 2019
Discovery and Evaluation of Clinical Candidate AZD3759, a Potent, Oral Active, Central Nervous System-Penetrant, Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor.Journal of medicinal chemistry, , Oct-22, Volume: 58, Issue:20, 2015
Discovery of Potent PROTACs Targeting EGFR Mutants through the Optimization of Covalent EGFR Ligands.Journal of medicinal chemistry, , 03-24, Volume: 65, Issue:6, 2022
Exploring Degradation of Mutant and Wild-Type Epidermal Growth Factor Receptors Induced by Proteolysis-Targeting Chimeras.Journal of medicinal chemistry, , 06-23, Volume: 65, Issue:12, 2022
VHL-based PROTACs as potential therapeutic agents: Recent progress and perspectives.European journal of medicinal chemistry, , Jan-05, Volume: 227, 2022
Discovery of potent small molecule PROTACs targeting mutant EGFR.European journal of medicinal chemistry, , Dec-15, Volume: 208, 2020
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
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 24 target(s):
| Target | Category | Definition |
|---|
| virus receptor activity | molecular function | Combining with a virus component and mediating entry of the virus into the cell. [GOC:bf, GOC:dph, PMID:7621403, UniProtKB-KW:KW-1183] |
| chromatin binding | molecular function | Binding to chromatin, the network of fibers of DNA, protein, and sometimes RNA, that make up the chromosomes of the eukaryotic nucleus during interphase. [GOC:jl, ISBN:0198506732, PMID:20404130] |
| double-stranded DNA binding | molecular function | Binding to double-stranded DNA. [GOC:elh, GOC:vw] |
| MAP kinase kinase kinase activity | molecular function | Catalysis of the phosphorylation and activation of a MAP kinase kinase; each MAP kinase kinase can be phosphorylated by any of several MAP kinase kinase kinases. [PMID:9561267] |
| 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] |
| transmembrane signaling receptor activity | molecular function | Combining with an extracellular or intracellular signal and transmitting the signal from one side of the membrane to the other to initiate a change in cell activity or state as part of signal transduction. [GOC:go_curators, Wikipedia:Transmembrane_receptor] |
| epidermal growth factor receptor activity | molecular function | Combining with an epidermal growth factor receptor ligand and transmitting the signal across the plasma membrane to initiate a change in cell activity. [GOC:bf] |
| integrin binding | molecular function | Binding to an integrin. [GOC:ceb] |
| protein binding | molecular function | Binding to a protein. [GOC:go_curators] |
| calmodulin binding | molecular function | Binding to calmodulin, a calcium-binding protein with many roles, both in the calcium-bound and calcium-free states. [GOC:krc] |
| ATP binding | molecular function | Binding to ATP, adenosine 5'-triphosphate, a universally important coenzyme and enzyme regulator. [ISBN:0198506732] |
| enzyme binding | molecular function | Binding to an enzyme, a protein with catalytic activity. [GOC:jl] |
| kinase binding | molecular function | Binding to a kinase, any enzyme that catalyzes the transfer of a phosphate group. [GOC:jl] |
| protein kinase binding | molecular function | Binding to a protein kinase, any enzyme that catalyzes the transfer of a phosphate group, usually from ATP, to a protein substrate. [GOC:jl] |
| protein phosphatase binding | molecular function | Binding to a protein phosphatase. [GOC:jl] |
| protein tyrosine kinase activator activity | molecular function | Increases the activity of a protein tyrosine kinase, an enzyme which phosphorylates a tyrosyl phenolic group on a protein. [GOC:ai, ISBN:0198506732] |
| transmembrane receptor protein tyrosine kinase activator activity | molecular function | Binds to and increases the activity of a transmembrane receptor protein tyrosine kinase. [GOC:mah] |
| ubiquitin protein ligase binding | molecular function | Binding to a ubiquitin protein ligase enzyme, any of the E3 proteins. [GOC:vp] |
| 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] |
| actin filament binding | molecular function | Binding to an actin filament, also known as F-actin, a helical filamentous polymer of globular G-actin subunits. [ISBN:0198506732] |
| ATPase binding | molecular function | Binding to an ATPase, any enzyme that catalyzes the hydrolysis of ATP. [GOC:ai] |
| epidermal growth factor binding | molecular function | Binding to epidermal growth factor. [GOC:dgh] |
Located In
This protein is located in 21 target(s):
| Target | Category | Definition |
|---|
| Golgi membrane | cellular component | The lipid bilayer surrounding any of the compartments of the Golgi apparatus. [GOC:mah] |
| extracellular space | cellular component | That part of a multicellular organism outside the cells proper, usually taken to be outside the plasma membranes, and occupied by fluid. [ISBN:0198547684] |
| 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] |
| cytoplasm | cellular component | The contents of a cell excluding the plasma membrane and nucleus, but including other subcellular structures. [ISBN:0198547684] |
| endosome | cellular component | A vacuole to which materials ingested by endocytosis are delivered. [ISBN:0198506732, PMID:19696797] |
| endoplasmic reticulum membrane | cellular component | The lipid bilayer surrounding the endoplasmic reticulum. [GOC:mah] |
| 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] |
| focal adhesion | cellular component | A cell-substrate junction that anchors the cell to the extracellular matrix and that forms a point of termination of actin filaments. In insects focal adhesion has also been referred to as hemi-adherens junction (HAJ). [GOC:aruk, GOC:bc, ISBN:0124325653, ISBN:0815316208, PMID:10419689, PMID:12191915, PMID:15246682, PMID:1643657, PMID:16805308, PMID:19197329, PMID:23033047, PMID:26923917, PMID:28796323, PMID:8314002] |
| cell surface | cellular component | The external part of the cell wall and/or plasma membrane. [GOC:jl, GOC:mtg_sensu, GOC:sm] |
| endosome membrane | cellular component | The lipid bilayer surrounding an endosome. [GOC:mah] |
| membrane | cellular component | A lipid bilayer along with all the proteins and protein complexes embedded in it and attached to it. [GOC:dos, GOC:mah, ISBN:0815316194] |
| basolateral plasma membrane | cellular component | The region of the plasma membrane that includes the basal end and sides of the cell. Often used in reference to animal polarized epithelial membranes, where the basal membrane is the part attached to the extracellular matrix, or in plant cells, where the basal membrane is defined with respect to the zygotic axis. [GOC:go_curators] |
| apical plasma membrane | cellular component | The region of the plasma membrane located at the apical end of the cell. [GOC:curators] |
| 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] |
| clathrin-coated endocytic vesicle membrane | cellular component | The lipid bilayer surrounding a clathrin-coated endocytic vesicle. [GOC:mah] |
| early endosome membrane | cellular component | The lipid bilayer surrounding an early endosome. [GOC:pz] |
| nuclear membrane | cellular component | Either of the lipid bilayers that surround the nucleus and form the nuclear envelope; excludes the intermembrane space. [GOC:mah, GOC:pz] |
| 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] |
| perinuclear region of cytoplasm | cellular component | Cytoplasm situated near, or occurring around, the nucleus. [GOC:jid] |
| multivesicular body, internal vesicle lumen | cellular component | The volume enclosed by the membrane of the multivesicular body internal vesicle. [GOC:pde, PMID:21183070] |
| intracellular vesicle | cellular component | Any vesicle that is part of the intracellular region. [GOC:vesicles] |
Active In
This protein is active in 3 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] |
| ruffle membrane | cellular component | The portion of the plasma membrane surrounding a ruffle. [GOC:mah] |
| basal plasma membrane | cellular component | The region of the plasma membrane located at the basal end of the cell. Often used in reference to animal polarized epithelial membranes, where the basal membrane is the part attached to the extracellular matrix, or in plant cells, where the basal membrane is defined with respect to the zygotic axis. [GOC:go_curators] |
Part Of
This protein is part of 3 target(s):
| Target | Category | Definition |
|---|
| protein-containing complex | cellular component | A stable assembly of two or more macromolecules, i.e. proteins, nucleic acids, carbohydrates or lipids, in which at least one component is a protein and the constituent parts function together. [GOC:dos, GOC:mah] |
| 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] |
| Shc-EGFR complex | cellular component | A protein complex that contains the epidermal growth factor receptor (EGFR) and the adaptor protein Shc, and is involved in linking EGFR activation to the p21-Ras pathway. [GOC:mah, PMID:7798267] |
Involved In
This protein is involved in 88 target(s):
| Target | Category | Definition |
|---|
| MAPK cascade | biological process | An intracellular protein kinase cascade containing at least a MAP kinase (MAPK). It starts with the activation of a MAP3K, and the consecutive activation of a MPK2K and a MAPK. The cascade can also contain an additional tier: the upstream MAP4K. The kinases in each tier phosphorylate and activate the kinase in the downstream tier to transmit a signal within a cell. [PMID:20811974, PMID:9561267] |
| ossification | biological process | The formation of bone or of a bony substance, or the conversion of fibrous tissue or of cartilage into bone or a bony substance. [GOC:mtg_mpo, PMID:17572649] |
| embryonic placenta development | biological process | The embryonically driven process whose specific outcome is the progression of the placenta over time, from its formation to the mature structure. The placenta is an organ of metabolic interchange between fetus and mother, partly of embryonic origin and partly of maternal origin. [GOC:add, ISBN:068340007X] |
| 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] |
| hair follicle development | biological process | The process whose specific outcome is the progression of the hair follicle over time, from its formation to the mature structure. A hair follicle is a tube-like opening in the epidermis where the hair shaft develops and into which the sebaceous glands open. [GOC:dph, UBERON:0002073] |
| translation | biological process | The cellular metabolic process in which a protein is formed, using the sequence of a mature mRNA or circRNA molecule to specify the sequence of amino acids in a polypeptide chain. Translation is mediated by the ribosome, and begins with the formation of a ternary complex between aminoacylated initiator methionine tRNA, GTP, and initiation factor 2, which subsequently associates with the small subunit of the ribosome and an mRNA or circRNA. Translation ends with the release of a polypeptide chain from the ribosome. [GOC:go_curators] |
| signal transduction | biological process | The cellular process in which a signal is conveyed to trigger a change in the activity or state of a cell. Signal transduction begins with reception of a signal (e.g. a ligand binding to a receptor or receptor activation by a stimulus such as light), or for signal transduction in the absence of ligand, signal-withdrawal or the activity of a constitutively active receptor. Signal transduction ends with regulation of a downstream cellular process, e.g. regulation of transcription or regulation of a metabolic process. Signal transduction covers signaling from receptors located on the surface of the cell and signaling via molecules located within the cell. For signaling between cells, signal transduction is restricted to events at and within the receiving cell. [GOC:go_curators, GOC:mtg_signaling_feb11] |
| epidermal growth factor receptor signaling pathway | biological process | The series of molecular signals initiated by binding of a ligand to the tyrosine kinase receptor EGFR (ERBB1) on the surface of a cell. The pathway ends with regulation of a downstream cellular process, e.g. transcription. [GOC:ceb] |
| activation of phospholipase C activity | biological process | The initiation of the activity of the inactive enzyme phospolipase C as the result of The series of molecular signals generated as a consequence of a G protein-coupled receptor binding to its physiological ligand. [GOC:dph, GOC:mah, GOC:tb, PMID:8280098] |
| salivary gland morphogenesis | biological process | The process in which the anatomical structures of the salivary gland are generated and organized. [GOC:jid] |
| midgut development | biological process | The process whose specific outcome is the progression of the midgut over time, from its formation to the mature structure. The midgut is the middle part of the alimentary canal from the stomach, or entrance of the bile duct, to, or including, the large intestine. [GOC:jid, UBERON:0001045] |
| learning or memory | biological process | The acquisition and processing of information and/or the storage and retrieval of this information over time. [GOC:jid, PMID:8938125] |
| circadian rhythm | biological process | Any biological process in an organism that recurs with a regularity of approximately 24 hours. [GOC:bf, GOC:go_curators] |
| positive regulation of cell population proliferation | biological process | Any process that activates or increases the rate or extent of cell proliferation. [GOC:go_curators] |
| diterpenoid metabolic process | biological process | The chemical reactions and pathways involving diterpenoid compounds, terpenoids with four isoprene units. [ISBN:0198547684] |
| peptidyl-tyrosine phosphorylation | biological process | The phosphorylation of peptidyl-tyrosine to form peptidyl-O4'-phospho-L-tyrosine. [RESID:AA0039] |
| cerebral cortex cell migration | biological process | The orderly movement of cells from one site to another in the cerebral cortex. [GO_REF:0000021, GOC:cls, GOC:dgh, GOC:dph, GOC:jid] |
| positive regulation of cell growth | biological process | Any process that activates or increases the frequency, rate, extent or direction of cell growth. [GOC:go_curators] |
| lung development | biological process | The process whose specific outcome is the progression of the lung over time, from its formation to the mature structure. In all air-breathing vertebrates the lungs are developed from the ventral wall of the oesophagus as a pouch which divides into two sacs. In amphibians and many reptiles the lungs retain very nearly this primitive sac-like character, but in the higher forms the connection with the esophagus becomes elongated into the windpipe and the inner walls of the sacs become more and more divided, until, in the mammals, the air spaces become minutely divided into tubes ending in small air cells, in the walls of which the blood circulates in a fine network of capillaries. In mammals the lungs are more or less divided into lobes, and each lung occupies a separate cavity in the thorax. [GOC:jid, UBERON:0002048] |
| 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 superoxide anion generation | biological process | Any process that activates or increases the frequency, rate or extent of enzymatic generation of superoxide by a cell. [GOC:mah] |
| positive regulation of peptidyl-serine phosphorylation | biological process | Any process that activates or increases the frequency, rate or extent of the phosphorylation of peptidyl-serine. [GOC:mah] |
| response to cobalamin | biological process | Any process that results in a change in state or activity of a cell or an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a cobalamin (vitamin B12) stimulus. [GOC:sl] |
| response to hydroxyisoflavone | biological process | Any process that results in a change in state or activity of a cell or an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a hydroxyisoflavone stimulus. [GOC:mah] |
| cellular response to reactive oxygen species | 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 reactive oxygen species stimulus. Reactive oxygen species include singlet oxygen, superoxide, and oxygen free radicals. [GOC:mah] |
| 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] |
| ERBB2-EGFR signaling pathway | biological process | The series of molecular signals initiated by binding of a ligand to an epidermal growth factor receptor (EGFR/ERBB1) on the surface of a cell, followed by transmission of the signal by a heterodimeric complex of ERBB2 and EGFR. ERBB2, which does not bind any known ligand, is activated through formation of a heterodimer with another ligand-activated ERBB family member such as EGFR. [GOC:signaling, PMID:16460914, Reactome:R-HSA-1963589] |
| negative regulation of epidermal growth factor receptor signaling pathway | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of epidermal growth factor receptor signaling pathway activity. [GOC:go_curators] |
| negative regulation of protein catabolic process | biological process | Any process that stops, prevents or reduces the frequency, rate or extent of protein catabolic process. [GO_REF:0000058, GOC:kmv, GOC:obol, GOC:TermGenie, PMID:24785082] |
| vasodilation | biological process | An increase in the internal diameter of blood vessels, especially arterioles or capillaries, due to relaxation of smooth muscle cells that line the vessels, and usually resulting in a decrease in blood pressure. [GOC:pr, ISBN:0192800981] |
| positive regulation of phosphorylation | biological process | Any process that activates or increases the frequency, rate or extent of addition of phosphate groups to a molecule. [GOC:jl] |
| ovulation cycle | biological process | The type of sexual cycle seen in females, often with physiologic changes in the endometrium that recur at regular intervals during the reproductive years. [ISBN:0721662544] |
| hydrogen peroxide metabolic process | biological process | The chemical reactions and pathways involving hydrogen peroxide (H2O2), a potentially harmful byproduct of aerobic cellular respiration which can cause damage to DNA. [GOC:jl, PMID:21734470] |
| negative regulation of apoptotic process | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of cell death by apoptotic process. [GOC:jl, GOC:mtg_apoptosis] |
| positive regulation of MAP kinase activity | biological process | Any process that activates or increases the frequency, rate or extent of MAP kinase activity. [GOC:dph, GOC:go_curators] |
| tongue development | biological process | The process whose specific outcome is the progression of the tongue over time, from its formation to the mature structure. The tongue is the movable, muscular organ on the floor of the mouth of most vertebrates, in many other mammals is the principal organ of taste, aids in the prehension of food, in swallowing, and in modifying the voice as in speech. [GOC:jl, UBERON:0001723] |
| positive regulation of cyclin-dependent protein serine/threonine kinase activity | biological process | Any process that activates or increases the frequency, rate or extent of CDK activity. [GOC:go_curators, GOC:pr] |
| positive regulation of DNA repair | biological process | Any process that activates or increases the frequency, rate or extent of DNA repair. [GOC:go_curators] |
| positive regulation of DNA replication | biological process | Any process that activates or increases the frequency, rate or extent of DNA replication. [GOC:go_curators] |
| positive regulation of bone resorption | biological process | Any process that activates or increases the frequency, rate or extent of bone resorption. [GOC:go_curators] |
| positive regulation of DNA-templated transcription | biological process | Any process that activates or increases the frequency, rate or extent of cellular DNA-templated transcription. [GOC:go_curators, GOC:txnOH] |
| positive regulation of vasoconstriction | biological process | Any process that activates or increases the frequency, rate or extent of vasoconstriction. [GOC:go_curators] |
| negative regulation of mitotic cell cycle | biological process | Any process that stops, prevents or reduces the rate or extent of progression through the mitotic cell cycle. [GOC:dph, GOC:go_curators, GOC:tb] |
| positive regulation of transcription by RNA polymerase II | biological process | Any process that activates or increases the frequency, rate or extent of transcription from an RNA polymerase II promoter. [GOC:go_curators, GOC:txnOH] |
| regulation of JNK cascade | biological process | Any process that modulates the frequency, rate or extent of signal transduction mediated by the JNK cascade. [GOC:bf] |
| symbiont entry into host cell | biological process | The process by which a symbiont breaches the plasma membrane or cell envelope and enters the host cell. The process ends when the symbiont or its genome is released into the host cell. [GOC:jl] |
| 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] |
| astrocyte activation | biological process | A change in morphology and behavior of an astrocyte resulting from exposure to a cytokine, chemokine, cellular ligand, or soluble factor. [GOC:mgi_curators, PMID:10526094, PMID:10695728, PMID:12529254, PMID:12580336, PMID:9585813] |
| positive regulation of fibroblast proliferation | biological process | Any process that activates or increases the frequency, rate or extent of multiplication or reproduction of fibroblast cells. [GOC:jid] |
| digestive tract morphogenesis | biological process | The process in which the anatomical structures of the digestive tract are generated and organized. The digestive tract is the anatomical structure through which food passes and is processed. [GOC:dph, GOC:go_curators, PMID:12618131] |
| positive regulation of smooth muscle cell proliferation | biological process | Any process that activates or increases the rate or extent of smooth muscle cell proliferation. [CL:0000192, GOC:ebc] |
| neuron projection morphogenesis | biological process | The process in which the anatomical structures of a neuron projection are generated and organized. A neuron projection is any process extending from a neural cell, such as axons or dendrites. [GOC:mah] |
| 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 epithelial cell proliferation | biological process | Any process that activates or increases the rate or extent of epithelial cell proliferation. [GOC:ai] |
| regulation of peptidyl-tyrosine phosphorylation | biological process | Any process that modulates the frequency, rate or extent of the phosphorylation of peptidyl-tyrosine. [GOC:ai] |
| protein insertion into membrane | biological process | The process that results in the incorporation of a protein into a biological membrane. Incorporation in this context means having some part or covalently attached group that is inserted into the the hydrophobic region of one or both bilayers. [GOC:ai] |
| response to calcium ion | biological process | Any process that results in a change in state or activity of a cell or an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a calcium ion stimulus. [GOC:ai] |
| regulation of phosphatidylinositol 3-kinase/protein kinase B signal transduction | biological process | Any process that modulates the frequency, rate or extent of phosphatidylinositol 3-kinase/protein kinase B signal transduction. [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] |
| positive regulation of synaptic transmission, glutamatergic | biological process | Any process that activates, maintains or increases the frequency, rate or extent of glutamatergic synaptic transmission, the process of communication from a neuron to another neuron across a synapse using the neurotransmitter glutamate. [GOC:ai] |
| positive regulation of glial cell proliferation | biological process | Any process that activates or increases the rate or extent of glial cell proliferation. [GOC:dph, GOC:sl, GOC:tb] |
| morphogenesis of an epithelial fold | biological process | The morphogenetic process in which an epithelial sheet bends along a linear axis. [GOC:dph] |
| eyelid development in camera-type eye | biological process | The progression of the eyelid in a camera-type eye from its formation to the mature state. The eyelid is a membranous cover that helps protect and lubricate the eye. [GOC:dph, GOC:yaf] |
| response to UV-A | biological process | Any process that results in a change in state or activity of a cell or an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a UV-A radiation stimulus. UV-A radiation (UV-A light) spans the wavelengths 315 to 400 nm. [GOC:BHF, GOC:mah] |
| positive regulation of mucus secretion | biological process | Any process that activates or increases the frequency, rate or extent of the regulated release of mucus from a cell or a tissue. [GOC:add] |
| regulation of ERK1 and ERK2 cascade | biological process | Any process that modulates the frequency, rate or extent of signal transduction mediated by the ERK1 and ERK2 cascade. [GOC:add, ISBN:0121245462, ISBN:0896039986] |
| 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] |
| cellular response to amino acid 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 an amino acid stimulus. An amino acid is a carboxylic acids containing one or more amino groups. [GOC:mah] |
| cellular response to mechanical 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 mechanical stimulus. [GOC:mah] |
| cellular response to cadmium ion | 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 cadmium (Cd) ion stimulus. [GOC:mah] |
| cellular response to epidermal 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 an epidermal growth factor stimulus. [GOC:mah] |
| cellular response to estradiol 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 stimulus by estradiol, a C18 steroid hormone hydroxylated at C3 and C17 that acts as a potent estrogen. [GOC:mah] |
| cellular response to xenobiotic 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 stimulus from a xenobiotic, a compound foreign to the organism exposed to it. It may be synthesized by another organism (like ampicilin) or it can be a synthetic chemical. [GOC:krc, GOC:mah] |
| cellular response to dexamethasone 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 dexamethasone stimulus. [GOC:mah, GOC:yaf] |
| positive regulation of canonical Wnt signaling pathway | biological process | Any process that increases the rate, frequency, or extent of the Wnt signaling pathway through beta-catenin, the series of molecular signals initiated by binding of a Wnt protein to a frizzled family receptor on the surface of the target cell, followed by propagation of the signal via beta-catenin, and ending with a change in transcription of target genes. [GOC:tb] |
| liver regeneration | biological process | The regrowth of lost or destroyed liver. [GOC:gap, PMID:19447520] |
| cell-cell adhesion | biological process | The attachment of one cell to another cell via adhesion molecules. [GOC:dos] |
| positive regulation of protein kinase C activity | biological process | Any process that activates or increases the frequency, rate or extent of protein kinase C activity. [GOC:signaling, GOC:TermGenie] |
| positive regulation of G1/S transition of mitotic cell cycle | biological process | Any signaling pathway that increases or activates a cell cycle cyclin-dependent protein kinase to modulate the switch from G1 phase to S phase of the mitotic cell cycle. [GOC:mtg_cell_cycle] |
| positive regulation of non-canonical NF-kappaB signal transduction | biological process | Any process that activates or increases the frequency, rate or extent of the non-canonical NF-kappaB cascade. [GOC:TermGenie] |
| positive regulation of prolactin secretion | biological process | Any process that activates or increases the frequency, rate or extent of prolactin secretion. [GO_REF:0000058, GOC:TermGenie, PMID:16159377] |
| positive regulation of miRNA transcription | biological process | Any process that activates or increases the frequency, rate or extent of microRNA (miRNA) gene transcription. [GO_REF:0000058, GOC:dph, GOC:kmv, GOC:TermGenie, PMID:24699545] |
| positive regulation of protein localization to plasma membrane | biological process | Any process that activates or increases the frequency, rate or extent of protein localization to plasma membrane. [GO_REF:0000058, GOC:BHF, GOC:rl, GOC:TermGenie, PMID:11602640] |
| negative regulation of cardiocyte differentiation | biological process | Any process that stops, prevents or reduces the frequency, rate or extent of cardiocyte differentiation. [GO_REF:0000058, GOC:bc, GOC:BHF, GOC:BHF_miRNA, GOC:TermGenie, PMID:23069713] |
| neurogenesis | biological process | Generation of cells within the nervous system. [GO_REF:0000021, GOC:cls, GOC:curators, GOC:dgh, GOC:dph, GOC:jid] |
| 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] |
| positive regulation of kinase activity | biological process | Any process that activates or increases the frequency, rate or extent of kinase activity, the catalysis of the transfer of a phosphate group, usually from ATP, to a substrate molecule. [GOC:mah] |
| cell 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] |