Proteins > Proto-oncogene tyrosine-protein kinase Src
Page last updated: 2024-08-07 15:57:11
Proto-oncogene tyrosine-protein kinase Src
A proto-oncogene tyrosine-protein kinase Src that is encoded in the genome of human. [PRO:CNA, UniProtKB:P12931]
Synonyms
EC 2.7.10.2;
Proto-oncogene c-Src;
pp60c-src;
p60-Src
Research
Bioassay Publications (203)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 13 (6.40) | 18.2507 |
| 2000's | 98 (48.28) | 29.6817 |
| 2010's | 77 (37.93) | 24.3611 |
| 2020's | 15 (7.39) | 2.80 |
Compounds (323)
Drugs with Inhibition Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| citric acid, anhydrous | Homo sapiens (human) | IC50 | 40,000.0000 | 2 | 2 |
| 4-nitrophenylphosphate | Homo sapiens (human) | IC50 | 1,000.0000 | 1 | 1 |
| malonic acid | Homo sapiens (human) | IC50 | 40,000.0000 | 2 | 2 |
| oxalic acid | Homo sapiens (human) | IC50 | 40,000.0000 | 2 | 2 |
| phosphoric acid | Homo sapiens (human) | IC50 | 40,000.0000 | 2 | 2 |
| pd 173074 | Homo sapiens (human) | IC50 | 13.5070 | 2 | 4 |
| cgp 52411 | Homo sapiens (human) | IC50 | 16.0000 | 1 | 1 |
| rtki cpd | Homo sapiens (human) | IC50 | 2.7000 | 1 | 1 |
| ro 31-8425 | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
| fosfosal | Homo sapiens (human) | IC50 | 2,000.0000 | 1 | 1 |
| nsc 664704 | Homo sapiens (human) | IC50 | 15.0000 | 1 | 1 |
| mebendazole | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| mebendazole | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| niclosamide | Homo sapiens (human) | IC50 | 10.2500 | 2 | 2 |
| pd 153035 | Homo sapiens (human) | IC50 | 33.8060 | 2 | 6 |
| pd168393 | Homo sapiens (human) | IC50 | 13.5365 | 2 | 2 |
| ag 1879 | Homo sapiens (human) | IC50 | 1.1814 | 8 | 8 |
| ag 1879 | Homo sapiens (human) | Ki | 0.5000 | 2 | 2 |
| imatinib | Homo sapiens (human) | GI50 | 2.1000 | 1 | 1 |
| imatinib | Homo sapiens (human) | IC50 | 62.5000 | 2 | 2 |
| imatinib | Homo sapiens (human) | Ki | 31.0000 | 3 | 3 |
| adenosine monophosphate | Homo sapiens (human) | IC50 | 0.1000 | 1 | 1 |
| indirubin | Homo sapiens (human) | IC50 | 18.0000 | 1 | 1 |
| indigo | Homo sapiens (human) | IC50 | 28.0000 | 1 | 1 |
| phenylphosphate | Homo sapiens (human) | IC50 | 2,960.0000 | 5 | 5 |
| adenosine 5'-tetraphosphate | Homo sapiens (human) | IC50 | 9.0000 | 1 | 1 |
| diadenosine tetraphosphate | Homo sapiens (human) | IC50 | 46.0000 | 1 | 1 |
| paclitaxel | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| aminomebendazole | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| aminomebendazole | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| staurosporine | Homo sapiens (human) | IC50 | 0.3642 | 25 | 25 |
| beta-naphthyl phosphate | Homo sapiens (human) | IC50 | 1,000.0000 | 1 | 1 |
| 7-amino-4-trifluoromethylcoumarin | Homo sapiens (human) | IC50 | 30.9000 | 1 | 1 |
| gefitinib | Homo sapiens (human) | IC50 | 1.1000 | 1 | 1 |
| (hydroxy-2-naphthalenylmethyl)phosphonic acid | Homo sapiens (human) | IC50 | 4,400.0000 | 1 | 1 |
| ptk 787 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| vatalanib | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| ruboxistaurin | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
| birb 796 | Homo sapiens (human) | IC50 | 35.0000 | 1 | 1 |
| sb 203580 | Homo sapiens (human) | IC50 | 5.0000 | 1 | 1 |
| enzastaurin | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
| sorafenib | Homo sapiens (human) | IC50 | 0.3900 | 1 | 1 |
| hematoxylin | Homo sapiens (human) | IC50 | 0.4400 | 1 | 1 |
| pd 173955 | Homo sapiens (human) | IC50 | 0.5928 | 2 | 5 |
| pd 166326 | Homo sapiens (human) | IC50 | 0.0646 | 4 | 10 |
| purvalanol a | Homo sapiens (human) | IC50 | 0.1833 | 2 | 3 |
| s 1033 | Homo sapiens (human) | GI50 | 0.4700 | 1 | 1 |
| s 1033 | Homo sapiens (human) | IC50 | 1.9300 | 2 | 4 |
| N-(3-cyano-4,5,6,7-tetrahydro-1-benzothiophen-2-yl)-1-naphthalenecarboxamide | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| tandutinib | Homo sapiens (human) | IC50 | 30.0000 | 1 | 1 |
| vx-745 | Homo sapiens (human) | IC50 | 3.0000 | 2 | 2 |
| dasatinib | Homo sapiens (human) | GI50 | 0.0003 | 1 | 1 |
| dasatinib | Homo sapiens (human) | IC50 | 0.0015 | 16 | 16 |
| dasatinib | Homo sapiens (human) | Ki | 0.0002 | 2 | 2 |
| zd 6474 | Homo sapiens (human) | IC50 | 0.0769 | 3 | 3 |
| gtp 14564 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| pd 407824 | Homo sapiens (human) | IC50 | 50.0000 | 1 | 1 |
| quercetin | Homo sapiens (human) | IC50 | 7.5600 | 2 | 2 |
| genistein | Homo sapiens (human) | IC50 | 61.6667 | 3 | 3 |
| butein | Homo sapiens (human) | IC50 | 65.0000 | 2 | 2 |
| norlichexanthone | Homo sapiens (human) | IC50 | 35.0000 | 1 | 1 |
| rosmarinic acid | Homo sapiens (human) | IC50 | 26.0000 | 1 | 1 |
| salvianolic acid a | Homo sapiens (human) | IC50 | 36.2000 | 1 | 1 |
| ellagic acid | Homo sapiens (human) | IC50 | 0.4667 | 3 | 3 |
| astrogorgiadiol | Homo sapiens (human) | IC50 | 1.9100 | 1 | 1 |
| ophiocordin | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| alvocidib | Homo sapiens (human) | IC50 | 34.0000 | 1 | 1 |
| su 5402 | Homo sapiens (human) | IC50 | 20.2933 | 2 | 6 |
| su 9516 | Homo sapiens (human) | IC50 | 8.0480 | 2 | 5 |
| pd 180970 | Homo sapiens (human) | IC50 | 0.4805 | 2 | 5 |
| cgp 77675 | Homo sapiens (human) | IC50 | 0.0102 | 2 | 2 |
| pd 166285 | Homo sapiens (human) | IC50 | 0.0461 | 4 | 9 |
| su 6656 | Homo sapiens (human) | IC50 | 229.4510 | 3 | 3 |
| granulatimide | Homo sapiens (human) | IC50 | 0.3500 | 1 | 1 |
| pd 089828 | Homo sapiens (human) | IC50 | 0.4000 | 3 | 5 |
| pd 166866 | Homo sapiens (human) | IC50 | 40.0096 | 3 | 5 |
| pd 161570 | Homo sapiens (human) | IC50 | 0.1148 | 2 | 4 |
| pd-173952 | Homo sapiens (human) | IC50 | 0.1681 | 4 | 9 |
| bosutinib | Homo sapiens (human) | IC50 | 0.0228 | 42 | 43 |
| semaxinib | Homo sapiens (human) | IC50 | 22.9543 | 3 | 7 |
| su 11248 | Homo sapiens (human) | IC50 | 0.2764 | 2 | 2 |
| m475271 | Homo sapiens (human) | IC50 | 0.2721 | 6 | 7 |
| d-64406 | Homo sapiens (human) | IC50 | 30.0000 | 1 | 1 |
| fosbretabulin | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| 2-tert-butyl-9-fluoro-3,6-dihydro-7h-benz(h)imidazo(4,5-f)isoquinoline-7-one | Homo sapiens (human) | IC50 | 8.0000 | 1 | 1 |
| vx680 | Homo sapiens (human) | Ki | 0.0805 | 1 | 6 |
| 2-((4-pyridyl)methyl)amino-n-(3-(trifluoromethyl)phenyl)benzamide | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| GSK3-XIII | Homo sapiens (human) | Ki | 0.0810 | 2 | 2 |
| cyc 116 | Homo sapiens (human) | Ki | 0.8200 | 1 | 1 |
| caftaric acid | Homo sapiens (human) | IC50 | 74.0000 | 1 | 1 |
| a 419259 | Homo sapiens (human) | IC50 | 0.3464 | 4 | 8 |
| b 43 | Homo sapiens (human) | IC50 | 0.3150 | 2 | 2 |
| gw2974 | Homo sapiens (human) | IC50 | 50.0000 | 1 | 1 |
| cgp 53353 | Homo sapiens (human) | IC50 | 50.0000 | 1 | 1 |
| a 770041 | Homo sapiens (human) | IC50 | 9.0500 | 1 | 1 |
| jnj 10198409 | Homo sapiens (human) | IC50 | 0.1850 | 2 | 2 |
| gw843682x | Homo sapiens (human) | IC50 | 30.0000 | 1 | 1 |
| ct52923 | Homo sapiens (human) | IC50 | 30.0000 | 1 | 2 |
| ap23464 | Homo sapiens (human) | IC50 | 3.4838 | 5 | 6 |
| bibw 2992 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| saracatinib | Homo sapiens (human) | IC50 | 1.6163 | 11 | 13 |
| pha 665752 | Homo sapiens (human) | IC50 | 6.0000 | 1 | 1 |
| PDGF receptor tyrosine kinase inhibitor III | Homo sapiens (human) | IC50 | 30.0000 | 1 | 1 |
| nvp-aew541 | Homo sapiens (human) | IC50 | 4.0000 | 1 | 1 |
| abt 869 | Homo sapiens (human) | IC50 | 50.0000 | 1 | 1 |
| pf 00299804 | Homo sapiens (human) | IC50 | 55.0550 | 2 | 2 |
| dorsomorphin | Homo sapiens (human) | IC50 | 0.0020 | 1 | 1 |
| gw 2580 | Homo sapiens (human) | IC50 | 16.0000 | 1 | 1 |
| tak 285 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| crizotinib | Homo sapiens (human) | IC50 | 5.5000 | 2 | 2 |
| 4-[2-(2-chloro-4-fluoroanilino)-5-methyl-4-pyrimidinyl]-N-[(1S)-1-(3-chlorophenyl)-2-hydroxyethyl]-1H-pyrrole-2-carboxamide | Homo sapiens (human) | Ki | 4.0000 | 1 | 1 |
| chir-265 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| motesanib | Homo sapiens (human) | IC50 | 1.0880 | 1 | 11 |
| N-(2,4-dimethoxyphenyl)-N-[2-[4-(4-methyl-1-piperazinyl)anilino]-4-pyrimidinyl]carbamic acid (2,6-dimethylphenyl) ester | Homo sapiens (human) | IC50 | 0.3908 | 2 | 5 |
| jnj-26483327 | Homo sapiens (human) | IC50 | 0.0110 | 1 | 1 |
| tg100801 | Homo sapiens (human) | IC50 | 10.0000 | 2 | 1 |
| azd 1152-hqpa | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| nvp-tae684 | Homo sapiens (human) | IC50 | 1.1460 | 1 | 1 |
| enmd 2076 | Homo sapiens (human) | IC50 | 0.0150 | 2 | 2 |
| 4-methyl-3-(2-(2-morpholinoethylamino)quinazolin-6-yl)-n-(3-(trifluoromethyl)phenyl)benzamide | Homo sapiens (human) | IC50 | 0.0020 | 1 | 1 |
| nvp-bhg712 | Homo sapiens (human) | IC50 | 1.2660 | 1 | 0 |
| kx-01 | Homo sapiens (human) | GI50 | 0.0200 | 1 | 1 |
| kx-01 | Homo sapiens (human) | IC50 | 21.1732 | 6 | 6 |
| plx 4720 | Homo sapiens (human) | IC50 | 1.3575 | 1 | 4 |
| cudc 101 | Homo sapiens (human) | IC50 | 11.0000 | 1 | 1 |
| amg 458 | Homo sapiens (human) | IC50 | 1.0000 | 1 | 1 |
| bms 777607 | Homo sapiens (human) | IC50 | 0.5000 | 1 | 1 |
| pci 32765 | Homo sapiens (human) | IC50 | 0.0768 | 5 | 5 |
| ponatinib | Homo sapiens (human) | IC50 | 0.0053 | 7 | 7 |
| PP121 | Homo sapiens (human) | IC50 | 0.0140 | 2 | 2 |
| cabozantinib | Homo sapiens (human) | IC50 | 0.1780 | 1 | 1 |
| defactinib | Homo sapiens (human) | IC50 | 1.0000 | 1 | 0 |
| 8-chloro-4-(3-chloro-4-fluoroanilino)-6-[[1-(1-ethyl-4-piperidinyl)-4-triazolyl]methylamino]-3-quinolinecarbonitrile | Homo sapiens (human) | IC50 | 53.0000 | 1 | 1 |
| 4-[6-[4-(methoxycarbonylamino)phenyl]-4-(4-morpholinyl)-1-pyrazolo[3,4-d]pyrimidinyl]-1-piperidinecarboxylic acid methyl ester | Homo sapiens (human) | IC50 | 50.0000 | 1 | 1 |
| tak-632 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| urmc-099 | Homo sapiens (human) | IC50 | 4.3300 | 1 | 1 |
| ceritinib | Homo sapiens (human) | IC50 | 1.6940 | 1 | 1 |
| debio 1347 | Homo sapiens (human) | IC50 | 5.9000 | 1 | 1 |
| pf-543 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| ly3009120 | Homo sapiens (human) | IC50 | 0.3100 | 1 | 1 |
| azd3759 | Homo sapiens (human) | IC50 | 0.6220 | 1 | 1 |
| at 9283 | Homo sapiens (human) | IC50 | 0.0100 | 1 | 1 |
| diguanosine tetraphosphate | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
| nintedanib | Homo sapiens (human) | IC50 | 0.1093 | 3 | 3 |
| pp242 | Homo sapiens (human) | IC50 | 2.4900 | 2 | 9 |
Drugs with Activation Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| fasudil | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| 4-(4'-hydroxyphenyl)-amino-6,7-dimethoxyquinazoline | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| sb 202190 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| imatinib | Homo sapiens (human) | Kd | 22.4527 | 4 | 4 |
| triciribine phosphate | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| staurosporine | Homo sapiens (human) | Kd | 0.0700 | 4 | 4 |
| picropodophyllin | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| gefitinib | Homo sapiens (human) | Kd | 10.6500 | 4 | 4 |
| lestaurtinib | Homo sapiens (human) | Kd | 10.4267 | 3 | 3 |
| perifosine | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| vatalanib | Homo sapiens (human) | Kd | 16.6667 | 3 | 3 |
| ruboxistaurin | Homo sapiens (human) | Kd | 16.6667 | 3 | 3 |
| canertinib | Homo sapiens (human) | Kd | 8.2400 | 4 | 4 |
| birb 796 | Homo sapiens (human) | Kd | 10.0000 | 2 | 2 |
| cyc 202 | Homo sapiens (human) | Kd | 20.0000 | 2 | 2 |
| sb 203580 | Homo sapiens (human) | Kd | 5.3000 | 2 | 2 |
| enzastaurin | Homo sapiens (human) | Kd | 20.0000 | 2 | 2 |
| erlotinib | Homo sapiens (human) | Kd | 8.3250 | 4 | 4 |
| lapatinib | Homo sapiens (human) | Kd | 16.6667 | 3 | 3 |
| sorafenib | Homo sapiens (human) | Kd | 15.0000 | 4 | 4 |
| pd 173955 | Homo sapiens (human) | Kd | 0.0007 | 1 | 1 |
| s 1033 | Homo sapiens (human) | Kd | 15.9500 | 2 | 2 |
| xl147 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| bms 387032 | Homo sapiens (human) | Kd | 16.6667 | 3 | 3 |
| sf 2370 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| tandutinib | Homo sapiens (human) | Kd | 14.9000 | 4 | 4 |
| vx-745 | Homo sapiens (human) | Kd | 3.9933 | 3 | 3 |
| dasatinib | Homo sapiens (human) | Kd | 0.0029 | 5 | 5 |
| 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 | 7.5775 | 4 | 4 |
| 4-(5-benzo(1,3)dioxol-5-yl-4-pyridin-2-yl-1h-imidazol-2-yl)benzamide | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| imd 0354 | Homo sapiens (human) | Kd | 30.0000 | 1 | 2 |
| sirolimus | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| alvocidib | Homo sapiens (human) | Kd | 16.6667 | 3 | 3 |
| bosutinib | Homo sapiens (human) | Kd | 0.0428 | 4 | 4 |
| orantinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| su 11248 | Homo sapiens (human) | Kd | 7.8800 | 5 | 5 |
| palbociclib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| jnj-7706621 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| vx680 | Homo sapiens (human) | Kd | 10.1133 | 3 | 3 |
| cyc 116 | Homo sapiens (human) | Kd | 30.0000 | 1 | 2 |
| everolimus | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| ekb 569 | Homo sapiens (human) | Kd | 10.1333 | 3 | 3 |
| axitinib | Homo sapiens (human) | Kd | 20.0000 | 2 | 2 |
| temsirolimus | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| pd 184352 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| on 01910 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| av 412 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| telatinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| y-39983 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| cp 547632 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| bms345541 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| lenvatinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| pd 0325901 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| midostaurin | Homo sapiens (human) | Kd | 8.4000 | 4 | 4 |
| 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 | 2.3000 | 1 | 1 |
| scio-469 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| cp 724714 | Homo sapiens (human) | Kd | 20.0000 | 2 | 2 |
| pi103 | Homo sapiens (human) | Kd | 10.0000 | 2 | 2 |
| hmn-214 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| tivozanib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| hki 272 | Homo sapiens (human) | Kd | 17.0500 | 2 | 2 |
| tofacitinib | Homo sapiens (human) | Kd | 16.6667 | 3 | 3 |
| n-(6-chloro-7-methoxy-9h-beta-carbolin-8-yl)-2-methylnicotinamide | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| cediranib | Homo sapiens (human) | Kd | 15.0405 | 2 | 2 |
| masitinib | Homo sapiens (human) | Kd | 15.4500 | 2 | 2 |
| ly-2157299 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| pazopanib | Homo sapiens (human) | Kd | 11.8667 | 3 | 3 |
| azd 6244 | Homo sapiens (human) | Kd | 20.0000 | 2 | 2 |
| su 14813 | Homo sapiens (human) | Kd | 13.2667 | 3 | 3 |
| bibw 2992 | Homo sapiens (human) | Kd | 16.4000 | 2 | 2 |
| binimetinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| sotrastaurin | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| aee 788 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| saracatinib | Homo sapiens (human) | Kd | 0.1320 | 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 | 20.0000 | 2 | 2 |
| cc 401 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| bms 599626 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| exel-7647 | Homo sapiens (human) | Kd | 1.1270 | 1 | 1 |
| volasertib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| pha 665752 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| azd 7762 | Homo sapiens (human) | Kd | 0.1090 | 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 | 15.0042 | 2 | 2 |
| brivanib | Homo sapiens (human) | Kd | 15.8000 | 2 | 2 |
| mp470 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| 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 | 20.0000 | 2 | 2 |
| bms-690514 | Homo sapiens (human) | Kd | 1.1530 | 1 | 1 |
| bi 2536 | Homo sapiens (human) | Kd | 20.0000 | 2 | 2 |
| inno-406 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| nvp-ast487 | Homo sapiens (human) | Kd | 0.3400 | 2 | 2 |
| kw 2449 | Homo sapiens (human) | Kd | 16.4000 | 2 | 2 |
| danusertib | Homo sapiens (human) | Kd | 0.0530 | 1 | 1 |
| abt 869 | Homo sapiens (human) | Kd | 16.6667 | 3 | 3 |
| azd 8931 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| arq 197 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| azd 1152 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| pf 00299804 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| ridaforolimus | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| ch 4987655 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| 6-(5-((cyclopropylamino)carbonyl)-3-fluoro-2-methylphenyl)-n-(2,2-dimethylprpyl)-3-pyridinecarboxamide | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| cc-930 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| gw 2580 | Homo sapiens (human) | Kd | 10.0000 | 2 | 2 |
| tak 285 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| idelalisib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| crizotinib | Homo sapiens (human) | Kd | 15.2800 | 2 | 2 |
| osi 906 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| chir-265 | Homo sapiens (human) | Kd | 10.7333 | 3 | 3 |
| motesanib | Homo sapiens (human) | Kd | 16.6667 | 3 | 3 |
| fostamatinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| trametinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 2 |
| mln8054 | Homo sapiens (human) | Kd | 10.5333 | 3 | 3 |
| pf-562,271 | Homo sapiens (human) | Kd | 30.0000 | 1 | 2 |
| GDC-0879 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| jnj-26483327 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| ly2603618 | Homo sapiens (human) | Kd | 30.0000 | 1 | 2 |
| 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 | 20.0000 | 2 | 2 |
| azd 1152-hqpa | Homo sapiens (human) | Kd | 16.6667 | 3 | 3 |
| nvp-tae684 | Homo sapiens (human) | EC50 | 1.0000 | 1 | 1 |
| nvp-tae684 | Homo sapiens (human) | Kd | 0.2800 | 1 | 1 |
| enmd 2076 | Homo sapiens (human) | Kd | 1.8580 | 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 | 0.0920 | 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 | 2 |
| pha 848125 | Homo sapiens (human) | Kd | 5.3130 | 1 | 1 |
| ro5126766 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| fedratinib | Homo sapiens (human) | Kd | 15.0375 | 2 | 2 |
| gsk690693 | Homo sapiens (human) | Kd | 20.0000 | 2 | 2 |
| 14-methyl-20-oxa-5,7,14,26-tetraazatetracyclo(19.3.1.1(2,6).1(8,12))heptacosa-1(25),2(26),3,5,8(27),9,11,16,21,23-decaene | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| azd5438 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| pf 04217903 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| gdc 0941 | Homo sapiens (human) | Kd | 20.0000 | 2 | 2 |
| icotinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| ph 797804 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| kx-01 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| plx 4720 | Homo sapiens (human) | Kd | 4.7000 | 1 | 1 |
| mk 5108 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| cx 4945 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| cudc 101 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| arry-614 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| tak 593 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| mln 8237 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| sgx 523 | Homo sapiens (human) | Kd | 20.0000 | 2 | 2 |
| 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) | Kd | 0.0970 | 1 | 1 |
| ponatinib | Homo sapiens (human) | Kd | 0.3670 | 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 | 16.6667 | 3 | 3 |
| 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 | 1 |
| n-(cyanomethyl)-4-(2-((4-(4-morpholinyl)phenyl)amino)-4-pyrimidinyl)benzamide | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| dcc-2036 | Homo sapiens (human) | Kd | 5.8520 | 1 | 1 |
| cabozantinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 2 |
| defactinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| ly2584702 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| incb-018424 | Homo sapiens (human) | Kd | 20.0000 | 2 | 2 |
| poziotinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| asp3026 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| entrectinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| pexidartinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| TAK-580 | Homo sapiens (human) | Kd | 30.0000 | 1 | 2 |
| 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 | 10.0000 | 1 | 1 |
| pf 3758309 | Homo sapiens (human) | Kd | 2.0850 | 1 | 1 |
| gdc 0980 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| azd2014 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| (5-(2,4-bis((3s)-3-methylmorpholin-4-yl)pyrido(2,3-d)pyrimidin-7-yl)-2-methoxyphenyl)methanol | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| plx4032 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| gsk 1363089 | Homo sapiens (human) | Kd | 0.0240 | 2 | 2 |
| arry-334543 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| kin-193 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| mk 2461 | Homo sapiens (human) | Kd | 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 | 2 |
| n-(3-fluoro-4-((1-methyl-6-(1h-pyrazol-4-yl)-1h-indazol-5 yl)oxy)phenyl)-1-(4-fluorophenyl)-6-methyl-2-oxo-1,2-dihydropyridine-3-carboxamide | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| ribociclib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| mk-8033 | Homo sapiens (human) | Kd | 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 | 2 |
| gilteritinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| alectinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| glpg0634 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| encorafenib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| bms-911543 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| gsk2141795 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| azd8186 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| byl719 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| cep-32496 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| rociletinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| 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 |
| osimertinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| at 9283 | Homo sapiens (human) | Kd | 0.5920 | 1 | 1 |
| otssp167 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| chir 258 | Homo sapiens (human) | Kd | 1.3940 | 3 | 3 |
| osi 027 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| nintedanib | Homo sapiens (human) | Kd | 15.2900 | 2 | 2 |
| bay 80-6946 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| pp242 | Homo sapiens (human) | Kd | 0.2200 | 1 | 1 |
Drugs with Other Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| phosphotyrosine | Homo sapiens (human) | ID50 | 3,500.0000 | 1 | 1 |
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
Synthesis and structure-activity relationships of soluble 7-substituted 3-(3,5-dimethoxyphenyl)-1,6-naphthyridin-2-amines and related ureas as dual inhibitors of the fibroblast growth factor receptor-1 and vascular endothelial growth factor receptor-2 tyrJournal of medicinal chemistry, , Jul-14, Volume: 48, Issue:14, 2005
Multiple determinants for selective inhibition of apicomplexan calcium-dependent protein kinase CDPK1.Journal of medicinal chemistry, , Mar-22, Volume: 55, Issue:6, 2012
Benzoylbenzimidazole-based selective inhibitors targeting Cryptosporidium parvum and Toxoplasma gondii calcium-dependent protein kinase-1.Bioorganic & medicinal chemistry letters, , Aug-15, Volume: 22, Issue:16, 2012
Pyrrolopyrimidines: An update on recent advancements in their medicinal attributes.European journal of medicinal chemistry, , Sep-05, Volume: 157, 2018
Cyclic peptides containing tryptophan and arginine as Src kinase inhibitors.Bioorganic & medicinal chemistry letters, , Jun-01, Volume: 23, Issue:11, 2013
Synthesis, biological evaluation and docking studies of new pyrrolo[2,3-d] pyrimidine derivatives as Src family-selective tyrosine kinase inhibitors.Journal of enzyme inhibition and medicinal chemistry, , Volume: 28, Issue:5, 2013
One-pot regioselective synthesis of tetrahydroindazolones and evaluation of their antiproliferative and Src kinase inhibitory activities.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 22, Issue:1, 2012
O-Aryl α,β-d-ribofuranosides: synthesis & highly efficient biocatalytic separation of anomers and evaluation of their Src kinase inhibitory activity.Bioorganic & medicinal chemistry, , Dec-01, Volume: 20, Issue:23, 2012
Click chemistry inspired one-pot synthesis of 1,4-disubstituted 1,2,3-triazoles and their Src kinase inhibitory activity.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 21, Issue:1, 2011
Synthesis of 3-phenylpyrazolopyrimidine-1,2,3-triazole conjugates and evaluation of their Src kinase inhibitory and anticancer activities.Bioorganic & medicinal chemistry letters, , Mar-01, Volume: 21, Issue:5, 2011
Discovery of novel purine derivatives with potent and selective inhibitory activity against c-Src tyrosine kinase.Bioorganic & medicinal chemistry, , Jul-01, Volume: 18, Issue:13, 2010
Identification of a novel pyrazolo[3,4-d]pyrimidine able to inhibit cell proliferation of a human osteogenic sarcoma in vitro and in a xenograft model in mice.Journal of medicinal chemistry, , Nov-15, Volume: 50, Issue:23, 2007
Pyrazolo[3,4-d]pyrimidines as potent antiproliferative and proapoptotic agents toward A431 and 8701-BC cells in culture via inhibition of c-Src phosphorylation.Journal of medicinal chemistry, , Mar-09, Volume: 49, Issue:5, 2006
Electrostatic Complementarity as a Fast and Effective Tool to Optimize Binding and Selectivity of Protein-Ligand Complexes.Journal of medicinal chemistry, , 03-28, Volume: 62, Issue:6, 2019
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Discovery of 2-((3-Amino-4-methylphenyl)amino)-N-(2-methyl-5-(3-(trifluoromethyl)benzamido)phenyl)-4-(methylamino)pyrimidine-5-carboxamide (CHMFL-ABL-053) as a Potent, Selective, and Orally Available BCR-ABL/SRC/p38 Kinase Inhibitor for Chronic Myeloid LeJournal of medicinal chemistry, , Mar-10, Volume: 59, Issue:5, 2016
Design, synthesis, biological activity, and ADME properties of pyrazolo[3,4-d]pyrimidines active in hypoxic human leukemia cells: a lead optimization study.Journal of medicinal chemistry, , Apr-28, Volume: 54, Issue:8, 2011
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
Discovery of aryl aminoquinazoline pyridones as potent, selective, and orally efficacious inhibitors of receptor tyrosine kinase c-Kit.Journal of medicinal chemistry, , Jun-12, Volume: 51, Issue:11, 2008
Synthesis, biological evaluation and docking studies of 4-amino substituted 1H-pyrazolo[3,4-d]pyrimidines.European journal of medicinal chemistry, , Volume: 43, Issue:12, 2008
Discovery and SAR of 1,3,4-thiadiazole derivatives as potent Abl tyrosine kinase inhibitors and cytodifferentiating agents.Bioorganic & medicinal chemistry letters, , Feb-01, Volume: 18, Issue:3, 2008
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
Designed multiple ligands. An emerging drug discovery paradigm.Journal of medicinal chemistry, , Oct-20, Volume: 48, Issue:21, 2005
Requirements for specific binding of low affinity inhibitor fragments to the SH2 domain of (pp60)Src are identical to those for high affinity binding of full length inhibitors.Journal of medicinal chemistry, , Nov-20, Volume: 46, Issue:24, 2003
Small ligands interacting with the phosphotyrosine binding pocket of the Src SH2 protein.Bioorganic & medicinal chemistry letters, , May-06, Volume: 12, Issue:9, 2002
SAR and X-ray. A new approach combining fragment-based screening and rational drug design: application to the discovery of nanomolar inhibitors of Src SH2.Journal of medicinal chemistry, , Jun-06, Volume: 45, Issue:12, 2002
Multiple determinants for selective inhibition of apicomplexan calcium-dependent protein kinase CDPK1.Journal of medicinal chemistry, , Mar-22, Volume: 55, Issue:6, 2012
Benzoylbenzimidazole-based selective inhibitors targeting Cryptosporidium parvum and Toxoplasma gondii calcium-dependent protein kinase-1.Bioorganic & medicinal chemistry letters, , Aug-15, Volume: 22, Issue:16, 2012
Design, synthesis, and biological evaluations of novel 3-amino-4-ethynyl indazole derivatives as Bcr-Abl kinase inhibitors with potent cellular antileukemic activity.European journal of medicinal chemistry, , Dec-01, Volume: 207, 2020
ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells.European journal of medicinal chemistry, , Jan-01, Volume: 161, 2019
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
New insights in the structure-activity relationships of 2-phenylamino-substituted benzothiopyrano[4,3-d]pyrimidines as kinase inhibitors.European journal of medicinal chemistry, , Apr-25, Volume: 150, 2018
Isolation, Characterization, and Structure-Activity Relationship Analysis of Abietane Diterpenoids from Callicarpa bodinieri as Spleen Tyrosine Kinase Inhibitors.Journal of natural products, , 04-27, Volume: 81, Issue:4, 2018
Challenging clinically unresponsive medullary thyroid cancer: Discovery and pharmacological activity of novel RET inhibitors.European journal of medicinal chemistry, , Apr-25, Volume: 150, 2018
Novel LCK/FMS inhibitors based on phenoxypyrimidine scaffold as potential treatment for inflammatory disorders.European journal of medicinal chemistry, , Dec-01, Volume: 141, 2017
Synthesis and biological evaluation of new [1,2,4]triazolo[4,3-a]pyridine derivatives as potential c-Met inhibitors.Bioorganic & medicinal chemistry, , 08-15, Volume: 24, Issue:16, 2016
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
Protein kinase and HDAC inhibitors from the endophytic fungus Epicoccum nigrum.Journal of natural products, , Jan-24, Volume: 77, Issue:1, 2014
Cyclic peptides containing tryptophan and arginine as Src kinase inhibitors.Bioorganic & medicinal chemistry letters, , Jun-01, Volume: 23, Issue:11, 2013
One-pot regioselective synthesis of tetrahydroindazolones and evaluation of their antiproliferative and Src kinase inhibitory activities.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 22, Issue:1, 2012
O-Aryl α,β-d-ribofuranosides: synthesis & highly efficient biocatalytic separation of anomers and evaluation of their Src kinase inhibitory activity.Bioorganic & medicinal chemistry, , Dec-01, Volume: 20, Issue:23, 2012
Imidazo[2,1-b]thiazole guanylhydrazones as RSK2 inhibitors.European journal of medicinal chemistry, , Volume: 46, Issue:9, 2011
Syntheses of phenylpyrazolodiazepin-7-ones as conformationally rigid analogs of aminopyrazole amide scaffold and their antiproliferative effects on cancer cells.Bioorganic & medicinal chemistry, , Nov-15, Volume: 19, Issue:22, 2011
Click chemistry inspired one-pot synthesis of 1,4-disubstituted 1,2,3-triazoles and their Src kinase inhibitory activity.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 21, Issue:1, 2011
Synthesis of 3-phenylpyrazolopyrimidine-1,2,3-triazole conjugates and evaluation of their Src kinase inhibitory and anticancer activities.Bioorganic & medicinal chemistry letters, , Mar-01, Volume: 21, Issue:5, 2011
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
Synthesis, activity, and pharmacophore development for isatin-beta-thiosemicarbazones with selective activity toward multidrug-resistant cells.Journal of medicinal chemistry, , May-28, Volume: 52, Issue:10, 2009
A new screening assay for allosteric inhibitors of cSrc.Nature chemical biology, , Volume: 5, Issue:6, 2009
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
Discovery of trans-3,4'-bispyridinylethylenes as potent and novel inhibitors of protein kinase B (PKB/Akt) for the treatment of cancer: Synthesis and biological evaluation.Bioorganic & medicinal chemistry letters, , Mar-15, Volume: 16, Issue:6, 2006
Synthesis and structure-activity relationship of 3,4'-bispyridinylethylenes: discovery of a potent 3-isoquinolinylpyridine inhibitor of protein kinase B (PKB/Akt) for the treatment of cancer.Bioorganic & medicinal chemistry letters, , Apr-01, Volume: 16, Issue:7, 2006
A small molecule-kinase interaction map for clinical kinase inhibitors.Nature biotechnology, , Volume: 23, Issue:3, 2005
Acyclic N-(azacycloalkyl)bisindolylmaleimides: isozyme selective inhibitors of PKCbeta.Bioorganic & medicinal chemistry letters, , Jun-02, Volume: 13, Issue:11, 2003
Identification of orally active, potent, and selective 4-piperazinylquinazolines as antagonists of the platelet-derived growth factor receptor tyrosine kinase family.Journal of medicinal chemistry, , Aug-15, Volume: 45, Issue:17, 2002
(S)-13-[(dimethylamino)methyl]-10,11,14,15-tetrahydro-4,9:16, 21-dimetheno-1H, 13H-dibenzo[e,k]pyrrolo[3,4-h][1,4,13]oxadiazacyclohexadecene-1,3(2H)-d ione (LY333531) and related analogues: isozyme selective inhibitors of protein kinase C beta.Journal of medicinal chemistry, , Jul-05, Volume: 39, Issue:14, 1996
Inhibitors of protein kinase C. 3. Potent and highly selective bisindolylmaleimides by conformational restriction.Journal of medicinal chemistry, , Jan-08, Volume: 36, Issue:1, 1993
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
Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases.Nature chemical biology, , Volume: 4, Issue:11, 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
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).Blood, , Oct-01, Volume: 114, Issue:14, 2009
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
Identification of a new chemical class of potent angiogenesis inhibitors based on conformational considerations and database searching.Bioorganic & medicinal chemistry letters, , Sep-15, Volume: 13, Issue:18, 2003
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
(S)-13-[(dimethylamino)methyl]-10,11,14,15-tetrahydro-4,9:16, 21-dimetheno-1H, 13H-dibenzo[e,k]pyrrolo[3,4-h][1,4,13]oxadiazacyclohexadecene-1,3(2H)-d ione (LY333531) and related analogues: isozyme selective inhibitors of protein kinase C beta.Journal of medicinal chemistry, , Jul-05, Volume: 39, Issue:14, 1996
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
A small molecule-kinase interaction map for clinical kinase inhibitors.Nature biotechnology, , Volume: 23, Issue:3, 2005
Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD).Bioorganic & medicinal chemistry letters, , Dec-01, Volume: 21, Issue:23, 2011
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
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
Rapid computational identification of the targets of protein kinase inhibitors.Journal of medicinal chemistry, , Jun-16, Volume: 48, Issue:12, 2005
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
Acyclic N-(azacycloalkyl)bisindolylmaleimides: isozyme selective inhibitors of PKCbeta.Bioorganic & medicinal chemistry letters, , Jun-02, Volume: 13, Issue:11, 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
A small molecule-kinase interaction map for clinical kinase inhibitors.Nature biotechnology, , Volume: 23, Issue:3, 2005
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).Blood, , Oct-01, Volume: 114, Issue:14, 2009
Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases.Nature chemical biology, , Volume: 4, Issue:11, 2008
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
Biochemical and cellular effects of c-Src kinase-selective pyrido[2, 3-d]pyrimidine tyrosine kinase inhibitors.Biochemical pharmacology, , Oct-01, Volume: 60, Issue:7, 2000
Structure-activity relationships of 6-(2,6-dichlorophenyl)-8-methyl-2-(phenylamino)pyrido[2,3-d]pyrimidin-7-ones: toward selective Abl inhibitors.Bioorganic & medicinal chemistry letters, , Dec-15, Volume: 19, Issue:24, 2009
Biochemical and cellular effects of c-Src kinase-selective pyrido[2, 3-d]pyrimidine tyrosine kinase inhibitors.Biochemical pharmacology, , Oct-01, Volume: 60, Issue:7, 2000
2-Substituted aminopyrido[2,3-d]pyrimidin-7(8H)-ones. structure-activity relationships against selected tyrosine kinases and in vitro and in vivo anticancer activity.Journal of medicinal chemistry, , Aug-13, Volume: 41, Issue:17, 1998
A small molecule inhibitor of PCSK9 that antagonizes LDL receptor binding via interaction with a cryptic PCSK9 binding groove.Bioorganic & medicinal chemistry, , 03-15, Volume: 28, Issue:6, 2020
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Discovery of 2-((3-Amino-4-methylphenyl)amino)-N-(2-methyl-5-(3-(trifluoromethyl)benzamido)phenyl)-4-(methylamino)pyrimidine-5-carboxamide (CHMFL-ABL-053) as a Potent, Selective, and Orally Available BCR-ABL/SRC/p38 Kinase Inhibitor for Chronic Myeloid LeJournal of medicinal chemistry, , Mar-10, Volume: 59, Issue:5, 2016
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
Structural analysis of DFG-in and DFG-out dual Src-Abl inhibitors sharing a common vinyl purine template.Chemical biology & drug design, , Volume: 75, Issue:1, 2010
N-(3-Cyano-4,5,6,7-tetrahydro-1-benzothien-2-yl)amides as potent, selective, inhibitors of JNK2 and JNK3.Bioorganic & medicinal chemistry letters, , Mar-01, Volume: 17, Issue:5, 2007
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).Blood, , Oct-01, Volume: 114, Issue:14, 2009
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
Identification of orally active, potent, and selective 4-piperazinylquinazolines as antagonists of the platelet-derived growth factor receptor tyrosine kinase family.Journal of medicinal chemistry, , Aug-15, Volume: 45, Issue:17, 2002
A Selective and Brain Penetrant p38αMAPK Inhibitor Candidate for Neurologic and Neuropsychiatric Disorders That Attenuates Neuroinflammation and Cognitive Dysfunction.Journal of medicinal chemistry, , 06-13, Volume: 62, Issue:11, 2019
The Discovery of VX-745: A Novel and Selective p38α Kinase Inhibitor.ACS medicinal chemistry letters, , Oct-13, Volume: 2, Issue:10, 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
A small molecule-kinase interaction map for clinical kinase inhibitors.Nature biotechnology, , Volume: 23, Issue:3, 2005
The progress of small-molecules and degraders against BCR-ABL for the treatment of CML.European journal of medicinal chemistry, , Aug-05, Volume: 238, 2022
Kinase Inhibitors as Underexplored Antiviral Agents.Journal of medicinal chemistry, , 01-27, Volume: 65, Issue:2, 2022
2-Aminothiazole: A privileged scaffold for the discovery of anti-cancer agents.European journal of medicinal chemistry, , Jan-15, Volume: 210, 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 p53 stabilizing agent CP-31398 and multi-kinase inhibitors. Designing, synthesizing and screening of styrylquinazoline series.European journal of medicinal chemistry, , Feb-01, Volume: 163, 2019
Controlling cellular distribution of drugs with permeability modifying moieties.MedChemComm, , Jun-01, Volume: 10, Issue:6, 2019
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Rapid Discovery and Structure-Activity Relationships of Pyrazolopyrimidines That Potently Suppress Breast Cancer Cell Growth via SRC Kinase Inhibition with Exceptional Selectivity over ABL Kinase.Journal of medicinal chemistry, , 05-26, Volume: 59, Issue:10, 2016
Discovery of 2-((3-Amino-4-methylphenyl)amino)-N-(2-methyl-5-(3-(trifluoromethyl)benzamido)phenyl)-4-(methylamino)pyrimidine-5-carboxamide (CHMFL-ABL-053) as a Potent, Selective, and Orally Available BCR-ABL/SRC/p38 Kinase Inhibitor for Chronic Myeloid LeJournal of medicinal chemistry, , Mar-10, Volume: 59, Issue:5, 2016
Design, Synthesis, and Structure-Activity Relationship Studies of 3-(Phenylethynyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine Derivatives as a New Class of Src Inhibitors with Potent Activities in Models of Triple Negative Breast Cancer.Journal of medicinal chemistry, , May-14, Volume: 58, Issue:9, 2015
Synthesis and pharmacological evaluation of thieno[2,3-b]pyridine derivatives as novel c-Src inhibitors.Bioorganic & medicinal chemistry, , Apr-15, Volume: 19, Issue:8, 2011
Imidazo[2,1-b]thiazole guanylhydrazones as RSK2 inhibitors.European journal of medicinal chemistry, , Volume: 46, Issue:9, 2011
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
Selectively nonselective kinase inhibition: striking the right balance.Journal of medicinal chemistry, , Feb-25, Volume: 53, Issue:4, 2010
Structure-based virtual screening of Src kinase inhibitors.Bioorganic & medicinal chemistry, , Apr-15, Volume: 17, Issue:8, 2009
A new screening assay for allosteric inhibitors of cSrc.Nature chemical biology, , Volume: 5, Issue:6, 2009
Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases.Nature chemical biology, , Volume: 4, Issue:11, 2008
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
Synthesis and biological evaluation of a fluorine-18 derivative of dasatinib.Journal of medicinal chemistry, , Nov-15, Volume: 50, Issue:23, 2007
2-aminothiazole as a novel kinase inhibitor template. Structure-activity relationship studies toward the discovery of N-(2-chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)-1- piperazinyl)]-2-methyl-4-pyrimidinyl]amino)]-1,3-thiazole-5-carboxamide (dasatinJournal of medicinal chemistry, , Nov-16, Volume: 49, Issue:23, 2006
Discovery of N-(2-chloro-6-methyl- phenyl)-2-(6-(4-(2-hydroxyethyl)- piperazin-1-yl)-2-methylpyrimidin-4- ylamino)thiazole-5-carboxamide (BMS-354825), a dual Src/Abl kinase inhibitor with potent antitumor activity in preclinical assays.Journal of medicinal chemistry, , Dec-30, Volume: 47, Issue:27, 2004
[no title available],
Kinase Inhibitors as Underexplored Antiviral Agents.Journal of medicinal chemistry, , 01-27, Volume: 65, Issue:2, 2022
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Discovery of biarylaminoquinazolines as novel tubulin polymerization inhibitors.Journal of medicinal chemistry, , Jun-12, Volume: 57, Issue:11, 2014
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
A small molecule-kinase interaction map for clinical kinase inhibitors.Nature biotechnology, , Volume: 23, Issue:3, 2005
Anthranilic acid amides: a novel class of antiangiogenic VEGF receptor kinase inhibitors.Journal of medicinal chemistry, , Dec-19, Volume: 45, Issue:26, 2002
Discovery of (E)-5-(benzylideneamino)-1H-benzo[d]imidazol-2(3H)-one derivatives as inhibitors for PTK6.Bioorganic & medicinal chemistry letters, , Oct-01, Volume: 24, Issue:19, 2014
Use of a pharmacophore model for the design of EGFR tyrosine kinase inhibitors: isoflavones and 3-phenyl-4(1H)-quinolones.Journal of medicinal chemistry, , Mar-25, Volume: 42, Issue:6, 1999
[(Alkylamino)methyl]acrylophenones: potent and selective inhibitors of the epidermal growth factor receptor protein tyrosine kinase.Journal of medicinal chemistry, , Jun-23, Volume: 38, Issue:13, 1995
Indeno[1,2-b]indole derivatives as a novel class of potent human protein kinase CK2 inhibitors.Bioorganic & medicinal chemistry, , Apr-01, Volume: 20, Issue:7, 2012
Identification of tricyclic analogs related to ellagic acid as potent/selective tyrosine protein kinase inhibitors.Journal of medicinal chemistry, , Jul-08, Volume: 37, Issue:14, 1994
A review on flavones targeting serine/threonine protein kinases for potential anticancer drugs.Bioorganic & medicinal chemistry, , 03-01, Volume: 27, Issue:5, 2019
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
Identification of substituted 3-[(4,5,6, 7-tetrahydro-1H-indol-2-yl)methylene]-1,3-dihydroindol-2-ones as growth factor receptor inhibitors for VEGF-R2 (Flk-1/KDR), FGF-R1, and PDGF-Rbeta tyrosine kinases.Journal of medicinal chemistry, , Jul-13, Volume: 43, Issue:14, 2000
Synthesis, biological evaluation and docking studies of new pyrrolo[2,3-d] pyrimidine derivatives as Src family-selective tyrosine kinase inhibitors.Journal of enzyme inhibition and medicinal chemistry, , Volume: 28, Issue:5, 2013
Docking, 3D-QSAR studies and in silico ADME prediction on c-Src tyrosine kinase inhibitors.European journal of medicinal chemistry, , Volume: 44, Issue:3, 2009
Synthetic Lethality through the Lens of Medicinal Chemistry.Journal of medicinal chemistry, , 12-10, Volume: 63, Issue:23, 2020
Synthesis and structure-activity relationships of 7-substituted 3-(2, 6-dichlorophenyl)-1,6-naphthyridin-2(1H)-ones as selective inhibitors of pp60(c-src).Journal of medicinal chemistry, , Aug-10, Volume: 43, Issue:16, 2000
Synthesis and tyrosine kinase inhibitory activity of a series of 2-amino-8H-pyrido[2,3-d]pyrimidines: identification of potent, selective platelet-derived growth factor receptor tyrosine kinase inhibitors.Journal of medicinal chemistry, , Oct-22, Volume: 41, Issue:22, 1998
2-Substituted aminopyrido[2,3-d]pyrimidin-7(8H)-ones. structure-activity relationships against selected tyrosine kinases and in vitro and in vivo anticancer activity.Journal of medicinal chemistry, , Aug-13, Volume: 41, Issue:17, 1998
Soluble 2-substituted aminopyrido[2,3-d]pyrimidin-7-yl ureas. Structure-activity relationships against selected tyrosine kinases and exploration of in vitro and in vivo anticancer activity.Journal of medicinal chemistry, , Jun-07, Volume: 44, Issue:12, 2001
3-(3,5-Dimethoxyphenyl)-1,6-naphthyridine-2,7-diamines and related 2-urea derivatives are potent and selective inhibitors of the FGF receptor-1 tyrosine kinase.Journal of medicinal chemistry, , Nov-02, Volume: 43, Issue:22, 2000
Structure-activity relationships for a novel series of pyrido[2,3-d]pyrimidine tyrosine kinase inhibitors.Journal of medicinal chemistry, , Jul-18, Volume: 40, Issue:15, 1997
Soluble 2-substituted aminopyrido[2,3-d]pyrimidin-7-yl ureas. Structure-activity relationships against selected tyrosine kinases and exploration of in vitro and in vivo anticancer activity.Journal of medicinal chemistry, , Jun-07, Volume: 44, Issue:12, 2001
3-(3,5-Dimethoxyphenyl)-1,6-naphthyridine-2,7-diamines and related 2-urea derivatives are potent and selective inhibitors of the FGF receptor-1 tyrosine kinase.Journal of medicinal chemistry, , Nov-02, Volume: 43, Issue:22, 2000
Structure-activity relationships for a novel series of pyrido[2,3-d]pyrimidine tyrosine kinase inhibitors.Journal of medicinal chemistry, , Jul-18, Volume: 40, Issue:15, 1997
Soluble 2-substituted aminopyrido[2,3-d]pyrimidin-7-yl ureas. Structure-activity relationships against selected tyrosine kinases and exploration of in vitro and in vivo anticancer activity.Journal of medicinal chemistry, , Jun-07, Volume: 44, Issue:12, 2001
Structure-activity relationships for a novel series of pyrido[2,3-d]pyrimidine tyrosine kinase inhibitors.Journal of medicinal chemistry, , Jul-18, Volume: 40, Issue:15, 1997
Synthesis and structure-activity relationships of 7-substituted 3-(2, 6-dichlorophenyl)-1,6-naphthyridin-2(1H)-ones as selective inhibitors of pp60(c-src).Journal of medicinal chemistry, , Aug-10, Volume: 43, Issue:16, 2000
Biochemical and cellular effects of c-Src kinase-selective pyrido[2, 3-d]pyrimidine tyrosine kinase inhibitors.Biochemical pharmacology, , Oct-01, Volume: 60, Issue:7, 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
The progress of small-molecules and degraders against BCR-ABL for the treatment of CML.European journal of medicinal chemistry, , Aug-05, Volume: 238, 2022
Kinase Inhibitors as Underexplored Antiviral Agents.Journal of medicinal chemistry, , 01-27, Volume: 65, Issue:2, 2022
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
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
AXL Inhibitors in Cancer: A Medicinal Chemistry Perspective.Journal of medicinal chemistry, , 04-28, Volume: 59, Issue:8, 2016
Discovery of 2-((3-Amino-4-methylphenyl)amino)-N-(2-methyl-5-(3-(trifluoromethyl)benzamido)phenyl)-4-(methylamino)pyrimidine-5-carboxamide (CHMFL-ABL-053) as a Potent, Selective, and Orally Available BCR-ABL/SRC/p38 Kinase Inhibitor for Chronic Myeloid LeJournal of medicinal chemistry, , Mar-10, Volume: 59, Issue:5, 2016
Synthesis and pharmacological evaluation of thieno[2,3-b]pyridine derivatives as novel c-Src inhibitors.Bioorganic & medicinal chemistry, , Apr-15, Volume: 19, Issue:8, 2011
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
Selectively nonselective kinase inhibition: striking the right balance.Journal of medicinal chemistry, , Feb-25, Volume: 53, Issue:4, 2010
Optimization of 7-alkene-3-quinolinecarbonitriles as Src kinase inhibitors.Bioorganic & medicinal chemistry letters, , May-01, Volume: 20, Issue:9, 2010
Structure-based virtual screening of Src kinase inhibitors.Bioorganic & medicinal chemistry, , Apr-15, Volume: 17, Issue:8, 2009
4-Anilino-7-pyridyl-3-quinolinecarbonitriles as Src kinase inhibitors.Bioorganic & medicinal chemistry letters, , Sep-01, Volume: 19, Issue:17, 2009
Global target profile of the kinase inhibitor bosutinib in primary chronic myeloid leukemia cells.Leukemia, , Volume: 23, Issue:3, 2009
Design and synthesis of 7-alkoxy-4-heteroarylamino-3-quinolinecarbonitriles as dual inhibitors of c-Src kinase and nitric oxide synthase.Bioorganic & medicinal chemistry, , Jun-01, Volume: 16, Issue:11, 2008
The design, synthesis and biological evaluation of 7-alkoxy-4-heteroarylamino-3-cyanoquinolines as dual inhibitors of c-Src and iNOS.Bioorganic & medicinal chemistry letters, , Dec-01, Volume: 18, Issue:23, 2008
Synthesis and Src kinase inhibitory activity of a series of 4-[(2,4-dichloro-5-methoxyphenyl)amino]-7-furyl-3-quinolinecarbonitriles.Journal of medicinal chemistry, , Dec-28, Volume: 49, Issue:26, 2006
Designed multiple ligands. An emerging drug discovery paradigm.Journal of medicinal chemistry, , Oct-20, Volume: 48, Issue:21, 2005
Further studies on ethenyl and ethynyl-4-phenylamino-3-quinolinecarbonitriles: identification of a subnanomolar Src kinase inhibitor.Bioorganic & medicinal chemistry letters, , Mar-15, Volume: 15, Issue:6, 2005
4-Anilino-7,8-dialkoxybenzo[g]quinoline-3-carbonitriles as potent Src kinase inhibitors.Journal of medicinal chemistry, , Sep-22, Volume: 48, Issue:19, 2005
Synthesis and Src kinase inhibitory activity of 2-phenyl- and 2-thienyl-7-phenylaminothieno[3,2-b]pyridine-6-carbonitriles.Journal of medicinal chemistry, , Jun-02, Volume: 48, Issue:11, 2005
Inhibition of Src kinase activity by 7-[(2,4-dichloro-5-methoxyphenyl)amino]-2-heteroaryl-thieno[3,2-b]pyridine-6-carbonitriles.Bioorganic & medicinal chemistry letters, , Nov-01, Volume: 15, Issue:21, 2005
Synthesis and inhibition of Src kinase activity by 7-ethenyl and 7-ethynyl-4-anilino-3-quinolinecarbonitriles.Bioorganic & medicinal chemistry letters, , May-03, Volume: 14, Issue:9, 2004
7-Alkoxy-4-phenylamino-3-quinolinecar-bonitriles as dual inhibitors of Src and Abl kinases.Journal of medicinal chemistry, , Mar-25, Volume: 47, Issue:7, 2004
Identification of 7-phenylaminothieno- [3,2-b]pyridine-6-carbonitriles as a new class of Src kinase inhibitors.Journal of medicinal chemistry, , Dec-30, Volume: 47, Issue:27, 2004
Investigation of the effect of varying the 4-anilino and 7-alkoxy groups of 3-quinolinecarbonitriles on the inhibition of Src kinase activity.Bioorganic & medicinal chemistry letters, , Nov-03, Volume: 13, Issue:21, 2003
Inhibition of Src kinase activity by 4-anilino-5,10-dihydro-pyrimido[4,5-b]quinolines.Bioorganic & medicinal chemistry letters, , Sep-15, Volume: 13, Issue:18, 2003
Substituted 4-anilino-7-phenyl-3-quinolinecarbonitriles as Src kinase inhibitors.Bioorganic & medicinal chemistry letters, , Oct-21, Volume: 12, Issue:20, 2002
Inhibition of Src kinase activity by 4-anilino-7-thienyl-3-quinolinecarbonitriles.Bioorganic & medicinal chemistry letters, , Aug-05, Volume: 12, Issue:15, 2002
Optimization of 4-phenylamino-3-quinolinecarbonitriles as potent inhibitors of Src kinase activity.Journal of medicinal chemistry, , Nov-08, Volume: 44, Issue:23, 2001
Anthranilic acid amides: a novel class of antiangiogenic VEGF receptor kinase inhibitors.Journal of medicinal chemistry, , Dec-19, Volume: 45, Issue:26, 2002
Identification of substituted 3-[(4,5,6, 7-tetrahydro-1H-indol-2-yl)methylene]-1,3-dihydroindol-2-ones as growth factor receptor inhibitors for VEGF-R2 (Flk-1/KDR), FGF-R1, and PDGF-Rbeta tyrosine kinases.Journal of medicinal chemistry, , Jul-13, Volume: 43, Issue:14, 2000
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Imidazo[2,1-b]thiazole guanylhydrazones as RSK2 inhibitors.European journal of medicinal chemistry, , Volume: 46, Issue:9, 2011
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
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
Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases.Nature chemical biology, , Volume: 4, Issue:11, 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
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
N-(5-chloro-1,3-benzodioxol-4-yl)-7-[2-(4-methylpiperazin-1-yl)ethoxy]-5- (tetrahydro-2H-pyran-4-yloxy)quinazolin-4-amine, a novel, highly selective, orally available, dual-specific c-Src/Abl kinase inhibitor.Journal of medicinal chemistry, , Nov-02, Volume: 49, Issue:22, 2006
Discovery of a new class of anilinoquinazoline inhibitors with high affinity and specificity for the tyrosine kinase domain of c-Src.Journal of medicinal chemistry, , Feb-12, Volume: 47, Issue:4, 2004
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
VX-680, a potent and selective small-molecule inhibitor of the Aurora kinases, suppresses tumor growth in vivo.Nature medicine, , Volume: 10, Issue:3, 2004
The discovery of the potent aurora inhibitor MK-0457 (VX-680).Bioorganic & medicinal chemistry letters, , Jul-01, Volume: 19, Issue:13, 2009
Discovery and development of aurora kinase inhibitors as anticancer agents.Journal of medicinal chemistry, , May-14, Volume: 52, Issue:9, 2009
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Discovery of N-phenyl-4-(thiazol-5-yl)pyrimidin-2-amine aurora kinase inhibitors.Journal of medicinal chemistry, , Jun-10, Volume: 53, Issue:11, 2010
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
A small molecule-kinase interaction map for clinical kinase inhibitors.Nature biotechnology, , Volume: 23, Issue:3, 2005
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
Synthesis, biological evaluation and docking studies of new pyrrolo[2,3-d] pyrimidine derivatives as Src family-selective tyrosine kinase inhibitors.Journal of enzyme inhibition and medicinal chemistry, , Volume: 28, Issue:5, 2013
Pyrazolo[3,4-d]pyrimidines containing an extended 3-substituent as potent inhibitors of Lck -- a selectivity insight.Bioorganic & medicinal chemistry letters, , Jun-17, Volume: 12, Issue:12, 2002
Pyrrolo[2,3-d]pyrimidines containing diverse N-7 substituents as potent inhibitors of Lck.Bioorganic & medicinal chemistry letters, , Jun-17, Volume: 12, Issue:12, 2002
Pyrrolo[2,3-d]pyrimidines containing diverse N-7 substituents as potent inhibitors of Lck.Bioorganic & medicinal chemistry letters, , Jun-17, Volume: 12, Issue:12, 2002
Pyrrolo[2,3-d]pyrimidines containing an extended 5-substituent as potent and selective inhibitors of lck I.Bioorganic & medicinal chemistry letters, , Oct-02, Volume: 10, Issue:19, 2000
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
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).Blood, , Oct-01, Volume: 114, Issue:14, 2009
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
Discovery of Brigatinib (AP26113), a Phosphine Oxide-Containing, Potent, Orally Active Inhibitor of Anaplastic Lymphoma Kinase.Journal of medicinal chemistry, , 05-26, Volume: 59, Issue:10, 2016
Application of MM-GB/SA and WaterMap to SRC Kinase Inhibitor Potency Prediction.ACS medicinal chemistry letters, , Feb-09, Volume: 3, Issue:2, 2012
Synthesis, biological evaluation and docking studies of 4-amino-tetrahydroquinazolino[3,2-e]purine derivatives.European journal of medicinal chemistry, , Volume: 45, Issue:12, 2010
Through the "gatekeeper door": exploiting the active kinase conformation.Journal of medicinal chemistry, , Apr-08, Volume: 53, Issue:7, 2010
Structural basis of Src tyrosine kinase inhibition with a new class of potent and selective trisubstituted purine-based compounds.Chemical biology & drug design, , Volume: 67, Issue:1, 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
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
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 Developments in the Use of Kinase Inhibitors for Management of Viral Infections.Journal of medicinal chemistry, , 01-27, Volume: 65, Issue:2, 2022
Kinase Inhibitors as Underexplored Antiviral Agents.Journal of medicinal chemistry, , 01-27, Volume: 65, Issue:2, 2022
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 pharmacological evaluation of thieno[2,3-b]pyridine derivatives as novel c-Src inhibitors.Bioorganic & medicinal chemistry, , Apr-15, Volume: 19, Issue:8, 2011
Emerging targets in osteoporosis disease modification.Journal of medicinal chemistry, , Jun-10, Volume: 53, Issue:11, 2010
Structure-based virtual screening of Src kinase inhibitors.Bioorganic & medicinal chemistry, , Apr-15, Volume: 17, Issue:8, 2009
c-Src protein kinase inhibitors block assembly and maturation of dengue virus.Proceedings of the National Academy of Sciences of the United States of America, , Feb-27, Volume: 104, Issue:9, 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
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
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
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
Discovery of N-(4-(3-amino-1H-indazol-4-yl)phenyl)-N'-(2-fluoro-5-methylphenyl)urea (ABT-869), a 3-aminoindazole-based orally active multitargeted receptor tyrosine kinase inhibitor.Journal of medicinal chemistry, , Apr-05, Volume: 50, Issue:7, 2007
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
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
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
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
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
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
Discovery of RAF265: A Potent mut-B-RAF Inhibitor for the Treatment of Metastatic Melanoma.ACS medicinal chemistry letters, , Sep-10, Volume: 6, Issue:9, 2015
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
AMG 706, an oral, multikinase inhibitor that selectively targets vascular endothelial growth factor, platelet-derived growth factor, and kit receptors, potently inhibits angiogenesis and induces regression in tumor xenografts.Cancer research, , Sep-01, Volume: 66, Issue:17, 2006
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
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
Development of prodrug 4-chloro-3-(5-methyl-3-{[4-(2-pyrrolidin-1-ylethoxy)phenyl]amino}-1,2,4-benzotriazin-7-yl)phenyl benzoate (TG100801): a topically administered therapeutic candidate in clinical trials for the treatment of age-related macular degenerJournal of medicinal chemistry, , Mar-27, Volume: 51, Issue:6, 2008
[no title available],
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
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, synthesis, and in vivo activity of a new class of pyrazoloquinazolines as selective inhibitors of aurora B kinase.Journal of medicinal chemistry, , May-03, Volume: 50, Issue:9, 2007
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling.Proceedings of the National Academy of Sciences of the United States of America, , Dec-11, Volume: 104, Issue:50, 2007
Identification of NVP-TAE684, a potent, selective, and efficacious inhibitor of NPM-ALK.Proceedings of the National Academy of Sciences of the United States of America, , Jan-02, Volume: 104, Issue:1, 2007
Discovery and development of extreme selective inhibitors of the ITD and D835Y mutant FLT3 kinases.European journal of medicinal chemistry, , Dec-15, Volume: 184, 2019
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Discovery and development of aurora kinase inhibitors as anticancer agents.Journal of medicinal chemistry, , May-14, Volume: 52, Issue:9, 2009
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
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 of Novel Dual Mechanism of Action Src Signaling and Tubulin Polymerization Inhibitors (KX2-391 and KX2-361).Journal of medicinal chemistry, , 06-14, Volume: 61, Issue:11, 2018
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Synthesis and pharmacological evaluation of thieno[2,3-b]pyridine derivatives as novel c-Src inhibitors.Bioorganic & medicinal chemistry, , Apr-15, Volume: 19, Issue:8, 2011
Novel synthesis and structural characterization of a high-affinity paramagnetic kinase probe for the identification of non-ATP site binders by nuclear magnetic resonance.Journal of medicinal chemistry, , Feb-11, Volume: 53, Issue:3, 2010
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
Discovery of a selective inhibitor of oncogenic B-Raf kinase with potent antimelanoma activity.Proceedings of the National Academy of Sciences of the United States of America, , Feb-26, Volume: 105, Issue:8, 2008
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
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Discovery of 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
Characterization of ibrutinib as a non-covalent inhibitor of SRC-family kinases.Bioorganic & medicinal chemistry letters, , 02-15, Volume: 34, 2021
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
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
[no title available]European journal of medicinal chemistry, , Feb-10, Volume: 145, 2018
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Kinase Inhibitors as Underexplored Antiviral Agents.Journal of medicinal chemistry, , 01-27, Volume: 65, Issue:2, 2022
The progress of small-molecules and degraders against BCR-ABL for the treatment of CML.European journal of medicinal chemistry, , Aug-05, Volume: 238, 2022
Targeting Rearranged during Transfection in Cancer: A Perspective on Small-Molecule Inhibitors and Their Clinical Development.Journal of medicinal chemistry, , 08-26, Volume: 64, Issue:16, 2021
Global PROTAC Toolbox for Degrading BCR-ABL Overcomes Drug-Resistant Mutants and Adverse Effects.Journal of medicinal chemistry, , 08-13, Volume: 63, Issue:15, 2020
Homogeneous Assay for Target Engagement Utilizing Bioluminescent Thermal Shift.ACS medicinal chemistry letters, , Jun-14, Volume: 9, Issue:6, 2018
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
Design, Synthesis, and Structure-Activity Relationship Studies of 3-(Phenylethynyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine Derivatives as a New Class of Src Inhibitors with Potent Activities in Models of Triple Negative Breast Cancer.Journal of medicinal chemistry, , May-14, Volume: 58, Issue:9, 2015
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
Identification of novel NEuropean journal of medicinal chemistry, , Feb-25, Volume: 146, 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
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
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
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Discovery of [5-Amino-1-(2-methyl-3H-benzimidazol-5-yl)pyrazol-4-yl]-(1H-indol-2-yl)methanone (CH5183284/Debio 1347), An Orally Available and Selective Fibroblast Growth Factor Receptor (FGFR) Inhibitor.Journal of medicinal chemistry, , 12-08, Volume: 59, Issue:23, 2016
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Fragment-based discovery of the pyrazol-4-yl urea (AT9283), a multitargeted kinase inhibitor with potent aurora kinase activity.Journal of medicinal chemistry, , Jan-22, Volume: 52, Issue:2, 2009
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
Structural modifications of indolinones bearing a pyrrole moiety and discovery of a multi-kinase inhibitor with potent antitumor activity.Bioorganic & medicinal chemistry, , 06-01, Volume: 28, Issue:11, 2020
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 23 target(s):
| Target | Category | Definition |
|---|
| protein kinase activity | molecular function | Catalysis of the phosphorylation of an amino acid residue in a protein, usually according to the reaction: a protein + ATP = a phosphoprotein + ADP. [PMID:25399640] |
| protein tyrosine kinase activity | molecular function | Catalysis of the reaction: ATP + a protein tyrosine = ADP + protein tyrosine phosphate. [RHEA:10596] |
| non-membrane spanning protein tyrosine kinase activity | molecular function | Catalysis of the reaction: ATP + protein L-tyrosine = ADP + protein L-tyrosine phosphate by a non-membrane spanning protein. [EC:2.7.10.2] |
| protein kinase C binding | molecular function | Binding to protein kinase C. [GOC:jl] |
| signaling receptor binding | molecular function | Binding to one or more specific sites on a receptor molecule, a macromolecule that undergoes combination with a hormone, neurotransmitter, drug or intracellular messenger to initiate a change in cell function. [GOC:bf, GOC:ceb, ISBN:0198506732] |
| insulin receptor binding | molecular function | Binding to an insulin receptor. [GOC:ai] |
| integrin binding | molecular function | Binding to an integrin. [GOC:ceb] |
| protein binding | molecular function | Binding to a protein. [GOC:go_curators] |
| ATP binding | molecular function | Binding to ATP, adenosine 5'-triphosphate, a universally important coenzyme and enzyme regulator. [ISBN:0198506732] |
| phospholipase activator activity | molecular function | Binds to and increases the activity of a phospholipase, an enzyme that catalyzes of the hydrolysis of a glycerophospholipid. [GOC:ai] |
| enzyme binding | molecular function | Binding to an enzyme, a protein with catalytic activity. [GOC:jl] |
| heme binding | molecular function | Binding to a heme, a compound composed of iron complexed in a porphyrin (tetrapyrrole) ring. [GOC:ai] |
| nuclear estrogen receptor binding | molecular function | Binding to a nuclear estrogen receptor. [GOC:ai] |
| SH2 domain binding | molecular function | Binding to a SH2 domain (Src homology 2) of a protein, a protein domain of about 100 amino-acid residues and belonging to the alpha + beta domain class. [GOC:go_curators, Pfam:PF00017] |
| phospholipase binding | molecular function | Binding to a phospholipase. [GOC:jl] |
| transmembrane transporter binding | molecular function | Binding to a transmembrane transporter, a protein or protein complex that enables the transfer of a substance, usually a specific substance or a group of related substances, from one side of a membrane to the other. [GOC:BHF, GOC:jl, PMID:33199372] |
| cadherin binding | molecular function | Binding to cadherin, a type I membrane protein involved in cell adhesion. [GOC:bf] |
| ephrin receptor binding | molecular function | Binding to an ephrin receptor. [GOC:ai] |
| ATPase binding | molecular function | Binding to an ATPase, any enzyme that catalyzes the hydrolysis of ATP. [GOC:ai] |
| phosphoprotein binding | molecular function | Binding to a phosphorylated protein. [GOC:ai] |
| BMP receptor binding | molecular function | Binding to a BMP receptor. [GOC:BHF, GOC:vk] |
| connexin binding | molecular function | Binding to a connexin, any of a group of related proteins that assemble to form gap junctions. [GOC:mah, PMID:19864490] |
| scaffold protein binding | molecular function | Binding to a scaffold protein. Scaffold proteins are crucial regulators of many key signaling pathways. Although not strictly defined in function, they are known to interact and/or bind with multiple members of a signaling pathway, tethering them into complexes. [GOC:BHF, GOC:sjp, PMID:10433269, Wikipedia:Scaffold_protein] |
Located In
This protein is located in 23 target(s):
| Target | Category | Definition |
|---|
| podosome | cellular component | An actin-rich adhesion structure characterized by formation upon cell substrate contact and localization at the substrate-attached part of the cell, contain an F-actin-rich core surrounded by a ring structure containing proteins such as vinculin and talin, and have a diameter of 0.5 mm. [PMID:12837608, PMID:15890982] |
| nucleoplasm | cellular component | That part of the nuclear content other than the chromosomes or the nucleolus. [GOC:ma, ISBN:0124325653] |
| cytoplasm | cellular component | The contents of a cell excluding the plasma membrane and nucleus, but including other subcellular structures. [ISBN:0198547684] |
| mitochondrion | cellular component | A semiautonomous, self replicating organelle that occurs in varying numbers, shapes, and sizes in the cytoplasm of virtually all eukaryotic cells. It is notably the site of tissue respiration. [GOC:giardia, ISBN:0198506732] |
| mitochondrial inner membrane | cellular component | The inner, i.e. lumen-facing, lipid bilayer of the mitochondrial envelope. It is highly folded to form cristae. [GOC:ai] |
| lysosome | cellular component | A small lytic vacuole that has cell cycle-independent morphology found in most animal cells and that contains a variety of hydrolases, most of which have their maximal activities in the pH range 5-6. The contained enzymes display latency if properly isolated. About 40 different lysosomal hydrolases are known and lysosomes have a great variety of morphologies and functions. [GOC:mah, ISBN:0198506732] |
| late endosome | cellular component | A prelysosomal endocytic organelle differentiated from early endosomes by lower lumenal pH and different protein composition. Late endosomes are more spherical than early endosomes and are mostly juxtanuclear, being concentrated near the microtubule organizing center. [NIF_Subcellular:nlx_subcell_20090702, PMID:11964142, PMID:2557062] |
| cytosol | cellular component | The part of the cytoplasm that does not contain organelles but which does contain other particulate matter, such as protein complexes. [GOC:hjd, GOC:jl] |
| actin filament | cellular component | A filamentous structure formed of a two-stranded helical polymer of the protein actin and associated proteins. Actin filaments are a major component of the contractile apparatus of skeletal muscle and the microfilaments of the cytoskeleton of eukaryotic cells. The filaments, comprising polymerized globular actin molecules, appear as flexible structures with a diameter of 5-9 nm. They are organized into a variety of linear bundles, two-dimensional networks, and three dimensional gels. In the cytoskeleton they are most highly concentrated in the cortex of the cell just beneath the plasma membrane. [GOC:mah, ISBN:0198506732, PMID:10666339] |
| 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] |
| caveola | cellular component | A membrane raft that forms small pit, depression, or invagination that communicates with the outside of a cell and extends inward, indenting the cytoplasm and the cell membrane. Examples include flask-shaped invaginations of the plasma membrane in adipocytes associated with caveolin proteins, and minute pits or incuppings of the cell membrane formed during pinocytosis. Caveolae may be pinched off to form free vesicles within the cytoplasm. [GOC:mah, ISBN:0721662544, PMID:16645198] |
| 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 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] |
| ruffle membrane | cellular component | The portion of the plasma membrane surrounding a ruffle. [GOC:mah] |
| neuronal cell body | cellular component | The portion of a neuron that includes the nucleus, but excludes cell projections such as axons and dendrites. [GOC:go_curators] |
| dendritic growth cone | cellular component | The migrating motile tip of a growing nerve cell dendrite. [GOC:jl] |
| 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] |
| extracellular exosome | cellular component | A vesicle that is released into the extracellular region by fusion of the limiting endosomal membrane of a multivesicular body with the plasma membrane. Extracellular exosomes, also simply called exosomes, have a diameter of about 40-100 nm. [GOC:BHF, GOC:mah, GOC:vesicles, PMID:15908444, PMID:17641064, PMID:19442504, PMID:19498381, PMID:22418571, PMID:24009894] |
| synaptic membrane | cellular component | A specialized area of membrane on either the presynaptic or the postsynaptic side of a synapse, the junction between a nerve fiber of one neuron and another neuron or muscle fiber or glial cell. [GOC:BHF, PMID:20410104] |
| glutamatergic synapse | cellular component | A synapse that uses glutamate as a neurotransmitter. [GOC:dos] |
| postsynaptic specialization, intracellular component | cellular component | A network of proteins adjacent to the postsynaptic membrane. Its major components include the proteins that spatially and functionally organize neurotransmitter receptors in the adjacent membrane, such as anchoring and scaffolding molecules, signaling enzymes and cytoskeletal components. [GOC:dos] |
| dendritic filopodium | cellular component | A small, membranous protrusion found primarily on dendritic stretches of developing neurons. May receive synaptic input, and can develop into dendritic spines. [GO_REF:0000064, GOC:pad, GOC:PARL, GOC:TermGenie, PMID:24464040, Wikipedia:Dendritic_filopodia] |
Active In
This protein is active in 1 target(s):
| Target | Category | Definition |
|---|
| plasma membrane | cellular component | The membrane surrounding a cell that separates the cell from its external environment. It consists of a phospholipid bilayer and associated proteins. [ISBN:0716731363] |
Involved In
This protein is involved in 116 target(s):
| Target | Category | Definition |
|---|
| primary ovarian follicle growth | biological process | Increase in size of primary follicles including oocyte growth and granulosa and/or theca cell proliferation until more than one layer of granulosa cells is present (preantral follicle). [GOC:mtg_mpo, https://www.ncbi.nlm.nih.gov/books/NBK279054/] |
| positive regulation of cytokine production | biological process | Any process that activates or increases the frequency, rate or extent of production of a cytokine. [GOC:add, ISBN:0781735149] |
| stimulatory C-type lectin receptor signaling pathway | biological process | The series of molecular signals initiated by the binding of C-type lectin to its receptor on the surface of a target cell, and resulting in cellular activation. [GO_REF:0000022, GOC:add, ISBN:0781735149] |
| negative regulation of inflammatory response to antigenic stimulus | biological process | Any process that stops, prevents, or reduces the frequency, rate, or extent of an inflammatory response to an antigenic stimulus. [GOC:add] |
| 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] |
| signal complex assembly | biological process | The aggregation, arrangement and bonding together of a set of components to form a complex capable of relaying a signal within a cell. [GOC:bf, GOC:signaling, PMID:9646862] |
| 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] |
| transforming growth factor beta receptor signaling pathway | biological process | The series of molecular signals initiated by an extracellular ligand binding to a transforming growth factor beta receptor on the surface of a target cell, and ending with the regulation of a downstream cellular process, e.g. transcription. [GOC:BHF, GOC:mah, GOC:signaling] |
| integrin-mediated signaling pathway | biological process | The series of molecular signals initiated by an extracellular ligand binding to an integrin on the surface of a target cell, and ending with the regulation of a downstream cellular process, e.g. transcription. [GOC:mah, GOC:signaling] |
| spermatogenesis | biological process | The developmental process by which male germ line stem cells self renew or give rise to successive cell types resulting in the development of a spermatozoa. [GOC:jid, ISBN:9780878933846, PMID:28073824, PMID:30990821] |
| 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] |
| response to xenobiotic stimulus | 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 stimulus from a xenobiotic, a compound foreign to the organim exposed to it. It may be synthesized by another organism (like ampicilin) or it can be a synthetic chemical. [GOC:jl, GOC:krc] |
| response to mechanical stimulus | 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 mechanical stimulus. [GOC:hb] |
| response to acidic pH | 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 pH stimulus with pH < 7. pH is a measure of the acidity or basicity of an aqueous solution. [GOC:go_curators, GOC:tb, Wikipedia:PH] |
| negative regulation of gene expression | biological process | Any process that decreases the frequency, rate or extent of gene expression. Gene expression is the process in which a gene's coding sequence is converted into a mature gene product (protein or RNA). [GOC:txnOH-2018] |
| regulation of epithelial cell migration | biological process | Any process that modulates the frequency, rate or extent of epithelial cell migration. [GOC:BHF, GOC:dph, GOC:tb] |
| positive regulation of epithelial cell migration | biological process | Any process that activates or increases the frequency, rate or extent of epithelial cell migration. [GOC:BHF, GOC:dph, GOC:tb] |
| positive regulation of glucose metabolic process | biological process | Any process that increases the rate, frequency or extent of glucose metabolism. Glucose metabolic processes are the chemical reactions and pathways involving glucose, the aldohexose gluco-hexose. [GOC:BHF, GOC:tb] |
| positive regulation of protein processing | biological process | Any process that increases the rate, frequency or extent of protein maturation by peptide bond cleavage. [GOC:dph, GOC:mah, GOC:tb] |
| skeletal muscle cell proliferation | biological process | The multiplication or reproduction of skeletal muscle cells, resulting in the expansion of a cell population. [CL:0000188, GOC:ef, GOC:mtg_muscle] |
| positive regulation of smooth muscle cell migration | biological process | Any process that activates, maintains or increases the frequency, rate or extent of smooth muscle cell migration. [CL:0000192, GOC:mtg_muscle] |
| macroautophagy | biological process | The autophagic process that proceeds via the formation of an autophagosome. [PMID:24366339] |
| peptidyl-tyrosine phosphorylation | biological process | The phosphorylation of peptidyl-tyrosine to form peptidyl-O4'-phospho-L-tyrosine. [RESID:AA0039] |
| regulation of cell-cell adhesion | biological process | Any process that modulates the frequency, rate or extent of attachment of a cell to another cell. [GOC:isa_complete] |
| platelet activation | biological process | A series of progressive, overlapping events triggered by exposure of the platelets to subendothelial tissue. These events include shape change, adhesiveness, aggregation, and release reactions. When carried through to completion, these events lead to the formation of a stable hemostatic plug. [http://www.graylab.ac.uk/omd/] |
| forebrain development | biological process | The process whose specific outcome is the progression of the forebrain over time, from its formation to the mature structure. The forebrain is the anterior of the three primary divisions of the developing chordate brain or the corresponding part of the adult brain (in vertebrates, includes especially the cerebral hemispheres, the thalamus, and the hypothalamus and especially in higher vertebrates is the main control center for sensory and associative information processing, visceral functions, and voluntary motor functions). [http://www2.merriam-webster.com/cgi-bin/mwmednlm?book=Medical&va=forebrain] |
| T cell costimulation | biological process | The process of providing, via surface-bound receptor-ligand pairs, a second, antigen-independent, signal in addition to that provided by the T cell receptor to augment T cell activation. [ISBN:0781735149] |
| negative regulation of protein-containing complex assembly | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of protein complex assembly. [GOC:mah] |
| protein destabilization | biological process | Any process that decreases the stability of a protein, making it more vulnerable to degradative processes or aggregation. [GOC:mah] |
| response to nutrient levels | 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 stimulus reflecting the presence, absence, or concentration of nutrients. [GOC:mah] |
| negative regulation of telomere maintenance via telomerase | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of the addition of telomeric repeats by telomerase. [GOC:mah] |
| cellular response to insulin 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 insulin stimulus. Insulin is a polypeptide hormone produced by the islets of Langerhans of the pancreas in mammals, and by the homologous organs of other organisms. [GOC:mah, ISBN:0198506732] |
| regulation of intracellular estrogen receptor signaling pathway | biological process | Any process that modulates the frequency, rate or extent of the activity of an intracellular estrogen receptor signaling pathway. [GOC:mah] |
| positive regulation of integrin activation | biological process | Any process that activates or increases the frequency, rate, or extent of integrin activation. [GOC:add] |
| regulation of toll-like receptor 3 signaling pathway | biological process | Any process that modulates the frequency, rate, or extent of toll-like receptor 3 signaling pathway. [GOC:add, PMID:16551253, PMID:17328678] |
| adherens junction organization | biological process | A process that is carried out at the cellular level which results in the assembly, arrangement of constituent parts, or disassembly of an adherens junction. An adherens junction is a cell-cell junction composed of the epithelial cadherin-catenin complex at which the cytoplasmic face of the plasma membrane is attached to actin filaments. [GOC:aruk, GOC:bc, GOC:dph, GOC:jl, GOC:mah] |
| substrate adhesion-dependent cell spreading | biological process | The morphogenetic process that results in flattening of a cell as a consequence of its adhesion to a substrate. [GOC:mah, GOC:pf, PMID:17050732] |
| positive regulation of dephosphorylation | biological process | Any process that activates or increases the frequency, rate or extent of removal of phosphate groups from a molecule. [GOC:bf] |
| negative regulation of hippo signaling | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of hippo signaling. [GOC:bf] |
| intracellular signal transduction | biological process | The process in which a signal is passed on to downstream components within the cell, which become activated themselves to further propagate the signal and finally trigger a change in the function or state of the cell. [GOC:bf, GOC:jl, GOC:signaling, ISBN:3527303782] |
| entry of bacterium into host cell | biological process | The process in which a bacterium enters a host cell. The host is defined as the larger of the organisms involved in a symbiotic interaction. [GOC:bf, PMID:21187937] |
| osteoclast development | biological process | The process whose specific outcome is the progression of a osteoclast from its formation to the mature structure. Cell development does not include the steps involved in committing a cell to a specific fate. An osteoclast is a specialized phagocytic cell associated with the absorption and removal of the mineralized matrix of bone tissue. [CL:0000092, GOC:bf, GOC:yaf] |
| cellular response to platelet-derived growth factor stimulus | biological process | Any process that results in a change in state or activity of a cell (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a platelet-derived growth factor stimulus. [GOC:yaf] |
| Fc-gamma receptor signaling pathway involved in phagocytosis | biological process | An Fc-gamma receptor signaling pathway that contributes to the endocytic engulfment of external particulate material by phagocytes. [GOC:phg, PMID:12488490, PMID:15466916] |
| ERBB2 signaling pathway | biological process | The series of molecular signals initiated by binding of a ligand to the tyrosine kinase receptor ERBB2 on the surface of a cell. The pathway ends with regulation of a downstream cellular process, e.g. transcription. ERBB2 receptors are themselves unable to bind to ligands, but act as a signal-amplifying tyrosine kinase within a heterodimeric pair. [GOC:jc, PMID:16460914, Reactome:R-HSA-1227986] |
| angiotensin-activated signaling pathway | biological process | A G protein-coupled receptor signaling pathway initiated by angiotensin II binding to its receptor on the surface of a target cell, and ending with the regulation of a downstream cellular process, e.g. transcription. [GOC:BHF, GOC:mtg_cardiac_conduct_nov11, GOC:nhn, GOC:signaling, PMID:10977869] |
| odontogenesis | biological process | The process whose specific outcome is the progression of a tooth or teeth over time, from formation to the mature structure(s). A tooth is any hard bony, calcareous, or chitinous organ found in the mouth or pharynx of an animal and used in procuring or masticating food. [GOC:jl, GOC:mah] |
| positive regulation of apoptotic process | biological process | Any process that activates or increases the frequency, rate or extent of cell death by apoptotic process. [GOC:jl, GOC:mtg_apoptosis] |
| 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] |
| regulation of vascular permeability | biological process | Any process that modulates the extent to which blood vessels can be pervaded by fluid. [GOC:jl] |
| stress fiber assembly | biological process | The aggregation, arrangement and bonding together of a set of components to form a stress fiber. A stress fiber is a contractile actin filament bundle that consists of short actin filaments with alternating polarity. [GOC:go_curators, GOC:mah, PMID:16651381] |
| negative regulation of cysteine-type endopeptidase activity involved in apoptotic process | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of a cysteine-type endopeptidase activity involved in the apoptotic process. [GOC:jl, GOC:mtg_apoptosis] |
| transcytosis | biological process | The directed movement of endocytosed material through the cell and its exocytosis from the plasma membrane at the opposite side. [ISBN:0716731363] |
| regulation of bone resorption | biological process | Any process that modulates the frequency, rate or extent of bone tissue loss (resorption). [GOC:ai] |
| bone resorption | biological process | The process in which specialized cells known as osteoclasts degrade the organic and inorganic portions of bone, and endocytose and transport the degradation products. [GOC:mah, PMID:10968780] |
| positive regulation of Notch signaling pathway | biological process | Any process that activates or increases the frequency, rate or extent of the Notch signaling pathway. [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 Ras protein signal transduction | biological process | Any process that activates or increases the frequency, rate or extent of Ras protein signal transduction. [GOC:bf] |
| positive regulation of insulin receptor signaling pathway | biological process | Any process that increases the frequency, rate or extent of insulin receptor signaling. [GOC:bf] |
| 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] |
| platelet-derived growth factor receptor signaling pathway | biological process | The series of molecular signals initiated by a ligand binding to a platelet-derived growth factor receptor on the surface of a target cell, and ending with the regulation of a downstream cellular process, e.g. transcription. [GOC:ceb] |
| vascular endothelial growth factor receptor signaling pathway | biological process | The series of molecular signals initiated by a ligand binding to a vascular endothelial growth factor receptor (VEGFR) on the surface of the target cell, and ending with the regulation of a downstream cellular process, e.g. transcription. [GOC:ceb, GOC:signaling] |
| neurotrophin TRK receptor signaling pathway | biological process | The series of molecular signals initiated by neurotrophin binding to its receptor on the surface of a target cell where the receptor possesses tyrosine kinase activity, and ending with the regulation of a downstream cellular process, e.g. transcription. [GOC:bf, GOC:ceb, GOC:jc, GOC:signaling, PMID:12065629, Wikipedia:Trk_receptor] |
| ephrin receptor signaling pathway | biological process | The series of molecular signals initiated by ephrin binding to its receptor, and ending with the regulation of a downstream cellular process, e.g. transcription. [GOC:ceb] |
| focal adhesion assembly | biological process | The aggregation and bonding together of a set of components to form a focal adhesion, a complex of intracellular signaling and structural proteins that provides a structural link between the internal actin cytoskeleton and the ECM, and also function as a locus of signal transduction activity. [GOC:jid, GOC:mah] |
| oogenesis | biological process | The complete process of formation and maturation of an ovum or female gamete from a primordial female germ cell. Examples of this process are found in Mus musculus and Drosophila melanogaster. [GOC:kmv, GOC:mtg_sensu, GOC:pr] |
| positive regulation of peptidyl-tyrosine phosphorylation | biological process | Any process that activates or increases the frequency, rate or extent of the phosphorylation of peptidyl-tyrosine. [GOC:ai] |
| progesterone receptor signaling pathway | biological process | The series of molecular signals initiated by progesterone binding to its receptor in the cytoplasm. [GOC:ai, GOC:mah, PMID:14744870] |
| leukocyte migration | biological process | The movement of a leukocyte within or between different tissues and organs of the body. [GOC:add, ISBN:0781735149, PMID:14680625, PMID:14708592, PMID:7507411, PMID:8600538] |
| positive regulation of small GTPase mediated signal transduction | biological process | Any process that activates or increases the frequency, rate or extent of small GTPase mediated signal transduction. [GOC:ai] |
| positive regulation of protein transport | biological process | Any process that activates or increases the frequency, rate or extent of the directed movement of a protein into, out of or within a cell, or between cells, by means of some agent such as a transporter or pore. [GOC:ai] |
| response to mineralocorticoid | 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 mineralocorticoid stimulus. Mineralocorticoids are hormonal C21 corticosteroids synthesized from cholesterol and characterized by their similarity to aldosterone. Mineralocorticoids act primarily on water and electrolyte balance. [GOC:ai, PMID:9884123] |
| myoblast proliferation | biological process | The multiplication or reproduction of myoblasts, resulting in the expansion of a myoblast cell population. A myoblast is a mononucleate cell type that, by fusion with other myoblasts, gives rise to the myotubes that eventually develop into skeletal muscle fibers. [CL:0000056, GOC:ai, GOC:mtg_muscle] |
| response to electrical stimulus | 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 an electrical stimulus. [GOC:ai] |
| negative regulation of focal adhesion assembly | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of focal adhesion assembly, the establishment and maturation of focal adhesions. [GOC:ai] |
| positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transduction | biological process | Any process that activates or increases the frequency, rate or extent of phosphatidylinositol 3-kinase/protein kinase B signal transduction. [GOC:ai] |
| negative regulation of mitochondrial depolarization | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of the change in the membrane potential of the mitochondria from negative to positive. [GOC:ai] |
| negative regulation of telomerase activity | biological process | Any process that stops or reduces the activity of the enzyme telomerase, which catalyzes of the reaction: deoxynucleoside triphosphate + DNA(n) = diphosphate + DNA(n+1). [GOC:ai] |
| uterus development | biological process | The reproductive developmental process whose specific outcome is the progression of the uterus over time, from its formation to the mature structure. [GOC:dph, GOC:ebc] |
| branching involved in mammary gland duct morphogenesis | biological process | The process in which the branching structure of the mammary gland duct is generated and organized. The mammary gland is a large compound sebaceous gland that in female mammals is modified to secrete milk. [GOC:dph] |
| regulation of cell projection assembly | biological process | Any process that modulates the rate, frequency, or extent of cell projection assembly. [GOC:dph, GOC:tb] |
| intestinal epithelial cell development | biological process | The process whose specific outcome is the progression of a columnar/cuboidal epithelial cell of the intestine over time, from its formation to the mature structure. [GOC:dph] |
| interleukin-6-mediated signaling pathway | biological process | The series of molecular signals initiated by interleukin-6 binding to a receptor on the surface of a target cell, and ending with the regulation of a downstream cellular process, e.g. transcription. [GOC:add, GOC:BHF, GOC:mah, GOC:signaling] |
| cellular response to hydrogen peroxide | biological process | Any process that results in a change in state or activity of a cell (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a hydrogen peroxide (H2O2) stimulus. [CHEBI:16240, GOC:mah] |
| 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] |
| response to interleukin-1 | 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 an interleukin-1 stimulus. [GOC:BHF, GOC:mah] |
| cellular response to lipopolysaccharide | 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 lipopolysaccharide stimulus; lipopolysaccharide is a major component of the cell wall of gram-negative bacteria. [GOC:mah] |
| cellular response to peptide hormone 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 peptide hormone stimulus. A peptide hormone is any of a class of peptides that are secreted into the blood stream and have endocrine functions in living animals. [GOC:mah] |
| cellular response to progesterone 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 progesterone stimulus. [GOC:mah] |
| cellular response to fatty acid | 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 fatty acid stimulus. [GOC:mah] |
| cellular response to hypoxia | 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 indicating lowered oxygen tension. Hypoxia, defined as a decline in O2 levels below normoxic levels of 20.8 - 20.95%, results in metabolic adaptation at both the cellular and organismal level. [GOC:mah] |
| cellular response to fluid shear stress | 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 fluid shear stress stimulus. Fluid shear stress is the force acting on an object in a system where the fluid is moving across a solid surface. [GOC:mah] |
| positive regulation of podosome assembly | biological process | Any process that activates or increases the rate or extent of podosome assembly. [GOC:mah, GOC:sl] |
| DNA biosynthetic process | biological process | The biosynthetic process resulting in the formation of DNA. [GOC:mah] |
| positive regulation of protein serine/threonine kinase activity | biological process | Any process that increases the rate, frequency, or extent of protein serine/threonine kinase activity. [GOC:mah] |
| regulation of heart rate by cardiac conduction | biological process | A cardiac conduction process that modulates the frequency or rate of heart contraction. [GOC:BHF, GOC:mtg_cardiac_conduct_nov11] |
| 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] |
| cell-cell adhesion | biological process | The attachment of one cell to another cell via adhesion molecules. [GOC:dos] |
| positive regulation of protein localization to nucleus | biological process | Any process that activates or increases the frequency, rate or extent of protein localization to nucleus. [GOC:TermGenie] |
| positive regulation of non-membrane spanning protein tyrosine kinase activity | biological process | Any process that activates or increases the frequency, rate or extent of non-membrane spanning protein tyrosine kinase activity. [GO_REF:0000059, GOC:BHF, GOC:nc, GOC:TermGenie, PMID:10518561] |
| positive regulation of TORC1 signaling | biological process | Any process that activates or increases the frequency, rate or extent of TORC1 signaling. [GO_REF:0000058, GOC:TermGenie, PMID:25366275] |
| positive regulation of vascular associated smooth muscle cell proliferation | biological process | Any process that activates or increases the frequency, rate or extent of vascular smooth muscle cell proliferation. [GO_REF:0000058, GOC:TermGenie, PMID:23246467] |
| cellular response to prolactin | 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 prolactin stimulus. [PMID:7760850] |
| positive regulation of male germ cell proliferation | biological process | Any process that activates or increases the frequency, rate or extent of male germ cell proliferation. [GOC:obol] |
| positive regulation of ovarian follicle development | biological process | Any process that activates or increases the frequency, rate or extent of ovarian follicle development. [GOC:obol] |
| positive regulation of lamellipodium morphogenesis | biological process | Any process that activates or increases the frequency, rate or extent of lamellipodium morphogenesis. [GOC:BHF, GOC:mah] |
| positive regulation of platelet-derived growth factor receptor-beta signaling pathway | biological process | Any process that activates or increases the frequency, rate or extent of platelet-derived growth factor receptor-beta signaling pathway. [GOC:obol] |
| regulation of early endosome to late endosome transport | biological process | Any process that modulates the frequency, rate or extent of early endosome to late endosome transport. [GOC:BHF] |
| negative regulation of anoikis | biological process | Any process that stops, prevents or reduces the frequency, rate or extent of anoikis. [GOC:obol] |
| negative regulation of extrinsic apoptotic signaling pathway | biological process | Any process that stops, prevents or reduces the frequency, rate or extent of extrinsic apoptotic signaling pathway. [GOC:mtg_apoptosis] |
| negative regulation of intrinsic apoptotic signaling pathway | biological process | Any process that stops, prevents or reduces the frequency, rate or extent of intrinsic apoptotic signaling pathway. [GOC:mtg_apoptosis] |
| regulation of caveolin-mediated endocytosis | biological process | Any process that modulates the frequency, rate or extent of caveolin-mediated endocytosis. [GOC:obol] |
| cell differentiation | biological process | The cellular developmental process in which a relatively unspecialized cell, e.g. embryonic or regenerative cell, acquires specialized structural and/or functional features that characterize a specific cell. Differentiation includes the processes involved in commitment of a cell to a specific fate and its subsequent development to the mature state. [ISBN:0198506732] |
| cell adhesion | biological process | The attachment of a cell, either to another cell or to an underlying substrate such as the extracellular matrix, via cell adhesion molecules. [GOC:hb, GOC:pf] |
| innate immune response | biological process | Innate immune responses are defense responses mediated by germline encoded components that directly recognize components of potential pathogens. [GO_REF:0000022, GOC:add, GOC:ebc, GOC:mtg_sensu] |
| protein phosphorylation | biological process | The process of introducing a phosphate group on to a protein. [GOC:hb] |