Proteins > Glycogen synthase kinase-3 beta
Page last updated: 2024-08-07 16:46:38
Glycogen synthase kinase-3 beta
A glycogen synthase kinase-3 beta that is encoded in the genome of human. [PRO:DNx, UniProtKB:P49841]
Synonyms
GSK-3 beta;
EC 2.7.11.26;
Serine/threonine-protein kinase GSK3B;
2.7.11.1
Research
Bioassay Publications (195)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 1 (0.51) | 18.2507 |
| 2000's | 68 (34.87) | 29.6817 |
| 2010's | 99 (50.77) | 24.3611 |
| 2020's | 27 (13.85) | 2.80 |
Compounds (344)
Drugs with Inhibition Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| tacrine | Homo sapiens (human) | IC50 | 34.0000 | 3 | 3 |
| bisindolylmaleimide i | Homo sapiens (human) | IC50 | 0.1900 | 1 | 1 |
| donepezil | Homo sapiens (human) | IC50 | 37.0000 | 3 | 3 |
| indirubin-3'-monoxime | Homo sapiens (human) | IC50 | 0.0599 | 10 | 10 |
| nsc 664704 | Homo sapiens (human) | IC50 | 0.0657 | 9 | 9 |
| 2-(4-morpholinyl)-8-phenyl-4h-1-benzopyran-4-one | Homo sapiens (human) | IC50 | 8.1000 | 1 | 1 |
| niclosamide | Homo sapiens (human) | IC50 | 77.5000 | 1 | 1 |
| nu6102 | Homo sapiens (human) | IC50 | 0.0400 | 1 | 1 |
| ro 31-8220 | Homo sapiens (human) | IC50 | 0.0116 | 3 | 4 |
| imatinib | Homo sapiens (human) | IC50 | 50.0000 | 1 | 1 |
| 2,4-thiazolidinedione | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
| phenacyl bromide | Homo sapiens (human) | IC50 | 5.0000 | 3 | 3 |
| phthalimide | Homo sapiens (human) | IC50 | 20.2200 | 1 | 1 |
| ethyl benzoate | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
| thiophene-2-carboxaldehyde | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
| acetophenone | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
| 4-bromophenacyl bromide | Homo sapiens (human) | IC50 | 0.5000 | 3 | 3 |
| 4-chloroacetophenone | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
| maleic anhydride | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
| hydantoins | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
| indirubin | Homo sapiens (human) | IC50 | 0.8515 | 6 | 6 |
| indigo | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
| maleimide | Homo sapiens (human) | IC50 | 6.0000 | 1 | 1 |
| succinimide | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
| staurosporine | Homo sapiens (human) | IC50 | 0.0435 | 40 | 40 |
| staurosporine | Homo sapiens (human) | Ki | 0.0220 | 1 | 1 |
| 2-bromo-4'-nitroacetophenone | Homo sapiens (human) | IC50 | 2.0000 | 3 | 3 |
| 4-cyclopentene-1,3-dione | Homo sapiens (human) | IC50 | 12.0000 | 1 | 1 |
| n-methylmaleimide | Homo sapiens (human) | IC50 | 5.0000 | 1 | 1 |
| n-benzylmaleimide | Homo sapiens (human) | IC50 | 1.0000 | 1 | 1 |
| 5-iodotubercidin | Homo sapiens (human) | IC50 | 50.0000 | 1 | 1 |
| homoorientin | Homo sapiens (human) | IC50 | 185.0000 | 1 | 1 |
| ro 32-0432 | Homo sapiens (human) | IC50 | 0.0200 | 1 | 1 |
| birb 796 | Homo sapiens (human) | IC50 | 26.2650 | 3 | 4 |
| schizandrin b | Homo sapiens (human) | IC50 | 0.0730 | 1 | 1 |
| cyc 202 | Homo sapiens (human) | IC50 | 106.6667 | 3 | 3 |
| rubschisandrin | Homo sapiens (human) | IC50 | 0.0810 | 1 | 1 |
| sb 216763 | Homo sapiens (human) | IC50 | 0.0342 | 18 | 18 |
| sorafenib | Homo sapiens (human) | IC50 | 12.4875 | 3 | 4 |
| paullone | Homo sapiens (human) | IC50 | 0.3359 | 4 | 4 |
| meridianin g | Homo sapiens (human) | IC50 | 238.2700 | 3 | 3 |
| 5-iodoindirubin-3'-monoxime | Homo sapiens (human) | IC50 | 0.0090 | 4 | 4 |
| lithium chloride | Homo sapiens (human) | IC50 | 6.5300 | 1 | 1 |
| 2H-pyrazolo[4,3-b]quinoxalin-3-amine | Homo sapiens (human) | IC50 | 1.0000 | 2 | 2 |
| n-(4-methoxybenzyl)-n'-(5-nitro-1,3-thiazol-2-yl)urea | Homo sapiens (human) | IC50 | 23.6893 | 14 | 14 |
| n-(4-methoxybenzyl)-n'-(5-nitro-1,3-thiazol-2-yl)urea | Homo sapiens (human) | Ki | 0.2820 | 3 | 3 |
| 7-n-butyl-6-(4'-hydroxyphenyl)-5h-pyrrolo(2,3b)pyrazine | Homo sapiens (human) | IC50 | 0.9326 | 6 | 6 |
| 6-bromoindirubin-3'-oxime | Homo sapiens (human) | IC50 | 0.3298 | 6 | 6 |
| purvalanol b | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| repsox | Homo sapiens (human) | IC50 | 16.0000 | 1 | 1 |
| h 89 | Homo sapiens (human) | IC50 | 15.0000 | 1 | 1 |
| purvalanol a | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| N-(3-cyano-4,5,6,7-tetrahydro-1-benzothiophen-2-yl)-1-naphthalenecarboxamide | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| curcumin | Homo sapiens (human) | IC50 | 17.9500 | 1 | 1 |
| rhodanine | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
| 4-hydroxyphenylmethylene hydantoin | Homo sapiens (human) | IC50 | 13.7000 | 1 | 1 |
| 7-butyl-6-(4-methoxyphenyl)-5H-pyrrolo[2,3-b]pyrazine | Homo sapiens (human) | IC50 | 0.9160 | 2 | 2 |
| 4-benzyl-2-methyl-1,2,4-thiadiazolidine-3,5-dione | Homo sapiens (human) | IC50 | 9.0564 | 14 | 14 |
| sb 415286 | Homo sapiens (human) | IC50 | 0.1108 | 9 | 9 |
| sb 415286 | Homo sapiens (human) | Ki | 0.0240 | 1 | 1 |
| alsterpaullone | Homo sapiens (human) | IC50 | 0.0105 | 12 | 14 |
| quercetin | Homo sapiens (human) | IC50 | 2.1000 | 1 | 1 |
| apigenin | Homo sapiens (human) | IC50 | 1.4000 | 1 | 1 |
| luteolin | Homo sapiens (human) | IC50 | 0.8000 | 1 | 1 |
| kaempferol | Homo sapiens (human) | IC50 | 3.5000 | 1 | 1 |
| harmine | Homo sapiens (human) | IC50 | 24.0333 | 6 | 6 |
| sulfuretin | Homo sapiens (human) | IC50 | 1.9500 | 1 | 1 |
| chrysin | Homo sapiens (human) | IC50 | 7.2000 | 1 | 1 |
| fisetin | Homo sapiens (human) | IC50 | 0.4200 | 1 | 1 |
| ellagic acid | Homo sapiens (human) | IC50 | 7.5000 | 1 | 1 |
| alvocidib | Homo sapiens (human) | IC50 | 0.6517 | 3 | 3 |
| su 9516 | Homo sapiens (human) | IC50 | 0.3500 | 1 | 1 |
| jnj-7706621 | Homo sapiens (human) | IC50 | 0.0410 | 1 | 1 |
| GSK3-XIII | Homo sapiens (human) | Ki | 0.0227 | 3 | 3 |
| cyc 116 | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| manzamine a | Homo sapiens (human) | IC50 | 10.2167 | 6 | 6 |
| 1-azakenpaullone | Homo sapiens (human) | IC50 | 0.0180 | 3 | 3 |
| 2-[(3-iodophenyl)methylthio]-5-pyridin-4-yl-1,3,4-oxadiazole | Homo sapiens (human) | IC50 | 1.7250 | 6 | 6 |
| tws 119 | Homo sapiens (human) | IC50 | 0.0300 | 3 | 3 |
| jnj 10198409 | Homo sapiens (human) | IC50 | 13.0000 | 1 | 1 |
| cp 547632 | Homo sapiens (human) | IC50 | 0.0715 | 1 | 2 |
| 6-methylsulfinylhexyl isothiocyanate | Homo sapiens (human) | IC50 | 70.0000 | 1 | 1 |
| tofacitinib | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| hypothemycin | Homo sapiens (human) | IC50 | 5.9815 | 2 | 2 |
| chir 99021 | Homo sapiens (human) | IC50 | 0.0133 | 7 | 7 |
| ly2090314 | Homo sapiens (human) | IC50 | 0.0010 | 6 | 6 |
| leucettamine b | Homo sapiens (human) | IC50 | 12.5000 | 2 | 2 |
| azd2858 | Homo sapiens (human) | IC50 | 0.0050 | 1 | 1 |
| azd2858 | Homo sapiens (human) | Ki | 0.0049 | 1 | 1 |
| 9-hydroxycanthin-6-one | Homo sapiens (human) | IC50 | 6.8000 | 1 | 1 |
| pik 75 | Homo sapiens (human) | IC50 | 0.0090 | 1 | 2 |
| sotrastaurin | Homo sapiens (human) | IC50 | 0.8700 | 1 | 1 |
| saracatinib | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| meridianin a | Homo sapiens (human) | IC50 | 1.3000 | 2 | 2 |
| pha 665752 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| l 783277 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| np 031112 | Homo sapiens (human) | IC50 | 1.5373 | 10 | 10 |
| at 7519 | Homo sapiens (human) | IC50 | 0.2000 | 1 | 1 |
| danusertib | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| N-[5-[[5-[(4-acetyl-1-piperazinyl)-oxomethyl]-4-methoxy-2-methylphenyl]thio]-2-thiazolyl]-4-[(3,3-dimethylbutan-2-ylamino)methyl]benzamide | Homo sapiens (human) | IC50 | 36.0000 | 1 | 1 |
| nvp-aew541 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| pf 573228 | Homo sapiens (human) | IC50 | 1.0000 | 2 | 2 |
| gw 2580 | Homo sapiens (human) | IC50 | 32.0000 | 1 | 1 |
| tak 285 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| 5-(5,6-dimethoxy-1-benzimidazolyl)-3-[(2-methylsulfonylphenyl)methoxy]-2-thiophenecarbonitrile | Homo sapiens (human) | IC50 | 15.8489 | 1 | 1 |
| 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 | 0.4472 | 1 | 4 |
| pha 767491 | Homo sapiens (human) | IC50 | 0.2200 | 1 | 1 |
| sesone | Homo sapiens (human) | IC50 | 0.7000 | 1 | 1 |
| pha 848125 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| gsk690693 | Homo sapiens (human) | IC50 | 0.1380 | 1 | 1 |
| cct 128930 | Homo sapiens (human) | IC50 | 1.8300 | 2 | 2 |
| bms 777607 | Homo sapiens (human) | IC50 | 2.0000 | 1 | 1 |
| ponatinib | Homo sapiens (human) | IC50 | 7.5500 | 1 | 2 |
| bi d1870 | Homo sapiens (human) | IC50 | 0.5628 | 1 | 10 |
| defactinib | Homo sapiens (human) | IC50 | 0.4160 | 1 | 0 |
| entrectinib | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| (1-(4-(naphthalen-2-yl)pyrimidin-2-yl)piperidin-4-yl)methanamine | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
| 3-(4-fluorophenylethylamino)-1-methyl-4-(2-methyl-1h-indol-3-yl)-1h-pyrrole-2,5-dione | Homo sapiens (human) | IC50 | 0.0530 | 1 | 1 |
| manzamine e | Homo sapiens (human) | IC50 | 25.0000 | 1 | 1 |
| pha 793887 | Homo sapiens (human) | IC50 | 0.0790 | 1 | 1 |
| tak-632 | Homo sapiens (human) | IC50 | 0.5000 | 1 | 1 |
| gsk 2334470 | Homo sapiens (human) | IC50 | 25.1180 | 1 | 1 |
| dinaciclib | Homo sapiens (human) | IC50 | 0.3240 | 1 | 1 |
| nms p937 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| nms-p118 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| chir 98014 | Homo sapiens (human) | IC50 | 0.0031 | 2 | 3 |
| palinurin | Homo sapiens (human) | IC50 | 2.9960 | 3 | 6 |
| urmc-099 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| ceritinib | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| vx-970 | Homo sapiens (human) | Ki | 0.1400 | 1 | 1 |
| vx-787 | Homo sapiens (human) | Ki | 1.6000 | 2 | 2 |
| chr-6494 | Homo sapiens (human) | IC50 | 0.0530 | 1 | 1 |
| CCT251545 | Homo sapiens (human) | IC50 | 0.6900 | 1 | 1 |
| CCT251545 | Homo sapiens (human) | Ki | 0.3450 | 1 | 1 |
| at 9283 | Homo sapiens (human) | IC50 | 0.0010 | 1 | 1 |
| ((5z)5-(1,3-benzodioxol-5-yl)methylene-2-phenylamino-3,5-dihydro-4h-imidazol-4-one) | Homo sapiens (human) | IC50 | 0.3800 | 1 | 1 |
| ro 3306 | Homo sapiens (human) | Ki | 0.5000 | 1 | 1 |
| hymenialdisine | Homo sapiens (human) | IC50 | 0.0267 | 7 | 9 |
| isogranulatimide | Homo sapiens (human) | IC50 | 0.5000 | 1 | 1 |
| 7-bromoindirubin-3'-oxime | Homo sapiens (human) | IC50 | 32.0000 | 1 | 1 |
| debromohymenialdisine | Homo sapiens (human) | IC50 | 6.1136 | 2 | 10 |
| 2-hydroxy-3-(5-((morpholin-4-yl)methyl)pyridin-2-yl)-1h-indole-5-carbonitrile | Homo sapiens (human) | IC50 | 0.0310 | 1 | 1 |
| 2-hydroxy-3-(5-((morpholin-4-yl)methyl)pyridin-2-yl)-1h-indole-5-carbonitrile | Homo sapiens (human) | Ki | 0.0310 | 1 | 1 |
| nms-e973 | Homo sapiens (human) | IC50 | 0.0100 | 1 | 1 |
Drugs with Activation Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| fasudil | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| 4-(4'-hydroxyphenyl)-amino-6,7-dimethoxyquinazoline | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| sb 202190 | Homo sapiens (human) | Kd | 2.7000 | 1 | 1 |
| imatinib | Homo sapiens (human) | Kd | 16.6667 | 3 | 3 |
| triciribine phosphate | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| staurosporine | Homo sapiens (human) | Kd | 0.0690 | 2 | 2 |
| picropodophyllin | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| gefitinib | Homo sapiens (human) | Kd | 16.6667 | 3 | 3 |
| lestaurtinib | Homo sapiens (human) | Kd | 13.7667 | 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 | 3.4210 | 3 | 3 |
| canertinib | Homo sapiens (human) | Kd | 16.6667 | 3 | 3 |
| 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 | 1.7000 | 2 | 2 |
| sb 216763 | Homo sapiens (human) | EC50 | 0.2000 | 1 | 1 |
| enzastaurin | Homo sapiens (human) | Kd | 0.0689 | 3 | 2 |
| erlotinib | Homo sapiens (human) | Kd | 16.6667 | 3 | 3 |
| lapatinib | Homo sapiens (human) | Kd | 16.6667 | 3 | 3 |
| sorafenib | Homo sapiens (human) | Kd | 15.0000 | 4 | 4 |
| lithium chloride | Homo sapiens (human) | EC50 | 3,000.0000 | 1 | 1 |
| pd 173955 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| s 1033 | Homo sapiens (human) | Kd | 20.0000 | 2 | 2 |
| xl147 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| bms 387032 | Homo sapiens (human) | Kd | 0.1243 | 3 | 3 |
| sf 2370 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| tandutinib | Homo sapiens (human) | Kd | 15.0000 | 4 | 4 |
| vx-745 | Homo sapiens (human) | Kd | 10.0000 | 2 | 2 |
| dasatinib | Homo sapiens (human) | Kd | 16.6667 | 3 | 3 |
| ha 1100 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| 7-epi-hydroxystaurosporine | Homo sapiens (human) | Kd | 30.0000 | 1 | 2 |
| zd 6474 | Homo sapiens (human) | Kd | 16.6667 | 3 | 3 |
| sb 415286 | Homo sapiens (human) | EC50 | 38.1100 | 2 | 2 |
| 4-(5-benzo(1,3)dioxol-5-yl-4-pyridin-2-yl-1h-imidazol-2-yl)benzamide | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| imd 0354 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| sirolimus | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| alvocidib | Homo sapiens (human) | Kd | 0.7333 | 3 | 3 |
| bosutinib | Homo sapiens (human) | Kd | 20.0000 | 2 | 2 |
| orantinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| su 11248 | Homo sapiens (human) | Kd | 15.0000 | 4 | 4 |
| palbociclib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| jnj-7706621 | Homo sapiens (human) | Kd | 0.9500 | 1 | 1 |
| vx680 | Homo sapiens (human) | Kd | 16.6667 | 3 | 3 |
| cyc 116 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| everolimus | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| ekb 569 | Homo sapiens (human) | Kd | 20.0000 | 2 | 2 |
| 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 | 0.9240 | 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 | 2 |
| midostaurin | Homo sapiens (human) | Kd | 8.8500 | 4 | 4 |
| px-866 | Homo sapiens (human) | Kd | 30.0000 | 1 | 2 |
| ripasudil | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| osi 930 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| ki 20227 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| scio-469 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| cp 724714 | Homo sapiens (human) | Kd | 23.3333 | 2 | 3 |
| 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 | 20.0000 | 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 | 20.0000 | 2 | 2 |
| chir 99021 | Homo sapiens (human) | EC50 | 1.5000 | 1 | 1 |
| masitinib | Homo sapiens (human) | Kd | 20.0000 | 2 | 2 |
| ly-2157299 | Homo sapiens (human) | Kd | 30.0000 | 1 | 2 |
| pazopanib | Homo sapiens (human) | Kd | 16.6667 | 3 | 3 |
| azd 6244 | Homo sapiens (human) | Kd | 23.3333 | 2 | 3 |
| su 14813 | Homo sapiens (human) | Kd | 16.6667 | 3 | 3 |
| bibw 2992 | Homo sapiens (human) | Kd | 20.0000 | 2 | 2 |
| binimetinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| sotrastaurin | Homo sapiens (human) | Kd | 0.7090 | 1 | 1 |
| aee 788 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| saracatinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| vx 702 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| crenolanib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| tg100-115 | Homo sapiens (human) | Kd | 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 | 30.0000 | 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 | 30.0000 | 1 | 1 |
| regorafenib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| 6-[[5-fluoro-2-(3,4,5-trimethoxyanilino)-4-pyrimidinyl]amino]-2,2-dimethyl-4H-pyrido[3,2-b][1,4]oxazin-3-one | Homo sapiens (human) | Kd | 20.0400 | 2 | 3 |
| brivanib | Homo sapiens (human) | Kd | 20.0000 | 2 | 2 |
| mp470 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| rgb 286638 | Homo sapiens (human) | Kd | 0.0080 | 1 | 1 |
| np 031112 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| at 7519 | Homo sapiens (human) | Kd | 0.0345 | 2 | 2 |
| bms-690514 | Homo sapiens (human) | Kd | 30.0000 | 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 | 10.0000 | 2 | 2 |
| kw 2449 | Homo sapiens (human) | Kd | 20.0000 | 2 | 2 |
| danusertib | Homo sapiens (human) | Kd | 30.0000 | 1 | 2 |
| abt 869 | Homo sapiens (human) | Kd | 16.6667 | 3 | 3 |
| azd 8931 | Homo sapiens (human) | Kd | 30.0000 | 1 | 2 |
| 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 | 20.0000 | 2 | 2 |
| osi 906 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| chir-265 | Homo sapiens (human) | Kd | 16.6667 | 3 | 3 |
| motesanib | Homo sapiens (human) | Kd | 16.6667 | 3 | 3 |
| fostamatinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 2 |
| trametinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| mln8054 | Homo sapiens (human) | Kd | 16.6667 | 3 | 3 |
| pf-562,271 | Homo sapiens (human) | Kd | 0.7070 | 1 | 1 |
| 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 | 1 |
| tg100801 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| dactolisib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| bgt226 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| gsk 461364 | Homo sapiens (human) | Kd | 23.3333 | 2 | 3 |
| azd 1152-hqpa | Homo sapiens (human) | Kd | 16.6667 | 3 | 3 |
| nvp-tae684 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| enmd 2076 | Homo sapiens (human) | Kd | 30.0000 | 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 | 6.1680 | 1 | 1 |
| gdc-0973 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| buparlisib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| azd 1480 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| azd8330 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| pha 848125 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| ro5126766 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| fedratinib | Homo sapiens (human) | Kd | 20.0000 | 2 | 2 |
| gsk690693 | Homo sapiens (human) | Kd | 0.2640 | 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 | 0.4470 | 1 | 1 |
| azd5438 | Homo sapiens (human) | Kd | 0.0620 | 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 | 10.0000 | 1 | 1 |
| mk 5108 | Homo sapiens (human) | Kd | 30.0000 | 1 | 2 |
| cx 4945 | Homo sapiens (human) | Kd | 4.8500 | 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 | 30.0000 | 1 | 1 |
| ponatinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| amg 900 | Homo sapiens (human) | Kd | 30.0000 | 1 | 2 |
| 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 | 20.0000 | 3 | 4 |
| 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 | 30.0000 | 1 | 1 |
| cabozantinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| defactinib | Homo sapiens (human) | Kd | 1.3220 | 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 | 1 |
| gsk 2126458 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| emd1214063 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| gsk 1838705a | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| pf 3758309 | Homo sapiens (human) | Kd | 0.6670 | 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 | 20.0000 | 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 | 2 |
| baricitinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 2 |
| dabrafenib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| pki 587 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| n-(3-fluoro-4-((1-methyl-6-(1h-pyrazol-4-yl)-1h-indazol-5 yl)oxy)phenyl)-1-(4-fluorophenyl)-6-methyl-2-oxo-1,2-dihydropyridine-3-carboxamide | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| 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 | 0.0120 | 1 | 1 |
| sb 1518 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| abemaciclib | Homo sapiens (human) | Kd | 0.0130 | 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 | 1.4300 | 1 | 1 |
| gilteritinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| alectinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| glpg0634 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| encorafenib | Homo sapiens (human) | Kd | 0.4250 | 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 | 2 |
| 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 | 0.0070 | 1 | 1 |
| otssp167 | Homo sapiens (human) | Kd | 0.0800 | 1 | 1 |
| chir 258 | Homo sapiens (human) | Kd | 10.2333 | 3 | 3 |
| osi 027 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| nintedanib | Homo sapiens (human) | Kd | 15.0415 | 2 | 2 |
| bay 80-6946 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| pp242 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
[no title available]Journal of medicinal chemistry, , 06-10, Volume: 64, Issue:11, 2021
Discovery of potent glycogen synthase kinase 3/cholinesterase inhibitors with neuroprotection as potential therapeutic agent for Alzheimer's disease.Bioorganic & medicinal chemistry, , 01-15, Volume: 30, 2021
Rational design and biological evaluation of a new class of thiazolopyridyl tetrahydroacridines as cholinesterase and GSK-3 dual inhibitors for Alzheimer's disease.European journal of medicinal chemistry, , Dec-01, Volume: 207, 2020
[no title available]Journal of medicinal chemistry, , 06-10, Volume: 64, Issue:11, 2021
Discovery of potent glycogen synthase kinase 3/cholinesterase inhibitors with neuroprotection as potential therapeutic agent for Alzheimer's disease.Bioorganic & medicinal chemistry, , 01-15, Volume: 30, 2021
Discovery of 2-(cyclopropanecarboxamido)-N-(5-((1-(4-fluorobenzyl)piperidin-4-yl)methoxy)pyridin-3-yl)isonicotinamide as a potent dual AChE/GSK3β inhibitor for the treatment of Alzheimer's disease: Significantly increasing the level of acetylcholine in thEuropean journal of medicinal chemistry, , Nov-05, Volume: 223, 2021
Discovery of thiazolidin-4-one analogue as selective GSK-3β inhibitor through structure based virtual screening.Bioorganic & medicinal chemistry letters, , 11-15, Volume: 52, 2021
Anticancer potential of indirubins in medicinal chemistry: Biological activity, structural modification, and structure-activity relationship.European journal of medicinal chemistry, , Nov-05, Volume: 223, 2021
Synthesis, Binding Mode, and Antihyperglycemic Activity of Potent and Selective (5-Imidazol-2-yl-4-phenylpyrimidin-2-yl)[2-(2-pyridylamino)ethyl]amine Inhibitors of Glycogen Synthase Kinase 3.Journal of medicinal chemistry, , 10-26, Volume: 60, Issue:20, 2017
Fragment and knowledge-based design of selective GSK-3beta inhibitors using virtual screening models.European journal of medicinal chemistry, , Volume: 44, Issue:6, 2009
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
3'-Substituted 7-halogenoindirubins, a new class of cell death inducing agents.Journal of medicinal chemistry, , Jul-27, Volume: 49, Issue:15, 2006
Mechanism of CDK5/p25 binding by CDK inhibitors.Journal of medicinal chemistry, , Feb-10, Volume: 48, Issue:3, 2005
Structural basis for the synthesis of indirubins as potent and selective inhibitors of glycogen synthase kinase-3 and cyclin-dependent kinases.Journal of medicinal chemistry, , Feb-12, Volume: 47, Issue:4, 2004
Pharmacological inhibitors of glycogen synthase kinase 3.Trends in pharmacological sciences, , Volume: 25, Issue:9, 2004
PROTACs suppression of GSK-3β, a crucial kinase in neurodegenerative diseases.European journal of medicinal chemistry, , Jan-15, Volume: 210, 2021
Synthesis, Binding Mode, and Antihyperglycemic Activity of Potent and Selective (5-Imidazol-2-yl-4-phenylpyrimidin-2-yl)[2-(2-pyridylamino)ethyl]amine Inhibitors of Glycogen Synthase Kinase 3.Journal of medicinal chemistry, , 10-26, Volume: 60, Issue:20, 2017
Discovery of 1,3,4-oxidiazole scaffold compounds as inhibitors of superoxide dismutase expression.Bioorganic & medicinal chemistry letters, , Mar-15, Volume: 24, Issue:6, 2014
Development of 5-benzylpaullones and paullone-9-carboxylic acid alkyl esters as selective inhibitors of mitochondrial malate dehydrogenase (mMDH).European journal of medicinal chemistry, , Volume: 45, Issue:1, 2010
9-cyano-1-azapaullone (cazpaullone), a glycogen synthase kinase-3 (GSK-3) inhibitor activating pancreatic beta cell protection and replication.Journal of medicinal chemistry, , Apr-10, Volume: 51, Issue:7, 2008
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
1-Azakenpaullone is a selective inhibitor of glycogen synthase kinase-3 beta.Bioorganic & medicinal chemistry letters, , Jan-19, Volume: 14, Issue:2, 2004
Evaluation and comparison of 3D-QSAR CoMSIA models for CDK1, CDK5, and GSK-3 inhibition by paullones.Journal of medicinal chemistry, , Jan-01, Volume: 47, Issue:1, 2004
Pharmacological inhibitors of glycogen synthase kinase 3.Trends in pharmacological sciences, , Volume: 25, Issue:9, 2004
Fragment and knowledge-based design of selective GSK-3beta inhibitors using virtual screening models.European journal of medicinal chemistry, , Volume: 44, Issue:6, 2009
Pharmacological inhibitors of glycogen synthase kinase 3.Trends in pharmacological sciences, , Volume: 25, Issue:9, 2004
Specificity and mechanism of action of some commonly used protein kinase inhibitors.The Biochemical journal, , Oct-01, Volume: 351, Issue:Pt 1, 2000
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Targeting GSK3 from Ustilago maydis: type-II kinase inhibitors as potential antifungals.ACS chemical biology, , Jul-20, Volume: 7, Issue:7, 2012
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
Pivotal role of glycogen synthase kinase-3: A therapeutic target for Alzheimer's disease.European journal of medicinal chemistry, , Jan-01, Volume: 107, 2016
Switching reversibility to irreversibility in glycogen synthase kinase 3 inhibitors: clues for specific design of new compounds.Journal of medicinal chemistry, , Jun-23, Volume: 54, Issue:12, 2011
Thienyl and phenyl alpha-halomethyl ketones: new inhibitors of glycogen synthase kinase (GSK-3beta) from a library of compound searching.Journal of medicinal chemistry, , Oct-23, Volume: 46, Issue:22, 2003
Pivotal role of glycogen synthase kinase-3: A therapeutic target for Alzheimer's disease.European journal of medicinal chemistry, , Jan-01, Volume: 107, 2016
Switching reversibility to irreversibility in glycogen synthase kinase 3 inhibitors: clues for specific design of new compounds.Journal of medicinal chemistry, , Jun-23, Volume: 54, Issue:12, 2011
Thienyl and phenyl alpha-halomethyl ketones: new inhibitors of glycogen synthase kinase (GSK-3beta) from a library of compound searching.Journal of medicinal chemistry, , Oct-23, Volume: 46, Issue:22, 2003
Identification of a Water-Soluble Indirubin Derivative as Potent Inhibitor of Insulin-like Growth Factor 1 Receptor through Structural Modification of the Parent Natural Molecule.Journal of medicinal chemistry, , 06-22, Volume: 60, Issue:12, 2017
Natural and synthetic bioactive inhibitors of glycogen synthase kinase.European journal of medicinal chemistry, , Jan-05, Volume: 125, 2017
Pivotal role of glycogen synthase kinase-3: A therapeutic target for Alzheimer's disease.European journal of medicinal chemistry, , Jan-01, Volume: 107, 2016
3'-Substituted 7-halogenoindirubins, a new class of cell death inducing agents.Journal of medicinal chemistry, , Jul-27, Volume: 49, Issue:15, 2006
Structural basis for the synthesis of indirubins as potent and selective inhibitors of glycogen synthase kinase-3 and cyclin-dependent kinases.Journal of medicinal chemistry, , Feb-12, Volume: 47, Issue:4, 2004
Generation of new protein kinase inhibitors utilizing cytochrome p450 mutant enzymes for indigoid synthesis.Journal of medicinal chemistry, , Jun-03, Volume: 47, Issue:12, 2004
Discovery of novel β-carboline derivatives as selective AChE inhibitors with GSK-3β inhibitory property for the treatment of Alzheimer's disease.European journal of medicinal chemistry, , Feb-05, Volume: 229, 2022
Discovery of a Potent Dual SLK/STK10 Inhibitor Based on a Maleimide Scaffold.Journal of medicinal chemistry, , 09-23, Volume: 64, Issue:18, 2021
Design, synthesis and biological evaluation of harmine derivatives as potent GSK-3β/DYRK1A dual inhibitors for the treatment of Alzheimer's disease.European journal of medicinal chemistry, , Oct-15, Volume: 222, 2021
Discovery of a 2-pyridinyl urea-containing compound YD57 as a potent inhibitor of apoptosis signal-regulating kinase 1 (ASK1).European journal of medicinal chemistry, , Jun-01, Volume: 195, 2020
Optimization of Indazole-Based GSK-3 Inhibitors with Mitigated hERG Issue and ACS medicinal chemistry letters, , May-14, Volume: 11, Issue:5, 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
Structure-activity relationship (SAR) studies of synthetic glycogen synthase kinase-3β inhibitors: A critical review.European journal of medicinal chemistry, , Feb-15, Volume: 164, 2019
Synthesis and evaluation of novel GSK-3β inhibitors as multifunctional agents against Alzheimer's disease.European journal of medicinal chemistry, , Apr-01, Volume: 167, 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
Discovery of new GSK-3β inhibitors through structure-based virtual screening.Bioorganic & medicinal chemistry letters, , 01-15, Volume: 28, Issue:2, 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
Benzisoxazole: a privileged scaffold for medicinal chemistry.MedChemComm, , Nov-01, Volume: 8, Issue:11, 2017
Novel LCK/FMS inhibitors based on phenoxypyrimidine scaffold as potential treatment for inflammatory disorders.European journal of medicinal chemistry, , Dec-01, Volume: 141, 2017
Synthesis of Novel Oxazolo[4,5-b]pyridine-2-one based 1,2,3-triazoles as Glycogen Synthase Kinase-3β Inhibitors with Anti-inflammatory Potential.Chemical biology & drug design, , Volume: 87, Issue:6, 2016
Pivotal role of glycogen synthase kinase-3: A therapeutic target for Alzheimer's disease.European journal of medicinal chemistry, , Jan-01, Volume: 107, 2016
Application of Fragment-Based de Novo Design to the Discovery of Selective Picomolar Inhibitors of Glycogen Synthase Kinase-3 Beta.Journal of medicinal chemistry, , 10-13, Volume: 59, Issue:19, 2016
Design, synthesis and biological evaluation of pyrazol-furan carboxamide analogues as novel Akt kinase inhibitors.European journal of medicinal chemistry, , Jul-19, Volume: 117, 2016
Synthesis of benzimidazole based thiadiazole and carbohydrazide conjugates as glycogen synthase kinase-3β inhibitors with anti-depressant activity.Bioorganic & medicinal chemistry letters, , 08-15, Volume: 26, Issue:16, 2016
Synthesis and biological evaluation of new [1,2,4]triazolo[4,3-a]pyridine derivatives as potential c-Met inhibitors.Bioorganic & medicinal chemistry, , 08-15, Volume: 24, Issue:16, 2016
Synthesis of pyrimidin-4-one-1,2,3-triazole conjugates as glycogen synthase kinase-3β inhibitors with anti-depressant activity.Bioorganic chemistry, , Volume: 68, 2016
Synthesis and biological evaluation of 3-([1,2,4]triazolo[4,3-a]pyridin-3-yl)-4-(indol-3-yl)-maleimides as potent, selective GSK-3β inhibitors and neuroprotective agents.Bioorganic & medicinal chemistry, , Mar-01, Volume: 23, Issue:5, 2015
Discovery of 4-arylamido 3-methyl isoxazole derivatives as novel FMS kinase inhibitors.European journal of medicinal chemistry, , Sep-18, Volume: 102, 2015
Synthesis and Evaluation of 3-(furo[2,3-b]pyridin-3-yl)-4-(1H-indol-3-yl)-maleimides as Novel GSK-3β Inhibitors and Anti-Ischemic Agents.Chemical biology & drug design, , Volume: 86, Issue:4, 2015
Syntheses, neural protective activities, and inhibition of glycogen synthase kinase-3β of substituted quinolines.Bioorganic & medicinal chemistry letters, , Aug-01, Volume: 24, Issue:15, 2014
Structure-based design, synthesis and biological evaluation of diphenylmethylamine derivatives as novel Akt1 inhibitors.European journal of medicinal chemistry, , Feb-12, Volume: 73, 2014
Indolinone based LRRK2 kinase inhibitors with a key hydrogen bond.Bioorganic & medicinal chemistry letters, , Oct-01, Volume: 24, Issue:19, 2014
Design, synthesis and evaluation of 7-azaindazolyl-indolyl-maleimides as glycogen synthase kinase-3β (GSK-3β) inhibitors.European journal of medicinal chemistry, , Volume: 68, 2013
Development of highly potent and selective diaminothiazole inhibitors of cyclin-dependent kinases.Journal of medicinal chemistry, , May-23, Volume: 56, Issue:10, 2013
Design and combinatorial synthesis of a novel kinase-focused library using click chemistry-based fragment assembly.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 22, Issue:1, 2012
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
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
3-Aryl-4-(arylhydrazono)-1H-pyrazol-5-ones: Highly ligand efficient and potent inhibitors of GSK3beta.Bioorganic & medicinal chemistry letters, , Mar-01, Volume: 20, Issue:5, 2010
Novel 8-arylated purines as inhibitors of glycogen synthase kinase.European journal of medicinal chemistry, , Volume: 45, Issue:8, 2010
Fragment and knowledge-based design of selective GSK-3beta inhibitors using virtual screening models.European journal of medicinal chemistry, , Volume: 44, Issue:6, 2009
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
Synthesis and biological evaluation of novel 4-azaindolyl-indolyl-maleimides as glycogen synthase kinase-3beta (GSK-3beta) inhibitors.Bioorganic & medicinal chemistry, , Jul-01, Volume: 17, Issue:13, 2009
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
Discovery of 2-pyrimidyl-5-amidothiophenes as potent inhibitors for AKT: synthesis and SAR studies.Bioorganic & medicinal chemistry letters, , Aug-15, Volume: 16, Issue:16, 2006
Substituted 3-imidazo[1,2-a]pyridin-3-yl- 4-(1,2,3,4-tetrahydro-[1,4]diazepino-[6,7,1-hi]indol-7-yl)pyrrole-2,5-diones as highly selective and potent inhibitors of glycogen synthase kinase-3.Journal of medicinal chemistry, , Jul-29, Volume: 47, Issue:16, 2004
Macrocyclic bisindolylmaleimides as inhibitors of protein kinase C and glycogen synthase kinase-3.Bioorganic & medicinal chemistry letters, , Sep-15, Volume: 13, Issue:18, 2003
Synthesis and in vitro characterization of 1-(4-aminofurazan-3-yl)-5-dialkylaminomethyl-1H-[1,2,3]triazole-4-carboxylic acid derivatives. A new class of selective GSK-3 inhibitors.Journal of medicinal chemistry, , Jul-17, Volume: 46, Issue:15, 2003
Pivotal role of glycogen synthase kinase-3: A therapeutic target for Alzheimer's disease.European journal of medicinal chemistry, , Jan-01, Volume: 107, 2016
Switching reversibility to irreversibility in glycogen synthase kinase 3 inhibitors: clues for specific design of new compounds.Journal of medicinal chemistry, , Jun-23, Volume: 54, Issue:12, 2011
Thienyl and phenyl alpha-halomethyl ketones: new inhibitors of glycogen synthase kinase (GSK-3beta) from a library of compound searching.Journal of medicinal chemistry, , Oct-23, Volume: 46, Issue:22, 2003
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
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
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
Structure-Based Design of Potent Selective Nanomolar Type-II Inhibitors of Glycogen Synthase Kinase-3β.Journal of medicinal chemistry, , 02-11, Volume: 64, Issue:3, 2021
Targeting GSK3 from Ustilago maydis: type-II kinase inhibitors as potential antifungals.ACS chemical biology, , Jul-20, Volume: 7, Issue:7, 2012
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
Synthesis and biological evaluation of selective and potent cyclin-dependent kinase inhibitors.European journal of medicinal chemistry, , Volume: 56, 2012
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
Novel 9-oxo-thiazolo[5,4-f]quinazoline-2-carbonitrile derivatives as dual cyclin-dependent kinase 1 (CDK1)/glycogen synthase kinase-3 (GSK-3) inhibitors: synthesis, biological evaluation and molecular modeling studies.European journal of medicinal chemistry, , Volume: 43, Issue:7, 2008
Meridianins, a new family of protein kinase inhibitors isolated from the ascidian Aplidium meridianum.Bioorganic & medicinal chemistry letters, , Apr-05, Volume: 14, Issue:7, 2004
Lessons Learned from Past Cyclin-Dependent Kinase Drug Discovery Efforts.Journal of medicinal chemistry, , 05-12, Volume: 65, Issue:9, 2022
Discovery of potent glycogen synthase kinase 3/cholinesterase inhibitors with neuroprotection as potential therapeutic agent for Alzheimer's disease.Bioorganic & medicinal chemistry, , 01-15, Volume: 30, 2021
PROTACs suppression of GSK-3β, a crucial kinase in neurodegenerative diseases.European journal of medicinal chemistry, , Jan-15, Volume: 210, 2021
Discovery of 2-(cyclopropanecarboxamido)-N-(5-((1-(4-fluorobenzyl)piperidin-4-yl)methoxy)pyridin-3-yl)isonicotinamide as a potent dual AChE/GSK3β inhibitor for the treatment of Alzheimer's disease: Significantly increasing the level of acetylcholine in thEuropean journal of medicinal chemistry, , Nov-05, Volume: 223, 2021
Rational design and biological evaluation of a new class of thiazolopyridyl tetrahydroacridines as cholinesterase and GSK-3 dual inhibitors for Alzheimer's disease.European journal of medicinal chemistry, , Dec-01, Volume: 207, 2020
Polycyclic maleimide-based derivatives as first dual modulators of neuronal calcium channels and GSK-3β for Alzheimer's disease treatment.European journal of medicinal chemistry, , Feb-01, Volume: 163, 2019
Synthesis and biological evaluation of 3-substituted 2-oxindole derivatives as new glycogen synthase kinase 3β inhibitors.Bioorganic & medicinal chemistry, , 05-01, Volume: 27, Issue:9, 2019
Pyridinylimidazoles as dual glycogen synthase kinase 3β/p38α mitogen-activated protein kinase inhibitors.European journal of medicinal chemistry, , Aug-01, Volume: 175, 2019
Tau-Centric Multitarget Approach for Alzheimer's Disease: Development of First-in-Class Dual Glycogen Synthase Kinase 3β and Tau-Aggregation Inhibitors.Journal of medicinal chemistry, , 09-13, Volume: 61, Issue:17, 2018
Natural and synthetic bioactive inhibitors of glycogen synthase kinase.European journal of medicinal chemistry, , Jan-05, Volume: 125, 2017
Discovery of 1,3,4-oxidiazole scaffold compounds as inhibitors of superoxide dismutase expression.Bioorganic & medicinal chemistry letters, , Mar-15, Volume: 24, Issue:6, 2014
Discovery of novel potent and highly selective glycogen synthase kinase-3β (GSK3β) inhibitors for Alzheimer's disease: design, synthesis, and characterization of pyrazines.Journal of medicinal chemistry, , Nov-08, Volume: 55, Issue:21, 2012
Benzo[e]isoindole-1,3-diones as potential inhibitors of glycogen synthase kinase-3 (GSK-3). Synthesis, kinase inhibitory activity, zebrafish phenotype, and modeling of binding mode.Journal of medicinal chemistry, , Feb-11, Volume: 53, Issue:3, 2010
Novel indolylmaleimide acts as GSK-3beta inhibitor in human neural progenitor cells.Bioorganic & medicinal chemistry, , Sep-15, Volume: 18, Issue:18, 2010
Fragment and knowledge-based design of selective GSK-3beta inhibitors using virtual screening models.European journal of medicinal chemistry, , Volume: 44, Issue:6, 2009
From a natural product lead to the identification of potent and selective benzofuran-3-yl-(indol-3-yl)maleimides as glycogen synthase kinase 3beta inhibitors that suppress proliferation and survival of pancreatic cancer cells.Journal of medicinal chemistry, , Apr-09, Volume: 52, Issue:7, 2009
Pharmacological inhibitors of glycogen synthase kinase 3.Trends in pharmacological sciences, , Volume: 25, Issue:9, 2004
3-(7-Azaindolyl)-4-arylmaleimides as potent, selective inhibitors of glycogen synthase kinase-3.Bioorganic & medicinal chemistry letters, , Jun-21, Volume: 14, Issue:12, 2004
Macrocyclic bisindolylmaleimides as inhibitors of protein kinase C and glycogen synthase kinase-3.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
[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
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
Structure-Based Design of Potent Selective Nanomolar Type-II Inhibitors of Glycogen Synthase Kinase-3β.Journal of medicinal chemistry, , 02-11, Volume: 64, Issue:3, 2021
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Targeting GSK3 from Ustilago maydis: type-II kinase inhibitors as potential antifungals.ACS chemical biology, , Jul-20, Volume: 7, Issue:7, 2012
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).Blood, , Oct-01, Volume: 114, Issue:14, 2009
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
Pivotal role of glycogen synthase kinase-3: A therapeutic target for Alzheimer's disease.European journal of medicinal chemistry, , Jan-01, Volume: 107, 2016
Discovery of potent and bioavailable GSK-3beta inhibitors.Bioorganic & medicinal chemistry letters, , Mar-01, Volume: 20, Issue:5, 2010
Development of 5-benzylpaullones and paullone-9-carboxylic acid alkyl esters as selective inhibitors of mitochondrial malate dehydrogenase (mMDH).European journal of medicinal chemistry, , Volume: 45, Issue:1, 2010
Evaluation and comparison of 3D-QSAR CoMSIA models for CDK1, CDK5, and GSK-3 inhibition by paullones.Journal of medicinal chemistry, , Jan-01, Volume: 47, Issue:1, 2004
Developing DYRK inhibitors derived from the meridianins as a means of increasing levels of NFAT in the nucleus.Bioorganic & medicinal chemistry letters, , 06-01, Volume: 27, Issue:11, 2017
Fragment and knowledge-based design of selective GSK-3beta inhibitors using virtual screening models.European journal of medicinal chemistry, , Volume: 44, Issue:6, 2009
Meridianins, a new family of protein kinase inhibitors isolated from the ascidian Aplidium meridianum.Bioorganic & medicinal chemistry letters, , Apr-05, Volume: 14, Issue:7, 2004
Fragment and knowledge-based design of selective GSK-3beta inhibitors using virtual screening models.European journal of medicinal chemistry, , Volume: 44, Issue:6, 2009
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
1-Azakenpaullone is a selective inhibitor of glycogen synthase kinase-3 beta.Bioorganic & medicinal chemistry letters, , Jan-19, Volume: 14, Issue:2, 2004
6-(4-Pyridyl)pyrimidin-4(3H)-ones as CNS penetrant glycogen synthase kinase-3β inhibitors.Bioorganic & medicinal chemistry letters, , Dec-15, Volume: 23, Issue:24, 2013
3-(7-Azaindolyl)-4-arylmaleimides as potent, selective inhibitors of glycogen synthase kinase-3.Bioorganic & medicinal chemistry letters, , Jun-21, Volume: 14, Issue:12, 2004
An insight into medicinal chemistry of anticancer quinoxalines.Bioorganic & medicinal chemistry, , 01-01, Volume: 27, Issue:1, 2019
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
[no title available]Journal of medicinal chemistry, , 06-10, Volume: 64, Issue:11, 2021
Optimization of Indazole-Based GSK-3 Inhibitors with Mitigated hERG Issue and ACS medicinal chemistry letters, , May-14, Volume: 11, Issue:5, 2020
1-Aryl-3-(4-methoxybenzyl)ureas as potentially irreversible glycogen synthase kinase 3 inhibitors: Synthesis and biological evaluation.Bioorganic & medicinal chemistry letters, , 07-01, Volume: 29, Issue:13, 2019
Discovery of new GSK-3β inhibitors through structure-based virtual screening.Bioorganic & medicinal chemistry letters, , 01-15, Volume: 28, Issue:2, 2018
Design, synthesis, and evaluation of 4,5,6,7-tetrahydrobenzo[MedChemComm, , Sep-01, Volume: 9, Issue:9, 2018
Natural and synthetic bioactive inhibitors of glycogen synthase kinase.European journal of medicinal chemistry, , Jan-05, Volume: 125, 2017
Discovery of novel potent and highly selective glycogen synthase kinase-3β (GSK3β) inhibitors for Alzheimer's disease: design, synthesis, and characterization of pyrazines.Journal of medicinal chemistry, , Nov-08, Volume: 55, Issue:21, 2012
Towards the preparation of radiolabeled 1-aryl-3-benzyl ureas: Radiosynthesis of [(11)C-carbonyl] AR-A014418 by [(11)C]CO(2) fixation.Bioorganic & medicinal chemistry letters, , Mar-01, Volume: 22, Issue:5, 2012
Exploring the binding sites of glycogen synthase kinase 3. Identification and characterization of allosteric modulation cavities.Journal of medicinal chemistry, , Dec-22, Volume: 54, Issue:24, 2011
Synthesis and biological evaluation of glycogen synthase kinase 3 (GSK-3) inhibitors: an fast and atom efficient access to 1-aryl-3-benzylureas.Bioorganic & medicinal chemistry letters, , Sep-15, Volume: 21, Issue:18, 2011
Fragment and knowledge-based design of selective GSK-3beta inhibitors using virtual screening models.European journal of medicinal chemistry, , Volume: 44, Issue:6, 2009
From a natural product lead to the identification of potent and selective benzofuran-3-yl-(indol-3-yl)maleimides as glycogen synthase kinase 3beta inhibitors that suppress proliferation and survival of pancreatic cancer cells.Journal of medicinal chemistry, , Apr-09, Volume: 52, Issue:7, 2009
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
Pharmacological inhibitors of glycogen synthase kinase 3.Trends in pharmacological sciences, , Volume: 25, Issue:9, 2004
Recent development of CDK inhibitors: An overview of CDK/inhibitor co-crystal structures.European journal of medicinal chemistry, , Feb-15, Volume: 164, 2019
Discovery of 1,3,4-oxidiazole scaffold compounds as inhibitors of superoxide dismutase expression.Bioorganic & medicinal chemistry letters, , Mar-15, Volume: 24, Issue:6, 2014
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
3D QSAR studies on GSK-3 inhibition by aloisines.Bioorganic & medicinal chemistry letters, , Jan-17, Volume: 15, Issue:2, 2005
Aloisines, a new family of CDK/GSK-3 inhibitors. SAR study, crystal structure in complex with CDK2, enzyme selectivity, and cellular effects.Journal of medicinal chemistry, , Jan-16, Volume: 46, Issue:2, 2003
Natural and synthetic bioactive inhibitors of glycogen synthase kinase.European journal of medicinal chemistry, , Jan-05, Volume: 125, 2017
Acridone alkaloids from Glycosmis chlorosperma as DYRK1A inhibitors.Journal of natural products, , May-23, Volume: 77, Issue:5, 2014
Design, synthesis, and biological evaluation of 1-phenylpyrazolo[3,4-e]pyrrolo[3,4-g]indolizine-4,6(1H,5H)-diones as new glycogen synthase kinase-3β inhibitors.Journal of medicinal chemistry, , Dec-27, Volume: 56, Issue:24, 2013
Soluble 3',6-substituted indirubins with enhanced selectivity toward glycogen synthase kinase -3 alter circadian period.Journal of medicinal chemistry, , Oct-23, Volume: 51, Issue:20, 2008
3'-Substituted 7-halogenoindirubins, a new class of cell death inducing agents.Journal of medicinal chemistry, , Jul-27, Volume: 49, Issue:15, 2006
Structural basis for the synthesis of indirubins as potent and selective inhibitors of glycogen synthase kinase-3 and cyclin-dependent kinases.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
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
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
3D QSAR studies on GSK-3 inhibition by aloisines.Bioorganic & medicinal chemistry letters, , Jan-17, Volume: 15, Issue:2, 2005
Aloisines, a new family of CDK/GSK-3 inhibitors. SAR study, crystal structure in complex with CDK2, enzyme selectivity, and cellular effects.Journal of medicinal chemistry, , Jan-16, Volume: 46, Issue:2, 2003
Development of inhibitors targeting glycogen synthase kinase-3β for human diseases: Strategies to improve selectivity.European journal of medicinal chemistry, , Jun-05, Volume: 236, 2022
Discovery of Novel Benzothiazepinones as Irreversible Covalent Glycogen Synthase Kinase 3β Inhibitors for the Treatment of Acute Promyelocytic Leukemia.Journal of medicinal chemistry, , 06-10, Volume: 64, Issue:11, 2021
PROTACs suppression of GSK-3β, a crucial kinase in neurodegenerative diseases.European journal of medicinal chemistry, , Jan-15, Volume: 210, 2021
Tau-Centric Multitarget Approach for Alzheimer's Disease: Development of First-in-Class Dual Glycogen Synthase Kinase 3β and Tau-Aggregation Inhibitors.Journal of medicinal chemistry, , 09-13, Volume: 61, Issue:17, 2018
The discovery of novel benzothiazinones as highly selective non-ATP competitive glycogen synthase kinase 3β inhibitors for the treatment of ovarian cancer.European journal of medicinal chemistry, , Jul-28, Volume: 135, 2017
New applications for known drugs: Human glycogen synthase kinase 3 inhibitors as modulators of Aspergillus fumigatus growth.European journal of medicinal chemistry, , Jun-30, Volume: 116, 2016
Hit Optimization of 5-Substituted-N-(piperidin-4-ylmethyl)-1H-indazole-3-carboxamides: Potent Glycogen Synthase Kinase-3 (GSK-3) Inhibitors with in Vivo Activity in Model of Mood Disorders.Journal of medicinal chemistry, , Nov-25, Volume: 58, Issue:22, 2015
Design, synthesis and biological evaluation of benzothiazepinones (BTZs) as novel non-ATP competitive inhibitors of glycogen synthase kinase-3β (GSK-3β).European journal of medicinal chemistry, , Volume: 61, 2013
Identification of novel scaffold of benzothiazepinones as non-ATP competitive glycogen synthase kinase-3β inhibitors through virtual screening.Bioorganic & medicinal chemistry letters, , Dec-01, Volume: 22, Issue:23, 2012
SAR and 3D-QSAR studies on thiadiazolidinone derivatives: exploration of structural requirements for glycogen synthase kinase 3 inhibitors.Journal of medicinal chemistry, , Nov-17, Volume: 48, Issue:23, 2005
Pharmacological inhibitors of glycogen synthase kinase 3.Trends in pharmacological sciences, , Volume: 25, Issue:9, 2004
First non-ATP competitive glycogen synthase kinase 3 beta (GSK-3beta) inhibitors: thiadiazolidinones (TDZD) as potential drugs for the treatment of Alzheimer's disease.Journal of medicinal chemistry, , Mar-14, Volume: 45, Issue:6, 2002
Design, synthesis and biological evaluation of harmine derivatives as potent GSK-3β/DYRK1A dual inhibitors for the treatment of Alzheimer's disease.European journal of medicinal chemistry, , Oct-15, Volume: 222, 2021
Glycogen Synthase Kinase 3β: A New Gold Rush in Anti-Alzheimer's Disease Multitarget Drug Discovery?Journal of medicinal chemistry, , 01-14, Volume: 64, Issue:1, 2021
Discovery of the First-in-Class GSK-3β/HDAC Dual Inhibitor as Disease-Modifying Agent To Combat Alzheimer's Disease.ACS medicinal chemistry letters, , Apr-11, Volume: 10, Issue:4, 2019
Eutypoids B-E produced by a Penicillium sp. strain from the North Sea.Journal of natural products, , Jan-28, Volume: 74, Issue:1, 2011
3-Aryl-4-(arylhydrazono)-1H-pyrazol-5-ones: Highly ligand efficient and potent inhibitors of GSK3beta.Bioorganic & medicinal chemistry letters, , Mar-01, Volume: 20, Issue:5, 2010
Discovery of potent and bioavailable GSK-3beta inhibitors.Bioorganic & medicinal chemistry letters, , Mar-01, Volume: 20, Issue:5, 2010
Fragment and knowledge-based design of selective GSK-3beta inhibitors using virtual screening models.European journal of medicinal chemistry, , Volume: 44, Issue:6, 2009
Pharmacophore modeling, quantitative structure-activity relationship analysis, and in silico screening reveal potent glycogen synthase kinase-3beta inhibitory activities for cimetidine, hydroxychloroquine, and gemifloxacin.Journal of medicinal chemistry, , Apr-10, Volume: 51, Issue:7, 2008
Pharmacological inhibitors of glycogen synthase kinase 3.Trends in pharmacological sciences, , Volume: 25, Issue:9, 2004
Synthesis and in vitro characterization of 1-(4-aminofurazan-3-yl)-5-dialkylaminomethyl-1H-[1,2,3]triazole-4-carboxylic acid derivatives. A new class of selective GSK-3 inhibitors.Journal of medicinal chemistry, , Jul-17, Volume: 46, Issue:15, 2003
PROTACs suppression of GSK-3β, a crucial kinase in neurodegenerative diseases.European journal of medicinal chemistry, , Jan-15, Volume: 210, 2021
A novel GSK-3 inhibitor binds to GSK-3β via a reversible, time and Cys-199-dependent mechanism.Bioorganic & medicinal chemistry, , 06-15, Volume: 40, 2021
Discovery of new GSK-3β inhibitors through structure-based virtual screening.Bioorganic & medicinal chemistry letters, , 01-15, Volume: 28, Issue:2, 2018
Pivotal role of glycogen synthase kinase-3: A therapeutic target for Alzheimer's disease.European journal of medicinal chemistry, , Jan-01, Volume: 107, 2016
Exploring the binding sites of glycogen synthase kinase 3. Identification and characterization of allosteric modulation cavities.Journal of medicinal chemistry, , Dec-22, Volume: 54, Issue:24, 2011
Development of 5-benzylpaullones and paullone-9-carboxylic acid alkyl esters as selective inhibitors of mitochondrial malate dehydrogenase (mMDH).European journal of medicinal chemistry, , Volume: 45, Issue:1, 2010
9-cyano-1-azapaullone (cazpaullone), a glycogen synthase kinase-3 (GSK-3) inhibitor activating pancreatic beta cell protection and replication.Journal of medicinal chemistry, , Apr-10, Volume: 51, Issue:7, 2008
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
Structure-aided optimization of kinase inhibitors derived from alsterpaullone.Chembiochem : a European journal of chemical biology, , Volume: 6, Issue:3, 2005
Pharmacological inhibitors of glycogen synthase kinase 3.Trends in pharmacological sciences, , Volume: 25, Issue:9, 2004
Evaluation and comparison of 3D-QSAR CoMSIA models for CDK1, CDK5, and GSK-3 inhibition by paullones.Journal of medicinal chemistry, , Jan-01, Volume: 47, Issue:1, 2004
Discovery of novel β-carboline derivatives as selective AChE inhibitors with GSK-3β inhibitory property for the treatment of Alzheimer's disease.European journal of medicinal chemistry, , Feb-05, Volume: 229, 2022
Design, synthesis and biological evaluation of harmine derivatives as potent GSK-3β/DYRK1A dual inhibitors for the treatment of Alzheimer's disease.European journal of medicinal chemistry, , Oct-15, Volume: 222, 2021
Selective DYRK1A Inhibitor for the Treatment of Type 1 Diabetes: Discovery of 6-Azaindole Derivative GNF2133.Journal of medicinal chemistry, , 03-26, Volume: 63, Issue:6, 2020
Synthesis, biological evaluation and molecular modeling studies of imidazo[1,2-a]pyridines derivatives as protein kinase inhibitors.European journal of medicinal chemistry, , Nov-10, Volume: 123, 2016
Synthesis of new pyridazino[4,5-b]indol-4-ones and pyridazin-3(2H)-one analogs as DYRK1A inhibitors.Bioorganic & medicinal chemistry letters, , Nov-01, Volume: 24, Issue:21, 2014
Selectivity, cocrystal structures, and neuroprotective properties of leucettines, a family of protein kinase inhibitors derived from the marine sponge alkaloid leucettamine B.Journal of medicinal chemistry, , Nov-08, Volume: 55, Issue:21, 2012
Discovery of Journal of medicinal chemistry, , 09-09, Volume: 64, Issue:17, 2021
Identification of a new series of flavopiridol-like structures as kinase inhibitors with high cytotoxic potency.European journal of medicinal chemistry, , Aug-01, Volume: 199, 2020
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
Crystal structure of a human cyclin-dependent kinase 6 complex with a flavonol inhibitor, fisetin.Journal of medicinal chemistry, , Feb-10, Volume: 48, 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
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
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
1-Acyl-1H-[1,2,4]triazole-3,5-diamine analogues as novel and potent anticancer cyclin-dependent kinase inhibitors: synthesis and evaluation of biological activities.Journal of medicinal chemistry, , Jun-30, Volume: 48, Issue:13, 2005
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 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
CH...O and CH...N hydrogen bonds in ligand design: a novel quinazolin-4-ylthiazol-2-ylamine protein kinase inhibitor.Journal of medicinal chemistry, , Feb-24, Volume: 48, Issue:4, 2005
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Discovery of 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
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
Identification of novel scaffold of benzothiazepinones as non-ATP competitive glycogen synthase kinase-3β inhibitors through virtual screening.Bioorganic & medicinal chemistry letters, , Dec-01, Volume: 22, Issue:23, 2012
Discovery of novel GSK-3β inhibitors with potent in vitro and in vivo activities and excellent brain permeability using combined ligand- and structure-based virtual screening.Journal of medicinal chemistry, , Dec-23, Volume: 53, Issue:24, 2010
The marine natural-derived inhibitors of glycogen synthase kinase-3beta phenylmethylene hydantoins: In vitro and in vivo activities and pharmacophore modeling.Bioorganic & medicinal chemistry, , Aug-15, Volume: 17, Issue:16, 2009
Kinetic studies and bioactivity of potential manzamine prodrugs.Journal of natural products, , Volume: 71, Issue:7, 2008
2-N-Methyl modifications and SAR studies of manzamine A.Bioorganic & medicinal chemistry, , Jul-15, Volume: 16, Issue:14, 2008
Glycogen synthase kinase-3 (GSK-3) inhibitory activity and structure-activity relationship (SAR) studies of the manzamine alkaloids. Potential for Alzheimer's disease.Journal of natural products, , Volume: 70, Issue:9, 2007
9-cyano-1-azapaullone (cazpaullone), a glycogen synthase kinase-3 (GSK-3) inhibitor activating pancreatic beta cell protection and replication.Journal of medicinal chemistry, , Apr-10, Volume: 51, Issue:7, 2008
1-Azakenpaullone is a selective inhibitor of glycogen synthase kinase-3 beta.Bioorganic & medicinal chemistry letters, , Jan-19, Volume: 14, Issue:2, 2004
Pharmacological inhibitors of glycogen synthase kinase 3.Trends in pharmacological sciences, , Volume: 25, Issue:9, 2004
Discovery of 1,3,4-oxidiazole scaffold compounds as inhibitors of superoxide dismutase expression.Bioorganic & medicinal chemistry letters, , Mar-15, Volume: 24, Issue:6, 2014
Identification of glycogen synthase kinase-3 inhibitors with a selective sting for glycogen synthase kinase-3α.Journal of medicinal chemistry, , May-10, Volume: 55, Issue:9, 2012
Pharmacological inhibitors of glycogen synthase kinase 3.Trends in pharmacological sciences, , Volume: 25, Issue:9, 2004
Scaffold hopping and optimization towards libraries of glycogen synthase kinase-3 inhibitors.Bioorganic & medicinal chemistry letters, , Jun-03, Volume: 12, Issue:11, 2002
PROTACs suppression of GSK-3β, a crucial kinase in neurodegenerative diseases.European journal of medicinal chemistry, , Jan-15, Volume: 210, 2021
Structure-activity relationship (SAR) studies of synthetic glycogen synthase kinase-3β inhibitors: A critical review.European journal of medicinal chemistry, , Feb-15, Volume: 164, 2019
Pharmacological inhibitors of glycogen synthase kinase 3.Trends in pharmacological sciences, , Volume: 25, Issue:9, 2004
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Targeting GSK3 from Ustilago maydis: type-II kinase inhibitors as potential antifungals.ACS chemical biology, , Jul-20, Volume: 7, Issue:7, 2012
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
Prevention of organ allograft rejection by a specific Janus kinase 3 inhibitor.Science (New York, N.Y.), , Oct-31, Volume: 302, Issue:5646, 2003
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
ARN25068, a versatile starting point towards triple GSK-3β/FYN/DYRK1A inhibitors to tackle tau-related neurological disorders.European journal of medicinal chemistry, , Feb-05, Volume: 229, 2022
PROTACs suppression of GSK-3β, a crucial kinase in neurodegenerative diseases.European journal of medicinal chemistry, , Jan-15, Volume: 210, 2021
1,2,4-Thiadiazole acyclic nucleoside phosphonates as inhibitors of cysteine dependent enzymes cathepsin K and GSK-3β.Bioorganic & medicinal chemistry, , 02-15, Volume: 32, 2021
Synthesis, Binding Mode, and Antihyperglycemic Activity of Potent and Selective (5-Imidazol-2-yl-4-phenylpyrimidin-2-yl)[2-(2-pyridylamino)ethyl]amine Inhibitors of Glycogen Synthase Kinase 3.Journal of medicinal chemistry, , 10-26, Volume: 60, Issue:20, 2017
Quinolone derivatives containing strained spirocycle as orally active glycogen synthase kinase 3β (GSK-3β) inhibitors for type 2 diabetics.Bioorganic & medicinal chemistry, , Feb-01, Volume: 20, Issue:3, 2012
Pharmacological inhibitors of glycogen synthase kinase 3.Trends in pharmacological sciences, , Volume: 25, Issue:9, 2004
Discovery of novel glycogen synthase kinase-3α inhibitors: Structure-based virtual screening, preliminary SAR and biological evaluation for treatment of acute myeloid leukemia.European journal of medicinal chemistry, , Jun-01, Volume: 171, 2019
Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure.Drug metabolism and disposition: the biological fate of chemicals, , Volume: 41, Issue:4, 2013
Fragment and knowledge-based design of selective GSK-3beta inhibitors using virtual screening models.European journal of medicinal chemistry, , Volume: 44, Issue:6, 2009
Substituted 3-imidazo[1,2-a]pyridin-3-yl- 4-(1,2,3,4-tetrahydro-[1,4]diazepino-[6,7,1-hi]indol-7-yl)pyrrole-2,5-diones as highly selective and potent inhibitors of glycogen synthase kinase-3.Journal of medicinal chemistry, , Jul-29, Volume: 47, Issue:16, 2004
Selectivity, cocrystal structures, and neuroprotective properties of leucettines, a family of protein kinase inhibitors derived from the marine sponge alkaloid leucettamine B.Journal of medicinal chemistry, , Nov-08, Volume: 55, Issue:21, 2012
Synthesis and preliminary biological evaluation of new derivatives of the marine alkaloid leucettamine B as kinase inhibitors.European journal of medicinal chemistry, , Volume: 45, Issue:2, 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
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
PROTACs suppression of GSK-3β, a crucial kinase in neurodegenerative diseases.European journal of medicinal chemistry, , Jan-15, Volume: 210, 2021
Discovery of novel potent and highly selective glycogen synthase kinase-3β (GSK3β) inhibitors for Alzheimer's disease: design, synthesis, and characterization of pyrazines.Journal of medicinal chemistry, , Nov-08, Volume: 55, Issue:21, 2012
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Discovery of 3-(1H-indol-3-yl)-4-[2-(4-methylpiperazin-1-yl)quinazolin-4-yl]pyrrole-2,5-dione (AEB071), a potent and selective inhibitor of protein kinase C isotypes.Journal of medicinal chemistry, , Oct-22, Volume: 52, Issue:20, 2009
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
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
CNS and antimalarial activity of synthetic meridianin and psammopemmin analogs.Bioorganic & medicinal chemistry, , Oct-01, Volume: 19, Issue:19, 2011
Meridianins, a new family of protein kinase inhibitors isolated from the ascidian Aplidium meridianum.Bioorganic & medicinal chemistry letters, , Apr-05, Volume: 14, Issue:7, 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
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
Small-Molecule Kinase Inhibitors for the Treatment of Nononcologic Diseases.Journal of medicinal chemistry, , 02-11, Volume: 64, Issue:3, 2021
PROTACs suppression of GSK-3β, a crucial kinase in neurodegenerative diseases.European journal of medicinal chemistry, , Jan-15, Volume: 210, 2021
1,2,4-Thiadiazole acyclic nucleoside phosphonates as inhibitors of cysteine dependent enzymes cathepsin K and GSK-3β.Bioorganic & medicinal chemistry, , 02-15, Volume: 32, 2021
A novel GSK-3 inhibitor binds to GSK-3β via a reversible, time and Cys-199-dependent mechanism.Bioorganic & medicinal chemistry, , 06-15, Volume: 40, 2021
Glycogen Synthase Kinase 3β: A New Gold Rush in Anti-Alzheimer's Disease Multitarget Drug Discovery?Journal of medicinal chemistry, , 01-14, Volume: 64, Issue:1, 2021
Discovery of new GSK-3β inhibitors through structure-based virtual screening.Bioorganic & medicinal chemistry letters, , 01-15, Volume: 28, Issue:2, 2018
Natural and synthetic bioactive inhibitors of glycogen synthase kinase.European journal of medicinal chemistry, , Jan-05, Volume: 125, 2017
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
New applications for known drugs: Human glycogen synthase kinase 3 inhibitors as modulators of Aspergillus fumigatus growth.European journal of medicinal chemistry, , Jun-30, Volume: 116, 2016
Hit Optimization of 5-Substituted-N-(piperidin-4-ylmethyl)-1H-indazole-3-carboxamides: Potent Glycogen Synthase Kinase-3 (GSK-3) Inhibitors with in Vivo Activity in Model of Mood Disorders.Journal of medicinal chemistry, , Nov-25, Volume: 58, Issue:22, 2015
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Cyclin dependent kinase (CDK) inhibitors as anticancer drugs.Bioorganic & medicinal chemistry letters, , Sep-01, Volume: 25, Issue:17, 2015
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazoles: identification of a potent Aurora kinase inhibitor with a favorable antitumor kinase inhibition profile.Journal of medicinal chemistry, , Nov-30, Volume: 49, Issue:24, 2006
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
Discovery of a Pyrimidothiazolodiazepinone as a Potent and Selective Focal Adhesion Kinase (FAK) Inhibitor.ACS medicinal chemistry letters, , Jan-14, Volume: 12, Issue:1, 2021
Cellular characterization of a novel focal adhesion kinase inhibitor.The Journal of biological chemistry, , May-18, Volume: 282, Issue:20, 2007
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
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
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Identification of N,1,4,4-tetramethyl-8-{[4-(4-methylpiperazin-1-yl)phenyl]amino}-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide (PHA-848125), a potent, orally available cyclin dependent kinase inhibitor.Journal of medicinal chemistry, , Aug-27, Volume: 52, Issue:16, 2009
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
Aminofurazans as potent inhibitors of AKT kinase.Bioorganic & medicinal chemistry letters, , Mar-01, Volume: 19, Issue:5, 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
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
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Targeting GSK3 from Ustilago maydis: type-II kinase inhibitors as potential antifungals.ACS chemical biology, , Jul-20, Volume: 7, Issue:7, 2012
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
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Discovery of Entrectinib: A New 3-Aminoindazole As a Potent Anaplastic Lymphoma Kinase (ALK), c-ros Oncogene 1 Kinase (ROS1), and Pan-Tropomyosin Receptor Kinases (Pan-TRKs) inhibitor.Journal of medicinal chemistry, , Apr-14, Volume: 59, Issue:7, 2016
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
Optimization of 6,6-dimethyl pyrrolo[3,4-c]pyrazoles: Identification of PHA-793887, a potent CDK inhibitor suitable for intravenous dosing.Bioorganic & medicinal chemistry, , Mar-01, Volume: 18, Issue:5, 2010
Discovery of Journal of medicinal chemistry, , 09-09, Volume: 64, Issue:17, 2021
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Synthesis, Binding Mode, and Antihyperglycemic Activity of Potent and Selective (5-Imidazol-2-yl-4-phenylpyrimidin-2-yl)[2-(2-pyridylamino)ethyl]amine Inhibitors of Glycogen Synthase Kinase 3.Journal of medicinal chemistry, , 10-26, Volume: 60, Issue:20, 2017
Targeting GSK3 from Ustilago maydis: type-II kinase inhibitors as potential antifungals.ACS chemical biology, , Jul-20, Volume: 7, Issue:7, 2012
Design, synthesis and biological evaluation of benzothiazepinones (BTZs) as novel non-ATP competitive inhibitors of glycogen synthase kinase-3β (GSK-3β).European journal of medicinal chemistry, , Volume: 61, 2013
Evidence for a new binding mode to GSK-3: allosteric regulation by the marine compound palinurin.European journal of medicinal chemistry, , Volume: 60, 2013
Identification of novel scaffold of benzothiazepinones as non-ATP competitive glycogen synthase kinase-3β inhibitors through virtual screening.Bioorganic & medicinal chemistry letters, , Dec-01, Volume: 22, Issue:23, 2012
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
Isosteric replacements of the carboxylic acid of drug candidate VX-787: Effect of charge on antiviral potency and kinase activity of azaindole-based influenza PB2 inhibitors.Bioorganic & medicinal chemistry letters, , May-01, Volume: 25, Issue:9, 2015
Discovery of a novel, first-in-class, orally bioavailable azaindole inhibitor (VX-787) of influenza PB2.Journal of medicinal chemistry, , Aug-14, Volume: 57, Issue:15, 2014
Potent and orally bioavailable CDK8 inhibitors: Design, synthesis, structure-activity relationship analysis and biological evaluation.European journal of medicinal chemistry, , Mar-15, Volume: 214, 2021
Discovery of potent, orally bioavailable, small-molecule inhibitors of WNT signaling from a cell-based pathway screen.Journal of medicinal chemistry, , Feb-26, Volume: 58, Issue:4, 2015
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
Natural and synthetic bioactive inhibitors of glycogen synthase kinase.European journal of medicinal chemistry, , Jan-05, Volume: 125, 2017
Pivotal role of glycogen synthase kinase-3: A therapeutic target for Alzheimer's disease.European journal of medicinal chemistry, , Jan-01, Volume: 107, 2016
Synthesis and evaluation of novel anti-proliferative pyrroloazepinone and indoloazepinone oximes derived from the marine natural product hymenialdisine.European journal of medicinal chemistry, , Volume: 56, 2012
Fragment and knowledge-based design of selective GSK-3beta inhibitors using virtual screening models.European journal of medicinal chemistry, , Volume: 44, Issue:6, 2009
1-Azakenpaullone is a selective inhibitor of glycogen synthase kinase-3 beta.Bioorganic & medicinal chemistry letters, , Jan-19, Volume: 14, Issue:2, 2004
Pharmacological inhibitors of glycogen synthase kinase 3.Trends in pharmacological sciences, , Volume: 25, Issue:9, 2004
Synthesis and target identification of hymenialdisine analogs.Chemistry & biology, , Volume: 11, Issue:2, 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
Enables
This protein enables 17 target(s):
| Target | Category | Definition |
|---|
| protease binding | molecular function | Binding to a protease or a peptidase. [GOC:hjd] |
| p53 binding | molecular function | Binding to one of the p53 family of proteins. [GOC:hjd] |
| 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 serine/threonine kinase activity | molecular function | Catalysis of the reactions: ATP + protein serine = ADP + protein serine phosphate, and ATP + protein threonine = ADP + protein threonine phosphate. [GOC:bf, MetaCyc:PROTEIN-KINASE-RXN, PMID:2956925] |
| 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] |
| beta-catenin binding | molecular function | Binding to a catenin beta subunit. [GOC:bf] |
| kinase activity | molecular function | Catalysis of the transfer of a phosphate group, usually from ATP, to a substrate molecule. [ISBN:0198506732] |
| protein kinase binding | molecular function | Binding to a protein kinase, any enzyme that catalyzes the transfer of a phosphate group, usually from ATP, to a protein substrate. [GOC:jl] |
| ubiquitin protein ligase binding | molecular function | Binding to a ubiquitin protein ligase enzyme, any of the E3 proteins. [GOC:vp] |
| protein kinase A catalytic subunit binding | molecular function | Binding to one or both of the catalytic subunits of protein kinase A. [GOC:mah] |
| dynactin binding | molecular function | Binding to a dynactin complex; a large protein complex that activates dynein-based motor activity. [GOC:BHF, GOC:mah] |
| tau protein binding | molecular function | Binding to tau protein. tau is a microtubule-associated protein, implicated in Alzheimer's disease, Down Syndrome and ALS. [GOC:jid] |
| tau-protein kinase activity | molecular function | Catalysis of the reaction: ATP + tau-protein = ADP + O-phospho-tau-protein. [EC:2.7.11.26, MetaCyc:TAU-PROTEIN-KINASE-RXN] |
| NF-kappaB binding | molecular function | Binding to NF-kappaB, a transcription factor for eukaryotic RNA polymerase II promoters. [GOC:ai] |
| RNA polymerase II-specific DNA-binding transcription factor binding | molecular function | Binding to a sequence-specific DNA binding RNA polymerase II transcription factor, any of the factors that interact selectively and non-covalently with a specific DNA sequence in order to modulate transcription. [GOC:dph, GOC:vw] |
| protein serine kinase activity | molecular function | Catalysis of the reactions: ATP + protein serine = ADP + protein serine phosphate. [RHEA:17989] |
Located In
This protein is located in 11 target(s):
| Target | Category | Definition |
|---|
| nucleus | cellular component | A membrane-bounded organelle of eukaryotic cells in which chromosomes are housed and replicated. In most cells, the nucleus contains all of the cell's chromosomes except the organellar chromosomes, and is the site of RNA synthesis and processing. In some species, or in specialized cell types, RNA metabolism or DNA replication may be absent. [GOC:go_curators] |
| 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] |
| centrosome | cellular component | A structure comprised of a core structure (in most organisms, a pair of centrioles) and peripheral material from which a microtubule-based structure, such as a spindle apparatus, is organized. Centrosomes occur close to the nucleus during interphase in many eukaryotic cells, though in animal cells it changes continually during the cell-division cycle. [GOC:mah, ISBN:0198547684] |
| 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] |
| 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] |
| axon | cellular component | The long process of a neuron that conducts nerve impulses, usually away from the cell body to the terminals and varicosities, which are sites of storage and release of neurotransmitter. [GOC:nln, ISBN:0198506732] |
| dendrite | cellular component | A neuron projection that has a short, tapering, morphology. Dendrites receive and integrate signals from other neurons or from sensory stimuli, and conduct nerve impulses towards the axon or the cell body. In most neurons, the impulse is conveyed from dendrites to axon via the cell body, but in some types of unipolar neuron, the impulse does not travel via the cell body. [GOC:aruk, GOC:bc, GOC:dos, GOC:mah, GOC:nln, ISBN:0198506732] |
| presynapse | cellular component | The part of a synapse that is part of the presynaptic cell. [GOC:dos] |
| postsynapse | cellular component | The part of a synapse that is part of the post-synaptic cell. [GOC:dos] |
Active In
This protein is active in 5 target(s):
| Target | Category | Definition |
|---|
| glutamatergic synapse | cellular component | A synapse that uses glutamate as a neurotransmitter. [GOC:dos] |
| 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] |
| axon | cellular component | The long process of a neuron that conducts nerve impulses, usually away from the cell body to the terminals and varicosities, which are sites of storage and release of neurotransmitter. [GOC:nln, ISBN:0198506732] |
| nucleus | cellular component | A membrane-bounded organelle of eukaryotic cells in which chromosomes are housed and replicated. In most cells, the nucleus contains all of the cell's chromosomes except the organellar chromosomes, and is the site of RNA synthesis and processing. In some species, or in specialized cell types, RNA metabolism or DNA replication may be absent. [GOC:go_curators] |
| cytoplasm | cellular component | The contents of a cell excluding the plasma membrane and nucleus, but including other subcellular structures. [ISBN:0198547684] |
Part Of
This protein is part of 2 target(s):
| Target | Category | Definition |
|---|
| beta-catenin destruction complex | cellular component | A cytoplasmic protein complex containing glycogen synthase kinase-3-beta (GSK-3-beta), the adenomatous polyposis coli protein (APC), and the scaffolding protein axin, among others; phosphorylates beta-catenin, targets it for degradation by the proteasome. [PMID:14600025] |
| Wnt signalosome | cellular component | A multiprotein protein complex containing membrane-localized Wnt receptors and cytosolic protein complexes, which is capable of transmitting the Wnt signal. Contains at least a Wnt protein, LRP5 or LRP6, a member of the Frizzled (Fz) family, Axin and and a Dishevelled (DVL) protein. [GOC:bf, GOC:PARL, PMID:22899650, PMID:25336320] |
Involved In
This protein is involved in 69 target(s):
| Target | Category | Definition |
|---|
| epithelial to mesenchymal transition | biological process | A transition where an epithelial cell loses apical/basolateral polarity, severs intercellular adhesive junctions, degrades basement membrane components and becomes a migratory mesenchymal cell. [GOC:dph, PMID:14701881] |
| positive regulation of cell-matrix adhesion | biological process | Any process that activates or increases the rate or extent of cell adhesion to an extracellular matrix. [GOC:hjd] |
| glycogen metabolic process | biological process | The chemical reactions and pathways involving glycogen, a polydisperse, highly branched glucan composed of chains of D-glucose residues in alpha-(1->4) glycosidic linkage, joined together by alpha-(1->6) glycosidic linkages. [ISBN:0198506732] |
| protein phosphorylation | biological process | The process of introducing a phosphate group on to a protein. [GOC:hb] |
| mitochondrion 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 a mitochondrion; includes mitochondrial morphogenesis and distribution, and replication of the mitochondrial genome as well as synthesis of new mitochondrial components. [GOC:dph, GOC:jl, GOC:mah, GOC:sgd_curators, PMID:9786946] |
| dopamine receptor signaling pathway | biological process | The series of molecular signals generated as a consequence of a dopamine receptor binding to one of its physiological ligands. [GOC:mah, PMID:21711983] |
| circadian rhythm | biological process | Any biological process in an organism that recurs with a regularity of approximately 24 hours. [GOC:bf, GOC:go_curators] |
| positive regulation of autophagy | biological process | Any process that activates, maintains or increases the rate of autophagy. Autophagy is the process in which cells digest parts of their own cytoplasm. [GOC:dph, GOC:tb] |
| positive regulation of gene expression | biological process | Any process that increases the frequency, rate or extent of gene expression. Gene expression is the process in which a gene's coding sequence is converted into a mature gene product (protein or RNA). [GOC:txnOH-2018] |
| peptidyl-serine phosphorylation | biological process | The phosphorylation of peptidyl-serine to form peptidyl-O-phospho-L-serine. [RESID:AA0037] |
| peptidyl-threonine phosphorylation | biological process | The phosphorylation of peptidyl-threonine to form peptidyl-O-phospho-L-threonine. [RESID:AA0038] |
| viral protein processing | biological process | Any protein maturation process achieved by the cleavage of a peptide bond or bonds within a viral protein. [GOC:bf, GOC:jl, ISBN:0781702534] |
| hippocampus development | biological process | The progression of the hippocampus over time from its initial formation until its mature state. [GO_REF:0000021, GOC:cls, GOC:dgh, GOC:dph, GOC:jid, ISBN:0878937420, UBERON:0002421] |
| establishment of cell polarity | biological process | The specification and formation of anisotropic intracellular organization or cell growth patterns. [GOC:mah] |
| maintenance of cell polarity | biological process | The maintenance of established anisotropic intracellular organization or cell growth patterns. [GOC:mah] |
| negative regulation of cell migration | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of cell migration. [GOC:go_curators] |
| regulation of axon extension | biological process | Any process that modulates the rate, direction or extent of axon extension. [GOC:go_curators] |
| neuron projection development | biological process | The process whose specific outcome is the progression of a neuron projection over time, from its formation to the mature structure. A neuron projection is any process extending from a neural cell, such as axons or dendrites (collectively called neurites). [GOC:mah] |
| 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] |
| positive regulation of protein-containing complex assembly | biological process | Any process that activates or increases the frequency, rate or extent of protein complex assembly. [GOC:mah] |
| positive regulation of protein ubiquitination | biological process | Any process that activates or increases the frequency, rate or extent of the addition of ubiquitin groups to a protein. [GOC:mah] |
| positive regulation of protein binding | biological process | Any process that activates or increases the frequency, rate or extent of protein binding. [GOC:mah] |
| positive regulation of proteasomal ubiquitin-dependent protein catabolic process | biological process | Any process that activates or increases the frequency, rate or extent of the breakdown of a protein or peptide by hydrolysis of its peptide bonds, initiated by the covalent attachment of ubiquitin, and mediated by the proteasome. [GOC:mah] |
| negative regulation of phosphoprotein phosphatase activity | biological process | Any process that stops or reduces the activity of a phosphoprotein phosphatase. [GOC:mah] |
| regulation of microtubule-based process | biological process | Any process that modulates the frequency, rate or extent of any cellular process that depends upon or alters the microtubule cytoskeleton. [GOC:mah] |
| 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] |
| cellular response to interleukin-3 | 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 interleukin-3 stimulus. [GOC:yaf] |
| regulation of circadian rhythm | biological process | Any process that modulates the frequency, rate or extent of a circadian rhythm. A circadian rhythm is a biological process in an organism that recurs with a regularity of approximately 24 hours. [GOC:dph, GOC:jl, GOC:tb] |
| proteasome-mediated ubiquitin-dependent protein catabolic process | biological process | The chemical reactions and pathways resulting in the breakdown of a protein or peptide by hydrolysis of its peptide bonds, initiated by the covalent attachment of ubiquitin, and mediated by the proteasome. [GOC:go_curators] |
| positive regulation of GTPase activity | biological process | Any process that activates or increases the activity of a GTPase. [GOC:jl, GOC:mah] |
| positive regulation of cell differentiation | biological process | Any process that activates or increases the frequency, rate or extent of cell differentiation. [GOC:go_curators] |
| negative regulation of osteoblast differentiation | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of osteoblast differentiation. [GOC:go_curators] |
| negative regulation of glycogen biosynthetic process | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of the chemical reactions and pathways resulting in the formation of glycogen. [GOC:go_curators] |
| positive regulation of cilium assembly | biological process | Any process that activates or increases the frequency, rate or extent of the formation of a cilium. [GOC:cilia, GOC:go_curators] |
| positive regulation of protein catabolic process | biological process | Any process that activates or increases the frequency, rate or extent of the chemical reactions and pathways resulting in the breakdown of a protein by the destruction of the native, active configuration, with or without the hydrolysis of peptide bonds. [GOC:go_curators] |
| protein autophosphorylation | biological process | The phosphorylation by a protein of one or more of its own amino acid residues (cis-autophosphorylation), or residues on an identical protein (trans-autophosphorylation). [ISBN:0198506732] |
| regulation of protein export from nucleus | biological process | Any process that modulates the frequency, rate or extent of the directed movement of proteins from the nucleus to the cytoplasm. [GOC:bf] |
| regulation of dendrite morphogenesis | biological process | Any process that modulates the frequency, rate or extent of dendrite morphogenesis. [GOC:ai] |
| regulation of axonogenesis | biological process | Any process that modulates the frequency, rate or extent of axonogenesis, the generation of an axon, the long process of a neuron. [GOC:ai] |
| canonical Wnt signaling pathway | biological process | A type of Wnt signaling pathway in which Wnt binding to its receptor on the surface of a target cell results in the by propagation of the molecular signals via beta-catenin, and end with a change in transcription of target genes. In this pathway, the activated receptor signals via downstream effectors that result in the inhibition of beta-catenin phosphorylation, thereby preventing degradation of beta-catenin. Stabilized beta-catenin can then accumulate and travel to the nucleus to trigger changes in transcription of target genes. [PMID:11532397, PMID:19619488] |
| excitatory postsynaptic potential | biological process | A process that leads to a temporary increase in postsynaptic potential due to the flow of positively charged ions into the postsynaptic cell. The flow of ions that causes an EPSP is an excitatory postsynaptic current (EPSC) and makes it easier for the neuron to fire an action potential. [GOC:dph, GOC:ef] |
| regulation of microtubule cytoskeleton organization | biological process | Any process that modulates the frequency, rate or extent of the formation, arrangement of constituent parts, or disassembly of cytoskeletal structures comprising microtubules and their associated proteins. [GOC:mah] |
| negative regulation of calcineurin-NFAT signaling cascade | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of the calcineurin-NFAT signaling cascade. [GOC:mah] |
| superior temporal gyrus development | biological process | The process whose specific outcome is the progression of the superior temporal gyrus over time, from its formation to the mature structure. The superior temporal gyrus is a portion of the cerebral cortex that extends from the lateral sulcus to the superior temporal sulcus. [FMA:61905, GOC:BHF, GOC:mah, PMID:11484000] |
| cellular response to retinoic 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 retinoic acid stimulus. [GOC:mah] |
| negative regulation of canonical Wnt signaling pathway | biological process | Any process that decreases 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:dph, GOC:tb] |
| extrinsic apoptotic signaling pathway | biological process | The series of molecular signals in which a signal is conveyed from the cell surface to trigger the apoptotic death of a cell. The pathway starts with either a ligand binding to a cell surface receptor, or a ligand being withdrawn from a cell surface receptor (e.g. in the case of signaling by dependence receptors), and ends when the execution phase of apoptosis is triggered. [GOC:mtg_apoptosis, GOC:yaf, PMID:17340152] |
| extrinsic apoptotic signaling pathway in absence of ligand | biological process | The series of molecular signals in which a signal is conveyed from the cell surface to trigger the apoptotic death of a cell. The pathway starts with withdrawal of a ligand from a cell surface receptor, and ends when the execution phase of apoptosis is triggered. [GOC:mtg_apoptosis, PMID:15044679, PMID:20816705] |
| presynaptic modulation of chemical synaptic transmission | biological process | Any process, acting in the presynapse that results in modulation of chemical synaptic transmission. [GOC:dos] |
| neuron projection 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 a prolongation or process extending from a neuron, e.g. an axon, or a dendrite. [GOC:aruk, GOC:bc, PMID:11585923] |
| regulation of microtubule anchoring at centrosome | biological process | Any process that modulates the frequency, rate or extent of microtubule anchoring at centrosome. [GOC:aruk, GOC:bc, PMID:17139249] |
| regulation of cellular response to heat | biological process | Any process that modulates the frequency, rate or extent of cellular response to heat. [GOC:TermGenie, GOC:yaf] |
| negative regulation of protein localization to nucleus | biological process | Any process that stops, prevents or reduces the frequency, rate or extent of protein localization to nucleus. [GOC:TermGenie] |
| regulation of long-term synaptic potentiation | biological process | Any process that modulates the frequency, rate or extent of long-term synaptic potentiation. [GOC:BHF, GOC:TermGenie] |
| positive regulation of mitochondrial outer membrane permeabilization involved in apoptotic signaling pathway | biological process | Any process that activates or increases the frequency, rate or extent of mitochondrial outer membrane permeabilization involved in apoptotic signaling pathway. [GOC:BHF, GOC:mtg_apoptosis, GOC:TermGenie] |
| negative regulation of protein acetylation | biological process | Any process that stops, prevents or reduces the frequency, rate or extent of protein acetylation. [GOC:TermGenie, PMID:22117195] |
| negative regulation of extrinsic apoptotic signaling pathway via death domain receptors | biological process | Any process that stops, prevents or reduces the frequency, rate or extent of extrinsic apoptotic signaling pathway via death domain receptors. [GOC:TermGenie, PMID:17245429] |
| positive regulation of protein localization to cilium | biological process | Any process that activates or increases the frequency, rate or extent of protein localization to cilium. [GO_REF:0000058, GOC:cilia, GOC:krc, GOC:TermGenie, PMID:22072986] |
| negative regulation of dopaminergic neuron differentiation | biological process | Any process that stops, prevents or reduces the frequency, rate or extent of dopaminergic neuron differentiation. [GO_REF:0000058, GOC:TermGenie, PMID:15522889] |
| cellular response to amyloid-beta | 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 amyloid-beta stimulus. [GO_REF:0000071, GOC:TermGenie, PMID:23555824] |
| positive regulation of protein localization to centrosome | biological process | Any process that activates or increases the frequency, rate or extent of protein localization to centrosome. [GO_REF:0000058, GOC:TermGenie, PMID:17115027] |
| beta-catenin destruction complex disassembly | biological process | The disaggregation of a beta-catenin destruction complex into its constituent components. [GO_REF:0000079, GOC:bf, GOC:PARL, GOC:TermGenie, PMID:23169527] |
| negative regulation of type B pancreatic cell development | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of pancreatic B cell development. [GOC:obol, GOC:yaf] |
| negative regulation of glycogen (starch) synthase activity | biological process | Any process that stops, prevents or reduces the frequency, rate or extent of glycogen (starch) synthase activity. [GOC:obol] |
| negative regulation of mesenchymal stem cell differentiation | biological process | Any process that stops, prevents or reduces the frequency, rate or extent of mesenchymal stem cell differentiation. [GOC:obol] |
| negative regulation of TOR signaling | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of TOR signaling. [GOC:mah] |
| regulation of neuron projection development | biological process | Any process that modulates the rate, frequency or extent of neuron projection development. Neuron projection development is the process whose specific outcome is the progression of a neuron projection over time, from its formation to the mature structure. A neuron projection is any process extending from a neural cell, such as axons or dendrites (collectively called neurites). [GOC:dph, GOC:tb] |
| 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] |
| insulin receptor signaling pathway | biological process | The series of molecular signals generated as a consequence of the insulin receptor binding to insulin. [GOC:ceb] |