Page last updated: 2024-08-07 15:55:55
Cyclin-dependent kinase 4
A cell division protein kinase 4 that is encoded in the genome of human. [PRO:DNx, UniProtKB:P11802]
Synonyms
EC 2.7.11.22;
Cell division protein kinase 4;
PSK-J3
Research
Bioassay Publications (127)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 1 (0.79) | 18.2507 |
| 2000's | 45 (35.43) | 29.6817 |
| 2010's | 57 (44.88) | 24.3611 |
| 2020's | 24 (18.90) | 2.80 |
Compounds (296)
Drugs with Inhibition Measurements
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 |
| imatinib | Homo sapiens (human) | Kd | 16.6667 | 3 | 3 |
| triciribine phosphate | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| staurosporine | Homo sapiens (human) | Kd | 0.0350 | 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 | 0.3103 | 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 | 10.1867 | 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 | 30.0000 | 1 | 1 |
| sb 203580 | Homo sapiens (human) | Kd | 10.0000 | 2 | 2 |
| enzastaurin | Homo sapiens (human) | Kd | 16.6667 | 3 | 3 |
| erlotinib | Homo sapiens (human) | Kd | 16.6667 | 3 | 3 |
| lapatinib | Homo sapiens (human) | Kd | 16.6667 | 3 | 3 |
| sorafenib | Homo sapiens (human) | Kd | 16.6667 | 3 | 3 |
| pd 173955 | Homo sapiens (human) | Kd | 10.0000 | 2 | 2 |
| s 1033 | Homo sapiens (human) | Kd | 16.6667 | 3 | 3 |
| xl147 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| bms 387032 | Homo sapiens (human) | Kd | 1.3663 | 3 | 3 |
| sf 2370 | Homo sapiens (human) | Kd | 0.0140 | 1 | 1 |
| tandutinib | Homo sapiens (human) | Kd | 16.6667 | 3 | 3 |
| vx-745 | Homo sapiens (human) | Kd | 10.0000 | 2 | 2 |
| dasatinib | Homo sapiens (human) | Kd | 20.0000 | 3 | 4 |
| ha 1100 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| 7-epi-hydroxystaurosporine | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| zd 6474 | Homo sapiens (human) | Kd | 20.0000 | 3 | 4 |
| imd 0354 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| sirolimus | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| alvocidib | Homo sapiens (human) | Kd | 10.0041 | 3 | 3 |
| bosutinib | Homo sapiens (human) | Kd | 16.6667 | 3 | 3 |
| orantinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| su 11248 | Homo sapiens (human) | Kd | 12.7333 | 3 | 3 |
| palbociclib | Homo sapiens (human) | Kd | 0.5720 | 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 | 2 |
| ekb 569 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| axitinib | Homo sapiens (human) | Kd | 16.6667 | 3 | 3 |
| temsirolimus | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| pd 184352 | Homo sapiens (human) | Kd | 10.0000 | 2 | 2 |
| on 01910 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| av 412 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| telatinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| y-39983 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| cp 547632 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| bms345541 | Homo sapiens (human) | Kd | 10.0000 | 2 | 2 |
| lenvatinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| pd 0325901 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| midostaurin | Homo sapiens (human) | Kd | 16.6667 | 3 | 3 |
| px-866 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| ripasudil | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| osi 930 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| ki 20227 | Homo sapiens (human) | Kd | 10.0000 | 2 | 2 |
| scio-469 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| cp 724714 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| 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 | 3 | 4 |
| 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 | 2 | 2 |
| cediranib | Homo sapiens (human) | Kd | 16.6667 | 3 | 3 |
| masitinib | Homo sapiens (human) | Kd | 16.6667 | 3 | 3 |
| ly-2157299 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| pazopanib | Homo sapiens (human) | Kd | 16.6667 | 3 | 3 |
| azd 6244 | Homo sapiens (human) | Kd | 16.6667 | 3 | 3 |
| su 14813 | Homo sapiens (human) | Kd | 14.0000 | 3 | 3 |
| bibw 2992 | Homo sapiens (human) | Kd | 16.6667 | 3 | 3 |
| binimetinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| sotrastaurin | Homo sapiens (human) | Kd | 30.0000 | 1 | 2 |
| 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 | 16.6667 | 3 | 3 |
| 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 | 1.4400 | 2 | 2 |
| azd 7762 | Homo sapiens (human) | Kd | 30.0000 | 1 | 2 |
| 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 | 16.6667 | 3 | 3 |
| brivanib | Homo sapiens (human) | Kd | 16.6667 | 3 | 3 |
| mp470 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| rgb 286638 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| np 031112 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| at 7519 | Homo sapiens (human) | Kd | 0.0543 | 3 | 3 |
| bms-690514 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| bi 2536 | Homo sapiens (human) | Kd | 13.9667 | 3 | 3 |
| inno-406 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| nvp-ast487 | Homo sapiens (human) | Kd | 0.9650 | 2 | 2 |
| kw 2449 | Homo sapiens (human) | Kd | 15.3875 | 3 | 4 |
| danusertib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| abt 869 | Homo sapiens (human) | Kd | 16.6667 | 3 | 3 |
| azd 8931 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| arq 197 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| azd 1152 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| pf 00299804 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| ridaforolimus | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| ch 4987655 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| 6-(5-((cyclopropylamino)carbonyl)-3-fluoro-2-methylphenyl)-n-(2,2-dimethylprpyl)-3-pyridinecarboxamide | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| cc-930 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| gw 2580 | Homo sapiens (human) | Kd | 10.0000 | 2 | 2 |
| tak 285 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| idelalisib | Homo sapiens (human) | Kd | 30.0000 | 1 | 2 |
| crizotinib | Homo sapiens (human) | Kd | 16.6667 | 3 | 3 |
| 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 | 1 |
| 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 | 30.0000 | 1 | 1 |
| GDC-0879 | Homo sapiens (human) | Kd | 10.0000 | 2 | 2 |
| 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 | 16.6667 | 3 | 3 |
| azd 1152-hqpa | Homo sapiens (human) | Kd | 16.6667 | 3 | 3 |
| nvp-tae684 | Homo sapiens (human) | Kd | 0.9000 | 2 | 2 |
| 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 | 2 |
| tak-901 | Homo sapiens (human) | Kd | 30.0000 | 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 | 4.1160 | 1 | 1 |
| ro5126766 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| fedratinib | Homo sapiens (human) | Kd | 16.4675 | 3 | 4 |
| gsk690693 | Homo sapiens (human) | Kd | 16.6667 | 3 | 3 |
| 14-methyl-20-oxa-5,7,14,26-tetraazatetracyclo(19.3.1.1(2,6).1(8,12))heptacosa-1(25),2(26),3,5,8(27),9,11,16,21,23-decaene | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| azd5438 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| pf 04217903 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| gdc 0941 | Homo sapiens (human) | Kd | 20.0000 | 3 | 4 |
| icotinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| ph 797804 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| kx-01 | Homo sapiens (human) | Kd | 30.0000 | 1 | 2 |
| plx 4720 | Homo sapiens (human) | Kd | 10.0000 | 2 | 2 |
| mk 5108 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| cx 4945 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| cudc 101 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| arry-614 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| tak 593 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| mln 8237 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| sgx 523 | Homo sapiens (human) | Kd | 16.6667 | 3 | 3 |
| 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 | 1 |
| mk-1775 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| AMG-208 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| quizartinib | Homo sapiens (human) | Kd | 16.6667 | 3 | 3 |
| at13148 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| tak 733 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| mk 2206 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| sns 314 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| lucitanib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| pf-04691502 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| n-(cyanomethyl)-4-(2-((4-(4-morpholinyl)phenyl)amino)-4-pyrimidinyl)benzamide | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| dcc-2036 | Homo sapiens (human) | Kd | 1.5620 | 1 | 1 |
| cabozantinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| defactinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| ly2584702 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| incb-018424 | Homo sapiens (human) | Kd | 16.6667 | 3 | 3 |
| 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 | 2 | 2 |
| pf 3758309 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| gdc 0980 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| azd2014 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| (5-(2,4-bis((3s)-3-methylmorpholin-4-yl)pyrido(2,3-d)pyrimidin-7-yl)-2-methoxyphenyl)methanol | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| plx4032 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| gsk 1363089 | Homo sapiens (human) | Kd | 16.6667 | 3 | 3 |
| arry-334543 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| mk 2461 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| bay 869766 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| as 703026 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| baricitinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| dabrafenib | Homo sapiens (human) | Kd | 0.1260 | 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 | 30.0000 | 1 | 1 |
| sb 1518 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| abemaciclib | Homo sapiens (human) | Kd | 0.0970 | 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 | 1.1450 | 1 | 1 |
| gilteritinib | Homo sapiens (human) | Kd | 1.9550 | 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 | 0.1120 | 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 | 2 |
| azd1208 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| vx-509 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| debio 1347 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| volitinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| osimertinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 2 |
| at 9283 | Homo sapiens (human) | Kd | 1.2870 | 1 | 1 |
| otssp167 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| chir 258 | Homo sapiens (human) | Kd | 11.3667 | 3 | 3 |
| osi 027 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| nintedanib | Homo sapiens (human) | Kd | 10.2933 | 3 | 3 |
| bay 80-6946 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| pp242 | Homo sapiens (human) | Kd | 7.9500 | 2 | 2 |
Drugs with Other Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| cyc 202 | Homo sapiens (human) | INH | 24.5000 | 1 | 1 |
| alvocidib | Homo sapiens (human) | ID50 | 0.4000 | 1 | 1 |
| olomoucine ii | Homo sapiens (human) | INH | 11.4000 | 1 | 1 |
| abemaciclib | Homo sapiens (human) | INH | 6.7000 | 1 | 1 |
| on123300 | Homo sapiens (human) | IC5 | 0.0039 | 1 | 1 |
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Structural classification of protein kinases using 3D molecular interaction field analysis of their ligand binding sites: target family landscapes.Journal of medicinal chemistry, , Jun-06, Volume: 45, Issue:12, 2002
Thio- and oxoflavopiridols, cyclin-dependent kinase 1-selective inhibitors: synthesis and biological effects.Journal of medicinal chemistry, , Nov-02, Volume: 43, Issue:22, 2000
5-Arylamino-2-methyl-4,7-dioxobenzothiazoles as inhibitors of cyclin-dependent kinase 4 and cytotoxic agents.Bioorganic & medicinal chemistry letters, , Mar-06, Volume: 10, Issue:5, 2000
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
From Structure Modification to Drug Launch: A Systematic Review of the Ongoing Development of Cyclin-Dependent Kinase Inhibitors for Multiple Cancer Therapy.Journal of medicinal chemistry, , 05-12, Volume: 65, Issue:9, 2022
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
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
Mushroom-Derived Indole Alkaloids.Journal of natural products, , 07-28, Volume: 80, Issue:7, 2017
Design, synthesis and biological evaluation of pteridine-7(8H)-one derivatives as potent and selective CDK4/6 inhibitors.Bioorganic & medicinal chemistry letters, , 11-15, Volume: 76, 2022
Ring closure strategy leads to potent RIPK3 inhibitors.European journal of medicinal chemistry, , May-05, Volume: 217, 2021
ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells.European journal of medicinal chemistry, , Jan-01, Volume: 161, 2019
Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors.Bioorganic & medicinal chemistry, , 05-01, Volume: 26, Issue:8, 2018
Novel pyrrolopyrimidines as Mps1/TTK kinase inhibitors for breast cancer.Bioorganic & medicinal chemistry, , 04-01, Volume: 25, Issue:7, 2017
Development of highly potent and selective diaminothiazole inhibitors of cyclin-dependent kinases.Journal of medicinal chemistry, , May-23, Volume: 56, Issue:10, 2013
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
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
Novel, potent and selective cyclin D1/CDK4 inhibitors: indolo[6,7-a]pyrrolo[3,4-c]carbazoles.Bioorganic & medicinal chemistry letters, , Jul-21, Volume: 13, Issue:14, 2003
Aryl[a]pyrrolo[3,4-c]carbazoles as selective cyclin D1-CDK4 inhibitors.Bioorganic & medicinal chemistry letters, , Nov-03, Volume: 13, Issue:21, 2003
Structural basis for Chk1 inhibition by UCN-01.The Journal of biological chemistry, , Nov-29, Volume: 277, Issue:48, 2002
Discovery of a marine-derived bis-indole alkaloid fascaplysin, as a new class of potent P-glycoprotein inducer and establishment of its structure-activity relationship.European journal of medicinal chemistry, , Jan-01, Volume: 107, 2016
Biphenyl-4-carboxylic acid [2-(1H-indol-3-yl)-ethyl]-methylamide (CA224), a nonplanar analogue of fascaplysin, inhibits Cdk4 and tubulin polymerization: evaluation of in vitro and in vivo anticancer activity.Journal of medicinal chemistry, , Nov-26, Volume: 57, Issue:22, 2014
Fascaplysin-inspired diindolyls as selective inhibitors of CDK4/cyclin D1.Bioorganic & medicinal chemistry, , Aug-15, Volume: 17, Issue:16, 2009
Design, synthesis and biological evaluation of new tryptamine and tetrahydro-beta-carboline-based selective inhibitors of CDK4.Bioorganic & medicinal chemistry, , Aug-15, Volume: 16, Issue:16, 2008
A common protein fold topology shared by flavonoid biosynthetic enzymes and therapeutic targets.Journal of natural products, , Volume: 69, Issue:1, 2006
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
Design, synthesis, and biological evaluation of 4-benzoylamino-1H-pyrazole-3-carboxamide derivatives as potent CDK2 inhibitors.European journal of medicinal chemistry, , Apr-05, Volume: 215, 2021
Recent advances in the development of cyclin-dependent kinase 7 inhibitors.European journal of medicinal chemistry, , Dec-01, Volume: 183, 2019
Third-generation CDK inhibitors: A review on the synthesis and binding modes of Palbociclib, Ribociclib and Abemaciclib.European journal of medicinal chemistry, , Jun-15, Volume: 172, 2019
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Discovery of 8-cyclopentyl-2-[4-(4-methyl-piperazin-1-yl)-phenylamino]-7-oxo-7,8-dihydro-pyrido[2,3-d]pyrimidine-6-carbonitrile (7x) as a potent inhibitor of cyclin-dependent kinase 4 (CDK4) and AMPK-related kinase 5 (ARK5).Journal of medicinal chemistry, , Feb-13, Volume: 57, Issue:3, 2014
Synthesis and in vitro biological evaluation of 2,6,9-trisubstituted purines targeting multiple cyclin-dependent kinases.European journal of medicinal chemistry, , Volume: 61, 2013
Design, synthesis and biological evaluation of 6-pyridylmethylaminopurines as CDK inhibitors.Bioorganic & medicinal chemistry, , Nov-15, Volume: 19, Issue:22, 2011
A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration.Journal of medicinal chemistry, , Dec-23, Volume: 53, Issue:24, 2010
Selectivity and potency of cyclin-dependent kinase inhibitors.The AAPS journal, , Mar-24, Volume: 8, Issue:1, 2006
Structural classification of protein kinases using 3D molecular interaction field analysis of their ligand binding sites: target family landscapes.Journal of medicinal chemistry, , Jun-06, Volume: 45, Issue:12, 2002
5-Arylamino-2-methyl-4,7-dioxobenzothiazoles as inhibitors of cyclin-dependent kinase 4 and cytotoxic agents.Bioorganic & medicinal chemistry letters, , Mar-06, Volume: 10, Issue:5, 2000
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Discovery of AMG 925, a FLT3 and CDK4 dual kinase inhibitor with preferential affinity for the activated state of FLT3.Journal of medicinal chemistry, , Apr-24, Volume: 57, Issue:8, 2014
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
Structural classification of protein kinases using 3D molecular interaction field analysis of their ligand binding sites: target family landscapes.Journal of medicinal chemistry, , Jun-06, Volume: 45, Issue:12, 2002
Exploiting chemical libraries, structure, and genomics in the search for kinase inhibitors.Science (New York, N.Y.), , Jul-24, Volume: 281, Issue:5376, 1998
Current progress and novel strategies that target CDK12 for drug discovery.European journal of medicinal chemistry, , Oct-05, Volume: 240, 2022
Recent Developments in the Use of Kinase Inhibitors for Management of Viral Infections.Journal of medicinal chemistry, , 01-27, Volume: 65, Issue:2, 2022
Structural classification of protein kinases using 3D molecular interaction field analysis of their ligand binding sites: target family landscapes.Journal of medicinal chemistry, , Jun-06, Volume: 45, Issue:12, 2002
Exploiting chemical libraries, structure, and genomics in the search for kinase inhibitors.Science (New York, N.Y.), , Jul-24, Volume: 281, Issue:5376, 1998
How Selective Are Pharmacological Inhibitors of Cell-Cycle-Regulating Cyclin-Dependent Kinases?Journal of medicinal chemistry, , 10-25, Volume: 61, Issue:20, 2018
5-Arylamino-2-methyl-4,7-dioxobenzothiazoles as inhibitors of cyclin-dependent kinase 4 and cytotoxic agents.Bioorganic & medicinal chemistry letters, , Mar-06, Volume: 10, Issue:5, 2000
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
How Selective Are Pharmacological Inhibitors of Cell-Cycle-Regulating Cyclin-Dependent Kinases?Journal of medicinal chemistry, , 10-25, Volume: 61, Issue:20, 2018
A triple exon-skipping luciferase reporter assay identifies a new CLK inhibitor pharmacophore.Bioorganic & medicinal chemistry letters, , 02-01, Volume: 27, Issue:3, 2017
Online informatics resources to facilitate cancer target and chemical probe discovery.RSC medicinal chemistry, , Jun-01, Volume: 11, Issue:6, 2020
Cyclin-Dependent Kinase 2 Inhibitors in Cancer Therapy: An Update.Journal of medicinal chemistry, , 05-09, Volume: 62, Issue:9, 2019
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Cyclin Dependent Kinase 9 Inhibitors for Cancer Therapy.Journal of medicinal chemistry, , 10-13, Volume: 59, Issue:19, 2016
Discovery of 8-cyclopentyl-2-[4-(4-methyl-piperazin-1-yl)-phenylamino]-7-oxo-7,8-dihydro-pyrido[2,3-d]pyrimidine-6-carbonitrile (7x) as a potent inhibitor of cyclin-dependent kinase 4 (CDK4) and AMPK-related kinase 5 (ARK5).Journal of medicinal chemistry, , Feb-13, Volume: 57, Issue:3, 2014
Comparative structural and functional studies of 4-(thiazol-5-yl)-2-(phenylamino)pyrimidine-5-carbonitrile CDK9 inhibitors suggest the basis for isotype selectivity.Journal of medicinal chemistry, , Feb-14, Volume: 56, Issue:3, 2013
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
N-(cycloalkylamino)acyl-2-aminothiazole inhibitors of cyclin-dependent kinase 2. N-[5-[[[5-(1,1-dimethylethyl)-2-oxazolyl]methyl]thio]-2-thiazolyl]-4- piperidinecarboxamide (BMS-387032), a highly efficacious and selective antitumor agent.Journal of medicinal chemistry, , Mar-25, Volume: 47, Issue:7, 2004
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Studies on cyclin-dependent kinase inhibitors: indolo-[2,3-a]pyrrolo[3,4-c]carbazoles versus bis-indolylmaleimides.Bioorganic & medicinal chemistry letters, , Nov-03, Volume: 13, Issue:21, 2003
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
Studies on cyclin-dependent kinase inhibitors: indolo-[2,3-a]pyrrolo[3,4-c]carbazoles versus bis-indolylmaleimides.Bioorganic & medicinal chemistry letters, , Nov-03, Volume: 13, Issue:21, 2003
Synthesis, structure-activity relationship, and biological studies of indolocarbazoles as potent cyclin D1-CDK4 inhibitors.Journal of medicinal chemistry, , May-22, Volume: 46, Issue:11, 2003
Current progress and novel strategies that target CDK12 for drug discovery.European journal of medicinal chemistry, , Oct-05, Volume: 240, 2022
Kinase Inhibitors as Underexplored Antiviral Agents.Journal of medicinal chemistry, , 01-27, Volume: 65, Issue:2, 2022
Recent Developments in the Use of Kinase Inhibitors for Management of Viral Infections.Journal of medicinal chemistry, , 01-27, Volume: 65, Issue:2, 2022
From Structure Modification to Drug Launch: A Systematic Review of the Ongoing Development of Cyclin-Dependent Kinase Inhibitors for Multiple Cancer Therapy.Journal of medicinal chemistry, , 05-12, Volume: 65, Issue:9, 2022
Design, synthesis, and biological evaluation of 4-benzoylamino-1H-pyrazole-3-carboxamide derivatives as potent CDK2 inhibitors.European journal of medicinal chemistry, , Apr-05, Volume: 215, 2021
Recent Developments in the Biology and Medicinal Chemistry of CDK9 Inhibitors: An Update.Journal of medicinal chemistry, , 11-25, Volume: 63, Issue:22, 2020
Online informatics resources to facilitate cancer target and chemical probe discovery.RSC medicinal chemistry, , Jun-01, Volume: 11, Issue:6, 2020
A review on flavones targeting serine/threonine protein kinases for potential anticancer drugs.Bioorganic & medicinal chemistry, , 03-01, Volume: 27, Issue:5, 2019
Recent advances in the development of cyclin-dependent kinase 7 inhibitors.European journal of medicinal chemistry, , Dec-01, Volume: 183, 2019
Third-generation CDK inhibitors: A review on the synthesis and binding modes of Palbociclib, Ribociclib and Abemaciclib.European journal of medicinal chemistry, , Jun-15, Volume: 172, 2019
Structural insights of cyclin dependent kinases: Implications in design of selective inhibitors.European journal of medicinal chemistry, , Dec-15, Volume: 142, 2017
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Feeling Nature's PAINS: Natural Products, Natural Product Drugs, and Pan Assay Interference Compounds (PAINS).Journal of natural products, , Mar-25, Volume: 79, Issue:3, 2016
Cyclin Dependent Kinase 9 Inhibitors for Cancer Therapy.Journal of medicinal chemistry, , 10-13, Volume: 59, Issue:19, 2016
Discovery of 8-cyclopentyl-2-[4-(4-methyl-piperazin-1-yl)-phenylamino]-7-oxo-7,8-dihydro-pyrido[2,3-d]pyrimidine-6-carbonitrile (7x) as a potent inhibitor of cyclin-dependent kinase 4 (CDK4) and AMPK-related kinase 5 (ARK5).Journal of medicinal chemistry, , Feb-13, Volume: 57, Issue:3, 2014
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
Selectivity and potency of cyclin-dependent kinase inhibitors.The AAPS journal, , Mar-24, Volume: 8, Issue:1, 2006
Structure-based design of a new class of highly selective aminoimidazo[1,2-a]pyridine-based inhibitors of cyclin dependent kinases.Bioorganic & medicinal chemistry letters, , Apr-01, Volume: 15, Issue:7, 2005
Synthesis and biological activity of N-aryl-2-aminothiazoles: potent pan inhibitors of cyclin-dependent kinases.Bioorganic & medicinal chemistry letters, , Jun-07, Volume: 14, Issue:11, 2004
1H-Pyrazolo[3,4-b]pyridine inhibitors of cyclin-dependent kinases.Bioorganic & medicinal chemistry letters, , Mar-24, Volume: 13, Issue:6, 2003
Structure-based design and synthesis of 2-benzylidene-benzofuran-3-ones as flavopiridol mimics.Journal of medicinal chemistry, , Apr-25, Volume: 45, Issue:9, 2002
Discovery of aminothiazole inhibitors of cyclin-dependent kinase 2: synthesis, X-ray crystallographic analysis, and biological activities.Journal of medicinal chemistry, , Aug-29, Volume: 45, Issue:18, 2002
Thio- and oxoflavopiridols, cyclin-dependent kinase 1-selective inhibitors: synthesis and biological effects.Journal of medicinal chemistry, , Nov-02, Volume: 43, Issue:22, 2000
Cyclin-dependent kinase inhibitors: useful targets in cell cycle regulation.Journal of medicinal chemistry, , Jan-13, Volume: 43, Issue:1, 2000
Cinnamaldehydes inhibit cyclin dependent kinase 4/cyclin D1.Bioorganic & medicinal chemistry letters, , Aug-21, Volume: 10, Issue:16, 2000
Structure-activity relationship studies of flavopiridol analogues.Bioorganic & medicinal chemistry letters, , May-15, Volume: 10, Issue:10, 2000
How Selective Are Pharmacological Inhibitors of Cell-Cycle-Regulating Cyclin-Dependent Kinases?Journal of medicinal chemistry, , 10-25, Volume: 61, Issue:20, 2018
Discovery of 8-cyclopentyl-2-[4-(4-methyl-piperazin-1-yl)-phenylamino]-7-oxo-7,8-dihydro-pyrido[2,3-d]pyrimidine-6-carbonitrile (7x) as a potent inhibitor of cyclin-dependent kinase 4 (CDK4) and AMPK-related kinase 5 (ARK5).Journal of medicinal chemistry, , Feb-13, Volume: 57, Issue:3, 2014
Selectivity and potency of cyclin-dependent kinase inhibitors.The AAPS journal, , Mar-24, Volume: 8, Issue:1, 2006
How Selective Are Pharmacological Inhibitors of Cell-Cycle-Regulating Cyclin-Dependent Kinases?Journal of medicinal chemistry, , 10-25, Volume: 61, Issue:20, 2018
Novel, potent and selective cyclin D1/CDK4 inhibitors: indolo[6,7-a]pyrrolo[3,4-c]carbazoles.Bioorganic & medicinal chemistry letters, , Jul-21, Volume: 13, Issue:14, 2003
Studies on cyclin-dependent kinase inhibitors: indolo-[2,3-a]pyrrolo[3,4-c]carbazoles versus bis-indolylmaleimides.Bioorganic & medicinal chemistry letters, , Nov-03, Volume: 13, Issue:21, 2003
Aryl[a]pyrrolo[3,4-c]carbazoles as selective cyclin D1-CDK4 inhibitors.Bioorganic & medicinal chemistry letters, , Nov-03, Volume: 13, Issue:21, 2003
Synthesis, structure-activity relationship, and biological studies of indolocarbazoles as potent cyclin D1-CDK4 inhibitors.Journal of medicinal chemistry, , May-22, Volume: 46, Issue:11, 2003
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
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
Radiosynthesis and radiopharmacological evaluation of cyclin-dependent kinase 4 (Cdk4) inhibitors.European journal of medicinal chemistry, , Volume: 45, Issue:2, 2010
Pyrido[2,3-d]pyrimidin-7-one inhibitors of cyclin-dependent kinases.Journal of medicinal chemistry, , Nov-30, Volume: 43, Issue:24, 2000
Design, synthesis and biological evaluation of pteridine-7(8H)-one derivatives as potent and selective CDK4/6 inhibitors.Bioorganic & medicinal chemistry letters, , 11-15, Volume: 76, 2022
Kinase Inhibitors as Underexplored Antiviral Agents.Journal of medicinal chemistry, , 01-27, Volume: 65, Issue:2, 2022
Recent Developments in the Use of Kinase Inhibitors for Management of Viral Infections.Journal of medicinal chemistry, , 01-27, Volume: 65, Issue:2, 2022
FDA-approved pyrimidine-fused bicyclic heterocycles for cancer therapy: Synthesis and clinical application.European journal of medicinal chemistry, , Mar-15, Volume: 214, 2021
Design, synthesis, and biological evaluation of 4-benzoylamino-1H-pyrazole-3-carboxamide derivatives as potent CDK2 inhibitors.European journal of medicinal chemistry, , Apr-05, Volume: 215, 2021
Discovery of a novel covalent CDK4/6 inhibitor based on palbociclib scaffold.European journal of medicinal chemistry, , Jul-05, Volume: 219, 2021
Discovery of a novel series of imidazo[1',2':1,6]pyrido[2,3-d]pyrimidin derivatives as potent cyclin-dependent kinase 4/6 inhibitors.European journal of medicinal chemistry, , May-01, Volume: 193, 2020
Online informatics resources to facilitate cancer target and chemical probe discovery.RSC medicinal chemistry, , Jun-01, Volume: 11, Issue:6, 2020
Selective CDK6 degradation mediated by cereblon, VHL, and novel IAP-recruiting PROTACs.Bioorganic & medicinal chemistry letters, , 05-01, Volume: 30, Issue:9, 2020
[no title available]European journal of medicinal chemistry, , Mar-01, Volume: 165, 2019
Third-generation CDK inhibitors: A review on the synthesis and binding modes of Palbociclib, Ribociclib and Abemaciclib.European journal of medicinal chemistry, , Jun-15, Volume: 172, 2019
How Selective Are Pharmacological Inhibitors of Cell-Cycle-Regulating Cyclin-Dependent Kinases?Journal of medicinal chemistry, , 10-25, Volume: 61, Issue:20, 2018
Highly Potent, Selective, and Orally Bioavailable 4-Thiazol-N-(pyridin-2-yl)pyrimidin-2-amine Cyclin-Dependent Kinases 4 and 6 Inhibitors as Anticancer Drug Candidates: Design, Synthesis, and Evaluation.Journal of medicinal chemistry, , 03-09, Volume: 60, Issue:5, 2017
Structural insights of cyclin dependent kinases: Implications in design of selective inhibitors.European journal of medicinal chemistry, , Dec-15, Volume: 142, 2017
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
New palbociclib analogues modified at the terminal piperazine ring and their anticancer activities.European journal of medicinal chemistry, , Oct-21, Volume: 122, 2016
5-Substituted 3-isopropyl-7-[4-(2-pyridyl)benzyl]amino-1(2)H-pyrazolo[4,3-d]pyrimidines with anti-proliferative activity as potent and selective inhibitors of cyclin-dependent kinases.European journal of medicinal chemistry, , Mar-03, Volume: 110, 2016
Cyclin Dependent Kinase 9 Inhibitors for Cancer Therapy.Journal of medicinal chemistry, , 10-13, Volume: 59, Issue:19, 2016
Cyclin dependent kinase (CDK) inhibitors as anticancer drugs.Bioorganic & medicinal chemistry letters, , Sep-01, Volume: 25, Issue:17, 2015
Discovery of AMG 925, a FLT3 and CDK4 dual kinase inhibitor with preferential affinity for the activated state of FLT3.Journal of medicinal chemistry, , Apr-24, Volume: 57, Issue:8, 2014
Discovery of 8-cyclopentyl-2-[4-(4-methyl-piperazin-1-yl)-phenylamino]-7-oxo-7,8-dihydro-pyrido[2,3-d]pyrimidine-6-carbonitrile (7x) as a potent inhibitor of cyclin-dependent kinase 4 (CDK4) and AMPK-related kinase 5 (ARK5).Journal of medicinal chemistry, , Feb-13, Volume: 57, Issue:3, 2014
Toward the development of innovative bifunctional agents to induce differentiation and to promote apoptosis in leukemia: clinical candidates and perspectives.Journal of medicinal chemistry, , Oct-14, Volume: 53, Issue:19, 2010
Radiosynthesis and radiopharmacological evaluation of cyclin-dependent kinase 4 (Cdk4) inhibitors.European journal of medicinal chemistry, , Volume: 45, Issue:2, 2010
Discovery of a potent and selective inhibitor of cyclin-dependent kinase 4/6.Journal of medicinal chemistry, , Apr-07, Volume: 48, Issue:7, 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 synthesis and SAR of 2-amino-pyrrolo[2,3-d]pyrimidines: a new class of Aurora-A kinase inhibitors.Bioorganic & medicinal chemistry letters, , Nov-15, Volume: 16, Issue:22, 2006
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
Structural determinants of CDK4 inhibition and design of selective ATP competitive inhibitors.Chemistry & biology, , Volume: 11, Issue:4, 2004
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases.Proceedings of the National Academy of Sciences of the United States of America, , Dec-18, Volume: 104, Issue:51, 2007
(6,7-Dimethoxy-2,4-dihydroindeno[1,2-c]pyrazol-3-yl)phenylamines: platelet-derived growth factor receptor tyrosine kinase inhibitors with broad antiproliferative activity against tumor cells.Journal of medicinal chemistry, , Dec-29, Volume: 48, Issue:26, 2005
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
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
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
Semi-synthetic aristolactams--inhibitors of CDK2 enzyme.Bioorganic & medicinal chemistry letters, , Feb-15, Volume: 20, Issue:4, 2010
New potential antitumor compounds from the plant Aristolochia manshuriensis as inhibitors of the CDK2 enzyme.Bioorganic & medicinal chemistry letters, , Feb-15, Volume: 20, Issue:4, 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
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
Lessons Learned from Past Cyclin-Dependent Kinase Drug Discovery Efforts.Journal of medicinal chemistry, , 05-12, Volume: 65, Issue:9, 2022
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Cyclin Dependent Kinase 9 Inhibitors for Cancer Therapy.Journal of medicinal chemistry, , 10-13, Volume: 59, Issue:19, 2016
From Structure Modification to Drug Launch: A Systematic Review of the Ongoing Development of Cyclin-Dependent Kinase Inhibitors for Multiple Cancer Therapy.Journal of medicinal chemistry, , 05-12, Volume: 65, Issue:9, 2022
Design, synthesis, and biological evaluation of 4-benzoylamino-1H-pyrazole-3-carboxamide derivatives as potent CDK2 inhibitors.European journal of medicinal chemistry, , Apr-05, Volume: 215, 2021
Recent Developments in the Biology and Medicinal Chemistry of CDK9 Inhibitors: An Update.Journal of medicinal chemistry, , 11-25, Volume: 63, Issue:22, 2020
Online informatics resources to facilitate cancer target and chemical probe discovery.RSC medicinal chemistry, , Jun-01, Volume: 11, Issue:6, 2020
Cyclin-Dependent Kinase 2 Inhibitors in Cancer Therapy: An Update.Journal of medicinal chemistry, , 05-09, Volume: 62, Issue:9, 2019
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Cyclin Dependent Kinase 9 Inhibitors for Cancer Therapy.Journal of medicinal chemistry, , 10-13, Volume: 59, Issue:19, 2016
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
Identification of N-(4-piperidinyl)-4-(2,6-dichlorobenzoylamino)-1H-pyrazole-3-carboxamide (AT7519), a novel cyclin dependent kinase inhibitor using fragment-based X-ray crystallography and structure based drug design.Journal of medicinal chemistry, , Aug-28, Volume: 51, Issue:16, 2008
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
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
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
Cyclin-Dependent Kinase 2 Inhibitors in Cancer Therapy: An Update.Journal of medicinal chemistry, , 05-09, Volume: 62, Issue:9, 2019
How Selective Are Pharmacological Inhibitors of Cell-Cycle-Regulating Cyclin-Dependent Kinases?Journal of medicinal chemistry, , 10-25, Volume: 61, Issue:20, 2018
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
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Imidazoles: SAR and development of a potent class of cyclin-dependent kinase inhibitors.Bioorganic & medicinal chemistry letters, , Oct-15, Volume: 18, Issue:20, 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 review on flavones targeting serine/threonine protein kinases for potential anticancer drugs.Bioorganic & medicinal chemistry, , 03-01, Volume: 27, Issue:5, 2019
[no title available]Journal of medicinal chemistry, , 02-22, Volume: 61, Issue:4, 2018
Cyclin Dependent Kinase 9 Inhibitors for Cancer Therapy.Journal of medicinal chemistry, , 10-13, Volume: 59, Issue:19, 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
How Selective Are Pharmacological Inhibitors of Cell-Cycle-Regulating Cyclin-Dependent Kinases?Journal of medicinal chemistry, , 10-25, Volume: 61, Issue:20, 2018
Discovery of 8-cyclopentyl-2-[4-(4-methyl-piperazin-1-yl)-phenylamino]-7-oxo-7,8-dihydro-pyrido[2,3-d]pyrimidine-6-carbonitrile (7x) as a potent inhibitor of cyclin-dependent kinase 4 (CDK4) and AMPK-related kinase 5 (ARK5).Journal of medicinal chemistry, , Feb-13, Volume: 57, Issue:3, 2014
Selectivity and potency of cyclin-dependent kinase inhibitors.The AAPS journal, , Mar-24, Volume: 8, Issue:1, 2006
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
Cyclin dependent kinase (CDK) inhibitors as anticancer drugs: Recent advances (2015-2019).Bioorganic & medicinal chemistry letters, , 10-15, Volume: 29, Issue:20, 2019
A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration.Journal of medicinal chemistry, , Dec-23, Volume: 53, Issue:24, 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
FDA-approved pyrimidine-fused bicyclic heterocycles for cancer therapy: Synthesis and clinical application.European journal of medicinal chemistry, , Mar-15, Volume: 214, 2021
First orally bioavailable prodrug of proteolysis targeting chimera (PROTAC) degrades cyclin-dependent kinases 2/4/6 in vivo.European journal of medicinal chemistry, , Jan-01, Volume: 209, 2021
Design, synthesis, and biological evaluation of 4-benzoylamino-1H-pyrazole-3-carboxamide derivatives as potent CDK2 inhibitors.European journal of medicinal chemistry, , Apr-05, Volume: 215, 2021
Design, synthesis, and biological evaluation of 2,6,7-substituted pyrrolo[2,3-d]pyrimidines as cyclin dependent kinase inhibitor in pancreatic cancer cells.Bioorganic & medicinal chemistry letters, , 02-01, Volume: 33, 2021
Novel cyclin-dependent kinase 9 (CDK9) inhibitor with suppression of cancer stemness activity against non-small-cell lung cancer.European journal of medicinal chemistry, , Nov-01, Volume: 181, 2019
Third-generation CDK inhibitors: A review on the synthesis and binding modes of Palbociclib, Ribociclib and Abemaciclib.European journal of medicinal chemistry, , Jun-15, Volume: 172, 2019
How Selective Are Pharmacological Inhibitors of Cell-Cycle-Regulating Cyclin-Dependent Kinases?Journal of medicinal chemistry, , 10-25, Volume: 61, Issue:20, 2018
Discovery of N1-(4-((7-Cyclopentyl-6-(dimethylcarbamoyl)-7 H-pyrrolo[2,3- d]pyrimidin-2-yl)amino)phenyl)- N8-hydroxyoctanediamide as a Novel Inhibitor Targeting Cyclin-dependent Kinase 4/9 (CDK4/9) and Histone Deacetlyase1 (HDAC1) against Malignant CancerJournal of medicinal chemistry, , 04-12, Volume: 61, Issue:7, 2018
Structural insights of cyclin dependent kinases: Implications in design of selective inhibitors.European journal of medicinal chemistry, , Dec-15, Volume: 142, 2017
Discovery of a highly potent, selective and novel CDK9 inhibitor as an anticancer drug candidate.Bioorganic & medicinal chemistry letters, , 08-01, Volume: 27, Issue:15, 2017
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
[no title available],
Lessons Learned from Past Cyclin-Dependent Kinase Drug Discovery Efforts.Journal of medicinal chemistry, , 05-12, Volume: 65, Issue:9, 2022
From Structure Modification to Drug Launch: A Systematic Review of the Ongoing Development of Cyclin-Dependent Kinase Inhibitors for Multiple Cancer Therapy.Journal of medicinal chemistry, , 05-12, Volume: 65, Issue:9, 2022
Development and Therapeutic Potential of NUAKs Inhibitors.Journal of medicinal chemistry, , 01-14, Volume: 64, Issue:1, 2021
Recent Developments in the Biology and Medicinal Chemistry of CDK9 Inhibitors: An Update.Journal of medicinal chemistry, , 11-25, Volume: 63, Issue:22, 2020
Cyclin-Dependent Kinase 2 Inhibitors in Cancer Therapy: An Update.Journal of medicinal chemistry, , 05-09, Volume: 62, Issue:9, 2019
Recent development of CDK inhibitors: An overview of CDK/inhibitor co-crystal structures.European journal of medicinal chemistry, , Feb-15, Volume: 164, 2019
Cyclin Dependent Kinase 9 Inhibitors for Cancer Therapy.Journal of medicinal chemistry, , 10-13, Volume: 59, Issue:19, 2016
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
[no title available]Journal of medicinal chemistry, , 05-12, Volume: 65, Issue:9, 2022
Design, synthesis, and biological evaluation of 4-benzoylamino-1H-pyrazole-3-carboxamide derivatives as potent CDK2 inhibitors.European journal of medicinal chemistry, , Apr-05, Volume: 215, 2021
Comprehensive review for anticancer hybridized multitargeting HDAC inhibitors.European journal of medicinal chemistry, , Jan-01, Volume: 209, 2021
Discovery of a novel series of imidazo[1',2':1,6]pyrido[2,3-d]pyrimidin derivatives as potent cyclin-dependent kinase 4/6 inhibitors.European journal of medicinal chemistry, , May-01, Volume: 193, 2020
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 6-(2-(dimethylamino)ethyl)-N-(5-fluoro-4-(4-fluoro-1-isopropyl-2-methyl-1H-benzo[d]imidazole-6-yl)pyrimidin-2-yl)-5,6,7,8-tetrahydro-1,6-naphthyridin-2-amine as a highly potent cyclin-dependent kinase 4/6 inhibitor for treatment of cancer.European journal of medicinal chemistry, , Sep-15, Volume: 178, 2019
Third-generation CDK inhibitors: A review on the synthesis and binding modes of Palbociclib, Ribociclib and Abemaciclib.European journal of medicinal chemistry, , Jun-15, Volume: 172, 2019
Design, synthesis and biological evaluation of tetrahydronaphthyridine derivatives as bioavailable CDK4/6 inhibitors for cancer therapy.European journal of medicinal chemistry, , Mar-25, Volume: 148, 2018
How Selective Are Pharmacological Inhibitors of Cell-Cycle-Regulating Cyclin-Dependent Kinases?Journal of medicinal chemistry, , 10-25, Volume: 61, Issue:20, 2018
Design and synthesis of 4-(2,3-dihydro-1H-benzo[d]pyrrolo[1,2-a]imidazol-7-yl)-N-(5-(piperazin-1-ylmethyl)pyridine-2-yl)pyrimidin-2-amine as a highly potent and selective cyclin-dependent kinases 4 and 6 inhibitors and the discovery of structure-activity Bioorganic & medicinal chemistry letters, , 03-01, Volume: 28, Issue:5, 2018
Discovery of a class of diheteroaromatic amines as orally bioavailable CDK1/4/6 inhibitors.Bioorganic & medicinal chemistry letters, , 12-01, Volume: 27, Issue:23, 2017
Structural insights of cyclin dependent kinases: Implications in design of selective inhibitors.European journal of medicinal chemistry, , Dec-15, Volume: 142, 2017
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Synthesis, biological evaluation and molecular modeling of a novel series of 7-azaindole based tri-heterocyclic compounds as potent CDK2/Cyclin E inhibitors.European journal of medicinal chemistry, , Jan-27, Volume: 108, 2016
Cyclin Dependent Kinase 9 Inhibitors for Cancer Therapy.Journal of medicinal chemistry, , 10-13, Volume: 59, Issue:19, 2016
Cyclin dependent kinase (CDK) inhibitors as anticancer drugs.Bioorganic & medicinal chemistry letters, , Sep-01, Volume: 25, Issue:17, 2015
Recent Developments in the Use of Kinase Inhibitors for Management of Viral Infections.Journal of medicinal chemistry, , 01-27, Volume: 65, Issue:2, 2022
[no title available]Journal of medicinal chemistry, , 10-14, Volume: 64, Issue:19, 2021
3,5,7-Substituted Pyrazolo[4,3- d]pyrimidine Inhibitors of Cyclin-Dependent Kinases and Their Evaluation in Lymphoma Models.Journal of medicinal chemistry, , 05-09, Volume: 62, Issue:9, 2019
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Synthesis, biological evaluation and molecular modeling of a novel series of 7-azaindole based tri-heterocyclic compounds as potent CDK2/Cyclin E inhibitors.European journal of medicinal chemistry, , Jan-27, Volume: 108, 2016
5-Substituted 3-isopropyl-7-[4-(2-pyridyl)benzyl]amino-1(2)H-pyrazolo[4,3-d]pyrimidines with anti-proliferative activity as potent and selective inhibitors of cyclin-dependent kinases.European journal of medicinal chemistry, , Mar-03, Volume: 110, 2016
CDK7 Inhibitors in Cancer Therapy: The Sweet Smell of Success?Journal of medicinal chemistry, , 07-23, Volume: 63, Issue:14, 2020
Cyclin dependent kinase (CDK) inhibitors as anticancer drugs: Recent advances (2015-2019).Bioorganic & medicinal chemistry letters, , 10-15, Volume: 29, Issue:20, 2019
Synthesis, biological evaluation and molecular modeling of a novel series of 7-azaindole based tri-heterocyclic compounds as potent CDK2/Cyclin E inhibitors.European journal of medicinal chemistry, , Jan-27, Volume: 108, 2016
5-Substituted 3-isopropyl-7-[4-(2-pyridyl)benzyl]amino-1(2)H-pyrazolo[4,3-d]pyrimidines with anti-proliferative activity as potent and selective inhibitors of cyclin-dependent kinases.European journal of medicinal chemistry, , Mar-03, Volume: 110, 2016
Selectivity and potency of cyclin-dependent kinase inhibitors.The AAPS journal, , Mar-24, Volume: 8, Issue:1, 2006
Thio- and oxoflavopiridols, cyclin-dependent kinase 1-selective inhibitors: synthesis and biological effects.Journal of medicinal chemistry, , Nov-02, Volume: 43, Issue:22, 2000
Development and Therapeutic Potential of NUAKs Inhibitors.Journal of medicinal chemistry, , 01-14, Volume: 64, Issue:1, 2021
How Selective Are Pharmacological Inhibitors of Cell-Cycle-Regulating Cyclin-Dependent Kinases?Journal of medicinal chemistry, , 10-25, Volume: 61, Issue:20, 2018
Discovery of 8-cyclopentyl-2-[4-(4-methyl-piperazin-1-yl)-phenylamino]-7-oxo-7,8-dihydro-pyrido[2,3-d]pyrimidine-6-carbonitrile (7x) as a potent inhibitor of cyclin-dependent kinase 4 (CDK4) and AMPK-related kinase 5 (ARK5).Journal of medicinal chemistry, , Feb-13, Volume: 57, Issue:3, 2014
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
FLT3 Inhibitors in Acute Myeloid Leukemia: Challenges and Recent Developments in Overcoming Resistance.Journal of medicinal chemistry, , 03-25, Volume: 64, Issue:6, 2021
Discovery of AMG 925, a FLT3 and CDK4 dual kinase inhibitor with preferential affinity for the activated state of FLT3.Journal of medicinal chemistry, , Apr-24, Volume: 57, Issue:8, 2014
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
Novel arylazopyrazole inhibitors of cyclin-dependent kinases.Bioorganic & medicinal chemistry, , May-01, Volume: 23, Issue:9, 2015
Arylazopyrazole AAP1742 inhibits CDKs and induces apoptosis in multiple myeloma cells via Mcl-1 downregulation.Chemical biology & drug design, , Volume: 84, Issue:4, 2014
4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects.Journal of medicinal chemistry, , Nov-02, Volume: 49, Issue:22, 2006
How Selective Are Pharmacological Inhibitors of Cell-Cycle-Regulating Cyclin-Dependent Kinases?Journal of medicinal chemistry, , 10-25, Volume: 61, Issue:20, 2018
Synthesis and activity of quinolinyl-methylene-thiazolinones as potent and selective cyclin-dependent kinase 1 inhibitors.Bioorganic & medicinal chemistry letters, , Apr-15, Volume: 17, Issue:8, 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
Design, synthesis, and evaluation of indolinones as triple angiokinase inhibitors and the discovery of a highly specific 6-methoxycarbonyl-substituted indolinone (BIBF 1120).Journal of medicinal chemistry, , Jul-23, Volume: 52, Issue:14, 2009
BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy.Cancer research, , Jun-15, Volume: 68, Issue:12, 2008
Enables
This protein enables 6 target(s):
| Target | Category | Definition |
|---|
| cyclin-dependent protein serine/threonine kinase activity | molecular function | Cyclin-dependent catalysis of the reactions: ATP + protein serine = ADP + protein serine phosphate, and ATP + protein threonine = ADP + protein threonine phosphate. [GOC:pr, GOC:rn, PMID:7877684, PMID:9841670] |
| 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] |
| cyclin-dependent protein serine/threonine kinase regulator activity | molecular function | Modulates the activity of a cyclin-dependent protein serine/threonine kinase, enzymes of the protein kinase family that are regulated through association with cyclins and other proteins. [GOC:pr, GOC:rn, PMID:7877684, PMID:9442875] |
| cyclin binding | molecular function | Binding to cyclins, proteins whose levels in a cell varies markedly during the cell cycle, rising steadily until mitosis, then falling abruptly to zero. As cyclins reach a threshold level, they are thought to drive cells into G2 phase and thus to mitosis. [GOC:ai] |
| 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 6 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] |
| nucleolus | cellular component | A small, dense body one or more of which are present in the nucleus of eukaryotic cells. It is rich in RNA and protein, is not bounded by a limiting membrane, and is not seen during mitosis. Its prime function is the transcription of the nucleolar DNA into 45S ribosomal-precursor RNA, the processing of this RNA into 5.8S, 18S, and 28S components of ribosomal RNA, and the association of these components with 5S RNA and proteins synthesized outside the nucleolus. This association results in the formation of ribonucleoprotein precursors; these pass into the cytoplasm and mature into the 40S and 60S subunits of the ribosome. [ISBN:0198506732] |
| 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] |
| bicellular tight junction | cellular component | An occluding cell-cell junction that is composed of a branching network of sealing strands that completely encircles the apical end of each cell in an epithelial sheet; the outer leaflets of the two interacting plasma membranes are seen to be tightly apposed where sealing strands are present. Each sealing strand is composed of a long row of transmembrane adhesion proteins embedded in each of the two interacting plasma membranes. [GOC:mah, ISBN:0815332181] |
| nuclear membrane | cellular component | Either of the lipid bilayers that surround the nucleus and form the nuclear envelope; excludes the intermembrane space. [GOC:mah, GOC:pz] |
Active In
This protein is active in 2 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] |
| 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 6 target(s):
| Target | Category | Definition |
|---|
| cyclin D1-CDK4 complex | cellular component | A protein complex consisting of cyclin D1 and cyclin-dependent kinase 4 (CDK4). Cyclins are characterized by periodicity in protein abundance throughout the cell cycle. Cyclin-dependent kinases represent a family of serine/threonine protein kinases that become active upon binding to a cyclin regulatory partner. [GOC:so, PMID:15935619] |
| cyclin D2-CDK4 complex | cellular component | A protein complex consisting of cyclin D2 and cyclin-dependent kinase 4 (CDK4). Cyclins are characterized by periodicity in protein abundance throughout the cell cycle. Cyclin-dependent kinases represent a family of serine/threonine protein kinases that become active upon binding to a cyclin regulatory partner. [GOC:so, PMID:15935619] |
| cyclin D3-CDK4 complex | cellular component | A protein complex consisting of cyclin D3 and cyclin-dependent kinase 4 (CDK4). Cyclins are characterized by periodicity in protein abundance throughout the cell cycle. Cyclin-dependent kinases represent a family of serine/threonine protein kinases that become active upon binding to a cyclin regulatory partner. [GOC:so, PMID:15935619] |
| cyclin-dependent protein kinase holoenzyme complex | cellular component | Cyclin-dependent protein kinases (CDKs) are enzyme complexes that contain a kinase catalytic subunit associated with a regulatory cyclin partner. [GOC:krc, PMID:11602261] |
| chromatin | cellular component | The ordered and organized complex of DNA, protein, and sometimes RNA, that forms the chromosome. [GOC:elh, PMID:20404130] |
| transcription regulator complex | cellular component | A protein complex that is capable of associating with DNA by direct binding, or via other DNA-binding proteins or complexes, and regulating transcription. [GOC:jl] |
Involved In
This protein is involved in 18 target(s):
| Target | Category | Definition |
|---|
| G1/S transition of mitotic cell cycle | biological process | The mitotic cell cycle transition by which a cell in G1 commits to S phase. The process begins with the build up of G1 cyclin-dependent kinase (G1 CDK), resulting in the activation of transcription of G1 cyclins. The process ends with the positive feedback of the G1 cyclins on the G1 CDK which commits the cell to S phase, in which DNA replication is initiated. [GOC:mtg_cell_cycle] |
| protein phosphorylation | biological process | The process of introducing a phosphate group on to a protein. [GOC:hb] |
| positive regulation of cell population proliferation | biological process | Any process that activates or increases the rate or extent of cell proliferation. [GOC:go_curators] |
| response to xenobiotic stimulus | biological process | Any process that results in a change in state or activity of a cell or an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a stimulus from a xenobiotic, a compound foreign to the organim exposed to it. It may be synthesized by another organism (like ampicilin) or it can be a synthetic chemical. [GOC:jl, GOC:krc] |
| regulation of gene expression | biological process | Any process that modulates 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] |
| positive regulation of G2/M transition of mitotic cell cycle | biological process | Any signaling pathway that activates or increases the activity of a cell cycle cyclin-dependent protein kinase to modulate the switch from G2 phase to M phase of the mitotic cell cycle. [GOC:dph, GOC:mtg_cell_cycle, GOC:tb] |
| positive regulation of fibroblast proliferation | biological process | Any process that activates or increases the frequency, rate or extent of multiplication or reproduction of fibroblast cells. [GOC:jid] |
| cell division | biological process | The process resulting in division and partitioning of components of a cell to form more cells; may or may not be accompanied by the physical separation of a cell into distinct, individually membrane-bounded daughter cells. [GOC:di, GOC:go_curators, GOC:pr] |
| regulation of cell cycle | biological process | Any process that modulates the rate or extent of progression through the cell cycle. [GOC:ai, GOC:dph, GOC:tb] |
| regulation of transcription initiation by RNA polymerase II | biological process | Any process that modulates the rate, frequency or extent of a process involved in starting transcription from an RNA polymerase II promoter. [GOC:dph, GOC:tb, GOC:txnOH] |
| regulation of type B pancreatic cell proliferation | biological process | Any process that modulates the frequency, rate or extent of type B pancreatic cell proliferation. [GOC:dph] |
| cellular response to lipopolysaccharide | biological process | Any process that results in a change in state or activity of a cell (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a lipopolysaccharide stimulus; lipopolysaccharide is a major component of the cell wall of gram-negative bacteria. [GOC:mah] |
| cellular response to interleukin-4 | 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-4 stimulus. [GOC:mah] |
| cellular response to phorbol 13-acetate 12-myristate | 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 phorbol 13-acetate 12-myristate stimulus. [GO_REF:0000071, GOC:TermGenie, PMID:2200903] |
| cellular response to ionomycin | 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 ionomycin stimulus. [GO_REF:0000071, GOC:TermGenie, PMID:17516843] |
| response to organic substance | biological process | Any process that results in a change in state or activity of a cell or an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of an organic substance stimulus. [GOC:sm, PMID:23356676] |
| regulation of G2/M transition of mitotic cell cycle | biological process | Any signaling pathway that modulates the activity of a cell cycle cyclin-dependent protein kinase to modulate the switch from G2 phase to M phase of the mitotic cell cycle. [GOC:mtg_cell_cycle, PMID:17329565] |
| signal transduction | biological process | The cellular process in which a signal is conveyed to trigger a change in the activity or state of a cell. Signal transduction begins with reception of a signal (e.g. a ligand binding to a receptor or receptor activation by a stimulus such as light), or for signal transduction in the absence of ligand, signal-withdrawal or the activity of a constitutively active receptor. Signal transduction ends with regulation of a downstream cellular process, e.g. regulation of transcription or regulation of a metabolic process. Signal transduction covers signaling from receptors located on the surface of the cell and signaling via molecules located within the cell. For signaling between cells, signal transduction is restricted to events at and within the receiving cell. [GOC:go_curators, GOC:mtg_signaling_feb11] |