Proteins > cAMP-dependent protein kinase catalytic subunit gamma
Page last updated: 2024-08-07 16:12:52
cAMP-dependent protein kinase catalytic subunit gamma
A cAMP-dependent protein kinase catalytic subunit gamma that is encoded in the genome of human. [PRO:DNx, UniProtKB:P22612]
Synonyms
PKA C-gamma;
EC 2.7.11.11
Research
Bioassay Publications (41)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 5 (12.20) | 18.2507 |
| 2000's | 30 (73.17) | 29.6817 |
| 2010's | 4 (9.76) | 24.3611 |
| 2020's | 2 (4.88) | 2.80 |
Compounds (206)
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 | 30.0000 | 1 | 1 |
| triciribine phosphate | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| picropodophyllin | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| gefitinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| perifosine | Homo sapiens (human) | Kd | 30.0000 | 1 | 2 |
| vatalanib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| ruboxistaurin | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| canertinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| cyc 202 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| enzastaurin | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| lapatinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| sorafenib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| s 1033 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| xl147 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| bms 387032 | Homo sapiens (human) | Kd | 30.0000 | 1 | 2 |
| sf 2370 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| tandutinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 2 |
| dasatinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| 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 | 30.0000 | 1 | 1 |
| imd 0354 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| alvocidib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| bosutinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| su 11248 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| palbociclib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| everolimus | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| axitinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| temsirolimus | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| on 01910 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| av 412 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| telatinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| y-39983 | Homo sapiens (human) | Kd | 30.0000 | 1 | 2 |
| cp 547632 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| lenvatinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| pd 0325901 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| midostaurin | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| px-866 | Homo sapiens (human) | Kd | 0.0070 | 1 | 1 |
| ripasudil | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| scio-469 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| cp 724714 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| hmn-214 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| tivozanib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| tofacitinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| masitinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| ly-2157299 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| pazopanib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| su 14813 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| bibw 2992 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| binimetinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| sotrastaurin | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| aee 788 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| saracatinib | Homo sapiens (human) | Kd | 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 | 30.0000 | 1 | 1 |
| 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 |
| azd 7762 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| regorafenib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| brivanib | 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 | 30.0000 | 1 | 1 |
| bms-690514 | Homo sapiens (human) | Kd | 30.0000 | 1 | 2 |
| bi 2536 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| inno-406 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| danusertib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| azd 8931 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| azd 1152 | 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 | 49.2780 | 1 | 1 |
| cc-930 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| tak 285 | Homo sapiens (human) | Kd | 30.0000 | 1 | 2 |
| idelalisib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| crizotinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| osi 906 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| fostamatinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| trametinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| mln8054 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| pf-562,271 | Homo sapiens (human) | Kd | 30.0000 | 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 | 2 |
| bgt226 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| azd 1152-hqpa | Homo sapiens (human) | Kd | 30.0000 | 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 | 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 | 30.0000 | 1 | 1 |
| fedratinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| gsk690693 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| 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 |
| gdc 0941 | 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 | 30.0000 | 1 | 1 |
| 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 | 0.0020 | 1 | 1 |
| quizartinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| mk 2206 | 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 |
| dcc-2036 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| cabozantinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| defactinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| ly2584702 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| incb-018424 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| 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 |
| pf 3758309 | Homo sapiens (human) | Kd | 0.0660 | 1 | 1 |
| gdc 0980 | 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 |
| gsk 1363089 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| arry-334543 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| kin-193 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| mk 2461 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| bay 869766 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| as 703026 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| baricitinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 2 |
| dabrafenib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| pki 587 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| ribociclib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| mk-8033 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| pha 793887 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| sb 1518 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| abemaciclib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| mk-8776 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| jnj38877605 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| dinaciclib | Homo sapiens (human) | Kd | 30.0000 | 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 | 30.0000 | 1 | 1 |
| bms-911543 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| gsk2141795 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| azd8186 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| byl719 | Homo sapiens (human) | Kd | 1.9900 | 1 | 1 |
| rociletinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| ceritinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| azd1208 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| vx-509 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| volitinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| osimertinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| at 9283 | Homo sapiens (human) | Kd | 0.0030 | 1 | 1 |
| otssp167 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| chir 258 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| osi 027 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| nintedanib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| bay 80-6946 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
Recent advances in development of hetero-bivalent kinase inhibitors.European journal of medicinal chemistry, , Apr-15, Volume: 216, 2021
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
The structure of dimeric ROCK I reveals the mechanism for ligand selectivity.The Journal of biological chemistry, , Jan-06, Volume: 281, Issue:1, 2006
Kinase inhibitors: not just for kinases anymore.Journal of medicinal chemistry, , Apr-10, Volume: 46, Issue:8, 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
Recent advances in development of hetero-bivalent kinase inhibitors.European journal of medicinal chemistry, , Apr-15, Volume: 216, 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
Discovery of 4-arylamido 3-methyl isoxazole derivatives as novel FMS kinase inhibitors.European journal of medicinal chemistry, , Sep-18, Volume: 102, 2015
Discovery of trans-3,4'-bispyridinylethylenes as potent and novel inhibitors of protein kinase B (PKB/Akt) for the treatment of cancer: Synthesis and biological evaluation.Bioorganic & medicinal chemistry letters, , Mar-15, Volume: 16, Issue:6, 2006
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
Synthesis and structure-activity relationship of 3,4'-bispyridinylethylenes: discovery of a potent 3-isoquinolinylpyridine inhibitor of protein kinase B (PKB/Akt) for the treatment of cancer.Bioorganic & medicinal chemistry letters, , Apr-01, Volume: 16, Issue:7, 2006
Macrocyclic bisindolylmaleimides as inhibitors of protein kinase C and glycogen synthase kinase-3.Bioorganic & medicinal chemistry letters, , Sep-15, Volume: 13, Issue:18, 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
Identification of orally active, potent, and selective 4-piperazinylquinazolines as antagonists of the platelet-derived growth factor receptor tyrosine kinase family.Journal of medicinal chemistry, , Aug-15, Volume: 45, Issue:17, 2002
Inhibitors of protein kinase C. 3. Potent and highly selective bisindolylmaleimides by conformational restriction.Journal of medicinal chemistry, , Jan-08, Volume: 36, Issue:1, 1993
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Identification of a new chemical class of potent angiogenesis inhibitors based on conformational considerations and database searching.Bioorganic & medicinal chemistry letters, , Sep-15, Volume: 13, Issue:18, 2003
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
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
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
Rapid evolution of 6-phenylpurine inhibitors of protein kinase B through structure-based design.Journal of medicinal chemistry, , May-17, Volume: 50, Issue:10, 2007
Synthesis of highly substituted dibenzo[b,f]azocines and their evaluation as protein kinase inhibitors.Bioorganic & medicinal chemistry letters, , Oct-15, Volume: 16, Issue:20, 2006
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
The structure of dimeric ROCK I reveals the mechanism for ligand selectivity.The Journal of biological chemistry, , Jan-06, Volume: 281, Issue:1, 2006
Identification of ellagic acid as potent inhibitor of protein kinase CK2: a successful example of a virtual screening application.Journal of medicinal chemistry, , Apr-20, Volume: 49, Issue:8, 2006
Identification of tricyclic analogs related to ellagic acid as potent/selective tyrosine protein kinase inhibitors.Journal of medicinal chemistry, , Jul-08, Volume: 37, Issue:14, 1994
Novel Aurora A and Protein Kinase C (α, β1, β2, and θ) Multitarget Inhibitors: Impact of Selenium Atoms on the Potency and Selectivity.Journal of medicinal chemistry, , 02-24, Volume: 65, Issue:4, 2022
Joys of molecules. 2. Endeavors in chemical biology and medicinal chemistry.Journal of medicinal chemistry, , Sep-08, Volume: 48, Issue:18, 2005
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
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
Structure-activity relationship studies of flavopiridol analogues.Bioorganic & medicinal chemistry letters, , May-15, Volume: 10, Issue:10, 2000
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
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
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
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Discovery, synthesis, and in vivo activity of a new class of pyrazoloquinazolines as selective inhibitors of aurora B kinase.Journal of medicinal chemistry, , May-03, Volume: 50, Issue:9, 2007
Enables
This protein enables 7 target(s):
| Target | Category | Definition |
|---|
| 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] |
| AMP-activated protein kinase activity | molecular function | Catalysis of the reaction: ATP + a protein = ADP + a phosphoprotein. This reaction requires the presence of AMP. [GOC:mah] |
| cAMP-dependent protein kinase activity | molecular function | cAMP-dependent catalysis of the reaction: ATP + a protein = ADP + a phosphoprotein. [EC:2.7.11.11] |
| 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] |
| protein serine kinase activity | molecular function | Catalysis of the reactions: ATP + protein serine = ADP + protein serine phosphate. [RHEA:17989] |
| protein kinase A regulatory subunit binding | molecular function | Binding to one or both of the regulatory subunits of protein kinase A. [GOC:mah] |
Located In
This protein is located in 3 target(s):
| Target | Category | Definition |
|---|
| nucleoplasm | cellular component | That part of the nuclear content other than the chromosomes or the nucleolus. [GOC:ma, ISBN:0124325653] |
| 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] |
| ciliary base | cellular component | Area of the cilium (also called flagellum) where the basal body and the axoneme are anchored to the plasma membrane. The ciliary base encompasses the distal part of the basal body, transition fibers and transition zone and is structurally and functionally very distinct from the rest of the cilium. In this area proteins are sorted and filtered before entering the cilium, and many ciliary proteins localize specifically to this area. [GOC:cilia, GOC:krc, PMID:22653444] |
Active In
This protein is active in 2 target(s):
| Target | Category | Definition |
|---|
| 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] |
| 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] |
Part Of
This protein is part of 1 target(s):
| Target | Category | Definition |
|---|
| cAMP-dependent protein kinase complex | cellular component | An enzyme complex, composed of regulatory and catalytic subunits, that catalyzes protein phosphorylation. Inactive forms of the enzyme have two regulatory chains and two catalytic chains; activation by cAMP produces two active catalytic monomers and a regulatory dimer. [PMID:18178622] |
Involved In
This protein is involved in 5 target(s):
| Target | Category | Definition |
|---|
| renal water homeostasis | biological process | Renal process involved in the maintenance of an internal steady state of water in the body. [GOC:mtg_cardio] |
| spermatogenesis | biological process | The developmental process by which male germ line stem cells self renew or give rise to successive cell types resulting in the development of a spermatozoa. [GOC:jid, ISBN:9780878933846, PMID:28073824, PMID:30990821] |
| male gonad development | biological process | The process whose specific outcome is the progression of the male gonad over time, from its formation to the mature structure. [GOC:jid] |
| high-density lipoprotein particle assembly | biological process | The non-covalent aggregation and arrangement of proteins and lipids to form a high-density lipoprotein particle. [GOC:BHF, GOC:mah] |
| protein kinase A signaling | biological process | An intracellular signaling cassette that starts with the activation of protein kinase A (PKA), and ends with the regulation of a downstream cellular process, e.g. transcription. The PKA catalytic subunit (PKA-C) is normally present in a complex with its regulatory subunit, PKA-R. The inhibitory action of PKA-R is released upon cAMP binding, which results in the activation of PKA-C. [PMID:35252178, PMID:36431013] |