Page last updated: 2024-08-07 16:03:15
Protein kinase C alpha type
A protein kinase C alpha type that is encoded in the genome of human. [PRO:CL, UniProtKB:P17252]
Synonyms
PKC-A;
PKC-alpha;
EC 2.7.11.13
Research
Bioassay Publications (130)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 1 (0.77) | 18.7374 |
| 1990's | 29 (22.31) | 18.2507 |
| 2000's | 63 (48.46) | 29.6817 |
| 2010's | 35 (26.92) | 24.3611 |
| 2020's | 2 (1.54) | 2.80 |
Compounds (300)
Drugs with Inhibition Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| edelfosine | Homo sapiens (human) | IC50 | 12.0000 | 1 | 1 |
| cgp 52411 | Homo sapiens (human) | IC50 | 80.0000 | 1 | 1 |
| rtki cpd | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
| bisindolylmaleimide i | Homo sapiens (human) | IC50 | 0.0055 | 2 | 7 |
| bisindolylmaleimide iv | Homo sapiens (human) | IC50 | 0.8945 | 2 | 2 |
| ro 31-8425 | Homo sapiens (human) | IC50 | 0.6000 | 1 | 1 |
| go 6976 | Homo sapiens (human) | IC50 | 0.0027 | 3 | 3 |
| n-(2-(methylamino)ethyl)-5-isoquinolinesulfonamide | Homo sapiens (human) | Ki | 15.0000 | 1 | 1 |
| n-(2-aminoethyl)-5-isoquinolinesulfonamide | Homo sapiens (human) | IC50 | 82.7667 | 2 | 6 |
| 1-(5-isoquinolinesulfonyl)piperazine | Homo sapiens (human) | IC50 | 12.0000 | 1 | 1 |
| 2,2',3,3',4,4'-hexahydroxy-1,1'-biphenyl-6,6'-dimethanol dimethyl ether | Homo sapiens (human) | IC50 | 43.0000 | 1 | 1 |
| 1-(2-naphthalenyl)-3-[(phenylmethyl)-propan-2-ylamino]-1-propanone | Homo sapiens (human) | IC50 | 18.0000 | 1 | 1 |
| staurosporine aglycone | Homo sapiens (human) | IC50 | 2.4500 | 3 | 3 |
| beta-lapachone | Homo sapiens (human) | IC50 | 1.8000 | 1 | 1 |
| vitamin k 3 | Homo sapiens (human) | IC50 | 2.2000 | 1 | 1 |
| minaprine | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
| niclosamide | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
| pd 153035 | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
| ro 31-8220 | Homo sapiens (human) | IC50 | 0.0330 | 2 | 2 |
| sb 239063 | Homo sapiens (human) | IC50 | 0.0830 | 1 | 1 |
| imatinib | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
| suramin | Homo sapiens (human) | IC50 | 29.0000 | 1 | 1 |
| tetradecanoylphorbol acetate | Homo sapiens (human) | Ki | 0.0044 | 2 | 2 |
| phorbol 12,13-dibutyrate | Homo sapiens (human) | Ki | 0.0049 | 4 | 4 |
| staurosporine | Homo sapiens (human) | IC50 | 0.0655 | 20 | 20 |
| paroxetine hydrochloride | Homo sapiens (human) | IC50 | 220.0000 | 1 | 1 |
| norharman | Homo sapiens (human) | IC50 | 25.0000 | 1 | 1 |
| rebeccamycin | Homo sapiens (human) | IC50 | 125.0000 | 3 | 3 |
| 1-(5-isoquinolinesulfonyl)-2-methylpiperazine dihydrochloride | Homo sapiens (human) | IC50 | 6.0000 | 1 | 1 |
| 1-(5-isoquinolinesulfonyl)-2-methylpiperazine dihydrochloride | Homo sapiens (human) | Ki | 6.0000 | 1 | 1 |
| indolactam v | Homo sapiens (human) | Ki | 1.2458 | 10 | 10 |
| ro 32-0432 | Homo sapiens (human) | IC50 | 0.0220 | 1 | 1 |
| cki 7 | Homo sapiens (human) | IC50 | 399.0833 | 1 | 6 |
| cercosporamide | Homo sapiens (human) | IC50 | 1.0100 | 2 | 2 |
| 1,2-dioctanoylglycerol | Homo sapiens (human) | Ki | 2.7596 | 3 | 6 |
| ruboxistaurin | Homo sapiens (human) | IC50 | 0.3600 | 4 | 4 |
| birb 796 | Homo sapiens (human) | IC50 | 30.0000 | 1 | 1 |
| 7-octylindolactam v | Homo sapiens (human) | Ki | 0.0005 | 1 | 1 |
| sb 203580 | Homo sapiens (human) | IC50 | 75.0000 | 1 | 1 |
| enzastaurin | Homo sapiens (human) | IC50 | 0.4695 | 4 | 2 |
| nsc 95397 | Homo sapiens (human) | IC50 | 1.0000 | 1 | 1 |
| n-(4-methoxybenzyl)-n'-(5-nitro-1,3-thiazol-2-yl)urea | Homo sapiens (human) | IC50 | 100,000.0000 | 1 | 1 |
| 7-n-butyl-6-(4'-hydroxyphenyl)-5h-pyrrolo(2,3b)pyrazine | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
| purvalanol b | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
| h 89 | Homo sapiens (human) | Ki | 46.3328 | 2 | 10 |
| 12-deoxyphorbol 13-acetate | Homo sapiens (human) | Ki | 0.2000 | 2 | 2 |
| purvalanol a | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| isoxanthohumol | Homo sapiens (human) | IC50 | 45.3000 | 1 | 1 |
| xanthohumol | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
| ag-213 | Homo sapiens (human) | IC50 | 3.0000 | 1 | 1 |
| tamoxifen | Homo sapiens (human) | IC50 | 10.5000 | 2 | 2 |
| cgp 74514a | Homo sapiens (human) | IC50 | 21.7500 | 1 | 2 |
| bms 387032 | Homo sapiens (human) | IC50 | 40.0000 | 1 | 1 |
| sf 2370 | Homo sapiens (human) | IC50 | 0.2500 | 1 | 1 |
| dasatinib | Homo sapiens (human) | IC50 | 50.0000 | 1 | 1 |
| pd 407824 | Homo sapiens (human) | IC50 | 3.4000 | 1 | 1 |
| calceolarioside a | Homo sapiens (human) | IC50 | 0.6000 | 1 | 1 |
| calceolarioside b | Homo sapiens (human) | IC50 | 4.6000 | 1 | 1 |
| bryostatin 1 | Homo sapiens (human) | Ki | 0.0005 | 1 | 1 |
| harmine | Homo sapiens (human) | IC50 | 250.0000 | 1 | 1 |
| genistein | Homo sapiens (human) | IC50 | 56.8750 | 2 | 8 |
| forsythiaside | Homo sapiens (human) | IC50 | 1.9000 | 1 | 1 |
| acteoside | Homo sapiens (human) | IC50 | 9.3000 | 1 | 1 |
| rottlerin | Homo sapiens (human) | IC50 | 20.0000 | 1 | 1 |
| ophiocordin | Homo sapiens (human) | IC50 | 0.0248 | 4 | 12 |
| ophiocordin | Homo sapiens (human) | Ki | 0.0053 | 1 | 1 |
| alvocidib | Homo sapiens (human) | IC50 | 6.9600 | 5 | 5 |
| arcyriaflavin a | Homo sapiens (human) | IC50 | 48.3367 | 3 | 3 |
| pd 161570 | Homo sapiens (human) | IC50 | 23.0000 | 1 | 1 |
| 2-tert-butyl-9-fluoro-3,6-dihydro-7h-benz(h)imidazo(4,5-f)isoquinoline-7-one | Homo sapiens (human) | IC50 | 1.2000 | 1 | 1 |
| gw-5074 | Homo sapiens (human) | IC50 | 15.0000 | 1 | 1 |
| a 419259 | Homo sapiens (human) | IC50 | 20.0000 | 1 | 1 |
| b 43 | Homo sapiens (human) | IC50 | 33.0000 | 1 | 1 |
| cgp 53353 | Homo sapiens (human) | IC50 | 32.0000 | 1 | 1 |
| a 770041 | Homo sapiens (human) | IC50 | 25.0000 | 1 | 1 |
| edotecarin | Homo sapiens (human) | IC50 | 200.0000 | 1 | 1 |
| sb 242235 | Homo sapiens (human) | IC50 | 0.0830 | 1 | 1 |
| ct52923 | Homo sapiens (human) | IC50 | 30.0000 | 1 | 1 |
| tofacitinib | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| ps1145 | Homo sapiens (human) | IC50 | 25.0000 | 1 | 1 |
| bryostatin 10 | Homo sapiens (human) | Ki | 0.0016 | 1 | 1 |
| sotrastaurin | Homo sapiens (human) | IC50 | 0.0026 | 5 | 10 |
| bryostatin 16 | Homo sapiens (human) | Ki | 0.1180 | 1 | 1 |
| ly 338522 | Homo sapiens (human) | IC50 | 0.2400 | 1 | 1 |
| PDGF receptor tyrosine kinase inhibitor III | Homo sapiens (human) | IC50 | 30.0000 | 1 | 1 |
| brivanib | Homo sapiens (human) | IC50 | 25.0000 | 1 | 1 |
| danusertib | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| N-[5-[[5-[(4-acetyl-1-piperazinyl)-oxomethyl]-4-methoxy-2-methylphenyl]thio]-2-thiazolyl]-4-[(3,3-dimethylbutan-2-ylamino)methyl]benzamide | Homo sapiens (human) | IC50 | 24.0000 | 1 | 1 |
| gw 2580 | Homo sapiens (human) | IC50 | 13.0000 | 1 | 1 |
| 4-[6-[4-(methoxycarbonylamino)phenyl]-4-(4-morpholinyl)-1-pyrazolo[3,4-d]pyrimidinyl]-1-piperidinecarboxylic acid methyl ester | Homo sapiens (human) | IC50 | 50.0000 | 1 | 1 |
| debromoaplysiatoxin | Homo sapiens (human) | Ki | 0.0200 | 1 | 1 |
| p505-15 | Homo sapiens (human) | IC50 | 0.0900 | 1 | 1 |
| pha 793887 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| gsk2141795 | Homo sapiens (human) | IC50 | 0.7530 | 1 | 1 |
| ro 3306 | Homo sapiens (human) | Ki | 2.0000 | 1 | 1 |
| hymenialdisine | Homo sapiens (human) | IC50 | 0.7000 | 1 | 1 |
Drugs with Activation Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| fasudil | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| 4-(4'-hydroxyphenyl)-amino-6,7-dimethoxyquinazoline | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| imatinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| tetradecanoylphorbol acetate | Homo sapiens (human) | EC50 | 850.0048 | 2 | 2 |
| phorbol 12,13-dibutyrate | Homo sapiens (human) | Kd | 0.0069 | 10 | 10 |
| triciribine phosphate | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| staurosporine | Homo sapiens (human) | Kd | 0.0500 | 1 | 1 |
| picropodophyllin | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| gefitinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| lestaurtinib | Homo sapiens (human) | Kd | 1.0095 | 2 | 2 |
| perifosine | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| vatalanib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| ruboxistaurin | Homo sapiens (human) | Kd | 0.0230 | 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 | 0.5240 | 1 | 1 |
| erlotinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 2 |
| lapatinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| sorafenib | Homo sapiens (human) | Kd | 20.0000 | 2 | 2 |
| resveratrol | Homo sapiens (human) | EC50 | 5,780.0000 | 1 | 1 |
| 12-deoxyphorbol 13-acetate | Homo sapiens (human) | EC50 | 0.9100 | 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 | 1 |
| sf 2370 | Homo sapiens (human) | Kd | 2.2800 | 1 | 1 |
| tandutinib | Homo sapiens (human) | Kd | 20.0000 | 2 | 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 | 0.0350 | 1 | 1 |
| zd 6474 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| imd 0354 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| sirolimus | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| ophiocordin | Homo sapiens (human) | Kd | 0.0064 | 1 | 1 |
| alvocidib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| bosutinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| orantinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| su 11248 | Homo sapiens (human) | Kd | 15.3333 | 3 | 3 |
| palbociclib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| 3,4',5-trimethoxystilbene | Homo sapiens (human) | EC50 | 1,560.0000 | 1 | 1 |
| vx680 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| cyc 116 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| everolimus | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| ekb 569 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| axitinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| temsirolimus | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| pep005 | Homo sapiens (human) | EC50 | 0.0725 | 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 | 3.2760 | 1 | 1 |
| 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 | 15.3600 | 2 | 2 |
| 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 |
| 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 | 2 |
| tivozanib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| hki 272 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| tofacitinib | Homo sapiens (human) | Kd | 28.0980 | 1 | 1 |
| cediranib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| masitinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 2 |
| ly-2157299 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| pazopanib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| azd 6244 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| su 14813 | Homo sapiens (human) | Kd | 30.0000 | 1 | 2 |
| bibw 2992 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| binimetinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| sotrastaurin | Homo sapiens (human) | Kd | 0.0130 | 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 |
| volasertib | 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 |
| 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 | 30.0000 | 1 | 1 |
| brivanib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| 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 | 30.0000 | 1 | 1 |
| bms-690514 | Homo sapiens (human) | Kd | 1.5570 | 1 | 1 |
| bi 2536 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| inno-406 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| kw 2449 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| danusertib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| abt 869 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| 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 |
| tak 285 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| 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 |
| chir-265 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| motesanib | 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 |
| gsk 461364 | 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 | 1.6090 | 1 | 1 |
| gdc-0973 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| buparlisib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| azd 1480 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| azd8330 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| pha 848125 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| ro5126766 | Homo sapiens (human) | Kd | 30.0000 | 1 | 2 |
| fedratinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| gsk690693 | Homo sapiens (human) | Kd | 0.5660 | 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 | 0.8850 | 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 | 30.0000 | 1 | 1 |
| icotinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| ph 797804 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| kx-01 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| 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 | 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 | 30.0000 | 1 | 1 |
| quizartinib | Homo sapiens (human) | Kd | 20.0000 | 2 | 2 |
| 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 | 2 |
| sns 314 | Homo sapiens (human) | Kd | 30.0000 | 1 | 2 |
| lucitanib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| pf-04691502 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| n-(cyanomethyl)-4-(2-((4-(4-morpholinyl)phenyl)amino)-4-pyrimidinyl)benzamide | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| dcc-2036 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| cabozantinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| defactinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| ly2584702 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| incb-018424 | Homo sapiens (human) | Kd | 16.4940 | 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 | 0.8730 | 1 | 1 |
| gdc 0980 | Homo sapiens (human) | Kd | 2.1340 | 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 | 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 | 2.0710 | 1 | 1 |
| dabrafenib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| pki 587 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| n-(3-fluoro-4-((1-methyl-6-(1h-pyrazol-4-yl)-1h-indazol-5 yl)oxy)phenyl)-1-(4-fluorophenyl)-6-methyl-2-oxo-1,2-dihydropyridine-3-carboxamide | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| 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 | 0.9340 | 1 | 1 |
| abemaciclib | Homo sapiens (human) | Kd | 0.5300 | 1 | 1 |
| mk-8776 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| afuresertib | Homo sapiens (human) | Kd | 21.3520 | 1 | 1 |
| gsk 1070916 | Homo sapiens (human) | Kd | 30.0000 | 1 | 2 |
| jnj38877605 | Homo sapiens (human) | Kd | 30.0000 | 1 | 2 |
| dinaciclib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| gilteritinib | Homo sapiens (human) | Kd | 0.5910 | 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 | 1.6670 | 1 | 1 |
| azd8186 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| byl719 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| cep-32496 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| rociletinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| ceritinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| azd1208 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| vx-509 | Homo sapiens (human) | Kd | 0.1170 | 1 | 1 |
| debio 1347 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| volitinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| osimertinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| at 9283 | Homo sapiens (human) | Kd | 1.5430 | 1 | 1 |
| otssp167 | Homo sapiens (human) | Kd | 0.1640 | 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 |
Drugs with Other Measurements
Synthesis of anilino-monoindolylmaleimides as potent and selective PKCbeta inhibitors.Bioorganic & medicinal chemistry letters, , Oct-18, Volume: 14, Issue:20, 2004
Dianilinophthalimides: potent and selective, ATP-competitive inhibitors of the EGF-receptor protein tyrosine kinase.Journal of medicinal chemistry, , Apr-01, Volume: 37, Issue:7, 1994
Identification of orally available naphthyridine protein kinase D inhibitors.Journal of medicinal chemistry, , Aug-12, Volume: 53, Issue:15, 2010
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
Minocycline down-regulates MHC II expression in microglia and macrophages through inhibition of IRF-1 and protein kinase C (PKC)alpha/betaII.The Journal of biological chemistry, , May-18, Volume: 282, Issue:20, 2007
Design of potent protein kinase inhibitors using the bisubstrate approach.Journal of medicinal chemistry, , Volume: 34, Issue:1, 1991
A newly synthesized selective casein kinase I inhibitor, N-(2-aminoethyl)-5-chloroisoquinoline-8-sulfonamide, and affinity purification of casein kinase I from bovine testis.The Journal of biological chemistry, , Mar-25, Volume: 264, Issue:9, 1989
Methyl 3-(3-(4-(2,4,4-Trimethylpentan-2-yl)phenoxy)-propanamido)benzoate as a Novel and Dual Malate Dehydrogenase (MDH) 1/2 Inhibitor Targeting Cancer Metabolism.Journal of medicinal chemistry, , 10-26, Volume: 60, Issue:20, 2017
Kinase inhibitors: not just for kinases anymore.Journal of medicinal chemistry, , Apr-10, Volume: 46, Issue:8, 2003
Structure-activity relationships in a series of substituted indolocarbazoles: topoisomerase I and protein kinase C inhibition and antitumoral and antimicrobial properties.Journal of medicinal chemistry, , Oct-25, Volume: 39, Issue:22, 1996
Kinase inhibitors: not just for kinases anymore.Journal of medicinal chemistry, , Apr-10, Volume: 46, Issue:8, 2003
Specificity and mechanism of action of some commonly used protein kinase inhibitors.The Biochemical journal, , Oct-01, Volume: 351, Issue:Pt 1, 2000
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Designed multiple ligands. An emerging drug discovery paradigm.Journal of medicinal chemistry, , Oct-20, Volume: 48, Issue:21, 2005
Isolation of Phorbol Esters from Euphorbia grandicornis and Evaluation of Protein Kinase C- and Human Platelet-Activating Effects of Euphorbiaceae Diterpenes.Journal of natural products, , 10-28, Volume: 79, Issue:10, 2016
Chemical modifications of resveratrol for improved protein kinase C alpha activity.Bioorganic & medicinal chemistry, , Sep-15, Volume: 19, Issue:18, 2011
Design and synthesis of protein kinase Cα activators based on 'out of pocket' interactions.Bioorganic & medicinal chemistry letters, , Jun-15, Volume: 21, Issue:12, 2011
Rational design, synthesis, and biological evaluation of rigid pyrrolidone analogues as potential inhibitors of prostate cancer cell growth.Bioorganic & medicinal chemistry letters, , Apr-23, Volume: 11, Issue:8, 2001
Design and synthesis of protein kinase C epsilon selective diacylglycerol lactones (DAG-lactones).European journal of medicinal chemistry, , Jan-27, Volume: 90, 2015
Generation of 'Unnatural Natural Product' library and identification of a small molecule inhibitor of XIAP.Bioorganic & medicinal chemistry, , Jul-15, Volume: 19, Issue:14, 2011
Role of the phenolic hydroxyl group in the biological activities of simplified analogue of aplysiatoxin with antiproliferative activity.Bioorganic & medicinal chemistry letters, , Oct-15, Volume: 20, Issue:20, 2010
Synthesis and binding selectivity of 7- and 15-decylbenzolactone-V8 for the C1 domains of protein kinase C isozymes.Bioorganic & medicinal chemistry letters, , Sep-15, Volume: 13, Issue:18, 2003
The C4 hydroxyl group of phorbol esters is not necessary for protein kinase C binding.Bioorganic & medicinal chemistry letters, , Mar-12, Volume: 11, Issue:5, 2001
Synthesis and PKC isozyme surrogate binding of indothiolactam-V, a new thioamide analogue of tumor promoting indolactam-V.Bioorganic & medicinal chemistry letters, , Sep-18, Volume: 10, Issue:18, 2000
Conformationally constrained analogues of diacylglycerol (DAG). 16. How much structural complexity is necessary for recognition and high binding affinity to protein kinase C?Journal of medicinal chemistry, , Mar-09, Volume: 43, Issue:5, 2000
Selective binding of bryostatin analogues to the cysteine rich domains of protein kinase C isozymes.Bioorganic & medicinal chemistry letters, , Jun-21, Volume: 9, Issue:12, 1999
Molecular modeling and site-directed mutagenesis studies of a phorbol ester-binding site in protein kinase C.Journal of medicinal chemistry, , Jun-21, Volume: 39, Issue:13, 1996
Protein kinase C. Modeling of the binding site and prediction of binding constants.Journal of medicinal chemistry, , Apr-29, Volume: 37, Issue:9, 1994
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
Chemistry-oriented synthesis (ChOS) and target deconvolution on neuroprotective effect of a novel scaffold, oxaza spiroquinone.European journal of medicinal chemistry, , Feb-01, Volume: 163, 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
Bioactive Indolocarbazoles from the Marine-Derived Streptomyces sp. DT-A61.Journal of natural products, , 04-27, Volume: 81, Issue:4, 2018
Novel LCK/FMS inhibitors based on phenoxypyrimidine scaffold as potential treatment for inflammatory disorders.European journal of medicinal chemistry, , Dec-01, Volume: 141, 2017
Novel pyrrolopyrimidines as Mps1/TTK kinase inhibitors for breast cancer.Bioorganic & medicinal chemistry, , 04-01, Volume: 25, Issue:7, 2017
Synthesis and biological evaluation of new [1,2,4]triazolo[4,3-a]pyridine derivatives as potential c-Met inhibitors.Bioorganic & medicinal chemistry, , 08-15, Volume: 24, Issue:16, 2016
Syntheses, neural protective activities, and inhibition of glycogen synthase kinase-3β of substituted quinolines.Bioorganic & medicinal chemistry letters, , Aug-01, Volume: 24, Issue:15, 2014
Structure-based design, synthesis and biological evaluation of diphenylmethylamine derivatives as novel Akt1 inhibitors.European journal of medicinal chemistry, , Feb-12, Volume: 73, 2014
The synthesis and evaluation of indolylureas as PKCα inhibitors.Bioorganic & medicinal chemistry, , Apr-15, Volume: 19, Issue:8, 2011
Synthesis, activity, and pharmacophore development for isatin-beta-thiosemicarbazones with selective activity toward multidrug-resistant cells.Journal of medicinal chemistry, , May-28, Volume: 52, Issue:10, 2009
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
A small molecule-kinase interaction map for clinical kinase inhibitors.Nature biotechnology, , Volume: 23, Issue:3, 2005
Novel indolylindazolylmaleimides as inhibitors of protein kinase C-beta: synthesis, biological activity, and cardiovascular safety.Journal of medicinal chemistry, , Mar-24, Volume: 48, Issue:6, 2005
Synthesis and biological evaluation of 1-aryl-4,5-dihydro-1H-pyrazolo[3,4-d]pyrimidin-4-one inhibitors of cyclin-dependent kinases.Journal of medicinal chemistry, , Nov-18, Volume: 47, Issue:24, 2004
Aryl[a]pyrrolo[3,4-c]carbazoles as selective cyclin D1-CDK4 inhibitors.Bioorganic & medicinal chemistry letters, , Nov-03, Volume: 13, Issue:21, 2003
Macrocyclic bisindolylmaleimides as inhibitors of protein kinase C and glycogen synthase kinase-3.Bioorganic & medicinal chemistry letters, , Sep-15, Volume: 13, Issue:18, 2003
Acyclic N-(azacycloalkyl)bisindolylmaleimides: isozyme selective inhibitors of PKCbeta.Bioorganic & medicinal chemistry letters, , Jun-02, Volume: 13, Issue:11, 2003
Identification of orally active, potent, and selective 4-piperazinylquinazolines as antagonists of the platelet-derived growth factor receptor tyrosine kinase family.Journal of medicinal chemistry, , Aug-15, Volume: 45, Issue:17, 2002
New dermatological agents for the treatment of psoriasis.Journal of medicinal chemistry, , Feb-01, Volume: 44, Issue:3, 2001
(S)-13-[(dimethylamino)methyl]-10,11,14,15-tetrahydro-4,9:16, 21-dimetheno-1H, 13H-dibenzo[e,k]pyrrolo[3,4-h][1,4,13]oxadiazacyclohexadecene-1,3(2H)-d ione (LY333531) and related analogues: isozyme selective inhibitors of protein kinase C beta.Journal of medicinal chemistry, , Jul-05, Volume: 39, Issue:14, 1996
Syntheses and biological activities of rebeccamycin analogues. Introduction of a halogenoacetyl substituent.Journal of medicinal chemistry, , Feb-25, Volume: 42, Issue:4, 1999
Syntheses and biological activities (topoisomerase inhibition and antitumor and antimicrobial properties) of rebeccamycin analogues bearing modified sugar moieties and substituted on the imide nitrogen with a methyl group.Journal of medicinal chemistry, , Oct-10, Volume: 40, Issue:21, 1997
Structure-activity relationships in a series of substituted indolocarbazoles: topoisomerase I and protein kinase C inhibition and antitumoral and antimicrobial properties.Journal of medicinal chemistry, , Oct-25, Volume: 39, Issue:22, 1996
Design and physicochemical properties of new fluorescent ligands of protein kinase C isozymes focused on CH/pi interaction.Bioorganic & medicinal chemistry, , Jan-15, Volume: 16, Issue:2, 2008
Synthesis, conformational analysis, and biological evaluation of 1-hexylindolactam-V10 as a selective activator for novel protein kinase C isozymes.Journal of medicinal chemistry, , Jan-10, Volume: 51, Issue:1, 2008
The amide hydrogen of (-)-indolactam-V and benzolactam-V8's plays a critical role in protein kinase C binding and tumor-promoting activities.Bioorganic & medicinal chemistry letters, , Mar-12, Volume: 11, Issue:5, 2001
Synthesis and PKC isozyme surrogate binding of indothiolactam-V, a new thioamide analogue of tumor promoting indolactam-V.Bioorganic & medicinal chemistry letters, , Sep-18, Volume: 10, Issue:18, 2000
Synthesis and protein kinase C binding activity of benzolactam-V7.Bioorganic & medicinal chemistry letters, , May-17, Volume: 9, Issue:10, 1999
Modeling, chemistry, and biology of the benzolactam analogues of indolactam V (ILV). 2. Identification of the binding site of the benzolactams in the CRD2 activator-binding domain of PKCdelta and discovery of an ILV analogue of improved isozyme selectivitJournal of medicinal chemistry, , Apr-25, Volume: 40, Issue:9, 1997
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).Blood, , Oct-01, Volume: 114, Issue:14, 2009
Benzofuro[3,2-d]pyrimidines inspired from cercosporamide CaPkc1 inhibitor: Synthesis and evaluation of fluconazole susceptibility restoration.Bioorganic & medicinal chemistry letters, , 07-15, Volume: 28, Issue:13, 2018
(-)-Cercosporamide derivatives as novel antihyperglycemic agents.Bioorganic & medicinal chemistry letters, , Feb-01, Volume: 19, Issue:3, 2009
Design, synthesis, and biological activity of isophthalic acid derivatives targeted to the C1 domain of protein kinase C.Journal of medicinal chemistry, , Jul-09, Volume: 52, Issue:13, 2009
Characterization of the interaction of phorbol esters with the C1 domain of MRCK (myotonic dystrophy kinase-related Cdc42 binding kinase) alpha/beta.The Journal of biological chemistry, , Apr-18, Volume: 283, Issue:16, 2008
Diacylglycerols with lipophilically equivalent branched acyl chains display high affinity for protein kinase C (PK-C). A direct measure of the effect of constraining the glycerol backbone in DAG lactones.Bioorganic & medicinal chemistry letters, , Apr-03, Volume: 10, Issue:7, 2000
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
Synthesis and anticancer activity of novel bisindolylhydroxymaleimide derivatives with potent GSK-3 kinase inhibition.Bioorganic & medicinal chemistry, , 08-07, Volume: 26, Issue:14, 2018
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Synthesis and discovery of macrocyclic polyoxygenated bis-7-azaindolylmaleimides as a novel series of potent and highly selective glycogen synthase kinase-3beta inhibitors.Journal of medicinal chemistry, , Sep-11, Volume: 46, Issue:19, 2003
(S)-13-[(dimethylamino)methyl]-10,11,14,15-tetrahydro-4,9:16, 21-dimetheno-1H, 13H-dibenzo[e,k]pyrrolo[3,4-h][1,4,13]oxadiazacyclohexadecene-1,3(2H)-d ione (LY333531) and related analogues: isozyme selective inhibitors of protein kinase C beta.Journal of medicinal chemistry, , Jul-05, Volume: 39, Issue:14, 1996
Synthesis and anticancer activity of novel bisindolylhydroxymaleimide derivatives with potent GSK-3 kinase inhibition.Bioorganic & medicinal chemistry, , 08-07, Volume: 26, Issue:14, 2018
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Acyclic N-(azacycloalkyl)bisindolylmaleimides: isozyme selective inhibitors of PKCbeta.Bioorganic & medicinal chemistry letters, , Jun-02, Volume: 13, Issue:11, 2003
[no title available],
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).Blood, , Oct-01, Volume: 114, Issue:14, 2009
Crystal structures of catalytic subunit of cAMP-dependent protein kinase in complex with isoquinolinesulfonyl protein kinase inhibitors H7, H8, and H89. Structural implications for selectivity.The Journal of biological chemistry, , Oct-18, Volume: 271, Issue:42, 1996
Inhibition of forskolin-induced neurite outgrowth and protein phosphorylation by a newly synthesized selective inhibitor of cyclic AMP-dependent protein kinase, N-[2-(p-bromocinnamylamino)ethyl]-5-isoquinolinesulfonamide (H-89), of PC12D pheochromocytoma The Journal of biological chemistry, , Mar-25, Volume: 265, Issue:9, 1990
Isolation of Phorbol Esters from Euphorbia grandicornis and Evaluation of Protein Kinase C- and Human Platelet-Activating Effects of Euphorbiaceae Diterpenes.Journal of natural products, , 10-28, Volume: 79, Issue:10, 2016
A nonpromoting phorbol from the samoan medicinal plant Homalanthus nutans inhibits cell killing by HIV-1.Journal of medicinal chemistry, , May-29, Volume: 35, Issue:11, 1992
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
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
Synthesis and kinase inhibitory activity of 3'-(S)-epi-K-252a.Bioorganic & medicinal chemistry letters, , Oct-21, Volume: 12, Issue:20, 2002
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).Blood, , Oct-01, Volume: 114, Issue:14, 2009
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Discovery of N-(2-chloro-6-methyl- phenyl)-2-(6-(4-(2-hydroxyethyl)- piperazin-1-yl)-2-methylpyrimidin-4- ylamino)thiazole-5-carboxamide (BMS-354825), a dual Src/Abl kinase inhibitor with potent antitumor activity in preclinical assays.Journal of medicinal chemistry, , Dec-30, Volume: 47, Issue:27, 2004
Use of a pharmacophore model for the design of EGFR tyrosine kinase inhibitors: isoflavones and 3-phenyl-4(1H)-quinolones.Journal of medicinal chemistry, , Mar-25, Volume: 42, Issue:6, 1999
Thiazolidine-diones. Biochemical and biological activity of a novel class of tyrosine protein kinase inhibitors.The Journal of biological chemistry, , Dec-25, Volume: 265, Issue:36, 1990
G-Protein-Coupled Receptor Kinase 2 (GRK2) Inhibitors: Current Trends and Future Perspectives.Journal of medicinal chemistry, , Oct-27, Volume: 59, Issue:20, 2016
Joys of molecules. 2. Endeavors in chemical biology and medicinal chemistry.Journal of medicinal chemistry, , Sep-08, Volume: 48, Issue:18, 2005
Synthesis and protein kinase inhibitory activity of balanol analogues with modified benzophenone subunits.Journal of medicinal chemistry, , Jun-06, Volume: 45, Issue:12, 2002
Synthesis and protein kinase C inhibitory activities of balanol analogs with replacement of the perhydroazepine moiety.Journal of medicinal chemistry, , Jan-17, Volume: 40, Issue:2, 1997
Synthesis and protein kinase C inhibitory activities of acyclic balanol analogs that are highly selective for protein kinase C over protein kinase A.Journal of medicinal chemistry, , Dec-20, Volume: 39, Issue:26, 1996
Discovery of Journal of medicinal chemistry, , 09-09, Volume: 64, Issue:17, 2021
A review on flavones targeting serine/threonine protein kinases for potential anticancer drugs.Bioorganic & medicinal chemistry, , 03-01, Volume: 27, Issue:5, 2019
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
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
Aryl[a]pyrrolo[3,4-c]carbazoles as selective cyclin D1-CDK4 inhibitors.Bioorganic & medicinal chemistry letters, , Nov-03, Volume: 13, Issue:21, 2003
Structure-activity relationships in a series of substituted indolocarbazoles: topoisomerase I and protein kinase C inhibition and antitumoral and antimicrobial properties.Journal of medicinal chemistry, , Oct-25, Volume: 39, Issue:22, 1996
Dianilinophthalimides: potent and selective, ATP-competitive inhibitors of the EGF-receptor protein tyrosine kinase.Journal of medicinal chemistry, , Apr-01, Volume: 37, Issue:7, 1994
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).Blood, , Oct-01, Volume: 114, Issue:14, 2009
A small molecule-kinase interaction map for clinical kinase inhibitors.Nature biotechnology, , Volume: 23, Issue:3, 2005
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).Blood, , Oct-01, Volume: 114, Issue:14, 2009
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Prevention of organ allograft rejection by a specific Janus kinase 3 inhibitor.Science (New York, N.Y.), , Oct-31, Volume: 302, Issue:5646, 2003
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
Indolyl-naphthyl-maleimides as potent and selective inhibitors of protein kinase C-α/β.Bioorganic & medicinal chemistry letters, , 02-15, Volume: 27, Issue:4, 2017
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Structure-activity relationship and pharmacokinetic studies of sotrastaurin (AEB071), a promising novel medicine for prevention of graft rejection and treatment of psoriasis.Journal of medicinal chemistry, , Sep-08, Volume: 54, Issue:17, 2011
Discovery of 3-(1H-indol-3-yl)-4-[2-(4-methylpiperazin-1-yl)quinazolin-4-yl]pyrrole-2,5-dione (AEB071), a potent and selective inhibitor of protein kinase C isotypes.Journal of medicinal chemistry, , Oct-22, Volume: 52, Issue:20, 2009
(S)-13-[(dimethylamino)methyl]-10,11,14,15-tetrahydro-4,9:16, 21-dimetheno-1H, 13H-dibenzo[e,k]pyrrolo[3,4-h][1,4,13]oxadiazacyclohexadecene-1,3(2H)-d ione (LY333531) and related analogues: isozyme selective inhibitors of protein kinase C beta.Journal of medicinal chemistry, , Jul-05, Volume: 39, Issue:14, 1996
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Discovery and preclinical studies of (R)-1-(4-(4-fluoro-2-methyl-1H-indol-5-yloxy)-5- methylpyrrolo[2,1-f][1,2,4]triazin-6-yloxy)propan- 2-ol (BMS-540215), an in vivo active potent VEGFR-2 inhibitor.Journal of medicinal chemistry, , Apr-06, Volume: 49, Issue:7, 2006
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazoles: identification of a potent Aurora kinase inhibitor with a favorable antitumor kinase inhibition profile.Journal of medicinal chemistry, , Nov-30, Volume: 49, Issue:24, 2006
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).Blood, , Oct-01, Volume: 114, Issue:14, 2009
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Optimization of 6,6-dimethyl pyrrolo[3,4-c]pyrazoles: Identification of PHA-793887, a potent CDK inhibitor suitable for intravenous dosing.Bioorganic & medicinal chemistry, , Mar-01, Volume: 18, Issue:5, 2010
Discovery of 3,4,6-Trisubstituted Piperidine Derivatives as Orally Active, Low hERG Blocking Akt Inhibitors via Conformational Restriction and Structure-Based Design.Journal of medicinal chemistry, , 08-08, Volume: 62, Issue:15, 2019
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Enables
This protein enables 11 target(s):
| Target | Category | Definition |
|---|
| protein kinase activity | molecular function | Catalysis of the phosphorylation of an amino acid residue in a protein, usually according to the reaction: a protein + ATP = a phosphoprotein + ADP. [PMID:25399640] |
| diacylglycerol-dependent serine/threonine kinase activity | molecular function | Catalysis of the reaction: ATP + a protein = ADP + a phosphoprotein. This reaction requires diacylglycerol. [EC:2.7.11.13] |
| calcium,diacylglycerol-dependent serine/threonine kinase activity | molecular function | Calcium-dependent catalysis of the reaction: ATP + a protein = ADP + a phosphoprotein. [GOC:mah] |
| integrin binding | molecular function | Binding to an integrin. [GOC:ceb] |
| protein binding | molecular function | Binding to a protein. [GOC:go_curators] |
| ATP binding | molecular function | Binding to ATP, adenosine 5'-triphosphate, a universally important coenzyme and enzyme regulator. [ISBN:0198506732] |
| zinc ion binding | molecular function | Binding to a zinc ion (Zn). [GOC:ai] |
| enzyme binding | molecular function | Binding to an enzyme, a protein with catalytic activity. [GOC:jl] |
| histone H3T6 kinase activity | molecular function | Catalysis of the reaction: histone H3-threonine (position 6) + ATP = histone H3-phosphothreonine (position 6) + ADP. This reaction is the addition of a phosphate group to the threonine residue at position 6 of histone H3. [GOC:bf] |
| protein serine kinase activity | molecular function | Catalysis of the reactions: ATP + protein serine = ADP + protein serine phosphate. [RHEA:17989] |
| 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] |
Located In
This protein is located in 9 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] |
| cytoplasm | cellular component | The contents of a cell excluding the plasma membrane and nucleus, but including other subcellular structures. [ISBN:0198547684] |
| mitochondrion | cellular component | A semiautonomous, self replicating organelle that occurs in varying numbers, shapes, and sizes in the cytoplasm of virtually all eukaryotic cells. It is notably the site of tissue respiration. [GOC:giardia, ISBN:0198506732] |
| endoplasmic reticulum | cellular component | The irregular network of unit membranes, visible only by electron microscopy, that occurs in the cytoplasm of many eukaryotic cells. The membranes form a complex meshwork of tubular channels, which are often expanded into slitlike cavities called cisternae. The ER takes two forms, rough (or granular), with ribosomes adhering to the outer surface, and smooth (with no ribosomes attached). [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] |
| plasma membrane | cellular component | The membrane surrounding a cell that separates the cell from its external environment. It consists of a phospholipid bilayer and associated proteins. [ISBN:0716731363] |
| mitochondrial membrane | cellular component | Either of the lipid bilayers that surround the mitochondrion and form the mitochondrial envelope. [GOC:mah, NIF_Subcellular:sao1045389829] |
| perinuclear region of cytoplasm | cellular component | Cytoplasm situated near, or occurring around, the nucleus. [GOC:jid] |
| extracellular exosome | cellular component | A vesicle that is released into the extracellular region by fusion of the limiting endosomal membrane of a multivesicular body with the plasma membrane. Extracellular exosomes, also simply called exosomes, have a diameter of about 40-100 nm. [GOC:BHF, GOC:mah, GOC:vesicles, PMID:15908444, PMID:17641064, PMID:19442504, PMID:19498381, PMID:22418571, PMID:24009894] |
Active In
This protein is active in 1 target(s):
| Target | Category | Definition |
|---|
| ciliary basal body | cellular component | A membrane-tethered, short cylindrical array of microtubules and associated proteins found at the base of a eukaryotic cilium (also called flagellum) that is similar in structure to a centriole and derives from it. The cilium basal body is the site of assembly and remodeling of the cilium and serves as a nucleation site for axoneme growth. As well as anchoring the cilium, it is thought to provide a selective gateway regulating the entry of ciliary proteins and vesicles by intraflagellar transport. [GOC:cilia, GOC:clt, PMID:21750193] |
Part Of
This protein is part of 1 target(s):
| Target | Category | Definition |
|---|
| alphav-beta3 integrin-PKCalpha complex | cellular component | A protein complex that consists of an alphav-beta3 integrin complex bound to protein kinase C alpha. [GOC:BHF, GOC:ebc, PMID:16014375] |
Involved In
This protein is involved in 30 target(s):
| Target | Category | Definition |
|---|
| angiogenesis | biological process | Blood vessel formation when new vessels emerge from the proliferation of pre-existing blood vessels. [ISBN:0878932453] |
| positive regulation of endothelial cell proliferation | biological process | Any process that activates or increases the rate or extent of endothelial cell proliferation. [GOC:add] |
| desmosome assembly | biological process | A cellular process that results in the aggregation, arrangement and bonding together of a set of components to form a desmosome. A desmosome is a patch-like intercellular junction found in vertebrate tissues, consisting of parallel zones of two cell membranes, separated by an space of 25-35 nm, and having dense fibrillar plaques in the subjacent cytoplasm. [GOC:hjd, ISBN:0198506732] |
| chromatin remodeling | biological process | A dynamic process of chromatin reorganization resulting in changes to chromatin structure. These changes allow DNA metabolic processes such as transcriptional regulation, DNA recombination, DNA repair, and DNA replication. [GOC:jid, GOC:vw, PMID:12042764, PMID:12697820] |
| protein phosphorylation | biological process | The process of introducing a phosphate group on to a protein. [GOC:hb] |
| mitotic nuclear membrane disassembly | biological process | The mitotic cell cycle process in which the controlled partial or complete breakdown of the nuclear membranes during occurs during mitosis. [GOC:bf, PMID:32848252] |
| cell adhesion | biological process | The attachment of a cell, either to another cell or to an underlying substrate such as the extracellular matrix, via cell adhesion molecules. [GOC:hb, GOC:pf] |
| positive regulation of endothelial cell migration | biological process | Any process that increases the rate, frequency, or extent of the orderly movement of an endothelial cell into the extracellular matrix to form an endothelium. [GOC:BHF, GOC:dph, GOC:tb] |
| positive regulation of cardiac muscle hypertrophy | biological process | Any process that increases the rate, frequency or extent of the enlargement or overgrowth of all or part of the heart due to an increase in size (not length) of individual cardiac muscle fibers, without cell division. [GOC:BHF, GOC:dph, GOC:tb] |
| peptidyl-serine phosphorylation | biological process | The phosphorylation of peptidyl-serine to form peptidyl-O-phospho-L-serine. [RESID:AA0037] |
| peptidyl-threonine phosphorylation | biological process | The phosphorylation of peptidyl-threonine to form peptidyl-O-phospho-L-threonine. [RESID:AA0038] |
| positive regulation of cell migration | biological process | Any process that activates or increases the frequency, rate or extent of cell migration. [GOC:go_curators] |
| positive regulation of lipopolysaccharide-mediated signaling pathway | biological process | Any process that activates or increases the frequency, rate or extent of signaling in response to detection of lipopolysaccharide. [GOC:mah] |
| negative regulation of glial cell apoptotic process | biological process | Any process that stops, prevents, or reduces the frequency, rate, or extent of glial cell apoptotic process. [GOC:mah, GOC:mtg_apoptosis] |
| regulation of mRNA stability | biological process | Any process that modulates the propensity of mRNA molecules to degradation. Includes processes that both stabilize and destabilize mRNAs. [GOC:jl] |
| positive regulation of blood vessel endothelial cell migration | biological process | Any process that activates or increases the frequency, rate or extent of the migration of the endothelial cells of blood vessels. [GOC:go_curators] |
| post-translational protein modification | biological process | The process of covalently altering one or more amino acids in a protein after the protein has been completely translated and released from the ribosome. [GOC:jsg] |
| positive regulation of macrophage differentiation | biological process | Any process that activates or increases the frequency, rate or extent of macrophage differentiation. [GOC:go_curators] |
| positive regulation of angiogenesis | biological process | Any process that activates or increases angiogenesis. [GOC:go_curators] |
| positive regulation of bone resorption | biological process | Any process that activates or increases the frequency, rate or extent of bone resorption. [GOC:go_curators] |
| positive regulation of cell adhesion | biological process | Any process that activates or increases the frequency, rate or extent of cell adhesion. [GOC:go_curators] |
| positive regulation of mitotic cell cycle | biological process | Any process that activates or increases the rate or extent of progression through the mitotic cell cycle. [GOC:dph, GOC:go_curators, GOC:tb] |
| positive regulation of ERK1 and ERK2 cascade | biological process | Any process that activates or increases the frequency, rate or extent of signal transduction mediated by the ERK1 and ERK2 cascade. [GOC:mah] |
| response to interleukin-1 | biological process | Any process that results in a change in state or activity of a cell or an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of an interleukin-1 stimulus. [GOC:BHF, GOC:mah] |
| regulation of platelet aggregation | biological process | Any process that modulates the rate, frequency or extent of platelet aggregation. Platelet aggregation is the adhesion of one platelet to one or more other platelets via adhesion molecules. [GOC:dph, GOC:tb] |
| apoptotic signaling pathway | biological process | The series of molecular signals which triggers the apoptotic death of a cell. The pathway starts with reception of a signal, and ends when the execution phase of apoptosis is triggered. [GOC:mtg_apoptosis] |
| positive regulation of adenylate cyclase-activating G protein-coupled receptor signaling pathway | biological process | Any process that activates or increases the frequency, rate or extent of an adenylate cyclase-activating G protein-coupled receptor signaling pathway. [GOC:hjd, PMID:19246489] |
| positive regulation of angiotensin-activated signaling pathway | biological process | Any process that activates or increases the frequency, rate or extent of the angiotensin-activated signaling pathway. [GOC:lf, PMID:28784619] |
| positive regulation of dense core granule biogenesis | biological process | Any process that activates or increases the frequency, rate or extent of dense core granule biogenesis. [GOC:obol] |
| intracellular signal transduction | biological process | The process in which a signal is passed on to downstream components within the cell, which become activated themselves to further propagate the signal and finally trigger a change in the function or state of the cell. [GOC:bf, GOC:jl, GOC:signaling, ISBN:3527303782] |