Proteins > Serine/threonine-protein kinase B-raf
Page last updated: 2024-08-07 15:59:52
Serine/threonine-protein kinase B-raf
A B-Raf proto-oncogene serine/threonine-protein kinase that is encoded in the genome of human. [PRO:DNx, UniProtKB:P15056]
Synonyms
EC 2.7.11.1;
Proto-oncogene B-Raf;
p94;
v-Raf murine sarcoma viral oncogene homolog B1
Research
Bioassay Publications (123)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 20 (16.26) | 29.6817 |
| 2010's | 83 (67.48) | 24.3611 |
| 2020's | 20 (16.26) | 2.80 |
Compounds (251)
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 |
| sb 202190 | Homo sapiens (human) | Kd | 2.7100 | 2 | 2 |
| imatinib | Homo sapiens (human) | Kd | 11.3200 | 5 | 5 |
| triciribine phosphate | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| staurosporine | Homo sapiens (human) | Kd | 10.0000 | 4 | 4 |
| picropodophyllin | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| gefitinib | Homo sapiens (human) | Kd | 14.0000 | 5 | 5 |
| lestaurtinib | Homo sapiens (human) | Kd | 14.0000 | 5 | 5 |
| perifosine | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| vatalanib | Homo sapiens (human) | Kd | 14.0000 | 5 | 5 |
| ruboxistaurin | Homo sapiens (human) | Kd | 14.0000 | 5 | 5 |
| canertinib | Homo sapiens (human) | Kd | 16.6667 | 5 | 6 |
| birb 796 | Homo sapiens (human) | Kd | 6.3500 | 4 | 4 |
| cyc 202 | Homo sapiens (human) | Kd | 16.6667 | 3 | 3 |
| sb 203580 | Homo sapiens (human) | Kd | 0.6200 | 4 | 4 |
| enzastaurin | Homo sapiens (human) | Kd | 16.6667 | 3 | 3 |
| erlotinib | Homo sapiens (human) | Kd | 14.0000 | 5 | 5 |
| lapatinib | Homo sapiens (human) | Kd | 14.0000 | 5 | 5 |
| sorafenib | Homo sapiens (human) | EC50 | 0.0030 | 1 | 1 |
| sorafenib | Homo sapiens (human) | Kd | 4.0855 | 8 | 8 |
| pd 173955 | Homo sapiens (human) | Kd | 0.0051 | 2 | 2 |
| s 1033 | Homo sapiens (human) | Kd | 10.7567 | 3 | 3 |
| xl147 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| bms 387032 | Homo sapiens (human) | Kd | 10.5800 | 5 | 5 |
| sf 2370 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| tandutinib | Homo sapiens (human) | Kd | 12.8571 | 7 | 7 |
| vx-745 | Homo sapiens (human) | Kd | 10.0000 | 4 | 4 |
| dasatinib | Homo sapiens (human) | Kd | 1.0742 | 5 | 5 |
| ha 1100 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| 7-epi-hydroxystaurosporine | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| zd 6474 | Homo sapiens (human) | Kd | 14.0000 | 5 | 5 |
| 4-(5-benzo(1,3)dioxol-5-yl-4-pyridin-2-yl-1h-imidazol-2-yl)benzamide | Homo sapiens (human) | Kd | 10.0000 | 2 | 2 |
| imd 0354 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| sirolimus | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| alvocidib | Homo sapiens (human) | Kd | 14.0000 | 5 | 5 |
| bosutinib | Homo sapiens (human) | Kd | 16.6667 | 3 | 3 |
| orantinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| su 11248 | Homo sapiens (human) | Kd | 12.8571 | 7 | 7 |
| palbociclib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| jnj-7706621 | Homo sapiens (human) | Kd | 10.0000 | 2 | 2 |
| vx680 | Homo sapiens (human) | Kd | 14.0000 | 5 | 5 |
| 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 | 16.6667 | 3 | 3 |
| 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 | 2 |
| pd 0325901 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| midostaurin | Homo sapiens (human) | Kd | 12.8571 | 7 | 7 |
| 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 | 16.6667 | 3 | 3 |
| pi103 | Homo sapiens (human) | Kd | 2.6000 | 4 | 4 |
| 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 | 16.6667 | 3 | 3 |
| tofacitinib | Homo sapiens (human) | Kd | 14.0000 | 5 | 5 |
| 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 |
| l-779,450 | Homo sapiens (human) | Kd | 0.0024 | 3 | 3 |
| masitinib | Homo sapiens (human) | Kd | 13.9333 | 3 | 3 |
| ly-2157299 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| pazopanib | Homo sapiens (human) | Kd | 6.4640 | 5 | 5 |
| azd 6244 | Homo sapiens (human) | Kd | 16.6667 | 3 | 3 |
| su 14813 | Homo sapiens (human) | Kd | 14.0000 | 5 | 5 |
| 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 | 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 | 11.3667 | 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 | 10.0000 | 2 | 2 |
| azd 7762 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| regorafenib | Homo sapiens (human) | Kd | 3.1250 | 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 | 10.2067 | 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 | 2 |
| at 7519 | Homo sapiens (human) | Kd | 16.6667 | 3 | 3 |
| bms-690514 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| bi 2536 | Homo sapiens (human) | Kd | 16.6667 | 3 | 3 |
| inno-406 | Homo sapiens (human) | Kd | 1.1350 | 1 | 1 |
| nvp-ast487 | Homo sapiens (human) | Kd | 0.9150 | 4 | 4 |
| kw 2449 | Homo sapiens (human) | Kd | 16.6667 | 3 | 3 |
| danusertib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| abt 869 | Homo sapiens (human) | Kd | 14.0000 | 5 | 5 |
| 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 | 4 | 4 |
| tak 285 | Homo sapiens (human) | Kd | 30.0000 | 1 | 2 |
| idelalisib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| 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 | 6.6120 | 5 | 5 |
| motesanib | Homo sapiens (human) | Kd | 6.3640 | 5 | 5 |
| fostamatinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| trametinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| mln8054 | Homo sapiens (human) | Kd | 14.0000 | 5 | 5 |
| pf-562,271 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| GDC-0879 | Homo sapiens (human) | Kd | 0.0002 | 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 | 14.0000 | 5 | 5 |
| nvp-tae684 | Homo sapiens (human) | Kd | 10.0000 | 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 | 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 |
| ro5126766 | Homo sapiens (human) | Kd | 0.0070 | 1 | 1 |
| fedratinib | Homo sapiens (human) | Kd | 16.3667 | 3 | 3 |
| 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 | 2 |
| gdc 0941 | Homo sapiens (human) | Kd | 16.6667 | 3 | 3 |
| icotinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| ph 797804 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| kx-01 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| plx 4720 | Homo sapiens (human) | Kd | 0.2150 | 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 | 5.2330 | 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 | 1.1940 | 1 | 1 |
| amg 900 | Homo sapiens (human) | Kd | 2.4820 | 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 | 14.0000 | 5 | 5 |
| 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 | 26.0180 | 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 | 12.1333 | 3 | 3 |
| poziotinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| asp3026 | Homo sapiens (human) | Kd | 30.0000 | 1 | 2 |
| entrectinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| pexidartinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| TAK-580 | Homo sapiens (human) | Kd | 3.7720 | 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) | EC50 | 1.2284 | 3 | 3 |
| plx4032 | Homo sapiens (human) | Kd | 1.1650 | 3 | 3 |
| gsk 1363089 | Homo sapiens (human) | Kd | 11.9333 | 3 | 3 |
| arry-334543 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| kin-193 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| mk 2461 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| bay 869766 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| as 703026 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| baricitinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| dabrafenib | Homo sapiens (human) | EC50 | 0.2649 | 2 | 2 |
| dabrafenib | Homo sapiens (human) | Kd | 0.0220 | 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 | 30.0000 | 1 | 1 |
| mk-8776 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| afuresertib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| gsk 1070916 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| jnj38877605 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| dinaciclib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| gilteritinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| alectinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| glpg0634 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| encorafenib | Homo sapiens (human) | Kd | 0.1240 | 1 | 1 |
| bms-911543 | Homo sapiens (human) | Kd | 30.0000 | 1 | 2 |
| gsk2141795 | Homo sapiens (human) | Kd | 30.0000 | 1 | 2 |
| azd8186 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| byl719 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| cep-32496 | Homo sapiens (human) | Kd | 0.5904 | 5 | 5 |
| 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 | 1 |
| at 9283 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| otssp167 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| chir 258 | Homo sapiens (human) | Kd | 14.0000 | 5 | 5 |
| osi 027 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| sb-590885 | Homo sapiens (human) | EC50 | 0.4300 | 8 | 8 |
| sb-590885 | Homo sapiens (human) | Kd | 0.0003 | 3 | 3 |
| nintedanib | Homo sapiens (human) | Kd | 16.6667 | 3 | 3 |
| bay 80-6946 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| pp242 | Homo sapiens (human) | Kd | 1.2400 | 2 | 2 |
Drugs with Other Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| plx4032 | Homo sapiens (human) | INH | 0.0655 | 2 | 2 |
| dabrafenib | Homo sapiens (human) | INH | 0.0030 | 2 | 2 |
Design, synthesis, and in vitro evaluation of N-(3-(3-alkyl-1H-pyrazol-5-yl) phenyl)-aryl amide for selective RAF inhibition.Bioorganic & medicinal chemistry letters, , 02-15, Volume: 29, Issue:4, 2019
Novel LCK/FMS inhibitors based on phenoxypyrimidine scaffold as potential treatment for inflammatory disorders.European journal of medicinal chemistry, , Dec-01, Volume: 141, 2017
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The design, synthesis, and evaluation of 8 hybrid DFG-out allosteric kinase inhibitors: a structural analysis of the binding interactions of Gleevec, Nexavar, and BIRB-796.Bioorganic & medicinal chemistry, , Aug-01, Volume: 18, Issue:15, 2010
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
Isoxazole derivatives as anticancer agent: A review on synthetic strategies, mechanism of action and SAR studies.European journal of medicinal chemistry, , Oct-05, Volume: 221, 2021
[no title available]European journal of medicinal chemistry, , Apr-05, Volume: 215, 2021
Discovery of first-in-class imidazothiazole-based potent and selective ErbB4 (HER4) kinase inhibitors.European journal of medicinal chemistry, , Nov-15, Volume: 224, 2021
Isolation, Characterization, and Structure-Activity Relationship Analysis of Abietane Diterpenoids from Callicarpa bodinieri as Spleen Tyrosine Kinase Inhibitors.Journal of natural products, , 04-27, Volume: 81, Issue:4, 2018
Design, synthesis and biological evaluation of pyrazol-furan carboxamide analogues as novel Akt kinase inhibitors.European journal of medicinal chemistry, , Jul-19, Volume: 117, 2016
Synthesis and biological evaluation of 3-([1,2,4]triazolo[4,3-a]pyridin-3-yl)-4-(indol-3-yl)-maleimides as potent, selective GSK-3β inhibitors and neuroprotective agents.Bioorganic & medicinal chemistry, , Mar-01, Volume: 23, Issue:5, 2015
Discovery of 4-arylamido 3-methyl isoxazole derivatives as novel FMS kinase inhibitors.European journal of medicinal chemistry, , Sep-18, Volume: 102, 2015
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Identification and optimization of new dual inhibitors of B-Raf and epidermal growth factor receptor kinases for overcoming resistance against vemurafenib.Journal of medicinal chemistry, , Mar-27, Volume: 57, Issue:6, 2014
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).Blood, , Oct-01, Volume: 114, Issue:14, 2009
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The design, synthesis, and evaluation of 8 hybrid DFG-out allosteric kinase inhibitors: a structural analysis of the binding interactions of Gleevec, Nexavar, and BIRB-796.Bioorganic & medicinal chemistry, , Aug-01, Volume: 18, Issue:15, 2010
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
A Selective and Brain Penetrant p38αMAPK Inhibitor Candidate for Neurologic and Neuropsychiatric Disorders That Attenuates Neuroinflammation and Cognitive Dysfunction.Journal of medicinal chemistry, , 06-13, Volume: 62, Issue:11, 2019
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
Design, synthesis and anticancer evaluation of novel spirobenzo[h]chromene and spirochromane derivatives with dual EGFR and B-RAF inhibitory activities.European journal of medicinal chemistry, , Apr-25, Volume: 150, 2018
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
Comprehensive review for anticancer hybridized multitargeting HDAC inhibitors.European journal of medicinal chemistry, , Jan-01, Volume: 209, 2021
[no title available]Journal of medicinal chemistry, , 11-11, Volume: 64, Issue:21, 2021
[no title available]Journal of medicinal chemistry, , 08-26, Volume: 64, Issue:16, 2021
Targeting Rearranged during Transfection in Cancer: A Perspective on Small-Molecule Inhibitors and Their Clinical Development.Journal of medicinal chemistry, , 08-26, Volume: 64, Issue:16, 2021
Design and synthesis of novel pyrrolo[2,3-b]pyridine derivatives targeting Bioorganic & medicinal chemistry, , 06-01, Volume: 28, Issue:11, 2020
[no title available]European journal of medicinal chemistry, , Feb-01, Volume: 163, 2019
Novel potent substituted 4-amino-2-thiopyrimidines as dual VEGFR-2 and BRAF kinase inhibitors.European journal of medicinal chemistry, , Oct-01, Volume: 179, 2019
The association between anti-tumor potency and structure-activity of protein-kinases inhibitors based on quinazoline molecular skeleton.Bioorganic & medicinal chemistry, , 02-01, Volume: 27, Issue:3, 2019
Discovery of novel phenoxybenzamide analogues as Raf/HDAC dual inhibitors.Bioorganic & medicinal chemistry letters, , 07-01, Volume: 29, Issue:13, 2019
Design and discovery of thioether and nicotinamide containing sorafenib analogues as multikinase inhibitors targeting B-Raf, B-RafBioorganic & medicinal chemistry, , 05-15, Volume: 26, Issue:9, 2018
Current Insights of BRAF Inhibitors in Cancer.Journal of medicinal chemistry, , 07-26, Volume: 61, Issue:14, 2018
[no title available]European journal of medicinal chemistry, , Jul-15, Volume: 155, 2018
Cyclin-Dependent Kinase 8: A New Hope in Targeted Cancer Therapy?Journal of medicinal chemistry, , 06-28, Volume: 61, Issue:12, 2018
Design, synthesis and antitumor activity of Novel Sorafenib derivatives bearing pyrazole scaffold.Bioorganic & medicinal chemistry, , 10-15, Volume: 25, Issue:20, 2017
Design, synthesis and evaluation of derivatives based on pyrimidine scaffold as potent Pan-Raf inhibitors to overcome resistance.European journal of medicinal chemistry, , Apr-21, Volume: 130, 2017
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
[no title available]Bioorganic & medicinal chemistry letters, , 11-15, Volume: 26, Issue:22, 2016
Design and synthesis of new potent anticancer benzothiazole amides and ureas featuring pyridylamide moiety and possessing dual B-Raf(V600E) and C-Raf kinase inhibitory activities.European journal of medicinal chemistry, , Jun-10, Volume: 115, 2016
Design, synthesis and biological evaluation of bis-aryl ureas and amides based on 2-amino-3-purinylpyridine scaffold as DFG-out B-Raf kinase inhibitors.European journal of medicinal chemistry, , Jan-07, Volume: 89, 2015
Probing a 3,4'-bis-guanidinium diaryl derivative as an allosteric inhibitor of the Ras pathway.Bioorganic & medicinal chemistry letters, , Oct-01, Volume: 25, Issue:19, 2015
Design, synthesis and evaluation of novel 2-(1H-imidazol-2-yl) pyridine Sorafenib derivatives as potential BRAF inhibitors and anti-tumor agents.European journal of medicinal chemistry, , Jan-27, Volume: 90, 2015
Identification of type II inhibitors targeting BRAF using privileged pharmacophores.Chemical biology & drug design, , Volume: 83, Issue:1, 2014
Design, synthesis and biological evaluation of novel thieno[3,2-d]pyrimidine derivatives containing diaryl urea moiety as potent antitumor agents.European journal of medicinal chemistry, , Oct-06, Volume: 85, 2014
Design, synthesis and evaluation of novel diaryl urea derivatives as potential antitumor agents.European journal of medicinal chemistry, , Apr-22, Volume: 77, 2014
Design, synthesis and biological evaluation of novel thieno[3,2-d]pyrimidine derivatives possessing diaryl semicarbazone scaffolds as potent antitumor agents.European journal of medicinal chemistry, , Nov-24, Volume: 87, 2014
Guanidinium-based derivatives: searching for new kinase inhibitors.European journal of medicinal chemistry, , Jun-23, Volume: 81, 2014
A new target for an old drug: identifying mitoxantrone as a nanomolar inhibitor of PIM1 kinase via kinome-wide selectivity modeling.Journal of medicinal chemistry, , Mar-28, Volume: 56, Issue:6, 2013
Synthesis and biological evaluation of sorafenib- and regorafenib-like sEH inhibitors.Bioorganic & medicinal chemistry letters, , Jul-01, Volume: 23, Issue:13, 2013
Conformation-specific effects of Raf kinase inhibitors.Journal of medicinal chemistry, , Sep-13, Volume: 55, Issue:17, 2012
Structure-based design of isoindoline-1,3-diones and 2,3-dihydrophthalazine-1,4-diones as novel B-Raf inhibitors.Bioorganic & medicinal chemistry letters, , Dec-01, Volume: 21, Issue:23, 2011
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
4-Quinazolinyloxy-diaryl ureas as novel BRAFV600E inhibitors.Bioorganic & medicinal chemistry letters, , Sep-15, Volume: 21, Issue:18, 2011
Design and optimization of potent and orally bioavailable tetrahydronaphthalene Raf inhibitors.Journal of medicinal chemistry, , Mar-24, Volume: 54, Issue:6, 2011
The discovery of furo[2,3-c]pyridine-based indanone oximes as potent and selective B-Raf inhibitors.Bioorganic & medicinal chemistry letters, , Feb-15, Volume: 21, Issue:4, 2011
The design, synthesis, and evaluation of 8 hybrid DFG-out allosteric kinase inhibitors: a structural analysis of the binding interactions of Gleevec, Nexavar, and BIRB-796.Bioorganic & medicinal chemistry, , Aug-01, Volume: 18, Issue:15, 2010
Synthesis of aminoquinazoline derivatives and their antiproliferative activities against melanoma cell line.Bioorganic & medicinal chemistry letters, , Oct-01, Volume: 20, Issue:19, 2010
1,4-dihydropyrazolo[4,3-d]imidazole phenyl derivatives: a novel type II Raf kinase inhibitors.Bioorganic & medicinal chemistry letters, , Jun-15, Volume: 20, Issue:12, 2010
Discovery and initial SAR of pyrimidin-4-yl-1H-imidazole derivatives with antiproliferative activity against melanoma cell lines.Bioorganic & medicinal chemistry letters, , Mar-01, Volume: 20, Issue:5, 2010
Pyridoimidazolones as novel potent inhibitors of v-Raf murine sarcoma viral oncogene homologue B1 (BRAF).Journal of medicinal chemistry, , Apr-23, Volume: 52, Issue:8, 2009
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
Novel inhibitors of the v-raf murine sarcoma viral oncogene homologue B1 (BRAF) based on a 2,6-disubstituted pyrazine scaffold.Journal of medicinal chemistry, , Jun-12, Volume: 51, Issue:11, 2008
Design and synthesis of orally bioavailable benzimidazoles as Raf kinase inhibitors.Journal of medicinal chemistry, , Nov-27, Volume: 51, Issue:22, 2008
Dual binding site inhibitors of B-RAF kinase.Bioorganic & medicinal chemistry letters, , May-01, Volume: 18, Issue:9, 2008
Identification of BRAF inhibitors through in silico screening.Journal of medicinal chemistry, , Oct-09, Volume: 51, Issue:19, 2008
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
The selectivity of protein kinase inhibitors: a further update.The Biochemical journal, , Dec-15, Volume: 408, Issue:3, 2007
Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling.Proceedings of the National Academy of Sciences of the United States of America, , Dec-11, Volume: 104, Issue:50, 2007
Novel inhibitors of B-RAF based on a disubstituted pyrazine scaffold. Generation of a nanomolar lead.Journal of medicinal chemistry, , Jan-12, Volume: 49, Issue:1, 2006
Rational design of inhibitors that bind to inactive kinase conformations.Nature chemical biology, , Volume: 2, Issue:7, 2006
Features of selective kinase inhibitors.Chemistry & biology, , Volume: 12, Issue:6, 2005
BAY 43-9006 exhibits broad spectrum oral antitumor activity and targets the RAF/MEK/ERK pathway and receptor tyrosine kinases involved in tumor progression and angiogenesis.Cancer research, , Oct-01, Volume: 64, Issue:19, 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
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).Blood, , Oct-01, Volume: 114, Issue:14, 2009
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).Blood, , Oct-01, Volume: 114, Issue:14, 2009
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
Encoding BRAF inhibitor functions in protein degraders.RSC medicinal chemistry, , Jun-22, Volume: 13, Issue:6, 2022
Ring closure strategy leads to potent RIPK3 inhibitors.European journal of medicinal chemistry, , May-05, Volume: 217, 2021
[no title available]European journal of medicinal chemistry, , Dec-15, Volume: 208, 2020
Design, synthesis, and biological evaluations of novel 3-amino-4-ethynyl indazole derivatives as Bcr-Abl kinase inhibitors with potent cellular antileukemic activity.European journal of medicinal chemistry, , Dec-01, Volume: 207, 2020
ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells.European journal of medicinal chemistry, , Jan-01, Volume: 161, 2019
Discovery of highly potent V600E-B-RAF kinase inhibitors: Molecular modeling study.Bioorganic & medicinal chemistry, , 02-15, Volume: 27, Issue:4, 2019
Integrating docking scores and key interaction profiles to improve the accuracy of molecular docking: towards novel B-RafMedChemComm, , Sep-01, Volume: 8, Issue:9, 2017
Design, synthesis and biological evaluation of benzyl 2-(1H-imidazole-1-yl) pyrimidine analogues as selective and potent Raf inhibitors.Bioorganic & medicinal chemistry letters, , Aug-01, Volume: 24, Issue:15, 2014
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Discovery of 3-benzyl-1,3-benzoxazine-2,4-dione analogues as allosteric mitogen-activated kinase kinase (MEK) inhibitors and anti-enterovirus 71 (EV71) agents.Bioorganic & medicinal chemistry, , 08-15, Volume: 24, Issue:16, 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
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).Blood, , Oct-01, Volume: 114, Issue:14, 2009
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The discovery of furo[2,3-c]pyridine-based indanone oximes as potent and selective B-Raf inhibitors.Bioorganic & medicinal chemistry letters, , Feb-15, Volume: 21, Issue:4, 2011
The identification of potent, selective and CNS penetrant furan-based inhibitors of B-Raf kinase.Bioorganic & medicinal chemistry letters, , Aug-01, Volume: 18, Issue:15, 2008
The identification of potent and selective imidazole-based inhibitors of B-Raf kinase.Bioorganic & medicinal chemistry letters, , Jan-15, Volume: 16, Issue:2, 2006
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
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
Targeting Rearranged during Transfection in Cancer: A Perspective on Small-Molecule Inhibitors and Their Clinical Development.Journal of medicinal chemistry, , 08-26, Volume: 64, Issue:16, 2021
Novel potent substituted 4-amino-2-thiopyrimidines as dual VEGFR-2 and BRAF kinase inhibitors.European journal of medicinal chemistry, , Oct-01, Volume: 179, 2019
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Small molecule inhibitors of BRAF in clinical trials.Bioorganic & medicinal chemistry letters, , Jan-15, Volume: 22, Issue:2, 2012
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
Inhibition of colony-stimulating-factor-1 signaling in vivo with the orally bioavailable cFMS kinase inhibitor GW2580.Proceedings of the National Academy of Sciences of the United States of America, , Nov-01, Volume: 102, Issue:44, 2005
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Design and synthesis of novel human epidermal growth factor receptor 2 (HER2)/epidermal growth factor receptor (EGFR) dual inhibitors bearing a pyrrolo[3,2-d]pyrimidine scaffold.Journal of medicinal chemistry, , Dec-08, Volume: 54, Issue:23, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
Privileged Structures and Polypharmacology within and between Protein Families.ACS medicinal chemistry letters, , Dec-13, Volume: 9, Issue:12, 2018
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Discovery of RAF265: A Potent mut-B-RAF Inhibitor for the Treatment of Metastatic Melanoma.ACS medicinal chemistry letters, , Sep-10, Volume: 6, Issue:9, 2015
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
Privileged Structures and Polypharmacology within and between Protein Families.ACS medicinal chemistry letters, , Dec-13, Volume: 9, Issue:12, 2018
Highly potent and selective 3-N-methylquinazoline-4(3H)-one based inhibitors of B-Raf(V600E) kinase.Bioorganic & medicinal chemistry letters, , Apr-15, Volume: 24, Issue:8, 2014
Discovery and optimization of a novel series of potent mutant B-Raf(V600E) selective kinase inhibitors.Journal of medicinal chemistry, , Mar-14, Volume: 56, Issue:5, 2013
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
Current Insights of BRAF Inhibitors in Cancer.Journal of medicinal chemistry, , 07-26, Volume: 61, Issue:14, 2018
Privileged Structures and Polypharmacology within and between Protein Families.ACS medicinal chemistry letters, , Dec-13, Volume: 9, Issue:12, 2018
Design, synthesis and biological evaluation of novel 5-phenyl-1H-pyrazole derivatives as potential BRAF(V600E) inhibitors.Bioorganic & medicinal chemistry, , Nov-01, Volume: 22, Issue:21, 2014
Conformation-specific effects of Raf kinase inhibitors.Journal of medicinal chemistry, , Sep-13, Volume: 55, Issue:17, 2012
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The discovery of furo[2,3-c]pyridine-based indanone oximes as potent and selective B-Raf inhibitors.Bioorganic & medicinal chemistry letters, , Feb-15, Volume: 21, Issue:4, 2011
Potent and selective pyrazole-based inhibitors of B-Raf kinase.Bioorganic & medicinal chemistry letters, , Aug-15, Volume: 18, 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
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Preclinical disposition of GDC-0973 and prospective and retrospective analysis of human dose and efficacy predictions.Drug metabolism and disposition: the biological fate of chemicals, , Volume: 40, Issue:5, 2012
The overview of Mitogen-activated extracellular signal-regulated kinase (MEK)-based dual inhibitor in the treatment of cancers.Bioorganic & medicinal chemistry, , 09-15, Volume: 70, 2022
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
Design and synthesis of novel pyrrolo[2,3-b]pyridine derivatives targeting Bioorganic & medicinal chemistry, , 06-01, Volume: 28, Issue:11, 2020
Current Insights of BRAF Inhibitors in Cancer.Journal of medicinal chemistry, , 07-26, Volume: 61, Issue:14, 2018
Privileged Structures and Polypharmacology within and between Protein Families.ACS medicinal chemistry letters, , Dec-13, Volume: 9, Issue:12, 2018
Discovery of EBI-907: A highly potent and orally active B-Raf(V600E) inhibitor for the treatment of melanoma and associated cancers.Bioorganic & medicinal chemistry letters, , Feb-01, Volume: 26, Issue:3, 2016
Conformation-specific effects of Raf kinase inhibitors.Journal of medicinal chemistry, , Sep-13, Volume: 55, Issue:17, 2012
Small molecule inhibitors of BRAF in clinical trials.Bioorganic & medicinal chemistry letters, , Jan-15, Volume: 22, Issue:2, 2012
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
Discovery of a selective inhibitor of oncogenic B-Raf kinase with potent antimelanoma activity.Proceedings of the National Academy of Sciences of the United States of America, , Feb-26, Volume: 105, Issue:8, 2008
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).Blood, , Oct-01, Volume: 114, Issue:14, 2009
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
Evaluation of imidazo[2,1-b]thiazole-based anticancer agents in one decade (2011-2020): Current status and future prospects.Bioorganic & medicinal chemistry, , 01-01, Volume: 29, 2021
Modification of imidazothiazole derivatives gives promising activity in B-Raf kinase enzyme inhibition; synthesis, in vitro studies and molecular docking.Bioorganic & medicinal chemistry letters, , 10-15, Volume: 30, Issue:20, 2020
Discovery of Selective Small Molecule Degraders of BRAF-V600E.Journal of medicinal chemistry, , 04-23, Volume: 63, Issue:8, 2020
Design and synthesis of novel pyrrolo[2,3-b]pyridine derivatives targeting Bioorganic & medicinal chemistry, , 06-01, Volume: 28, Issue:11, 2020
[no title available]European journal of medicinal chemistry, , Feb-01, Volume: 163, 2019
Rigidification Dramatically Improves Inhibitor Selectivity for RAF Kinases.ACS medicinal chemistry letters, , Jul-11, Volume: 10, Issue:7, 2019
The association between anti-tumor potency and structure-activity of protein-kinases inhibitors based on quinazoline molecular skeleton.Bioorganic & medicinal chemistry, , 02-01, Volume: 27, Issue:3, 2019
Light-controlled inhibition of BRAFV600E kinase.European journal of medicinal chemistry, , Oct-01, Volume: 179, 2019
Design and biological evaluation of novel triaryl pyrazoline derivatives with dioxane moiety for selective BRAFEuropean journal of medicinal chemistry, , Jul-15, Volume: 155, 2018
Current Insights of BRAF Inhibitors in Cancer.Journal of medicinal chemistry, , 07-26, Volume: 61, Issue:14, 2018
Privileged Structures and Polypharmacology within and between Protein Families.ACS medicinal chemistry letters, , Dec-13, Volume: 9, Issue:12, 2018
Effects of rigidity on the selectivity of protein kinase inhibitors.European journal of medicinal chemistry, , Feb-25, Volume: 146, 2018
Non-kinase targets of protein kinase inhibitors.Nature reviews. Drug discovery, , Volume: 16, Issue:6, 2017
Structure Based Design of N-(3-((1H-Pyrazolo[3,4-b]pyridin-5-yl)ethynyl)benzenesulfonamides as Selective Leucine-Zipper and Sterile-α Motif Kinase (ZAK) Inhibitors.Journal of medicinal chemistry, , 07-13, Volume: 60, Issue:13, 2017
Design and Discovery of N-(2-Methyl-5'-morpholino-6'-((tetrahydro-2H-pyran-4-yl)oxy)-[3,3'-bipyridin]-5-yl)-3-(trifluoromethyl)benzamide (RAF709): A Potent, Selective, and Efficacious RAF Inhibitor Targeting RAS Mutant Cancers.Journal of medicinal chemistry, , 06-22, Volume: 60, Issue:12, 2017
Integrating docking scores and key interaction profiles to improve the accuracy of molecular docking: towards novel B-RafMedChemComm, , Sep-01, Volume: 8, Issue:9, 2017
Design, synthesis and evaluation of derivatives based on pyrimidine scaffold as potent Pan-Raf inhibitors to overcome resistance.European journal of medicinal chemistry, , Apr-21, Volume: 130, 2017
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Natural Products as Sources of New Drugs from 1981 to 2014.Journal of natural products, , Mar-25, Volume: 79, Issue:3, 2016
Design and synthesis of new imidazo[1,2-a]pyridine and imidazo[1,2-a]pyrazine derivatives with antiproliferative activity against melanoma cells.European journal of medicinal chemistry, , Jan-27, Volume: 108, 2016
[no title available]Bioorganic & medicinal chemistry letters, , 10-15, Volume: 26, Issue:20, 2016
Purinylpyridinylamino-based DFG-in/αC-helix-out B-Raf inhibitors: Applying mutant versus wild-type B-Raf selectivity indices for compound profiling.Bioorganic & medicinal chemistry, , 05-15, Volume: 24, Issue:10, 2016
Design and synthesis of N-(4-aminopyridin-2-yl)amides as B-Raf(V600E) inhibitors.Bioorganic & medicinal chemistry letters, , 06-15, Volume: 26, Issue:12, 2016
Design, synthesis and biological evaluation of bis-aryl ureas and amides based on 2-amino-3-purinylpyridine scaffold as DFG-out B-Raf kinase inhibitors.European journal of medicinal chemistry, , Jan-07, Volume: 89, 2015
N-(3-Ethynyl-2,4-difluorophenyl)sulfonamide Derivatives as Selective Raf Inhibitors.ACS medicinal chemistry letters, , May-14, Volume: 6, Issue:5, 2015
Discovery of 1-(3,3-dimethylbutyl)-3-(2-fluoro-4-methyl-5-(7-methyl-2-(methylamino)pyrido[2,3-d]pyrimidin-6-yl)phenyl)urea (LY3009120) as a pan-RAF inhibitor with minimal paradoxical activation and activity against BRAF or RAS mutant tumor cells.Journal of medicinal chemistry, , May-28, Volume: 58, Issue:10, 2015
Recent progress on MAP kinase pathway inhibitors.Bioorganic & medicinal chemistry letters, , Oct-01, Volume: 25, Issue:19, 2015
Identification and optimization of new dual inhibitors of B-Raf and epidermal growth factor receptor kinases for overcoming resistance against vemurafenib.Journal of medicinal chemistry, , Mar-27, Volume: 57, Issue:6, 2014
Synthetic approaches to the 2011 new drugs.Bioorganic & medicinal chemistry, , Jun-01, Volume: 21, Issue:11, 2013
Combining pharmacophore, docking and substructure search approaches to identify and optimize novel B-RafV600E inhibitors.Bioorganic & medicinal chemistry letters, , Sep-01, Volume: 22, Issue:17, 2012
Conformation-specific effects of Raf kinase inhibitors.Journal of medicinal chemistry, , Sep-13, Volume: 55, Issue:17, 2012
Pyrazolopyridine Inhibitors of B-Raf(V600E). Part 1: The Development of Selective, Orally Bioavailable, and Efficacious Inhibitors.ACS medicinal chemistry letters, , May-12, Volume: 2, Issue:5, 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
Structure-Based and Knowledge-Informed Design of B-Raf Inhibitors Devoid of Deleterious PXR Binding.Journal of medicinal chemistry, , 01-27, Volume: 65, Issue:2, 2022
[no title available]European journal of medicinal chemistry, , Apr-05, Volume: 215, 2021
Modification of imidazothiazole derivatives gives promising activity in B-Raf kinase enzyme inhibition; synthesis, in vitro studies and molecular docking.Bioorganic & medicinal chemistry letters, , 10-15, Volume: 30, Issue:20, 2020
Design, synthesis, biological evaluation, QSAR analysis and molecular modelling of new thiazol-benzimidazoles as EGFR inhibitors.Bioorganic & medicinal chemistry, , 09-15, Volume: 28, Issue:18, 2020
Current Insights of BRAF Inhibitors in Cancer.Journal of medicinal chemistry, , 07-26, Volume: 61, Issue:14, 2018
Privileged Structures and Polypharmacology within and between Protein Families.ACS medicinal chemistry letters, , Dec-13, Volume: 9, Issue:12, 2018
Integrating docking scores and key interaction profiles to improve the accuracy of molecular docking: towards novel B-RafMedChemComm, , Sep-01, Volume: 8, Issue:9, 2017
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Purinylpyridinylamino-based DFG-in/αC-helix-out B-Raf inhibitors: Applying mutant versus wild-type B-Raf selectivity indices for compound profiling.Bioorganic & medicinal chemistry, , 05-15, Volume: 24, Issue:10, 2016
Photoinduced Conversion of Antimelanoma Agent Dabrafenib to a Novel Fluorescent BRAFACS medicinal chemistry letters, , Oct-13, Volume: 7, Issue:10, 2016
Discovery of 1-(3,3-dimethylbutyl)-3-(2-fluoro-4-methyl-5-(7-methyl-2-(methylamino)pyrido[2,3-d]pyrimidin-6-yl)phenyl)urea (LY3009120) as a pan-RAF inhibitor with minimal paradoxical activation and activity against BRAF or RAS mutant tumor cells.Journal of medicinal chemistry, , May-28, Volume: 58, Issue:10, 2015
Recent progress on MAP kinase pathway inhibitors.Bioorganic & medicinal chemistry letters, , Oct-01, Volume: 25, Issue:19, 2015
Discovery of Dabrafenib: A Selective Inhibitor of Raf Kinases with Antitumor Activity against B-Raf-Driven Tumors.ACS medicinal chemistry letters, , Mar-14, Volume: 4, Issue:3, 2013
N-(7-Cyano-6-(4-fluoro-3-(2-(3-(trifluoromethyl)phenyl)acetamido)phenoxy)benzo[d]thiazol-2-yl)cyclopropanecarboxamide (TAK632) Promotes Inhibition of BRAF through the Induction of Inhibited Dimers.Journal of medicinal chemistry, , 06-14, Volume: 61, Issue:11, 2018
Privileged Structures and Polypharmacology within and between Protein Families.ACS medicinal chemistry letters, , Dec-13, Volume: 9, Issue:12, 2018
Design and synthesis of N-(4-aminopyridin-2-yl)amides as B-Raf(V600E) inhibitors.Bioorganic & medicinal chemistry letters, , 06-15, Volume: 26, Issue:12, 2016
Discovery of a selective kinase inhibitor (TAK-632) targeting pan-RAF inhibition: design, synthesis, and biological evaluation of C-7-substituted 1,3-benzothiazole derivatives.Journal of medicinal chemistry, , Aug-22, Volume: 56, Issue:16, 2013
[no title available]European journal of medicinal chemistry, , Apr-05, Volume: 215, 2021
Design and synthesis of novel pyrrolo[2,3-b]pyridine derivatives targeting Bioorganic & medicinal chemistry, , 06-01, Volume: 28, Issue:11, 2020
Recent advances of RAF (rapidly accelerated fibrosarcoma) inhibitors as anti-cancer agents.European journal of medicinal chemistry, , Oct-05, Volume: 158, 2018
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
[no title available],
Targeting Rearranged during Transfection in Cancer: A Perspective on Small-Molecule Inhibitors and Their Clinical Development.Journal of medicinal chemistry, , 08-26, Volume: 64, Issue:16, 2021
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Identification of 1-(3-(6,7-dimethoxyquinazolin-4-yloxy)phenyl)-3-(5-(1,1,1-trifluoro-2-methylpropan-2-yl)isoxazol-3-yl)urea hydrochloride (CEP-32496), a highly potent and orally efficacious inhibitor of V-RAF murine sarcoma viral oncogene homologue B1 (BJournal of medicinal chemistry, , Feb-09, Volume: 55, Issue:3, 2012
Targeting KRAS Mutant Cancers via Combination Treatment: Discovery of a Pyridopyridazinone pan-RAF Kinase Inhibitor.ACS medicinal chemistry letters, , May-13, Volume: 12, Issue:5, 2021
Targeting KRAS Mutant Cancers via Combination Treatment: Discovery of a 5-Fluoro-4-(3Journal of medicinal chemistry, , 04-08, Volume: 64, Issue:7, 2021
Design and synthesis of novel pyrrolo[2,3-b]pyridine derivatives targeting Bioorganic & medicinal chemistry, , 06-01, Volume: 28, Issue:11, 2020
[no title available]European journal of medicinal chemistry, , Feb-01, Volume: 163, 2019
Recent advances of RAF (rapidly accelerated fibrosarcoma) inhibitors as anti-cancer agents.European journal of medicinal chemistry, , Oct-05, Volume: 158, 2018
Discovery of 1-(3,3-dimethylbutyl)-3-(2-fluoro-4-methyl-5-(7-methyl-2-(methylamino)pyrido[2,3-d]pyrimidin-6-yl)phenyl)urea (LY3009120) as a pan-RAF inhibitor with minimal paradoxical activation and activity against BRAF or RAS mutant tumor cells.Journal of medicinal chemistry, , May-28, Volume: 58, Issue:10, 2015
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
Current Insights of BRAF Inhibitors in Cancer.Journal of medicinal chemistry, , 07-26, Volume: 61, Issue:14, 2018
Synthesis, biological evaluation and 3D-QSAR studies of novel 4,5-dihydro-1H-pyrazole niacinamide derivatives as BRAF inhibitors.Bioorganic & medicinal chemistry, , Jun-15, Volume: 20, Issue:12, 2012
Conformation-specific effects of Raf kinase inhibitors.Journal of medicinal chemistry, , Sep-13, Volume: 55, Issue:17, 2012
Small molecule inhibitors of BRAF in clinical trials.Bioorganic & medicinal chemistry letters, , Jan-15, Volume: 22, Issue:2, 2012
Structure-based design of isoindoline-1,3-diones and 2,3-dihydrophthalazine-1,4-diones as novel B-Raf inhibitors.Bioorganic & medicinal chemistry letters, , Dec-01, Volume: 21, Issue:23, 2011
Identification of BRAF inhibitors through in silico screening.Journal of medicinal chemistry, , Oct-09, Volume: 51, Issue:19, 2008
The identification of potent, selective and CNS penetrant furan-based inhibitors of B-Raf kinase.Bioorganic & medicinal chemistry letters, , Aug-01, Volume: 18, Issue:15, 2008
The identification of potent and selective imidazole-based inhibitors of B-Raf kinase.Bioorganic & medicinal chemistry letters, , Jan-15, Volume: 16, Issue:2, 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
Enables
This protein enables 12 target(s):
| Target | Category | Definition |
|---|
| protein kinase activity | molecular function | Catalysis of the phosphorylation of an amino acid residue in a protein, usually according to the reaction: a protein + ATP = a phosphoprotein + ADP. [PMID:25399640] |
| protein 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] |
| MAP kinase kinase activity | molecular function | Catalysis of the concomitant phosphorylation of threonine (T) and tyrosine (Y) residues in a Thr-Glu-Tyr (TEY) thiolester sequence in a MAP kinase (MAPK) substrate. [ISBN:0198547684] |
| calcium ion binding | molecular function | Binding to a calcium ion (Ca2+). [GOC:ai] |
| 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] |
| mitogen-activated protein kinase kinase binding | molecular function | Binding to a mitogen-activated protein kinase kinase, a protein that can phosphorylate a MAP kinase. [GOC:mah] |
| identical protein binding | molecular function | Binding to an identical protein or proteins. [GOC:jl] |
| protein-containing complex binding | molecular function | Binding to a macromolecular complex. [GOC:jl] |
| scaffold protein binding | molecular function | Binding to a scaffold protein. Scaffold proteins are crucial regulators of many key signaling pathways. Although not strictly defined in function, they are known to interact and/or bind with multiple members of a signaling pathway, tethering them into complexes. [GOC:BHF, GOC:sjp, PMID:10433269, Wikipedia:Scaffold_protein] |
| protein serine kinase activity | molecular function | Catalysis of the reactions: ATP + protein serine = ADP + protein serine phosphate. [RHEA:17989] |
| MAP kinase kinase kinase activity | molecular function | Catalysis of the phosphorylation and activation of a MAP kinase kinase; each MAP kinase kinase can be phosphorylated by any of several MAP kinase kinase kinases. [PMID:9561267] |
Located In
This protein is located in 7 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] |
| 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] |
| neuron projection | cellular component | A prolongation or process extending from a nerve cell, e.g. an axon or dendrite. [GOC:jl, http://www.cogsci.princeton.edu/~wn/] |
| intracellular membrane-bounded organelle | cellular component | Organized structure of distinctive morphology and function, bounded by a single or double lipid bilayer membrane and occurring within the cell. Includes the nucleus, mitochondria, plastids, vacuoles, and vesicles. Excludes the plasma membrane. [GOC:go_curators] |
| cell body | cellular component | The portion of a cell bearing surface projections such as axons, dendrites, cilia, or flagella that includes the nucleus, but excludes all cell projections. [GOC:go_curators] |
| presynapse | cellular component | The part of a synapse that is part of the presynaptic cell. [GOC:dos] |
Active In
This protein is active in 3 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] |
| 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] |
| plasma membrane | cellular component | The membrane surrounding a cell that separates the cell from its external environment. It consists of a phospholipid bilayer and associated proteins. [ISBN:0716731363] |
Involved In
This protein is involved in 42 target(s):
| Target | Category | Definition |
|---|
| MAPK cascade | biological process | An intracellular protein kinase cascade containing at least a MAP kinase (MAPK). It starts with the activation of a MAP3K, and the consecutive activation of a MPK2K and a MAPK. The cascade can also contain an additional tier: the upstream MAP4K. The kinases in each tier phosphorylate and activate the kinase in the downstream tier to transmit a signal within a cell. [PMID:20811974, PMID:9561267] |
| myeloid progenitor cell differentiation | biological process | The process in which a precursor cell type acquires the specialized features of a myeloid progenitor cell. Myeloid progenitor cells include progenitor cells for any of the myeloid lineages. [GOC:add, PMID:16551264] |
| protein phosphorylation | biological process | The process of introducing a phosphate group on to a protein. [GOC:hb] |
| epidermal growth factor receptor signaling pathway | biological process | The series of molecular signals initiated by binding of a ligand to the tyrosine kinase receptor EGFR (ERBB1) on the surface of a cell. The pathway ends with regulation of a downstream cellular process, e.g. transcription. [GOC:ceb] |
| visual learning | biological process | Any process in an organism in which a change in behavior of an individual occurs in response to repeated exposure to a visual cue. [GOC:jid, ISBN:0582227089] |
| animal organ morphogenesis | biological process | Morphogenesis of an animal organ. An organ is defined as a tissue or set of tissues that work together to perform a specific function or functions. Morphogenesis is the process in which anatomical structures are generated and organized. Organs are commonly observed as visibly distinct structures, but may also exist as loosely associated clusters of cells that work together to perform a specific function or functions. [GOC:dgh, GOC:go_curators, ISBN:0471245208, ISBN:0721662544] |
| positive regulation of gene expression | biological process | Any process that increases the frequency, rate or extent of gene expression. Gene expression is the process in which a gene's coding sequence is converted into a mature gene product (protein or RNA). [GOC:txnOH-2018] |
| negative regulation of fibroblast migration | biological process | Any process that decreases the rate, frequency or extent of fibroblast cell migration. Fibroblast cell migration is accomplished by extension and retraction of a pseudopodium. [GOC:dph, GOC:tb] |
| positive regulation of glucose transmembrane transport | biological process | Any process that increases the frequency, rate or extent of glucose transport across a membrane. Glucose transport is the directed movement of the hexose monosaccharide glucose into, out of or within a cell, or between cells, by means of some agent such as a transporter or pore. [GOC:BHF, GOC:dph, GOC:tb] |
| synaptic vesicle exocytosis | biological process | Fusion of intracellular membrane-bounded vesicles with the pre-synaptic membrane of the neuronal cell resulting in release of neurotransmitter into the synaptic cleft. [GOC:jid, GOC:lmg] |
| thyroid gland development | biological process | The process whose specific outcome is the progression of the thyroid gland over time, from its formation to the mature structure. The thyroid gland is an endoderm-derived gland that produces thyroid hormone. [GOC:dgh] |
| T cell differentiation in thymus | biological process | The process in which a precursor cell type acquires the specialized features of a T cell via a differentiation pathway dependent upon transit through the thymus. [GOC:add, ISBN:0781735149] |
| positive regulation of peptidyl-serine phosphorylation | biological process | Any process that activates or increases the frequency, rate or extent of the phosphorylation of peptidyl-serine. [GOC:mah] |
| substrate adhesion-dependent cell spreading | biological process | The morphogenetic process that results in flattening of a cell as a consequence of its adhesion to a substrate. [GOC:mah, GOC:pf, PMID:17050732] |
| somatic stem cell population maintenance | biological process | Any process by which an organism retains a population of somatic stem cells, undifferentiated cells in the embryo or adult which can undergo unlimited division and give rise to cell types of the body other than those of the germ-line. [GOC:bf, ISBN:0582227089] |
| regulation of cell population proliferation | biological process | Any process that modulates the frequency, rate or extent of cell proliferation. [GOC:jl] |
| negative regulation of apoptotic process | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of cell death by apoptotic process. [GOC:jl, GOC:mtg_apoptosis] |
| stress fiber assembly | biological process | The aggregation, arrangement and bonding together of a set of components to form a stress fiber. A stress fiber is a contractile actin filament bundle that consists of short actin filaments with alternating polarity. [GOC:go_curators, GOC:mah, PMID:16651381] |
| CD4-positive, alpha-beta T cell differentiation | biological process | The process in which a relatively unspecialized T cell acquires specialized features of a mature CD4-positive, alpha-beta T cell. [CL:0000624, ISBN:0781735149] |
| CD4-positive or CD8-positive, alpha-beta T cell lineage commitment | biological process | The process in which an immature T cell commits to CD4-positive T cell lineage or the CD8-positive lineage of alpha-beta T cells. [ISBN:0781735149] |
| response to peptide hormone | 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 peptide hormone stimulus. A peptide hormone is any of a class of peptides that are secreted into the blood stream and have endocrine functions in living animals. [PMID:11027914, PMID:15134857, Wikipedia:Peptide_hormone] |
| negative regulation of neuron apoptotic process | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of cell death by apoptotic process in neurons. [GOC:go_curators, GOC:mtg_apoptosis] |
| regulation of T cell differentiation | biological process | Any process that modulates the frequency, rate or extent of T cell differentiation. [GOC:go_curators] |
| thymus development | biological process | The process whose specific outcome is the progression of the thymus over time, from its formation to the mature structure. The thymus is a symmetric bi-lobed organ involved primarily in the differentiation of immature to mature T cells, with unique vascular, nervous, epithelial, and lymphoid cell components. [GOC:add, ISBN:0781735149] |
| positive regulation of axon regeneration | biological process | Any process that activates, maintains or increases the rate of axon regeneration. [GOC:dgh, GOC:dph, GOC:jid, GOC:lm] |
| positive regulation of axonogenesis | biological process | Any process that activates or increases the frequency, rate or extent of axonogenesis. [GOC:ai] |
| T cell receptor signaling pathway | biological process | The series of molecular signals initiated by the cross-linking of an antigen receptor on a T cell. [GOC:add] |
| positive regulation of stress fiber assembly | biological process | Any process that activates or increases the frequency, rate or extent of the assembly of a stress fiber, a bundle of microfilaments and other proteins found in fibroblasts. [GOC:ai] |
| response to cAMP | 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 cAMP (cyclic AMP, adenosine 3',5'-cyclophosphate) stimulus. [GOC:ai] |
| long-term synaptic potentiation | biological process | A process that modulates synaptic plasticity such that synapses are changed resulting in the increase in the rate, or frequency of synaptic transmission at the synapse. [GOC:dgh, GOC:dph] |
| head morphogenesis | biological process | The process in which the anatomical structures of the head are generated and organized. The head is the anterior-most division of the body. [GOC:dph] |
| face development | biological process | The biological process whose specific outcome is the progression of a face from an initial condition to its mature state. The face is the ventral division of the head. [GOC:dph] |
| ERK1 and ERK2 cascade | biological process | A MAPK cascade containing at least the ERK1 or ERK2 MAP kinases. It starts with the activation of a MAP3K, and the consecutive activation of a MPK2K and of ERK1 or ERK2. The cascade can also contain an additional tier: the upstream MAP4K. The kinases in each tier phosphorylate and activate the kinase in the downstream tier. The ERK1/ERK2 cascade is activated by mitogens, growth factors, G protein-coupled receptors, and results in cellular responses such as cell proliferation, cell differentiation and development. [PMID:20811974, PMID:23125017, PMID:28903453] |
| 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] |
| cellular response to calcium ion | 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 calcium ion stimulus. [GOC:mah] |
| cellular response to xenobiotic stimulus | biological process | Any process that results in a change in state or activity of a cell (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a stimulus from a xenobiotic, a compound foreign to the organism exposed to it. It may be synthesized by another organism (like ampicilin) or it can be a synthetic chemical. [GOC:krc, GOC:mah] |
| endothelial cell apoptotic process | biological process | Any apoptotic process in an endothelial cell. An endothelial cell comprises the outermost layer or lining of anatomical structures and can be squamous or cuboidal. [CL:0000115, GOC:BHF, GOC:mah, GOC:mtg_apoptosis] |
| establishment of protein localization to membrane | biological process | The directed movement of a protein to a specific location in a membrane. [GOC:ascb_2009, GOC:dph, GOC:tb] |
| positive regulation of substrate adhesion-dependent cell spreading | biological process | Any process that activates or increases the frequency, rate or extent of substrate adhesion-dependent cell spreading. [GOC:TermGenie, GOC:yaf] |
| cellular response to nerve growth factor stimulus | biological process | A 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 nerve growth factor stimulus. [PMID:22399805, Wikipedia:Nerve_growth_factor] |
| negative regulation of synaptic vesicle exocytosis | biological process | Any process that stops, prevents or reduces the frequency, rate or extent of synaptic vesicle exocytosis. [GOC:obol] |
| negative regulation of endothelial cell apoptotic process | biological process | Any process that stops, prevents or reduces the frequency, rate or extent of endothelial cell apoptotic process. [GOC:BHF, GOC:mah, GOC:mtg_apoptosis] |