Proteins > Proto-oncogene tyrosine-protein kinase receptor Ret
Page last updated: 2024-08-07 18:28:59
Proto-oncogene tyrosine-protein kinase receptor Ret
A proto-oncogene tyrosine-protein kinase receptor Ret that is encoded in the genome of human. [PRO:DNx, UniProtKB:P07949]
Synonyms
EC 2.7.10.1;
Cadherin family member 12;
Proto-oncogene c-Ret
Research
Bioassay Publications (86)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 16 (18.60) | 29.6817 |
| 2010's | 58 (67.44) | 24.3611 |
| 2020's | 12 (13.95) | 2.80 |
Compounds (261)
Drugs with Inhibition Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| 4-(4'-hydroxyphenyl)-amino-6,7-dimethoxyquinazoline | Homo sapiens (human) | IC50 | 0.7200 | 1 | 1 |
| whi p180 | Homo sapiens (human) | IC50 | 0.1922 | 2 | 2 |
| staurosporine | Homo sapiens (human) | IC50 | 0.0021 | 12 | 12 |
| gefitinib | Homo sapiens (human) | IC50 | 1.7000 | 1 | 1 |
| birb 796 | Homo sapiens (human) | IC50 | 0.5150 | 2 | 2 |
| sorafenib | Homo sapiens (human) | GI50 | 0.1013 | 3 | 3 |
| sorafenib | Homo sapiens (human) | IC50 | 0.0260 | 8 | 8 |
| 3,3-dimethyl-5-oxo-5-[(3-phenyl-1H-pyrazol-5-yl)amino]pentanoic acid | Homo sapiens (human) | IC50 | 82.6000 | 1 | 1 |
| dasatinib | Homo sapiens (human) | IC50 | 1.2665 | 2 | 2 |
| zd 6474 | Homo sapiens (human) | IC50 | 1.0379 | 16 | 16 |
| quercetin | Homo sapiens (human) | IC50 | 78.1000 | 1 | 1 |
| ellagic acid | Homo sapiens (human) | IC50 | 40.0000 | 1 | 1 |
| su 9516 | Homo sapiens (human) | IC50 | 1.6000 | 1 | 1 |
| su 6656 | Homo sapiens (human) | IC50 | 0.7700 | 1 | 1 |
| semaxinib | Homo sapiens (human) | IC50 | 0.1700 | 1 | 1 |
| su 11248 | Homo sapiens (human) | IC50 | 0.3500 | 5 | 5 |
| su 4984 | Homo sapiens (human) | IC50 | 1.1000 | 1 | 1 |
| su 4312 | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
| su 5614 | Homo sapiens (human) | IC50 | 1.0000 | 1 | 1 |
| lenvatinib | Homo sapiens (human) | IC50 | 0.0162 | 4 | 4 |
| lenvatinib | Homo sapiens (human) | Ki | 0.0015 | 1 | 1 |
| 3-(4-dimethylamino-naphthalen-1-ylmethylene)-1,3-dihydro-indol-2-one | Homo sapiens (human) | IC50 | 45.0000 | 1 | 1 |
| bibw 2992 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| sotrastaurin | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| aee 788 | Homo sapiens (human) | IC50 | 0.7400 | 1 | 1 |
| l 783277 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| regorafenib | Homo sapiens (human) | IC50 | 0.0015 | 2 | 2 |
| 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) | IC50 | 0.0050 | 1 | 1 |
| danusertib | Homo sapiens (human) | IC50 | 0.0310 | 1 | 1 |
| nvp-aew541 | Homo sapiens (human) | IC50 | 3.3000 | 2 | 2 |
| abt 869 | Homo sapiens (human) | IC50 | 1.9000 | 1 | 1 |
| crizotinib | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| motesanib | Homo sapiens (human) | IC50 | 0.9326 | 3 | 13 |
| pha 767491 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| nvp-tae684 | Homo sapiens (human) | IC50 | 1.3850 | 1 | 1 |
| enmd 2076 | Homo sapiens (human) | IC50 | 0.0100 | 1 | 1 |
| pha 848125 | Homo sapiens (human) | IC50 | 1.9330 | 1 | 1 |
| fedratinib | Homo sapiens (human) | IC50 | 0.0325 | 2 | 2 |
| cudc 101 | Homo sapiens (human) | IC50 | 3.2000 | 1 | 1 |
| amg 458 | Homo sapiens (human) | IC50 | 25.0000 | 1 | 1 |
| tak 593 | Homo sapiens (human) | IC50 | 0.0180 | 1 | 1 |
| bms 777607 | Homo sapiens (human) | IC50 | 0.5940 | 1 | 1 |
| pci 32765 | Homo sapiens (human) | IC50 | 0.0262 | 3 | 3 |
| ponatinib | Homo sapiens (human) | IC50 | 0.0357 | 9 | 9 |
| AMG-208 | Homo sapiens (human) | IC50 | 0.0767 | 1 | 3 |
| PP121 | Homo sapiens (human) | IC50 | 0.0010 | 1 | 1 |
| al8697 | Homo sapiens (human) | IC50 | 2.0000 | 1 | 1 |
| cabozantinib | Homo sapiens (human) | GI50 | 0.3166 | 10 | 10 |
| cabozantinib | Homo sapiens (human) | IC50 | 0.1699 | 31 | 31 |
| entrectinib | Homo sapiens (human) | IC50 | 0.3930 | 1 | 1 |
| mk 2461 | Homo sapiens (human) | IC50 | 0.6400 | 1 | 1 |
| pha 793887 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| abt-348 | Homo sapiens (human) | IC50 | 0.0070 | 1 | 1 |
| nms p937 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| alectinib | Homo sapiens (human) | IC50 | 0.0197 | 8 | 8 |
| nms-p118 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| bix 02565 | Homo sapiens (human) | IC50 | 0.1610 | 2 | 1 |
| 7-methyl-5-(1-((3-(trifluoromethyl)phenyl)acetyl)-2,3-dihydro-1h-indol-5-yl)-7h-pyrrolo(2,3-d)pyrimidin-4-amine | Homo sapiens (human) | IC50 | 1.2150 | 1 | 1 |
| on123300 | Homo sapiens (human) | IC50 | 0.0092 | 1 | 1 |
| cep-32496 | Homo sapiens (human) | IC50 | 0.0543 | 10 | 10 |
| ceritinib | Homo sapiens (human) | IC50 | 1.3520 | 2 | 2 |
| pf-543 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| at 9283 | Homo sapiens (human) | IC50 | 0.0010 | 1 | 1 |
| pf-477736 | Homo sapiens (human) | IC50 | 0.0390 | 1 | 0 |
| nms-e973 | Homo sapiens (human) | IC50 | 0.0100 | 1 | 1 |
Drugs with Activation Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| fasudil | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| 4-(4'-hydroxyphenyl)-amino-6,7-dimethoxyquinazoline | Homo sapiens (human) | Kd | 21.8870 | 1 | 1 |
| sb 202190 | Homo sapiens (human) | Kd | 10.0000 | 2 | 2 |
| imatinib | Homo sapiens (human) | Kd | 12.8571 | 7 | 7 |
| triciribine phosphate | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| staurosporine | Homo sapiens (human) | Kd | 0.0188 | 6 | 6 |
| picropodophyllin | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| gefitinib | Homo sapiens (human) | Kd | 12.8571 | 7 | 7 |
| lestaurtinib | Homo sapiens (human) | Kd | 0.0329 | 9 | 9 |
| perifosine | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| vatalanib | Homo sapiens (human) | Kd | 12.1714 | 7 | 7 |
| ruboxistaurin | Homo sapiens (human) | Kd | 12.8571 | 7 | 7 |
| canertinib | Homo sapiens (human) | Kd | 4.6521 | 7 | 7 |
| birb 796 | Homo sapiens (human) | Kd | 3.5800 | 6 | 6 |
| cyc 202 | Homo sapiens (human) | Kd | 16.6667 | 3 | 3 |
| sb 203580 | Homo sapiens (human) | Kd | 10.0000 | 6 | 6 |
| enzastaurin | Homo sapiens (human) | Kd | 14.0000 | 5 | 5 |
| erlotinib | Homo sapiens (human) | Kd | 3.5156 | 7 | 7 |
| lapatinib | Homo sapiens (human) | Kd | 12.8571 | 7 | 7 |
| sorafenib | Homo sapiens (human) | Kd | 0.0302 | 12 | 12 |
| pd 173955 | Homo sapiens (human) | Kd | 4.0310 | 4 | 4 |
| s 1033 | Homo sapiens (human) | Kd | 10.3940 | 5 | 5 |
| xl147 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| bms 387032 | Homo sapiens (human) | Kd | 12.8571 | 7 | 7 |
| sf 2370 | Homo sapiens (human) | Kd | 0.6690 | 1 | 1 |
| tandutinib | Homo sapiens (human) | Kd | 11.8182 | 11 | 11 |
| vx-745 | Homo sapiens (human) | Kd | 10.0000 | 6 | 6 |
| dasatinib | Homo sapiens (human) | Kd | 2.3421 | 7 | 7 |
| ha 1100 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| 7-epi-hydroxystaurosporine | Homo sapiens (human) | Kd | 0.5210 | 1 | 1 |
| zd 6474 | Homo sapiens (human) | Kd | 2.9449 | 7 | 7 |
| 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 | 12.8571 | 7 | 7 |
| bosutinib | Homo sapiens (human) | Kd | 10.5600 | 5 | 5 |
| orantinib | Homo sapiens (human) | Kd | 0.3160 | 1 | 1 |
| su 11248 | Homo sapiens (human) | Kd | 0.0142 | 11 | 11 |
| palbociclib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| jnj-7706621 | Homo sapiens (human) | Kd | 2.6000 | 2 | 2 |
| vx680 | Homo sapiens (human) | Kd | 0.0731 | 8 | 8 |
| cyc 116 | Homo sapiens (human) | Kd | 2.1780 | 1 | 1 |
| everolimus | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| ekb 569 | Homo sapiens (human) | Kd | 20.0000 | 3 | 4 |
| axitinib | Homo sapiens (human) | Kd | 0.6450 | 5 | 5 |
| temsirolimus | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| pd 184352 | Homo sapiens (human) | Kd | 10.0000 | 4 | 4 |
| on 01910 | Homo sapiens (human) | Kd | 30.0000 | 1 | 2 |
| 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 | 0.3410 | 1 | 1 |
| bms345541 | Homo sapiens (human) | Kd | 10.0000 | 4 | 4 |
| lenvatinib | Homo sapiens (human) | Kd | 0.0090 | 1 | 1 |
| pd 0325901 | Homo sapiens (human) | Kd | 30.0000 | 1 | 2 |
| midostaurin | Homo sapiens (human) | Kd | 1.9415 | 11 | 11 |
| 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 | 0.3880 | 1 | 1 |
| ki 20227 | Homo sapiens (human) | Kd | 5.8550 | 4 | 4 |
| 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 | 10.0000 | 6 | 6 |
| hmn-214 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| tivozanib | Homo sapiens (human) | Kd | 0.0120 | 1 | 1 |
| hki 272 | Homo sapiens (human) | Kd | 16.6667 | 5 | 6 |
| tofacitinib | Homo sapiens (human) | Kd | 11.9000 | 7 | 7 |
| n-(6-chloro-7-methoxy-9h-beta-carbolin-8-yl)-2-methylnicotinamide | Homo sapiens (human) | Kd | 10.0000 | 4 | 4 |
| cediranib | Homo sapiens (human) | Kd | 2.7681 | 5 | 5 |
| masitinib | Homo sapiens (human) | Kd | 14.0000 | 5 | 5 |
| ly-2157299 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| pazopanib | Homo sapiens (human) | Kd | 1.3789 | 7 | 7 |
| azd 6244 | Homo sapiens (human) | Kd | 14.0000 | 5 | 5 |
| su 14813 | Homo sapiens (human) | Kd | 0.0267 | 7 | 7 |
| bibw 2992 | Homo sapiens (human) | Kd | 14.0000 | 5 | 5 |
| 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 | 0.1780 | 1 | 1 |
| vx 702 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| crenolanib | Homo sapiens (human) | Kd | 0.8100 | 1 | 1 |
| tg100-115 | Homo sapiens (human) | Kd | 14.0000 | 5 | 5 |
| 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 | 0.0640 | 1 | 1 |
| volasertib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| pha 665752 | Homo sapiens (human) | Kd | 0.5600 | 4 | 4 |
| azd 7762 | Homo sapiens (human) | Kd | 0.0230 | 1 | 1 |
| regorafenib | Homo sapiens (human) | Kd | 0.1260 | 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) | EC50 | 0.0580 | 2 | 2 |
| 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 | 0.0105 | 5 | 5 |
| brivanib | Homo sapiens (human) | Kd | 4.7220 | 5 | 5 |
| 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 | 14.0000 | 5 | 5 |
| bms-690514 | Homo sapiens (human) | Kd | 0.1295 | 2 | 2 |
| bi 2536 | Homo sapiens (human) | Kd | 14.0000 | 5 | 5 |
| inno-406 | Homo sapiens (human) | Kd | 2.4160 | 1 | 1 |
| nvp-ast487 | Homo sapiens (human) | Kd | 0.0084 | 6 | 6 |
| kw 2449 | Homo sapiens (human) | Kd | 0.1344 | 5 | 5 |
| danusertib | Homo sapiens (human) | Kd | 0.0060 | 1 | 1 |
| abt 869 | Homo sapiens (human) | Kd | 0.4146 | 7 | 7 |
| azd 8931 | Homo sapiens (human) | Kd | 0.3900 | 1 | 1 |
| arq 197 | Homo sapiens (human) | Kd | 30.0000 | 1 | 2 |
| azd 1152 | Homo sapiens (human) | Kd | 0.1445 | 2 | 2 |
| 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 | 6 | 6 |
| tak 285 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| idelalisib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| crizotinib | Homo sapiens (human) | Kd | 10.6800 | 5 | 5 |
| osi 906 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| chir-265 | Homo sapiens (human) | Kd | 4.4076 | 7 | 7 |
| motesanib | Homo sapiens (human) | Kd | 2.8784 | 7 | 7 |
| fostamatinib | Homo sapiens (human) | Kd | 1.1470 | 1 | 1 |
| trametinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| mln8054 | Homo sapiens (human) | Kd | 12.8571 | 7 | 7 |
| pf-562,271 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| GDC-0879 | Homo sapiens (human) | Kd | 10.0000 | 4 | 4 |
| jnj-26483327 | Homo sapiens (human) | Kd | 2.4160 | 1 | 1 |
| ly2603618 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| tg100801 | Homo sapiens (human) | Kd | 1.0280 | 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 | 14.0000 | 5 | 5 |
| azd 1152-hqpa | Homo sapiens (human) | Kd | 0.2940 | 7 | 7 |
| nvp-tae684 | Homo sapiens (human) | EC50 | 1.0000 | 1 | 1 |
| nvp-tae684 | Homo sapiens (human) | Kd | 0.1375 | 4 | 4 |
| enmd 2076 | Homo sapiens (human) | Kd | 0.4870 | 1 | 1 |
| e 7050 | Homo sapiens (human) | Kd | 0.1750 | 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 | 0.1110 | 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 | 0.2380 | 1 | 1 |
| azd8330 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| pha 848125 | Homo sapiens (human) | Kd | 1.3220 | 1 | 1 |
| ro5126766 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| fedratinib | Homo sapiens (human) | Kd | 0.4140 | 5 | 5 |
| gsk690693 | Homo sapiens (human) | Kd | 12.2600 | 5 | 5 |
| 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 | 21.8580 | 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 | 14.0000 | 5 | 5 |
| icotinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| ph 797804 | Homo sapiens (human) | Kd | 30.0000 | 1 | 2 |
| kx-01 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| plx 4720 | Homo sapiens (human) | Kd | 10.0000 | 4 | 4 |
| mk 5108 | Homo sapiens (human) | Kd | 0.3880 | 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 | 1.2000 | 1 | 1 |
| tak 593 | Homo sapiens (human) | Kd | 0.0100 | 1 | 1 |
| mln 8237 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| sgx 523 | Homo sapiens (human) | Kd | 14.0000 | 5 | 5 |
| bms 754807 | Homo sapiens (human) | Kd | 0.6750 | 1 | 1 |
| bms 777607 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| sgi 1776 | Homo sapiens (human) | Kd | 3.2170 | 1 | 1 |
| pci 32765 | Homo sapiens (human) | Kd | 18.0500 | 1 | 1 |
| ponatinib | Homo sapiens (human) | Kd | 0.0250 | 1 | 1 |
| amg 900 | Homo sapiens (human) | Kd | 1.1390 | 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 | 0.0204 | 13 | 13 |
| 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 | 0.0050 | 1 | 1 |
| pf-04691502 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| n-(cyanomethyl)-4-(2-((4-(4-morpholinyl)phenyl)amino)-4-pyrimidinyl)benzamide | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| dcc-2036 | Homo sapiens (human) | Kd | 1.2150 | 1 | 1 |
| cabozantinib | Homo sapiens (human) | Kd | 0.0860 | 1 | 1 |
| defactinib | Homo sapiens (human) | Kd | 27.5420 | 1 | 1 |
| ly2584702 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| incb-018424 | Homo sapiens (human) | Kd | 0.6756 | 5 | 5 |
| poziotinib | Homo sapiens (human) | Kd | 1.1850 | 1 | 1 |
| asp3026 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| entrectinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| pexidartinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| TAK-580 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| gsk 2126458 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| emd1214063 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| gsk 1838705a | Homo sapiens (human) | Kd | 10.0000 | 4 | 4 |
| pf 3758309 | Homo sapiens (human) | Kd | 0.7280 | 1 | 1 |
| gdc 0980 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| azd2014 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| (5-(2,4-bis((3s)-3-methylmorpholin-4-yl)pyrido(2,3-d)pyrimidin-7-yl)-2-methoxyphenyl)methanol | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| plx4032 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| gsk 1363089 | Homo sapiens (human) | Kd | 0.0024 | 5 | 5 |
| 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 | 0.9730 | 1 | 1 |
| dabrafenib | Homo sapiens (human) | Kd | 30.0000 | 1 | 2 |
| 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 | 1.3820 | 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 | 2.5490 | 1 | 1 |
| afuresertib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| gsk 1070916 | Homo sapiens (human) | Kd | 0.0670 | 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 | 0.0500 | 1 | 1 |
| alectinib | Homo sapiens (human) | Kd | 0.3690 | 1 | 1 |
| glpg0634 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| encorafenib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| bms-911543 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| gsk2141795 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| azd8186 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| byl719 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| cep-32496 | Homo sapiens (human) | Kd | 0.0048 | 3 | 3 |
| rociletinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| ceritinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| azd1208 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| vx-509 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| gs-9973 | Homo sapiens (human) | EC50 | 1.0000 | 1 | 1 |
| debio 1347 | Homo sapiens (human) | Kd | 0.7830 | 1 | 1 |
| volitinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| osimertinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| at 9283 | Homo sapiens (human) | Kd | 0.0110 | 1 | 1 |
| otssp167 | Homo sapiens (human) | Kd | 0.0280 | 1 | 1 |
| chir 258 | Homo sapiens (human) | Kd | 0.0446 | 7 | 7 |
| osi 027 | Homo sapiens (human) | Kd | 0.0570 | 1 | 1 |
| nintedanib | Homo sapiens (human) | Kd | 0.0167 | 5 | 5 |
| bay 80-6946 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| pp242 | Homo sapiens (human) | Kd | 0.1747 | 4 | 4 |
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
The discovery of 2-substituted phenol quinazolines as potent RET kinase inhibitors with improved KDR selectivity.European journal of medicinal chemistry, , Apr-13, Volume: 112, 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
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
Discovery of 4-methyl-N-(4-((4-methylpiperazin- 1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((6-(pyridin-3-yl)-1H-pyrazolo[3,4-d]pyrimidin-4-yl)-oxy)benzamide as a potent inhibitor of RET and its gatekeeper mutant.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
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
Synthesis and evaluation of a series of pyridine and pyrimidine derivatives as type II c-Met inhibitors.Bioorganic & medicinal chemistry, , 06-15, Volume: 25, Issue:12, 2017
Novel LCK/FMS inhibitors based on phenoxypyrimidine scaffold as potential treatment for inflammatory disorders.European journal of medicinal chemistry, , Dec-01, Volume: 141, 2017
Synthesis 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
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 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
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
Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases.Nature chemical biology, , Volume: 4, Issue:11, 2008
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
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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
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
Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD).Bioorganic & medicinal chemistry letters, , Dec-01, Volume: 21, Issue:23, 2011
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
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
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
[no title available]European journal of medicinal chemistry, , Apr-15, Volume: 234, 2022
Discovery of N-Trisubstituted Pyrimidine Derivatives as Type I RET and RET Gatekeeper Mutant Inhibitors with a Novel Kinase Binding Pose.Journal of medicinal chemistry, , 01-27, Volume: 65, Issue:2, 2022
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
A multi-scale systems pharmacology approach uncovers the anti-cancer molecular mechanism of Ixabepilone.European journal of medicinal chemistry, , Aug-01, Volume: 199, 2020
Structural optimization and structure-activity relationship studies of N-phenyl-7,8-dihydro-6H-pyrimido[5,4-b][1,4]oxazin-4-amine derivatives as a new class of inhibitors of RET and its drug resistance mutants.European journal of medicinal chemistry, , Jan-01, Volume: 143, 2018
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Progress in Discovery of KIF5B-RET Kinase Inhibitors for the Treatment of Non-Small-Cell Lung Cancer.Journal of medicinal chemistry, , May-14, Volume: 58, Issue:9, 2015
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
Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases.Nature chemical biology, , Volume: 4, Issue:11, 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
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
Rapid Discovery and Structure-Activity Relationships of Pyrazolopyrimidines That Potently Suppress Breast Cancer Cell Growth via SRC Kinase Inhibition with Exceptional Selectivity over ABL Kinase.Journal of medicinal chemistry, , 05-26, Volume: 59, Issue:10, 2016
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
Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases.Nature chemical biology, , Volume: 4, Issue:11, 2008
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
Discovery and Optimization of wt-RET/KDR-Selective Inhibitors of RETACS medicinal chemistry letters, , Apr-09, Volume: 11, Issue:4, 2020
Structural optimization and structure-activity relationship studies of N-phenyl-7,8-dihydro-6H-pyrimido[5,4-b][1,4]oxazin-4-amine derivatives as a new class of inhibitors of RET and its drug resistance mutants.European journal of medicinal chemistry, , Jan-01, Volume: 143, 2018
Challenging clinically unresponsive medullary thyroid cancer: Discovery and pharmacological activity of novel RET inhibitors.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
The discovery of 2-substituted phenol quinazolines as potent RET kinase inhibitors with improved KDR selectivity.European journal of medicinal chemistry, , Apr-13, Volume: 112, 2016
Progress in Discovery of KIF5B-RET Kinase Inhibitors for the Treatment of Non-Small-Cell Lung Cancer.Journal of medicinal chemistry, , May-14, Volume: 58, Issue:9, 2015
Identification of two novel RET kinase inhibitors through MCR-based drug discovery: design, synthesis and evaluation.European journal of medicinal chemistry, , Oct-30, Volume: 86, 2014
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
Inhibitors of the RET tyrosine kinase based on a 2-(alkylsulfanyl)-4-(3-thienyl)nicotinonitrile scaffold.European journal of medicinal chemistry, , Volume: 45, Issue:7, 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
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
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
Progress in Discovery of KIF5B-RET Kinase Inhibitors for the Treatment of Non-Small-Cell Lung Cancer.Journal of medicinal chemistry, , May-14, Volume: 58, Issue:9, 2015
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
Synthesis, structure-activity relationship and crystallographic studies of 3-substituted indolin-2-one RET inhibitors.Bioorganic & medicinal chemistry, , Feb-15, Volume: 18, Issue:4, 2010
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
Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases.Nature chemical biology, , Volume: 4, Issue:11, 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
Discovery and development of aurora kinase inhibitors as anticancer agents.Journal of medicinal chemistry, , May-14, Volume: 52, Issue:9, 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
Design, synthesis and biological evaluation of novel 2,4-diaryl pyrimidine derivatives as selective EGFREuropean journal of medicinal chemistry, , Feb-15, Volume: 212, 2021
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Progress in Discovery of KIF5B-RET Kinase Inhibitors for the Treatment of Non-Small-Cell Lung Cancer.Journal of medicinal chemistry, , May-14, Volume: 58, Issue:9, 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
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 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
Discovery of N-(3-bromo-1H-indol-5-yl)-quinazolin-4-amine as an effective molecular skeleton to develop reversible/irreversible pan-HER inhibitors.European journal of medicinal chemistry, , Apr-05, Volume: 233, 2022
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Discovery of 3-(1H-indol-3-yl)-4-[2-(4-methylpiperazin-1-yl)quinazolin-4-yl]pyrrole-2,5-dione (AEB071), a potent and selective inhibitor of protein kinase C isotypes.Journal of medicinal chemistry, , Oct-22, Volume: 52, Issue:20, 2009
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Pharmacophore modeling and virtual screening to identify potential RET kinase inhibitors.Bioorganic & medicinal chemistry letters, , Aug-01, Volume: 21, Issue:15, 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
[no title available]European journal of medicinal chemistry, , Apr-15, Volume: 234, 2022
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
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Discovery of GS-9973, a selective and orally efficacious inhibitor of spleen tyrosine kinase.Journal of medicinal chemistry, , May-08, Volume: 57, Issue:9, 2014
Discovery and development of spleen tyrosine kinase (SYK) inhibitors.Journal of medicinal chemistry, , Apr-26, Volume: 55, Issue:8, 2012
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 of a Cyclin G Associated Kinase (GAK)/Epidermal Growth Factor Receptor (EGFR) Inhibitor Set to Interrogate the Relationship of EGFR and GAK in Chordoma.Journal of medicinal chemistry, , 05-09, Volume: 62, Issue:9, 2019
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazoles: identification of a potent Aurora kinase inhibitor with a favorable antitumor kinase inhibition profile.Journal of medicinal chemistry, , Nov-30, Volume: 49, Issue:24, 2006
Identification of a 5-[3-phenyl-(2-cyclic-ether)-methylether]-4-aminopyrrolo[2,3-d]pyrimidine series of IGF-1R inhibitors.Bioorganic & medicinal chemistry letters, , Apr-15, Volume: 26, Issue:8, 2016
Optimisation of a 5-[3-phenyl-(2-cyclic-ether)-methyl-ether]-4-aminopyrrolopyrimidine series of IGF-1R inhibitors.Bioorganic & medicinal chemistry letters, , Apr-15, Volume: 26, Issue:8, 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
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
Discovery of N-(4-(3-amino-1H-indazol-4-yl)phenyl)-N'-(2-fluoro-5-methylphenyl)urea (ABT-869), a 3-aminoindazole-based orally active multitargeted receptor tyrosine kinase inhibitor.Journal of medicinal chemistry, , Apr-05, Volume: 50, Issue:7, 2007
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Discovery and development of aurora kinase inhibitors as anticancer agents.Journal of medicinal chemistry, , May-14, Volume: 52, Issue:9, 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
Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling.Proceedings of the National Academy of Sciences of the United States of America, , Dec-11, Volume: 104, Issue:50, 2007
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
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
Progress in Discovery of KIF5B-RET Kinase Inhibitors for the Treatment of Non-Small-Cell Lung Cancer.Journal of medicinal chemistry, , May-14, Volume: 58, 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
AMG 706, an oral, multikinase inhibitor that selectively targets vascular endothelial growth factor, platelet-derived growth factor, and kit receptors, potently inhibits angiogenesis and induces regression in tumor xenografts.Cancer research, , Sep-01, Volume: 66, Issue:17, 2006
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
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
Identification of NVP-TAE684, a potent, selective, and efficacious inhibitor of NPM-ALK.Proceedings of the National Academy of Sciences of the United States of America, , Jan-02, Volume: 104, Issue:1, 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
Discovery and development of extreme selective inhibitors of the ITD and D835Y mutant FLT3 kinases.European journal of medicinal chemistry, , Dec-15, Volume: 184, 2019
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
Identification of N,1,4,4-tetramethyl-8-{[4-(4-methylpiperazin-1-yl)phenyl]amino}-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide (PHA-848125), a potent, orally available cyclin dependent kinase inhibitor.Journal of medicinal chemistry, , Aug-27, Volume: 52, Issue:16, 2009
Small-Molecule Kinase Inhibitors for the Treatment of Nononcologic Diseases.Journal of medicinal chemistry, , 02-11, Volume: 64, Issue:3, 2021
Non-kinase targets of protein kinase inhibitors.Nature reviews. Drug discovery, , Volume: 16, Issue:6, 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
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Discovery of 7-(4-(3-ethynylphenylamino)-7-methoxyquinazolin-6-yloxy)-N-hydroxyheptanamide (CUDc-101) as a potent multi-acting HDAC, EGFR, and HER2 inhibitor for the treatment of cancer.Journal of medicinal chemistry, , Mar-11, Volume: 53, Issue:5, 2010
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Discovery of N-[5-({2-[(cyclopropylcarbonyl)amino]imidazo[1,2-b]pyridazin-6-yl}oxy)-2-methylphenyl]-1,3-dimethyl-1H-pyrazole-5-carboxamide (TAK-593), a highly potent VEGFR2 kinase inhibitor.Bioorganic & medicinal chemistry, , Apr-15, Volume: 21, Issue:8, 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
Synthesis and evaluation of a series of pyridine and pyrimidine derivatives as type II c-Met inhibitors.Bioorganic & medicinal chemistry, , 06-15, Volume: 25, Issue:12, 2017
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
[no title available]European journal of medicinal chemistry, , Feb-10, Volume: 145, 2018
Discovery of 4,7-Diamino-5-(4-phenoxyphenyl)-6-methylene-pyrimido[5,4- b]pyrrolizines as Novel Bruton's Tyrosine Kinase Inhibitors.Journal of medicinal chemistry, , 05-24, Volume: 61, Issue:10, 2018
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Bruton's tyrosine kinase inhibitors: approaches to potent and selective inhibition, preclinical and clinical evaluation for inflammatory diseases and B cell malignancies.Journal of medicinal chemistry, , May-24, Volume: 55, Issue:10, 2012
[no title available]European journal of medicinal chemistry, , Apr-15, Volume: 234, 2022
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
Discovery of novel Ponatinib analogues for reducing KDR activity as potent FGFRs inhibitors.European journal of medicinal chemistry, , Jan-27, Volume: 126, 2017
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Discovery of 4-chloro-3-(5-(pyridin-3-yl)-1,2,4-oxadiazole-3-yl)benzamides as novel RET kinase inhibitors.Bioorganic & medicinal chemistry letters, , 12-01, Volume: 26, Issue:23, 2016
Progress in Discovery of KIF5B-RET Kinase Inhibitors for the Treatment of Non-Small-Cell Lung Cancer.Journal of medicinal chemistry, , May-14, Volume: 58, Issue:9, 2015
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Discovery of imidazopyridine derivatives as novel c-Met kinase inhibitors: Synthesis, SAR study, and biological activity.Bioorganic chemistry, , Volume: 70, 2017
Identification and Development of 1,4-Diaryl-1,2,3-triazolo-Based Ureas as Novel FLT3 Inhibitors.ACS medicinal chemistry letters, , Aug-13, Volume: 11, Issue:8, 2020
Discovery of 1-(4-(4-Amino-3-(4-(2-morpholinoethoxy)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)phenyl)-3-(5-(tert-butyl)isoxazol-3-yl)urea (CHMFL-FLT3-213) as a Highly Potent Type II FLT3 Kinase Inhibitor Capable of Overcoming a Variety of FLT3 Kinase MutanJournal of medicinal chemistry, , 10-26, Volume: 60, Issue:20, 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
Toward the development of innovative bifunctional agents to induce differentiation and to promote apoptosis in leukemia: clinical candidates and perspectives.Journal of medicinal chemistry, , Oct-14, Volume: 53, Issue:19, 2010
Identification of N-(5-tert-butyl-isoxazol-3-yl)-N'-{4-[7-(2-morpholin-4-yl-ethoxy)imidazo[2,1-b][1,3]benzothiazol-2-yl]phenyl}urea dihydrochloride (AC220), a uniquely potent, selective, and efficacious FMS-like tyrosine kinase-3 (FLT3) inhibitor.Journal of medicinal chemistry, , Dec-10, Volume: 52, Issue:23, 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
[no title available]European journal of medicinal chemistry, , Apr-15, Volume: 234, 2022
Design, synthesis and biological evaluation of novel 2,4-diaryl pyrimidine derivatives as selective EGFREuropean journal of medicinal chemistry, , Feb-15, Volume: 212, 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
Discovery and Optimization of wt-RET/KDR-Selective Inhibitors of RETACS medicinal chemistry letters, , Apr-09, Volume: 11, Issue:4, 2020
Discovery of 4-methyl-N-(4-((4-methylpiperazin- 1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((6-(pyridin-3-yl)-1H-pyrazolo[3,4-d]pyrimidin-4-yl)-oxy)benzamide as a potent inhibitor of RET and its gatekeeper mutant.European journal of medicinal chemistry, , Dec-01, Volume: 207, 2020
Structural optimization and structure-activity relationship studies of N-phenyl-7,8-dihydro-6H-pyrimido[5,4-b][1,4]oxazin-4-amine derivatives as a new class of inhibitors of RET and its drug resistance mutants.European journal of medicinal chemistry, , Jan-01, Volume: 143, 2018
Identification of novel NEuropean journal of medicinal chemistry, , Feb-25, Volume: 146, 2018
Identification of a novel 5-amino-3-(5-cyclopropylisoxazol-3-yl)-1-isopropyl-1H-pyrazole-4-carboxamide as a specific RET kinase inhibitor.European journal of medicinal chemistry, , Jan-05, Volume: 125, 2017
Structure-based design, synthesis, and evaluation of 4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine derivatives as novel c-Met inhibitors.European journal of medicinal chemistry, , Sep-29, Volume: 138, 2017
The discovery of novel benzothiazinones as highly selective non-ATP competitive glycogen synthase kinase 3β inhibitors for the treatment of ovarian cancer.European journal of medicinal chemistry, , Jul-28, Volume: 135, 2017
Synthesis and evaluation of a series of pyridine and pyrimidine derivatives as type II c-Met inhibitors.Bioorganic & medicinal chemistry, , 06-15, Volume: 25, Issue:12, 2017
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
The "Cyclopropyl Fragment" is a Versatile Player that Frequently Appears in Preclinical/Clinical Drug Molecules.Journal of medicinal chemistry, , 10-13, Volume: 59, Issue:19, 2016
The discovery of 2-substituted phenol quinazolines as potent RET kinase inhibitors with improved KDR selectivity.European journal of medicinal chemistry, , Apr-13, Volume: 112, 2016
An orally available tyrosine kinase ALK and RET dual inhibitor bearing the tetracyclic benzo[b]carbazolone core.European journal of medicinal chemistry, , Aug-08, Volume: 118, 2016
Recent advances in the development of dual VEGFR and c-Met small molecule inhibitors as anticancer drugs.European journal of medicinal chemistry, , Jan-27, Volume: 108, 2016
A Pyrazolo[3,4-d]pyrimidin-4-amine Derivative Containing an Isoxazole Moiety Is a Selective and Potent Inhibitor of RET Gatekeeper Mutants.Journal of medicinal chemistry, , Jan-14, Volume: 59, Issue:1, 2016
Progress in Discovery of KIF5B-RET Kinase Inhibitors for the Treatment of Non-Small-Cell Lung Cancer.Journal of medicinal chemistry, , May-14, Volume: 58, Issue:9, 2015
Design, synthesis and evaluation of highly selective pyridone-based class II MET 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
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Discovery of Entrectinib: A New 3-Aminoindazole As a Potent Anaplastic Lymphoma Kinase (ALK), c-ros Oncogene 1 Kinase (ROS1), and Pan-Tropomyosin Receptor Kinases (Pan-TRKs) inhibitor.Journal of medicinal chemistry, , Apr-14, Volume: 59, Issue:7, 2016
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Discovery of a 5H-benzo[4,5]cyclohepta[1,2-b]pyridin-5-one (MK-2461) inhibitor of c-Met kinase for the treatment of cancer.Journal of medicinal chemistry, , Jun-23, Volume: 54, Issue:12, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Optimization of 6,6-dimethyl pyrrolo[3,4-c]pyrazoles: Identification of PHA-793887, a potent CDK inhibitor suitable for intravenous dosing.Bioorganic & medicinal chemistry, , Mar-01, Volume: 18, Issue:5, 2010
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
An orally available tyrosine kinase ALK and RET dual inhibitor bearing the tetracyclic benzo[b]carbazolone core.European journal of medicinal chemistry, , Aug-08, Volume: 118, 2016
[no title available]European journal of medicinal chemistry, , Apr-15, Volume: 234, 2022
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
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Synthesis, structure-activity relationships, and in vivo efficacy of the novel potent and selective anaplastic lymphoma kinase (ALK) inhibitor 5-chloro-N2-(2-isopropoxy-5-methyl-4-(piperidin-4-yl)phenyl)-N4-(2-(isopropylsulfonyl)phenyl)pyrimidine-2,4-diamJournal of medicinal chemistry, , Jul-25, Volume: 56, Issue:14, 2013
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Fragment-based discovery of the pyrazol-4-yl urea (AT9283), a multitargeted kinase inhibitor with potent aurora kinase activity.Journal of medicinal chemistry, , Jan-22, Volume: 52, Issue:2, 2009
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
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 6 target(s):
| Target | Category | Definition |
|---|
| protein tyrosine kinase activity | molecular function | Catalysis of the reaction: ATP + a protein tyrosine = ADP + protein tyrosine phosphate. [RHEA:10596] |
| transmembrane receptor protein tyrosine kinase activity | molecular function | Combining with a signal and transmitting the signal from one side of the membrane to the other to initiate a change in cell activity by catalysis of the reaction: ATP + a protein-L-tyrosine = ADP + a protein-L-tyrosine phosphate. [EC:2.7.10.1, GOC:mah] |
| 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] |
| signaling receptor activity | molecular function | Receiving a signal and transmitting it in the cell to initiate a change in cell activity. A signal is a physical entity or change in state that is used to transfer information in order to trigger a response. [GOC:bf, GOC:signaling] |
Located In
This protein is located in 5 target(s):
| Target | Category | Definition |
|---|
| early endosome | cellular component | A membrane-bounded organelle that receives incoming material from primary endocytic vesicles that have been generated by clathrin-dependent and clathrin-independent endocytosis; vesicles fuse with the early endosome to deliver cargo for sorting into recycling or degradation pathways. [GOC:mah, NIF_Subcellular:nlx_subcell_20090701, PMID:19696797] |
| 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] |
| endosome membrane | cellular component | The lipid bilayer surrounding an endosome. [GOC:mah] |
| dendrite | cellular component | A neuron projection that has a short, tapering, morphology. Dendrites receive and integrate signals from other neurons or from sensory stimuli, and conduct nerve impulses towards the axon or the cell body. In most neurons, the impulse is conveyed from dendrites to axon via the cell body, but in some types of unipolar neuron, the impulse does not travel via the cell body. [GOC:aruk, GOC:bc, GOC:dos, GOC:mah, GOC:nln, ISBN:0198506732] |
| neuronal cell body | cellular component | The portion of a neuron that includes the nucleus, but excludes cell projections such as axons and dendrites. [GOC:go_curators] |
Active In
This protein is active in 2 target(s):
| Target | Category | Definition |
|---|
| plasma membrane | cellular component | The membrane surrounding a cell that separates the cell from its external environment. It consists of a phospholipid bilayer and associated proteins. [ISBN:0716731363] |
| axon | cellular component | The long process of a neuron that conducts nerve impulses, usually away from the cell body to the terminals and varicosities, which are sites of storage and release of neurotransmitter. [GOC:nln, ISBN:0198506732] |
Part Of
This protein is part of 2 target(s):
| Target | Category | Definition |
|---|
| receptor complex | cellular component | Any protein complex that undergoes combination with a hormone, neurotransmitter, drug or intracellular messenger to initiate a change in cell function. [GOC:go_curators] |
| plasma membrane protein complex | cellular component | Any protein complex that is part of the plasma membrane. [GOC:dos] |
Involved In
This protein is involved in 40 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] |
| ureteric bud development | biological process | The process whose specific outcome is the progression of the ureteric bud over time, from its formation to the mature structure. [GOC:go_curators] |
| neural crest cell migration | biological process | The characteristic movement of cells from the dorsal ridge of the neural tube to a variety of locations in a vertebrate embryo. [GOC:ascb_2009, GOC:dph, GOC:tb, ISBN:0878932437] |
| embryonic epithelial tube formation | biological process | The morphogenesis of an embryonic epithelium into a tube-shaped structure. [GOC:dph, ISBN:0824072820] |
| protein phosphorylation | biological process | The process of introducing a phosphate group on to a protein. [GOC:hb] |
| homophilic cell adhesion via plasma membrane adhesion molecules | biological process | The attachment of a plasma membrane adhesion molecule in one cell to an identical molecule in an adjacent cell. [ISBN:0198506732] |
| neuron cell-cell adhesion | biological process | The attachment of a neuron to another cell via adhesion molecules. [GOC:go_curators] |
| signal transduction | biological process | The cellular process in which a signal is conveyed to trigger a change in the activity or state of a cell. Signal transduction begins with reception of a signal (e.g. a ligand binding to a receptor or receptor activation by a stimulus such as light), or for signal transduction in the absence of ligand, signal-withdrawal or the activity of a constitutively active receptor. Signal transduction ends with regulation of a downstream cellular process, e.g. regulation of transcription or regulation of a metabolic process. Signal transduction covers signaling from receptors located on the surface of the cell and signaling via molecules located within the cell. For signaling between cells, signal transduction is restricted to events at and within the receiving cell. [GOC:go_curators, GOC:mtg_signaling_feb11] |
| axon guidance | biological process | The chemotaxis process that directs the migration of an axon growth cone to a specific target site in response to a combination of attractive and repulsive cues. [ISBN:0878932437] |
| posterior midgut development | biological process | The process whose specific outcome is the progression of the posterior midgut over time, from its formation to the mature structure. [GOC:go_curators] |
| response to xenobiotic stimulus | biological process | Any process that results in a change in state or activity of a cell or an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a stimulus from a xenobiotic, a compound foreign to the organim exposed to it. It may be synthesized by another organism (like ampicilin) or it can be a synthetic chemical. [GOC:jl, GOC:krc] |
| 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] |
| positive regulation of neuron projection development | biological process | Any process that increases the rate, frequency or extent of neuron projection development. Neuron projection development is the process whose specific outcome is the progression of a neuron projection over time, from its formation to the mature structure. A neuron projection is any process extending from a neural cell, such as axons or dendrites (collectively called neurites). [GOC:dph, GOC:tb] |
| positive regulation of neuron maturation | biological process | Any process that activates or increases the frequency, rate or extent of neuron maturation. [GOC:ef] |
| regulation of cell adhesion | biological process | Any process that modulates the frequency, rate or extent of attachment of a cell to another cell or to the extracellular matrix. [GOC:mah] |
| 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 peptidyl-serine phosphorylation of STAT protein | biological process | Any process that activates or increases the frequency, rate or extent of the phosphorylation of a serine residue of a STAT (Signal Transducer and Activator of Transcription) protein. [GOC:mah] |
| membrane protein proteolysis | biological process | The proteolytic cleavage of a transmembrane protein leading to the release of its intracellular or ecto-domains. [GOC:pde] |
| positive regulation of cell adhesion mediated by integrin | biological process | Any process that activates or increases the frequency, rate, or extent of cell adhesion mediated by integrin. [GOC:add] |
| ureter maturation | biological process | A developmental process, independent of morphogenetic (shape) change, that is required for the ureter to attain its fully functional state. The ureter is a muscular tube that transports urine from the kidney to the urinary bladder or from the Malpighian tubule to the hindgut. [GOC:bf, GOC:mtg_kidney_jan10, GOC:yaf, PMID:17881463] |
| glial cell-derived neurotrophic factor receptor signaling pathway | biological process | The series of molecular signals initiated by a ligand binding to a glial cell-derived neurotrophic factor receptor. [GOC:yaf, PMID:12953054, PMID:29245123] |
| neuron maturation | biological process | A developmental process, independent of morphogenetic (shape) change, that is required for a neuron to attain its fully functional state. [GOC:dph, GOC:jl] |
| positive regulation of MAPK cascade | biological process | Any process that activates or increases the frequency, rate or extent of signal transduction mediated by the MAPK cascade. [GOC:go_curators] |
| positive regulation of cell size | biological process | Any process that increases cell size. [GOC:go_curators] |
| positive regulation of DNA-templated transcription | biological process | Any process that activates or increases the frequency, rate or extent of cellular DNA-templated transcription. [GOC:go_curators, GOC:txnOH] |
| response to pain | 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 pain stimulus. Pain stimuli cause activation of nociceptors, peripheral receptors for pain, include receptors which are sensitive to painful mechanical stimuli, extreme heat or cold, and chemical stimuli. [GOC:jid, PMID:10203867, PMID:12723742, PMID:12843304, Wikipedia:Pain] |
| enteric nervous system development | biological process | The process whose specific outcome is the progression of the enteric nervous system over time, from its formation to the mature structure. The enteric nervous system is composed of two ganglionated neural plexuses in the gut wall which form one of the three major divisions of the autonomic nervous system. The enteric nervous system innervates the gastrointestinal tract, the pancreas, and the gallbladder. It contains sensory neurons, interneurons, and motor neurons. Thus the circuitry can autonomously sense the tension and the chemical environment in the gut and regulate blood vessel tone, motility, secretions, and fluid transport. The system is itself governed by the central nervous system and receives both parasympathetic and sympathetic innervation. [FMA:66070, GOC:jid, GOC:sr] |
| regulation of axonogenesis | biological process | Any process that modulates the frequency, rate or extent of axonogenesis, the generation of an axon, the long process of a neuron. [GOC:ai] |
| positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transduction | biological process | Any process that activates or increases the frequency, rate or extent of phosphatidylinositol 3-kinase/protein kinase B signal transduction. [GOC:ai] |
| retina development in camera-type eye | biological process | The process whose specific outcome is the progression of the retina over time, from its formation to the mature structure. The retina is the innermost layer or coating at the back of the eyeball, which is sensitive to light and in which the optic nerve terminates. [GOC:bf, GOC:dph, ISBN:0815340729] |
| innervation | biological process | The process in which a nerve invades a tissue and makes functional synaptic connection within the tissue. [GOC:dph, GOC:sart] |
| Peyer's patch morphogenesis | biological process | The process in which a Peyer's patch is generated and organized. Peyer's patches are typically found as nodules associated with gut epithelium with distinct internal structures including B- and T-zones for the activation of lymphocytes. [GOC:dph] |
| cellular response to retinoic acid | biological process | Any process that results in a change in state or activity of a cell (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a retinoic acid stimulus. [GOC:mah] |
| positive regulation of metanephric glomerulus development | biological process | Any process that increases the rate, frequency or extent of metanephric glomerulus development, the progression of the metanephric glomerulus over time from its initial formation until its mature state. The metanephric glomerulus is a capillary tuft surrounded by Bowman's capsule in nephrons of the vertebrate kidney, or metanephros. [GOC:mtg_kidney_jan10] |
| lymphocyte migration into lymphoid organs | biological process | The movement of a lymphocyte within the lymphatic system into lymphoid organs such as lymph nodes, spleen or Peyer's patches, and its subsequent positioning within defined functional compartments such as sites of cell activation by antigen. [GOC:BHF, GOC:pr, PMID:18379575] |
| GDF15-GFRAL signaling pathway | biological process | The series of molecular signals initiated by GDF15 binding to GFRAL coreceptor, triggering RET autophosphorylation and activation, in response to stress. [PMID:30639358, PMID:31535977, PMID:33593916, PMID:37437602] |
| positive regulation of extrinsic apoptotic signaling pathway in absence of ligand | biological process | Any process that activates or increases the frequency, rate or extent of extrinsic apoptotic signaling pathway in absence of ligand. [GOC:mtg_apoptosis] |
| positive regulation of kinase activity | biological process | Any process that activates or increases the frequency, rate or extent of kinase activity, the catalysis of the transfer of a phosphate group, usually from ATP, to a substrate molecule. [GOC:mah] |
| cell surface receptor protein tyrosine kinase signaling pathway | biological process | The series of molecular signals initiated by an extracellular ligand binding to a receptor on the surface of the target cell where the receptor possesses tyrosine kinase activity, and ending with the regulation of a downstream cellular process, e.g. transcription. [GOC:ceb, GOC:signaling] |
| multicellular organism development | biological process | The biological process whose specific outcome is the progression of a multicellular organism over time from an initial condition (e.g. a zygote or a young adult) to a later condition (e.g. a multicellular animal or an aged adult). [GOC:dph, GOC:ems, GOC:isa_complete, GOC:tb] |