Page last updated: 2024-08-07 18:28:19
Tyrosine-protein kinase ABL1
A tyrosine-protein kinase ABL1 that is encoded in the genome of human. [PRO:DNx, UniProtKB:P00519]
Synonyms
EC 2.7.10.2;
Abelson murine leukemia viral oncogene homolog 1;
Abelson tyrosine-protein kinase 1;
Proto-oncogene c-Abl;
p150
Research
Bioassay Publications (195)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 6 (3.08) | 18.2507 |
| 2000's | 57 (29.23) | 29.6817 |
| 2010's | 111 (56.92) | 24.3611 |
| 2020's | 21 (10.77) | 2.80 |
Compounds (297)
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 | 10.0000 | 7 | 7 |
| imatinib | Homo sapiens (human) | EC50 | 0.5170 | 2 | 2 |
| imatinib | Homo sapiens (human) | Kd | 1.2732 | 34 | 45 |
| triciribine phosphate | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| staurosporine | Homo sapiens (human) | Kd | 0.2729 | 29 | 29 |
| picropodophyllin | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| imatinib mesylate | Homo sapiens (human) | EC50 | 0.0900 | 1 | 1 |
| gefitinib | Homo sapiens (human) | Kd | 6.2874 | 23 | 23 |
| lestaurtinib | Homo sapiens (human) | Kd | 6.5919 | 25 | 26 |
| methotrexate | Homo sapiens (human) | EC50 | 0.0010 | 1 | 1 |
| perifosine | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| vatalanib | Homo sapiens (human) | Kd | 10.8696 | 23 | 23 |
| ruboxistaurin | Homo sapiens (human) | Kd | 10.8696 | 23 | 23 |
| canertinib | Homo sapiens (human) | Kd | 1.5812 | 30 | 30 |
| birb 796 | Homo sapiens (human) | Kd | 4.8452 | 28 | 39 |
| cyc 202 | Homo sapiens (human) | Kd | 12.5000 | 8 | 8 |
| sb 203580 | Homo sapiens (human) | Kd | 9.3864 | 22 | 22 |
| enzastaurin | Homo sapiens (human) | Kd | 11.2500 | 16 | 16 |
| erlotinib | Homo sapiens (human) | Kd | 0.8031 | 31 | 31 |
| lapatinib | Homo sapiens (human) | Kd | 10.8696 | 23 | 23 |
| sorafenib | Homo sapiens (human) | Kd | 2.1288 | 40 | 40 |
| pd 173955 | Homo sapiens (human) | Kd | 0.1736 | 15 | 15 |
| s 1033 | Homo sapiens (human) | Kd | 0.5620 | 20 | 20 |
| N-[4-(5-bromo-2-thiophenyl)-2-thiazolyl]acetamide | Homo sapiens (human) | EC50 | 50.1187 | 1 | 1 |
| xl147 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| bms 387032 | Homo sapiens (human) | Kd | 10.8696 | 23 | 23 |
| sf 2370 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| tandutinib | Homo sapiens (human) | Kd | 9.7275 | 33 | 44 |
| vx-745 | Homo sapiens (human) | Kd | 6.8361 | 28 | 28 |
| dasatinib | Homo sapiens (human) | EC50 | 3.6667 | 3 | 3 |
| dasatinib | Homo sapiens (human) | Kd | 0.3313 | 25 | 37 |
| 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 | 0.1827 | 30 | 30 |
| 4-(5-benzo(1,3)dioxol-5-yl-4-pyridin-2-yl-1h-imidazol-2-yl)benzamide | Homo sapiens (human) | Kd | 10.0000 | 7 | 7 |
| imd 0354 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| sirolimus | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| alvocidib | Homo sapiens (human) | Kd | 6.8039 | 23 | 23 |
| pd 180970 | Homo sapiens (human) | Kd | 0.3263 | 1 | 12 |
| 3-[6-[4-(trifluoromethoxy)anilino]-4-pyrimidinyl]benzamide | Homo sapiens (human) | EC50 | 0.1400 | 1 | 1 |
| 3-[6-[4-(trifluoromethoxy)anilino]-4-pyrimidinyl]benzamide | Homo sapiens (human) | Kd | 0.0920 | 1 | 1 |
| bosutinib | Homo sapiens (human) | Kd | 0.0028 | 16 | 16 |
| orantinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| su 11248 | Homo sapiens (human) | EC50 | 1.0000 | 1 | 1 |
| su 11248 | Homo sapiens (human) | Kd | 1.8825 | 40 | 51 |
| palbociclib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| jnj-7706621 | Homo sapiens (human) | Kd | 1.1840 | 7 | 7 |
| vx680 | Homo sapiens (human) | Kd | 0.3456 | 24 | 35 |
| cyc 116 | Homo sapiens (human) | Kd | 5.0570 | 1 | 1 |
| everolimus | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| ekb 569 | Homo sapiens (human) | Kd | 2.3787 | 15 | 15 |
| axitinib | Homo sapiens (human) | Kd | 0.4033 | 16 | 16 |
| temsirolimus | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| pd 184352 | Homo sapiens (human) | Kd | 10.0000 | 15 | 15 |
| 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 | 2.1640 | 1 | 1 |
| bms345541 | Homo sapiens (human) | Kd | 10.0000 | 15 | 15 |
| lenvatinib | Homo sapiens (human) | Kd | 3.7710 | 1 | 1 |
| pd 0325901 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| midostaurin | Homo sapiens (human) | Kd | 9.3997 | 32 | 32 |
| 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 | 1.8853 | 15 | 15 |
| scio-469 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| cp 724714 | Homo sapiens (human) | Kd | 12.5000 | 8 | 8 |
| pi103 | Homo sapiens (human) | Kd | 10.0000 | 22 | 22 |
| hmn-214 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| tivozanib | Homo sapiens (human) | Kd | 0.1950 | 1 | 1 |
| hki 272 | Homo sapiens (human) | Kd | 11.9471 | 16 | 17 |
| tofacitinib | Homo sapiens (human) | Kd | 10.1478 | 23 | 23 |
| n-(6-chloro-7-methoxy-9h-beta-carbolin-8-yl)-2-methylnicotinamide | Homo sapiens (human) | Kd | 10.0000 | 15 | 15 |
| cediranib | Homo sapiens (human) | Kd | 1.1856 | 16 | 16 |
| masitinib | Homo sapiens (human) | Kd | 1.3327 | 16 | 16 |
| ly-2157299 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| pazopanib | Homo sapiens (human) | Kd | 5.3630 | 23 | 23 |
| azd 6244 | Homo sapiens (human) | Kd | 11.2500 | 16 | 16 |
| su 14813 | Homo sapiens (human) | Kd | 2.7278 | 23 | 23 |
| bibw 2992 | Homo sapiens (human) | Kd | 2.7762 | 16 | 16 |
| binimetinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| sotrastaurin | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| aee 788 | Homo sapiens (human) | Kd | 1.0910 | 1 | 1 |
| saracatinib | Homo sapiens (human) | Kd | 0.0530 | 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 | 10.9524 | 16 | 17 |
| 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 | 0.9210 | 1 | 1 |
| volasertib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| pha 665752 | Homo sapiens (human) | Kd | 6.2247 | 15 | 15 |
| azd 7762 | Homo sapiens (human) | Kd | 0.6100 | 1 | 1 |
| regorafenib | Homo sapiens (human) | Kd | 0.7530 | 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 | 4.7350 | 16 | 16 |
| brivanib | Homo sapiens (human) | Kd | 4.1344 | 16 | 16 |
| 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 | 11.2500 | 16 | 16 |
| bms-690514 | Homo sapiens (human) | Kd | 0.1765 | 2 | 2 |
| bi 2536 | Homo sapiens (human) | Kd | 9.1500 | 16 | 16 |
| inno-406 | Homo sapiens (human) | Kd | 0.0260 | 1 | 1 |
| nvp-ast487 | Homo sapiens (human) | Kd | 0.0155 | 22 | 22 |
| kw 2449 | Homo sapiens (human) | Kd | 0.3125 | 16 | 16 |
| danusertib | Homo sapiens (human) | Kd | 0.0240 | 1 | 1 |
| abt 869 | Homo sapiens (human) | Kd | 11.0875 | 23 | 24 |
| 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 | 22 | 22 |
| tak 285 | Homo sapiens (human) | Kd | 30.0000 | 1 | 2 |
| idelalisib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| crizotinib | Homo sapiens (human) | Kd | 0.5482 | 16 | 16 |
| osi 906 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| chir-265 | Homo sapiens (human) | Kd | 4.9817 | 23 | 23 |
| motesanib | Homo sapiens (human) | Kd | 8.2809 | 23 | 23 |
| fostamatinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| trametinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| mln8054 | Homo sapiens (human) | Kd | 2.7163 | 23 | 23 |
| pf-562,271 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| GDC-0879 | Homo sapiens (human) | Kd | 9.5467 | 15 | 15 |
| jnj-26483327 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| ly2603618 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| tg100801 | Homo sapiens (human) | Kd | 10.7070 | 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 | 11.2500 | 16 | 16 |
| azd 1152-hqpa | Homo sapiens (human) | Kd | 6.6200 | 23 | 23 |
| nvp-tae684 | Homo sapiens (human) | Kd | 0.0890 | 15 | 15 |
| enmd 2076 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| e 7050 | Homo sapiens (human) | Kd | 0.6310 | 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 | 0.3100 | 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 | 1.1670 | 1 | 1 |
| ro5126766 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| fedratinib | Homo sapiens (human) | Kd | 2.1397 | 16 | 16 |
| gsk690693 | Homo sapiens (human) | Kd | 11.2500 | 16 | 16 |
| 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 | 32.2000 | 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 | 11.2500 | 16 | 16 |
| 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 | 3.6273 | 15 | 15 |
| mk 5108 | Homo sapiens (human) | Kd | 0.0620 | 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 | 0.2110 | 1 | 1 |
| tak 593 | Homo sapiens (human) | Kd | 0.9180 | 1 | 1 |
| mln 8237 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| sgx 523 | Homo sapiens (human) | Kd | 10.8375 | 16 | 16 |
| bms 754807 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| bms 777607 | Homo sapiens (human) | Kd | 0.5230 | 1 | 1 |
| sgi 1776 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| pci 32765 | Homo sapiens (human) | Kd | 1.6940 | 1 | 1 |
| ponatinib | Homo sapiens (human) | EC50 | 0.0036 | 3 | 3 |
| ponatinib | Homo sapiens (human) | Kd | 0.0125 | 3 | 3 |
| amg 900 | Homo sapiens (human) | Kd | 1.8990 | 1 | 1 |
| mk-1775 | Homo sapiens (human) | Kd | 1.7570 | 2 | 2 |
| AMG-208 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| quizartinib | Homo sapiens (human) | Kd | 10.1168 | 25 | 25 |
| 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 | 0.1117 | 3 | 3 |
| cabozantinib | Homo sapiens (human) | Kd | 1.0980 | 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 | 8.1500 | 16 | 16 |
| poziotinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| asp3026 | Homo sapiens (human) | Kd | 5.2580 | 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 | 0.4980 | 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 | 15 | 15 |
| pf 3758309 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| gdc 0980 | Homo sapiens (human) | Kd | 0.8140 | 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 | 0.0900 | 16 | 16 |
| 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) | Kd | 1.5450 | 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 | 2 |
| 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 | 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 | 0.0186 | 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 | 0.8420 | 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 | 0.3150 | 1 | 1 |
| otssp167 | Homo sapiens (human) | Kd | 0.2800 | 1 | 1 |
| chir 258 | Homo sapiens (human) | Kd | 1.4930 | 23 | 23 |
| osi 027 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| nintedanib | Homo sapiens (human) | Kd | 0.8592 | 16 | 16 |
| bay 80-6946 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| pp242 | Homo sapiens (human) | Kd | 1.5778 | 15 | 15 |
Drugs with Other Measurements
Benzoylbenzimidazole-based selective inhibitors targeting Cryptosporidium parvum and Toxoplasma gondii calcium-dependent protein kinase-1.Bioorganic & medicinal chemistry letters, , Aug-15, Volume: 22, Issue:16, 2012
Multiple determinants for selective inhibition of apicomplexan calcium-dependent protein kinase CDPK1.Journal of medicinal chemistry, , Mar-22, Volume: 55, Issue:6, 2012
The progress of small-molecules and degraders against BCR-ABL for the treatment of CML.European journal of medicinal chemistry, , Aug-05, Volume: 238, 2022
Designing Novel BCR-ABL Inhibitors for Chronic Myeloid Leukemia with Improved Cardiac Safety.Journal of medicinal chemistry, , 08-25, Volume: 65, Issue:16, 2022
Kinase Inhibitors as Underexplored Antiviral Agents.Journal of medicinal chemistry, , 01-27, Volume: 65, Issue:2, 2022
[no title available]European journal of medicinal chemistry, , Aug-05, Volume: 238, 2022
Comprehensive review for anticancer hybridized multitargeting HDAC inhibitors.European journal of medicinal chemistry, , Jan-01, Volume: 209, 2021
Design, synthesis, and biological evaluation of novel Bcr-AblBioorganic & medicinal chemistry, , 10-15, Volume: 48, 2021
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
Medicinal Chemistry Strategies for the Development of Kinase Inhibitors Targeting Point Mutations.Journal of medicinal chemistry, , 10-08, Volume: 63, Issue:19, 2020
Electrostatic Complementarity as a Fast and Effective Tool to Optimize Binding and Selectivity of Protein-Ligand Complexes.Journal of medicinal chemistry, , 03-28, Volume: 62, Issue:6, 2019
Structure-based analysis and biological characterization of imatinib derivatives reveal insights towards the inhibition of wild-type BCR-ABL and its mutants.Bioorganic & medicinal chemistry letters, , 12-15, Volume: 29, Issue:24, 2019
Discovery of novel Bcr-AblEuropean journal of medicinal chemistry, , Sep-15, Volume: 178, 2019
ROCK inhibitors 2. Improving potency, selectivity and solubility through the application of rationally designed solubilizing groups.Bioorganic & medicinal chemistry letters, , 08-15, Volume: 28, Issue:15, 2018
Discovery of Asciminib (ABL001), an Allosteric Inhibitor of the Tyrosine Kinase Activity of BCR-ABL1.Journal of medicinal chemistry, , 09-27, Volume: 61, Issue:18, 2018
Discovery of (E)-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((3-(2-(pyridin-2-yl)vinyl)-1H-indazol-6-yl)thio)propanamide (CHMFL-ABL-121) as a highly potent ABL kinase inhibitor capable of overcoming a variety of ABL mutants includiEuropean journal of medicinal chemistry, , Dec-05, Volume: 160, 2018
Discovery of 4-Methyl-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((1-nicotinoylpiperidin-4-yl)oxy)benzamide (CHMFL-ABL/KIT-155) as a Novel Highly Potent Type II ABL/KIT Dual Kinase Inhibitor with a Distinct Hinge Binding.Journal of medicinal chemistry, , 01-12, Volume: 60, Issue:1, 2017
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
RETRACTED: Design, synthesis, structure-activity relationship and kinase inhibitory activity of substituted 3-methyl-1-phenyl-1H-pyrazolo[3,4-d]pyrimidin-4-ones.Bioorganic & medicinal chemistry letters, , 07-01, Volume: 26, Issue:13, 2016
Rational Design, Synthesis, and Biological Evaluation of 7-Azaindole Derivatives as Potent Focused Multi-Targeted Kinase Inhibitors.Journal of medicinal chemistry, , 04-28, Volume: 59, Issue:8, 2016
Discovery of 2-((3-Amino-4-methylphenyl)amino)-N-(2-methyl-5-(3-(trifluoromethyl)benzamido)phenyl)-4-(methylamino)pyrimidine-5-carboxamide (CHMFL-ABL-053) as a Potent, Selective, and Orally Available BCR-ABL/SRC/p38 Kinase Inhibitor for Chronic Myeloid LeJournal of medicinal chemistry, , Mar-10, Volume: 59, Issue:5, 2016
Conformation-Selective Analogues of Dasatinib Reveal Insight into Kinase Inhibitor Binding and Selectivity.ACS chemical biology, , 05-20, Volume: 11, Issue:5, 2016
New approaches to the synthesis of sildenafil analogues and their enzyme inhibitory activity.Bioorganic & medicinal chemistry, , Apr-01, Volume: 23, Issue:7, 2015
Synthesis and biological evaluation of novel aromatic-heterocyclic biphenyls as potent anti-leukemia agents.European journal of medicinal chemistry, , Aug-28, Volume: 101, 2015
Development of Alkyne-Containing Pyrazolopyrimidines To Overcome Drug Resistance of Bcr-Abl Kinase.Journal of medicinal chemistry, , Dec-10, Volume: 58, Issue:23, 2015
Synthesis and biological evaluation of di-aryl urea derivatives as c-Kit inhibitors.Bioorganic & medicinal chemistry, , Nov-15, Volume: 23, Issue:22, 2015
Expanding the structural diversity of Bcr-Abl inhibitors: Hybrid molecules based on GNF-2 and Imatinib.Bioorganic & medicinal chemistry letters, , Oct-01, Volume: 25, Issue:19, 2015
Hybrid pyrimidine alkynyls inhibit the clinically resistance related Bcr-Abl(T315I) mutant.Bioorganic & medicinal chemistry letters, , Sep-01, Volume: 25, Issue:17, 2015
Expanding the structural diversity of Bcr-Abl inhibitors: Dibenzoylpiperazin incorporated with 1H-indazol-3-amine.European journal of medicinal chemistry, , Nov-02, Volume: 104, 2015
Discovery of novel Bcr-Abl inhibitors targeting myristoyl pocket and ATP site.Bioorganic & medicinal chemistry, , Dec-15, Volume: 22, Issue:24, 2014
Synthesis and kinase inhibitory activity of new sulfonamide derivatives of pyrazolo[4,3-e][1,2,4]triazines.European journal of medicinal chemistry, , May-06, Volume: 78, 2014
Imatinib analogs as potential agents for PET imaging of Bcr-Abl and c-KIT expression at a kinase level.Bioorganic & medicinal chemistry, , Jan-01, Volume: 22, Issue:1, 2014
The kinetic deuterium isotope effect as applied to metabolic deactivation of imatinib to the des-methyl metabolite, CGP74588.Bioorganic & medicinal chemistry, , Jun-01, Volume: 21, Issue:11, 2013
BCR-ABL tyrosine kinase inhibitor pharmacophore model derived from a series of phenylaminopyrimidine-based (PAP) derivatives.Bioorganic & medicinal chemistry letters, , Apr-15, Volume: 23, Issue:8, 2013
Rapid discovery of a novel series of Abl kinase inhibitors by application of an integrated microfluidic synthesis and screening platform.Journal of medicinal chemistry, , Apr-11, Volume: 56, Issue:7, 2013
Targeting gain of function and resistance mutations in Abl and KIT by hybrid compound design.Journal of medicinal chemistry, , Jul-25, Volume: 56, Issue:14, 2013
Identification of GZD824 as an orally bioavailable inhibitor that targets phosphorylated and nonphosphorylated breakpoint cluster region-Abelson (Bcr-Abl) kinase and overcomes clinically acquired mutation-induced resistance against imatinib.Journal of medicinal chemistry, , Feb-14, Volume: 56, Issue:3, 2013
Design, synthesis, biological activity, and ADME properties of pyrazolo[3,4-d]pyrimidines active in hypoxic human leukemia cells: a lead optimization study.Journal of medicinal chemistry, , Apr-28, Volume: 54, Issue:8, 2011
Synthesis and docking study of 2-phenylaminopyrimidine Abl tyrosine kinase inhibitors.Bioorganic & medicinal chemistry letters, , Dec-01, Volume: 21, Issue:23, 2011
Cysteine mapping in conformationally distinct kinase nucleotide binding sites: application to the design of selective covalent inhibitors.Journal of medicinal chemistry, , Mar-10, Volume: 54, Issue:5, 2011
Hybrid compounds as new Bcr/Abl inhibitors.Bioorganic & medicinal chemistry letters, , Apr-01, Volume: 21, Issue:7, 2011
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
Structural resemblances and comparisons of the relative pharmacological properties of imatinib and nilotinib.Bioorganic & medicinal chemistry, , Oct-01, Volume: 18, Issue:19, 2010
Design, synthesis and evaluation of (E)-alpha-benzylthio chalcones as novel inhibitors of BCR-ABL kinase.Bioorganic & medicinal chemistry, , Mar-15, Volume: 18, Issue:6, 2010
Selectively nonselective kinase inhibition: striking the right balance.Journal of medicinal chemistry, , Feb-25, Volume: 53, Issue:4, 2010
Kinase domain mutations in cancer: implications for small molecule drug design strategies.Journal of medicinal chemistry, , Mar-26, Volume: 52, Issue:6, 2009
Discovery and exploitation of inhibitor-resistant aurora and polo kinase mutants for the analysis of mitotic networks.The Journal of biological chemistry, , Jun-05, Volume: 284, Issue:23, 2009
Design of chimeric histone deacetylase- and tyrosine kinase-inhibitors: a series of imatinib hybrides as potent inhibitors of wild-type and mutant BCR-ABL, PDGF-Rbeta, and histone deacetylases.Journal of medicinal chemistry, , Apr-23, Volume: 52, Issue:8, 2009
Discovery of aryl aminoquinazoline pyridones as potent, selective, and orally efficacious inhibitors of receptor tyrosine kinase c-Kit.Journal of medicinal chemistry, , Jun-12, Volume: 51, Issue:11, 2008
Synthesis, biological evaluation and docking studies of 4-amino substituted 1H-pyrazolo[3,4-d]pyrimidines.European journal of medicinal chemistry, , Volume: 43, Issue:12, 2008
Discovery of a potent and selective c-Kit inhibitor for the treatment of inflammatory diseases.Bioorganic & medicinal chemistry letters, , Jul-15, Volume: 18, Issue:14, 2008
Discovery and SAR of 1,3,4-thiadiazole derivatives as potent Abl tyrosine kinase inhibitors and cytodifferentiating agents.Bioorganic & medicinal chemistry letters, , Feb-01, Volume: 18, Issue:3, 2008
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
Crystal structure of the T315I mutant of AbI kinase.Chemical biology & drug design, , Volume: 70, Issue:3, 2007
Structural factors contributing to the Abl/Lyn dual inhibitory activity of 3-substituted benzamide derivatives.Bioorganic & medicinal chemistry letters, , May-15, Volume: 17, Issue:10, 2007
Optimization of novel combi-molecules: identification of balanced and mixed bcr-abl/DNA targeting properties.Bioorganic & medicinal chemistry letters, , Aug-01, Volume: 17, Issue:15, 2007
Allosteric inhibitors of Bcr-abl-dependent cell proliferation.Nature chemical biology, , Volume: 2, Issue:2, 2006
A general strategy for creating "inactive-conformation" abl inhibitors.Chemistry & biology, , Volume: 13, Issue:7, 2006
Rational design of inhibitors that bind to inactive kinase conformations.Nature chemical biology, , Volume: 2, Issue:7, 2006
MASPIT: three-hybrid trap for quantitative proteome fingerprinting of small molecule-protein interactions in mammalian cells.Chemistry & biology, , Volume: 13, Issue:7, 2006
Designed multiple ligands. An emerging drug discovery paradigm.Journal of medicinal chemistry, , Oct-20, Volume: 48, Issue:21, 2005
Inhibition of drug-resistant mutants of ABL, KIT, and EGF receptor kinases.Proceedings of the National Academy of Sciences of the United States of America, , Aug-02, Volume: 102, Issue:31, 2005
Features of selective kinase inhibitors.Chemistry & biology, , Volume: 12, Issue:6, 2005
A small molecule-kinase interaction map for clinical kinase inhibitors.Nature biotechnology, , Volume: 23, Issue:3, 2005
Synthesis of pyrimidinopyridine-triazene conjugates targeted to abl tyrosine kinase.Bioorganic & medicinal chemistry letters, , Oct-06, Volume: 13, Issue:19, 2003
[no title available],
Benzoylbenzimidazole-based selective inhibitors targeting Cryptosporidium parvum and Toxoplasma gondii calcium-dependent protein kinase-1.Bioorganic & medicinal chemistry letters, , Aug-15, Volume: 22, Issue:16, 2012
Multiple determinants for selective inhibition of apicomplexan calcium-dependent protein kinase CDPK1.Journal of medicinal chemistry, , Mar-22, Volume: 55, Issue:6, 2012
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
Challenging clinically unresponsive medullary thyroid cancer: Discovery and pharmacological activity of novel RET inhibitors.European journal of medicinal chemistry, , Apr-25, Volume: 150, 2018
Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors.Bioorganic & medicinal chemistry, , 05-01, Volume: 26, Issue:8, 2018
Novel pyrrolopyrimidines as Mps1/TTK kinase inhibitors for breast cancer.Bioorganic & medicinal chemistry, , 04-01, Volume: 25, Issue:7, 2017
Novel LCK/FMS inhibitors based on phenoxypyrimidine scaffold as potential treatment for inflammatory disorders.European journal of medicinal chemistry, , Dec-01, Volume: 141, 2017
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
Design, synthesis, and biological activity of 4-(imidazo[1,2-b]pyridazin-3-yl)-1H-pyrazol-1-yl-phenylbenzamide derivatives as BCR-ABL kinase inhibitors.Bioorganic & medicinal chemistry letters, , 12-01, Volume: 26, Issue:23, 2016
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
Design, synthesis, and biological activity of phenyl-pyrazole derivatives as BCR-ABL kinase inhibitors.Bioorganic & medicinal chemistry, , Jul-01, Volume: 23, Issue:13, 2015
Discovery of N-(3-((7H-purin-6-yl)thio)-4-hydroxynaphthalen-1-yl)-sulfonamide derivatives as novel protein kinase and angiogenesis inhibitors for the treatment of cancer: Synthesis and biological evaluation. Part III.Bioorganic & medicinal chemistry, , Feb-15, Volume: 22, Issue:4, 2014
Syntheses of phenylpyrazolodiazepin-7-ones as conformationally rigid analogs of aminopyrazole amide scaffold and their antiproliferative effects on cancer cells.Bioorganic & medicinal chemistry, , Nov-15, Volume: 19, Issue:22, 2011
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
A small molecule-kinase interaction map for clinical kinase inhibitors.Nature biotechnology, , Volume: 23, Issue:3, 2005
Synthesis and biological evaluation of 1-aryl-4,5-dihydro-1H-pyrazolo[3,4-d]pyrimidin-4-one inhibitors of cyclin-dependent kinases.Journal of medicinal chemistry, , Nov-18, Volume: 47, Issue:24, 2004
Identification of orally active, potent, and selective 4-piperazinylquinazolines as antagonists of the platelet-derived growth factor receptor tyrosine kinase family.Journal of medicinal chemistry, , Aug-15, Volume: 45, Issue:17, 2002
Recent Developments in the Use of Kinase Inhibitors for Management of Viral Infections.Journal of medicinal chemistry, , 01-27, Volume: 65, Issue:2, 2022
3-Benzimidazol-2-yl-1H-indazoles as potent c-ABL inhibitors.Bioorganic & medicinal chemistry letters, , Jul-15, Volume: 16, Issue:14, 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
Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases.Nature chemical biology, , Volume: 4, Issue:11, 2008
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
A small molecule-kinase interaction map for clinical kinase inhibitors.Nature biotechnology, , Volume: 23, Issue:3, 2005
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
Inhibition of drug-resistant mutants of ABL, KIT, and EGF receptor kinases.Proceedings of the National Academy of Sciences of the United States of America, , Aug-02, Volume: 102, Issue:31, 2005
A small molecule-kinase interaction map for clinical kinase inhibitors.Nature biotechnology, , Volume: 23, Issue:3, 2005
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
RETRACTED: Design, synthesis, structure-activity relationship and kinase inhibitory activity of substituted 3-methyl-1-phenyl-1H-pyrazolo[3,4-d]pyrimidin-4-ones.Bioorganic & medicinal chemistry letters, , 07-01, Volume: 26, Issue:13, 2016
New approaches to the synthesis of sildenafil analogues and their enzyme inhibitory activity.Bioorganic & medicinal chemistry, , Apr-01, Volume: 23, Issue:7, 2015
Synthesis and kinase inhibitory activity of new sulfonamide derivatives of pyrazolo[4,3-e][1,2,4]triazines.European journal of medicinal chemistry, , May-06, Volume: 78, 2014
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
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
A small molecule-kinase interaction map for clinical kinase inhibitors.Nature biotechnology, , Volume: 23, Issue:3, 2005
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
Novel chimeric histone deacetylase inhibitors: a series of lapatinib hybrides as potent inhibitors of epidermal growth factor receptor (EGFR), human epidermal growth factor receptor 2 (HER2), and histone deacetylase activity.Journal of medicinal chemistry, , Dec-23, Volume: 53, Issue:24, 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
Identification of a potent 5-phenyl-thiazol-2-ylamine-based inhibitor of FLT3 with activity against drug resistance-conferring point mutations.European journal of medicinal chemistry, , Jul-15, Volume: 100, 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
Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases.Nature chemical biology, , Volume: 4, Issue:11, 2008
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
Design and synthesis of orally bioavailable benzimidazoles as Raf kinase inhibitors.Journal of medicinal chemistry, , Nov-27, Volume: 51, Issue:22, 2008
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
A small molecule-kinase interaction map for clinical kinase inhibitors.Nature biotechnology, , Volume: 23, Issue:3, 2005
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
New effective inhibitors of the Abelson kinase.Bioorganic & medicinal chemistry, , Sep-01, Volume: 18, Issue:17, 2010
A general strategy for creating "inactive-conformation" abl inhibitors.Chemistry & biology, , Volume: 13, Issue:7, 2006
Structural insights into the ATP binding pocket of the anaplastic lymphoma kinase by site-directed mutagenesis, inhibitor binding analysis, and homology modeling.Journal of medicinal chemistry, , Sep-21, Volume: 49, Issue:19, 2006
MASPIT: three-hybrid trap for quantitative proteome fingerprinting of small molecule-protein interactions in mammalian cells.Chemistry & biology, , Volume: 13, Issue:7, 2006
Recent Developments in the Use of Kinase Inhibitors for Management of Viral Infections.Journal of medicinal chemistry, , 01-27, Volume: 65, Issue:2, 2022
Structure-activity relationships of 6-(2,6-dichlorophenyl)-8-methyl-2-(phenylamino)pyrido[2,3-d]pyrimidin-7-ones: toward selective Abl inhibitors.Bioorganic & medicinal chemistry letters, , Dec-15, Volume: 19, Issue:24, 2009
Discovery of 4-methyl-3-(pyridin-2-ylamino)benzamide derivatives as C-Abl inhibitors with potential neuroprotective effect.Bioorganic & medicinal chemistry, , Nov-15, Volume: 74, 2022
Designing Novel BCR-ABL Inhibitors for Chronic Myeloid Leukemia with Improved Cardiac Safety.Journal of medicinal chemistry, , 08-25, Volume: 65, Issue:16, 2022
Kinase Inhibitors as Underexplored Antiviral Agents.Journal of medicinal chemistry, , 01-27, Volume: 65, Issue:2, 2022
Recent Developments in the Use of Kinase Inhibitors for Management of Viral Infections.Journal of medicinal chemistry, , 01-27, Volume: 65, Issue:2, 2022
The progress of small-molecules and degraders against BCR-ABL for the treatment of CML.European journal of medicinal chemistry, , Aug-05, Volume: 238, 2022
A small molecule inhibitor of PCSK9 that antagonizes LDL receptor binding via interaction with a cryptic PCSK9 binding groove.Bioorganic & medicinal chemistry, , 03-15, Volume: 28, Issue:6, 2020
Accelerated Discovery of Novel Ponatinib Analogs with Improved Properties for the Treatment of Parkinson's Disease.ACS medicinal chemistry letters, , Apr-09, Volume: 11, Issue:4, 2020
Structure-based analysis and biological characterization of imatinib derivatives reveal insights towards the inhibition of wild-type BCR-ABL and its mutants.Bioorganic & medicinal chemistry letters, , 12-15, Volume: 29, Issue:24, 2019
Why Some Targets Benefit from beyond Rule of Five Drugs.Journal of medicinal chemistry, , 11-27, Volume: 62, Issue:22, 2019
Brain penetrant kinase inhibitors: Learning from kinase neuroscience discovery.Bioorganic & medicinal chemistry letters, , 06-15, Volume: 28, Issue:11, 2018
Discovery of Asciminib (ABL001), an Allosteric Inhibitor of the Tyrosine Kinase Activity of BCR-ABL1.Journal of medicinal chemistry, , 09-27, Volume: 61, Issue:18, 2018
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
Discovery of 2-((3-Amino-4-methylphenyl)amino)-N-(2-methyl-5-(3-(trifluoromethyl)benzamido)phenyl)-4-(methylamino)pyrimidine-5-carboxamide (CHMFL-ABL-053) as a Potent, Selective, and Orally Available BCR-ABL/SRC/p38 Kinase Inhibitor for Chronic Myeloid LeJournal of medicinal chemistry, , Mar-10, Volume: 59, Issue:5, 2016
Conformation-Selective Analogues of Dasatinib Reveal Insight into Kinase Inhibitor Binding and Selectivity.ACS chemical biology, , 05-20, Volume: 11, Issue:5, 2016
Hybrid pyrimidine alkynyls inhibit the clinically resistance related Bcr-Abl(T315I) mutant.Bioorganic & medicinal chemistry letters, , Sep-01, Volume: 25, Issue:17, 2015
Synthesis and biological evaluation of analogues of the kinase inhibitor nilotinib as Abl and Kit inhibitors.Bioorganic & medicinal chemistry letters, , Feb-01, Volume: 23, Issue:3, 2013
Design, synthesis and biological activities of Nilotinib derivates as antitumor agents.Bioorganic & medicinal chemistry, , May-01, Volume: 21, Issue:9, 2013
Identification of GZD824 as an orally bioavailable inhibitor that targets phosphorylated and nonphosphorylated breakpoint cluster region-Abelson (Bcr-Abl) kinase and overcomes clinically acquired mutation-induced resistance against imatinib.Journal of medicinal chemistry, , Feb-14, Volume: 56, Issue:3, 2013
Hybrid compounds as new Bcr/Abl inhibitors.Bioorganic & medicinal chemistry letters, , Apr-01, Volume: 21, Issue:7, 2011
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
Structural analysis of DFG-in and DFG-out dual Src-Abl inhibitors sharing a common vinyl purine template.Chemical biology & drug design, , Volume: 75, Issue:1, 2010
Selectively nonselective kinase inhibition: striking the right balance.Journal of medicinal chemistry, , Feb-25, Volume: 53, Issue:4, 2010
Structural resemblances and comparisons of the relative pharmacological properties of imatinib and nilotinib.Bioorganic & medicinal chemistry, , Oct-01, Volume: 18, Issue:19, 2010
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
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
Inhibition of drug-resistant mutants of ABL, KIT, and EGF receptor kinases.Proceedings of the National Academy of Sciences of the United States of America, , Aug-02, Volume: 102, Issue:31, 2005
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
A small molecule-kinase interaction map for clinical kinase inhibitors.Nature biotechnology, , Volume: 23, Issue:3, 2005
The progress of small-molecules and degraders against BCR-ABL for the treatment of CML.European journal of medicinal chemistry, , Aug-05, Volume: 238, 2022
Designing Novel BCR-ABL Inhibitors for Chronic Myeloid Leukemia with Improved Cardiac Safety.Journal of medicinal chemistry, , 08-25, Volume: 65, Issue:16, 2022
Kinase Inhibitors as Underexplored Antiviral Agents.Journal of medicinal chemistry, , 01-27, Volume: 65, Issue:2, 2022
Recent Developments in the Use of Kinase Inhibitors for Management of Viral Infections.Journal of medicinal chemistry, , 01-27, Volume: 65, Issue:2, 2022
Comprehensive review for anticancer hybridized multitargeting HDAC inhibitors.European journal of medicinal chemistry, , Jan-01, Volume: 209, 2021
Discovery of novel BCR-ABL PROTACs based on the cereblon E3 ligase design, synthesis, and biological evaluation.European journal of medicinal chemistry, , Nov-05, Volume: 223, 2021
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
Global PROTAC Toolbox for Degrading BCR-ABL Overcomes Drug-Resistant Mutants and Adverse Effects.Journal of medicinal chemistry, , 08-13, Volume: 63, Issue:15, 2020
The p53 stabilizing agent CP-31398 and multi-kinase inhibitors. Designing, synthesizing and screening of styrylquinazoline series.European journal of medicinal chemistry, , Feb-01, Volume: 163, 2019
Controlling cellular distribution of drugs with permeability modifying moieties.MedChemComm, , Jun-01, Volume: 10, Issue:6, 2019
Discovery of Novel Dual Mechanism of Action Src Signaling and Tubulin Polymerization Inhibitors (KX2-391 and KX2-361).Journal of medicinal chemistry, , 06-14, Volume: 61, Issue:11, 2018
Discovery of Asciminib (ABL001), an Allosteric Inhibitor of the Tyrosine Kinase Activity of BCR-ABL1.Journal of medicinal chemistry, , 09-27, Volume: 61, Issue:18, 2018
Design and synthesis of novel dasatinib derivatives as inhibitors of leukemia stem cells.Bioorganic & medicinal chemistry letters, , 02-15, Volume: 28, Issue:4, 2018
Synthesis and biological evaluation of novel dasatinib analogues as potent DDR1 and DDR2 kinase inhibitors.Chemical biology & drug design, , Volume: 89, Issue:3, 2017
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Conformation-Selective Analogues of Dasatinib Reveal Insight into Kinase Inhibitor Binding and Selectivity.ACS chemical biology, , 05-20, Volume: 11, Issue:5, 2016
Part-1: Design, synthesis and biological evaluation of novel bromo-pyrimidine analogs as tyrosine kinase inhibitors.European journal of medicinal chemistry, , Aug-25, Volume: 119, 2016
Novel pyrazolo[3,4-d]pyrimidines as dual Src-Abl inhibitors active against mutant form of Abl and the leukemia K-562 cell line.European journal of medicinal chemistry, , Nov-10, Volume: 123, 2016
Rational Design, Synthesis, and Biological Evaluation of 7-Azaindole Derivatives as Potent Focused Multi-Targeted Kinase Inhibitors.Journal of medicinal chemistry, , 04-28, Volume: 59, Issue:8, 2016
Discovery of 2-((3-Amino-4-methylphenyl)amino)-N-(2-methyl-5-(3-(trifluoromethyl)benzamido)phenyl)-4-(methylamino)pyrimidine-5-carboxamide (CHMFL-ABL-053) as a Potent, Selective, and Orally Available BCR-ABL/SRC/p38 Kinase Inhibitor for Chronic Myeloid LeJournal of medicinal chemistry, , Mar-10, Volume: 59, Issue:5, 2016
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
Hybrid pyrimidine alkynyls inhibit the clinically resistance related Bcr-Abl(T315I) mutant.Bioorganic & medicinal chemistry letters, , Sep-01, Volume: 25, Issue:17, 2015
Expanding the structural diversity of Bcr-Abl inhibitors: Dibenzoylpiperazin incorporated with 1H-indazol-3-amine.European journal of medicinal chemistry, , Nov-02, Volume: 104, 2015
Identification of GZD824 as an orally bioavailable inhibitor that targets phosphorylated and nonphosphorylated breakpoint cluster region-Abelson (Bcr-Abl) kinase and overcomes clinically acquired mutation-induced resistance against imatinib.Journal of medicinal chemistry, , Feb-14, Volume: 56, Issue:3, 2013
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
Selectively nonselective kinase inhibition: striking the right balance.Journal of medicinal chemistry, , Feb-25, Volume: 53, Issue:4, 2010
Global target profile of the kinase inhibitor bosutinib in primary chronic myeloid leukemia cells.Leukemia, , Volume: 23, Issue:3, 2009
Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases.Nature chemical biology, , Volume: 4, Issue:11, 2008
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Crystal structure of the T315I mutant of AbI kinase.Chemical biology & drug design, , Volume: 70, Issue:3, 2007
Synthesis and biological evaluation of a fluorine-18 derivative of dasatinib.Journal of medicinal chemistry, , Nov-15, Volume: 50, Issue:23, 2007
The Btk tyrosine kinase is a major target of the Bcr-Abl inhibitor dasatinib.Proceedings of the National Academy of Sciences of the United States of America, , Aug-14, Volume: 104, Issue:33, 2007
2-aminothiazole as a novel kinase inhibitor template. Structure-activity relationship studies toward the discovery of N-(2-chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)-1- piperazinyl)]-2-methyl-4-pyrimidinyl]amino)]-1,3-thiazole-5-carboxamide (dasatinJournal of medicinal chemistry, , Nov-16, Volume: 49, Issue:23, 2006
Inhibition of drug-resistant mutants of ABL, KIT, and EGF receptor kinases.Proceedings of the National Academy of Sciences of the United States of America, , Aug-02, Volume: 102, Issue:31, 2005
Discovery of N-(2-chloro-6-methyl- phenyl)-2-(6-(4-(2-hydroxyethyl)- piperazin-1-yl)-2-methylpyrimidin-4- ylamino)thiazole-5-carboxamide (BMS-354825), a dual Src/Abl kinase inhibitor with potent antitumor activity in preclinical assays.Journal of medicinal chemistry, , Dec-30, Volume: 47, Issue:27, 2004
[no title available],
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Discovery of biarylaminoquinazolines as novel tubulin polymerization inhibitors.Journal of medicinal chemistry, , Jun-12, Volume: 57, Issue:11, 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
A small molecule-kinase interaction map for clinical kinase inhibitors.Nature biotechnology, , Volume: 23, Issue:3, 2005
Anthranilic acid amides: a novel class of antiangiogenic VEGF receptor kinase inhibitors.Journal of medicinal chemistry, , Dec-19, Volume: 45, Issue:26, 2002
Use of a pharmacophore model for the design of EGFR tyrosine kinase inhibitors: isoflavones and 3-phenyl-4(1H)-quinolones.Journal of medicinal chemistry, , Mar-25, Volume: 42, Issue:6, 1999
[(Alkylamino)methyl]acrylophenones: potent and selective inhibitors of the epidermal growth factor receptor protein tyrosine kinase.Journal of medicinal chemistry, , Jun-23, Volume: 38, Issue:13, 1995
Thiazolidine-diones. Biochemical and biological activity of a novel class of tyrosine protein kinase inhibitors.The Journal of biological chemistry, , Dec-25, Volume: 265, Issue:36, 1990
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
Recent Developments in the Use of Kinase Inhibitors for Management of Viral Infections.Journal of medicinal chemistry, , 01-27, Volume: 65, Issue:2, 2022
Kinase Atlas: Druggability Analysis of Potential Allosteric Sites in Kinases.Journal of medicinal chemistry, , 07-25, Volume: 62, Issue:14, 2019
Discovery of Asciminib (ABL001), an Allosteric Inhibitor of the Tyrosine Kinase Activity of BCR-ABL1.Journal of medicinal chemistry, , 09-27, Volume: 61, Issue:18, 2018
Targeting the Allosteric Site of Oncoprotein BCR-ABL as an Alternative Strategy for Effective Target Protein Degradation.ACS medicinal chemistry letters, , Oct-12, Volume: 8, Issue:10, 2017
Expanding the diversity of allosteric bcr-abl inhibitors.Journal of medicinal chemistry, , Oct-14, Volume: 53, Issue:19, 2010
Allosteric inhibitors of Bcr-abl-dependent cell proliferation.Nature chemical biology, , Volume: 2, Issue:2, 2006
Recent Developments in the Use of Kinase Inhibitors for Management of Viral Infections.Journal of medicinal chemistry, , 01-27, Volume: 65, Issue:2, 2022
The progress of small-molecules and degraders against BCR-ABL for the treatment of CML.European journal of medicinal chemistry, , Aug-05, Volume: 238, 2022
Discovery of Asciminib (ABL001), an Allosteric Inhibitor of the Tyrosine Kinase Activity of BCR-ABL1.Journal of medicinal chemistry, , 09-27, Volume: 61, Issue:18, 2018
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
AXL Inhibitors in Cancer: A Medicinal Chemistry Perspective.Journal of medicinal chemistry, , 04-28, Volume: 59, Issue:8, 2016
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
Selectively nonselective kinase inhibition: striking the right balance.Journal of medicinal chemistry, , Feb-25, Volume: 53, Issue:4, 2010
Global target profile of the kinase inhibitor bosutinib in primary chronic myeloid leukemia cells.Leukemia, , Volume: 23, Issue:3, 2009
Structural insights into the ATP binding pocket of the anaplastic lymphoma kinase by site-directed mutagenesis, inhibitor binding analysis, and homology modeling.Journal of medicinal chemistry, , Sep-21, Volume: 49, Issue:19, 2006
Inhibition of Src kinase activity by 7-[(2,4-dichloro-5-methoxyphenyl)amino]-2-heteroaryl-thieno[3,2-b]pyridine-6-carbonitriles.Bioorganic & medicinal chemistry letters, , Nov-01, Volume: 15, Issue:21, 2005
Designed multiple ligands. An emerging drug discovery paradigm.Journal of medicinal chemistry, , Oct-20, Volume: 48, Issue:21, 2005
4-Anilino-7,8-dialkoxybenzo[g]quinoline-3-carbonitriles as potent Src kinase inhibitors.Journal of medicinal chemistry, , Sep-22, Volume: 48, Issue:19, 2005
Synthesis and Src kinase inhibitory activity of 2-phenyl- and 2-thienyl-7-phenylaminothieno[3,2-b]pyridine-6-carbonitriles.Journal of medicinal chemistry, , Jun-02, Volume: 48, Issue:11, 2005
7-Alkoxy-4-phenylamino-3-quinolinecar-bonitriles as dual inhibitors of Src and Abl kinases.Journal of medicinal chemistry, , Mar-25, Volume: 47, Issue:7, 2004
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
Anthranilic acid amides: a novel class of antiangiogenic VEGF receptor kinase inhibitors.Journal of medicinal chemistry, , Dec-19, Volume: 45, Issue:26, 2002
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Rational Design, Synthesis, and Biological Evaluation of 7-Azaindole Derivatives as Potent Focused Multi-Targeted Kinase Inhibitors.Journal of medicinal chemistry, , 04-28, Volume: 59, Issue:8, 2016
Targeting gain of function and resistance mutations in Abl and KIT by hybrid compound design.Journal of medicinal chemistry, , Jul-25, Volume: 56, Issue:14, 2013
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
Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases.Nature chemical biology, , Volume: 4, Issue:11, 2008
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
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
Inhibition of drug-resistant mutants of ABL, KIT, and EGF receptor kinases.Proceedings of the National Academy of Sciences of the United States of America, , Aug-02, Volume: 102, Issue:31, 2005
A small molecule-kinase interaction map for clinical kinase inhibitors.Nature biotechnology, , Volume: 23, Issue:3, 2005
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Discovery of 8-cyclopentyl-2-[4-(4-methyl-piperazin-1-yl)-phenylamino]-7-oxo-7,8-dihydro-pyrido[2,3-d]pyrimidine-6-carbonitrile (7x) as a potent inhibitor of cyclin-dependent kinase 4 (CDK4) and AMPK-related kinase 5 (ARK5).Journal of medicinal chemistry, , Feb-13, Volume: 57, Issue:3, 2014
The progress of small-molecules and degraders against BCR-ABL for the treatment of CML.European journal of medicinal chemistry, , Aug-05, Volume: 238, 2022
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
BCR-ABL tyrosine kinase inhibitor pharmacophore model derived from a series of phenylaminopyrimidine-based (PAP) derivatives.Bioorganic & medicinal chemistry letters, , Apr-15, Volume: 23, Issue:8, 2013
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
Discovery and exploitation of inhibitor-resistant aurora and polo kinase mutants for the analysis of mitotic networks.The Journal of biological chemistry, , Jun-05, Volume: 284, Issue:23, 2009
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
Crystal structure of the T315I mutant of AbI kinase.Chemical biology & drug design, , Volume: 70, Issue:3, 2007
Inhibition of drug-resistant mutants of ABL, KIT, and EGF receptor kinases.Proceedings of the National Academy of Sciences of the United States of America, , Aug-02, Volume: 102, Issue:31, 2005
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Discovery of N-phenyl-4-(thiazol-5-yl)pyrimidin-2-amine aurora kinase inhibitors.Journal of medicinal chemistry, , Jun-10, Volume: 53, Issue:11, 2010
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 small molecule-kinase interaction map for clinical kinase inhibitors.Nature biotechnology, , Volume: 23, Issue:3, 2005
Discovery of (E)-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((3-(2-(pyridin-2-yl)vinyl)-1H-indazol-6-yl)thio)propanamide (CHMFL-ABL-121) as a highly potent ABL kinase inhibitor capable of overcoming a variety of ABL mutants includiEuropean journal of medicinal chemistry, , Dec-05, Volume: 160, 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 systematic interaction map of validated kinase inhibitors with Ser/Thr kinases.Proceedings of the National Academy of Sciences of the United States of America, , Dec-18, Volume: 104, Issue:51, 2007
(6,7-Dimethoxy-2,4-dihydroindeno[1,2-c]pyrazol-3-yl)phenylamines: platelet-derived growth factor receptor tyrosine kinase inhibitors with broad antiproliferative activity against tumor cells.Journal of medicinal chemistry, , Dec-29, Volume: 48, Issue:26, 2005
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Identification of a potent 5-phenyl-thiazol-2-ylamine-based inhibitor of FLT3 with activity against drug resistance-conferring point mutations.European journal of medicinal chemistry, , Jul-15, Volume: 100, 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
BCR-ABL tyrosine kinase inhibitor pharmacophore model derived from a series of phenylaminopyrimidine-based (PAP) derivatives.Bioorganic & medicinal chemistry letters, , Apr-15, Volume: 23, Issue:8, 2013
Synthesis and docking study of 2-phenylaminopyrimidine Abl tyrosine kinase inhibitors.Bioorganic & medicinal chemistry letters, , Dec-01, Volume: 21, Issue:23, 2011
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
Design, synthesis and biological evaluation of pazopanib derivatives as antitumor agents.Chemical biology & drug design, , Volume: 83, Issue:3, 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
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
Emerging targets in osteoporosis disease modification.Journal of medicinal chemistry, , Jun-10, Volume: 53, Issue:11, 2010
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
N-(5-chloro-1,3-benzodioxol-4-yl)-7-[2-(4-methylpiperazin-1-yl)ethoxy]-5- (tetrahydro-2H-pyran-4-yloxy)quinazolin-4-amine, a novel, highly selective, orally available, dual-specific c-Src/Abl kinase inhibitor.Journal of medicinal chemistry, , Nov-02, Volume: 49, Issue:22, 2006
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
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
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
Identification of N-(4-piperidinyl)-4-(2,6-dichlorobenzoylamino)-1H-pyrazole-3-carboxamide (AT7519), a novel cyclin dependent kinase inhibitor using fragment-based X-ray crystallography and structure based drug design.Journal of medicinal chemistry, , Aug-28, Volume: 51, Issue:16, 2008
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 progress of small-molecules and degraders against BCR-ABL for the treatment of CML.European journal of medicinal chemistry, , Aug-05, Volume: 238, 2022
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Structural factors contributing to the Abl/Lyn dual inhibitory activity of 3-substituted benzamide derivatives.Bioorganic & medicinal chemistry letters, , May-15, Volume: 17, Issue:10, 2007
Structure-Activity Relationship Studies of Mitogen Activated Protein Kinase Interacting Kinase (MNK) 1 and 2 and BCR-ABL1 Inhibitors Targeting Chronic Myeloid Leukemic Cells.Journal of medicinal chemistry, , Apr-14, Volume: 59, Issue:7, 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
The progress of small-molecules and degraders against BCR-ABL for the treatment of CML.European journal of medicinal chemistry, , Aug-05, Volume: 238, 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
Selectivity data: assessment, predictions, concordance, and implications.Journal of medicinal chemistry, , Sep-12, Volume: 56, Issue:17, 2013
A type-II kinase inhibitor capable of inhibiting the T315I "gatekeeper" mutant of Bcr-Abl.Journal of medicinal chemistry, , Aug-12, Volume: 53, Issue:15, 2010
1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazoles: identification of a potent Aurora kinase inhibitor with a favorable antitumor kinase inhibition profile.Journal of medicinal chemistry, , Nov-30, Volume: 49, Issue:24, 2006
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
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
Pyridazinone derivatives displaying highly potent and selective inhibitory activities against c-Met tyrosine kinase.European journal of medicinal chemistry, , Jan-27, Volume: 108, 2016
Structure based drug design of crizotinib (PF-02341066), a potent and selective dual inhibitor of mesenchymal-epithelial transition factor (c-MET) kinase and anaplastic lymphoma kinase (ALK).Journal of medicinal chemistry, , Sep-22, Volume: 54, Issue:18, 2011
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
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
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
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
Identification of N,1,4,4-tetramethyl-8-{[4-(4-methylpiperazin-1-yl)phenyl]amino}-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide (PHA-848125), a potent, orally available cyclin dependent kinase inhibitor.Journal of medicinal chemistry, , Aug-27, Volume: 52, Issue:16, 2009
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
Discovery of Novel Dual Mechanism of Action Src Signaling and Tubulin Polymerization Inhibitors (KX2-391 and KX2-361).Journal of medicinal chemistry, , 06-14, Volume: 61, Issue:11, 2018
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 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
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
Designing Novel BCR-ABL Inhibitors for Chronic Myeloid Leukemia with Improved Cardiac Safety.Journal of medicinal chemistry, , 08-25, Volume: 65, Issue:16, 2022
The progress of small-molecules and degraders against BCR-ABL for the treatment of CML.European journal of medicinal chemistry, , Aug-05, Volume: 238, 2022
Discovery of a benzimidazole-based dual FLT3/TrKA inhibitor targeting acute myeloid leukemia.Bioorganic & medicinal chemistry, , 02-15, Volume: 56, 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
Small-Molecule Inhibitors of Necroptosis: Current Status and Perspectives.Journal of medicinal chemistry, , 02-27, Volume: 63, Issue:4, 2020
Medicinal Chemistry Strategies for the Development of Kinase Inhibitors Targeting Point Mutations.Journal of medicinal chemistry, , 10-08, Volume: 63, Issue:19, 2020
Global PROTAC Toolbox for Degrading BCR-ABL Overcomes Drug-Resistant Mutants and Adverse Effects.Journal of medicinal chemistry, , 08-13, Volume: 63, Issue:15, 2020
Accelerated Discovery of Novel Ponatinib Analogs with Improved Properties for the Treatment of Parkinson's Disease.ACS medicinal chemistry letters, , Apr-09, Volume: 11, Issue:4, 2020
Homogeneous Assay for Target Engagement Utilizing Bioluminescent Thermal Shift.ACS medicinal chemistry letters, , Jun-14, Volume: 9, Issue:6, 2018
Discovery of Asciminib (ABL001), an Allosteric Inhibitor of the Tyrosine Kinase Activity of BCR-ABL1.Journal of medicinal chemistry, , 09-27, Volume: 61, Issue:18, 2018
An overview of the binding models of FGFR tyrosine kinases in complex with small molecule inhibitors.European journal of medicinal chemistry, , Jan-27, Volume: 126, 2017
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
Rational Design, Synthesis, and Biological Evaluation of 7-Azaindole Derivatives as Potent Focused Multi-Targeted Kinase Inhibitors.Journal of medicinal chemistry, , 04-28, Volume: 59, Issue:8, 2016
Conformation-Selective Analogues of Dasatinib Reveal Insight into Kinase Inhibitor Binding and Selectivity.ACS chemical biology, , 05-20, Volume: 11, Issue:5, 2016
Hybrid pyrimidine alkynyls inhibit the clinically resistance related Bcr-Abl(T315I) mutant.Bioorganic & medicinal chemistry letters, , Sep-01, Volume: 25, Issue:17, 2015
Discovery of new benzothiazole-based inhibitors of breakpoint cluster region-Abelson kinase including the T315I mutant.Journal of medicinal chemistry, , May-09, Volume: 56, Issue:9, 2013
Targeting gain of function and resistance mutations in Abl and KIT by hybrid compound design.Journal of medicinal chemistry, , Jul-25, Volume: 56, Issue:14, 2013
Identification of GZD824 as an orally bioavailable inhibitor that targets phosphorylated and nonphosphorylated breakpoint cluster region-Abelson (Bcr-Abl) kinase and overcomes clinically acquired mutation-induced resistance against imatinib.Journal of medicinal chemistry, , Feb-14, Volume: 56, Issue:3, 2013
Discovery of 5-(arenethynyl) hetero-monocyclic derivatives as potent inhibitors of BCR-ABL including the T315I gatekeeper mutant.Bioorganic & medicinal chemistry letters, , Jun-15, Volume: 21, Issue:12, 2011
Discovery of 3-[2-(imidazo[1,2-b]pyridazin-3-yl)ethynyl]-4-methyl-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzamide (AP24534), a potent, orally active pan-inhibitor of breakpoint cluster region-abelson (BCR-ABL) kinase including thJournal of medicinal chemistry, , Jun-24, Volume: 53, Issue:12, 2010
Structural Basis of Wee Kinases Functionality and Inactivation by Diverse Small Molecule Inhibitors.Journal of medicinal chemistry, , 09-28, Volume: 60, Issue:18, 2017
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 a potent 5-phenyl-thiazol-2-ylamine-based inhibitor of FLT3 with activity against drug resistance-conferring point mutations.European journal of medicinal chemistry, , Jul-15, Volume: 100, 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
Discovery of a benzimidazole-based dual FLT3/TrKA inhibitor targeting acute myeloid leukemia.Bioorganic & medicinal chemistry, , 02-15, Volume: 56, 2022
The progress of small-molecules and degraders against BCR-ABL for the treatment of CML.European journal of medicinal chemistry, , Aug-05, Volume: 238, 2022
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Conformation-Selective Analogues of Dasatinib Reveal Insight into Kinase Inhibitor Binding and Selectivity.ACS chemical biology, , 05-20, Volume: 11, Issue:5, 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 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
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 progress of small-molecules and degraders against BCR-ABL for the treatment of CML.European journal of medicinal chemistry, , Aug-05, Volume: 238, 2022
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
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
Targeting gain of function and resistance mutations in Abl and KIT by hybrid compound design.Journal of medicinal chemistry, , Jul-25, Volume: 56, Issue:14, 2013
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 26 target(s):
| Target | Category | Definition |
|---|
| magnesium ion binding | molecular function | Binding to a magnesium (Mg) ion. [GOC:ai] |
| four-way junction DNA binding | molecular function | Binding to a DNA segment containing four-way junctions, also known as Holliday junctions, a structure where two DNA double strands are held together by reciprocal exchange of two of the four strands, one strand each from the two original helices. [GOC:krc, ISBN:0815332181, PMID:15563464] |
| bubble DNA binding | molecular function | Binding to DNA segment that contains a bubble. A bubble occurs when DNA contains a region of unpaired, single-stranded DNA flanked on both sides by regions of paired, double-stranded DNA. [GOC:elh, GOC:vw, PMID:16781730] |
| phosphotyrosine residue binding | molecular function | Binding to a phosphorylated tyrosine residue within a protein. [PMID:14636584] |
| DNA binding | molecular function | Any molecular function by which a gene product interacts selectively and non-covalently with DNA (deoxyribonucleic acid). [GOC:dph, GOC:jl, GOC:tb, GOC:vw] |
| transcription coactivator activity | molecular function | A transcription coregulator activity that activates or increases the transcription of specific gene sets via binding to a DNA-bound DNA-binding transcription factor, either on its own or as part of a complex. Coactivators often act by altering chromatin structure and modifications. For example, one class of transcription coactivators modifies chromatin structure through covalent modification of histones. A second class remodels the conformation of chromatin in an ATP-dependent fashion. A third class modulates interactions of DNA-bound DNA-binding transcription factors with other transcription coregulators. A fourth class of coactivator activity is the bridging of a DNA-binding transcription factor to the general (basal) transcription machinery. The Mediator complex, which bridges sequence-specific DNA binding transcription factors and RNA polymerase, is also a transcription coactivator. [GOC:txnOH-2018, PMID:10213677, PMID:16858867] |
| actin monomer binding | molecular function | Binding to monomeric actin, also known as G-actin. [GOC:ai] |
| nicotinate-nucleotide adenylyltransferase activity | molecular function | Catalysis of the reaction: ATP + nicotinate ribonucleotide = diphosphate + deamido-NAD+. [EC:2.7.7.18] |
| 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 tyrosine kinase activity | molecular function | Catalysis of the reaction: ATP + a protein tyrosine = ADP + protein tyrosine phosphate. [RHEA:10596] |
| non-membrane spanning protein tyrosine kinase activity | molecular function | Catalysis of the reaction: ATP + protein L-tyrosine = ADP + protein L-tyrosine phosphate by a non-membrane spanning protein. [EC:2.7.10.2] |
| protein kinase C binding | molecular function | Binding to protein kinase C. [GOC:jl] |
| 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] |
| kinase activity | molecular function | Catalysis of the transfer of a phosphate group, usually from ATP, to a substrate molecule. [ISBN:0198506732] |
| SH3 domain binding | molecular function | Binding to a SH3 domain (Src homology 3) of a protein, small protein modules containing approximately 50 amino acid residues found in a great variety of intracellular or membrane-associated proteins. [GOC:go_curators, Pfam:PF00018] |
| syntaxin binding | molecular function | Binding to a syntaxin, a SNAP receptor involved in the docking of synaptic vesicles at the presynaptic zone of a synapse. [ISBN:0198506732] |
| manganese ion binding | molecular function | Binding to a manganese ion (Mn). [GOC:ai] |
| neuropilin binding | molecular function | Binding to a member of the neuropilin family. [GOC:bf, PMID:23871893] |
| SH2 domain binding | molecular function | Binding to a SH2 domain (Src homology 2) of a protein, a protein domain of about 100 amino-acid residues and belonging to the alpha + beta domain class. [GOC:go_curators, Pfam:PF00017] |
| ephrin receptor binding | molecular function | Binding to an ephrin receptor. [GOC:ai] |
| actin filament binding | molecular function | Binding to an actin filament, also known as F-actin, a helical filamentous polymer of globular G-actin subunits. [ISBN:0198506732] |
| mitogen-activated protein kinase binding | molecular function | Binding to a mitogen-activated protein kinase. [GOC:ai] |
| proline-rich region binding | molecular function | Binding to a proline-rich region, i.e. a region that contains a high proportion of proline residues, in a protein. [GOC:mah] |
| delta-catenin binding | molecular function | Binding to the delta subunit of the catenin complex. [GOC:rph] |
| sequence-specific double-stranded DNA binding | molecular function | Binding to double-stranded DNA of a specific nucleotide composition, e.g. GC-rich DNA binding, or with a specific sequence motif or type of DNA, e.g. promotor binding or rDNA binding. [GOC:dos, GOC:sl] |
Located In
This protein is located in 15 target(s):
| Target | Category | Definition |
|---|
| ruffle | cellular component | Projection at the leading edge of a crawling cell; the protrusions are supported by a microfilament meshwork. [ISBN:0124325653] |
| nucleus | cellular component | A membrane-bounded organelle of eukaryotic cells in which chromosomes are housed and replicated. In most cells, the nucleus contains all of the cell's chromosomes except the organellar chromosomes, and is the site of RNA synthesis and processing. In some species, or in specialized cell types, RNA metabolism or DNA replication may be absent. [GOC:go_curators] |
| nucleoplasm | cellular component | That part of the nuclear content other than the chromosomes or the nucleolus. [GOC:ma, ISBN:0124325653] |
| nucleolus | cellular component | A small, dense body one or more of which are present in the nucleus of eukaryotic cells. It is rich in RNA and protein, is not bounded by a limiting membrane, and is not seen during mitosis. Its prime function is the transcription of the nucleolar DNA into 45S ribosomal-precursor RNA, the processing of this RNA into 5.8S, 18S, and 28S components of ribosomal RNA, and the association of these components with 5S RNA and proteins synthesized outside the nucleolus. This association results in the formation of ribonucleoprotein precursors; these pass into the cytoplasm and mature into the 40S and 60S subunits of the ribosome. [ISBN:0198506732] |
| cytoplasm | cellular component | The contents of a cell excluding the plasma membrane and nucleus, but including other subcellular structures. [ISBN:0198547684] |
| mitochondrion | cellular component | A semiautonomous, self replicating organelle that occurs in varying numbers, shapes, and sizes in the cytoplasm of virtually all eukaryotic cells. It is notably the site of tissue respiration. [GOC:giardia, ISBN:0198506732] |
| 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] |
| actin cytoskeleton | cellular component | The part of the cytoskeleton (the internal framework of a cell) composed of actin and associated proteins. Includes actin cytoskeleton-associated complexes. [GOC:jl, ISBN:0395825172, ISBN:0815316194] |
| nuclear body | cellular component | Extra-nucleolar nuclear domains usually visualized by confocal microscopy and fluorescent antibodies to specific proteins. [GOC:ma, PMID:10330182] |
| 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] |
| growth cone | cellular component | The migrating motile tip of a growing neuron projection, where actin accumulates, and the actin cytoskeleton is the most dynamic. [GOC:aruk, GOC:bc, ISBN:0815316194, PMID:10082468] |
| nuclear membrane | cellular component | Either of the lipid bilayers that surround the nucleus and form the nuclear envelope; excludes the intermembrane space. [GOC:mah, GOC:pz] |
| 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] |
| perinuclear region of cytoplasm | cellular component | Cytoplasm situated near, or occurring around, the nucleus. [GOC:jid] |
| postsynapse | cellular component | The part of a synapse that is part of the post-synaptic cell. [GOC:dos] |
Active In
This protein is active in 1 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] |
Part Of
This protein is part of 1 target(s):
| Target | Category | Definition |
|---|
| protein-containing complex | cellular component | A stable assembly of two or more macromolecules, i.e. proteins, nucleic acids, carbohydrates or lipids, in which at least one component is a protein and the constituent parts function together. [GOC:dos, GOC:mah] |
Involved In
This protein is involved in 112 target(s):
| Target | Category | Definition |
|---|
| mitotic cell cycle | biological process | Progression through the phases of the mitotic cell cycle, the most common eukaryotic cell cycle, which canonically comprises four successive phases called G1, S, G2, and M and includes replication of the genome and the subsequent segregation of chromosomes into daughter cells. In some variant cell cycles nuclear replication or nuclear division may not be followed by cell division, or G1 and G2 phases may be absent. [GOC:mah, ISBN:0815316194, Reactome:69278] |
| neural tube closure | biological process | The last step in the formation of the neural tube, where the paired neural folds are brought together and fuse at the dorsal midline. [GOC:dph, ISBN:0878932437] |
| B-1 B cell homeostasis | biological process | The process of regulating the proliferation and elimination of B cells of the B-1 subset such that the total number of B-1 B cells within a whole or part of an organism is stable over time in the absence of an outside stimulus. B-1 B cells are a distinct subset of B cells characterized as being CD5 positive, found predominantly in the peritoneum, pleural cavities, and spleen, and enriched for self-reactivity. [GOC:add, ISBN:0781735149] |
| positive regulation of protein phosphorylation | biological process | Any process that activates or increases the frequency, rate or extent of addition of phosphate groups to amino acids within a protein. [GOC:hjd] |
| B cell proliferation involved in immune response | biological process | The expansion of a B cell population by cell division following B cell activation during an immune response. [GOC:jal] |
| transitional one stage B cell differentiation | biological process | The process in which immature B cells from the bone marrow acquire the specialized features of T1 stage B cells in the spleen. T1 stage B cells do not express either CD23 or CD21. [GOC:jal, ISBN:0781735149] |
| mismatch repair | biological process | A system for the correction of errors in which an incorrect base, which cannot form hydrogen bonds with the corresponding base in the parent strand, is incorporated into the daughter strand. The mismatch repair system promotes genomic fidelity by repairing base-base mismatches, insertion-deletion loops and heterologies generated during DNA replication and recombination. [ISBN:0198506732, PMID:11687886] |
| regulation of DNA-templated transcription | biological process | Any process that modulates the frequency, rate or extent of cellular DNA-templated transcription. [GOC:go_curators, GOC:txnOH] |
| autophagy | biological process | The cellular catabolic process in which cells digest cellular materials, such as organelles and other macromolecular constituents, or non-self materials such as intracellular pathogens. Autophagy serves to provide essential nutrients under conditions of cellular stress; or can remodel intracellular structures during cell differentiation. [GOC:autophagy, ISBN:0198547684, PMID:11099404, PMID:29455577, PMID:9412464] |
| DNA damage response | 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 indicating damage to its DNA from environmental insults or errors during metabolism. [GOC:go_curators] |
| integrin-mediated signaling pathway | biological process | The series of molecular signals initiated by an extracellular ligand binding to an integrin on the surface of a target cell, and ending with the regulation of a downstream cellular process, e.g. transcription. [GOC:mah, GOC:signaling] |
| canonical NF-kappaB signal transduction | biological process | An intracellular signaling cassette characterized by the I-kappaB-kinase (IKK)-dependent activation of NF-kappaB, also known as the canonical NF-kappaB signaling cascade. The cascade begins with activation of a trimeric IKK complex (consisting of catalytic kinase subunits IKKalpha and/or IKKbeta, and the regulatory scaffold protein NEMO) and ends with the regulation of transcription of target genes by NF-kappaB. In a resting state, NF-kappaB dimers are bound to I-kappaB proteins, sequestering NF-kappaB in the cytoplasm. Phosphorylation of I-kappaB targets I-kappaB for ubiquitination and proteasomal degradation, thus releasing the NF-kappaB dimers, which can translocate to the nucleus to bind DNA and regulate transcription. The canonical NF-kappaB pathway is mainly stimulated by proinflammatory cytokines such as IL-1beta, tumor necrosis factor (TNF)-alpha, antigen ligands, and toll-like receptors (TLRs). [GOC:bf, PMID:12773372, PMID:34659217] |
| associative learning | biological process | Learning by associating a stimulus (the cause) with a particular outcome (the effect). [ISBN:0582227089] |
| intrinsic apoptotic signaling pathway in response to DNA damage | biological process | The series of molecular signals in which an intracellular signal is conveyed to trigger the apoptotic death of a cell. The pathway is induced by the detection of DNA damage, and ends when the execution phase of apoptosis is triggered. [GOC:go_curators, GOC:mtg_apoptosis] |
| 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] |
| post-embryonic development | biological process | The process whose specific outcome is the progression of the organism over time, from the completion of embryonic development to the mature structure. See embryonic development. [GOC:go_curators] |
| regulation of autophagy | biological process | Any process that modulates the frequency, rate or extent of autophagy. Autophagy is the process in which cells digest parts of their own cytoplasm. [GOC:dph, GOC:tb] |
| positive regulation of endothelial cell migration | biological process | Any process that increases the rate, frequency, or extent of the orderly movement of an endothelial cell into the extracellular matrix to form an endothelium. [GOC:BHF, GOC:dph, GOC:tb] |
| peptidyl-tyrosine phosphorylation | biological process | The phosphorylation of peptidyl-tyrosine to form peptidyl-O4'-phospho-L-tyrosine. [RESID:AA0039] |
| cerebellum morphogenesis | biological process | The process in which the anatomical structure of the cerebellum is generated and organized. The cerebellum is the portion of the brain in the back of the head between the cerebrum and the pons. The cerebellum controls balance for walking and standing, modulates the force and range of movement and is involved in the learning of motor skills. [GO_REF:0000021, GOC:cls, GOC:dgh, GOC:dph, GOC:jid, ISBN:0838580343] |
| negative regulation of cell-cell adhesion | biological process | Any process that stops, prevents or reduces the rate or extent of cell adhesion to another cell. [GOC:isa_complete] |
| microspike assembly | biological process | Formation of a microspike, a dynamic, actin-rich projection extending from the surface of a migrating animal cell. [ISBN:0815316194, PMID:11429692, PMID:12153987, PMID:19095735] |
| actin cytoskeleton organization | biological process | A process that is carried out at the cellular level which results in the assembly, arrangement of constituent parts, or disassembly of cytoskeletal structures comprising actin filaments and their associated proteins. [GOC:dph, GOC:jl, GOC:mah] |
| actin filament polymerization | biological process | Assembly of actin filaments by the addition of actin monomers to a filament. [GOC:mah] |
| regulation of endocytosis | biological process | Any process that modulates the frequency, rate or extent of endocytosis. [GOC:go_curators] |
| 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] |
| neuron differentiation | biological process | The process in which a relatively unspecialized cell acquires specialized features of a neuron. [GOC:mah] |
| BMP signaling pathway | biological process | The series of molecular signals initiated by the binding of a member of the BMP (bone morphogenetic protein) family to a receptor on the surface of a target cell, and ending with the regulation of a downstream cellular process, e.g. transcription. [GOC:signaling, ISBN:0878932437, PMID:17428827] |
| negative regulation of BMP signaling pathway | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of the BMP signaling pathway. [GOC:go_curators] |
| regulation of axon extension | biological process | Any process that modulates the rate, direction or extent of axon extension. [GOC:go_curators] |
| regulation of microtubule polymerization | biological process | Any process that modulates the frequency, rate or extent of microtubule polymerization. [GOC:mah] |
| regulation of Cdc42 protein signal transduction | biological process | Any process that modulates the frequency, rate or extent of Cdc42 protein signal transduction. [GOC:mah] |
| positive regulation of type II interferon production | biological process | Any process that activates or increases the frequency, rate, or extent of interferon-gamma production. Interferon-gamma is also known as type II interferon. [GOC:add, GOC:mah, PMID:15546383] |
| positive regulation of interleukin-2 production | biological process | Any process that activates or increases the frequency, rate, or extent of interleukin-2 production. [GOC:mah] |
| regulation of actin cytoskeleton organization | biological process | Any process that modulates the frequency, rate or extent of the formation, arrangement of constituent parts, or disassembly of cytoskeletal structures comprising actin filaments and their associated proteins. [GOC:mah] |
| positive regulation of osteoblast proliferation | biological process | Any process that activates or increases the rate or extent of osteoblast proliferation. [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] |
| cellular response to oxidative stress | 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 oxidative stress, a state often resulting from exposure to high levels of reactive oxygen species, e.g. superoxide anions, hydrogen peroxide (H2O2), and hydroxyl radicals. [GOC:mah] |
| response to endoplasmic reticulum stress | 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 stress acting at the endoplasmic reticulum. ER stress usually results from the accumulation of unfolded or misfolded proteins in the ER lumen. [GOC:cjm, GOC:mah] |
| platelet-derived growth factor receptor-beta signaling pathway | biological process | The series of molecular signals initiated by the binding of a ligand to a beta-type platelet-derived growth factor receptor (PDGFbeta) on the surface of a signal-receiving cell, and ending with the regulation of a downstream cellular process, e.g. transcription. [GOC:bf, GOC:signaling, GOC:yaf, PMID:10372961] |
| protein modification process | biological process | The covalent alteration of one or more amino acids occurring in proteins, peptides and nascent polypeptides (co-translational, post-translational modifications). Includes the modification of charged tRNAs that are destined to occur in a protein (pre-translation modification). [GOC:bf, GOC:jl] |
| peptidyl-tyrosine autophosphorylation | biological process | The phosphorylation by a protein of one or more of its own tyrosine amino acid residues, or a tyrosine residue on an identical protein. [PMID:10037737, PMID:10068444, PMID:10940390] |
| Fc-gamma receptor signaling pathway involved in phagocytosis | biological process | An Fc-gamma receptor signaling pathway that contributes to the endocytic engulfment of external particulate material by phagocytes. [GOC:phg, PMID:12488490, PMID:15466916] |
| neuropilin signaling pathway | biological process | The series of molecular signals initiated by an extracellular ligand binding to a neuropilin protein on the surface of a target cell, and ending with the regulation of a downstream cellular process, e.g. transcription. [GOC:BHF, PMID:12852851] |
| signal transduction in response to DNA damage | biological process | A cascade of processes induced by the detection of DNA damage within a cell. [GOC:go_curators] |
| positive regulation of apoptotic process | biological process | Any process that activates or increases the frequency, rate or extent of cell death by apoptotic process. [GOC:jl, GOC:mtg_apoptosis] |
| positive regulation of canonical NF-kappaB signal transduction | biological process | Any process that activates or increases the frequency, rate or extent of a canonical NF-kappaB signaling cascade. [GOC:jl] |
| positive regulation of neuron apoptotic process | biological process | Any process that activates or increases the frequency, rate or extent of cell death of neurons by apoptotic process. [GOC:go_curators, GOC:mtg_apoptosis] |
| endothelial cell migration | biological process | The orderly movement of an endothelial cell into the extracellular matrix to form an endothelium. [GOC:go_curators] |
| regulation of T cell differentiation | biological process | Any process that modulates the frequency, rate or extent of T cell differentiation. [GOC:go_curators] |
| positive regulation of vasoconstriction | biological process | Any process that activates or increases the frequency, rate or extent of vasoconstriction. [GOC:go_curators] |
| negative regulation of mitotic cell cycle | biological process | Any process that stops, prevents or reduces the rate or extent of progression through the mitotic cell cycle. [GOC:dph, GOC:go_curators, GOC:tb] |
| positive regulation of mitotic cell cycle | biological process | Any process that activates or increases the rate or extent of progression through the mitotic cell cycle. [GOC:dph, GOC:go_curators, GOC:tb] |
| positive regulation of transcription by RNA polymerase II | biological process | Any process that activates or increases the frequency, rate or extent of transcription from an RNA polymerase II promoter. [GOC:go_curators, GOC:txnOH] |
| alpha-beta T cell differentiation | biological process | The process in which a precursor cell type acquires the specialized features of an alpha-beta T cell. An alpha-beta T cell is a T cell that expresses an alpha-beta T cell receptor complex. [CL:0000789, GOC:ai] |
| protein autophosphorylation | biological process | The phosphorylation by a protein of one or more of its own amino acid residues (cis-autophosphorylation), or residues on an identical protein (trans-autophosphorylation). [ISBN:0198506732] |
| positive regulation of fibroblast proliferation | biological process | Any process that activates or increases the frequency, rate or extent of multiplication or reproduction of fibroblast cells. [GOC:jid] |
| spleen development | biological process | The process whose specific outcome is the progression of the spleen over time, from its formation to the mature structure. The spleen is a large vascular lymphatic organ composed of white and red pulp, involved both in hemopoietic and immune system functions. [GOC:add, ISBN:0781735149] |
| 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 peptidyl-tyrosine phosphorylation | biological process | Any process that activates or increases the frequency, rate or extent of the phosphorylation of peptidyl-tyrosine. [GOC:ai] |
| activated T cell proliferation | biological process | The expansion of a T cell population following activation by an antigenic stimulus. [GOC:add, GOC:dph] |
| 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] |
| B cell receptor signaling pathway | biological process | The series of molecular signals initiated by the cross-linking of an antigen receptor on a B cell. [GOC:add] |
| neuromuscular process controlling balance | biological process | Any process that an organism uses to control its balance, the orientation of the organism (or the head of the organism) in relation to the source of gravity. In humans and animals, balance is perceived through visual cues, the labyrinth system of the inner ears and information from skin pressure receptors and muscle and joint receptors. [GOC:ai, GOC:dph] |
| positive regulation of release of sequestered calcium ion into cytosol | biological process | Any process that activates or increases the frequency, rate or extent of the release into the cytosolic compartment of calcium ions sequestered in the endoplasmic reticulum or mitochondria. [GOC:ai] |
| positive regulation of oxidoreductase activity | biological process | Any process that activates or increases the frequency, rate or extent of oxidoreductase activity, the catalysis of an oxidation-reduction (redox) reaction, a reversible chemical reaction in which the oxidation state of an atom or atoms within a molecule is altered. [GOC:ai] |
| neuron apoptotic process | biological process | Any apoptotic process in a neuron, the basic cellular unit of nervous tissue. Each neuron consists of a body, an axon, and dendrites. Their purpose is to receive, conduct, and transmit impulses in the nervous system. [CL:0000540, GOC:mtg_apoptosis] |
| negative regulation of ubiquitin-protein transferase activity | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of ubiquitin transferase activity. [GOC:ai, GOC:tb] |
| myoblast proliferation | biological process | The multiplication or reproduction of myoblasts, resulting in the expansion of a myoblast cell population. A myoblast is a mononucleate cell type that, by fusion with other myoblasts, gives rise to the myotubes that eventually develop into skeletal muscle fibers. [CL:0000056, GOC:ai, GOC:mtg_muscle] |
| 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] |
| establishment of localization in cell | biological process | Any process, occuring in a cell, that localizes a substance or cellular component. This may occur via movement, tethering or selective degradation. [GOC:ai, GOC:dos, GOC:dph, GOC:tb] |
| regulation of cell cycle | biological process | Any process that modulates the rate or extent of progression through the cell cycle. [GOC:ai, GOC:dph, GOC:tb] |
| mitochondrial depolarization | biological process | The process in which the potential difference across the mitochondrial membrane is reduced from its steady state level. [Wikipedia:Depolarization, Wikipedia:Mitochondrion] |
| positive regulation of focal adhesion assembly | biological process | Any process that activates or increases the frequency, rate or extent of focal adhesion assembly, the establishment and maturation of focal adhesions. [GOC:ai] |
| Bergmann glial cell differentiation | biological process | The process in which neuroepithelial cells of the neural tube give rise to Brgmann glial cells, specialized bipotential progenitors cells of the cerebellum. Differentiation includes the processes involved in commitment of a cell to a specific fate. [GOC:dph, PMID:10375501] |
| cardiac muscle cell proliferation | biological process | The expansion of a cardiac muscle cell population by cell division. [GOC:dph, GOC:rph, PMID:11161571] |
| neuroepithelial cell differentiation | biological process | The process in which epiblast cells acquire specialized features of neuroepithelial cells. [GOC:dph, GOC:tb] |
| cellular response to hydrogen peroxide | 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 hydrogen peroxide (H2O2) stimulus. [CHEBI:16240, GOC:mah] |
| 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] |
| negative regulation of ERK1 and ERK2 cascade | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of signal transduction mediated by the ERK1 and ERK2 cascade. [GOC:add, ISBN:0121245462, ISBN:0896039986] |
| 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] |
| DNA conformation change | biological process | A cellular process that results in a change in the spatial configuration of a DNA molecule. A conformation change can bend DNA, or alter the, twist, writhe, or linking number of a DNA molecule. [GOC:mah] |
| cellular response to lipopolysaccharide | biological process | Any process that results in a change in state or activity of a cell (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a lipopolysaccharide stimulus; lipopolysaccharide is a major component of the cell wall of gram-negative bacteria. [GOC:mah] |
| cellular response to transforming growth factor beta 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 transforming growth factor beta stimulus. [GOC:ecd, PMID:15451575] |
| response to epinephrine | biological process | Any process that results in a change in state or activity of a cell or an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of an epinephrine stimulus. Epinephrine is a catecholamine that has the formula C9H13NO3; it is secreted by the adrenal medulla to act as a hormone, and released by certain neurons to act as a neurotransmitter active in the central nervous system. [GOC:BHF, GOC:mah] |
| negative regulation of protein serine/threonine kinase activity | biological process | Any process that decreases the rate, frequency, or extent of protein serine/threonine kinase activity. [GOC:BHF, GOC:mah] |
| positive regulation of cell migration involved in sprouting angiogenesis | biological process | Any process that increases the frequency, rate or extent of cell migration involved in sprouting angiogenesis. Cell migration involved in sprouting angiogenesis is the orderly movement of endothelial cells into the extracellular matrix in order to form new blood vessels contributing to the process of sprouting angiogenesis. [GOC:BHF, GOC:dph, GOC:rl, GOC:tb] |
| cellular senescence | biological process | A cell aging process stimulated in response to cellular stress, whereby normal cells lose the ability to divide through irreversible cell cycle arrest. [GOC:BHF, PMID:28682291] |
| cell-cell adhesion | biological process | The attachment of one cell to another cell via adhesion molecules. [GOC:dos] |
| positive regulation of dendrite development | biological process | Any process that activates or increases the frequency, rate or extent of dendrite development. [GOC:TermGenie] |
| 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] |
| negative regulation of long-term synaptic potentiation | biological process | Any process that stops, prevents or reduces the frequency, rate or extent of long-term synaptic potentiation. [GOC:BHF, GOC:TermGenie] |
| regulation of hematopoietic stem cell differentiation | biological process | Any process that modulates the frequency, rate or extent of hematopoietic stem cell differentiation. [GOC:TermGenie, PMID:23403623] |
| positive regulation of extracellular matrix organization | biological process | Any process that activates or increases the frequency, rate or extent of extracellular matrix organization. [GO_REF:0000058, GOC:BHF, GOC:rl, GOC:TermGenie, PMID:22357537] |
| podocyte apoptotic process | biological process | Any apoptotic process in a glomerular visceral epithelial cell. [GO_REF:0000085, GOC:TermGenie, PMID:23515840] |
| cellular response to dopamine | 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 dopamine stimulus. [GO_REF:0000071, GOC:mr, GOC:TermGenie, PMID:11118945] |
| positive regulation of establishment of T cell polarity | biological process | Any process that activates or increases the frequency, rate or extent of establishment of T cell polarity. [GO_REF:0000058, GOC:als, GOC:TermGenie, PMID:23575248] |
| DN4 thymocyte differentiation | biological process | The process in which a relatively unspecialized cell acquires the specialized features of a DN4 thymocyte. A DN4 thymocyte is a CD4-,CD8- thymocyte that is also CD44-,CD25-. [GO_REF:0000086, GOC:dph, GOC:TermGenie, PMID:25398325] |
| protein localization to cytoplasmic microtubule plus-end | biological process | A process in which a protein is transported to, or maintained in, a location at a cytoplasmic microtubule plus-end. [GO_REF:0000087, GOC:TermGenie, PMID:15772152] |
| positive regulation of microtubule binding | biological process | Any process that activates or increases the frequency, rate or extent of microtubule binding. [GO_REF:0000059, GOC:als, GOC:TermGenie, PMID:24520051] |
| positive regulation of actin filament binding | biological process | Any process that activates or increases the frequency, rate or extent of actin filament binding. [GO_REF:0000059, GOC:als, GOC:TermGenie, PMID:24520051] |
| regulation of modification of synaptic structure | biological process | Any process that modulates the frequency, rate or extent of modification of synaptic structure. [GO_REF:0000058, GOC:TermGenie, PMID:25164660] |
| positive regulation of blood vessel branching | biological process | Any process that activates or increases the frequency, rate or extent of blood vessel branching. [GO_REF:0000058, GOC:BHF, GOC:BHF_telomere, GOC:nc, GOC:TermGenie, PMID:23201774] |
| activation of protein kinase C activity | biological process | Any process that initiates the activity of the inactive enzyme protein kinase C. [PMID:3156004] |
| negative regulation of double-strand break repair via homologous recombination | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of double-strand break repair via homologous recombination. [GOC:vw] |
| positive regulation of Wnt signaling pathway, planar cell polarity pathway | biological process | Any process that activates or increases the frequency, rate or extent of Wnt signaling pathway, planar cell polarity pathway. [GOC:BHF] |
| regulation of cell motility | biological process | Any process that modulates the frequency, rate or extent of cell motility. [GOC:mah] |
| 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] |
| positive regulation of T cell migration | biological process | Any process that activates or increases the frequency, rate or extent of T cell migration. [GOC:mah] |
| negative regulation of cellular senescence | biological process | Any process that stops, prevents or reduces the frequency, rate or extent of cellular senescence. [GOC:BHF] |
| 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] |
| protein phosphorylation | biological process | The process of introducing a phosphate group on to a protein. [GOC:hb] |