Proteins > Receptor-type tyrosine-protein kinase FLT3
Page last updated: 2024-08-07 16:35:43
Receptor-type tyrosine-protein kinase FLT3
A receptor-type tyrosine-protein kinase FLT3 that is encoded in the genome of human. [PRO:WCB, UniProtKB:P36888]
Synonyms
EC 2.7.10.1;
FL cytokine receptor;
Fetal liver kinase-2;
FLK-2;
Fms-like tyrosine kinase 3;
FLT-3;
Stem cell tyrosine kinase 1;
STK-1
Research
Bioassay Publications (173)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 32 (18.50) | 29.6817 |
| 2010's | 105 (60.69) | 24.3611 |
| 2020's | 36 (20.81) | 2.80 |
Compounds (305)
Drugs with Inhibition Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| ag 1295 | Homo sapiens (human) | IC50 | 1.1000 | 2 | 2 |
| indirubin-3'-monoxime | Homo sapiens (human) | IC50 | 0.0785 | 4 | 4 |
| niclosamide | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
| imatinib | Homo sapiens (human) | IC50 | 15.0655 | 2 | 2 |
| vorinostat | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| indirubin | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| staurosporine | Homo sapiens (human) | IC50 | 0.0014 | 23 | 23 |
| eupatorin | Homo sapiens (human) | IC50 | 1.1000 | 1 | 1 |
| aromadedrin | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| 5'-iodoindirubin | Homo sapiens (human) | IC50 | 4.7220 | 1 | 1 |
| lestaurtinib | Homo sapiens (human) | IC50 | 0.0039 | 6 | 6 |
| birb 796 | Homo sapiens (human) | IC50 | 30.0000 | 1 | 1 |
| salvigenin | Homo sapiens (human) | IC50 | 0.4733 | 3 | 3 |
| sorafenib | Homo sapiens (human) | GI50 | 3.1330 | 3 | 3 |
| sorafenib | Homo sapiens (human) | IC50 | 0.0348 | 21 | 21 |
| 5-iodoindirubin-3'-monoxime | Homo sapiens (human) | IC50 | 0.4180 | 1 | 1 |
| naringenin | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| taxifolin | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| eriodictyol | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| s 1033 | Homo sapiens (human) | IC50 | 9.5480 | 1 | 1 |
| ax 20017 | Homo sapiens (human) | IC50 | 1.3000 | 1 | 1 |
| 2-[[(3,4-dimethoxyphenyl)-oxomethyl]amino]-4,5,6,7-tetrahydro-1-benzothiophene-3-carboxamide | Homo sapiens (human) | IC50 | 1.4710 | 2 | 2 |
| tandutinib | Homo sapiens (human) | IC50 | 0.9345 | 15 | 15 |
| dasatinib | Homo sapiens (human) | IC50 | 25.7000 | 1 | 0 |
| gtp 14564 | Homo sapiens (human) | IC50 | 0.3000 | 1 | 1 |
| quercetin | Homo sapiens (human) | IC50 | 0.5900 | 1 | 1 |
| acacetin | Homo sapiens (human) | IC50 | 0.6967 | 3 | 3 |
| apigenin | Homo sapiens (human) | IC50 | 1.4500 | 1 | 1 |
| luteolin | Homo sapiens (human) | IC50 | 0.8300 | 1 | 1 |
| quercetin 3-o-glucopyranoside | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| kaempferol | Homo sapiens (human) | IC50 | 2.3200 | 1 | 1 |
| baicalein | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| chrysin | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| galangin | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| genkwanin | Homo sapiens (human) | IC50 | 1.7000 | 1 | 1 |
| hispidulin | Homo sapiens (human) | IC50 | 0.3533 | 3 | 3 |
| myricetin | Homo sapiens (human) | IC50 | 1.6900 | 1 | 1 |
| scutellarein | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| ellagic acid | Homo sapiens (human) | IC50 | 40.0000 | 1 | 1 |
| su 6656 | Homo sapiens (human) | IC50 | 8.7000 | 1 | 1 |
| 5,7-dihydroxy-6-methoxy-2-phenylchromen-4-one | Homo sapiens (human) | IC50 | 1.4800 | 1 | 1 |
| 5,7-dihydroxy-4',6-dimethoxyflavone | Homo sapiens (human) | IC50 | 0.7033 | 3 | 3 |
| semaxinib | Homo sapiens (human) | IC50 | 0.1600 | 1 | 1 |
| su 11248 | Homo sapiens (human) | IC50 | 0.0581 | 24 | 24 |
| palbociclib | Homo sapiens (human) | IC50 | 5.4933 | 3 | 3 |
| d-64406 | Homo sapiens (human) | IC50 | 0.5700 | 1 | 1 |
| vx680 | Homo sapiens (human) | IC50 | 0.0300 | 1 | 1 |
| vx680 | Homo sapiens (human) | Ki | 0.0300 | 5 | 5 |
| cyc 116 | Homo sapiens (human) | IC50 | 0.0566 | 2 | 2 |
| cyc 116 | Homo sapiens (human) | Ki | 0.0440 | 1 | 1 |
| a 419259 | Homo sapiens (human) | IC50 | 0.0240 | 1 | 1 |
| gdp 366 | Homo sapiens (human) | IC50 | 0.0020 | 1 | 1 |
| spc-839 | Homo sapiens (human) | IC50 | 0.6180 | 1 | 1 |
| midostaurin | Homo sapiens (human) | GI50 | 0.1643 | 3 | 3 |
| midostaurin | Homo sapiens (human) | IC50 | 0.1663 | 7 | 7 |
| ct52923 | Homo sapiens (human) | IC50 | 14.9000 | 1 | 1 |
| cp 31398 | Homo sapiens (human) | IC50 | 3.8100 | 1 | 1 |
| pik 75 | Homo sapiens (human) | IC50 | 0.0052 | 1 | 1 |
| crenolanib | Homo sapiens (human) | IC50 | 0.0089 | 10 | 10 |
| l 783277 | Homo sapiens (human) | GI50 | 0.2700 | 1 | 1 |
| l 783277 | Homo sapiens (human) | IC50 | 0.0225 | 5 | 5 |
| PDGF receptor tyrosine kinase inhibitor III | Homo sapiens (human) | IC50 | 0.2300 | 1 | 1 |
| regorafenib | Homo sapiens (human) | IC50 | 0.0820 | 1 | 1 |
| nvp-ast487 | Homo sapiens (human) | IC50 | 0.0050 | 1 | 1 |
| kw 2449 | Homo sapiens (human) | IC50 | 0.0066 | 1 | 1 |
| danusertib | Homo sapiens (human) | IC50 | 0.6690 | 1 | 1 |
| nvp-aew541 | Homo sapiens (human) | IC50 | 1.4000 | 1 | 1 |
| abt 869 | Homo sapiens (human) | IC50 | 0.0126 | 7 | 7 |
| azd2932 | Homo sapiens (human) | IC50 | 0.0070 | 3 | 3 |
| dorsomorphin | Homo sapiens (human) | IC50 | 0.0010 | 1 | 1 |
| gw 2580 | Homo sapiens (human) | IC50 | 13.0000 | 1 | 1 |
| crizotinib | Homo sapiens (human) | IC50 | 1.0000 | 1 | 1 |
| 4-[2-(2-chloro-4-fluoroanilino)-5-methyl-4-pyrimidinyl]-N-[(1S)-1-(3-chlorophenyl)-2-hydroxyethyl]-1H-pyrrole-2-carboxamide | Homo sapiens (human) | Ki | 1.4000 | 1 | 1 |
| 4-cyano-N-[4-(4-methyl-1-piperazinyl)-2-(4-methyl-1-piperidinyl)phenyl]-1H-pyrrole-2-carboxamide | Homo sapiens (human) | IC50 | 0.0094 | 2 | 2 |
| jnj 28312141 | Homo sapiens (human) | IC50 | 0.0255 | 2 | 2 |
| azd 1152-hqpa | Homo sapiens (human) | IC50 | 0.1000 | 1 | 1 |
| nvp-tae684 | Homo sapiens (human) | IC50 | 0.7385 | 6 | 6 |
| enmd 2076 | Homo sapiens (human) | IC50 | 0.0022 | 3 | 3 |
| tg101209 | Homo sapiens (human) | IC50 | 0.0250 | 1 | 1 |
| fedratinib | Homo sapiens (human) | IC50 | 0.0200 | 2 | 2 |
| 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) | IC50 | 0.0397 | 3 | 3 |
| cx 4945 | Homo sapiens (human) | IC50 | 0.0417 | 3 | 2 |
| cudc 101 | Homo sapiens (human) | IC50 | 1.5000 | 1 | 1 |
| amg 458 | Homo sapiens (human) | IC50 | 0.3910 | 1 | 1 |
| bms 777607 | Homo sapiens (human) | IC50 | 0.0167 | 3 | 2 |
| sgi 1776 | Homo sapiens (human) | IC50 | 0.0382 | 4 | 4 |
| pci 32765 | Homo sapiens (human) | GI50 | 0.1200 | 1 | 1 |
| pci 32765 | Homo sapiens (human) | IC50 | 0.5365 | 2 | 2 |
| ponatinib | Homo sapiens (human) | IC50 | 0.0086 | 3 | 3 |
| quizartinib | Homo sapiens (human) | GI50 | 0.2194 | 12 | 12 |
| quizartinib | Homo sapiens (human) | IC50 | 0.1024 | 45 | 45 |
| dcc-2036 | Homo sapiens (human) | IC50 | 0.0020 | 1 | 1 |
| cabozantinib | Homo sapiens (human) | IC50 | 0.8877 | 9 | 9 |
| entrectinib | Homo sapiens (human) | IC50 | 0.1640 | 1 | 1 |
| pexidartinib | Homo sapiens (human) | IC50 | 0.0270 | 7 | 7 |
| gsk 1363089 | Homo sapiens (human) | IC50 | 0.1806 | 10 | 17 |
| mk 2461 | Homo sapiens (human) | IC50 | 0.0220 | 1 | 1 |
| pha 793887 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| nps-1034 | Homo sapiens (human) | IC50 | 0.0631 | 1 | 1 |
| sb 1518 | Homo sapiens (human) | IC50 | 0.0183 | 4 | 4 |
| dinaciclib | Homo sapiens (human) | IC50 | 2.0000 | 1 | 1 |
| nms p937 | Homo sapiens (human) | IC50 | 0.5100 | 2 | 1 |
| gilteritinib | Homo sapiens (human) | IC50 | 1.8336 | 6 | 6 |
| gilteritinib | Homo sapiens (human) | Ki | 0.0060 | 2 | 2 |
| glpg0634 | Homo sapiens (human) | IC50 | 0.3380 | 2 | 1 |
| nms-p118 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| bix 02565 | Homo sapiens (human) | IC50 | 0.7140 | 2 | 1 |
| urmc-099 | Homo sapiens (human) | IC50 | 0.2820 | 2 | 2 |
| on123300 | Homo sapiens (human) | IC50 | 0.0122 | 1 | 1 |
| cep-28122 | Homo sapiens (human) | IC50 | 0.0880 | 1 | 1 |
| ceritinib | Homo sapiens (human) | IC50 | 1.0965 | 3 | 3 |
| vx-970 | Homo sapiens (human) | Ki | 0.0740 | 2 | 2 |
| amg 925 | Homo sapiens (human) | IC50 | 0.0020 | 4 | 4 |
| pf-543 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| vx-787 | Homo sapiens (human) | Ki | 4.0000 | 1 | 1 |
| erdafitinib | Homo sapiens (human) | IC50 | 10.0000 | 2 | 0 |
| unc1062 | Homo sapiens (human) | IC50 | 0.0030 | 1 | 1 |
| sar131675 | Homo sapiens (human) | GI50 | 18.0000 | 1 | 1 |
| sar131675 | Homo sapiens (human) | IC50 | 0.2900 | 1 | 1 |
| unc2025 | Homo sapiens (human) | IC50 | 0.0050 | 3 | 3 |
| at 9283 | Homo sapiens (human) | IC50 | 0.0100 | 2 | 2 |
| chir 258 | Homo sapiens (human) | IC50 | 0.0020 | 2 | 2 |
| nintedanib | Homo sapiens (human) | IC50 | 0.0260 | 2 | 2 |
| pf-477736 | Homo sapiens (human) | IC50 | 0.0250 | 1 | 0 |
| nms-e973 | Homo sapiens (human) | IC50 | 0.0100 | 1 | 1 |
Drugs with Activation Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| fasudil | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| 4-(4'-hydroxyphenyl)-amino-6,7-dimethoxyquinazoline | Homo sapiens (human) | Kd | 1.3130 | 1 | 1 |
| sb 202190 | Homo sapiens (human) | Kd | 10.0000 | 5 | 5 |
| imatinib | Homo sapiens (human) | Kd | 11.1643 | 14 | 14 |
| triciribine phosphate | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| staurosporine | Homo sapiens (human) | Kd | 0.0023 | 14 | 14 |
| picropodophyllin | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| gefitinib | Homo sapiens (human) | Kd | 5.7538 | 13 | 13 |
| lestaurtinib | Homo sapiens (human) | Kd | 0.0120 | 15 | 15 |
| perifosine | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| vatalanib | Homo sapiens (human) | Kd | 11.5385 | 13 | 13 |
| ruboxistaurin | Homo sapiens (human) | Kd | 2.7786 | 14 | 14 |
| canertinib | Homo sapiens (human) | Kd | 4.0115 | 13 | 13 |
| birb 796 | Homo sapiens (human) | Kd | 6.1377 | 13 | 13 |
| cyc 202 | Homo sapiens (human) | Kd | 13.3333 | 6 | 6 |
| sb 203580 | Homo sapiens (human) | Kd | 10.0000 | 12 | 12 |
| enzastaurin | Homo sapiens (human) | Kd | 3.0111 | 11 | 8 |
| erlotinib | Homo sapiens (human) | Kd | 4.3154 | 13 | 13 |
| lapatinib | Homo sapiens (human) | Kd | 11.5385 | 13 | 13 |
| sorafenib | Homo sapiens (human) | Kd | 0.1466 | 28 | 28 |
| pd 173955 | Homo sapiens (human) | Kd | 2.3262 | 8 | 8 |
| s 1033 | Homo sapiens (human) | Kd | 15.5556 | 9 | 9 |
| xl147 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| bms 387032 | Homo sapiens (human) | Kd | 10.0077 | 13 | 13 |
| sf 2370 | Homo sapiens (human) | Kd | 0.2270 | 1 | 1 |
| tandutinib | Homo sapiens (human) | Kd | 0.3439 | 20 | 20 |
| vx-745 | Homo sapiens (human) | Kd | 10.0000 | 12 | 12 |
| dasatinib | Homo sapiens (human) | Kd | 9.6846 | 13 | 13 |
| ha 1100 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| 7-epi-hydroxystaurosporine | Homo sapiens (human) | Kd | 0.0670 | 1 | 1 |
| zd 6474 | Homo sapiens (human) | Kd | 3.0836 | 14 | 14 |
| 4-(5-benzo(1,3)dioxol-5-yl-4-pyridin-2-yl-1h-imidazol-2-yl)benzamide | Homo sapiens (human) | Kd | 10.0000 | 5 | 5 |
| imd 0354 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| sirolimus | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| alvocidib | Homo sapiens (human) | Kd | 8.3538 | 13 | 13 |
| bosutinib | Homo sapiens (human) | Kd | 6.6000 | 8 | 8 |
| orantinib | Homo sapiens (human) | Kd | 0.0008 | 1 | 1 |
| su 11248 | Homo sapiens (human) | Kd | 0.0021 | 25 | 25 |
| palbociclib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| jnj-7706621 | Homo sapiens (human) | Kd | 1.0160 | 5 | 5 |
| vx680 | Homo sapiens (human) | Kd | 0.0540 | 17 | 17 |
| cyc 116 | Homo sapiens (human) | Kd | 0.2760 | 1 | 1 |
| everolimus | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| ekb 569 | Homo sapiens (human) | Kd | 9.6833 | 6 | 6 |
| axitinib | Homo sapiens (human) | Kd | 4.1904 | 8 | 8 |
| temsirolimus | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| pd 184352 | Homo sapiens (human) | Kd | 10.0000 | 7 | 7 |
| 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 | 0.8940 | 1 | 1 |
| bms345541 | Homo sapiens (human) | Kd | 10.0000 | 7 | 7 |
| lenvatinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| pd 0325901 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| midostaurin | Homo sapiens (human) | Kd | 0.0232 | 24 | 24 |
| 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 | 5.1914 | 7 | 7 |
| scio-469 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| cp 724714 | Homo sapiens (human) | Kd | 13.3333 | 6 | 6 |
| pi103 | Homo sapiens (human) | Kd | 8.8000 | 12 | 12 |
| hmn-214 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| tivozanib | Homo sapiens (human) | Kd | 30.0000 | 1 | 2 |
| hki 272 | Homo sapiens (human) | Kd | 9.3000 | 8 | 8 |
| tofacitinib | Homo sapiens (human) | Kd | 12.8571 | 13 | 14 |
| n-(6-chloro-7-methoxy-9h-beta-carbolin-8-yl)-2-methylnicotinamide | Homo sapiens (human) | Kd | 10.0000 | 7 | 7 |
| cediranib | Homo sapiens (human) | Kd | 11.5375 | 8 | 8 |
| masitinib | Homo sapiens (human) | Kd | 12.5000 | 8 | 8 |
| ly-2157299 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| pazopanib | Homo sapiens (human) | Kd | 2.7682 | 14 | 14 |
| azd 6244 | Homo sapiens (human) | Kd | 12.5000 | 8 | 8 |
| su 14813 | Homo sapiens (human) | Kd | 0.0067 | 13 | 13 |
| bibw 2992 | Homo sapiens (human) | Kd | 9.9250 | 8 | 8 |
| binimetinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 2 |
| sotrastaurin | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| aee 788 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| saracatinib | Homo sapiens (human) | Kd | 0.1400 | 1 | 1 |
| vx 702 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| crenolanib | Homo sapiens (human) | Kd | 0.0081 | 5 | 5 |
| tg100-115 | Homo sapiens (human) | Kd | 8.7555 | 8 | 8 |
| cc 401 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| bms 599626 | Homo sapiens (human) | Kd | 30.0000 | 1 | 2 |
| exel-7647 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| volasertib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| pha 665752 | Homo sapiens (human) | Kd | 0.8406 | 7 | 7 |
| azd 7762 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| regorafenib | Homo sapiens (human) | Kd | 0.5620 | 1 | 1 |
| 6-[[5-fluoro-2-(3,4,5-trimethoxyanilino)-4-pyrimidinyl]amino]-2,2-dimethyl-4H-pyrido[3,2-b][1,4]oxazin-3-one | Homo sapiens (human) | EC50 | 0.0100 | 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 | 0.0031 | 9 | 9 |
| brivanib | Homo sapiens (human) | Kd | 12.5000 | 8 | 8 |
| mp470 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| rgb 286638 | Homo sapiens (human) | Kd | 0.3230 | 1 | 1 |
| np 031112 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| at 7519 | Homo sapiens (human) | Kd | 12.5000 | 8 | 8 |
| bms-690514 | Homo sapiens (human) | Kd | 2.0110 | 1 | 1 |
| bi 2536 | Homo sapiens (human) | Kd | 11.6250 | 8 | 8 |
| inno-406 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| nvp-ast487 | Homo sapiens (human) | Kd | 0.0051 | 12 | 12 |
| kw 2449 | Homo sapiens (human) | Kd | 0.0214 | 9 | 9 |
| danusertib | Homo sapiens (human) | Kd | 1.4170 | 1 | 1 |
| abt 869 | Homo sapiens (human) | Kd | 0.0161 | 13 | 13 |
| 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 | 0.1325 | 2 | 2 |
| pf 00299804 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| ridaforolimus | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| ch 4987655 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| 6-(5-((cyclopropylamino)carbonyl)-3-fluoro-2-methylphenyl)-n-(2,2-dimethylprpyl)-3-pyridinecarboxamide | Homo sapiens (human) | Kd | 30.0000 | 1 | 2 |
| cc-930 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| gw 2580 | Homo sapiens (human) | Kd | 10.0000 | 12 | 12 |
| tak 285 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| idelalisib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| crizotinib | Homo sapiens (human) | Kd | 4.6312 | 8 | 8 |
| osi 906 | Homo sapiens (human) | Kd | 0.3080 | 1 | 1 |
| chir-265 | Homo sapiens (human) | Kd | 9.5023 | 13 | 13 |
| motesanib | Homo sapiens (human) | Kd | 5.1305 | 13 | 13 |
| fostamatinib | Homo sapiens (human) | Kd | 0.8430 | 1 | 1 |
| trametinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| mln8054 | Homo sapiens (human) | Kd | 11.5000 | 13 | 13 |
| pf-562,271 | Homo sapiens (human) | Kd | 1.3240 | 1 | 1 |
| GDC-0879 | Homo sapiens (human) | Kd | 10.0000 | 7 | 7 |
| jnj-26483327 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| ly2603618 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| tg100801 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| dactolisib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| bgt226 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| gsk 461364 | Homo sapiens (human) | Kd | 4.8875 | 8 | 8 |
| azd 1152-hqpa | Homo sapiens (human) | Kd | 0.1849 | 13 | 13 |
| nvp-tae684 | Homo sapiens (human) | EC50 | 0.5000 | 1 | 1 |
| nvp-tae684 | Homo sapiens (human) | Kd | 0.0123 | 8 | 8 |
| enmd 2076 | Homo sapiens (human) | Kd | 0.0080 | 1 | 1 |
| e 7050 | Homo sapiens (human) | Kd | 0.0040 | 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 | 0.5540 | 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 | 1.6850 | 1 | 1 |
| azd8330 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| pha 848125 | Homo sapiens (human) | Kd | 0.0540 | 1 | 1 |
| ro5126766 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| fedratinib | Homo sapiens (human) | Kd | 0.0965 | 8 | 8 |
| gsk690693 | Homo sapiens (human) | Kd | 12.5000 | 8 | 8 |
| 14-methyl-20-oxa-5,7,14,26-tetraazatetracyclo(19.3.1.1(2,6).1(8,12))heptacosa-1(25),2(26),3,5,8(27),9,11,16,21,23-decaene | Homo sapiens (human) | Kd | 0.4180 | 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 | 6.7137 | 8 | 8 |
| 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 | 4.1714 | 7 | 7 |
| mk 5108 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| cx 4945 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| cudc 101 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| arry-614 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| tak 593 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| mln 8237 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| sgx 523 | Homo sapiens (human) | Kd | 12.5000 | 8 | 8 |
| bms 754807 | Homo sapiens (human) | Kd | 1.7980 | 1 | 1 |
| bms 777607 | Homo sapiens (human) | Kd | 0.2280 | 1 | 1 |
| sgi 1776 | Homo sapiens (human) | Kd | 0.1430 | 1 | 1 |
| pci 32765 | Homo sapiens (human) | Kd | 1.5780 | 1 | 1 |
| ponatinib | Homo sapiens (human) | Kd | 0.0070 | 1 | 1 |
| amg 900 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| mk-1775 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| AMG-208 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| quizartinib | Homo sapiens (human) | Kd | 0.0362 | 28 | 28 |
| 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 | 0.8140 | 1 | 1 |
| cabozantinib | Homo sapiens (human) | Kd | 0.0530 | 1 | 1 |
| defactinib | Homo sapiens (human) | Kd | 0.3400 | 1 | 1 |
| ly2584702 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| incb-018424 | Homo sapiens (human) | Kd | 12.5000 | 8 | 8 |
| poziotinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| asp3026 | Homo sapiens (human) | Kd | 0.6270 | 1 | 1 |
| entrectinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| pexidartinib | Homo sapiens (human) | Kd | 0.0550 | 1 | 1 |
| cct 137690 | Homo sapiens (human) | Kd | 0.0012 | 1 | 1 |
| TAK-580 | Homo sapiens (human) | Kd | 30.0000 | 1 | 2 |
| 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 | 7.9143 | 7 | 7 |
| pf 3758309 | Homo sapiens (human) | Kd | 1.4430 | 1 | 1 |
| gdc 0980 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| azd2014 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| (5-(2,4-bis((3s)-3-methylmorpholin-4-yl)pyrido(2,3-d)pyrimidin-7-yl)-2-methoxyphenyl)methanol | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| plx4032 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| gsk 1363089 | Homo sapiens (human) | Kd | 0.0090 | 9 | 9 |
| 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 | 30.0000 | 1 | 1 |
| pki 587 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| n-(3-fluoro-4-((1-methyl-6-(1h-pyrazol-4-yl)-1h-indazol-5 yl)oxy)phenyl)-1-(4-fluorophenyl)-6-methyl-2-oxo-1,2-dihydropyridine-3-carboxamide | Homo sapiens (human) | Kd | 0.3090 | 1 | 1 |
| ribociclib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| mk-8033 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| blz 945 | Homo sapiens (human) | Kd | 8.7000 | 1 | 1 |
| pha 793887 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| sb 1518 | Homo sapiens (human) | Kd | 0.2280 | 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 | 0.0530 | 1 | 1 |
| jnj38877605 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| dinaciclib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| gilteritinib | Homo sapiens (human) | Kd | 0.0070 | 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 | 2 |
| 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 | 2 |
| cep-32496 | Homo sapiens (human) | Kd | 0.5500 | 1 | 1 |
| rociletinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| ceritinib | Homo sapiens (human) | Kd | 4.2550 | 1 | 1 |
| azd1208 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| vx-509 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| gs-9973 | Homo sapiens (human) | EC50 | 0.3270 | 1 | 1 |
| amg 925 | Homo sapiens (human) | Kd | 0.0027 | 9 | 9 |
| 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 | 0.0640 | 1 | 1 |
| otssp167 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| chir 258 | Homo sapiens (human) | Kd | 0.0038 | 13 | 13 |
| osi 027 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| nintedanib | Homo sapiens (human) | Kd | 0.0042 | 9 | 9 |
| bay 80-6946 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| pp242 | Homo sapiens (human) | Kd | 2.3986 | 7 | 7 |
Drugs with Other Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| su 11248 | Homo sapiens (human) | INH | 0.0566 | 2 | 2 |
| crenolanib | Homo sapiens (human) | INH | 0.0231 | 2 | 2 |
Inhibition of FLT3 and PDGFR tyrosine kinase activity by bis(benzo[b]furan-2-yl)methanones.Bioorganic & medicinal chemistry, , Mar-01, Volume: 15, Issue:5, 2007
Novel bis(1H-indol-2-yl)methanones as potent inhibitors of FLT3 and platelet-derived growth factor receptor tyrosine kinase.Journal of medicinal chemistry, , Jun-01, Volume: 49, Issue:11, 2006
Anticancer potential of indirubins in medicinal chemistry: Biological activity, structural modification, and structure-activity relationship.European journal of medicinal chemistry, , Nov-05, Volume: 223, 2021
Indirubin derivatives as potent FLT3 inhibitors with anti-proliferative activity of acute myeloid leukemic cells.Bioorganic & medicinal chemistry letters, , Mar-15, Volume: 20, Issue:6, 2010
A multi-scale systems pharmacology approach uncovers the anti-cancer molecular mechanism of Ixabepilone.European journal of medicinal chemistry, , Aug-01, Volume: 199, 2020
Identification of a Multitargeted Tyrosine Kinase Inhibitor for the Treatment of Gastrointestinal Stromal Tumors and Acute Myeloid Leukemia.Journal of medicinal chemistry, , 12-26, Volume: 62, Issue:24, 2019
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 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
Discovery of a benzimidazole-based dual FLT3/TrKA inhibitor targeting acute myeloid leukemia.Bioorganic & medicinal chemistry, , 02-15, Volume: 56, 2022
Isoxazole derivatives as anticancer agent: A review on synthetic strategies, mechanism of action and SAR studies.European journal of medicinal chemistry, , Oct-05, Volume: 221, 2021
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
Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors.Bioorganic & medicinal chemistry, , 05-01, Volume: 26, Issue:8, 2018
Discovery of the selective and efficacious inhibitors of FLT3 mutations.European journal of medicinal chemistry, , Jul-15, Volume: 155, 2018
Novel LCK/FMS inhibitors based on phenoxypyrimidine scaffold as potential treatment for inflammatory disorders.European journal of medicinal chemistry, , Dec-01, Volume: 141, 2017
Synthesis and evaluation of a series of pyridine and pyrimidine derivatives as type II c-Met inhibitors.Bioorganic & medicinal chemistry, , 06-15, Volume: 25, Issue:12, 2017
Discovery and Rational Design of Pteridin-7(8H)-one-Based Inhibitors Targeting FMS-like Tyrosine Kinase 3 (FLT3) and Its Mutants.Journal of medicinal chemistry, , 07-14, Volume: 59, Issue:13, 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
Discovery of 4-arylamido 3-methyl isoxazole derivatives as novel FMS kinase inhibitors.European journal of medicinal chemistry, , Sep-18, Volume: 102, 2015
Novel acylureidoindolin-2-one derivatives as dual Aurora B/FLT3 inhibitors for the treatment of acute myeloid leukemia.European journal of medicinal chemistry, , Oct-06, Volume: 85, 2014
Discovery, synthesis, and characterization of an orally bioavailable, brain penetrant inhibitor of mixed lineage kinase 3.Journal of medicinal chemistry, , Oct-24, Volume: 56, Issue:20, 2013
Design and combinatorial synthesis of a novel kinase-focused library using click chemistry-based fragment assembly.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 22, Issue:1, 2012
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
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 a benzimidazole-based dual FLT3/TrKA inhibitor targeting acute myeloid leukemia.Bioorganic & medicinal chemistry, , 02-15, Volume: 56, 2022
[no title available]European journal of medicinal chemistry, , Jun-01, Volume: 195, 2020
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Flavonoids as receptor tyrosine kinase FLT3 inhibitors.Bioorganic & medicinal chemistry letters, , Mar-15, Volume: 23, Issue:6, 2013
Discovery, synthesis, and characterization of an orally bioavailable, brain penetrant inhibitor of mixed lineage kinase 3.Journal of medicinal chemistry, , Oct-24, Volume: 56, Issue:20, 2013
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
Indirubin derivatives as potent FLT3 inhibitors with anti-proliferative activity of acute myeloid leukemic cells.Bioorganic & medicinal chemistry letters, , Mar-15, Volume: 20, Issue:6, 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
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
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 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
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
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
[no title available],
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
Discovery of a benzimidazole-based dual FLT3/TrKA inhibitor targeting acute myeloid leukemia.Bioorganic & medicinal chemistry, , 02-15, Volume: 56, 2022
Discovery of imidazo[1,2-a]pyridine-thiophene derivatives as FLT3 and FLT3 mutants inhibitors for acute myeloid leukemia through structure-based optimization of an NEK2 inhibitor.European journal of medicinal chemistry, , Dec-05, Volume: 225, 2021
Targeting Rearranged during Transfection in Cancer: A Perspective on Small-Molecule Inhibitors and Their Clinical Development.Journal of medicinal chemistry, , 08-26, Volume: 64, Issue:16, 2021
[no title available]European journal of medicinal chemistry, , Jun-01, Volume: 195, 2020
Virtual Screening Identifies Irreversible FMS-like Tyrosine Kinase 3 Inhibitors with Activity toward Resistance-Conferring Mutations.Journal of medicinal chemistry, , 03-14, Volume: 62, Issue:5, 2019
Combining structure- and property-based optimization to identify selective FLT3-ITD inhibitors with good antitumor efficacy in AML cell inoculated mouse xenograft model.European journal of medicinal chemistry, , Aug-15, Volume: 176, 2019
Cyclin-Dependent Kinase 8: A New Hope in Targeted Cancer Therapy?Journal of medicinal chemistry, , 06-28, Volume: 61, Issue:12, 2018
Discovery of 4-((7H-Pyrrolo[2,3-d]pyrimidin-4-yl)amino)-N-(4-((4-methylpiperazin-1-yl)methyl)phenyl)-1H-pyrazole-3-carboxamide (FN-1501), an FLT3- and CDK-Kinase Inhibitor with Potentially High Efficiency against Acute Myelocytic Leukemia.Journal of medicinal chemistry, , 02-22, Volume: 61, Issue:4, 2018
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
Discovery of AMG 925, a FLT3 and CDK4 dual kinase inhibitor with preferential affinity for the activated state of FLT3.Journal of medicinal chemistry, , Apr-24, Volume: 57, Issue:8, 2014
Discovery of 3-phenyl-1H-5-pyrazolylamine derivatives containing a urea pharmacophore as potent and efficacious inhibitors of FMS-like tyrosine kinase-3 (FLT3).Bioorganic & medicinal chemistry, , Jun-01, Volume: 21, Issue:11, 2013
Structure-activity relationship studies of pyrazolo[3,4-d]pyrimidine derivatives leading to the discovery of a novel multikinase inhibitor that potently inhibits FLT3 and VEGFR2 and evaluation of its activity against acute myeloid leukemia in vitro and inJournal of medicinal chemistry, , Feb-28, Volume: 56, Issue:4, 2013
3-Phenyl-1H-5-pyrazolylamine-based derivatives as potent and efficacious inhibitors of FMS-like tyrosine kinase-3 (FLT3).Bioorganic & medicinal chemistry letters, , Jul-15, Volume: 22, Issue:14, 2012
Discovery and evaluation of 3-phenyl-1H-5-pyrazolylamine-based derivatives as potent, selective and efficacious inhibitors of FMS-like tyrosine kinase-3 (FLT3).Bioorganic & medicinal chemistry, , Jul-15, Volume: 19, Issue:14, 2011
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
Identification of N-(5-tert-butyl-isoxazol-3-yl)-N'-{4-[7-(2-morpholin-4-yl-ethoxy)imidazo[2,1-b][1,3]benzothiazol-2-yl]phenyl}urea dihydrochloride (AC220), a uniquely potent, selective, and efficacious FMS-like tyrosine kinase-3 (FLT3) inhibitor.Journal of medicinal chemistry, , Dec-10, Volume: 52, Issue:23, 2009
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).Blood, , Oct-01, Volume: 114, Issue:14, 2009
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
Rational design of inhibitors that bind to inactive kinase conformations.Nature chemical biology, , Volume: 2, Issue:7, 2006
A small molecule-kinase interaction map for clinical kinase inhibitors.Nature biotechnology, , Volume: 23, Issue:3, 2005
Discovery, synthesis, and characterization of an orally bioavailable, brain penetrant inhibitor of mixed lineage kinase 3.Journal of medicinal chemistry, , Oct-24, Volume: 56, Issue:20, 2013
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
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
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
Single agents with designed combination chemotherapy potential: synthesis and evaluation of substituted pyrimido[4,5-b]indoles as receptor tyrosine kinase and thymidylate synthase inhibitors and as antitumor agents.Journal of medicinal chemistry, , Feb-25, Volume: 53, Issue:4, 2010
Identification of 2-acylaminothiophene-3-carboxamides as potent inhibitors of FLT3.Bioorganic & medicinal chemistry letters, , Jun-15, Volume: 16, Issue:12, 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
[no title available]European journal of medicinal chemistry, , Jun-01, Volume: 195, 2020
Dual FLT3 inhibitors: Against the drug resistance of acute myeloid leukemia in recent decade.European journal of medicinal chemistry, , Sep-15, Volume: 178, 2019
Discovery and development of extreme selective inhibitors of the ITD and D835Y mutant FLT3 kinases.European journal of medicinal chemistry, , Dec-15, Volume: 184, 2019
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Discovery and Rational Design of Pteridin-7(8H)-one-Based Inhibitors Targeting FMS-like Tyrosine Kinase 3 (FLT3) and Its Mutants.Journal of medicinal chemistry, , 07-14, Volume: 59, Issue:13, 2016
Synthesis and biological evaluation of novel thieno[2,3-d]pyrimidine-based FLT3 inhibitors as anti-leukemic agents.European journal of medicinal chemistry, , Oct-06, Volume: 85, 2014
Discovery of thienopyrimidine-based FLT3 inhibitors from the structural modification of known IKKβ inhibitors.Bioorganic & medicinal chemistry letters, , Jun-15, Volume: 24, Issue:12, 2014
VX-322: a novel dual receptor tyrosine kinase inhibitor for the treatment of acute myelogenous leukemia.Journal of medicinal chemistry, , Jan-26, Volume: 55, Issue:2, 2012
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
Synthesis and structure-activity relationship of 6-arylureido-3-pyrrol-2-ylmethylideneindolin-2-one derivatives as potent receptor tyrosine kinase inhibitors.Bioorganic & medicinal chemistry, , Jul-01, Volume: 18, Issue:13, 2010
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).Blood, , Oct-01, Volume: 114, Issue:14, 2009
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
A small molecule-kinase interaction map for clinical kinase inhibitors.Nature biotechnology, , Volume: 23, Issue:3, 2005
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
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
[no title available],
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
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
Discovery of a benzimidazole-based dual FLT3/TrKA inhibitor targeting acute myeloid leukemia.Bioorganic & medicinal chemistry, , 02-15, Volume: 56, 2022
Discovery and structure - activity relationship exploration of pyrazolo[1,5-a]pyrimidine derivatives as potent FLT3-ITD inhibitors.Bioorganic & medicinal chemistry, , 10-15, Volume: 48, 2021
[no title available]Journal of medicinal chemistry, , 04-22, Volume: 64, Issue:8, 2021
Targeting Rearranged during Transfection in Cancer: A Perspective on Small-Molecule Inhibitors and Their Clinical Development.Journal of medicinal chemistry, , 08-26, Volume: 64, Issue:16, 2021
[no title available]European journal of medicinal chemistry, , Jun-01, Volume: 195, 2020
Identification of a Multitargeted Tyrosine Kinase Inhibitor for the Treatment of Gastrointestinal Stromal Tumors and Acute Myeloid Leukemia.Journal of medicinal chemistry, , 12-26, Volume: 62, Issue:24, 2019
Discovery and development of extreme selective inhibitors of the ITD and D835Y mutant FLT3 kinases.European journal of medicinal chemistry, , Dec-15, Volume: 184, 2019
Virtual Screening Identifies Irreversible FMS-like Tyrosine Kinase 3 Inhibitors with Activity toward Resistance-Conferring Mutations.Journal of medicinal chemistry, , 03-14, Volume: 62, Issue:5, 2019
Design, synthesis and biological evaluation of indolin-2-one-based derivatives as potent, selective and efficacious inhibitors of FMS-like tyrosine kinase3 (FLT3).European journal of medicinal chemistry, , Feb-15, Volume: 127, 2017
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
VX-322: a novel dual receptor tyrosine kinase inhibitor for the treatment of acute myelogenous leukemia.Journal of medicinal chemistry, , Jan-26, Volume: 55, Issue:2, 2012
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
Novel azulene-based derivatives as potent multi-receptor tyrosine kinase inhibitors.Bioorganic & medicinal chemistry letters, , Oct-15, Volume: 20, Issue:20, 2010
Synthesis and structure-activity relationship of 6-arylureido-3-pyrrol-2-ylmethylideneindolin-2-one derivatives as potent receptor tyrosine kinase inhibitors.Bioorganic & medicinal chemistry, , Jul-01, Volume: 18, Issue:13, 2010
Selectively nonselective kinase inhibition: striking the right balance.Journal of medicinal chemistry, , Feb-25, Volume: 53, Issue:4, 2010
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
Identification of N-(5-tert-butyl-isoxazol-3-yl)-N'-{4-[7-(2-morpholin-4-yl-ethoxy)imidazo[2,1-b][1,3]benzothiazol-2-yl]phenyl}urea dihydrochloride (AC220), a uniquely potent, selective, and efficacious FMS-like tyrosine kinase-3 (FLT3) inhibitor.Journal of medicinal chemistry, , Dec-10, Volume: 52, Issue:23, 2009
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).Blood, , Oct-01, Volume: 114, Issue:14, 2009
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
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
Discovery of AMG 925, a FLT3 and CDK4 dual kinase inhibitor with preferential affinity for the activated state of FLT3.Journal of medicinal chemistry, , Apr-24, Volume: 57, Issue:8, 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
Virtual Screening Identifies Irreversible FMS-like Tyrosine Kinase 3 Inhibitors with Activity toward Resistance-Conferring Mutations.Journal of medicinal chemistry, , 03-14, Volume: 62, Issue:5, 2019
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Discovery, synthesis, and characterization of an orally bioavailable, brain penetrant inhibitor of mixed lineage kinase 3.Journal of medicinal chemistry, , Oct-24, Volume: 56, Issue:20, 2013
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
3-Cyano-6-(5-methyl-3-pyrazoloamino)pyridines: selective Aurora A kinase inhibitors.Bioorganic & medicinal chemistry letters, , Aug-01, Volume: 20, Issue:15, 2010
Discovery and development of aurora kinase inhibitors as anticancer agents.Journal of medicinal chemistry, , May-14, Volume: 52, Issue:9, 2009
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
Assessment of chemical coverage of kinome space and its implications for kinase drug discovery.Journal of medicinal chemistry, , Dec-25, Volume: 51, Issue:24, 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
Discovery of novel and potent thiazoloquinazolines as selective Aurora A and B kinase inhibitors.Journal of medicinal chemistry, , Feb-09, Volume: 49, Issue:3, 2006
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
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
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
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
Discovery of a benzimidazole-based dual FLT3/TrKA inhibitor targeting acute myeloid leukemia.Bioorganic & medicinal chemistry, , 02-15, Volume: 56, 2022
[no title available]European journal of medicinal chemistry, , Jun-01, Volume: 195, 2020
Discovery and development of extreme selective inhibitors of the ITD and D835Y mutant FLT3 kinases.European journal of medicinal chemistry, , Dec-15, Volume: 184, 2019
Identification of a Multitargeted Tyrosine Kinase Inhibitor for the Treatment of Gastrointestinal Stromal Tumors and Acute Myeloid Leukemia.Journal of medicinal chemistry, , 12-26, Volume: 62, Issue:24, 2019
Dual FLT3 inhibitors: Against the drug resistance of acute myeloid leukemia in recent decade.European journal of medicinal chemistry, , Sep-15, Volume: 178, 2019
Virtual Screening Identifies Irreversible FMS-like Tyrosine Kinase 3 Inhibitors with Activity toward Resistance-Conferring Mutations.Journal of medicinal chemistry, , 03-14, Volume: 62, Issue:5, 2019
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
Discovery, synthesis, and characterization of an orally bioavailable, brain penetrant inhibitor of mixed lineage kinase 3.Journal of medicinal chemistry, , Oct-24, Volume: 56, Issue:20, 2013
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).Blood, , Oct-01, Volume: 114, Issue:14, 2009
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Discovery, synthesis, and characterization of an orally bioavailable, brain penetrant inhibitor of mixed lineage kinase 3.Journal of medicinal chemistry, , Oct-24, Volume: 56, Issue:20, 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
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
Discovery of a benzimidazole-based dual FLT3/TrKA inhibitor targeting acute myeloid leukemia.Bioorganic & medicinal chemistry, , 02-15, Volume: 56, 2022
[no title available]European journal of medicinal chemistry, , Jun-01, Volume: 195, 2020
Dual FLT3 inhibitors: Against the drug resistance of acute myeloid leukemia in recent decade.European journal of medicinal chemistry, , Sep-15, Volume: 178, 2019
Virtual Screening Identifies Irreversible FMS-like Tyrosine Kinase 3 Inhibitors with Activity toward Resistance-Conferring Mutations.Journal of medicinal chemistry, , 03-14, Volume: 62, Issue:5, 2019
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Discovery of a Highly Potent and Selective Indenoindolone Type 1 Pan-FLT3 Inhibitor.ACS medicinal chemistry letters, , May-12, Volume: 7, 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
Identification of a Unique Resorcylic Acid Lactone Derivative That Targets Both Lymphangiogenesis and Angiogenesis.Journal of medicinal chemistry, , 10-24, Volume: 62, Issue:20, 2019
Identification of the First Selective Activin Receptor-Like Kinase 1 Inhibitor, a Reversible Version of L-783277.Journal of medicinal chemistry, , 02-23, Volume: 60, Issue:4, 2017
Design, synthesis and biological evaluation of FLT3 covalent inhibitors with a resorcylic acid core.Bioorganic & medicinal chemistry, , Dec-01, Volume: 22, Issue:23, 2014
Identification of a Multitargeted Tyrosine Kinase Inhibitor for the Treatment of Gastrointestinal Stromal Tumors and Acute Myeloid Leukemia.Journal of medicinal chemistry, , 12-26, Volume: 62, Issue:24, 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
Discovery of GS-9973, a selective and orally efficacious inhibitor of spleen tyrosine kinase.Journal of medicinal chemistry, , May-08, Volume: 57, Issue:9, 2014
Discovery, synthesis, and characterization of an orally bioavailable, brain penetrant inhibitor of mixed lineage kinase 3.Journal of medicinal chemistry, , Oct-24, Volume: 56, Issue:20, 2013
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
Selectivity data: assessment, predictions, concordance, and implications.Journal of medicinal chemistry, , Sep-12, Volume: 56, Issue:17, 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
Discovery and development of extreme selective inhibitors of the ITD and D835Y mutant FLT3 kinases.European journal of medicinal chemistry, , Dec-15, Volume: 184, 2019
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Discovery, synthesis, and characterization of an orally bioavailable, brain penetrant inhibitor of mixed lineage kinase 3.Journal of medicinal chemistry, , Oct-24, Volume: 56, Issue:20, 2013
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazoles: identification of a potent Aurora kinase inhibitor with a favorable antitumor kinase inhibition profile.Journal of medicinal chemistry, , Nov-30, Volume: 49, Issue:24, 2006
Synthesis and biological evaluation of 4-(4-aminophenyl)-6-methylisoxazolo[3,4-b] pyridin-3-amine covalent inhibitors as potential agents for the treatment of acute myeloid leukemia.Bioorganic & medicinal chemistry, , 09-15, Volume: 70, 2022
Design, synthesis and structure-activity relationship of diaryl-ureas with novel isoxazol[3,4-b]pyridine-3-amino-structure as multi-target inhibitors against receptor tyrosine kinase.Bioorganic & medicinal chemistry, , 09-01, Volume: 26, Issue:16, 2018
Cyclin-Dependent Kinase 8: A New Hope in Targeted Cancer Therapy?Journal of medicinal chemistry, , 06-28, Volume: 61, Issue:12, 2018
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Discovery of 3-phenyl-1H-5-pyrazolylamine derivatives containing a urea pharmacophore as potent and efficacious inhibitors of FMS-like tyrosine kinase-3 (FLT3).Bioorganic & medicinal chemistry, , Jun-01, Volume: 21, Issue:11, 2013
3-Phenyl-1H-5-pyrazolylamine-based derivatives as potent and efficacious inhibitors of FMS-like tyrosine kinase-3 (FLT3).Bioorganic & medicinal chemistry letters, , Jul-15, Volume: 22, Issue:14, 2012
Discovery and evaluation of 3-phenyl-1H-5-pyrazolylamine-based derivatives as potent, selective and efficacious inhibitors of FMS-like tyrosine kinase-3 (FLT3).Bioorganic & medicinal chemistry, , Jul-15, Volume: 19, Issue:14, 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
Discovery of N-(4-(3-amino-1H-indazol-4-yl)phenyl)-N'-(2-fluoro-5-methylphenyl)urea (ABT-869), a 3-aminoindazole-based orally active multitargeted receptor tyrosine kinase inhibitor.Journal of medicinal chemistry, , Apr-05, Volume: 50, Issue:7, 2007
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Discovery and development of aurora kinase inhibitors as anticancer agents.Journal of medicinal chemistry, , May-14, Volume: 52, Issue:9, 2009
Design, synthesis, and biological evaluation of 4-((6,7-dimethoxyquinoline-4-yl)oxy)aniline derivatives as FLT3 inhibitors for the treatment of acute myeloid leukemia.Bioorganic & medicinal chemistry letters, , 10-01, Volume: 29, Issue:19, 2019
Discovery of AZD2932, a new Quinazoline Ether Inhibitor with high affinity for VEGFR-2 and PDGFR tyrosine kinases.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 22, Issue:1, 2012
Discovery of new quinoline ether inhibitors with high affinity and selectivity for PDGFR tyrosine kinases.Bioorganic & medicinal chemistry letters, , May-01, Volume: 22, Issue:9, 2012
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
Inhibition of colony-stimulating-factor-1 signaling in vivo with the orally bioavailable cFMS kinase inhibitor GW2580.Proceedings of the National Academy of Sciences of the United States of America, , Nov-01, Volume: 102, Issue:44, 2005
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Pyridazinone derivatives displaying highly potent and selective inhibitory activities against c-Met tyrosine kinase.European journal of medicinal chemistry, , Jan-27, Volume: 108, 2016
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
Pyrido[2,3-d]pyrimidin-5-ones: a novel class of antiinflammatory macrophage colony-stimulating factor-1 receptor inhibitors.Journal of medicinal chemistry, , Feb-26, Volume: 52, Issue:4, 2009
Discovery of novel FMS kinase inhibitors as anti-inflammatory agents.Bioorganic & medicinal chemistry letters, , Mar-01, Volume: 18, Issue:5, 2008
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Selectivity data: assessment, predictions, concordance, and implications.Journal of medicinal chemistry, , Sep-12, Volume: 56, Issue:17, 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
Dual FLT3 inhibitors: Against the drug resistance of acute myeloid leukemia in recent decade.European journal of medicinal chemistry, , Sep-15, Volume: 178, 2019
Discovery, synthesis, and characterization of an orally bioavailable, brain penetrant inhibitor of mixed lineage kinase 3.Journal of medicinal chemistry, , Oct-24, Volume: 56, Issue:20, 2013
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
Identification of NVP-TAE684, a potent, selective, and efficacious inhibitor of NPM-ALK.Proceedings of the National Academy of Sciences of the United States of America, , Jan-02, Volume: 104, Issue:1, 2007
Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling.Proceedings of the National Academy of Sciences of the United States of America, , Dec-11, Volume: 104, Issue:50, 2007
Discovery and development of extreme selective inhibitors of the ITD and D835Y mutant FLT3 kinases.European journal of medicinal chemistry, , Dec-15, Volume: 184, 2019
Synthesis and identification of 2,4-bisanilinopyrimidines bearing 2,2,6,6-tetramethylpiperidine-N-oxyl as potential Aurora A inhibitors.Bioorganic & medicinal chemistry, , 01-01, Volume: 27, Issue:1, 2019
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
Small-Molecule Kinase Inhibitors for the Treatment of Nononcologic Diseases.Journal of medicinal chemistry, , 02-11, Volume: 64, Issue:3, 2021
Non-kinase targets of protein kinase inhibitors.Nature reviews. Drug discovery, , Volume: 16, Issue:6, 2017
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Cyclin Dependent Kinase 9 Inhibitors for Cancer Therapy.Journal of medicinal chemistry, , 10-13, Volume: 59, Issue:19, 2016
Macrocyclic compounds as anti-cancer agents: design and synthesis of multi-acting inhibitors against HDAC, FLT3 and JAK2.European journal of medicinal chemistry, , May-05, Volume: 95, 2015
Discovery of kinase spectrum selective macrocycle (16E)-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 (SB1317/TG02), a potent inhibitor of cyclin dependent kinases (CDKs), Janus kJournal of medicinal chemistry, , Jan-12, Volume: 55, Issue:1, 2012
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
Optimization of pyrazolo[1,5-a]pyrimidines lead to the identification of a highly selective casein kinase 2 inhibitor.European journal of medicinal chemistry, , Dec-15, Volume: 208, 2020
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Discovery and SAR of 5-(3-chlorophenylamino)benzo[c][2,6]naphthyridine-8-carboxylic acid (CX-4945), the first clinical stage inhibitor of protein kinase CK2 for the treatment of cancer.Journal of medicinal chemistry, , Jan-27, Volume: 54, Issue:2, 2011
[no title available],
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
Synthesis and evaluation of a series of pyridine and pyrimidine derivatives as type II c-Met inhibitors.Bioorganic & medicinal chemistry, , 06-15, Volume: 25, Issue:12, 2017
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Discovery of N-(4-(2-amino-3-chloropyridin-4-yloxy)-3-fluorophenyl)-4-ethoxy-1-(4-fluorophenyl)-2-oxo-1,2-dihydropyridine-3-carboxamide (BMS-777607), a selective and orally efficacious inhibitor of the Met kinase superfamily.Journal of medicinal chemistry, , Mar-12, Volume: 52, Issue:5, 2009
[no title available],
Dual FLT3 inhibitors: Against the drug resistance of acute myeloid leukemia in recent decade.European journal of medicinal chemistry, , Sep-15, Volume: 178, 2019
Discovery of novel triazolo[4,3-b]pyridazin-3-yl-quinoline derivatives as PIM inhibitors.European journal of medicinal chemistry, , Apr-15, Volume: 168, 2019
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Potential use of selective and nonselective Pim kinase inhibitors for cancer therapy.Journal of medicinal chemistry, , Oct-11, Volume: 55, Issue:19, 2012
Discovery of 4,7-Diamino-5-(4-phenoxyphenyl)-6-methylene-pyrimido[5,4- b]pyrrolizines as Novel Bruton's Tyrosine Kinase Inhibitors.Journal of medicinal chemistry, , 05-24, Volume: 61, Issue:10, 2018
[no title available]European journal of medicinal chemistry, , Feb-10, Volume: 145, 2018
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Discovery of (R)-1-(3-(4-Amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)-2-(dimethylamino)ethanone (CHMFL-FLT3-122) as a Potent and Orally Available FLT3 Kinase Inhibitor for FLT3-ITD Positive Acute Myeloid Leukemia.Journal of medicinal chemistry, , Dec-24, Volume: 58, Issue:24, 2015
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
[no title available]European journal of medicinal chemistry, , Jun-01, Volume: 195, 2020
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Synthesis of 2H-Imidazo[2',1':2,3] [1,3]thiazolo[4,5-e]isoindol-8-yl-phenylureas with promising therapeutic features for the treatment of acute myeloid leukemia (AML) with FLT3/ITD mutations.European journal of medicinal chemistry, , May-05, Volume: 235, 2022
Synthesis and biological activity evaluation of novel 2,6,9-trisubstituted purine conjugates as potential protein kinases inhibitors.Bioorganic & medicinal chemistry letters, , 03-15, Volume: 60, 2022
Discovery of a benzimidazole-based dual FLT3/TrKA inhibitor targeting acute myeloid leukemia.Bioorganic & medicinal chemistry, , 02-15, Volume: 56, 2022
Discovery and structure - activity relationship exploration of pyrazolo[1,5-a]pyrimidine derivatives as potent FLT3-ITD inhibitors.Bioorganic & medicinal chemistry, , 10-15, Volume: 48, 2021
3Journal of medicinal chemistry, , 08-12, Volume: 64, Issue:15, 2021
[no title available]European journal of medicinal chemistry, , Jun-01, Volume: 195, 2020
A series of novel aryl-methanone derivatives as inhibitors of FMS-like tyrosine kinase 3 (FLT3) in FLT3-ITD-positive acute myeloid leukemia.European journal of medicinal chemistry, , May-01, Volume: 193, 2020
Synthesis and biological evaluation of diaryl urea derivatives as FLT3 inhibitors.Bioorganic & medicinal chemistry letters, , 12-01, Volume: 30, Issue:23, 2020
Identification and Development of 1,4-Diaryl-1,2,3-triazolo-Based Ureas as Novel FLT3 Inhibitors.ACS medicinal chemistry letters, , Aug-13, Volume: 11, Issue:8, 2020
Discovery of small molecule FLT3 inhibitors that are able to overcome drug-resistant mutations.Bioorganic & medicinal chemistry letters, , 11-15, Volume: 30, Issue:22, 2020
[no title available]Journal of medicinal chemistry, , 04-25, Volume: 62, Issue:8, 2019
Virtual Screening Identifies Irreversible FMS-like Tyrosine Kinase 3 Inhibitors with Activity toward Resistance-Conferring Mutations.Journal of medicinal chemistry, , 03-14, Volume: 62, Issue:5, 2019
Discovery and development of extreme selective inhibitors of the ITD and D835Y mutant FLT3 kinases.European journal of medicinal chemistry, , Dec-15, Volume: 184, 2019
Identification of a Unique Resorcylic Acid Lactone Derivative That Targets Both Lymphangiogenesis and Angiogenesis.Journal of medicinal chemistry, , 10-24, Volume: 62, Issue:20, 2019
Discovery of NJournal of medicinal chemistry, , 05-10, Volume: 61, Issue:9, 2018
Synthetic strategy for increasing solubility of potential FLT3 inhibitor thieno[2,3-d]pyrimidine derivatives through structural modifications at the CBioorganic & medicinal chemistry letters, , 02-01, Volume: 27, Issue:3, 2017
Discovery of 1-(4-(4-Amino-3-(4-(2-morpholinoethoxy)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)phenyl)-3-(5-(tert-butyl)isoxazol-3-yl)urea (CHMFL-FLT3-213) as a Highly Potent Type II FLT3 Kinase Inhibitor Capable of Overcoming a Variety of FLT3 Kinase MutanJournal of medicinal chemistry, , 10-26, Volume: 60, Issue:20, 2017
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Discovery of a Highly Potent and Selective Indenoindolone Type 1 Pan-FLT3 Inhibitor.ACS medicinal chemistry letters, , May-12, Volume: 7, Issue:5, 2016
Discovery and Rational Design of Pteridin-7(8H)-one-Based Inhibitors Targeting FMS-like Tyrosine Kinase 3 (FLT3) and Its Mutants.Journal of medicinal chemistry, , 07-14, Volume: 59, Issue:13, 2016
Structural modifications at the 6-position of thieno[2,3-d]pyrimidines and their effects on potency at FLT3 for treatment of acute myeloid leukemia.European journal of medicinal chemistry, , Sep-14, Volume: 120, 2016
Computer aided drug discovery of highly ligand efficient, low molecular weight imidazopyridine analogs as FLT3 inhibitors.European journal of medicinal chemistry, , Apr-13, Volume: 94, 2015
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
Synthesis and biological evaluation of novel thieno[2,3-d]pyrimidine-based FLT3 inhibitors as anti-leukemic agents.European journal of medicinal chemistry, , Oct-06, Volume: 85, 2014
Discovery of thienopyrimidine-based FLT3 inhibitors from the structural modification of known IKKβ inhibitors.Bioorganic & medicinal chemistry letters, , Jun-15, Volume: 24, Issue:12, 2014
3-Phenyl-1H-5-pyrazolylamine-based derivatives as potent and efficacious inhibitors of FMS-like tyrosine kinase-3 (FLT3).Bioorganic & medicinal chemistry letters, , Jul-15, Volume: 22, Issue:14, 2012
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
Toward the development of innovative bifunctional agents to induce differentiation and to promote apoptosis in leukemia: clinical candidates and perspectives.Journal of medicinal chemistry, , Oct-14, Volume: 53, Issue:19, 2010
Identification of N-(5-tert-butyl-isoxazol-3-yl)-N'-{4-[7-(2-morpholin-4-yl-ethoxy)imidazo[2,1-b][1,3]benzothiazol-2-yl]phenyl}urea dihydrochloride (AC220), a uniquely potent, selective, and efficacious FMS-like tyrosine kinase-3 (FLT3) inhibitor.Journal of medicinal chemistry, , Dec-10, Volume: 52, Issue:23, 2009
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).Blood, , Oct-01, Volume: 114, Issue:14, 2009
Discovery of a benzimidazole-based dual FLT3/TrKA inhibitor targeting acute myeloid leukemia.Bioorganic & medicinal chemistry, , 02-15, Volume: 56, 2022
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Targeting Rearranged during Transfection in Cancer: A Perspective on Small-Molecule Inhibitors and Their Clinical Development.Journal of medicinal chemistry, , 08-26, Volume: 64, Issue:16, 2021
Design, synthesis and biological evaluation of novel 2,4-diaryl pyrimidine derivatives as selective EGFREuropean journal of medicinal chemistry, , Feb-15, Volume: 212, 2021
FLT3 Inhibitors in Acute Myeloid Leukemia: Challenges and Recent Developments in Overcoming Resistance.Journal of medicinal chemistry, , 03-25, Volume: 64, Issue:6, 2021
Design, synthesis, and biological evaluation of 4-((6,7-dimethoxyquinoline-4-yl)oxy)aniline derivatives as FLT3 inhibitors for the treatment of acute myeloid leukemia.Bioorganic & medicinal chemistry letters, , 10-01, Volume: 29, Issue:19, 2019
Structure-based design, synthesis, and evaluation of 4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine derivatives as novel c-Met inhibitors.European journal of medicinal chemistry, , Sep-29, Volume: 138, 2017
Synthesis and evaluation of a series of pyridine and pyrimidine derivatives as type II c-Met inhibitors.Bioorganic & medicinal chemistry, , 06-15, Volume: 25, Issue:12, 2017
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
The "Cyclopropyl Fragment" is a Versatile Player that Frequently Appears in Preclinical/Clinical Drug Molecules.Journal of medicinal chemistry, , 10-13, Volume: 59, Issue:19, 2016
Recent advances in the development of dual VEGFR and c-Met small molecule inhibitors as anticancer drugs.European journal of medicinal chemistry, , Jan-27, Volume: 108, 2016
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
Discovery of vimseltinib (DCC-3014), a highly selective CSF1R switch-control kinase inhibitor, in clinical development for the treatment of Tenosynovial Giant Cell Tumor (TGCT).Bioorganic & medicinal chemistry letters, , 10-15, Volume: 74, 2022
Discovery of acyl ureas as highly selective small molecule CSF1R kinase inhibitors.Bioorganic & medicinal chemistry letters, , 10-15, Volume: 74, 2022
FLT3 Inhibitors in Acute Myeloid Leukemia: Challenges and Recent Developments in Overcoming Resistance.Journal of medicinal chemistry, , 03-25, Volume: 64, Issue:6, 2021
Discovery and development of extreme selective inhibitors of the ITD and D835Y mutant FLT3 kinases.European journal of medicinal chemistry, , Dec-15, Volume: 184, 2019
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Discovery of a Highly Potent and Selective Indenoindolone Type 1 Pan-FLT3 Inhibitor.ACS medicinal chemistry letters, , May-12, Volume: 7, Issue:5, 2016
Design, synthesis and biological evaluation of novel N-sulfonylamidine-based derivatives as c-Met inhibitors via Cu-catalyzed three-component reaction.European journal of medicinal chemistry, , Aug-15, Volume: 200, 2020
Structure-based discovery of novel 4-(2-fluorophenoxy)quinoline derivatives as c-Met inhibitors using isocyanide-involved multicomponent reactions.European journal of medicinal chemistry, , May-01, Volume: 193, 2020
Design, synthesis, and biological evaluation of 4-((6,7-dimethoxyquinoline-4-yl)oxy)aniline derivatives as FLT3 inhibitors for the treatment of acute myeloid leukemia.Bioorganic & medicinal chemistry letters, , 10-01, Volume: 29, Issue:19, 2019
Design, synthesis and evaluation of sulfonylurea-containing 4-phenoxyquinolines as highly selective c-Met kinase inhibitors.Bioorganic & medicinal chemistry, , 07-01, Volume: 27, Issue:13, 2019
Design, synthesis and biological evaluation of novel 4-phenoxyquinoline derivatives containing 3-oxo-3,4-dihydroquinoxaline moiety as c-Met kinase inhibitors.Bioorganic & medicinal chemistry, , 08-15, Volume: 25, Issue:16, 2017
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
The "Cyclopropyl Fragment" is a Versatile Player that Frequently Appears in Preclinical/Clinical Drug Molecules.Journal of medicinal chemistry, , 10-13, Volume: 59, Issue:19, 2016
Design, synthesis and structure-activity relationships of novel 4-phenoxyquinoline derivatives containing 1,2,4-triazolone moiety as c-Met kinase inhibitors.European journal of medicinal chemistry, , Nov-10, Volume: 123, 2016
Design and biological evaluation of novel 4-(2-fluorophenoxy)quinoline derivatives bearing an imidazolone moiety as c-Met kinase inhibitors.Bioorganic & medicinal chemistry, , Aug-01, Volume: 23, Issue:15, 2015
Design, synthesis and pharmacological evaluation of 6,7-disubstituted-4-phenoxyquinoline derivatives as potential antitumor agents.Bioorganic chemistry, , Volume: 57, 2014
Design and optimization of novel 4-(2-fluorophenoxy)quinoline derivatives bearing a hydrazone moiety as c-Met kinase inhibitors.European journal of medicinal chemistry, , Nov-24, Volume: 87, 2014
Discovery, synthesis, and characterization of an orally bioavailable, brain penetrant inhibitor of mixed lineage kinase 3.Journal of medicinal chemistry, , Oct-24, Volume: 56, Issue:20, 2013
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
FLT3 Inhibitors in Acute Myeloid Leukemia: Challenges and Recent Developments in Overcoming Resistance.Journal of medicinal chemistry, , 03-25, Volume: 64, Issue:6, 2021
Dual FLT3 inhibitors: Against the drug resistance of acute myeloid leukemia in recent decade.European journal of medicinal chemistry, , Sep-15, Volume: 178, 2019
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Discovery of the macrocycle 11-(2-pyrrolidin-1-yl-ethoxy)-14,19-dioxa-5,7,26-triaza-tetracyclo[19.3.1.1(2,6).1(8,12)]heptacosa-1(25),2(26),3,5,8,10,12(27),16,21,23-decaene (SB1518), a potent Janus kinase 2/fms-like tyrosine kinase-3 (JAK2/FLT3) inhibitor Journal of medicinal chemistry, , Jul-14, Volume: 54, Issue:13, 2011
3Journal of medicinal chemistry, , 08-12, Volume: 64, Issue:15, 2021
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Recent Developments in the Use of Kinase Inhibitors for Management of Viral Infections.Journal of medicinal chemistry, , 01-27, Volume: 65, Issue:2, 2022
FLT3 Inhibitors in Acute Myeloid Leukemia: Challenges and Recent Developments in Overcoming Resistance.Journal of medicinal chemistry, , 03-25, Volume: 64, Issue:6, 2021
Discovery of novel 4-azaaryl-N-phenylpyrimidin-2-amine derivatives as potent and selective FLT3 inhibitors for acute myeloid leukaemia with FLT3 mutations.European journal of medicinal chemistry, , Mar-05, Volume: 213, 2021
Discovery of Venturicidin Congeners and Identification of the Biosynthetic Gene Cluster from Journal of natural products, , 01-22, Volume: 84, Issue:1, 2021
[no title available]European journal of medicinal chemistry, , Jun-01, Volume: 195, 2020
Dual FLT3 inhibitors: Against the drug resistance of acute myeloid leukemia in recent decade.European journal of medicinal chemistry, , Sep-15, Volume: 178, 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
Triazolopyridines as selective JAK1 inhibitors: from hit identification to GLPG0634.Journal of medicinal chemistry, , Nov-26, Volume: 57, Issue:22, 2014
[no title available],
Discovery and antitumor activity of Benzo[d]imidazol-containing 2,4-diarylaminopyrimidine analogues as ALK inhibitors with mutation-combating effects.Bioorganic & medicinal chemistry, , 05-01, Volume: 37, 2021
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
From Structure Modification to Drug Launch: A Systematic Review of the Ongoing Development of Cyclin-Dependent Kinase Inhibitors for Multiple Cancer Therapy.Journal of medicinal chemistry, , 05-12, Volume: 65, Issue:9, 2022
FLT3 Inhibitors in Acute Myeloid Leukemia: Challenges and Recent Developments in Overcoming Resistance.Journal of medicinal chemistry, , 03-25, Volume: 64, Issue:6, 2021
Discovery of AMG 925, a FLT3 and CDK4 dual kinase inhibitor with preferential affinity for the activated state of FLT3.Journal of medicinal chemistry, , Apr-24, Volume: 57, Issue:8, 2014
Highly Selective MERTK Inhibitors Achieved by a Single Methyl Group.Journal of medicinal chemistry, , 11-21, Volume: 61, Issue:22, 2018
UNC2025, a potent and orally bioavailable MER/FLT3 dual inhibitor.Journal of medicinal chemistry, , Aug-28, Volume: 57, Issue:16, 2014
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
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
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
Design, structure-activity relationships and in vivo characterization of 4-amino-3-benzimidazol-2-ylhydroquinolin-2-ones: a novel class of receptor tyrosine kinase inhibitors.Journal of medicinal chemistry, , Jan-22, Volume: 52, Issue:2, 2009
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Discovery, synthesis, and characterization of an orally bioavailable, brain penetrant inhibitor of mixed lineage kinase 3.Journal of medicinal chemistry, , Oct-24, Volume: 56, Issue:20, 2013
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
Design, synthesis, and evaluation of indolinones as triple angiokinase inhibitors and the discovery of a highly specific 6-methoxycarbonyl-substituted indolinone (BIBF 1120).Journal of medicinal chemistry, , Jul-23, Volume: 52, Issue:14, 2009
BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy.Cancer research, , Jun-15, Volume: 68, Issue:12, 2008
Enables
This protein enables 10 target(s):
| Target | Category | Definition |
|---|
| protein tyrosine kinase activity | molecular function | Catalysis of the reaction: ATP + a protein tyrosine = ADP + protein tyrosine phosphate. [RHEA:10596] |
| transmembrane receptor protein tyrosine kinase activity | molecular function | Combining with a signal and transmitting the signal from one side of the membrane to the other to initiate a change in cell activity by catalysis of the reaction: ATP + a protein-L-tyrosine = ADP + a protein-L-tyrosine phosphate. [EC:2.7.10.1, GOC:mah] |
| cytokine receptor activity | molecular function | Combining with a cytokine and transmitting the signal from one side of the membrane to the other to initiate a change in cell activity. [GOC:add, GOC:mah] |
| vascular endothelial growth factor receptor activity | molecular function | Combining with a vascular endothelial growth factor (VEGF) receptor ligand and transmitting the signal across the plasma membrane to initiate a change in cell activity. [GOC:mah, GOC:signaling, PMID:19909239] |
| 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] |
| nuclear glucocorticoid receptor binding | molecular function | Binding to a nuclear glucocorticoid receptor. [GOC:bf] |
| protein-containing complex binding | molecular function | Binding to a macromolecular complex. [GOC:jl] |
| phosphatidylinositol 3-kinase activator activity | molecular function | Binds to and increases the activity of a phosphatidylinositol 3-kinase (PI3K). [PMID:31686003] |
| growth factor binding | molecular function | Binding to a growth factor, proteins or polypeptides that stimulate a cell or organism to grow or proliferate. [GOC:curators] |
Located In
This protein is located in 4 target(s):
| Target | Category | Definition |
|---|
| endoplasmic reticulum | cellular component | The irregular network of unit membranes, visible only by electron microscopy, that occurs in the cytoplasm of many eukaryotic cells. The membranes form a complex meshwork of tubular channels, which are often expanded into slitlike cavities called cisternae. The ER takes two forms, rough (or granular), with ribosomes adhering to the outer surface, and smooth (with no ribosomes attached). [ISBN:0198506732] |
| endoplasmic reticulum lumen | cellular component | The volume enclosed by the membranes of the endoplasmic reticulum. [ISBN:0198547684] |
| plasma membrane | cellular component | The membrane surrounding a cell that separates the cell from its external environment. It consists of a phospholipid bilayer and associated proteins. [ISBN:0716731363] |
| endosome membrane | cellular component | The lipid bilayer surrounding an endosome. [GOC:mah] |
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 |
|---|
| receptor complex | cellular component | Any protein complex that undergoes combination with a hormone, neurotransmitter, drug or intracellular messenger to initiate a change in cell function. [GOC:go_curators] |
Involved In
This protein is involved in 24 target(s):
| Target | Category | Definition |
|---|
| leukocyte homeostasis | biological process | The process of regulating the proliferation and elimination of cells of the immune system such that the total number of cells of a particular cell type within a whole or part of an organism is stable over time in the absence of an outside stimulus. [GOC:add, ISBN:0781735149] |
| myeloid progenitor cell differentiation | biological process | The process in which a precursor cell type acquires the specialized features of a myeloid progenitor cell. Myeloid progenitor cells include progenitor cells for any of the myeloid lineages. [GOC:add, PMID:16551264] |
| pro-B cell differentiation | biological process | The process in which a precursor cell type acquires the specialized features of a pro-B cell. Pro-B cells are the earliest stage of the B cell lineage and undergo heavy chain D and J gene rearrangements, although they are not fully committed. [GOC:jal, ISBN:0781735149] |
| cell surface receptor protein tyrosine kinase signaling pathway | biological process | The series of molecular signals initiated by an extracellular ligand binding to a receptor on the surface of the target cell where the receptor possesses tyrosine kinase activity, and ending with the regulation of a downstream cellular process, e.g. transcription. [GOC:ceb, GOC:signaling] |
| positive regulation of cell population proliferation | biological process | Any process that activates or increases the rate or extent of cell proliferation. [GOC:go_curators] |
| response to organonitrogen compound | 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 organonitrogen stimulus. An organonitrogen compound is formally a compound containing at least one carbon-nitrogen bond. [PMID:9869419] |
| peptidyl-tyrosine phosphorylation | biological process | The phosphorylation of peptidyl-tyrosine to form peptidyl-O4'-phospho-L-tyrosine. [RESID:AA0039] |
| cytokine-mediated signaling pathway | biological process | The series of molecular signals initiated by the binding of a cytokine to a receptor on the surface of a cell, and ending with the regulation of a downstream cellular process, e.g. transcription. [GOC:mah, GOC:signaling, PMID:19295629] |
| B cell differentiation | biological process | The process in which a precursor cell type acquires the specialized features of a B cell. A B cell is a lymphocyte of B lineage with the phenotype CD19-positive and capable of B cell mediated immunity. [GO_REF:0000022, GOC:mah] |
| animal organ regeneration | biological process | The regrowth of a lost or destroyed animal organ. [GOC:mah] |
| common myeloid progenitor cell proliferation | biological process | The multiplication or reproduction of common myeloid progenitor cells, resulting in the expansion of a cell population. A common myeloid progenitor cell is a progenitor cell committed to the myeloid lineage. [CL:0000049, GOC:BHF] |
| vascular endothelial growth factor signaling pathway | biological process | The series of molecular signals initiated by vascular endothelial growth factor (VEGF) binding its receptor on the surface of the target cell, and ending with the regulation of a downstream cellular process, e.g. transcription. [GOC:signaling, PMID:17470632] |
| positive regulation of tyrosine phosphorylation of STAT protein | biological process | Any process that activates or increases the frequency, rate or extent of the introduction of a phosphate group to a tyrosine residue of a STAT (Signal Transducer and Activator of Transcription) protein. [GOC:jl, PMID:11426647] |
| regulation of apoptotic process | biological process | Any process that modulates the occurrence or rate of cell death by apoptotic process. [GOC:jl, GOC:mtg_apoptosis] |
| positive regulation of MAP kinase activity | biological process | Any process that activates or increases the frequency, rate or extent of MAP kinase activity. [GOC:dph, GOC:go_curators] |
| positive regulation of MAPK cascade | biological process | Any process that activates or increases the frequency, rate or extent of signal transduction mediated by the MAPK cascade. [GOC:go_curators] |
| lymphocyte proliferation | biological process | The expansion of a lymphocyte population by cell division. [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 phosphatidylinositol 3-kinase/protein kinase B signal transduction | biological process | Any process that activates or increases the frequency, rate or extent of phosphatidylinositol 3-kinase/protein kinase B signal transduction. [GOC:ai] |
| cellular response to cytokine 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 cytokine stimulus. [GOC:mah] |
| cellular response to glucocorticoid 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 glucocorticoid stimulus. Glucocorticoids are hormonal C21 corticosteroids synthesized from cholesterol with the ability to bind with the cortisol receptor and trigger similar effects. Glucocorticoids act primarily on carbohydrate and protein metabolism, and have anti-inflammatory effects. [GOC:mah] |
| dendritic cell differentiation | biological process | The process in which a precursor cell type acquires the specialized features of a dendritic cell. A dendritic cell is a leukocyte of dendritic lineage specialized in the uptake, processing, and transport of antigens to lymph nodes for the purpose of stimulating an immune response via T cell activation. [CL:0000451, GOC:pr] |
| positive regulation of kinase activity | biological process | Any process that activates or increases the frequency, rate or extent of kinase activity, the catalysis of the transfer of a phosphate group, usually from ATP, to a substrate molecule. [GOC:mah] |
| multicellular organism development | biological process | The biological process whose specific outcome is the progression of a multicellular organism over time from an initial condition (e.g. a zygote or a young adult) to a later condition (e.g. a multicellular animal or an aged adult). [GOC:dph, GOC:ems, GOC:isa_complete, GOC:tb] |