Binding Site Information of Target
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T74312 | Target Info | |||
| Target Name | Fms-like tyrosine kinase 3 (FLT-3) | ||||
| Synonyms | Stem cell tyrosine kinase 1; STK1; STK-1; Receptor-type tyrosine-protein kinase FLT3; Fetal liver kinase-2; FLT-3; FLK2; FLK-2; FL cytokine receptor; CD135 | ||||
| Target Type | Successful Target | ||||
| Gene Name | FLT3 | ||||
| Biochemical Class | Kinase | ||||
| UniProt ID | |||||
| Drug Binding Sites of Target | Top | |||||
|---|---|---|---|---|---|---|
| Ligand Name: Gilteritinib | Ligand Info | |||||
| Structure Description | Crystal structure of FLT3 in complex with gilteritinib | PDB:6JQR | ||||
| Method | X-ray diffraction | Resolution | 2.20 Å | Mutation | No | [1] |
| PDB Sequence |
RYESQLQMVQ
580 VTGSSDNEYF590 YVDFREYEYD600 LKWEFPRENL610 EFGKVLGSGA620 FGKVMNATAY 630 GISVSIQVAV643 KMLKEDSSER655 EALMSELKMM665 TQLGSHENIV675 NLLGACTLSG 685 PIYLIFEYCC695 YGDLLNYLRS705 KREKFSNVLT784 FEDLLCFAYQ794 VAKGMEFLEF 804 KSCVHRDLAA814 RNVLVTHGKV824 VKICDFMSDS840 NYVVRGNARL850 PVKWMAPESL 860 FEGIYTIKSD870 VWSYGILLWE880 IFSLGVNPYP890 GIPVDANFYK900 LIQNGFKMDQ 910 PFYATEEIYI920 IMQSCWAFDS930 RKRPSFPNLT940 SFLGCQLADA950 E |
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| Ligand Name: AC220 | Ligand Info | |||||
| Structure Description | Crystal Structure of FLT3 with a small molecule inhibitor | PDB:4RT7 | ||||
| Method | X-ray diffraction | Resolution | 3.10 Å | Mutation | No | [2] |
| PDB Sequence |
YDLKWEFPRE
608 NLEFGKVLGS618 GAFGKVMNAT628 AYGISGVSIQ640 VAVKMLKDSS653 EREALMSELK 663 MMTQLGSHEN673 IVNLLGACTL683 SGPIYLIFEY693 CCYGDLLNYL703 RSKRNVLTFE 786 DLLCFAYQVA796 KGMEFLEFKS806 CVHRDLAARN816 VLVTHGKVVK826 ICDFGLARDI 836 MSDSNYVVRG846 NARLPVKWMA856 PESLFEGIYT866 IKSDVWSYGI876 LLWEIFSLGV 886 NPYPGIPVDA896 NFYKLIQNGF906 KMDQPFYATE916 EIYIIMQSCW926 AFDSRKRPSF 936 PNLTSFLGCQ946 LADA
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LYS614
3.931
LEU616
3.618
VAL624
4.059
ALA642
3.482
LYS644
3.460
GLU661
2.840
MET664
4.588
MET665
3.715
LEU668
3.595
ILE674
4.579
VAL675
3.915
PHE691
3.593
GLU692
4.562
TYR693
3.410
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| Click to View More Binding Site Information of This Target and Ligand Pair | ||||||
| Ligand Name: FF-10101 | Ligand Info | |||||
| Structure Description | Crystal structure of the FLT3 kinase domain bound to the inhibitor FF-10101 | PDB:5X02 | ||||
| Method | X-ray diffraction | Resolution | 2.40 Å | Mutation | No | [3] |
| PDB Sequence |
ESQLQMVQVT
582 GSSDNEYFYV592 DFREYEYDLK602 WEFPRENLEF612 GKVLGSGAFG622 KVMNATAYGI 632 SKTGVSIQVA642 VKMLKEKADS652 SEREALMSEL662 KMMTQLGSHE672 NIVNLLGACT 682 LSGPIYLIFE692 YCCYGDLLNY702 LRSKREKFSV782 LTFEDLLCFA792 YQVAKGMEFL 802 EFKSCVHRDL812 AARNVLVTHG822 KVVKICDFGL832 ARDIMSDSNY842 VVRGNARLPV 852 KWMAPESLFE862 GIYTIKSDVW872 SYGILLWEIF882 SLGVNPYPGI892 PVDANFYKLI 902 QNGFKMDQPF912 YATEEIYIIM922 QSCWAFDSRK932 RPSFPNLTSF942 LGCQL |
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Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .F6M or .F6M2 or .F6M3 or :3F6M;style chemicals stick;color identity;select .A:616 or .A:617 or .A:624 or .A:642 or .A:644 or .A:661 or .A:675 or .A:691 or .A:692 or .A:693 or .A:694 or .A:695 or .A:696 or .A:697 or .A:698 or .A:818 or .A:821 or .A:828 or .A:829 or .A:830; color #00ffc7; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
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LEU616
3.574
GLY617
4.482
VAL624
3.581
ALA642
3.328
LYS644
3.240
GLU661
4.724
VAL675
3.474
PHE691
3.494
GLU692
3.506
TYR693
3.626
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| Ligand Name: 7-Methoxy-6-(1-methylpyrazol-4-yl)-3-pyridin-2-ylimidazo[1,2-a]pyridine | Ligand Info | |||||
| Structure Description | Crystal structure of the FLT3 kinase bound to a small molecule inhibitor | PDB:6IL3 | ||||
| Method | X-ray diffraction | Resolution | 2.50 Å | Mutation | No | [4] |
| PDB Sequence |
QFRYESQLQM
578 VQVTGSSDNE588 YFYVDFREYE598 YDLKWEFPRE608 NLEFGKVLGS618 GAFGKVMNAT 628 AYGISKTGVS638 IQVAVKMLKE648 KADSSEREAL658 MSELKMMTQL668 GSHENIVNLL 678 GACTLSGPIY688 LIFEYCCYGD698 LLNYLRSKRE708 KFSNVLTFED787 LLCFAYQVAK 797 GMEFLEFKSC807 VHRDLAARNV817 LVTHGKVVKI827 CDFGLARDIM837 SDSNYVVRGN 847 ARLPVKWMAP857 ESLFEGIYTI867 KSDVWSYGIL877 LWEIFSLGVN887 PYPGIPVDAN 897 FYKLIQNGFK907 MDQPFYATEE917 IYIIMQSCWA927 FDSRKRPSFP937 NLTSFLGCQL 947
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Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .A9R or .A9R2 or .A9R3 or :3A9R;style chemicals stick;color identity;select .A:614 or .A:616 or .A:617 or .A:624 or .A:642 or .A:644 or .A:675 or .A:691 or .A:692 or .A:693 or .A:694 or .A:695 or .A:697 or .A:698 or .A:701 or .A:818 or .A:828 or .A:829 or .A:830; color #f3c393; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
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| Ligand Name: 3-Cyclohexyl-1-propylsulfonic acid | Ligand Info | |||||
| Structure Description | Crystal structure of FLT3 in complex with gilteritinib | PDB:6JQR | ||||
| Method | X-ray diffraction | Resolution | 2.20 Å | Mutation | No | [1] |
| PDB Sequence |
RYESQLQMVQ
580 VTGSSDNEYF590 YVDFREYEYD600 LKWEFPRENL610 EFGKVLGSGA620 FGKVMNATAY 630 GISVSIQVAV643 KMLKEDSSER655 EALMSELKMM665 TQLGSHENIV675 NLLGACTLSG 685 PIYLIFEYCC695 YGDLLNYLRS705 KREKFSNVLT784 FEDLLCFAYQ794 VAKGMEFLEF 804 KSCVHRDLAA814 RNVLVTHGKV824 VKICDFMSDS840 NYVVRGNARL850 PVKWMAPESL 860 FEGIYTIKSD870 VWSYGILLWE880 IFSLGVNPYP890 GIPVDANFYK900 LIQNGFKMDQ 910 PFYATEEIYI920 IMQSCWAFDS930 RKRPSFPNLT940 SFLGCQLADA950 E |
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Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .CXS or .CXS2 or .CXS3 or :3CXS;style chemicals stick;color identity;select .A:704 or .A:707 or .A:885 or .A:886 or .A:887; color #00ffc7; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
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| Click to View More Binding Site Information of This Target and Ligand Pair | ||||||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Effect of Fms-like tyrosine kinase 3 (FLT3) ligand (FL) on antitumor activity of gilteritinib, a FLT3 inhibitor, in mice xenografted with FL-overexpressing cells. Oncotarget. 2019 Oct 22;10(58):6111-6123. | ||||
| REF 2 | Characterizing and Overriding the Structural Mechanism of the Quizartinib-Resistant FLT3 "Gatekeeper" F691L Mutation with PLX3397. Cancer Discov. 2015 Jun;5(6):668-79. | ||||
| REF 3 | A novel irreversible FLT3 inhibitor, FF-10101, shows excellent efficacy against AML cells with FLT3 mutations. Blood. 2018 Jan 25;131(4):426-438. | ||||
| REF 4 | Crystal structure of the FLT3 kinase bound to a small molecule inhibitor | ||||
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