Binding Site Information of Target
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T20333 | Target Info | |||
| Target Name | Macrophage colony-stimulating factor 1 receptor (CSF1R) | ||||
| Synonyms | Proto-oncogene c-Fms; M-CSF-R; FMS; CSF-1R; CSF-1-R; CSF-1 receptor; CD115 | ||||
| Target Type | Successful Target | ||||
| Gene Name | CSF1R | ||||
| Biochemical Class | Kinase | ||||
| UniProt ID | |||||
| Drug Binding Sites of Target | Top | |||||
|---|---|---|---|---|---|---|
| Ligand Name: Imatinib | Ligand Info | |||||
| Structure Description | Crystal structure of FMS kinase domain with a small molecular inhibitor, GLEEVEC | PDB:4R7I | ||||
| Method | X-ray diffraction | Resolution | 2.75 Å | Mutation | Yes | [1] |
| PDB Sequence |
TQLPYNEKWE
576 FPRNNLQFGK586 TLGAGAFGKV596 VEATAFGLGK606 EDAVLKVAVK616 MLKSTAHADE 626 KEALMSELKI636 MSHLGQHENI646 VNLLGACTHG656 GPVLVITEYC666 TYGDLLNFLR 676 RKAEAMLGPS686 LSGRPLELRD754 LLHFSSQVAQ764 GMAFLASKNC774 IHRDVAARNV 784 LLTNGHVAKI794 GDFGLARDIM804 NDSNYIVKGN814 ARLPVKWMAP824 ESIFDSVYTV 834 QSDVWSYGIL844 LWEIFSLGLN854 PYPGILVNSK864 FYKLVKDGYQ874 MAQPAFAPKN 884 IYSIMQACWA894 LEPTHRPTFQ904 QITSFLQEQA914
|
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|
|
LEU588
3.904
VAL596
3.512
ALA614
3.781
VAL615
4.110
LYS616
3.473
GLU633
2.983
ILE636
4.242
MET637
3.600
LEU640
4.354
VAL647
3.814
VAL661
3.834
THR663
3.028
GLU664
4.110
|
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| Ligand Name: Pexidartinib | Ligand Info | |||||
| Structure Description | Crystal structure of FMS KINASE domain with a small molecular inhibitor, PLX3397 | PDB:4R7H | ||||
| Method | X-ray diffraction | Resolution | 2.80 Å | Mutation | Yes | [1] |
| PDB Sequence |
PKYQVRWKII
553 ESYTFIDPTQ568 LPYNEKWEFP578 RNNLQFGKTL588 GAGAFGKVVE598 ATAFGLGKED 608 AVLKVAVKML618 KSTAHADEKE628 ALMSELKIMS638 HLGQHENIVN648 LLGACTHGGP 658 VLVITEYCTY668 GDLLNFLRRK678 AEAMLGPSLG747 RPLELRDLLH757 FSSQVAQGMA 767 FLASKNCIHR777 DVAARNVLLT787 NGHVAKIGDF797 GLARDIMNDS807 NYIVKGNARL 817 PVKWMAPESI827 FDSVYTVQSD837 VWSYGILLWE847 IFSLGLNPYP857 GILVNSKFYK 867 LVKDGYQMAQ877 PAFAPKNIYS887 IMQACWALEP897 THRPTFQQIT907 SFLQEQAQ |
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VAL548
4.225
ARG549
3.782
TRP550
2.699
LEU588
3.694
VAL596
3.980
ALA614
3.361
LYS616
3.909
SER632
4.469
GLU633
3.016
ILE636
3.612
MET637
3.473
|
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| Ligand Name: DCC-3014 | Ligand Info | |||||
| Structure Description | Crystal structure of CSF1R in complex with vimseltinib | PDB:7MFC | ||||
| Method | X-ray diffraction | Resolution | 2.80 Å | Mutation | Yes | [2] |
| PDB Sequence |
TQLPYNEKWE
576 FPRNNLQFGK586 TLGAGAFGKV596 VEATAFGLGK606 EDAVLKVAVK616 MLKSTAHADE 626 KEALMSELKI636 MSHLGQHENI646 VNLLGACTHG656 GPVLVITEYC666 TYGDLLNFLR 676 RKAEAMLGPS686 LRPLELRDLL756 HFSSQVAQGM766 AFLASKNCIH776 RDVAARNVLL 786 TNGHVAKIGD796 FGLARDIMND806 SNYIVKGNAR816 LPVKWMAPES826 IFDSVYTVQS 836 DVWSYGILLW846 EIFSLGLNPY856 PGILVNSKFY866 KLVKDGYQMA876 QPAFAPKNIY 886 SIMQACWALE896 PTHRPTFQQI906 TSFLQEQ
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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 .Z6V or .Z6V2 or .Z6V3 or :3Z6V;style chemicals stick;color identity;select .A:588 or .A:596 or .A:614 or .A:616 or .A:633 or .A:636 or .A:637 or .A:640 or .A:647 or .A:663 or .A:664 or .A:665 or .A:666 or .A:667 or .A:668 or .A:669 or .A:769 or .A:774 or .A:776 or .A:785 or .A:794 or .A:795 or .A:796 or .A:797; color #00ffc7; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
|
LEU588
3.596
VAL596
3.641
ALA614
3.672
LYS616
3.454
GLU633
3.436
ILE636
4.890
MET637
3.558
LEU640
3.482
VAL647
4.059
THR663
3.459
GLU664
3.106
TYR665
3.697
|
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| Ligand Name: 6-Fluoro-N-((5-fluoro-2-methoxypyridin-3-yl)methyl)-5-((5-methyl-1H-pyrrolo[2,3-b]pyridin-3-yl)methyl)pyridin-2-amine | Ligand Info | |||||
| Structure Description | Crystal structure of fms kinase domain with a small molecular inhibitor, PLX5622 | PDB:6N33 | ||||
| Method | X-ray diffraction | Resolution | 2.25 Å | Mutation | Yes | [3] |
| PDB Sequence |
PTQLPYNEKW
575 EFPRNNLQFG585 KTLGAGAFGK595 VVEATAFGLG605 KEDAVLKVAV615 KMLKSTAHAD 625 EKEALMSELK635 IMSHLGQHEN645 IVNLLGACTH655 GGPVLVITEY665 CTYGDLLNFL 675 RRKAEAMLGP685 SLSGRPLELR753 DLLHFSSQVA763 QGMAFLASKN773 CIHRDVAARN 783 VLLTNGHVAK793 IGDFGLARDI803 MNDSNYIVKG813 NARLPVKWMA823 PESIFDSVYT 833 VQSDVWSYGI843 LLWEIFSLGL853 NPYPGILVNS863 KFYKLVKDGY873 QMAQPAFAPK 883 NIYSIMQACW893 ALEPTHRPTF903 QQITSFLQEQ913 AQ
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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 .622 or .6222 or .6223 or :3622;style chemicals stick;color identity;select .A:588 or .A:596 or .A:614 or .A:616 or .A:633 or .A:636 or .A:637 or .A:640 or .A:646 or .A:647 or .A:663 or .A:664 or .A:665 or .A:666 or .A:669 or .A:670 or .A:769 or .A:776 or .A:783 or .A:785 or .A:794 or .A:795 or .A:796 or .A:797; color #f3c393; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
|
LEU588
3.936
VAL596
4.066
ALA614
3.332
LYS616
3.529
GLU633
3.305
ILE636
4.883
MET637
3.515
LEU640
4.603
ILE646
4.417
VAL647
3.867
THR663
3.424
GLU664
2.805
|
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| Ligand Name: 5-[(5-Methoxy-1h-Pyrrolo[2,3-B]pyridin-3-Yl)methyl]-N-[4-(Trifluoromethyl)benzyl]pyridin-2-Amine | Ligand Info | |||||
| Structure Description | Crystal structure of FMS kinase domain with a small molecular inhibitor, PLX647-OME | PDB:4HW7 | ||||
| Method | X-ray diffraction | Resolution | 2.90 Å | Mutation | Yes | [4] |
| PDB Sequence |
PTQLPYNEKW
575 EFPRNNLQFG585 KTLGAGAFGK595 VVEATAFGLG605 KEDAVLKVAV615 KMLKSTAHAD 625 EKEALMSELK635 IMSHLGQHEN645 IVNLLGACTH655 GGPVLVITEY665 CTYGDLLNFL 675 RRKAEAMLGP685 SGRPLELRDL755 LHFSSQVAQG765 MAFLASKNCI775 HRDVAARNVL 785 LTNGHVAKIG795 DFGLARDIMN805 DSNYIVKGNA815 RLPVKWMAPE825 SIFDSVYTVQ 835 SDVWSYGILL845 WEIFSLGLNP855 YPGILVNSKF865 YKLVKDGYQM875 AQPAFAPKNI 885 YSIMQACWAL895 EPTHRPTFQQ905 ITSFLQEQA
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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 .64M or .64M2 or .64M3 or :364M;style chemicals stick;color identity;select .A:588 or .A:596 or .A:614 or .A:616 or .A:633 or .A:637 or .A:640 or .A:646 or .A:647 or .A:663 or .A:664 or .A:665 or .A:666 or .A:667 or .A:669 or .A:670 or .A:769 or .A:774 or .A:776 or .A:785 or .A:794 or .A:795 or .A:796 or .A:797; color #00ffc7; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
|
LEU588
3.710
VAL596
3.835
ALA614
3.421
LYS616
3.635
GLU633
3.186
MET637
3.892
LEU640
3.622
ILE646
4.075
VAL647
3.663
THR663
3.587
GLU664
2.635
TYR665
3.325
|
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| Ligand Name: 6-chloro-3-(3-methylisoxazol-5-yl)-4-phenylquinolin-2(1H)-one | Ligand Info | |||||
| Structure Description | c-FMS tyrosine kinase in complex with a quinolone inhibitor | PDB:2I0V | ||||
| Method | X-ray diffraction | Resolution | 2.80 Å | Mutation | No | [5] |
| PDB Sequence |
PKYQVRWKII
553 ESYEGNSYTF563 IDPTQLPYNE573 KWEFPRNNLQ583 FGKTLGAGAF593 GKVVEATAFG 603 LGKEDAVLKV613 AVKMLKSTAH623 ADEKEALMSE633 LKIMSHLGQH643 ENIVNLLGAC 653 THGGPVLVIT663 EYCCYGDLLN673 FLRRKRQLSS699 RDLLHFSSQV762 AQGMAFLASK 772 NCIHRDVAAR782 NVLLTNGHVA792 KIGDFGLARD802 IMNDSNYIVK812 GARLPVKWMA 823 PESIFDCVYT833 VQSDVWSYGI843 LLWEIFSLGL853 NPYPGILVNS863 KFYKLVKDGY 873 QMAQPAFAPK883 NIYSIMQACW893 ALEPTHRPTF903 QQICSFLQEQ913 AQE |
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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 .6C3 or .6C32 or .6C33 or :36C3;style chemicals stick;color identity;select .A:588 or .A:589 or .A:596 or .A:614 or .A:616 or .A:647 or .A:663 or .A:664 or .A:665 or .A:666 or .A:667 or .A:669 or .A:670 or .A:785 or .A:796 or .A:797 or .A:800 or .A:801; color #f3c393; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
|
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| Ligand Name: 5-Cyano-Furan-2-Carboxylic Acid [5-Hydroxymethyl-2-(4-Methyl-Piperidin-1-Yl)-Phenyl]-Amide | Ligand Info | |||||
| Structure Description | cFMS tyrosine kinase (tie2 KID) in complex with an arylamide inhibitor | PDB:2I1M | ||||
| Method | X-ray diffraction | Resolution | 1.80 Å | Mutation | No | [5] |
| PDB Sequence |
QVRWKIIESY
556 NSYTFIDPTQ568 LPYNEKWEFP578 RNNLQFGKTL588 GAGAFGKVVE598 ATAFGLGKED 608 AVLKVAVKML618 KSTAHADEKE628 ALMSELKIMS638 HLGQHENIVN648 LLGACTHGGP 658 VLVITEYCCY668 GDLLNFLRRK678 SRVLETDSTA697 STRDLLHFSS760 QVAQGMAFLA 770 SKNCIHRDVA780 ARNVLLTNGH790 VAKIGDFGLA800 RDIMNDSNYI810 VKGNARLPVK 820 WMAPESIFDC830 VYTVQSDVWS840 YGILLWEIFS850 LGLNPYPGIL860 VNSKFYKLVK 870 DGYQMAQPAF880 APKNIYSIMQ890 ACWALEPTHR900 PTFQQICSFL910 QEQAQEDRRE 920 R
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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 .5CN or .5CN2 or .5CN3 or :35CN;style chemicals stick;color identity;select .A:586 or .A:588 or .A:589 or .A:590 or .A:596 or .A:614 or .A:616 or .A:647 or .A:663 or .A:664 or .A:665 or .A:666 or .A:667 or .A:668 or .A:669 or .A:670 or .A:785 or .A:796 or .A:797 or .A:800 or .A:801; color #00ffc7; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
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LYS586
4.876
LEU588
3.125
GLY589
3.647
ALA590
4.984
VAL596
3.684
ALA614
3.473
LYS616
3.770
VAL647
3.842
THR663
3.295
GLU664
3.382
TYR665
2.775
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| Click to View More Binding Site Information of This Target and Ligand Pair | ||||||
| Ligand Name: 2-[(4-Methoxy-2-methyl-phenyl)amino]-7-methyl-9-(4-oxidanylcyclohexyl)purin-8-one | Ligand Info | |||||
| Structure Description | Crystal structure of the CSF1R kinase domain with a dihydropurinone inhibitor (compound 4) | PDB:6T2W | ||||
| Method | X-ray diffraction | Resolution | 1.70 Å | Mutation | No | [6] |
| PDB Sequence |
QVRWKIIESY
556 NSYTFIDPTQ568 LPYNEKWEFP578 RNNLQFGKTL588 GAGAFGKVVE598 ATAFGLGKED 608 AVLKVAVKML618 KSTAHADEKE628 ALMSELKIMS638 HLGQHENIVN648 LLGACTHGGP 658 VLVITEYCCY668 GDLLNFLRRK678 AEAMLRPLEL752 RDLLHFSSQV762 AQGMAFLASK 772 NCIHRDVAAR782 NVLLTNGHVA792 KIGDFGLARD802 IMNDSNYIVK812 GNARLPVKWM 822 APESIFDCVY832 TVQSDVWSYG842 ILLWEIFSLG852 LNPYPGILVN862 SKFYKLVKDG 872 YQMAQPAFAP882 KNIYSIMQAC892 WALEPTHRPT902 FQQICSFLQE912 QAQE |
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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 .M9T or .M9T2 or .M9T3 or :3M9T;style chemicals stick;color identity;select .A:588 or .A:589 or .A:596 or .A:614 or .A:616 or .A:647 or .A:663 or .A:664 or .A:665 or .A:666 or .A:667 or .A:669 or .A:670 or .A:782 or .A:785 or .A:797 or .A:800 or .A:801; color #f3c393; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
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| Ligand Name: (s)-4-(3-((2-(6-Methoxypyridin-3-yl)-2,3-dihydrobenzo[b][1,4]dioxin-6-yl)methyl)-3h-imidazo[4,5-b]pyridin-6-yl)-2-methylbut-3-yn-2-amine | Ligand Info | |||||
| Structure Description | CSF1R signaling is a regulator of pathogenesis in progressive MS | PDB:6WXJ | ||||
| Method | X-ray diffraction | Resolution | 2.62 Å | Mutation | No | [7] |
| PDB Sequence |
NSYTFIDPTQ
568 LPYNEKWEFP578 RNNLQFGKTL588 GAGAFGKVVE598 ATAFGLGKED608 AVLKVAVKML 618 KSTAHADEKE628 ALMSELKIMS638 HLGQHENIVN648 LLGACTHGGP658 VLVITEYCCY 668 GDLLNFLRRK678 SRDLLHFSSQ761 VAQGMAFLAS771 KNCIHRDVAA781 RNVLLTNGHV 791 AKIGDFGLAR801 DIMNDSNYIV811 KGLPVKWMAP824 ESIFDCVYTV834 QSDVWSYGIL 844 LWEFSLGLNP855 YPGILVNSKF865 YKLVKDGYQM875 AQPAFAPKNI885 YSIMQACWAL 895 EPTHRPTFQQ905 ICSFLQEQAQ915 ED
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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 .UF4 or .UF42 or .UF43 or :3UF4;style chemicals stick;color identity;select .A:586 or .A:588 or .A:596 or .A:614 or .A:616 or .A:633 or .A:637 or .A:640 or .A:646 or .A:647 or .A:663 or .A:664 or .A:665 or .A:666 or .A:667 or .A:668 or .A:669 or .A:769 or .A:774 or .A:776 or .A:785 or .A:794 or .A:795 or .A:796 or .A:797; color #00ffc7; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
|
LYS586
4.524
LEU588
3.642
VAL596
3.522
ALA614
3.611
LYS616
3.751
GLU633
3.703
MET637
3.885
LEU640
4.485
ILE646
4.712
VAL647
3.111
THR663
3.458
GLU664
3.190
TYR665
3.431
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| Ligand Name: N~3~-(2,6-Dichlorobenzyl)-5-(4-{[(2r)-2-(Pyrrolidin-1-Ylmethyl)pyrrolidin-1-Yl]carbonyl}phenyl)pyrazine-2,3-Diamine | Ligand Info | |||||
| Structure Description | Inhibitor Bound to A DFG-In structure of the Kinase Domain of CSF-1R | PDB:3LCD | ||||
| Method | X-ray diffraction | Resolution | 2.50 Å | Mutation | No | [8] |
| PDB Sequence |
GNSYTFIDPT
567 QLPYNEKWEF577 PRNNLQFGKT587 LGAGAFGKVV597 EATAFGLGKE607 DAVLKVAVKM 617 LKSTAHADEK627 EALMSELKIM637 SHLGQHENIV647 NLLGACTHGG657 PVLVITEYCC 667 YGDLLNFLRR677 KAEADLDPLE751 LRDLLHFSSQ761 VAQGMAFLAS771 KNCIHRDVAA 781 RNVLLTNGHV791 AKIGDFGLAR801 DIMSNYIVKG813 NARLPVKWMA823 PESIFDCVYT 833 VQSDVWSYGI843 LLWEIFSLGL853 NPYPGILVNS863 KFYKLVKDGY873 QMAQPAFAPK 883 NIYSIMQACW893 ALEPTHRPTF903 QQICSFLQEQ913
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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 .BDY or .BDY2 or .BDY3 or :3BDY;style chemicals stick;color identity;select .A:586 or .A:588 or .A:589 or .A:596 or .A:614 or .A:647 or .A:663 or .A:664 or .A:665 or .A:666 or .A:667 or .A:668 or .A:669 or .A:670 or .A:782 or .A:783 or .A:785 or .A:795 or .A:796; 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-{4-[(4-cyclopropylphenyl)methoxy]-3-methoxyphenyl}azetidin-1-yl)(4-{[(2S)-2,3-dihydroxypropoxy]methyl}pyridin-2-yl)methanone | Ligand Info | |||||
| Structure Description | Crystal structure of CSF-1R kinase domain with a small molecular inhibitor, JTE-952 | PDB:6IG8 | ||||
| Method | X-ray diffraction | Resolution | 1.80 Å | Mutation | Yes | [9] |
| PDB Sequence |
WKIIETFIDP
566 TQLPYNEKWE576 FPRNNLQFGK586 TLGAGAFGKV596 VEATAFGLGK606 EDAVLKVAVK 616 MLKSTAHADE626 KEALMSELKI636 MSHLGQHENI646 VNLLGACTHG656 GPVLVITEYC 666 CYGDLLNFLR676 RKAEAMLGPS686 LGRPLELRDL755 LHFSSQVAQG765 MAFLASKNCI 775 HRDVAARNVL785 LTNGHVAKIG795 DFGLARDIMN805 DSNYIVKGNA815 RLPVKWMAPE 825 SIFDCVYTVQ835 SDVWSYGILL845 WEIFSLGLNP855 YPGILVNSKF865 YKLVKDGYQM 875 AQPAFAPKNI885 YSIMQACWAL895 EPTHRPTFQQ905 ICSFLQEQAQ915 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 .A7O or .A7O2 or .A7O3 or :3A7O;style chemicals stick;color identity;select .A:550 or .A:588 or .A:596 or .A:614 or .A:616 or .A:633 or .A:636 or .A:637 or .A:640 or .A:647 or .A:663 or .A:664 or .A:665 or .A:666 or .A:667 or .A:668 or .A:669 or .A:670 or .A:769 or .A:774 or .A:776 or .A:783 or .A:785 or .A:794 or .A:795 or .A:796 or .A:797; color #00ffc7; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
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TRP550
3.560
LEU588
3.840
VAL596
3.994
ALA614
3.696
LYS616
3.737
GLU633
3.753
ILE636
4.250
MET637
3.475
LEU640
3.890
VAL647
3.833
THR663
3.464
GLU664
3.549
TYR665
3.456
CYS666
2.827
|
|||||
| Ligand Name: 3-({4-methoxy-5-[(4-methoxybenzyl)oxy]pyridin-2-yl}methoxy)-5-(1-methyl-1H-pyrazol-4-yl)pyrazin-2-amine | Ligand Info | |||||
| Structure Description | Inhibitor Bound to A DFG-Out structure of the Kinase Domain of CSF-1R | PDB:3LCO | ||||
| Method | X-ray diffraction | Resolution | 3.40 Å | Mutation | No | [8] |
| PDB Sequence |
KIIEFIDPTQ
568 LPYNEKWEFP578 RNNLQFGKTL588 GAGAFGKVVE598 ATAFGLGKED608 AVLKVAVKML 618 KSTAHADEKE628 ALMSELKIMS638 HLGQHENIVN648 LLGACTHGGP658 VLVITEYCCY 668 GDLLNFLRRK678 AEAMLGPSGR748 PLELRDLLHF758 SSQVAQGMAF768 LASKNCIHRD 778 VAARNVLLTN788 GHVAKIGDFG798 LARDIMNDSN808 YIVRLPVKWM822 APESIFDCVY 832 TVQSDVWSYG842 ILLWEIFSLG852 LNPYPGILVN862 SKFYKLVKDG872 YQMAQPAFAP 882 KNIYSIMQAC892 WALEPTHRPT902 FQQICSFLQE912 QAQ
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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 .LC0 or .LC02 or .LC03 or :3LC0;style chemicals stick;color identity;select .A:588 or .A:589 or .A:596 or .A:614 or .A:616 or .A:633 or .A:636 or .A:637 or .A:640 or .A:647 or .A:663 or .A:664 or .A:665 or .A:666 or .A:669 or .A:769 or .A:776 or .A:783 or .A:785 or .A:794 or .A:795 or .A:796 or .A:797; color #f3c393; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
|
LEU588
3.537
GLY589
4.776
VAL596
3.787
ALA614
3.248
LYS616
3.454
GLU633
3.260
ILE636
4.632
MET637
3.923
LEU640
3.769
VAL647
3.567
THR663
3.622
GLU664
2.346
|
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| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Structure-Guided Blockade of CSF1R Kinase in Tenosynovial Giant-Cell Tumor. N Engl J Med. 2015 Jul 30;373(5):428-37. | ||||
| REF 2 | Vimseltinib: A Precision CSF1R Therapy for Tenosynovial Giant Cell Tumors and Diseases Promoted by Macrophages. Mol Cancer Ther. 2021 Nov;20(11):2098-2109. | ||||
| REF 3 | Sustained microglial depletion with CSF1R inhibitor impairs parenchymal plaque development in an Alzheimer's disease model. Nat Commun. 2019 Aug 21;10(1):3758. | ||||
| REF 4 | Design and pharmacology of a highly specific dual FMS and KIT kinase inhibitor. Proc Natl Acad Sci U S A. 2013 Apr 2;110(14):5689-94. | ||||
| REF 5 | Crystal structure of the tyrosine kinase domain of colony-stimulating factor-1 receptor (cFMS) in complex with two inhibitors. J Biol Chem. 2007 Feb 9;282(6):4094-101. | ||||
| REF 6 | The Discovery of 7-Methyl-2-[(7-methyl[1,2,4]triazolo[1,5-a]pyridin-6-yl)amino]-9-(tetrahydro-2H-pyran-4-yl)-7,9-dihydro-8H-purin-8-one (AZD7648), a Potent and Selective DNA-Dependent Protein Kinase (DNA-PK) Inhibitor. J Med Chem. 2020 Apr 9;63(7):3461-3471. | ||||
| REF 7 | CSF1R signaling is a regulator of pathogenesis in progressive MS. Cell Death Dis. 2020 Oct 23;11(10):904. | ||||
| REF 8 | Structure-based drug design enables conversion of a DFG-in binding CSF-1R kinase inhibitor to a DFG-out binding mode. Bioorg Med Chem Lett. 2010 Mar 1;20(5):1543-7. | ||||
| REF 9 | Discovery of a novel azetidine scaffold for colony stimulating factor-1 receptor (CSF-1R) Type II inhibitors by the use of docking models. Bioorg Med Chem Lett. 2019 Jan 1;29(1):115-118. | ||||
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