Co-Target(s) Information

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Target General Information
Co-Targets of This Target
References
Target General Information  Top
Target ID T98913 Target Info
Target Name Granulocyte colony-stimulating factor receptor (G-CSF-R)
Synonyms
c-fms; GCSFR; GCSF receptor; G-CSF receptor; Fms proto-oncogene; CD114
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Target Type Successful Target
Gene Name CSF3R
Biochemical Class Cytokine receptor
UniProt ID
CSF3R_HUMAN
Co-Targets of This Target  Top
Co-Target Name Fms-like tyrosine kinase 3 (FLT-3) Successful Target
UniProt ID FLT3_HUMAN
Gene Name FLT3
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
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Representative Drug(s) Pexidartinib Drug Info IC50 = 5 nM [1]
Co-Target Name Tyrosine-protein kinase Kit (KIT) Successful Target
UniProt ID KIT_HUMAN
Gene Name KIT
Synonyms
v-kit Hardy-Zuckerman 4 feline sarcoma viral oncogene homolog; p145 c-kit; Proto-oncogene tyrosine-protein kinase Kit; Proto-oncogene c-Kit; Piebald trait protein; PBT; Mast/stem cell growth factor receptor Kit; CD117 antigen; CD117; C-kit
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Representative Drug(s) Pexidartinib Drug Info IC50 = 27 nM [2]
Co-Target Name Macrophage colony-stimulating factor 1 receptor (CSF1R) Clinical trial Target
UniProt ID CSF1R_HUMAN
Gene Name CSF1R
Synonyms
Proto-oncogene c-Fms; M-CSF-R; FMS; CSF-1R; CSF-1-R; CSF-1 receptor; CD115
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Representative Drug(s) BLZ-945 Drug Info IC50 = 1.2 nM Click to Show More [3]
2 Pexidartinib Drug Info IC50 = 10.8 nM [4]
References  Top
REF 1 Discovery of a Highly Potent and Selective Indenoindolone Type 1 Pan-FLT3 Inhibitor. ACS Med Chem Lett. 2016 Mar 8;7(5):476-81.
REF 2 Discovery and development of extreme selective inhibitors of the ITD and D835Y mutant FLT3 kinases. Eur J Med Chem. 2019 Dec 15;184:111710.
REF 3 Recent Advances of Colony-Stimulating Factor-1 Receptor (CSF-1R) Kinase and Its Inhibitors. J Med Chem. 2018 Jul 12;61(13):5450-66.
REF 4 Design, Synthesis, and Structure-Activity Relationship Study of 2-Oxo-3,4-dihydropyrimido[4,5- d]pyrimidines as New Colony Stimulating Factor 1 Receptor (CSF1R) Kinase Inhibitors. J Med Chem. 2018 Mar 22;61(6):2353-71.

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