colony stimulating factor 1 receptor | Type III RTKs: PDGFR, CSFR, Kit, FLT3 receptor family | IUPHAR Guide to IMMUNOPHARMACOLOGY

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colony stimulating factor 1 receptor

  Target has curated data in GtoImmuPdb

Target id: 1806

Nomenclature: colony stimulating factor 1 receptor

Abbreviated Name: CSFR

Family: Type III RTKs: PDGFR, CSFR, Kit, FLT3 receptor family

Annotation status:  image of an orange circle Annotated and awaiting review. Please contact us if you can help with reviewing.  » Email us

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 1 972 5q32 CSF1R colony stimulating factor 1 receptor
Mouse 1 977 18 D Csf1r colony stimulating factor 1 receptor
Rat 1 1022 18 q12.1 Csf1r colony stimulating factor 1 receptor
Previous and Unofficial Names
CD115 | C-FMS | CSF-1 receptor | Csfmr | Fim-2 | macrophage colony-stimulating factor 1 receptor | McDonough feline sarcoma viral (v-fms) oncogene homolog | M-CSFR
Database Links
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
RefSeq Nucleotide
RefSeq Protein
Selected 3D Structures
Image of receptor 3D structure from RCSB PDB
Description:  cFMS tyrosine kinase (tie2 KID) in complex with an arylamide inhibitor
PDB Id:  2I1M
Resolution:  1.8Å
Species:  Human
References:  30
Image of receptor 3D structure from RCSB PDB
Description:  Crystal structure of FMS KINASE domain with a small molecular inhibitor, PLX3397.
PDB Id:  4R7H
Ligand:  pexidartinib
Resolution:  2.8Å
Species:  Human
References:  33
Enzyme Reaction
EC Number:
Natural/Endogenous Ligands
G-CSF {Sp: Human}
GM-CSF {Sp: Human}
IL-34 {Sp: Human}
M-CSF {Sp: Human}

Download all structure-activity data for this target as a CSV file

Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
Ki-20227 Hs Inhibition 9.1 pKd 10
pKd 9.1 (Kd 8.3x10-10 M) [10]
AC710 Hs Inhibition 8.8 pKd 24
pKd 8.8 (Kd 1.57x10-9 M) [24]
GW-2580 Hs Inhibition 8.7 pKd 10
pKd 8.7 (Kd 2.2x10-9 M) [10]
JNJ-28312141 Hs Inhibition 8.5 pKd 10
pKd 8.5 (Kd 3.2x10-9 M) [10]
quizartinib Hs Inhibition 7.9 pKd 6
pKd 7.9 (Kd 1.2x10-8 M) [6]
crenolanib Hs Inhibition 7.5 pKd 20
pKd 7.5 (Kd 3x10-8 M) [20]
JNJ-28312141 Hs Inhibition 9.2 pIC50 25
pIC50 9.2 (IC50 6.9x10-10 M) [25]
compound 29 [PMID: 31934767] Hs Inhibition 9.1 pIC50 39
pIC50 9.1 (IC50 7x10-10 M) [39]
Description: Determined in an ELISA assay detecting tyrosine phosphorylation using immobilised recombinant CSF-1R protein.
BLZ945 Hs Inhibition 9.0 pIC50 32
pIC50 9.0 (IC50 1x10-9 M) [32]
Ki-20227 Hs Inhibition 8.7 pIC50 28
pIC50 8.7 (IC50 2x10-9 M) [28]
GR-389988 Hs Inhibition 8.7 pIC50 21
pIC50 8.7 (IC50 2x10-9 M) [21]
Description: In a biochemical assay measuring inhibition of peptide substrate phosphorylation by the test compound in the presence ot recombinant human c-FMS.
linifanib Hs Inhibition 8.5 pIC50 2
pIC50 8.5 (IC50 3x10-9 M) [2]
ilorasertib Hs Inhibition 8.5 pIC50 17
pIC50 8.5 (IC50 3x10-9 M) [17]
Description: Measuring inhibition of kinase activity in a biochemical assay.
edicotinib Hs Inhibition 8.5 pIC50 16
pIC50 8.5 (IC50 3.2x10-9 M) [16]
cerdulatinib Hs Inhibition 8.3 pIC50 7
pIC50 8.3 (IC50 5x10-9 M) [7]
AZD6495 Hs Inhibition 8.2 pIC50 31
pIC50 8.2 (IC50 6x10-9 M) [31]
CS2164 Hs Inhibition 8.1 pIC50 40
pIC50 8.1 (IC50 7x10-9 M) [40]
ARRY-382 Hs Inhibition 8.1 pIC50 4
pIC50 8.1 (IC50 9x10-9 M) [4]
dovitinib Hs Inhibition 7.4 – 8.5 pIC50 29,34
pIC50 7.4 – 8.5 (IC50 3.6x10-8 – 3x10-9 M) [29,34]
pexidartinib Hs Inhibition 7.9 pIC50 33
pIC50 7.9 (IC50 1.3x10-8 M) [33]
OSI-930 Hs Inhibition 7.8 pIC50 15
pIC50 7.8 (IC50 1.5x10-8 M) [15]
CHMFL-KIT-64 Hs Inhibition 7.7 pIC50 38
pIC50 7.7 (IC50 1.8x10-8 M) [38]
Description: In a biochemical assay.
TG02 Hs Inhibition 7.6 pIC50 18
pIC50 7.6 (IC50 2.7x10-8 M) [18]
CC-223 Hs Inhibition 7.6 pIC50 26
pIC50 7.6 (IC50 2.8x10-8 M) [26]
GW-2580 Hs Inhibition 7.2 pIC50 8
pIC50 7.2 (IC50 6x10-8 M) [8]
cediranib Hs Inhibition 7.0 pIC50 35
pIC50 7.0 (IC50 1.1x10-7 M) [35]
pazopanib Hs Inhibition 6.8 pIC50 19
pIC50 6.8 (IC50 1.46x10-7 M) [19]
GTP-14564 Hs Inhibition 6.5 pIC50 27
pIC50 6.5 (IC50 3x10-7 M) [27]
tandutinib Hs Inhibition 5.5 pIC50 22
pIC50 5.5 (IC50 3.43x10-6 M) [22]
Key to terms and symbols Click column headers to sort
Ligand Sp. Action Value Parameter Reference
IL-34 {Sp: Human} Hs Agonist - - 23
Key to terms and symbols Click column headers to sort
Antibody Sp. Action Value Parameter Reference
emactuzumab Hs Binding 9.5 pKd 11
pKd 9.5 (Kd 2.9x10-10 M) [11]
Description: Affinity data measured by surface plasmon resonance.
AMG820 Hs Binding >9.3 pKd 5
pKd >9.3 (Kd <5.5x10-10 M) [5]
cabiralizumab Hs Binding >9.0 pKd 37
pKd >9.0 (Kd <1x10-9 M) [37]
LY3022855 Hs Binding 10.1 pEC50 12
pEC50 10.1 (EC50 9x10-11 M) [12]
Description: Measured in an ELISA binding assay.
DiscoveRx KINOMEscan® screen
A screen of 72 inhibitors against 456 human kinases. Quantitative data were derived using DiscoveRx KINOMEscan® platform.
Reference: 10,36

Key to terms and symbols Click column headers to sort
Target used in screen: CSF1R
Ligand Sp. Type Action Value Parameter
dasatinib Hs Inhibitor Inhibition 9.2 pKd
PD-173955 Hs Inhibitor Inhibition 9.2 pKd
Ki-20227 Hs Inhibitor Inhibition 9.1 pKd
foretinib Hs Inhibitor Inhibition 8.7 pKd
GW-2580 Hs Inhibitor Inhibition 8.7 pKd
sunitinib Hs Inhibitor Inhibition 8.6 pKd
JNJ-28312141 Hs Inhibitor Inhibition 8.5 pKd
linifanib Hs Inhibitor Inhibition 8.5 pKd
SU-14813 Hs Inhibitor Inhibition 8.4 pKd
tandutinib Hs Inhibitor Inhibition 8.3 pKd
Target used in screen: CSF1R-autoinhibited
Ligand Sp. Type Action Value Parameter
dasatinib Hs Inhibitor Inhibition 9.0 pKd
staurosporine Hs Inhibitor Inhibition 8.6 pKd
sunitinib Hs Inhibitor Inhibition 8.4 pKd
PD-173955 Hs Inhibitor Inhibition 7.8 pKd
Ki-20227 Hs Inhibitor Inhibition 7.7 pKd
GW-2580 Hs Inhibitor Inhibition 7.6 pKd
midostaurin Hs Inhibitor Inhibition 6.7 pKd
lestaurtinib Hs Inhibitor Inhibition 6.2 pKd
quizartinib Hs Inhibitor Inhibition 6.0 pKd
bosutinib Hs Inhibitor Inhibition 6.0 pKd
Displaying the top 10 most potent ligands  View all ligands in screen »
EMD Millipore KinaseProfilerTM screen/Reaction Biology Kinase HotspotSM screen
A screen profiling 158 kinase inhibitors (Calbiochem Protein Kinase Inhibitor Library I and II, catalogue numbers 539744 and 539745) for their inhibitory activity at 1µM and 10µM against 234 human recombinant kinases using the EMD Millipore KinaseProfilerTM service.

A screen profiling the inhibitory activity of 178 commercially available kinase inhibitors at 0.5µM against a panel of 300 recombinant protein kinases using the Reaction Biology Corporation Kinase HotspotSM platform.

Reference: 3,14

Key to terms and symbols Click column headers to sort
Target used in screen: Fms/FMS
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
dasatinib Hs Inhibitor Inhibition 0.8
staurosporine Hs Inhibitor Inhibition 1.8 0.5 0.0
sorafenib Hs Inhibitor Inhibition 5.6
Cdk2 inhibitor IV Hs Inhibitor Inhibition 5.7 1.0 2.0
midostaurin Hs Inhibitor Inhibition 6.6 0.0 1.0
sunitinib Hs Inhibitor Inhibition 7.3
SU11652 Hs Inhibitor Inhibition 7.4 0.0 0.0
masitinib Hs Inhibitor Inhibition 8.4
PDGF RTK inhibitor Hs Inhibitor Inhibition 10.5 0.0 -1.0
Cdk1/2 inhibitor III Hs Inhibitor Inhibition 10.6 5.0 0.0
Displaying the top 10 most potent ligands  View all ligands in screen »
Immunopharmacology Comments
Activation of the CSF1R induces myeloid proliferation, and in the tumour microenvironment this promotes M1 to M2 polarization and accumulation of tumour-associated macrophages (TAMs). The CSF1R is therefore being investigated as an immuno-oncology drug target [1]. It is the primary target of several in development tyrosine kinase inhibitors such as pexidartinib, GW-2580 and BLZ945, and the investigational monoclonal antibodies AMG820, LY3022855 and cabiralizumab (FPA-008).
Cell Type Associations
Immuno Cell Type:  Other T cells
Comment:  Expression down-regulated in response to HMB-PP or OKT-3 activation
References:  9
Immuno Cell Type:  Natural killer cells
Comment:  Down-regulated expression measured by Affymetrix GeneChip array, in experiments designed to expand NK cell populations as a potential cancer immunotherapy tool.
References:  13
Immuno Process Associations
Immuno Process:  Inflammation
GO Annotations:  Associated to 2 GO processes
GO:0006954 inflammatory response TAS
click arrow to show/hide IEA associations
GO:0045087 innate immune response IEA
Immuno Process:  Immune system development
GO Annotations:  Associated to 6 GO processes
GO:0002244 hematopoietic progenitor cell differentiation IBA
GO:0030097 hemopoiesis IMP
GO:0030224 monocyte differentiation TAS
GO:0030225 macrophage differentiation TAS
GO:0030316 osteoclast differentiation ISS
GO:0045672 positive regulation of osteoclast differentiation ISO
Immuno Process:  Cytokine production & signalling
GO Annotations:  Associated to 6 GO processes
GO:0005011 macrophage colony-stimulating factor receptor activity IMP
GO:0019221 cytokine-mediated signaling pathway IMP
GO:0036006 cellular response to macrophage colony-stimulating factor stimulus IMP
GO:0038145 macrophage colony-stimulating factor signaling pathway ISS
GO:0071345 cellular response to cytokine stimulus ISS
GO:0090197 positive regulation of chemokine secretion IMP
Immuno Process:  Chemotaxis & migration
GO Annotations:  Associated to 1 GO processes
GO:0090197 positive regulation of chemokine secretion IMP
Immuno Process:  Immune regulation
GO Annotations:  Associated to 1 GO processes
GO:0045672 positive regulation of osteoclast differentiation ISO
Clinically-Relevant Mutations and Pathophysiology
Disease:  Leukoencephalopathy, diffuse hereditary, with spheroids
Synonyms: Hereditary diffuse leukoencephalopathy with axonal spheroids and pigmented glia [Orphanet: ORPHA313808]
OMIM: 221820
Orphanet: ORPHA313808


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11. Dimoudis N, Fertig G, Fidler A, Pickl M, Ries C, Seeber S, Lanzendoerfer M, Krueger K. (2011) Antibodies against human csf-1r and uses thereof. Patent number: US20110165156 A1. Assignee: Dimoudis N, Fertig G, Fidler A, Pickl M, Ries C, Seeber S, Lanzendoerfer M, Krueger K.. Priority date: 10/12/2009. Publication date: 07/07/2011.

12. Doody JF, Li Y. (2011) Antibodies against csf-1r. Patent number: WO2011123381 A1. Assignee: Imclone Llc. Priority date: 01/04/2010. Publication date: 06/10/2011.

13. Fujisaki H, Kakuda H, Shimasaki N, Imai C, Ma J, Lockey T, Eldridge P, Leung WH, Campana D. (2009) Expansion of highly cytotoxic human natural killer cells for cancer cell therapy. Cancer Res., 69 (9): 4010-7. [PMID:19383914]

14. Gao Y, Davies SP, Augustin M, Woodward A, Patel UA, Kovelman R, Harvey KJ. (2013) A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. Biochem. J., 451 (2): 313-28. [PMID:23398362]

15. Garton AJ, Crew AP, Franklin M, Cooke AR, Wynne GM, Castaldo L, Kahler J, Winski SL, Franks A, Brown EN et al.. (2006) OSI-930: a novel selective inhibitor of Kit and kinase insert domain receptor tyrosine kinases with antitumor activity in mouse xenograft models. Cancer Res., 66 (2): 1015-24. [PMID:16424037]

16. Genovese MC, Hsia E, Belkowski SM, Chien C, Masterson T, Thurmond RL, Manthey CL, Yan XD, Ge T, Franks C et al.. (2015) Results from a Phase IIA Parallel Group Study of JNJ-40346527, an Oral CSF-1R Inhibitor, in Patients with Active Rheumatoid Arthritis despite Disease-modifying Antirheumatic Drug Therapy. J. Rheumatol., 42 (10): 1752-60. [PMID:26233509]

17. Glaser KB, Li J, Marcotte PA, Magoc TJ, Guo J, Reuter DR, Tapang P, Wei RQ, Pease LJ, Bui MH et al.. (2012) Preclinical characterization of ABT-348, a kinase inhibitor targeting the aurora, vascular endothelial growth factor receptor/platelet-derived growth factor receptor, and Src kinase families. J. Pharmacol. Exp. Ther., 343 (3): 617-27. [PMID:22935731]

18. Goh KC, Novotny-Diermayr V, Hart S, Ong LC, Loh YK, Cheong A, Tan YC, Hu C, Jayaraman R, William AD et al.. (2012) TG02, a novel oral multi-kinase inhibitor of CDKs, JAK2 and FLT3 with potent anti-leukemic properties. Leukemia, 26 (2): 236-43. [PMID:21860433]

19. Harris PA, Boloor A, Cheung M, Kumar R, Crosby RM, Davis-Ward RG, Epperly AH, Hinkle KW, Hunter 3rd RN, Johnson JH et al.. (2008) Discovery of 5-[[4-[(2,3-dimethyl-2H-indazol-6-yl)methylamino]-2-pyrimidinyl]amino]-2-methyl-benzenesulfonamide (Pazopanib), a novel and potent vascular endothelial growth factor receptor inhibitor. J. Med. Chem., 51 (15): 4632-40. [PMID:18620382]

20. Heinrich MC, Griffith D, McKinley A, Patterson J, Presnell A, Ramachandran A, Debiec-Rychter M. (2012) Crenolanib inhibits the drug-resistant PDGFRA D842V mutation associated with imatinib-resistant gastrointestinal stromal tumors. Clin. Cancer Res., 18 (16): 4375-84. [PMID:22745105]

21. Kane JL Jr, Matthews G, Metz M, Kothe M, Liu J, Scholte A. (2015) Tropomyosin-related kinase (Trk) inhibitors. Patent number: US9174986B2. Assignee: Genzyme Corp.. Priority date: 10/12/2013. Publication date: 03/11/2015.

22. Kelly LM, Yu JC, Boulton CL, Apatira M, Li J, Sullivan CM, Williams I, Amaral SM, Curley DP, Duclos N et al.. (2002) CT53518, a novel selective FLT3 antagonist for the treatment of acute myelogenous leukemia (AML). Cancer Cell, 1 (5): 421-32. [PMID:12124172]

23. Lin H, Lee E, Hestir K, Leo C, Huang M, Bosch E, Halenbeck R, Wu G, Zhou A, Behrens D et al.. (2008) Discovery of a cytokine and its receptor by functional screening of the extracellular proteome. Science, 320 (5877): 807-11. [PMID:18467591]

24. Liu G, Campbell BT, Holladay MW, Ford Pulido JM, Hua H, Gitnick D, Gardner MF, James J, Breider MA, Brigham D et al.. (2012) Discovery of AC710, a Globally Selective Inhibitor of Platelet-Derived Growth Factor Receptor-Family Kinases. ACS Med Chem Lett, 3 (12): 997-1002. [PMID:24900421]

25. Manthey CL, Johnson DL, Illig CR, Tuman RW, Zhou Z, Baker JF, Chaikin MA, Donatelli RR, Franks CF, Zeng L et al.. (2009) JNJ-28312141, a novel orally active colony-stimulating factor-1 receptor/FMS-related receptor tyrosine kinase-3 receptor tyrosine kinase inhibitor with potential utility in solid tumors, bone metastases, and acute myeloid leukemia. Mol. Cancer Ther., 8 (11): 3151-61. [PMID:19887542]

26. Mortensen DS, Perrin-Ninkovic SM, Shevlin G, Zhao J, Packard G, Bahmanyar S, Correa M, Elsner J, Harris R, Lee BG et al.. (2015) Discovery of mammalian target of rapamycin (mTOR) kinase inhibitor CC-223. J. Med. Chem., 58 (13): 5323-33. [PMID:26083478]

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28. Ohno H, Kubo K, Murooka H, Kobayashi Y, Nishitoba T, Shibuya M, Yoneda T, Isoe T. (2006) A c-fms tyrosine kinase inhibitor, Ki20227, suppresses osteoclast differentiation and osteolytic bone destruction in a bone metastasis model. Mol. Cancer Ther., 5 (11): 2634-43. [PMID:17121910]

29. Renhowe PA, Pecchi S, Shafer CM, Machajewski TD, Jazan EM, Taylor C, Antonios-McCrea W, McBride CM, Frazier K, Wiesmann M et al.. (2009) 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. J. Med. Chem., 52 (2): 278-92. [PMID:19113866]

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32. Strachan DC, Ruffell B, Oei Y, Bissell MJ, Coussens LM, Pryer N, Daniel D. (2013) CSF1R inhibition delays cervical and mammary tumor growth in murine models by attenuating the turnover of tumor-associated macrophages and enhancing infiltration by CD8(+) T cells. Oncoimmunology, 2 (12): e26968. [PMID:24498562]

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37. Wong J, Vasquez M. (2011) Antibodies That Bind CSF1R. Patent number: US20110274683 A1. Assignee: Five Prime Therapeutics, Inc.. Priority date: 04/05/2010. Publication date: 10/11/2011.

38. Wu Y, Wang B, Wang J, Qi S, Zou F, Qi Z, Liu F, Liu Q, Chen C, Hu C et al.. (2019) Discovery of 2-(4-Chloro-3-(trifluoromethyl)phenyl)-N-(4-((6,7-dimethoxyquinolin-4-yl)oxy)phenyl)acetamide (CHMFL-KIT-64) as a Novel Orally Available Potent Inhibitor against Broad-Spectrum Mutants of c-KIT Kinase for Gastrointestinal Stromal Tumors. J. Med. Chem., 62 (13): 6083-6101. [PMID:31250638]

39. Xie Z, Wu B, Liu Y, Ren W, Tong L, Xiang C, Wei A, Gao Y, Zeng L, Xie H et al.. (2020) Novel Class of Colony-Stimulating Factor 1 Receptor Kinase Inhibitors Based on an o-Aminopyridyl Alkynyl Scaffold as Potential Treatment for Inflammatory Disorders. J. Med. Chem., 63 (3): 1397-1414. [PMID:31934767]

40. Zhou Y, Shan S, Li ZB, Xin LJ, Pan DS, Yang QJ, Liu YP, Yue XP, Liu XR, Gao JZ et al.. (2017) CS2164, a novel multi-target inhibitor against tumor angiogenesis, mitosis and chronic inflammation with anti-tumor potency. Cancer Sci., 108 (3): 469-477. [PMID:28004478]

How to cite this page

Type III RTKs: PDGFR, CSFR, Kit, FLT3 receptor family: colony stimulating factor 1 receptor. Last modified on 15/01/2020. Accessed on 11/08/2020. IUPHAR/BPS Guide to PHARMACOLOGY,