colony stimulating factor 1 receptor

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
McDonough feline sarcoma viral (v-fms) oncogene homolog
CSF-1 receptor
macrophage colony-stimulating factor 1 receptor
Database Links
Ensembl Gene
Entrez Gene
GenitoUrinary Development Molecular Anatomy Project
Human Protein Reference Database
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:  15
Enzyme Reaction
EC Number:

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 Affinity Units Reference
Ki-20227 Hs Inhibition 9.1 pKd 5
pKd 9.1 (Kd 8.3x10-10 M) [5]
AC710 Hs Inhibition 8.8 pKd 10
pKd 8.8 (Kd 1.57x10-9 M) [10]
GW-2580 Hs Inhibition 8.7 pKd 5
pKd 8.7 (Kd 2.2x10-9 M) [5]
JNJ-28312141 Hs Inhibition 8.5 pKd 5
pKd 8.5 (Kd 3.2x10-9 M) [5]
quizartinib Hs Inhibition 7.9 pKd 3
pKd 7.9 (Kd 1.2x10-8 M) [3]
crenolanib Hs Inhibition 7.5 pKd 8
pKd 7.5 (Kd 3x10-8 M) [8]
JNJ-28312141 Hs Inhibition 9.2 pIC50 11
pIC50 9.2 (IC50 6.9x10-10 M) [11]
BLZ945 Hs Inhibition 9.0 pIC50 17
pIC50 9.0 (IC50 1x10-9 M) [17]
Ki-20227 Hs Inhibition 8.7 pIC50 13
pIC50 8.7 (IC50 2x10-9 M) [13]
linifanib Hs Inhibition 8.5 pIC50 1
pIC50 8.5 (IC50 3x10-9 M) [1]
AZD6495 Hs Inhibition 8.2 pIC50 16
pIC50 8.2 (IC50 6x10-9 M) [16]
dovitinib Hs Inhibition 7.4 – 8.5 pIC50 14,18
pIC50 7.4 – 8.5 (IC50 3.6x10-8 – 3x10-9 M) [14,18]
GW-2580 Hs Inhibition 7.2 pIC50 4
pIC50 7.2 (IC50 6x10-8 M) [4]
cediranib Hs Inhibition 7.0 pIC50 19
pIC50 7.0 (IC50 1.1x10-7 M) [19]
pazopanib Hs Inhibition 6.8 pIC50 7
pIC50 6.8 (IC50 1.46x10-7 M) [7]
GTP-14564 Hs Inhibition 6.5 pIC50 12
pIC50 6.5 (IC50 3x10-7 M) [12]
tandutinib Hs Inhibition 5.5 pIC50 9
pIC50 5.5 (IC50 3.43x10-6 M) [9]
DiscoveRx KINOMEscan® screen
A screen of 72 inhibitors against 456 human kinases. Quantitative data were derived using DiscoveRx KINOMEscan® platform.
Reference: 5,20

Key to terms and symbols Click column headers to sort
Target used in screen: CSF1R
Ligand Sp. Type Action Affinity Units
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 Affinity Units
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: 2,6

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 »
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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1. Albert DH, Tapang P, Magoc TJ, Pease LJ, Reuter DR, Wei RQ, Li J, Guo J, Bousquet PF, Ghoreishi-Haack NS et al.. (2006) Preclinical activity of ABT-869, a multitargeted receptor tyrosine kinase inhibitor. Mol. Cancer Ther.5 (4): 995-1006. [PMID:16648571]

2. Anastassiadis T, Deacon SW, Devarajan K, Ma H, Peterson JR. (2011) Comprehensive assay of kinase catalytic activity reveals features of kinase inhibitor selectivity. Nat. Biotechnol.29 (11): 1039-45. [PMID:22037377]

3. Chao Q, Sprankle KG, Grotzfeld RM, Lai AG, Carter TA, Velasco AM, Gunawardane RN, Cramer MD, Gardner MF, James J et al.. (2009) 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. J. Med. Chem.52 (23): 7808-16. [PMID:19754199]

4. Conway JG, McDonald B, Parham J, Keith B, Rusnak DW, Shaw E, Jansen M, Lin P, Payne A, Crosby RM et al.. (2005) Inhibition of colony-stimulating-factor-1 signaling in vivo with the orally bioavailable cFMS kinase inhibitor GW2580. Proc. Natl. Acad. Sci. U.S.A.102 (44): 16078-83. [PMID:16249345]

5. Davis MI, Hunt JP, Herrgard S, Ciceri P, Wodicka LM, Pallares G, Hocker M, Treiber DK, Zarrinkar PP. (2011) Comprehensive analysis of kinase inhibitor selectivity. Nat. Biotechnol.29 (11): 1046-51. [PMID:22037378]

6. 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]

7. 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]

8. 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]

9. 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 Cell1 (5): 421-32. [PMID:12124172]

10. 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 Lett3 (12): 997-1002. [PMID:24900421]

11. 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]

12. Murata K, Kumagai H, Kawashima T, Tamitsu K, Irie M, Nakajima H, Suzu S, Shibuya M, Kamihira S, Nosaka T et al.. (2003) Selective cytotoxic mechanism of GTP-14564, a novel tyrosine kinase inhibitor in leukemia cells expressing a constitutively active Fms-like tyrosine kinase 3 (FLT3). J. Biol. Chem.278 (35): 32892-8. [PMID:12815052]

13. 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]

14. 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]

15. Schubert C, Schalk-Hihi C, Struble GT, Ma HC, Petrounia IP, Brandt B, Deckman IC, Patch RJ, Player MR, Spurlino JC et al.. (2007) Crystal structure of the tyrosine kinase domain of colony-stimulating factor-1 receptor (cFMS) in complex with two inhibitors. J. Biol. Chem.282 (6): 4094-101. [PMID:17132624]

16. Scott DA, Bell KJ, Campbell CT, Cook DJ, Dakin LA, Del Valle DJ, Drew L, Gero TW, Hattersley MM, Omer CA et al.. (2009) 3-amido-4-anilinoquinolines as CSF-1R kinase inhibitors 2: Optimization of the PK profile. Bioorg. Med. Chem. Lett.19 (3): 701-5. [PMID:19114305]

17. 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. Oncoimmunology2 (12): e26968. [PMID:24498562]

18. Trudel S, Li ZH, Wei E, Wiesmann M, Chang H, Chen C, Reece D, Heise C, Stewart AK. (2005) CHIR-258, a novel, multitargeted tyrosine kinase inhibitor for the potential treatment of t(4;14) multiple myeloma. Blood105 (7): 2941-8. [PMID:15598814]

19. Wedge SR, Kendrew J, Hennequin LF, Valentine PJ, Barry ST, Brave SR, Smith NR, James NH, Dukes M, Curwen JO et al.. (2005) AZD2171: a highly potent, orally bioavailable, vascular endothelial growth factor receptor-2 tyrosine kinase inhibitor for the treatment of cancer. Cancer Res.65 (10): 4389-400. [PMID:15899831]

20. Wodicka LM, Ciceri P, Davis MI, Hunt JP, Floyd M, Salerno S, Hua XH, Ford JM, Armstrong RC, Zarrinkar PP et al.. (2010) Activation state-dependent binding of small molecule kinase inhibitors: structural insights from biochemistry. Chem. Biol.17 (11): 1241-9. [PMID:21095574]

How to cite this page

Type III RTKs: PDGFR, CSFR, Kit, FLT3 receptor family: colony stimulating factor 1 receptor. Last modified on 09/03/2015. Accessed on 07/10/2015. IUPHAR/BPS Guide to PHARMACOLOGY,