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colony stimulating factor 1 receptor

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Immunopharmacology Ligand  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

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 1 972 5q32 CSF1R colony stimulating factor 1 receptor
Mouse 1 977 18 34.41 cM Csf1r colony stimulating factor 1 receptor
Rat 1 978 18q12.1 Csf1r colony stimulating factor 1 receptor
Previous and Unofficial Names Click here for help
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 Click here for help
Alphafold P07333 (Hs), P09581 (Mm), Q00495 (Rn)
BRENDA 2.7.10.1
CATH/Gene3D 2.60.40.10
ChEMBL Target CHEMBL1844 (Hs), CHEMBL5570 (Mm)
Ensembl Gene ENSG00000182578 (Hs), ENSMUSG00000024621 (Mm), ENSRNOG00000018414 (Rn)
Entrez Gene 1436 (Hs), 12978 (Mm), 307403 (Rn)
Human Protein Atlas ENSG00000182578 (Hs)
KEGG Enzyme 2.7.10.1
KEGG Gene hsa:1436 (Hs), mmu:12978 (Mm), rno:307403 (Rn)
OMIM 164770 (Hs)
Orphanet ORPHA317674 (Hs)
Pharos P07333 (Hs)
RefSeq Nucleotide NM_005211 (Hs), NM_001037859 (Mm), NM_001029901 (Rn)
RefSeq Protein NP_005202 (Hs), NP_001032948 (Mm), NP_001025072 (Rn)
UniProtKB P07333 (Hs), P09581 (Mm), Q00495 (Rn)
Wikipedia CSF1R (Hs)
Selected 3D Structures Click here for help
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:  38
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:  41
Enzyme Reaction Click here for help
EC Number: 2.7.10.1
Natural/Endogenous Ligands Click here for help
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 go icon to follow link

Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
Ki-20227 Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Inhibition 9.1 pKd 15
⤷ pKd 9.1 (Kd 8.3x10-10 M) [15]
IACS-9439 Small molecule or natural product Click here for species-specific activity table Hs Inhibition 9.0 pKd 14
⤷ pKd 9.0 (Kd 1x10-9 M) [14]
AC710 Small molecule or natural product Click here for species-specific activity table Hs Inhibition 8.8 pKd 30
⤷ pKd 8.8 (Kd 1.57x10-9 M) [30]
GW-2580 Small molecule or natural product Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 8.7 pKd 15
⤷ pKd 8.7 (Kd 2.2x10-9 M) [15]
JNJ-28312141 Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Inhibition 8.5 pKd 15
⤷ pKd 8.5 (Kd 3.2x10-9 M) [15]
sotuletinib Small molecule or natural product Click here for species-specific activity table Immunopharmacology Ligand Hs Inhibition 8.5 pKd 14
⤷ pKd 8.5 (Kd 3.4x10-9 M) [14]
quizartinib Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 7.9 pKd 9
⤷ pKd 7.9 (Kd 1.2x10-8 M) [9]
crenolanib Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibition 7.5 pKd 25
⤷ pKd 7.5 (Kd 3x10-8 M) [25]
adrixetinib Small molecule or natural product Click here for species-specific activity table Hs Inhibition >7.0 pKd 34
⤷ pKd >7.0 (Kd <1x10-7 M) [34]
elzovantinib Small molecule or natural product Click here for species-specific activity table Hs Inhibition 9.9 pIC50 13
⤷ pIC50 9.9 (IC50 1.2x10-10 M) [13]
BPR1R024 Small molecule or natural product Click here for species-specific activity table Hs Inhibition 9.3 pIC50 28
⤷ pIC50 9.3 (IC50 5.3x10-10 M) [28]
JNJ-28312141 Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Inhibition 9.2 pIC50 31
⤷ pIC50 9.2 (IC50 6.9x10-10 M) [31]
compound 29 [PMID: 31934767] Small molecule or natural product Immunopharmacology Ligand Hs Inhibition 9.1 pIC50 47
⤷ pIC50 9.1 (IC50 7x10-10 M) [47]
Description: Determined in an ELISA assay detecting tyrosine phosphorylation using immobilised recombinant CSF-1R protein.
sotuletinib Small molecule or natural product Primary target of this compound Click here for species-specific activity table Immunopharmacology Ligand Hs Inhibition 9.0 pIC50 40
⤷ pIC50 9.0 (IC50 1x10-9 M) [40]
IACS-9439 Small molecule or natural product Click here for species-specific activity table Hs Inhibition 8.8 pIC50 14
⤷ pIC50 8.8 (IC50 1.7x10-9 M) [14]
Ki-20227 Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Inhibition 8.7 pIC50 35
⤷ pIC50 8.7 (IC50 2x10-9 M) [35]
GR-389988 Small molecule or natural product Click here for species-specific activity table Immunopharmacology Ligand Hs Inhibition 8.7 pIC50 26
⤷ pIC50 8.7 (IC50 2x10-9 M) [26]
Description: In a biochemical assay measuring inhibition of peptide substrate phosphorylation by the test compound in the presence ot recombinant human c-FMS.
linifanib Small molecule or natural product Click here for species-specific activity table Hs Inhibition 8.5 pIC50 3
⤷ pIC50 8.5 (IC50 3x10-9 M) [3]
ilorasertib Small molecule or natural product Click here for species-specific activity table Hs Inhibition 8.5 pIC50 22
⤷ pIC50 8.5 (IC50 3x10-9 M) [22]
Description: Measuring inhibition of kinase activity in a biochemical assay.
edicotinib Small molecule or natural product Primary target of this compound Click here for species-specific activity table Immunopharmacology Ligand Hs Inhibition 8.5 pIC50 21
⤷ pIC50 8.5 (IC50 3.2x10-9 M) [21]
segigratinib Small molecule or natural product Click here for species-specific activity table Hs Inhibition 8.4 pIC50 36
⤷ pIC50 8.4 (IC50 3.8x10-9 M) [36]
cerdulatinib Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibition 8.3 pIC50 10
⤷ pIC50 8.3 (IC50 5x10-9 M) [10]
M4205 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 8.3 pIC50 6
⤷ pIC50 8.3 (IC50 5.5x10-9 M) [6]
Description: Biochemical inhibitory potency
AZD6495 Small molecule or natural product Primary target of this compound Hs Inhibition 8.2 pIC50 39
⤷ pIC50 8.2 (IC50 6x10-9 M) [39]
vimseltinib Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition >8.0 – 8.4 pIC50 2,8
⤷ pIC50 8.4 (IC50 3.7x10-9 M) [8]
pIC50 >8.0 (IC50 <1x10-8 M) [2]
ibcasertib Small molecule or natural product Click here for species-specific activity table Hs Inhibition 8.1 pIC50 49
⤷ pIC50 8.1 (IC50 7x10-9 M) [49]
ARRY-382 Small molecule or natural product Immunopharmacology Ligand Hs Inhibition 8.1 pIC50 5
⤷ pIC50 8.1 (IC50 9x10-9 M) [5]
dovitinib Small molecule or natural product Click here for species-specific activity table Hs Inhibition 7.4 – 8.5 pIC50 37,42
⤷ pIC50 7.4 – 8.5 (IC50 3.6x10-8 – 3x10-9 M) [37,42]
pexidartinib Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 7.9 pIC50 41
⤷ pIC50 7.9 (IC50 1.3x10-8 M) [41]
OSI-930 Small molecule or natural product Click here for species-specific activity table Hs Inhibition 7.8 pIC50 20
⤷ pIC50 7.8 (IC50 1.5x10-8 M) [20]
CHMFL-KIT-64 Small molecule or natural product Click here for species-specific activity table Hs Inhibition 7.7 pIC50 46
⤷ pIC50 7.7 (IC50 1.8x10-8 M) [46]
Description: In a biochemical assay.
zotiraciclib Small molecule or natural product Click here for species-specific activity table Hs Inhibition 7.6 pIC50 23
⤷ pIC50 7.6 (IC50 2.7x10-8 M) [23]
onatasertib Small molecule or natural product Click here for species-specific activity table Hs Inhibition 7.6 pIC50 32
⤷ pIC50 7.6 (IC50 2.8x10-8 M) [32]
GW-2580 Small molecule or natural product Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 7.2 pIC50 11
⤷ pIC50 7.2 (IC50 6x10-8 M) [11]
cediranib Small molecule or natural product Click here for species-specific activity table Hs Inhibition 7.0 pIC50 43
⤷ pIC50 7.0 (IC50 1.1x10-7 M) [43]
pazopanib Small molecule or natural product Approved drug Click here for species-specific activity table Hs Inhibition 6.8 pIC50 24
⤷ pIC50 6.8 (IC50 1.46x10-7 M) [24]
GTP-14564 Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Inhibition 6.5 pIC50 33
⤷ pIC50 6.5 (IC50 3x10-7 M) [33]
pimicotinib Small molecule or natural product Hs Inhibition 6.3 pIC50 48
⤷ pIC50 6.3 (IC50 4.44x10-7 M) [48]
tandutinib Small molecule or natural product Click here for species-specific activity table Hs Inhibition 5.5 pIC50 27
⤷ pIC50 5.5 (IC50 3.43x10-6 M) [27]
Agonists
Key to terms and symbols Click column headers to sort
Ligand Sp. Action Value Parameter Reference
IL-34 {Sp: Human} Peptide Immunopharmacology Ligand Hs Agonist - - 29
⤷ [29]
Antibodies
Key to terms and symbols Click column headers to sort
Antibody Sp. Action Value Parameter Reference
emactuzumab Peptide Primary target of this compound Immunopharmacology Ligand Hs Binding 9.5 pKd 16
⤷ pKd 9.5 (Kd 2.9x10-10 M) [16]
Description: Affinity data measured by surface plasmon resonance.
AMG820 Peptide Primary target of this compound Immunopharmacology Ligand Hs Binding >9.3 pKd 7
⤷ pKd >9.3 (Kd <5.5x10-10 M) [7]
cabiralizumab Peptide Primary target of this compound Immunopharmacology Ligand Hs Binding >9.0 pKd 45
⤷ pKd >9.0 (Kd <1x10-9 M) [45]
LY3022855 Peptide Primary target of this compound Immunopharmacology Ligand Hs Binding 10.1 pEC50 17
⤷ pEC50 10.1 (EC50 9x10-11 M) [17]
Description: Measured in an ELISA binding assay.
DiscoveRx KINOMEscan® screen Click here for help
A screen of 72 inhibitors against 456 human kinases. Quantitative data were derived using DiscoveRx KINOMEscan® platform.
http://www.discoverx.com/services/drug-discovery-development-services/kinase-profiling/kinomescan
Reference: 15,44
Key to terms and symbols Click column headers to sort
Target used in screen: CSF1R
Ligand Sp. Type Action Value Parameter
dasatinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 9.2 pKd
PD-173955 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 9.2 pKd
Ki-20227 Small molecule or natural product Hs Inhibitor Inhibition 9.1 pKd
foretinib Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 8.7 pKd
GW-2580 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 8.7 pKd
sunitinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 8.6 pKd
JNJ-28312141 Small molecule or natural product Hs Inhibitor Inhibition 8.5 pKd
linifanib Small molecule or natural product Hs Inhibitor Inhibition 8.5 pKd
SU-14813 Small molecule or natural product Hs Inhibitor Inhibition 8.4 pKd
tandutinib Small molecule or natural product Hs Inhibitor Inhibition 8.3 pKd
Target used in screen: CSF1R-autoinhibited
Ligand Sp. Type Action Value Parameter
dasatinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 9.0 pKd
staurosporine Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 8.6 pKd
sunitinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 8.4 pKd
PD-173955 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.8 pKd
Ki-20227 Small molecule or natural product Hs Inhibitor Inhibition 7.7 pKd
GW-2580 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.6 pKd
midostaurin Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 6.7 pKd
lestaurtinib Small molecule or natural product Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 6.2 pKd
quizartinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 6.0 pKd
bosutinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand 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 Click here for help
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.

http://www.millipore.com/techpublications/tech1/pf3036
http://www.reactionbiology.com/webapps/main/pages/kinase.aspx

Reference: 4,19
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 Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 0.8
staurosporine Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 1.8 0.5 0.0
sorafenib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 5.6
Cdk2 inhibitor IV Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 5.7 1.0 2.0
midostaurin Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 6.6 0.0 1.0
sunitinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 7.3
SU11652 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.4 0.0 0.0
masitinib Small molecule or natural product Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 8.4
PDGF RTK inhibitor Small molecule or natural product Hs Inhibitor Inhibition 10.5 0.0 -1.0
Cdk1/2 inhibitor III Small molecule or natural product Ligand has a PDB structure 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:  12
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:  18
Immuno Process Associations
Immuno Process:  Inflammation
Immuno Process:  Immune system development
Immuno Process:  Cytokine production & signalling
Immuno Process:  Chemotaxis & migration
Immuno Process:  Immune regulation
Clinically-Relevant Mutations and Pathophysiology Click here for help
Disease:  Leukoencephalopathy, diffuse hereditary, with spheroids
Synonyms: Hereditary diffuse leukoencephalopathy with axonal spheroids and pigmented glia [Orphanet: ORPHA313808]
OMIM: 221820
Orphanet: ORPHA313808

References

Show »

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5. Bendell J et al.. A Phase 1 Study of ARRY-382, an Oral Inhibitor of Colony-stimulating Factor-1 Receptor (CSF1R), in Patients with Advanced or Metastatic Cancers. Accessed on 14/04/2016. Modified on 14/04/2016. Arraybiopharma.com, http://www.arraybiopharma.com/files/3014/4501/8593/382-101_AACR-NCI-EORTC_poster.pdf

6. Blum A, Dorsch D, Linde N, Brandstetter S, Buchstaller HP, Busch M, Glaser N, Grädler U, Ruff A, Petersson C et al.. (2023) Identification of M4205─A Highly Selective Inhibitor of KIT Mutations for Treatment of Unresectable Metastatic or Recurrent Gastrointestinal Stromal Tumors. J Med Chem, 66 (4): 2386-2395. [PMID:36728508]

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8. Caldwell TM, Ahn YM, Bulfer SL, Leary CB, Hood MM, Lu WP, Vogeti L, Vogeti S, Kaufman MD, Wise SC et al.. (2022) Discovery of vimseltinib (DCC-3014), a highly selective CSF1R switch-control kinase inhibitor, in clinical development for the treatment of Tenosynovial Giant Cell Tumor (TGCT). Bioorg Med Chem Lett, 74: 128928. [PMID:35961460]

9. 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]

10. Coffey G, Betz A, DeGuzman F, Pak Y, Inagaki M, Baker DC, Hollenbach SJ, Pandey A, Sinha U. (2014) The novel kinase inhibitor PRT062070 (Cerdulatinib) demonstrates efficacy in models of autoimmunity and B-cell cancer. J Pharmacol Exp Ther, 351 (3): 538-48. [PMID:25253883]

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12. Correia DV, d'Orey F, Cardoso BA, Lança T, Grosso AR, deBarros A, Martins LR, Barata JT, Silva-Santos B. (2009) Highly active microbial phosphoantigen induces rapid yet sustained MEK/Erk- and PI-3K/Akt-mediated signal transduction in anti-tumor human gammadelta T-cells. PLoS ONE, 4 (5): e5657. [PMID:19479075]

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14. Czako B, Marszalek JR, Burke JP, Mandal P, Leonard PG, Cross JB, Mseeh F, Jiang Y, Chang EQ, Suzuki E et al.. (2020) Discovery of IACS-9439, a Potent, Exquisitely Selective, and Orally Bioavailable Inhibitor of CSF1R. J Med Chem, 63 (17): 9888-9911. [PMID:32787110]

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17. 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.

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20. 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]

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How to cite this page

Type III RTKs: PDGFR, CSFR, Kit, FLT3 receptor family: colony stimulating factor 1 receptor. Last modified on 06/03/2024. Accessed on 19/04/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetoimmunopharmacology.org/GRAC/ObjectDisplayForward?objectId=1806.