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:  26
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:  29
Enzyme Reaction
EC Number:
Natural/Endogenous Ligands
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 Affinity Units Reference
Ki-20227 Hs Inhibition 9.1 pKd 10
pKd 9.1 (Kd 8.3x10-10 M) [10]
AC710 Hs Inhibition 8.8 pKd 20
pKd 8.8 (Kd 1.57x10-9 M) [20]
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 17
pKd 7.5 (Kd 3x10-8 M) [17]
JNJ-28312141 Hs Inhibition 9.2 pIC50 21
pIC50 9.2 (IC50 6.9x10-10 M) [21]
BLZ945 Hs Inhibition 9.0 pIC50 28
pIC50 9.0 (IC50 1x10-9 M) [28]
Ki-20227 Hs Inhibition 8.7 pIC50 24
pIC50 8.7 (IC50 2x10-9 M) [24]
linifanib Hs Inhibition 8.5 pIC50 2
pIC50 8.5 (IC50 3x10-9 M) [2]
JNJ-40346527 Hs Inhibition 8.5 pIC50 14
pIC50 8.5 (IC50 3.2x10-9 M) [14]
cerdulatinib Hs Inhibition 8.3 pIC50 7
pIC50 8.3 (IC50 5x10-9 M) [7]
AZD6495 Hs Inhibition 8.2 pIC50 27
pIC50 8.2 (IC50 6x10-9 M) [27]
ARRY-382 Hs Inhibition 8.1 pIC50 4
pIC50 8.1 (IC50 9x10-9 M) [4]
dovitinib Hs Inhibition 7.4 – 8.5 pIC50 25,30
pIC50 7.4 – 8.5 (IC50 3.6x10-8 – 3x10-9 M) [25,30]
pexidartinib Hs Inhibition 7.9 pIC50 29
pIC50 7.9 (IC50 1.3x10-8 M) [29]
TG02 Hs Inhibition 7.6 pIC50 15
pIC50 7.6 (IC50 2.7x10-8 M) [15]
CC-223 Hs Inhibition 7.6 pIC50 22
pIC50 7.6 (IC50 2.8x10-8 M) [22]
GW-2580 Hs Inhibition 7.2 pIC50 8
pIC50 7.2 (IC50 6x10-8 M) [8]
cediranib Hs Inhibition 7.0 pIC50 31
pIC50 7.0 (IC50 1.1x10-7 M) [31]
pazopanib Hs Inhibition 6.8 pIC50 16
pIC50 6.8 (IC50 1.46x10-7 M) [16]
GTP-14564 Hs Inhibition 6.5 pIC50 23
pIC50 6.5 (IC50 3x10-7 M) [23]
tandutinib Hs Inhibition 5.5 pIC50 18
pIC50 5.5 (IC50 3.43x10-6 M) [18]
Key to terms and symbols Click column headers to sort
Ligand Sp. Action Affinity Units Reference
IL-34 {Sp: Human} Hs Agonist - - 19
Key to terms and symbols Click column headers to sort
Antibody Sp. Action Affinity Units Reference
AMG820 Hs Binding >9.3 pKd 5
pKd >9.3 (Kd <5.5x10-10 M) [5]
cabiralizumab Hs Binding >9.0 pKd 33
pKd >9.0 (Kd <1x10-9 M) [33]
LY3022855 Hs Binding 10.1 pEC50 11
pEC50 10.1 (EC50 9x10-11 M) [11]
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: 10,32

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: 3,13

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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How to cite this page

Type III RTKs: PDGFR, CSFR, Kit, FLT3 receptor family: colony stimulating factor 1 receptor. Last modified on 03/08/2016. Accessed on 21/10/2016. IUPHAR/BPS Guide to PHARMACOLOGY,