platelet derived growth factor receptor beta | Type III RTKs: PDGFR, CSFR, Kit, FLT3 receptor family | IUPHAR/BPS Guide to PHARMACOLOGY

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platelet derived growth factor receptor beta

Target not currently curated in GtoImmuPdb

Target id: 1804

Nomenclature: platelet derived growth factor receptor beta

Abbreviated Name: PDGFRβ

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

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 1 1106 5q33.1 PDGFRB platelet derived growth factor receptor beta
Mouse 1 1099 18 Pdgfrb platelet derived growth factor receptor, beta polypeptide
Rat 1 1097 18q12.1 Pdgfrb platelet derived growth factor receptor beta
Previous and Unofficial Names
CD140b | JTK12 | PDGFR1 | PDGFR-beta | platelet-derived growth factor receptor beta polypeptide | platelet-derived growth factor receptor, beta polypeptide | platelet derived growth factor receptor, beta polypeptide | platelet derived growth factor receptor
Database Links
ChEMBL Target
DrugBank 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:  The structure of a platelet derived growth factor receptor complex
Resolution:  2.3Å
Species:  Human
References:  38
Enzyme Reaction
EC Number:
Endogenous ligands (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
CHMFL-KIT-64 Hs Inhibition 7.0 pIC50 46
pIC50 7.0 (IC50 9.7x10-8 M) [46]
Description: In a biochemical assay.
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
AC710 Hs Inhibition 9.0 pKd 22
pKd 9.0 (Kd 1x10-9 M) [22]
crenolanib Hs Inhibition 8.5 pKd 13
pKd 8.5 (Kd 3.2x10-9 M) [13]
quizartinib Hs Inhibition 8.1 pKd 4
pKd 8.1 (Kd 7.7x10-9 M) [4]
LXH254 Hs Inhibition 7.8 pKd 35
pKd 7.8 (Kd 1.4x10-8 M) [35]
Description: Binding affinity determined using the KinomeScan® platform.
compound 5e [PMID: 28580438] Hs Inhibition 7.6 pKd 17
pKd 7.6 (Kd 2.8x10-8 M) [17]
sunitinib Hs Inhibition 8.1 pKi 26
pKi 8.1 (Ki 8x10-9 M) [26]
PD166285 Hs Inhibition 7.0 pKi 33
pKi 7.0 (Ki 9.83x10-8 M) [33]
CP-673451 Hs Inhibition 9.0 pIC50 37
pIC50 9.0 (IC50 1x10-9 M) [37]
compound 8h [PMID: 22765894] Hs Inhibition 8.9 pIC50 20
pIC50 8.9 (IC50 1.3x10-9 M) [20]
compound 8i [PMID: 22765894] Hs Inhibition 8.8 pIC50 47
pIC50 8.8 (IC50 1.5x10-9 M) [47]
SU11652 Hs Inhibition 8.5 pIC50 40
pIC50 8.5 (IC50 3x10-9 M) [40]
SU-14813 Hs Inhibition 8.4 pIC50 34
pIC50 8.4 (IC50 4x10-9 M) [34]
famitinib Hs Inhibition 8.4 pIC50 5
pIC50 8.4 (IC50 4x10-9 M) [5]
PDGF receptor tyrosine kinase inhibitor IV Hs Inhibition 8.4 pIC50 15
pIC50 8.4 (IC50 4.2x10-9 M) [15]
cediranib Hs Inhibition 8.3 pIC50 43
pIC50 8.3 (IC50 5x10-9 M) [43]
sunitinib Hs Inhibition 8.2 pIC50 21
pIC50 8.2 (IC50 5.7x10-9 M) [21]
lucitanib Hs Inhibition 8.1 pIC50 48
pIC50 8.1 (IC50 8x10-9 M) [48]
henatinib Hs Inhibition 8.0 pIC50 5
pIC50 8.0 (IC50 1.1x10-8 M) [5]
dovitinib Hs Inhibition 7.6 – 8.3 pIC50 36,41
pIC50 7.6 – 8.3 (IC50 2.7x10-8 – 5x10-9 M) [36,41]
PDGF RTK inhibitor Hs Inhibition 7.9 pIC50 8
pIC50 7.9 (IC50 1.2x10-8 M) [8]
Description: Inhibition of PDGFR autophosphorylation in human G292 cells
ilorasertib Hs Inhibition 7.9 pIC50 11
pIC50 7.9 (IC50 1.3x10-8 M) [11]
Description: Measuring inhibition of kinase activity in a biochemical assay.
tafetinib Hs Inhibition 7.8 pIC50 42
pIC50 7.8 (IC50 1.4x10-8 M) [42]
Description: In a radiometric biochemical protein kinase assay.
MK-2461 Hs Inhibition 7.7 pIC50 32
pIC50 7.7 (IC50 2.2x10-8 M) [32]
KBP-7018 Hs Inhibition 7.6 pIC50 16
pIC50 7.6 (IC50 2.5x10-8 M) [16]
orantinib Hs Inhibition 7.3 pIC50 18
pIC50 7.3 (IC50 5x10-8 M) [18]
sorafenib Hs Inhibition 7.2 pIC50 47
pIC50 7.2 (IC50 5.7x10-8 M) [47]
sorafenib Mm Inhibition 7.2 pIC50 44
pIC50 7.2 (IC50 5.7x10-8 M) [44]
nintedanib Hs Inhibition 7.2 pIC50 14
pIC50 7.2 (IC50 6.5x10-8 M) [14]
linifanib Hs Inhibition 7.2 pIC50 1
pIC50 7.2 (IC50 6.6x10-8 M) [1]
PDGF receptor tyrosine kinase inhibitor III Hs Inhibition 7.1 pIC50 25
pIC50 7.1 (IC50 8x10-8 M) [25]
pazopanib Hs Inhibition 7.1 pIC50 12
pIC50 7.1 (IC50 8.4x10-8 M) [12]
AGL 2043 Hs Inhibition 7.1 pIC50 10
pIC50 7.1 (IC50 9x10-8 M) [10]
Description: Using purified human PDGFRβ
CS2164 Hs Inhibition 7.0 pIC50 49
pIC50 7.0 (IC50 9.3x10-8 M) [49]
Description: Inhibition in a biochemical assay.
TAK-632 Hs Inhibition 6.9 pIC50 31
pIC50 6.9 (IC50 1.2x10-7 M) [31]
Description: Biochemical enzyme inhibition assay.
Flt-3 inhibitor II Hs Inhibition 6.8 pIC50 24
pIC50 6.8 (IC50 1.71x10-7 M) [24]
tandutinib Hs Inhibition 6.7 pIC50 19
pIC50 6.7 (IC50 2x10-7 M) [19]
Ki-20227 Hs Inhibition 6.7 pIC50 30
pIC50 6.7 (IC50 2.17x10-7 M) [30]
flumatinib Hs Inhibition 6.5 pIC50 23
pIC50 6.5 (IC50 3.07x10-7 M) [23]
DEBIO1347 Hs Inhibition 6.3 pIC50 28
pIC50 6.3 (IC50 5.6x10-7 M) [28]
vatalanib Hs Inhibition 6.2 pIC50 3
pIC50 6.2 (IC50 6x10-7 M) [3]
semaxanib Hs Inhibition 6.2 pIC50 3
pIC50 6.2 (IC50 6.8x10-7 M) [3]
masitinib Hs Inhibition 6.1 pIC50 7
pIC50 6.1 (IC50 8x10-7 M) [7]
GTP-14564 Hs Inhibition 6.0 pIC50 27
pIC50 6.0 (IC50 1x10-6 M) [27]
BLZ945 Hs Inhibition 5.2 pIC50 39
pIC50 5.2 (IC50 5.86x10-6 M) [39]
PK10571 Hs Inhibition - - 50
View species-specific inhibitor tables
Inhibitor Comments
Note that sunitinib inhibits a range of additional kinases, including platelet-derived growth factor receptor α (PDGFRα), vascular endothelial growth factor receptors (VEGFR1, VEGFR2 and VEGFR3), stem cell factor receptor (KIT), Fms-like tyrosine kinase-3 (FLT3) and colony stimulating factor receptor Type 1 (CSF-1R).
The experiments measuring the ability of PDGF RTK inhibitor to inhibit PDGFR autophosphorylation were carried out in intact human cells, so it is impossible to specify the isozyme involved in the interaction. We nominally map the interaction to the beta isozyme for data retrieval purposes only.
DiscoveRx KINOMEscan® screen
A screen of 72 inhibitors against 456 human kinases. Quantitative data were derived using DiscoveRx KINOMEscan® platform.
Reference: 6,45

Key to terms and symbols Click column headers to sort
Target used in screen: PDGFRB
Ligand Sp. Type Action Value Parameter
sunitinib Hs Inhibitor Inhibition 10.1 pKd
SU-14813 Hs Inhibitor Inhibition 9.5 pKd
Ki-20227 Hs Inhibitor Inhibition 9.5 pKd
cediranib Hs Inhibitor Inhibition 9.5 pKd
axitinib Hs Inhibitor Inhibition 9.2 pKd
dasatinib Hs Inhibitor Inhibition 9.2 pKd
foretinib Hs Inhibitor Inhibition 9.0 pKd
PD-173955 Hs Inhibitor Inhibition 8.9 pKd
staurosporine Hs Inhibitor Inhibition 8.7 pKd
linifanib Hs Inhibitor Inhibition 8.7 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: 2,9

Key to terms and symbols Click column headers to sort
Target used in screen: PDGFRβ/PDGFRb
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
staurosporine Hs Inhibitor Inhibition 2.3 3.0 1.0
dasatinib Hs Inhibitor Inhibition 2.5
SU11652 Hs Inhibitor Inhibition 9.3 1.0 1.0
PDK1/Akt/Flt dual pathway inhibitor Hs Inhibitor Inhibition 11.4 120.0 111.0
sorafenib Hs Inhibitor Inhibition 12.0
K-252a Hs Inhibitor Inhibition 14.6 46.0 8.0
midostaurin Hs Inhibitor Inhibition 14.8 46.0 25.0
dovitinib Hs Inhibitor Inhibition 17.2
masitinib Hs Inhibitor Inhibition 17.3
sunitinib Hs Inhibitor Inhibition 17.6
Displaying the top 10 most potent ligands  View all ligands in screen »
Immuno Process Associations
Immuno Process:  Immune system development
GO Annotations:  Associated to 1 GO processes
GO:0002244 hematopoietic progenitor cell differentiation IBA
Clinically-Relevant Mutations and Pathophysiology
Disease:  Basal ganglia calcification, idiopathic, 4; IBGC4
Synonyms: Basal ganglia calcification [Disease Ontology: DOID:0060230]
Bilateral striopallidodentate calcinosis [Orphanet: ORPHA1980]
Disease Ontology: DOID:0060230
OMIM: 615007
Orphanet: ORPHA1980
References:  29
Disease:  Chronic myelomonocytic leukemia
Orphanet: ORPHA98823
Disease:  Myeloid neoplasm associated with PDGFRB rearrangement
Orphanet: ORPHA168950
Disease:  Myeloproliferative disorder, chronic, with eosinophilia
Synonyms: Unclassified chronic myeloproliferative disease [Orphanet: ORPHA86830]
OMIM: 131440
Orphanet: ORPHA86830
Disease:  Myofibromatosis, infantile, 1; IMF1
Synonyms: Infantile myofibromatosis [Orphanet: ORPHA2591]
OMIM: 228550
Orphanet: ORPHA2591


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How to cite this page

Type III RTKs: PDGFR, CSFR, Kit, FLT3 receptor family: platelet derived growth factor receptor beta. Last modified on 07/02/2020. Accessed on 19/09/2020. IUPHAR/BPS Guide to PHARMACOLOGY,