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platelet derived growth factor receptor beta

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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 Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 1 1106 5q32 PDGFRB platelet derived growth factor receptor beta
Mouse 1 1098 18 34.41 cM Pdgfrb platelet derived growth factor receptor, beta polypeptide
Rat 1 1097 18q12.1 Pdgfrb platelet derived growth factor receptor beta
Previous and Unofficial Names Click here for help
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 Click here for help
Alphafold
BRENDA
CATH/Gene3D
ChEMBL Target
DrugBank Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
Orphanet
Pharos
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
Selected 3D Structures Click here for help
Image of receptor 3D structure from RCSB PDB
Description:  The structure of a platelet derived growth factor receptor complex
PDB Id:  3MJG
Resolution:  2.3Å
Species:  Human
References:  39
Enzyme Reaction Click here for help
EC Number: 2.7.10.1
Endogenous ligands (Human)
PDGF

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
AC710 Small molecule or natural product Click here for species-specific activity table Hs Inhibition 9.0 pKd 23
pKd 9.0 (Kd 1x10-9 M) [23]
crenolanib Small molecule or natural product Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibition 8.5 pKd 14
pKd 8.5 (Kd 3.2x10-9 M) [14]
quizartinib Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 8.1 pKd 4
pKd 8.1 (Kd 7.7x10-9 M) [4]
naporafenib Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 7.8 pKd 36
pKd 7.8 (Kd 1.4x10-8 M) [36]
Description: Binding affinity determined using the KinomeScan® platform.
compound 5e [PMID: 28580438] Small molecule or natural product Click here for species-specific activity table Immunopharmacology Ligand Hs Inhibition 7.6 pKd 18
pKd 7.6 (Kd 2.8x10-8 M) [18]
IACS-9439 Small molecule or natural product Click here for species-specific activity table Hs Inhibition 6.3 pKd 6
pKd 6.3 (Kd 4.5x10-7 M) [6]
sunitinib 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 8.1 pKi 27
pKi 8.1 (Ki 8x10-9 M) [27]
PD166285 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 7.0 pKi 34
pKi 7.0 (Ki 9.83x10-8 M) [34]
CP-673451 Small molecule or natural product Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 9.0 pIC50 38
pIC50 9.0 (IC50 1x10-9 M) [38]
compound 8h [PMID: 22765894] Small molecule or natural product Click here for species-specific activity table Hs Inhibition 8.9 pIC50 21
pIC50 8.9 (IC50 1.3x10-9 M) [21]
compound 8i [PMID: 22765894] Small molecule or natural product Click here for species-specific activity table Hs Inhibition 8.8 pIC50 48
pIC50 8.8 (IC50 1.5x10-9 M) [48]
SU11652 Small molecule or natural product Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 8.5 pIC50 41
pIC50 8.5 (IC50 3x10-9 M) [41]
SU-14813 Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Inhibition 8.4 pIC50 35
pIC50 8.4 (IC50 4x10-9 M) [35]
famitinib Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Inhibition 8.4 pIC50 5
pIC50 8.4 (IC50 4x10-9 M) [5]
PDGF receptor tyrosine kinase inhibitor IV Small molecule or natural product Primary target of this compound Hs Inhibition 8.4 pIC50 16
pIC50 8.4 (IC50 4.2x10-9 M) [16]
cediranib Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Inhibition 8.3 pIC50 44
pIC50 8.3 (IC50 5x10-9 M) [44]
sunitinib 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 8.2 pIC50 22
pIC50 8.2 (IC50 5.7x10-9 M) [22]
lucitanib Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 8.1 pIC50 49
pIC50 8.1 (IC50 8x10-9 M) [49]
henatinib Small molecule or natural product Click here for species-specific activity table Hs Inhibition 8.0 pIC50 5
pIC50 8.0 (IC50 1.1x10-8 M) [5]
dovitinib Small molecule or natural product Click here for species-specific activity table Hs Inhibition 7.6 – 8.3 pIC50 37,42
pIC50 7.6 – 8.3 (IC50 2.7x10-8 – 5x10-9 M) [37,42]
PDGF RTK inhibitor Small molecule or natural product Primary target of this compound Hs Inhibition 7.9 pIC50 9
pIC50 7.9 (IC50 1.2x10-8 M) [9]
Description: Inhibition of PDGFR autophosphorylation in human G292 cells
ilorasertib Small molecule or natural product Click here for species-specific activity table Hs Inhibition 7.9 pIC50 12
pIC50 7.9 (IC50 1.3x10-8 M) [12]
Description: Measuring inhibition of kinase activity in a biochemical assay.
tafetinib Small molecule or natural product Click here for species-specific activity table Hs Inhibition 7.8 pIC50 43
pIC50 7.8 (IC50 1.4x10-8 M) [43]
Description: In a radiometric biochemical protein kinase assay.
MK-2461 Small molecule or natural product Click here for species-specific activity table Hs Inhibition 7.7 pIC50 33
pIC50 7.7 (IC50 2.2x10-8 M) [33]
KBP-7018 Small molecule or natural product Click here for species-specific activity table Immunopharmacology Ligand Hs Inhibition 7.6 pIC50 17
pIC50 7.6 (IC50 2.5x10-8 M) [17]
orantinib Small molecule or natural product Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 7.3 pIC50 19
pIC50 7.3 (IC50 5x10-8 M) [19]
sorafenib Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 7.2 pIC50 48
pIC50 7.2 (IC50 5.7x10-8 M) [48]
sorafenib Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Mm Inhibition 7.2 pIC50 45
pIC50 7.2 (IC50 5.7x10-8 M) [45]
nintedanib Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 7.2 pIC50 15
pIC50 7.2 (IC50 6.5x10-8 M) [15]
linifanib Small molecule or natural product Click here for species-specific activity table Hs Inhibition 7.2 pIC50 1
pIC50 7.2 (IC50 6.6x10-8 M) [1]
PDGF receptor tyrosine kinase inhibitor III Small molecule or natural product Primary target of this compound Hs Inhibition 7.1 pIC50 26
pIC50 7.1 (IC50 8x10-8 M) [26]
pazopanib Small molecule or natural product Approved drug Click here for species-specific activity table Hs Inhibition 7.1 pIC50 13
pIC50 7.1 (IC50 8.4x10-8 M) [13]
AGL 2043 Small molecule or natural product Primary target of this compound Hs Inhibition 7.1 pIC50 11
pIC50 7.1 (IC50 9x10-8 M) [11]
Description: Using purified human PDGFRβ
CS2164 Small molecule or natural product Click here for species-specific activity table Hs Inhibition 7.0 pIC50 50
pIC50 7.0 (IC50 9.3x10-8 M) [50]
Description: Inhibition in a biochemical assay.
CHMFL-KIT-64 Small molecule or natural product Click here for species-specific activity table Hs Inhibition 7.0 pIC50 47
pIC50 7.0 (IC50 9.7x10-8 M) [47]
Description: In a biochemical assay.
TAK-632 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibition 6.9 pIC50 32
pIC50 6.9 (IC50 1.2x10-7 M) [32]
Description: Biochemical enzyme inhibition assay.
Flt-3 inhibitor II Small molecule or natural product Click here for species-specific activity table Hs Inhibition 6.8 pIC50 25
pIC50 6.8 (IC50 1.71x10-7 M) [25]
tandutinib Small molecule or natural product Click here for species-specific activity table Hs Inhibition 6.7 pIC50 20
pIC50 6.7 (IC50 2x10-7 M) [20]
Ki-20227 Small molecule or natural product Click here for species-specific activity table Hs Inhibition 6.7 pIC50 31
pIC50 6.7 (IC50 2.17x10-7 M) [31]
flumbatinib Small molecule or natural product Approved drug Click here for species-specific activity table Hs Inhibition 6.5 pIC50 24
pIC50 6.5 (IC50 3.07x10-7 M) [24]
zoligratinib Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 6.3 pIC50 29
pIC50 6.3 (IC50 5.6x10-7 M) [29]
vatalanib Small molecule or natural product Click here for species-specific activity table Hs Inhibition 6.2 pIC50 3
pIC50 6.2 (IC50 6x10-7 M) [3]
semaxanib Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 6.2 pIC50 3
pIC50 6.2 (IC50 6.8x10-7 M) [3]
masitinib Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibition 6.1 pIC50 8
pIC50 6.1 (IC50 8x10-7 M) [8]
GTP-14564 Small molecule or natural product Click here for species-specific activity table Hs Inhibition 6.0 pIC50 28
pIC50 6.0 (IC50 1x10-6 M) [28]
sotuletinib Small molecule or natural product Click here for species-specific activity table Immunopharmacology Ligand Hs Inhibition 5.2 pIC50 40
pIC50 5.2 (IC50 5.86x10-6 M) [40]
seralutinib Small molecule or natural product Click here for species-specific activity table Hs Inhibition - - 51
[51]
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 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: 7,46

Key to terms and symbols Click column headers to sort
Target used in screen: PDGFRB
Ligand Sp. Type Action Value Parameter
sunitinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 10.1 pKd
SU-14813 Small molecule or natural product Hs Inhibitor Inhibition 9.5 pKd
Ki-20227 Small molecule or natural product Hs Inhibitor Inhibition 9.5 pKd
cediranib Small molecule or natural product Hs Inhibitor Inhibition 9.5 pKd
axitinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 9.2 pKd
dasatinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 9.2 pKd
foretinib Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 9.0 pKd
PD-173955 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 8.9 pKd
staurosporine Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 8.7 pKd
linifanib Small molecule or natural product 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 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: 2,10

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 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 2.3 3.0 1.0
dasatinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 2.5
SU11652 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 9.3 1.0 1.0
PDK1/Akt/Flt dual pathway inhibitor Small molecule or natural product Hs Inhibitor Inhibition 11.4 120.0 111.0
sorafenib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 12.0
K-252a Small molecule or natural product Hs Inhibitor Inhibition 14.6 46.0 8.0
midostaurin Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 14.8 46.0 25.0
dovitinib Small molecule or natural product Hs Inhibitor Inhibition 17.2
masitinib Small molecule or natural product Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 17.3
sunitinib Small molecule or natural product Approved drug Ligand has a PDB structure 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 Click here for help
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:  30
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

References

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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]

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8. Dubreuil P, Letard S, Ciufolini M, Gros L, Humbert M, Castéran N, Borge L, Hajem B, Lermet A, Sippl W et al.. (2009) Masitinib (AB1010), a potent and selective tyrosine kinase inhibitor targeting KIT. PLoS ONE, 4 (9): e7258. [PMID:19789626]

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10. 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]

11. Gazit A, Yee K, Uecker A, Böhmer FD, Sjöblom T, Ostman A, Waltenberger J, Golomb G, Banai S, Heinrich MC et al.. (2003) Tricyclic quinoxalines as potent kinase inhibitors of PDGFR kinase, Flt3 and Kit. Bioorg Med Chem, 11 (9): 2007-18. [PMID:12670652]

12. 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]

13. 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]

14. 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]

15. Hilberg F, Roth GJ, Krssak M, Kautschitsch S, Sommergruber W, Tontsch-Grunt U, Garin-Chesa P, Bader G, Zoephel A, Quant J et al.. (2008) BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy. Cancer Res, 68 (12): 4774-82. [PMID:18559524]

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17. Huang Z, Li H, Zhang Q, Lu F, Hong M, Zhang Z, Guo X, Zhu Y, Li S, Liu H. (2017) Discovery of Indolinone-Based Multikinase Inhibitors as Potential Therapeutics for Idiopathic Pulmonary Fibrosis. ACS Med Chem Lett, 8 (11): 1142-1147. [PMID:29152045]

18. Jarusiewicz JA, Jeon JY, Connelly MC, Chen Y, Yang L, Baker SD, Guy RK. (2017) Discovery of a Diaminopyrimidine FLT3 Inhibitor Active against Acute Myeloid Leukemia. ACS Omega, 2 (5): 1985-2009. [PMID:28580438]

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20. 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]

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26. Matsuno K, Ushiki J, Seishi T, Ichimura M, Giese NA, Yu JC, Takahashi S, Oda S, Nomoto Y. (2003) Potent and selective inhibitors of platelet-derived growth factor receptor phosphorylation. 3. Replacement of quinazoline moiety and improvement of metabolic polymorphism of 4-[4-(N-substituted (thio)carbamoyl)-1-piperazinyl]-6,7-dimethoxyquinazoline derivatives. J Med Chem, 46 (23): 4910-25. [PMID:14584942]

27. Mendel DB, Laird AD, Xin X, Louie SG, Christensen JG, Li G, Schreck RE, Abrams TJ, Ngai TJ, Lee LB et al.. (2003) In vivo antitumor activity of SU11248, a novel tyrosine kinase inhibitor targeting vascular endothelial growth factor and platelet-derived growth factor receptors: determination of a pharmacokinetic/pharmacodynamic relationship. Clin Cancer Res, 9 (1): 327-37. [PMID:12538485]

28. 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]

29. Nakanishi Y, Akiyama N, Tsukaguchi T, Fujii T, Sakata K, Sase H, Isobe T, Morikami K, Shindoh H, Mio T et al.. (2014) The fibroblast growth factor receptor genetic status as a potential predictor of the sensitivity to CH5183284/Debio 1347, a novel selective FGFR inhibitor. Mol Cancer Ther, 13 (11): 2547-58. [PMID:25169980]

30. Nicolas G, Pottier C, Charbonnier C, Guyant-Maréchal L, Le Ber I, Pariente J, Labauge P, Ayrignac X, Defebvre L, Maltête D et al.. (2013) Phenotypic spectrum of probable and genetically-confirmed idiopathic basal ganglia calcification. Brain, 136 (Pt 11): 3395-407. [PMID:24065723]

31. 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]

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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 25/06/2021. Accessed on 19/10/2021. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1804.