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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

Contents:

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 P09619 (Hs), P05622 (Mm), Q05030 (Rn)
BRENDA 2.7.10.1
CATH/Gene3D 2.60.40.10
ChEMBL Target CHEMBL1913 (Hs), CHEMBL2749 (Mm), CHEMBL4125 (Rn)
DrugBank Target P09619 (Hs)
Ensembl Gene ENSG00000113721 (Hs), ENSMUSG00000024620 (Mm), ENSRNOG00000018461 (Rn)
Entrez Gene 5159 (Hs), 18596 (Mm), 24629 (Rn)
Human Protein Atlas ENSG00000113721 (Hs)
KEGG Enzyme 2.7.10.1
KEGG Gene hsa:5159 (Hs), mmu:18596 (Mm), rno:24629 (Rn)
OMIM 173410 (Hs)
Orphanet ORPHA138376 (Hs)
Pharos P09619 (Hs)
RefSeq Nucleotide NM_002609 (Hs), NM_001146268 (Mm), NM_031525 (Rn)
RefSeq Protein NP_002600 (Hs), NP_032835 (Mm), NP_001139740 (Mm), NP_113713 (Rn)
UniProtKB P09619 (Hs), P05622 (Mm), Q05030 (Rn)
Wikipedia PDGFRB (Hs)
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:  41
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 25
⤷ pKd 9.0 (Kd 1x10-9 M) [25]
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 15
⤷ pKd 8.5 (Kd 3.2x10-9 M) [15]
quizartinib Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 8.1 pKd 5
⤷ pKd 8.1 (Kd 7.7x10-9 M) [5]
naporafenib Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 7.8 pKd 38
⤷ pKd 7.8 (Kd 1.4x10-8 M) [38]
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 19
⤷ pKd 7.6 (Kd 2.8x10-8 M) [19]
IACS-9439 Small molecule or natural product Click here for species-specific activity table Hs Inhibition 6.3 pKd 7
⤷ pKd 6.3 (Kd 4.5x10-7 M) [7]
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 29
⤷ pKi 8.1 (Ki 8x10-9 M) [29]
PD166285 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 7.0 pKi 36
⤷ pKi 7.0 (Ki 9.83x10-8 M) [36]
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 40
⤷ pIC50 9.0 (IC50 1x10-9 M) [40]
compound 8h [PMID: 22765894] Small molecule or natural product Click here for species-specific activity table Hs Inhibition 8.9 pIC50 22
⤷ pIC50 8.9 (IC50 1.3x10-9 M) [22]
compound 8i [PMID: 22765894] Small molecule or natural product Click here for species-specific activity table Hs Inhibition 8.8 pIC50 51
⤷ pIC50 8.8 (IC50 1.5x10-9 M) [51]
M4205 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 8.6 pIC50 3
⤷ pIC50 8.6 (IC50 2.6x10-9 M) [3]
Description: Biochemical inhibitory potency
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 43
⤷ pIC50 8.5 (IC50 3x10-9 M) [43]
SU-14813 Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Inhibition 8.4 pIC50 37
⤷ pIC50 8.4 (IC50 4x10-9 M) [37]
famitinib Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Inhibition 8.4 pIC50 6
⤷ pIC50 8.4 (IC50 4x10-9 M) [6]
PDGF receptor tyrosine kinase inhibitor IV Small molecule or natural product Primary target of this compound Hs Inhibition 8.4 pIC50 17
⤷ pIC50 8.4 (IC50 4.2x10-9 M) [17]
cediranib Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Inhibition 8.3 pIC50 47
⤷ pIC50 8.3 (IC50 5x10-9 M) [47]
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 23
⤷ pIC50 8.2 (IC50 5.7x10-9 M) [23]
lucitanib Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 8.1 pIC50 52
⤷ pIC50 8.1 (IC50 8x10-9 M) [52]
henatinib Small molecule or natural product Click here for species-specific activity table Hs Inhibition 8.0 pIC50 6
⤷ pIC50 8.0 (IC50 1.1x10-8 M) [6]
dovitinib Small molecule or natural product Click here for species-specific activity table Hs Inhibition 7.6 – 8.3 pIC50 39,45
⤷ pIC50 7.6 – 8.3 (IC50 2.7x10-8 – 5x10-9 M) [39,45]
PDGF RTK inhibitor Small molecule or natural product Primary target of this compound Hs Inhibition 7.9 pIC50 10
⤷ pIC50 7.9 (IC50 1.2x10-8 M) [10]
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 13
⤷ pIC50 7.9 (IC50 1.3x10-8 M) [13]
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 46
⤷ pIC50 7.8 (IC50 1.4x10-8 M) [46]
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 35
⤷ pIC50 7.7 (IC50 2.2x10-8 M) [35]
KBP-7018 Small molecule or natural product Click here for species-specific activity table Immunopharmacology Ligand Hs Inhibition 7.6 pIC50 18
⤷ pIC50 7.6 (IC50 2.5x10-8 M) [18]
BPR1R024 Small molecule or natural product Click here for species-specific activity table Hs Inhibition 7.5 pIC50 24
⤷ pIC50 7.5 (IC50 3.15x10-8 M) [24]
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 20
⤷ pIC50 7.3 (IC50 5x10-8 M) [20]
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 51
⤷ pIC50 7.2 (IC50 5.7x10-8 M) [51]
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 48
⤷ pIC50 7.2 (IC50 5.7x10-8 M) [48]
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 16
⤷ pIC50 7.2 (IC50 6.5x10-8 M) [16]
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 28
⤷ pIC50 7.1 (IC50 8x10-8 M) [28]
pazopanib Small molecule or natural product Approved drug Click here for species-specific activity table Hs Inhibition 7.1 pIC50 14
⤷ pIC50 7.1 (IC50 8.4x10-8 M) [14]
AGL 2043 Small molecule or natural product Primary target of this compound Hs Inhibition 7.1 pIC50 12
⤷ pIC50 7.1 (IC50 9x10-8 M) [12]
Description: Using purified human PDGFRβ
ibcasertib Small molecule or natural product Click here for species-specific activity table Hs Inhibition 7.0 pIC50 53
⤷ pIC50 7.0 (IC50 9.3x10-8 M) [53]
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 50
⤷ pIC50 7.0 (IC50 9.7x10-8 M) [50]
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 34
⤷ pIC50 6.9 (IC50 1.2x10-7 M) [34]
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 27
⤷ pIC50 6.8 (IC50 1.71x10-7 M) [27]
tandutinib Small molecule or natural product Click here for species-specific activity table Hs Inhibition 6.7 pIC50 21
⤷ pIC50 6.7 (IC50 2x10-7 M) [21]
Ki-20227 Small molecule or natural product Click here for species-specific activity table Hs Inhibition 6.7 pIC50 33
⤷ pIC50 6.7 (IC50 2.17x10-7 M) [33]
flumbatinib Small molecule or natural product Approved drug Click here for species-specific activity table Hs Inhibition 6.5 pIC50 26
⤷ pIC50 6.5 (IC50 3.07x10-7 M) [26]
SU5402 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 6.3 pIC50 44
⤷ pIC50 6.3 (IC50 5.1x10-7 M) [44]
zoligratinib Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 6.3 pIC50 31
⤷ pIC50 6.3 (IC50 5.6x10-7 M) [31]
vatalanib Small molecule or natural product Click here for species-specific activity table Hs Inhibition 6.2 pIC50 4
⤷ pIC50 6.2 (IC50 6x10-7 M) [4]
semaxanib Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 6.2 pIC50 4
⤷ pIC50 6.2 (IC50 6.8x10-7 M) [4]
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 9
⤷ pIC50 6.1 (IC50 8x10-7 M) [9]
GTP-14564 Small molecule or natural product Click here for species-specific activity table Hs Inhibition 6.0 pIC50 30
⤷ pIC50 6.0 (IC50 1x10-6 M) [30]
sotuletinib Small molecule or natural product Click here for species-specific activity table Immunopharmacology Ligand Hs Inhibition 5.2 pIC50 42
⤷ pIC50 5.2 (IC50 5.86x10-6 M) [42]
seralutinib Small molecule or natural product Click here for species-specific activity table Hs Inhibition - - 54
⤷ [54]
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: 8,49
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
Ki-20227 Small molecule or natural product Hs Inhibitor Inhibition 9.5 pKd
SU-14813 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: 2,11
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
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:  32
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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How to cite this page

Type III RTKs: PDGFR, CSFR, Kit, FLT3 receptor family: platelet derived growth factor receptor beta. Last modified on 03/02/2023. Accessed on 16/04/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1804.