PDGFRB

Summary

PDGFRB (platelet derived growth factor receptor beta, HGNC:8804) is a protein-coding gene on chromosome 5q32, encoding Platelet-derived growth factor receptor beta (P09619). Tyrosine-protein kinase that acts as a cell-surface receptor for homodimeric PDGFB and PDGFD and for heterodimers formed by PDGFA and PDGFB, and plays an essential role in the regulation of embryonic development, cell proliferation, survival, differentiation, chemotaxis and migr…. In precision oncology, PDGFRB Overexpression confers sensitivity to Sunitinib in Dermatofibrosarcoma Protuberans (CIViC Level C); 1 further curated variant–drug associations are listed below.

The protein encoded by this gene is a cell surface tyrosine kinase receptor for members of the platelet-derived growth factor family. These growth factors are mitogens for cells of mesenchymal origin. The identity of the growth factor bound to a receptor monomer determines whether the functional receptor is a homodimer (PDGFB or PDGFD) or a heterodimer (PDGFA and PDGFB). This gene is essential for normal development of the cardiovascular system and aids in rearrangement of the actin cytoskeleton. This gene is flanked on chromosome 5 by the genes for granulocyte-macrophage colony-stimulating factor and macrophage-colony stimulating factor receptor; all three genes may be implicated in the 5-q syndrome. A translocation between chromosomes 5 and 12, that fuses this gene to that of the ETV6 gene, results in chronic myeloproliferative disorder with eosinophilia.

Source: NCBI Gene 5159 — RefSeq curated summary.

At a glance

• Gene–disease (curated): myofibromatosis, infantile, 1 (Definitive, GenCC) — +7 more curated relationships
• GWAS associations: 8
• Clinical variants (ClinVar): 875 total — 19 pathogenic, 6 likely-pathogenic (top 4% of genes corpus-wide)
• GTEx eGene: eQTL in 7 tissues, sQTL in 23 (q < 0.05)
• Phenotypes (HPO): 179
• Drug target: yes — 17 curated mechanism-of-action drugs, 24 via a complex or family; 102 molecules with ChEMBL bioactivity (top 1% of genes corpus-wide)
• Approved drugs (ChEMBL mechanism of action): 5 — Dasatinib Anhydrous, Imatinib Mesylate, Sorafenib Tosylate, +2 more
• Approved drugs acting on a complex or family including it: 6 — Becaplermin, Midostaurin, Nintedanib Esylate, +3 more (Platelet-derived growth factor receptor)
• Precision-oncology evidence (CIViC): 2 curated variant–drug associations
• Cancer driver (intOGen): activating (oncogene-like) across 3 cancer types (inferred from mutation patterns)
• Constraint (gnomAD): pLI 0.94 (loss-of-function intolerant), LOEUF 0.50 (moderately constrained)
• MANE Select transcript: NM_002609
• Interaction hub: 4,032 STRING partners (top 1% of genes corpus-wide)

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:8804
Approved symbol	PDGFRB
Name	platelet derived growth factor receptor beta
Location	5q32
Locus type	gene with protein product
Status	Approved
Aliases	JTK12, CD140b, PDGFR1
Ensembl gene	ENSG00000113721
Ensembl biotype	protein_coding
OMIM	173410
Entrez	5159

Gene structure

Transcript identifiers

Ensembl transcripts: 36 — 28 protein_coding, 5 protein_coding_CDS_not_defined, 2 retained_intron, 1 nonsense_mediated_decay

MANE Select: ENST00000261799

Transcript support level (Ensembl TSL; 1 = fully mRNA-supported): TSL 1: 2, TSL 2: 2, TSL 3: 5, TSL 4: 1, TSL 5: 1

ENST00000261799, ENST00000517488, ENST00000517660, ENST00000517957, ENST00000519575, ENST00000520229, ENST00000520579, ENST00000520851, ENST00000521723, ENST00000522466, ENST00000523456, ENST00000890715, ENST00000890716, ENST00000890717, ENST00000890718, ENST00000890719, ENST00000890720, ENST00000890721, ENST00000890722, ENST00000890723, ENST00000890724, ENST00000890725, ENST00000890726, ENST00000890727, ENST00000951660, ENST00000951661, ENST00000951662, ENST00000951663, ENST00000951664, ENST00001111350, ENST00001111351, ENST00001111352, ENST00001111353, ENST00001118160, ENST00001118161, ENST00001133371

RefSeq mRNA: 3 — MANE Select: NM_002609 NM_001355016, NM_001355017, NM_002609

CCDS: CCDS4303

Canonical transcript exons

ENST00000261799 — 23 exons

Exon	Start	End
ENSE00001277266	150113839	150115946
ENSE00001277271	150137008	150137053
ENSE00003460521	150126520	150126614
ENSE00003464042	150121204	150121322
ENSE00003469927	150120888	150121010
ENSE00003474441	150125445	150125577
ENSE00003513640	150133586	150133760
ENSE00003517537	150119467	150119566
ENSE00003564035	150121880	150122040
ENSE00003584504	150118747	150118852
ENSE00003600881	150117618	150117850
ENSE00003600936	150124250	150124360
ENSE00003603285	150130539	150130662
ENSE00003607028	150123042	150123201
ENSE00003643730	150124727	150124831
ENSE00003648053	150132750	150132942
ENSE00003652119	150131979	150132094
ENSE00003654111	150135555	150135878
ENSE00003667728	150133881	150134008
ENSE00003682400	150129757	150129968
ENSE00003687411	150120012	150120123
ENSE00003788938	150134750	150135016
ENSE00003845888	150155397	150155845

Expression profiles

Bgee: expression breadth ubiquitous, 270 present calls, max score 99.59.

FANTOM5 (CAGE): breadth ubiquitous, TPM avg 42.3191 / max 697.8902, expressed in 1070 samples.

Highest expression (Bgee): stromal cell of endometrium, coronary artery, endocervix, popliteal artery, tibial artery.

Genetic regulation across tissues (GTEx eQTL / sQTL)

PDGFRB is an eGene in GTEx v10 — its expression is genetically regulated (eQTL) in 7 tissues and its splicing (sQTL) in 23 (q < 0.05). Strongest associations first; slope = normalized effect of the lead variant’s alternative allele.

showing 20 of 30 significant tissue × QTL associations:

Tissue	QTL	q-value	Slope	Lead variant
Adipose Subcutaneous	sqtl	6.1e-56	-0.93	5:150119196:A:T
Cells Cultured fibroblasts	sqtl	1.2e-52	+1.12	5:150119196:A:T
Lung	sqtl	7.3e-42	+0.87	5:150119196:A:T
Adipose Visceral Omentum	sqtl	6.0e-34	+0.86	5:150119196:A:T
Breast Mammary Tissue	sqtl	7.9e-27	+0.95	5:150119196:A:T
Thyroid	sqtl	1.3e-26	+0.85	5:150119196:A:T
Artery Aorta	sqtl	3.1e-25	+0.70	5:150119196:A:T
Cells EBV-transformed lymphocytes	eqtl	3.3e-19	-0.59	5:150157517:A:G
Esophagus Gastroesophageal Junction	sqtl	1.2e-16	+0.91	5:150119196:A:T
Esophagus Muscularis	sqtl	7.1e-16	+0.81	5:150119196:A:T
Artery Tibial	eqtl	1.4e-14	+0.28	5:150066032:A:G
Heart Atrial Appendage	sqtl	4.6e-14	+0.85	5:150119196:A:T
Cells Cultured fibroblasts	eqtl	9.8e-14	-0.16	5:150154285:C:T
Artery Coronary	sqtl	4.8e-13	+0.83	5:150119196:A:T
Ovary	sqtl	7.0e-11	-0.98	5:150119196:A:T
Skin Sun Exposed Lower leg	sqtl	2.6e-09	+0.58	5:150119196:A:T
Colon Transverse	sqtl	1.2e-08	+0.68	5:150119196:A:T
Muscle Skeletal	sqtl	5.1e-08	+0.57	5:150119196:A:T
Colon Sigmoid	sqtl	2.1e-07	+0.75	5:150119196:A:T
Heart Left Ventricle	sqtl	9.9e-07	+0.78	5:150119196:A:T

FANTOM5 promoters

7 alternative TSS:

Promoter ID	TPM avg	Samples expressed
64169	24.2718	961
64170	9.3152	1012
64167	3.9117	737
64165	3.5911	714
64168	0.6448	380
64166	0.5411	286
64164	0.0433	17

Top tissues by expression

showing 100 of 296 tissues by Bgee expression score (0-100, higher = more expressed):

Tissue	Anatomy ID	Expression score	Quality
stromal cell of endometrium	CL:0002255	99.59	gold quality
right coronary artery	UBERON:0001625	98.97	gold quality
endocervix	UBERON:0000458	98.95	gold quality
popliteal artery	UBERON:0002250	98.83	gold quality
tibial artery	UBERON:0007610	98.83	gold quality
gall bladder	UBERON:0002110	98.69	gold quality
descending thoracic aorta	UBERON:0002345	98.58	gold quality
aorta	UBERON:0000947	98.56	gold quality
right ovary	UBERON:0002118	98.47	gold quality
calcaneal tendon	UBERON:0003701	98.36	gold quality
right lung	UBERON:0002167	98.33	gold quality
left coronary artery	UBERON:0001626	98.32	gold quality
thoracic aorta	UBERON:0001515	98.29	gold quality
ascending aorta	UBERON:0001496	98.27	gold quality
coronary artery	UBERON:0001621	98.27	gold quality
body of uterus	UBERON:0009853	98.27	gold quality
left uterine tube	UBERON:0001303	98.17	gold quality
left ovary	UBERON:0002119	97.93	gold quality
mucosa of stomach	UBERON:0001199	97.90	gold quality
omental fat pad	UBERON:0010414	97.86	gold quality
peritoneum	UBERON:0002358	97.84	gold quality
peripheral nervous system	UBERON:0000010	97.53	gold quality
nerve	UBERON:0001021	97.53	gold quality
tibial nerve	UBERON:0001323	97.53	gold quality
pericardium	UBERON:0002407	97.51	gold quality
subcutaneous adipose tissue	UBERON:0002190	97.46	gold quality
saphenous vein	UBERON:0007318	97.43	gold quality
adipose tissue of abdominal region	UBERON:0007808	97.42	gold quality
apex of heart	UBERON:0002098	97.39	gold quality
ectocervix	UBERON:0012249	97.38	gold quality
right lobe of thyroid gland	UBERON:0001119	97.18	gold quality
upper lobe of left lung	UBERON:0008952	97.15	gold quality
upper lobe of lung	UBERON:0008948	96.82	gold quality
sural nerve	UBERON:0015488	96.70	gold quality
islet of Langerhans	UBERON:0000006	96.34	gold quality
colonic epithelium	UBERON:0000397	96.30	gold quality
metanephros cortex	UBERON:0010533	96.29	gold quality
lower esophagus muscularis layer	UBERON:0035833	95.95	gold quality
lower esophagus	UBERON:0013473	95.91	gold quality
left lobe of thyroid gland	UBERON:0001120	95.82	gold quality
vena cava	UBERON:0004087	95.78	gold quality
myometrium	UBERON:0001296	95.75	gold quality
esophagogastric junction muscularis propria	UBERON:0035841	95.53	gold quality
urethra	UBERON:0000057	95.41	gold quality
smooth muscle tissue	UBERON:0001135	95.33	gold quality
tendon	UBERON:0000043	95.19	gold quality
thyroid gland	UBERON:0002046	95.19	gold quality
adipose tissue	UBERON:0001013	95.16	gold quality
skin of leg	UBERON:0001511	95.16	gold quality
right atrium auricular region	UBERON:0006631	95.13	gold quality
synovial joint	UBERON:0002217	95.03	gold quality
heart left ventricle	UBERON:0002084	94.96	gold quality
vagina	UBERON:0000996	94.81	gold quality
connective tissue	UBERON:0002384	94.80	gold quality
cardiac ventricle	UBERON:0002082	94.79	gold quality
tendon of biceps brachii	UBERON:0008188	94.77	gold quality
heart	UBERON:0000948	94.39	gold quality
ovary	UBERON:0000992	93.92	gold quality
cardiac atrium	UBERON:0002081	93.52	gold quality
decidua	UBERON:0002450	93.44	gold quality
lung	UBERON:0002048	93.35	gold quality
muscle layer of sigmoid colon	UBERON:0035805	93.33	gold quality
ventricular zone	UBERON:0003053	93.01	gold quality
fundus of stomach	UBERON:0001160	92.86	gold quality
uterus	UBERON:0000995	92.85	gold quality
right uterine tube	UBERON:0001302	92.79	gold quality
female reproductive system	UBERON:0000474	92.65	gold quality
muscle of leg	UBERON:0001383	92.63	gold quality
zone of skin	UBERON:0000014	92.61	gold quality
skin of abdomen	UBERON:0001416	92.61	gold quality
skin of hip	UBERON:0001554	92.58	gold quality
gastrocnemius	UBERON:0001388	92.43	gold quality
minor salivary gland	UBERON:0001830	92.34	gold quality
uterine cervix	UBERON:0000002	92.14	gold quality
prostate gland	UBERON:0002367	92.11	gold quality
spleen	UBERON:0002106	91.98	gold quality
lymph node	UBERON:0000029	91.70	gold quality
small intestine Peyer’s patch	UBERON:0003454	91.70	gold quality
layer of synovial tissue	UBERON:0007616	91.68	gold quality
esophagus	UBERON:0001043	91.54	gold quality
dorsal root ganglion	UBERON:0000044	91.40	gold quality
adrenal tissue	UBERON:0018303	91.23	gold quality
lower lobe of lung	UBERON:0008949	91.14	gold quality
adenohypophysis	UBERON:0002196	90.85	gold quality
triceps brachii	UBERON:0001509	90.84	gold quality
hindlimb stylopod muscle	UBERON:0004252	90.78	gold quality
right adrenal gland cortex	UBERON:0035827	90.71	gold quality
adrenal gland	UBERON:0002369	90.67	gold quality
type B pancreatic cell	CL:0000169	90.64	silver quality
right adrenal gland	UBERON:0001233	90.61	gold quality
trigeminal ganglion	UBERON:0001675	90.57	gold quality
nipple	UBERON:0002030	90.56	gold quality
adrenal cortex	UBERON:0001235	90.53	gold quality
pancreas	UBERON:0001264	90.44	gold quality
left adrenal gland cortex	UBERON:0035825	90.38	gold quality
left adrenal gland	UBERON:0001234	90.31	gold quality
saliva-secreting gland	UBERON:0001044	90.26	gold quality
muscle organ	UBERON:0001630	90.26	gold quality
skeletal muscle organ	UBERON:0014892	90.26	gold quality
mammary duct	UBERON:0001765	90.23	gold quality

Single-cell (SCXA)

Detected in 23 experiment(s), a significant marker in 23.

Experiment	Marker?	Max mean expression
E-ANND-2	yes	2094.99
E-GEOD-134144	yes	1979.16
E-MTAB-11268	yes	1902.31
E-MTAB-6678	yes	1153.93
E-MTAB-9906	yes	934.63
E-MTAB-10662	yes	572.93
E-GEOD-83139	yes	321.81
E-GEOD-81608	yes	270.69
E-HCAD-10	yes	60.17
E-MTAB-8142	yes	55.95
E-MTAB-6701	yes	37.61
E-GEOD-135922	yes	28.98
E-MTAB-8410	yes	26.46
E-HCAD-11	yes	20.66
E-CURD-119	yes	14.91

HPA expression

RNA tissue specificity: Low tissue specificity

showing 60 of 78 HPA tissues / cells by nTPM:

Tissue / cell	Axis	nTPM	Protein (IHC)
Gallbladder	tissue	116.6	not detected
Placenta	tissue	106.4	medium
Cervix	tissue	99.0	not detected
Vagina	tissue	94.4	not detected
Adipose tissue	tissue	89.5	not detected
Ovary	tissue	76.3	medium
Choroid plexus	tissue	67.6
Endometrium 1	tissue	64.7	medium
Smooth muscle	tissue	64.4	not detected
Fallopian tube	tissue	43.9	not detected
Urinary bladder	tissue	41.7	not detected
Tongue	tissue	41.2
Seminal vesicle	tissue	40.7	not detected
Lung	tissue	40.3	not detected
Heart muscle	tissue	36.2	not detected
Skeletal muscle	tissue	29.2	not detected
Breast	tissue	26.8	medium
Spleen	tissue	26.0	not detected
Appendix	tissue	25.9	not detected
Lymph node	tissue	25.8	not detected
Skin 1	tissue	25.4	low
Prostate	tissue	25.2	low
Epididymis	tissue	22.9	low
Spinal cord	tissue	22.9
Nucleus accumbens	tissue	22.8
Pituitary gland	tissue	22.4
Adrenal gland	tissue	22.1	not detected
Hippocampus	tissue	20.7	not detected
Parathyroid gland	tissue	20.6	low
Esophagus	tissue	20.5	not detected
Superior colliculi	tissue	20.4
Postcentral gyrus	tissue	20.0
Thyroid gland	tissue	19.8	not detected
Locus coeruleus	tissue	19.8
Kidney	tissue	19.1	medium
Pancreas	tissue	16.7	not detected
Colon	tissue	16.2	not detected
Substantia nigra	tissue	16.1
Cerebral cortex	tissue	15.0	low
Insular cortex	tissue	15.0
Hippocampal formation	tissue	14.6
Entorhinal cortex	tissue	14.6
Testis	tissue	14.2	high
Temporal cortex	tissue	14.1
Rectum	tissue	13.3	not detected
Motor cortex	tissue	13.2
Amygdala	tissue	13.1
Tonsil	tissue	12.9	low
Somatosensory cortex	tissue	12.8
Salivary gland	tissue	12.6	not detected
Prefrontal cortex	tissue	12.4
Basal ganglia	tissue	12.3	not detected
Retrosplenial cortex	tissue	12.1
Retrosplenial and cingulate cortex	tissue	11.9
Medulla oblongata	tissue	11.7
Occipital cortex	tissue	11.6
Small intestine	tissue	11.5	not detected
Caudate putamen	tissue	11.3
Thalamus	tissue	11.2
Duodenum	tissue	11.2	not detected

Brain sub-regions (HPA Brain Atlas): detected in 191; highest nTPM — Blood vessel (190.0), Orbitofrontal gyrus, anterior (42.4), Posterior thalamic nucleus (35.0), Nucleus basalis of Meynert (33.3), Inferior frontal gyrus, opercular (30.8).

Regulation

Is transcription factor: no

Upstream regulators (CollecTRI, top): AP1, ATM, FGF9, JUN, JUND, MYC, MYCN, NFKB, PBX1, PPARG, SPI1, TP53, TP73, ZFHX3, ZNF24

miRNA regulators (miRDB)

Targeting PDGFRB by miRDB confidence (max_score; target_count = how many genes the miRNA targets in total — lower means more specific).

showing 30 of 117 miRNAs:

miRNA	Max score	Avg score	miRNA target_count
HSA-MIR-9-5P	100.00	72.28	2361
HSA-MIR-30A-5P	100.00	76.31	3233
HSA-MIR-30B-5P	100.00	76.29	3248
HSA-MIR-30C-5P	100.00	76.29	3248
HSA-MIR-30D-5P	100.00	76.32	3233
HSA-MIR-30E-5P	100.00	76.32	3242
HSA-MIR-574-5P	100.00	66.01	989
HSA-MIR-3134	100.00	66.43	777
HSA-MIR-4692	100.00	67.32	2066
HSA-MIR-548N	99.98	71.94	4170
HSA-MIR-568	99.98	69.86	2084
HSA-MIR-12136	99.98	72.81	5713
HSA-MIR-499A-5P	99.98	70.79	1323
HSA-MIR-6778-3P	99.96	67.29	2693
HSA-MIR-4725-3P	99.96	69.53	2520
HSA-MIR-6780B-5P	99.96	69.60	2562
HSA-MIR-6721-5P	99.93	68.92	2981
HSA-MIR-498-3P	99.91	71.27	1114
HSA-MIR-106A-5P	99.90	73.94	2683
HSA-MIR-4731-5P	99.89	67.23	2537
HSA-MIR-17-5P	99.89	73.83	2665
HSA-MIR-106B-5P	99.88	74.72	2795
HSA-MIR-20A-5P	99.88	74.76	2769
HSA-MIR-20B-5P	99.88	74.01	2621
HSA-MIR-519D-3P	99.88	73.97	2607
HSA-MIR-526B-3P	99.88	74.06	2587
HSA-MIR-93-5P	99.88	73.98	2606
HSA-MIR-4492	99.87	68.25	3611
HSA-MIR-4728-5P	99.85	69.39	4718
HSA-MIR-1321	99.84	65.30	1811

Functional genomics

gnomAD constraint: pLI 0.938, LOEUF 0.504, missense Z 2.86 — population loss-of-function intolerance (pLI ≥ 0.9 = LoF-intolerant; lower LOEUF = more constrained). gnomAD

Regional missense constraint (gnomAD)

ENST00000261799 splits into 3 regions with different missense tolerance; 0 are missense-constrained. Missense variants in a constrained region (low observed/expected) are more likely to be pathogenic. gnomAD

Region (GRCh38)	Missense obs / exp	o/e	Constrained
5:150,115,766–150,118,840	202 / 214.3	0.94	no
5:150,118,841–150,121,004	68 / 153.3	0.44	no
5:150,121,005–150,137,047	879 / 1108.6	0.79	no

Literature-anchored findings (GeneRIF, showing 40)

• activates phosphatidylinositol 3 (PI3) kinase and requires PI3 kinase to regulate the cell cycle [TEL/platelet-derived growth factor receptor beta] (PMID:11861293)
• With the advent of targeted signal transduction therapy, patients with rearrangement of PDGFRB might be better classified as a distinct subgroup of MPD/MDS. (PMID:11919393)
• Eight out of nine ESFT cell lines were found to express significant levels of beta-PDGFR. Beta-platelet-derived growth factor receptor mediates motility and growth of Ewing’s sarcoma cells. (PMID:12700668)
• overexpressing wild-type PDGFR on exposure to cognate growth factor activate glucose transport, GLUT4 translocation, and the serine-threonine protein kinase Akt/protein kinase B to a degree comparable with that produced in response to insulin. (PMID:12933652)
• YXXM motifs in the PDGFR serve two distinct functions: PI 3-kinase recruitment and lysosomal targeting (PMID:12941951)
• PDGFR is degraded in a process in which NF2 inhibits schwannoma cell growth (PMID:14612918)
• a unique interaction between S1P3 and PDGFR, and demonstration of a specific role for S1P3 in S1P-induced Akt activation (PMID:14657000)
• Both types of PDGF receptors are expressed in follicular keratinocytes, whereas dermal papilla cells only express PDGF receptor beta on the protein level (PMID:14705808)
• results confirm the high frequency of BCR-ABL kinase domain mutations in patients with secondary resistance to imatinib and exclude mutations of the activation loops of KIT, PDGFRA and PDGFRB as causes of resistance in patients without ABL mutations (PMID:14745431)
• ligand-activated KIT and platelet-derived growth factor receptor beta tyrosine kinase receptors are expressed in synovial sarcoma (PMID:14871970)
• allosteric inhibition of the PDGF beta-receptor by its C-terminal tail is one of the mechanisms involved in keeping the receptor inactive in the absence of ligand (PMID:14996833)
• the WW-like domain in the context of TELPDGFbetaR may have both positive and negative regulatory roles in kinase activation. (PMID:15054045)
• GPRK2-mediated PDGFRbeta seryl phosphorylation plays an important role in desensitizing PDGFRbeta; this desensitization involves GPRK2-mediated phosphorylation of PDGFRbeta Ser(1104), with consequent dissociation of the PDGFRbeta from NHERF. (PMID:15271984)
• an activating point mutation results in a deregulated PDGFRbeta with oncogenic predisposition (PMID:15284236)
• In transgenic mice PDGF stimulated glucose transport into skeletal muscle in vitro and in vivo. (PMID:15504957)
• Data demonstrate that type I collagen synergistically enhances platelet-derived growth factor (PDGF)-induced smooth muscle cell proliferation through Src-dependent crosstalk between the alpha2beta1 integrin and the PDGF receptor beta. (PMID:15522237)
• hyperchemotaxis towards PDGFRB is likely to depend in part on phosphorylation of the cytoplasmic domain of TF (PMID:15630487)
• Data show that growth factor-dependent cell survival in vascular smooth muscle cells is mediated only by activation of platelet-derived growth factor-beta receptors and the PI3K/Akt pathway. (PMID:15640155)
• Blocking VEGF and PDGF receptor signaling in cardiac allografts has distinctive effects on inflammation and survival. (PMID:15665766)
• study demonstrates that platelet-derived growth factor receptor alpha and beta, and c-kit protein are expressed in a high percentage of epithelial ovarian cancers (PMID:15791568)
• Western blot showed a high amount of PDGFRalpha and beta proteins in primary stromal cells that could not be detected in prostatic cancer cells. (PMID:15862965)
• PDGFR-beta activation promotes its association with the low density lipoprotein receptor-related protein (PMID:15944146)
• PDGFR-dependent cell detachment is induced by S1P via inhibition of beta1 integrin in HEK293 cells (PMID:15987639)
• Resultrs suggest that activated platelet-derived growth factor receptor-beta (PDGFRbeta) phosphorylates GRK2 tyrosyl residues and thereby activates GRK2, which then serine-phosphorylates and desensitizes the PDGFRbeta. (PMID:15994317)
• alpha-PDGFR expression might identify prostate cancer cells with the highest propensity to metastasize to the skeleton (PMID:16007172)
• PDGF-BB/PDGF-R interaction is vital in nicotine’s mitogenic actions on human aortic smooth muscle cells (PMID:16149045)
• Serum starvation significantly increases PDGFbeta-R mRNA and protein expression in smooth muscle cells. PDGF-BB stimulates cell survival but not proliferation in serum-starved SMCs (PMID:16407661)
• As such, caveolae and caveolin-1 coordinate PDGF receptor signaling, leading to myocyte proliferation, and inhibit constitutive activity of p42/p44 MAPK to sustain cell quiescence. (PMID:16617096)
• The involvement of the PDGFRbeta gene in SFT is compatible with a pericytic derivation, also supporting a possible role of this tyrosine kinase in malignant transformation and in the adoption of novel molecular therapies. (PMID:16899864)
• In midgut carcinoid tumor stroma PDGFRalpha was expressed in 35%, PDGFRbeta in 94% and EGFR in 9%. (PMID:17047316)
• Alix inhibits down-regulation of PDGFRbeta by modulating the interaction between c-Cbl and the receptor, thereby affecting the ubiquitination of the receptor (PMID:17082185)
• The PDGFRB was highly expressed and phosphorylated with the absence of gain-of-function mutations and the presence of the cognate ligands, strongly support the hypothesis that the activation mechanism is the autocrine/paracrine loop in chordoma. (PMID:17145809)
• PDGFRbeta and FLT3 mutants are inhibited by sorafenib (PMID:17229632)
• numerous partner genes fuse to PDGFRB in BCR-ABL negative chronic myeloproliferative disorders (PMID:17296564)
• no activating mutations in the PDGFRB gene were found in children with Ewing sarcoma (PMID:17298867)
• Gene rearrangement found in a case of underlying chronic myelomonocytic leukaemia in Noonan Syndrome. (PMID:17301821)
• these observations indicate that an IE and/or E human cytomegalovirus protein(s) downregulates the expression of PDGFR-alpha and -beta in smooth muscle cells (PMID:17344284)
• Stimulatory antibodies to PDGFR-A&-B were found selectively in all patients with extensive cGVHD but in none of the patients without cGVHD. Higher levels were detected in patients with generalized skin involvement and/or lung fibrosis. (PMID:17363728)
• association of the PDGFRbeta with lipid raft microdomains renders it susceptible to LXA(4)-mediated dephosphorylation by possible reactivation of oxidatively inactivated SHP-2. (PMID:17403678)
• The presence of PDGFB and PDGFRB mRNAs was demonstrated in 26 and 21 of 26 cases dermatofibrosarcoma protuberans. The fusion protein, which is processed by the COL1A1-PDGFB transcripts, can serve as a functional ligand for PDGFRB (PMID:17431412)

Cross-species orthologs

3 orthologs

Organism	Symbol	Gene ID
danio_rerio	pdgfrb	ENSDARG00000100897
mus_musculus	Pdgfrb	ENSMUSG00000024620
rattus_norvegicus	Pdgfrb	ENSRNOG00000018461

Paralogs (53): INSRR (ENSG00000027644), MUSK (ENSG00000030304), FLT4 (ENSG00000037280), EPHA3 (ENSG00000044524), ROS1 (ENSG00000047936), LTK (ENSG00000062524), ERBB3 (ENSG00000065361), TIE1 (ENSG00000066056), FGFR2 (ENSG00000066468), FGFR3 (ENSG00000068078), EPHA8 (ENSG00000070886), FGFR1 (ENSG00000077782), EPHA6 (ENSG00000080224), TYRO3 (ENSG00000092445), FLT1 (ENSG00000102755), MET (ENSG00000105976), EPHB6 (ENSG00000106123), EPHA4 (ENSG00000116106), TEK (ENSG00000120156), FLT3 (ENSG00000122025), KDR (ENSG00000128052), EPHB2 (ENSG00000133216), PDGFRA (ENSG00000134853), EPHA7 (ENSG00000135333), IGF1R (ENSG00000140443), NTRK3 (ENSG00000140538), ERBB2 (ENSG00000141736), EPHA2 (ENSG00000142627), EPHA5 (ENSG00000145242), EGFR (ENSG00000146648), EPHA1 (ENSG00000146904), NTRK2 (ENSG00000148053), MERTK (ENSG00000153208), EPHB1 (ENSG00000154928), KIT (ENSG00000157404), FGFR4 (ENSG00000160867), DDR2 (ENSG00000162733), RYK (ENSG00000163785), MST1R (ENSG00000164078), LMTK2 (ENSG00000164715), RET (ENSG00000165731), AXL (ENSG00000167601), ROR2 (ENSG00000169071), ALK (ENSG00000171094), INSR (ENSG00000171105), ERBB4 (ENSG00000178568), CSF1R (ENSG00000182578), EPHB3 (ENSG00000182580), EPHA10 (ENSG00000183317), ROR1 (ENSG00000185483), EPHB4 (ENSG00000196411), NTRK1 (ENSG00000198400), DDR1 (ENSG00000204580)

Mouse-model phenotypes

Observed phenotypes of the mouse ortholog (MGI:97531) from MGI (Alliance of Genome Resources) — knockout/mutant phenotypes, ranked by annotation count. 87 distinct phenotype terms.

Mouse phenotype (MP)	Records
abnormal pericyte morphology	3
kidney hemorrhage	2
abnormal blood vessel morphology	2
hemorrhage	2
hydrops fetalis	2
abnormal retina vasculature morphology	2
eye hemorrhage	2
perimembraneous ventricular septal defect	2
abnormal angiogenesis	1
abnormal heart morphology	1
overriding aortic valve	1
enlarged heart	1
double outlet right ventricle	1
schistocytosis	1
decreased cell proliferation	1
short snout	1
abnormal pulmonary artery morphology	1
abnormal kidney vasculature morphology	1
abnormal social investigation	1
increased circulating triglyceride level	1
anemia	1
postnatal growth retardation	1
impaired wound healing	1
thymus hypoplasia	1
intracranial hemorrhage	1

+62 more (showing top 25).

Additional cross-species homologs

Sequence homologs in species beyond Ensembl Compara’s model organisms, by Diamond local protein alignment (% sequence identity; best hit per species). Lower-identity rows are more distant homologs. The matched accessions’ gene symbols aren’t in biobtree yet, so each row shows the UniProt accession.

Organism	UniProt	Identity	Method
Bos taurus	P43481	99.4%	Diamond
Capra hircus	Q28317	99.4%	Diamond
Felis catus	Q28889	99.2%	Diamond
Canis lupus familiaris	O97799	98.4%	Diamond
Sus scrofa	Q2HWD6	98.1%	Diamond
Callithrix jacchus	Q76II0	94.6%	Diamond
Gallus gallus	P18461	92.7%	Diamond
Sibon nebulatus	Q8AX00	91.1%	Diamond
Notophthalmus viridescens	Q91147	87.9%	Diamond
Pleurodeles waltl	Q91285	87.8%	Diamond
Coturnix coturnix	Q90330	81.0%	Diamond
Xenopus laevis	P22182	80.6%	Diamond
Takifugu rubripes	Q8AXC7	73.2%	Diamond
Coturnix japonica	P52583	73.1%	Diamond
Ciona intestinalis	Q4H3K6	60.1%	Diamond
Drosophila melanogaster	Q09147	55.0%	Diamond
Dugesia japonica	Q8MY86	51.0%	Diamond
Hydra vulgaris	Q86PM4	50.2%	Diamond
Caenorhabditis elegans	Q21038	49.5%	Diamond
Strongylocentrotus purpuratus	Q26614	46.4%	Diamond
Bombyx mori	D2IYS2	44.0%	Diamond
Feline sarcoma virus (STRAIN HARDY-ZUCKERMAN 4)	P04048	99.2%	Diamond
Feline sarcoma virus (STRAIN MCDONOUGH)	P00545	99.1%	Diamond

Genomic neighbors (locus context)

Genes flanking this one on the chromosome (NCBI/Entrez gene neighborhood). Positional context only — some neighbors share regulatory elements (bidirectional promoters, antisense/overlapping transcripts), but chromosomal adjacency is not itself a functional relationship (see Interactions for that).

Symbol	Type	Entrez
CSF1R	protein-coding	1436
SLC6A7	protein-coding	6534
CAMK2A	protein-coding	815
CDX1	protein-coding	1044
HMGXB3	protein-coding	22993
TIGD6	protein-coding	81789
ARSI	protein-coding	340075
SLC26A2	protein-coding	1836

Protein

Protein identifiers

Platelet-derived growth factor receptor beta — P09619 (reviewed: P09619)

Alternative names: Beta platelet-derived growth factor receptor, Beta-type platelet-derived growth factor receptor, CD140 antigen-like family member B, Platelet-derived growth factor receptor 1

All UniProt accessions (4): P09619, E5RH16, E5RII0, E5RJ14

UniProt curated annotations — full annotation on UniProt →

Function. Tyrosine-protein kinase that acts as a cell-surface receptor for homodimeric PDGFB and PDGFD and for heterodimers formed by PDGFA and PDGFB, and plays an essential role in the regulation of embryonic development, cell proliferation, survival, differentiation, chemotaxis and migration. Plays an essential role in blood vessel development by promoting proliferation, migration and recruitment of pericytes and smooth muscle cells to endothelial cells. Plays a role in the migration of vascular smooth muscle cells and the formation of neointima at vascular injury sites. Required for normal development of the cardiovascular system. Required for normal recruitment of pericytes (mesangial cells) in the kidney glomerulus, and for normal formation of a branched network of capillaries in kidney glomeruli. Promotes rearrangement of the actin cytoskeleton and the formation of membrane ruffles. Binding of its cognate ligands - homodimeric PDGFB, heterodimers formed by PDGFA and PDGFB or homodimeric PDGFD -leads to the activation of several signaling cascades; the response depends on the nature of the bound ligand and is modulated by the formation of heterodimers between PDGFRA and PDGFRB. Phosphorylates PLCG1, PIK3R1, PTPN11, RASA1/GAP, CBL, SHC1 and NCK1. Activation of PLCG1 leads to the production of the cellular signaling molecules diacylglycerol and inositol 1,4,5-trisphosphate, mobilization of cytosolic Ca(2+) and the activation of protein kinase C. Phosphorylation of PIK3R1, the regulatory subunit of phosphatidylinositol 3-kinase, leads to the activation of the AKT1 signaling pathway. Phosphorylation of SHC1, or of the C-terminus of PTPN11, creates a binding site for GRB2, resulting in the activation of HRAS, RAF1 and down-stream MAP kinases, including MAPK1/ERK2 and/or MAPK3/ERK1. Promotes phosphorylation and activation of SRC family kinases. Promotes phosphorylation of PDCD6IP/ALIX and STAM. Receptor signaling is down-regulated by protein phosphatases that dephosphorylate the receptor and its down-stream effectors, and by rapid internalization of the activated receptor.

Subunit / interactions. Interacts with homodimeric PDGFB and PDGFD, and with heterodimers formed by PDGFA and PDGFB. May also interact with homodimeric PDGFC. Monomer in the absence of bound ligand. Interaction with homodimeric PDGFB, heterodimers formed by PDGFA and PDGFB or homodimeric PDGFD, leads to receptor dimerization, where both PDGFRA homodimers and heterodimers with PDGFRB are observed. Interacts with SH2B2/APS. Interacts directly (tyrosine phosphorylated) with SHB. Interacts (tyrosine phosphorylated) with PIK3R1 and RASA1. Interacts (tyrosine phosphorylated) with CBL. Interacts (tyrosine phosphorylated) with SRC and SRC family kinases. Interacts (tyrosine phosphorylated) with PIK3C2B, maybe indirectly. Interacts (tyrosine phosphorylated) with SHC1, GRB7, GRB10 and NCK1. Interaction with GRB2 is mediated by SHC1. Interacts (via C-terminus) with NHERF1.

Subcellular location. Cell membrane. Cytoplasmic vesicle. Lysosome lumen.

Post-translational modifications. Autophosphorylated on tyrosine residues upon ligand binding. Autophosphorylation occurs in trans, i.e. one subunit of the dimeric receptor phosphorylates tyrosine residues on the other subunit. Phosphorylation at Tyr-579, and to a lesser degree, at Tyr-581, is important for interaction with SRC family kinases. Phosphorylation at Tyr-740 and Tyr-751 is important for interaction with PIK3R1. Phosphorylation at Tyr-751 is important for interaction with NCK1. Phosphorylation at Tyr-771 and Tyr-857 is important for interaction with RASA1/GAP. Phosphorylation at Tyr-857 is important for efficient phosphorylation of PLCG1 and PTPN11, resulting in increased phosphorylation of AKT1, MAPK1/ERK2 and/or MAPK3/ERK1, PDCD6IP/ALIX and STAM, and in increased cell proliferation. Phosphorylation at Tyr-1009 is important for interaction with PTPN11. Phosphorylation at Tyr-1009 and Tyr-1021 is important for interaction with PLCG1. Phosphorylation at Tyr-1021 is important for interaction with CBL; PLCG1 and CBL compete for the same binding site. Dephosphorylated by PTPRJ at Tyr-751, Tyr-857, Tyr-1009 and Tyr-1021. Dephosphorylated by PTPN2 at Tyr-579 and Tyr-1021. N-glycosylated. Ubiquitinated. After autophosphorylation, the receptor is polyubiquitinated, leading to its degradation.

Disease relevance. A chromosomal aberration involving PDGFRB is found in a form of chronic myelomonocytic leukemia (CMML). Translocation t(5;12)(q33;p13) with EVT6/TEL. It is characterized by abnormal clonal myeloid proliferation and by progression to acute myelogenous leukemia (AML). Myeloproliferative disorder chronic with eosinophilia (MPE) [MIM:131440] A hematologic disorder characterized by malignant eosinophils proliferation. The gene represented in this entry may be involved in disease pathogenesis. Chromosomal aberrations involving PDGFRB have been found in many instances of chronic myeloproliferative disorder with eosinophilia. Translocation t(5;12) with ETV6 on chromosome 12 creating an PDGFRB-ETV6 fusion protein. Translocation t(5;15)(q33;q22) with TP53BP1 creating a PDGFRB-TP53BP1 fusion protein. Translocation t(1;5)(q23;q33) that forms a PDE4DIP-PDGFRB fusion protein. Translocation t(5;6)(q33-34;q23) with CEP85L that fuses the 5’-end of CEP85L (isoform 4) to the 3’-end of PDGFRB. Leukemia, acute myelogenous (AML) [MIM:601626] A subtype of acute leukemia, a cancer of the white blood cells. AML is a malignant disease of bone marrow characterized by maturational arrest of hematopoietic precursors at an early stage of development. Clonal expansion of myeloid blasts occurs in bone marrow, blood, and other tissue. Myelogenous leukemias develop from changes in cells that normally produce neutrophils, basophils, eosinophils and monocytes. The gene represented in this entry may be involved in disease pathogenesis. A chromosomal aberration involving PDGFRB has been found in a patient with AML. Translocation t(5;14)(q33;q32) with TRIP11. Leukemia, juvenile myelomonocytic (JMML) [MIM:607785] An aggressive pediatric myelodysplastic syndrome/myeloproliferative disorder characterized by malignant transformation in the hematopoietic stem cell compartment with proliferation of differentiated progeny. Patients have splenomegaly, enlarged lymph nodes, rashes, and hemorrhages. The gene represented in this entry may be involved in disease pathogenesis. A chromosomal aberration involving PDGFRB has been found in a patient with JMML. Translocation t(5;17)(q33;p11.2) with SPECC1. Basal ganglia calcification, idiopathic, 4 (IBGC4) [MIM:615007] A form of basal ganglia calcification, an autosomal dominant condition characterized by symmetric calcification in the basal ganglia and other brain regions. Affected individuals can either be asymptomatic or show a wide spectrum of neuropsychiatric symptoms, including parkinsonism, dystonia, tremor, ataxia, dementia, psychosis, seizures, and chronic headache. Serum levels of calcium, phosphate, alkaline phosphatase and parathyroid hormone are normal. The neuropathological hallmark of the disease is vascular and pericapillary calcification, mainly of calcium phosphate, in the affected brain areas. The disease is caused by variants affecting the gene represented in this entry. Myofibromatosis, infantile 1 (IMF1) [MIM:228550] A rare mesenchymal disorder characterized by the development of benign tumors in the skin, striated muscles, bones, and, more rarely, visceral organs. Subcutaneous or soft tissue nodules commonly involve the skin of the head, neck, and trunk. Skeletal and muscular lesions occur in about half of the patients. Lesions may be solitary or multicentric, and they may be present at birth or become apparent in early infancy or occasionally in adult life. Visceral lesions are associated with high morbidity and mortality. The disease is caused by variants affecting the gene represented in this entry. Kosaki overgrowth syndrome (KOGS) [MIM:616592] A syndrome characterized by somatic overgrowth, distinctive facial features, hyperelastic and fragile skin, and progressive neurologic deterioration with white matter lesions on brain imaging. The disease is caused by variants affecting the gene represented in this entry. Premature aging syndrome, Penttinen type (PENTT) [MIM:601812] An autosomal dominant syndrome characterized by a prematurely aged appearance with lipoatrophy, epidermal and dermal atrophy along with hypertrophic lesions that resemble scars, thin hair, proptosis, underdeveloped cheekbones, and marked acro-osteolysis. The disease is caused by variants affecting the gene represented in this entry. Ocular pterygium-digital keloid dysplasia syndrome (OPDKD) [MIM:621091] An autosomal dominant disorder that presents in childhood with aggressive ingrowth of vascularized connective tissue on the cornea, ultimately leading to loss of vision. Later, affected individuals develop keloids on digits after minor trauma, but are otherwise healthy. The disease may be caused by variants affecting the gene represented in this entry.

Activity regulation. Present in an inactive conformation in the absence of bound ligand. Binding of PDGFB and/or PDGFD leads to dimerization and activation by autophosphorylation on tyrosine residues. Inhibited by imatinib.

Similarity. Belongs to the protein kinase superfamily. Tyr protein kinase family. CSF-1/PDGF receptor subfamily.

Isoforms (2)

UniProt ID	Names	Canonical?
P09619-1	1	yes
P09619-2	2

RefSeq proteins (3): NP_001341945, NP_001341946, NP_002600* (*=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR000719	Prot_kinase_dom	Domain
IPR001245	Ser-Thr/Tyr_kinase_cat_dom	Domain
IPR001824	Tyr_kinase_rcpt_3_CS	Conserved_site
IPR003598	Ig_sub2	Domain
IPR003599	Ig_sub	Domain
IPR007110	Ig-like_dom	Domain
IPR008266	Tyr_kinase_AS	Active_site
IPR011009	Kinase-like_dom_sf	Homologous_superfamily
IPR013783	Ig-like_fold	Homologous_superfamily
IPR017441	Protein_kinase_ATP_BS	Binding_site
IPR020635	Tyr_kinase_cat_dom	Domain
IPR027288	PGFRB	Family
IPR036179	Ig-like_dom_sf	Homologous_superfamily
IPR050122	RTK	Family
IPR055238	VEGFR1-3_N_Ig-like	Domain

Pfam: PF07714, PF13927, PF22854, PF25305

Enzyme classification (BRENDA)

• EC 2.7.10.1 — receptor protein-tyrosine kinase (BRENDA: 44 organisms, 214 substrates, 574 inhibitors, 11 Km, 0 kcat entries)

Substrate kinetics (BRENDA)

4 substrates with measured Km, best-characterized 4. Km ranges are aggregated across organisms/conditions.

Substrate	Km (mM)	Measurements
ATP	0.0011–0.129	4
AC-DYFE-6-CHLORO-W-NHME	0.0051	1
AC-DYFGW-NHME	0.07	1
YFEW	0.232	1

Catalyzed reactions (Rhea)

• L-tyrosyl-[protein] + ATP = O-phospho-L-tyrosyl-[protein] + ADP + H(+) (RHEA:10596)

UniProt features (113 total): strand 23, sequence variant 17, modified residue 16, mutagenesis site 13, glycosylation site 11, domain 6, disulfide bond 4, turn 3, helix 3, site 3, compositionally biased region 2, binding site 2, topological domain 2, splice variant 2, signal peptide 1, chain 1, region of interest 1, active site 1, transmembrane region 1, sequence conflict 1

Structure

Experimental structures (PDB)

9 structures by resolution:

PDB	Title	Method	Resolution (Å)
1SHA	CRYSTAL STRUCTURE OF THE PHOSPHOTYROSINE RECOGNITION DOMAIN SH2 OF V-SRC COMPLEXED WITH …	X-RAY DIFFRACTION	1.5
1H9O	PHOSPHATIDYLINOSITOL 3-KINASE, P85-ALPHA SUBUNIT: C-TERMINAL SH2 DOMAIN COMPLEXED WITH A …	X-RAY DIFFRACTION	1.79
1GQ5	Structural Determinants of the NHERF Interaction with beta2-AR and PDGFR	X-RAY DIFFRACTION	2.2
3MJG	The structure of a platelet derived growth factor receptor complex	X-RAY DIFFRACTION	2.3
11UE	Structure of PDGFRb Kinase Domain Bound to JNJ-PDGFRBi-1	X-RAY DIFFRACTION	2.32
2IUI	Crystal structure of the PI3-kinase p85 N-terminal SH2 domain in complex with PDGFR …	X-RAY DIFFRACTION	2.4
2L6W	PDGFR beta-TM	SOLUTION NMR
2PLD	NUCLEAR MAGNETIC RESONANCE STRUCTURE OF AN SH2 DOMAIN OF PHOSPHOLIPASE C-GAMMA1 COMPLEXED …	SOLUTION NMR
2PLE	NUCLEAR MAGNETIC RESONANCE STRUCTURE OF AN SH2 DOMAIN OF PHOSPHOLIPASE C-GAMMA1 COMPLEXED …	SOLUTION NMR

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-P09619-F1	72.96	0.30

Human Protein Atlas

Protein class: Enzymes, ENZYME proteins, Transferases, Kinases, Tyr protein kinases, CD markers, Transporters, Accessory Factors Involved in Transport, Predicted membrane proteins, Predicted intracellular proteins, Plasma proteins, RAS pathway related proteins, Cancer-related genes, Candidate cancer biomarkers, Disease related genes, FDA approved drug targets, Biotech drugs, Small molecule drugs, Human disease related genes

Protein evidence: Evidence at protein level

Subcellular location (HPA, imaging): vesicles; golgi apparatus

Antibody reliability (HPA): IH enhanced · IF supported

Functional residue map

Curated UniProt residues grouped by drug-discovery relevance — catalytic, ligand-binding, modification, and mutation-validated positions. Source: UniProtKB sequence features.

Catalytic / active sites (4)

Position	Role
826	proton acceptor
527–528	breakpoint for insertion to form pde4dip-pdgfrb fusion protein
527–528	breakpoint for translocation to form trip11-pdgfrb
558–559	breakpoint for translocation to form the cep85l-pdgfrb fusion protein

Ligand- & substrate-binding residues (2)

Position	Role
606–614	ATP
634	ATP

Post-translational modifications (16)

Type	Positions
Phosphotyrosine	562, 579, 581, 686, 716, 740, 751, 763, 771, 775, 778, 857, 934, 970, 1009, 1021

Disulfide bonds (4)

Type	Positions
Disulfide bond	54–100, 149–190, 235–291, 436–508

Glycosylation sites (11)

Type	Positions
N-linked (glcnac…) asparagine	45, 89, 103, 215, 230, 292, 307, 354, 371, 468, 479

Mutagenesis-validated functional residues (13)

Position	Phenotype
579	loss of kinase activity; when associated with f-581. strongly reduces interaction with src family kinases. no effect on interaction with …
581	loss of kinase activity; when associated with f-579. no effect on interaction with grb10.
634	loss of kinase activity. abolishes interaction with rasa1. no effect on phosphatidylinositol 3-kinase activity.
716	no effect neither on interaction with grb10 and rasa1 nor on phosphatidylinositol 3-kinase activity.
740	strongly reduces up-regulation of cell proliferation; when associated with f-751. strongly decreases phosphatidylinositol 3-kinase …
751	strongly reduces up-regulation of cell proliferation; when associated with f-740. abolishes phosphatidylinositol 3-kinase activity and …
763	no effect on interaction with rasa1 and on phosphatidylinositol 3-kinase activity.
771	loss of interaction with grb10. abolishes interaction with rasa1. no effect on phosphatidylinositol 3-kinase activity.
775	no effect on interaction with rasa1 and on phosphatidylinositol 3-kinase activity.
778	strongly reduces expression levels.
857	reduces kinase activity. no effect on interaction with grb10. abolishes interaction with rasa1. no effect on phosphatidylinositol 3-kinase …
1009	no effect on interaction with grb10. abolishes interaction with plcg1; when associated with f-1021.
1021	strongly reduces up-regulation of cell proliferation. abolishes interaction with plcg1; when associated with f-1009. no effect on …

Function

Pathways and Gene Ontology

Reactome pathways

6 curated (TAS) of 15; 4 disease pathways. Curated-first; evidence = TAS (manually curated) vs IEA (electronic inference).

15 pathways:

ID	Pathway	Evidence
R-HSA-2219530	Constitutive Signaling by Aberrant PI3K in Cancer ⚕	curated
R-HSA-186763	Downstream signal transduction	curated
R-HSA-6811558	PI5P, PP2A and IER3 Regulate PI3K/AKT Signaling	curated
R-HSA-1257604	PIP3 activates AKT signaling	curated
R-HSA-5673001	RAF/MAP kinase cascade	curated
R-HSA-186797	Signaling by PDGF	curated
R-HSA-1643685	Disease ⚕	—
R-HSA-5663202	Diseases of signal transduction by growth factor receptors and second messengers ⚕	—
R-HSA-2219528	PI3K/AKT Signaling in Cancer ⚕	—
R-HSA-9006925	Intracellular signaling by second messengers	—
R-HSA-5683057	MAPK family signaling cascades	—
R-HSA-5684996	MAPK1/MAPK3 signaling	—
R-HSA-199418	Negative regulation of the PI3K/AKT network	—
R-HSA-162582	Signal Transduction	—
R-HSA-9006934	Signaling by Receptor Tyrosine Kinases	—

MSigDB gene sets: 843 (showing top): PID_SHP2_PATHWAY, GOBP_PLATELET_DERIVED_GROWTH_FACTOR_RECEPTOR_SIGNALING_PATHWAY, GOBP_POSITIVE_REGULATION_OF_CALCIUM_ION_TRANSPORT, TGGTGCT_MIR29A_MIR29B_MIR29C, RNGTGGGC_UNKNOWN, GOBP_POSITIVE_REGULATION_OF_MITOTIC_NUCLEAR_DIVISION, GOBP_CELL_MIGRATION_INVOLVED_IN_HEART_DEVELOPMENT, PID_S1P_S1P1_PATHWAY, GOBP_MUSCLE_TISSUE_DEVELOPMENT, CHIBA_RESPONSE_TO_TSA_UP, GOBP_VASCULAR_ENDOTHELIAL_GROWTH_FACTOR_SIGNALING_PATHWAY, GOBP_POSITIVE_REGULATION_OF_DNA_BIOSYNTHETIC_PROCESS, GOBP_REGULATION_OF_CALCIUM_MEDIATED_SIGNALING, GOBP_METANEPHROS_DEVELOPMENT, GOBP_CORONARY_VASCULATURE_DEVELOPMENT

GO Biological Process (41): angiogenesis (GO:0001525), signal transduction (GO:0007165), cell surface receptor protein tyrosine kinase signaling pathway (GO:0007169), positive regulation of cell population proliferation (GO:0008284), smooth muscle adaptation (GO:0014805), positive regulation of smooth muscle cell migration (GO:0014911), peptidyl-tyrosine phosphorylation (GO:0018108), positive regulation of cell migration (GO:0030335), regulation of actin cytoskeleton organization (GO:0032956), cell migration involved in vasculogenesis (GO:0035441), platelet-derived growth factor receptor-beta signaling pathway (GO:0035791), positive regulation of metanephric mesenchymal cell migration by platelet-derived growth factor receptor-beta signaling pathway (GO:0035793), aorta morphogenesis (GO:0035909), positive regulation of cell proliferation by VEGF-activated platelet derived growth factor receptor signaling pathway (GO:0038091), positive regulation of MAP kinase activity (GO:0043406), positive regulation of mitotic nuclear division (GO:0045840), protein autophosphorylation (GO:0046777), platelet-derived growth factor receptor signaling pathway (GO:0048008), positive regulation of smooth muscle cell proliferation (GO:0048661), positive regulation of calcium-mediated signaling (GO:0050850), positive regulation of chemotaxis (GO:0050921), positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transduction (GO:0051897), cardiac myofibril assembly (GO:0055003), cell chemotaxis (GO:0060326), cell migration involved in coronary angiogenesis (GO:0060981), retina vasculature development in camera-type eye (GO:0061298), positive regulation of ERK1 and ERK2 cascade (GO:0070374), smooth muscle cell chemotaxis (GO:0071670), metanephric glomerular mesangial cell proliferation involved in metanephros development (GO:0072262), metanephric glomerular capillary formation (GO:0072277), positive regulation of calcium ion import (GO:0090280), positive regulation of reactive oxygen species metabolic process (GO:2000379), positive regulation of DNA biosynthetic process (GO:2000573), blood vessel development (GO:0001568), protein phosphorylation (GO:0006468), chemotaxis (GO:0006935), G protein-coupled receptor signaling pathway (GO:0007186), cell migration (GO:0016477), cellular response to platelet-derived growth factor stimulus (GO:0036120), embryonic organ development (GO:0048568), metanephric glomerular mesangium development (GO:0072223)

GO Molecular Function (19): protein kinase activity (GO:0004672), protein tyrosine kinase activity (GO:0004713), platelet activating factor receptor activity (GO:0004992), platelet-derived growth factor receptor activity (GO:0005017), platelet-derived growth factor beta-receptor activity (GO:0005019), GTPase activator activity (GO:0005096), signaling receptor binding (GO:0005102), platelet-derived growth factor receptor binding (GO:0005161), ATP binding (GO:0005524), enzyme binding (GO:0019899), protein kinase binding (GO:0019901), vascular endothelial growth factor binding (GO:0038085), platelet-derived growth factor binding (GO:0048407), phospholipase C activator activity (GO:0160185), nucleotide binding (GO:0000166), transmembrane receptor protein tyrosine kinase activity (GO:0004714), protein binding (GO:0005515), kinase activity (GO:0016301), transferase activity (GO:0016740)

GO Cellular Component (11): nucleus (GO:0005634), cytoplasm (GO:0005737), plasma membrane (GO:0005886), focal adhesion (GO:0005925), membrane (GO:0016020), apical plasma membrane (GO:0016324), cytoplasmic vesicle (GO:0031410), lysosomal lumen (GO:0043202), signaling receptor complex (GO:0043235), ruffle (GO:0001726), cell surface (GO:0009986)

Reactome top-level categories

11 top-level categories:

Category	Pathways
Signal Transduction	3
Intracellular signaling by second messengers	1
Signaling by PDGF	1
Signaling by Receptor Tyrosine Kinases	1
PI3K/AKT Signaling in Cancer	1
MAPK1/MAPK3 signaling	1
Negative regulation of the PI3K/AKT network	1
PIP3 activates AKT signaling	1
Diseases of signal transduction by growth factor receptors and second messengers	1
Disease	1
MAPK family signaling cascades	1

GO top-level categories

showing 60 of 89 GO namespaces:

Category	Terms
cellular anatomical structure	3
cell population proliferation	2
protein phosphorylation	2
cell migration	2
platelet-derived growth factor receptor signaling pathway	2
positive regulation of cell population proliferation	2
protein binding	2
growth factor binding	2
blood vessel morphogenesis	1
anatomical structure formation involved in morphogenesis	1
cell communication	1
cellular process	1
signaling	1
regulation of cellular process	1
cellular response to stimulus	1
enzyme-linked receptor protein signaling pathway	1
regulation of cell population proliferation	1
positive regulation of cellular process	1
muscle adaptation	1
smooth muscle cell migration	1
regulation of smooth muscle cell migration	1
positive regulation of cell migration	1
regulation of cell migration	1
positive regulation of cell motility	1
actin cytoskeleton organization	1
regulation of actin filament-based process	1
regulation of cytoskeleton organization	1
vasculogenesis	1
metanephric mesenchymal cell migration	1
regulation of metanephric mesenchymal cell migration by platelet-derived growth factor receptor-beta signaling pathway	1
positive regulation of metanephric mesenchymal cell migration	1
aorta development	1
artery morphogenesis	1
VEGF-activated platelet-derived growth factor receptor signaling pathway	1
MAP kinase activity	1
regulation of MAP kinase activity	1
positive regulation of MAPK cascade	1
positive regulation of protein serine/threonine kinase activity	1
regulation of mitotic nuclear division	1
positive regulation of nuclear division	1
positive regulation of cell cycle process	1
mitotic nuclear division	1
cell surface receptor protein tyrosine kinase signaling pathway	1
smooth muscle cell proliferation	1
regulation of smooth muscle cell proliferation	1
calcium-mediated signaling	1
regulation of calcium-mediated signaling	1
positive regulation of intracellular signal transduction	1
kinase activity	1
phosphotransferase activity, alcohol group as acceptor	1
catalytic activity, acting on a protein	1
protein kinase activity	1
G protein-coupled receptor activity	1
transmembrane receptor protein tyrosine kinase activity	1
cellular response to platelet-derived growth factor stimulus	1
platelet-derived growth factor binding	1
platelet-derived growth factor receptor activity	1
platelet-derived growth factor receptor-beta signaling pathway	1
GTPase activity	1
enzyme activator activity	1

Experimentally-supported GO annotations

GO terms backed by direct experimental evidence (ECO experimental codes) — 28 of 71 annotations. The rest are phylogenetic / computational / electronic (IEA).

28 experimentally-supported GO terms:

GO term	NS	Evidence
cell chemotaxis	BP	direct assay
peptidyl-tyrosine phosphorylation	BP	direct assay
platelet-derived growth factor receptor signaling pathway	BP	direct assay
platelet-derived growth factor receptor-beta signaling pathway	BP	mutant phenotype
positive regulation of ERK1 and ERK2 cascade	BP	mutant phenotype
positive regulation of calcium-mediated signaling	BP	mutant phenotype
positive regulation of cell migration	BP	direct assay
positive regulation of cell population proliferation	BP	mutant phenotype
positive regulation of cell proliferation by VEGF-activated platelet derived growth factor receptor signaling pathway	BP	direct assay
positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transduction	BP	direct assay
positive regulation of smooth muscle cell migration	BP	mutant phenotype
positive regulation of smooth muscle cell proliferation	BP	mutant phenotype
protein autophosphorylation	BP	direct assay
signal transduction	BP	direct assay
focal adhesion	CC	high-throughput assay
membrane	CC	direct assay
plasma membrane	CC	direct assay
GTPase activator activity	MF	mutant phenotype
enzyme binding	MF	physical interaction
phospholipase C activator activity	MF	mutant phenotype
platelet-derived growth factor beta-receptor activity	MF	direct assay
platelet-derived growth factor binding	MF	direct assay
platelet-derived growth factor receptor binding	MF	physical interaction
protein kinase activity	MF	direct assay
protein kinase binding	MF	physical interaction
protein tyrosine kinase activity	MF	direct assay
signaling receptor binding	MF	physical interaction
vascular endothelial growth factor binding	MF	physical interaction

Protein interactions and networks

STRING

showing 15 of 4,032 interactions by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
PDGFRB	PDGFB	P01127	919
PDGFRB	PDGFA	P04085	850
PDGFRB	PDGFC	Q9NRA1	838
PDGFRB	PDGFD	Q9GZP0	829
PDGFRB	PIK3CA	P42336	789
PDGFRB	PIK3CG	P48736	784
PDGFRB	ETV6	P41212	770
PDGFRB	PECAM1	P16284	768
PDGFRB	FGF2	P09038	758
PDGFRB	FIP1L1	Q6UN15	758
PDGFRB	EGF	P01133	739
PDGFRB	CD34	P28906	688
PDGFRB	TGFB1	P01137	682
PDGFRB	PIK3CD	O00329	676
PDGFRB	PIK3CB	P42338	676

IntAct

Human interaction partners of PDGFRB in IntAct, one row per partner (best MIscore; records = supporting IntAct interaction records).

showing 30 of 146 partners by confidence:

Partner	Interaction type	MIscore	Records
PIK3R1	association	0.950	25
PDGFB	physical association	0.900	16
PTPN11	proximity	0.900	8
PLCG1	direct interaction	0.850	9
PDGFRA	association	0.770	2
NHERF1	proximity	0.730	8
KLHL12	physical association	0.720	6
PTPRJ	dephosphorylation reaction	0.720	4
PTPN1	physical association	0.710	3
PTPN12	physical association	0.700	3
PTEN	proximity	0.670	2
FYN	association	0.640	3
RASA1	association	0.640	3
NHERF2	direct interaction	0.620	2
PIK3R2	association	0.610	2
GOPC	direct interaction	0.570	1
GORASP2	direct interaction	0.570	1
APP	physical association	0.560	3
CEP76	physical association	0.560	3
KPRP	physical association	0.560	3
KRT31	physical association	0.560	3
KRT34	physical association	0.560	3
KRTAP10-9	physical association	0.560	3
KRTAP12-3	physical association	0.560	3
LRIG2	colocalization	0.560	3
TRIP6	physical association	0.560	3
YES1	association	0.530	2
LRP6	physical association	0.520	3
PIK3R3	proximity	0.480	1
GRB7	association	0.460	4

BioGRID (294 interactions; top human partners by supporting records): PIK3R1 (Affinity Capture-MS; 8 records), PLCG1 (Affinity Capture-Western; 8 records), SLC9A3R1 (Reconstituted Complex; 8 records), PDGFRA (Affinity Capture-MS; 5 records), PTEN (Co-localization; 5 records), PTPN11 (Reconstituted Complex; 5 records), SRC (Affinity Capture-Western; 4 records), CAV1 (Affinity Capture-Western; 3 records), EGFR (Affinity Capture-Western; 3 records), FOXK1 (Affinity Capture-MS; 3 records), GRB2 (Reconstituted Complex; 3 records), NCK2 (Reconstituted Complex; 3 records), PDGFB (Affinity Capture-Western; 3 records), SLC9A3R2 (Reconstituted Complex; 3 records), TNK2 (Affinity Capture-Western; 3 records)

SIGNOR signaling

showing 39 of 95 signaling interactions:

A	Effect	B	Mechanism
PDGFB	up-regulates	PDGFRB	binding
PDGFRB	up-regulates	RASA1	binding
sunitinib	down-regulates	PDGFRB	“chemical inhibition”
PDGFRB	up-regulates	PTK2	phosphorylation
PDGFRB	up-regulates	PDGFRB	phosphorylation
axitinib	down-regulates	PDGFRB	“chemical inhibition”
PTPN1	down-regulates	PDGFRB	dephosphorylation
ABL1	down-regulates	PDGFRB	phosphorylation
PDGFRB	up-regulates	CRK	binding
Crenolanib	down-regulates	PDGFRB	“chemical inhibition”
linifanib	down-regulates	PDGFRB	“chemical inhibition”
MK-2461	down-regulates	PDGFRB	“chemical inhibition”
Telatinib	down-regulates	PDGFRB	“chemical inhibition”
orantinib	down-regulates	PDGFRB	“chemical inhibition”
PDGFRB	unknown	PDGFRB	phosphorylation
PDGFRB	“up-regulates activity”	SRC	phosphorylation
ACP1	“down-regulates activity”	PDGFRB	dephosphorylation
PTPRJ	“down-regulates activity”	PDGFRB	dephosphorylation
PDGFRB	“up-regulates activity”	PDGFRB	phosphorylation
pazopanib	“down-regulates activity”	PDGFRB	“chemical inhibition”
regorafenib	“down-regulates activity”	PDGFRB	“chemical inhibition”
ABL1	“down-regulates activity”	PDGFRB	phosphorylation
CBL	“down-regulates quantity by destabilization”	PDGFRB	polyubiquitination
PDGFRB	“up-regulates activity”	TNK2	phosphorylation
PRKG2	“down-regulates activity”	PDGFRB	phosphorylation
PDGFRB	“up-regulates activity”	ABL1	phosphorylation
GRK2	“down-regulates activity”	PDGFRB	phosphorylation
PDGFRB	“up-regulates activity”	GRK2	phosphorylation
PDGFRB	“up-regulates activity”	ABL2	phosphorylation
PDGFRB	“up-regulates activity”	GRK5	phosphorylation
PDGFRB	up-regulates	PLCG1	phosphorylation
PDGFRB	up-regulates	GRB2	binding
PDGFRB	up-regulates	SHC1	phosphorylation
PDGFRB	up-regulates	NCK1	binding
PDGFRB	up-regulates	NCK2	binding
PTPN2	“down-regulates activity”	PDGFRB	dephosphorylation
PDGFRB	“up-regulates activity”	PTPN11	phosphorylation
PTPN1	“down-regulates activity”	PDGFRB	dephosphorylation
PTPN11	“down-regulates activity”	PDGFRB	dephosphorylation

Protein complexes (CORUM) (18)

Experimentally-characterized complexes this protein is a subunit of (★ = the complex contains a known drug target).

18 complexes by size:

Complex	Subunits	Members
★ GRB2-PDGFRB-PTPN11 complex	3	GRB2, PDGFRB, PTPN11
★ PDGFRB-SNX1 complex	2	PDGFRB, SNX1
★ PDGFRA-PDGFRB complex	2	PDGFRA, PDGFRB
★ GRB2-PDGFRB complex	2	GRB2, PDGFRB
★ PDGFRB-YES1 complex	2	PDGFRB, YES1
★ FYN-PDGFRB complex	2	FYN, PDGFRB
★ PDGFRB-STAT1 complex	2	PDGFRB, STAT1
★ PDGFRB-STAT3 complex	2	PDGFRB, STAT3
★ PDGFRB-STAT5A complex	2	PDGFRB, STAT5A
★ JAK1-PDGFRB complex	2	JAK1, PDGFRB
★ JAK2-PDGFRB complex	2	JAK2, PDGFRB
★ PDGFRB-TYK2 complex	2	PDGFRB, TYK2
★ PDGFRB-SIGMAR1 complex	2	PDGFRB, SIGMAR1
★ PDGFB-PDGFRB complex	2	PDGFB, PDGFRB
★ PDGFRB-SNX1A complex	2	PDGFRB, SNX1
★ PDGFRB-SNX2 complex	2	PDGFRB, SNX2
★ PDGFRB-SNX4 complex	2	PDGFRB, SNX4
★ PDGFRB homodimer	1	PDGFRB

Ligand–receptor pairs (CellPhoneDB) (3)

Curated ligand–receptor partners (cell-cell communication), distinct from the protein–protein interactions above.

3 ligand–receptor pairs:

Partner	This gene’s role	Signaling class
PDGFRA;PDGFRB		Signaling by Platelet-derived growth factor
PDGFB	receptor	Signaling by Platelet-derived growth factor
PDGFD	receptor	Signaling by Platelet-derived growth factor

Enriched among interaction partners

Reactome pathways and GO biological processes over-represented among this gene’s 146 IntAct physical interaction partners (hypergeometric vs the genome-wide background, BH-FDR, gene-set size 15–500, ranked by fold). A functional readout of the neighbourhood — distinct from this gene’s own memberships above, and biased toward well-studied / hub proteins, so read it as themes rather than proof.

Reactome pathways:

Pathway	Partners	Fold	FDR
Downstream signal transduction	17	58.8×	1e-24
Signaling by phosphorylated juxtamembrane, extracellular and kinase domain KIT mutants	10	47.2×	7e-13
Regulation of signaling by CBL	9	40.6×	7e-11
Regulation of KIT signaling	7	38.2×	3e-08
Signaling by SCF-KIT	16	36.1×	5e-19
Spry regulation of FGF signaling	5	32.4×	1e-05
Constitutive Signaling by EGFRvIII	5	32.4×	1e-05
Signaling by ALK	6	31.1×	9e-07

GO biological processes:

GO term	Partners	Fold	FDR
peptidyl-tyrosine dephosphorylation	6	38.3×	2e-06
establishment or maintenance of epithelial cell apical/basal polarity	9	37.6×	2e-09
receptor clustering	7	31.4×	5e-07
cellular response to platelet-derived growth factor stimulus	6	28.0×	7e-06
protein localization to synapse	5	27.6×	5e-05
negative regulation of epidermal growth factor receptor signaling pathway	5	27.6×	5e-05
ephrin receptor signaling pathway	9	22.3×	8e-08
regulation of postsynaptic membrane neurotransmitter receptor levels	6	21.4×	2e-05

Disease & clinical

Cancer significance

From intOGen — cancer-driver classification: activating (oncogene-like) across 3 cancer types — ANGS, NETNOS, UCS.

intOGen’s role is a computational inference from cohort mutation patterns and may diverge from the gene’s curated/literature role; read it alongside the evidence above.

Genetic variants

Variant evidence for PDGFRB: 875 ClinVar records (25 pathogenic / likely pathogenic); 2 CIViC cancer variants; 8 GWAS associations. Per-variant detail is on Sugi Variant.

ClinVar

875 variants total. Per-class counts are floors (≥ shown; pagination cap):

Classification	Count (floor)
Pathogenic	19
Likely pathogenic	6
Uncertain significance	333
Likely benign	293
Benign	103

Top pathogenic / likely-pathogenic (15)

Showing the 15 best-reviewed of 25 pathogenic / likely-pathogenic ClinVar records, ranked by ClinVar review status (expert panel → multiple submitters → single submitter), then by number of submitting labs.

Variant ID	HGVS	Classification	Review	Submitters
55848	NM_002609.4(PDGFRB):c.1681C>T (p.Arg561Cys)	Pathogenic	criteria provided, multiple submitters, no conflicts	10
375682	NM_002609.4(PDGFRB):c.1696T>C (p.Trp566Arg)	Pathogenic	criteria provided, multiple submitters, no conflicts	8
217122	NM_002609.4(PDGFRB):c.1751C>G (p.Pro584Arg)	Pathogenic	criteria provided, multiple submitters, no conflicts	4
495300	NM_002609.4(PDGFRB):c.1994T>C (p.Val665Ala)	Pathogenic	criteria provided, single submitter	2
375556	NM_002609.4(PDGFRB):c.1998C>G (p.Asn666Lys)	Pathogenic	criteria provided, single submitter	1
375681	NM_002609.4(PDGFRB):c.2549A>T (p.Asp850Val)	Pathogenic	criteria provided, single submitter	1
973194	NM_002609.4(PDGFRB):c.1519_1520insTACTGTCGGTGC (p.Val506_Arg507insLeuLeuSerVal)	Pathogenic	criteria provided, single submitter	1
973195	NM_002609.4(PDGFRB):c.1716_1717insGAGCTGATCCGATGGAAGGTGATTGAGTCTGTG (p.Val572_Ser573insGluLeuIleArgTrpLysValIleGluSerVal)	Pathogenic	criteria provided, single submitter	1
973196	NM_002609.4(PDGFRB):c.1682_1684del (p.Arg561_Tyr562delinsHis)	Pathogenic	criteria provided, single submitter	1
973197	NM_002609.4(PDGFRB):c.1684T>G (p.Tyr562Asp)	Pathogenic	criteria provided, single submitter	1
973198	NM_002609.4(PDGFRB):c.1613T>A (p.Ile538Asn)	Pathogenic	criteria provided, single submitter	1
2096300	NM_002609.4(PDGFRB):c.2483C>A (p.Ala828Glu)	Pathogenic	criteria provided, single submitter	1
3237207	NM_002609.4(PDGFRB):c.2548G>T (p.Asp850Tyr)	Pathogenic	criteria provided, single submitter	1
3392579	NM_002609.4(PDGFRB):c.2476G>T (p.Asp826Tyr)	Pathogenic	criteria provided, single submitter	1
375237	NM_002609.4(PDGFRB):c.1699A>G (p.Lys567Glu)	Likely pathogenic	criteria provided, single submitter	2

Per-variant reference — Sugi Variant

Explore PDGFRB’s pathogenic and likely-pathogenic variants individually — each with its ClinVar classification and conditions, applied ACMG criteria (ClinGen expert panel, where curated), the calibrated in-silico predictors (AlphaMissense, REVEL, SaProt, conservation), gnomAD frequency, and the predictor-disagreement QC signal — on Sugi Variant.

SpliceAI

Top 10 splice-impact sites by Δscore (adjacent positions with the same effect merged into one range; 27 predictions of 2,348):

Position(s)	Effect	Δscore	Sites
5:150115947	acceptor_loss	1.0000
5:150117616–150117617	donor_loss	1.0000	4
5:150117858–150117859	acceptor_gain	1.0000	2
5:150117864	acceptor_gain	1.0000
5:150117873–150117874	acceptor_gain	1.0000	2
5:150118745–150118746	donor_loss	1.0000	4
5:150118853–150118854	acceptor_loss	1.0000	4
5:150119465–150119466	donor_loss	1.0000	3
5:150119567–150119568	acceptor_loss	1.0000	5
5:150119579	acceptor_gain	1.0000

AlphaMissense

2,383 missense substitutions predicted likely pathogenic (of 7,221 scored), across 566 residues. Top 20 hotspot residues, ranked by the number of likely-pathogenic substitutions (of those reachable by a single-nucleotide change), then by mean score:

Residue	Likely-pathogenic substitutions	Mean am_pathogenicity	Max am_pathogenicity
M870	9	0.994	1.000
M923	9	0.972	0.999
M814	9	0.967	0.999
M635	9	0.959	0.993
M937	9	0.955	0.998
M743	9	0.904	0.987
M649	9	0.831	0.984
D826	8	1.000	1.000
N831	8	1.000	1.000
D844	8	1.000	1.000
F611	8	0.999	1.000
D885	8	0.999	1.000
H824	8	0.998	1.000
F845	8	0.997	1.000
D854	8	0.994	0.999
D850	8	0.992	0.999
F876	8	0.991	1.000
F913	8	0.991	1.000
D688	8	0.990	0.999
F951	8	0.988	0.999

HPA cancer prognostics

RNA cancer specificity: Low cancer specificity

Human Protein Atlas survival analysis — favorable = higher expression predicts better survival.

1 prognostic cancer types:

Cancer	Prognostic	p-value
Kidney Renal Papillary Cell Carcinoma (TCGA)	unfavorable	5.35e-05

Disease associations

OMIM: gene MIM:173410 | disease phenotypes: MIM:616592, MIM:131440, MIM:601812, MIM:615007, MIM:228550, MIM:621091, MIM:220200

GenCC curated gene-disease

8 curated gene-disease records:

Disease	Classification	Inheritance	Records
skeletal overgrowth-craniofacial dysmorphism-hyperelastic skin-white matter lesions syndrome	Definitive	Autosomal dominant	4
myofibromatosis, infantile, 1	Definitive	Autosomal dominant	2
acroosteolysis-keloid-like lesions-premature aging syndrome	Definitive	Autosomal dominant	4
basal ganglia calcification, idiopathic, 4	Strong	Autosomal dominant	4
bilateral striopallidodentate calcinosis	Supportive	Autosomal dominant
infantile myofibromatosis	Supportive	Autosomal dominant
ocular pterygium-digital keloid dysplasia syndrome	Limited	Autosomal dominant
hereditary progressive mucinous histiocytosis	Limited	Autosomal dominant

Genomics England panels (PanelApp)

Clinical diagnostic gene panels including this gene (15 panels, 15 green/diagnostic-grade). Confidence: green = diagnostic, amber = moderate.

15 panels:

Panel	Rating
Adult-onset neurological disorders	green
Beckwith-Wiedemann syndrome (BWS) and other congenital overgrowth disorders	green
Childhood solid tumours	green
DDG2P	green
Dystonia, chorea or related movement disorder, adult onset	green
Fetal anomalies	green
Hypotonic infant	green
Intellectual disability	green
Intracerebral calcification disorders	green
Leukodystrophy, childhood onset	green
Multiple monogenic benign skin tumours	green
Neurodegenerative disorders, adult onset	green
Paediatric disorders	green
Structural basal ganglia disorders	green
White matter disorders and cerebral calcification - childhood onset	green

Mondo (11): skeletal overgrowth-craniofacial dysmorphism-hyperelastic skin-white matter lesions syndrome (MONDO:0014704), myeloproliferative disorder, chronic, with eosinophilia (MONDO:0007546), acroosteolysis-keloid-like lesions-premature aging syndrome (MONDO:0011150), basal ganglia calcification, idiopathic, 4 (MONDO:0014004), infantile myofibromatosis (MONDO:0016824), myofibromatosis, infantile, 1 (MONDO:0009227), ocular pterygium-digital keloid dysplasia syndrome (MONDO:0976136), hydrocephalus (MONDO:0001150), Dandy-Walker syndrome (MONDO:0009072), bilateral striopallidodentate calcinosis (MONDO:0008947), hereditary progressive mucinous histiocytosis (MONDO:0007725)

Orphanet (5): Kosaki overgrowth syndrome (Orphanet:477831), Acroosteolysis-keloid-like lesions-premature aging syndrome (Orphanet:363665), Bilateral striopallidodentate calcinosis (Orphanet:1980), Infantile myofibromatosis (Orphanet:2591), Isolated Dandy-Walker malformation (Orphanet:217)

HPO phenotypes

showing 60 of 179 phenotypes (HPO-id order):

HPO	Term
HP:0000002	Abnormality of body height
HP:0000006	Autosomal dominant inheritance
HP:0000012	Urinary urgency
HP:0000020	Urinary incontinence
HP:0000077	Abnormality of the kidney
HP:0000098	Tall stature
HP:0000169	Gingival fibromatosis
HP:0000219	Thin upper lip vermilion
HP:0000233	Thin vermilion border
HP:0000256	Macrocephaly
HP:0000270	Delayed cranial suture closure
HP:0000271	Abnormality of the face
HP:0000278	Retrognathia
HP:0000298	Mask-like facies
HP:0000307	Pointed chin
HP:0000316	Hypertelorism
HP:0000326	Abnormal maxilla morphology
HP:0000327	Hypoplasia of the maxilla
HP:0000336	Prominent supraorbital ridges
HP:0000347	Micrognathia
HP:0000407	Sensorineural hearing impairment
HP:0000422	Abnormal nasal bridge morphology
HP:0000426	Prominent nasal bridge
HP:0000431	Wide nasal bridge
HP:0000444	Convex nasal ridge
HP:0000460	Narrow nose
HP:0000478	Abnormality of the eye
HP:0000494	Downslanted palpebral fissures
HP:0000508	Ptosis
HP:0000520	Proptosis
HP:0000540	Hypermetropia
HP:0000568	Microphthalmia
HP:0000586	Shallow orbits
HP:0000601	Hypotelorism
HP:0000666	Horizontal nystagmus
HP:0000684	Delayed eruption of teeth
HP:0000709	Psychosis
HP:0000716	Depression
HP:0000726	Dementia
HP:0000739	Anxiety
HP:0000751	Personality changes
HP:0000765	Abnormal thorax morphology
HP:0000802	Impotence
HP:0000822	Hypertension
HP:0000883	Thin ribs
HP:0000891	Cervical ribs
HP:0000929	Abnormal skull morphology
HP:0000934	Chondrocalcinosis
HP:0000939	Osteoporosis
HP:0000944	Abnormal metaphysis morphology
HP:0000962	Hyperkeratosis
HP:0000963	Thin skin
HP:0000972	Palmoplantar hyperkeratosis
HP:0000974	Hyperextensible skin
HP:0001015	Prominent superficial veins
HP:0001030	Fragile skin
HP:0001072	Thickened skin
HP:0001114	Xanthelasma
HP:0001156	Brachydactyly
HP:0001249	Intellectual disability

GWAS associations

8 associations:

Study	Trait	p-value
GCST006585_1655	Blood protein levels	0.000000e+00
GCST90002393_664	Monocyte count	1e-129
GCST90002394_347	Monocyte percentage of white cells	1e-128
GCST004625_117	Monocyte count	1e-54
GCST004609_7	Monocyte percentage of white cells	2e-46
GCST004608_18	Granulocyte percentage of myeloid white cells	7e-36
GCST90000584_8	Inflammatory biomarkers (multivariate analysis)	1e-15
GCST009244_7	Cytokine network levels (multivariate analysis)	4e-9

EFO canonical traits (from GWAS)

11 canonical traits:

EFO ID	Trait name
EFO:0007997	granulocyte percentage of myeloid white cells
EFO:0007989	monocyte percentage of leukocytes
EFO:0005091	monocyte count
EFO:0004750	interleukin 10 measurement
EFO:0004753	interleukin 12 measurement
EFO:0004810	interleukin-6 measurement
EFO:0008165	interferon gamma measurement
EFO:0008174	interleukin 17 measurement
EFO:0008184	interleukin 4 measurement
EFO:0008293	stromal cell-derived factor 1 alpha measurement
EFO:0004872	inflammatory biomarker measurement

MeSH disease descriptors

8 disease descriptors:

Descriptor	Name	Tree numbers
D003616	Dandy-Walker Syndrome	C10.228.140.252.300; C10.228.140.602.500; C10.500.205; C16.131.666.205
D006849	Hydrocephalus	C10.228.140.602
D018224	Myofibromatosis	C04.557.450.565.590.550
C536275	Fahr’s disease *(supp.)*
C562978	Fibromatosis, Congenital Generalized *(supp.)*
C564186	Histiocytosis, Progressive Mucinous *(supp.)*
C565054	Myeloproliferative Disorder, Chronic, with Eosinophilia *(supp.)*
C536653	Penttinen-Aula syndrome *(supp.)*

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (5): CHEMBL1913 (SINGLE PROTEIN), CHEMBL2095189 (PROTEIN COMPLEX), CHEMBL2111440 (SELECTIVITY GROUP), CHEMBL4523729 (PROTEIN-PROTEIN INTERACTION), CHEMBL4879531 (PROTEIN-PROTEIN INTERACTION)

Drugs by curated mechanism of action (ChEMBL)

Drugs whose curated ChEMBL mechanism of action targets the PDGFRB protein itself — single-protein targets only (drugs acting on a protein family or complex that merely includes it are excluded). Includes antibodies and oligonucleotides that bioactivity screening does not capture.

17 curated-mechanism drugs:

Drug	Modality	Max phase
DASATINIB ANHYDROUS	Small molecule	4
IMATINIB MESYLATE	Small molecule	4
SORAFENIB TOSYLATE	Small molecule	4
SUNITINIB	Small molecule	4
TIVOZANIB HYDROCHLORIDE	Small molecule	4
CATEQUENTINIB	Small molecule	3
CM-082	Unknown	3
CDP-860	Unknown	2
JI-101	Small molecule	2
RINUCUMAB	Antibody	2
TANDUTINIB	Small molecule	2
TELATINIB	Small molecule	2
TG100-801	Small molecule	2
CEP-2563 DIHYDROCHLORIDE	Small molecule	1
PD-0166285 HYDROCHLORIDE	Small molecule	1
PUQUITINIB MESYLATE DIHYDRATE	Small molecule	1
RG-1530	Small molecule	1

Drugs acting on a complex or family that includes this protein

Curated ChEMBL mechanism-of-action drugs whose target is a protein complex or family of ≤10 members that includes PDGFRB — the drug acts on the assembly or class, not necessarily on this subunit alone.

24 drugs via a complex or family:

Drug	Target (ChEMBL)	Members	Max phase
BECAPLERMIN	Platelet-derived growth factor receptor	2	4
MIDOSTAURIN	Platelet-derived growth factor receptor	2	4
NINTEDANIB ESYLATE	Platelet-derived growth factor receptor	2	4
PAZOPANIB HYDROCHLORIDE	Platelet-derived growth factor receptor	2	4
QUIZARTINIB	Platelet-derived growth factor receptor	2	4
REGORAFENIB	Platelet-derived growth factor receptor	2	4
CEDIRANIB	Platelet-derived growth factor receptor	2	3
CRENOLANIB	Platelet-derived growth factor receptor	2	3
DOVITINIB	Platelet-derived growth factor receptor	2	3
FAMITINIB	Platelet-derived growth factor receptor	2	3
LINIFANIB	Platelet-derived growth factor receptor	2	3
MASITINIB	Platelet-derived growth factor receptor	2	3
MOTESANIB	Platelet-derived growth factor receptor	2	3
ORANTINIB	Platelet-derived growth factor receptor	2	3
SERALUTINIB	Platelet-derived growth factor receptor	2	3
VATALANIB	Platelet-derived growth factor receptor	2	3
ENMD-981693	Platelet-derived growth factor receptor	2	2
FORETINIB	Platelet-derived growth factor receptor	2	2
ILORASERTIB	Platelet-derived growth factor receptor	2	2
SU-014813	Platelet-derived growth factor receptor	2	2
X-82	Platelet-derived growth factor receptor	2	2
XL-820	Platelet-derived growth factor receptor	2	2
XL-999	Platelet-derived growth factor receptor	2	2
TAK-593	Platelet-derived growth factor receptor	2	1

Molecules with ChEMBL bioactivity

Phase ≥1, by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 591,758 (via chembl_molecule»patent_compound — counts attach to the compound, not the gene–compound relationship, so off-target/promiscuous molecules can dominate).

showing 60 of 102 molecules by phase:

Molecule	Name	Phase	Patents
CHEMBL5416410	DASATINIB	4	674
CHEMBL941	IMATINIB	4	113,105
CHEMBL1336	SORAFENIB	4	87,476
CHEMBL535	SUNITINIB	4	80,232
CHEMBL1567	SUNITINIB MALATE	4	166
CHEMBL1289494	TIVOZANIB	4	4,697
CHEMBL1289926	AXITINIB	4	16,510
CHEMBL288441	BOSUTINIB	4	12,869
CHEMBL553	ERLOTINIB	4	109,860
CHEMBL1287853	FEDRATINIB	4	3,770
CHEMBL3301622	GILTERITINIB	4	2,542
CHEMBL554	LAPATINIB	4	70,425
CHEMBL1289601	LENVATINIB	4	9,224
CHEMBL608533	MIDOSTAURIN	4	7,641
CHEMBL255863	NILOTINIB	4	39,362
CHEMBL502835	NINTEDANIB	4	8,978
CHEMBL3039504	NINTEDANIB ESYLATE	4	691
CHEMBL2035187	PACRITINIB	4	3,544
CHEMBL477772	PAZOPANIB	4	16,241
CHEMBL3813873	PEXIDARTINIB	4	3,751
CHEMBL1171837	PONATINIB	4
CHEMBL576982	QUIZARTINIB	4
CHEMBL1946170	REGORAFENIB	4
CHEMBL3348923	TOVORAFENIB	4
CHEMBL24828	VANDETANIB	4
CHEMBL4303201	CATEQUENTINIB	3
CHEMBL415049	BARASERTIB	3
CHEMBL377300	BRIVANIB	3
CHEMBL270995	BRIVANIB ALANINATE	3
CHEMBL31965	CANERTINIB	3
CHEMBL491473	CEDIRANIB	3
CHEMBL2105728	CRENOLANIB	3
CHEMBL522892	DOVITINIB	3
CHEMBL300138	ENZASTAURIN	3
CHEMBL1278146	FAMITINIB	3
CHEMBL3545413	FLUMATINIB	3
CHEMBL603469	LESTAURTINIB	3
CHEMBL223360	LINIFANIB	3
CHEMBL1908391	MASITINIB	3
CHEMBL572881	MOTESANIB	3
CHEMBL4583691	NAPORAFENIB	3
CHEMBL274654	ORANTINIB	3
CHEMBL91829	RUBOXISTAURIN	3
CHEMBL217092	SARACATINIB	3
CHEMBL276711	SEMAXANIB	3
CHEMBL101253	VATALANIB	3
CHEMBL5095202	VIMSELTINIB	3
CHEMBL124660	TANDUTINIB	2
CHEMBL2079588	TELATINIB	2
CHEMBL403989	TG100-801	2
CHEMBL587723	AEE-788	2
CHEMBL206834	BAFETINIB	2
CHEMBL4080062	BFH-772	2
CHEMBL1967878	CENISERTIB	2
CHEMBL2029988	CEP-32496	2
CHEMBL105442	CI-1040	2
CHEMBL215152	DEFOSBARASERTIB	2
CHEMBL103667	DORAMAPIMOD	2
CHEMBL6246	ELLAGIC ACID	2
CHEMBL1230609	FORETINIB	2

Clinical evidence (CIViC)

Drug × variant × indication, from 2 curated evidence items. CIViC evidence level: A (validated) → B (clinical) → C (case study) → D (preclinical) → E (inferential).

2 predictive associations by evidence level:

Variant	Therapy	Indication	Effect	Level	CIViC
PDGFRB Overexpression	Sunitinib	Dermatofibrosarcoma Protuberans	Sensitivity/Response	CIViC C	EID7992
AGGF1::PDGFRB Fusion AND PDGFRB C843G	CHZ868	B-lymphoblastic Leukemia/lymphoma, BCR-ABL1–like	Sensitivity/Response	CIViC D	EID6999

CIViC curated variants (2)

Named clinical variants curated in CIViC for this gene (the catalogue beneath the predictive evidence above):

Overexpression, C843G (missense variant).

PharmGKB: 1 entry (CPIC guideline: no)

PharmGKB variant annotations

Per-publication pharmacogenomic findings for this gene (significant associations).

2 published findings:

Variant	Drug(s)	Category	Finding	PMID
rs2302273	bevacizumab, fluorouracil, irinotecan, leucovorin	Efficacy	Genotypes AA + AG is associated with increased progression-free survival when treated with bevacizumab, fluorouracil, irinotecan and leucovorin in people with Colorectal Neoplasms as compared to genotype GG.	PMID:25069475
rs55712339	imatinib	Toxicity	Genotypes C/del + CC is associated with increased likelihood of Myelosuppression when treated with imatinib in people with Gastrointestinal Stromal Tumors as compared to genotype del/del.	PMID:41193444

GtoPdb / IUPHAR curated pharmacology

(IUPHAR/BPS Guide to Pharmacology — expert-curated)

Target class: catalytic receptor — Type III RTKs: PDGFR, CSFR, Kit, FLT3 receptor family

Most potent curated ligand interactions (48 total), top 25:

Ligand	Action	Affinity	Parameter
CP-673451	Inhibition	9.0	pIC50
AC710	Inhibition	9.0	pKd
compound 8h [PMID: 22765894]	Inhibition	8.89	pIC50
compound 8i [PMID: 22765894]	Inhibition	8.82	pIC50
velzatinib	Inhibition	8.59	pIC50
SU11652	Inhibition	8.52	pIC50
crenolanib	Inhibition	8.49	pKd
SU-14813	Inhibition	8.4	pIC50
famitinib	Inhibition	8.4	pIC50
PDGF receptor tyrosine kinase inhibitor IV	Inhibition	8.38	pIC50
cediranib	Inhibition	8.3	pIC50
dovitinib	Inhibition	8.3	pIC50
quizartinib	Inhibition	8.11	pKd
sunitinib	Inhibition	8.1	pKi
lucitanib	Inhibition	8.1	pIC50
henatinib	Inhibition	7.96	pIC50
PDGF RTK inhibitor	Inhibition	7.92	pIC50
ilorasertib	Inhibition	7.89	pIC50
naporafenib	Inhibition	7.85	pKd
tafetinib	Inhibition	7.85	pIC50
MK-2461	Inhibition	7.66	pIC50
KBP-7018	Inhibition	7.6	pIC50
compound 5e [PMID: 28580438]	Inhibition	7.55	pKd
BPR1R024	Inhibition	7.5	pIC50
orantinib	Inhibition	7.3	pIC50

Binding affinities (BindingDB)

3033 measured of 3947 human assays (3987 total across all organisms); most potent 50 below. Values come from heterogeneous assays and are not directly comparable.

Ligand	Measure	Value	Patent
1-Phenylbenzimidazole deriv. 76	EC50	0.00399 nM
3-[2-(Imidazo[1,2-b]pyridazin-3-yl)ethynyl]-4-methyl-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzamide	EC50	0.05 nM
2-Chloro-N-[4-(4,5-dichloro-2-fluoro-phenylamino)-quinazolin-6-yl]-acetamide	IC50	0.07 nM
N-(5-(3-(2,2-dimethylpyrrolidin- 1-yl)propanamido)-2- methylpyridin-3-yl)-2-(1- methyl-1H-indazol-4- yl)pyrazolo[5,1-b]thiazole-7- carboxamide	IC50	0.1 nM	US-20240109917: PYRAZOLOTHIAZOLE CARBOXAMIDES AND THEIR USES AS PDGFR INHIBITORS
N-(5-(2-(3,3-dimethylazetidin-1- yl)acetamido)-2-methylpyridin- 3-yl)-2-(thiophen-3- yl)pyrazolo[5,1-b]thiazole-7- carboxamide	IC50	0.1 nM	US-20240109917: PYRAZOLOTHIAZOLE CARBOXAMIDES AND THEIR USES AS PDGFR INHIBITORS
N-(5-(2-(3,3-dimethylazetidin-1- yl)acetamido)-2-methylpyridin- 3-yl)-2-(furan-3-yl)pyrazolo[5,1- b]thiazole-7-carboxamide	IC50	0.1 nM	US-20240109917: PYRAZOLOTHIAZOLE CARBOXAMIDES AND THEIR USES AS PDGFR INHIBITORS
N-(5-(2-(3,3-dimethylazetidin-1- yl)acetamido)-2-methylpyridin- 3-yl)-2-(1H-pyrrol-3- yl)pyrazolo[5,1-b]thiazole-7- carboxamide	IC50	0.1 nM	US-20240109917: PYRAZOLOTHIAZOLE CARBOXAMIDES AND THEIR USES AS PDGFR INHIBITORS
N-(5-(2-(3,3-dimethylazetidin-1- yl)acetamido)-2-methylpyridin- 3-yl)-2-(1-methyl-1H-indazol-4- yl)pyrazolo[5,1-b]thiazole-7- carboxamide	IC50	0.1 nM	US-20240109917: PYRAZOLOTHIAZOLE CARBOXAMIDES AND THEIR USES AS PDGFR INHIBITORS
N-(5-(2-(3,3-dimethylazetidin-1- yl)acetamido)-2-methylpyridin- 3-yl)-2-(1H-indol-3- yl)pyrazolo[5,1-b]thiazole-7- carboxamide	IC50	0.1 nM	US-20240109917: PYRAZOLOTHIAZOLE CARBOXAMIDES AND THEIR USES AS PDGFR INHIBITORS
N-(5-(2-(5-azaspiro[2.4]heptan- 5-yl)acetamido)-2- methylpyridin-3-yl)-2-(2- methoxypyridin-3- yl)pyrazolo[5,1-b]thiazole-7- carboxamide	IC50	0.1 nM	US-20240109917: PYRAZOLOTHIAZOLE CARBOXAMIDES AND THEIR USES AS PDGFR INHIBITORS
N-(5-(2-(3,3-Dimethylazetidin- 1-yl)acetamido)-2- methylpyridin-3-yl)-2-(2- ethoxypyridin-3-yl)pyrazolo[5,1- b]thiazole-7-carboxamide	IC50	0.1 nM	US-20240109917: PYRAZOLOTHIAZOLE CARBOXAMIDES AND THEIR USES AS PDGFR INHIBITORS
N-(5-(2- (cyclobutylamino)acetamido)- 2-methylpyridin-3-yl)-2-(5,6- dihydro-4H-pyrrolo[1,2- b]pyrazol-3-yl)pyrazolo[5,1- b]thiazole-7-carboxamide	IC50	0.1 nM	US-20240109917: PYRAZOLOTHIAZOLE CARBOXAMIDES AND THEIR USES AS PDGFR INHIBITORS
(E)-4-Dimethylamino-but-2-enoic acid [4-(4,5-dichloro-2-fluoro-phenylamino)-quinazolin-6-yl]-amide	IC50	0.11 nM
3-(2,6-Difluoro-3,5-dimethoxyphenyl)-1-methyl-1,3,4,7-tetrahydro-2H-pyrrolo[3’,2’:5,6]pyrido[4,3-d]pyrimidin-2-one	IC50	0.12 nM
4-fluoro-3-[[1-methyl-6-[(1-methylpyrazol-4-yl)amino]pyrazolo[3,4-d]pyrimidin-3-yl]amino]-N-[2-[(2S)-2-methylpyrrolidin-1-yl]ethyl]benzamide	IC50	0.13 nM	US-20240360134: PYRAZOLOPYRIMIDINES AND THEIR USES AS PDGFR INHIBITORS
(3E)-2-amino-3-[hydroxy(phenyl)methylidene]-7,7-dimethyl-4-[4-(4-methylphenyl)sulfonylphenyl]-6,8-dihydro-4H-quinolin-5-one	IC50	0.14 nM	US-11505527: Tetrahydroquinoline derivatives and a process of preparation thereof
N-[2-(5-azaspiro[2.4]heptan-5-yl)ethyl]-4-fluoro-3-[[1-methyl-6-[(1-methylpyrazol-4-yl)amino]pyrazolo[3,4-d]pyrimidin-3-yl]amino]benzamide	IC50	0.15 nM	US-20240360134: PYRAZOLOPYRIMIDINES AND THEIR USES AS PDGFR INHIBITORS
CHEMBL6150730	IC50	0.18 nM
1-[6-methyl-5-[[1-methyl-6-[(1-methylpyrazol-4-yl)amino]pyrazolo[3,4-d]pyrimidin-3-yl]amino]-3-pyridinyl]-4-[(2R)-2-methylpiperidin-1-yl]butan-1-one	IC50	0.18 nM	US-20240360134: PYRAZOLOPYRIMIDINES AND THEIR USES AS PDGFR INHIBITORS
CHEMBL2023485	IC50	0.2 nM
N-(5-((2-(2- azabicyclo[2.2.2]octan-2- yl)ethyl)carb-amoyl)-2- methylpyridin-3-yl)-2-(1- methyl-1H-pyrazol-4- yl)pyrazolo[5,1-b]thiazole-7- carboxamide	IC50	0.2 nM	US-20240109917: PYRAZOLOTHIAZOLE CARBOXAMIDES AND THEIR USES AS PDGFR INHIBITORS
2-(1-cyclopropyl-1H-pyrazol-4- yl)-N-(5-((2-(2,2- dimethylpyrroli-din-1- yl)ethyl)carbamoyl)-2- methylpyridin-3- yl)pyrazolo[5,1-b]thiazole-7- carboxamide	IC50	0.2 nM	US-20240109917: PYRAZOLOTHIAZOLE CARBOXAMIDES AND THEIR USES AS PDGFR INHIBITORS
(S)-N-(5-(2-(3- ethylmorpholino)acetamido)-2- methylpyridin-3-yl)-2-(1- methyl-1H-pyrazol-4- yl)pyrazolo[5,1-b]thiazole-7- carboxamide	IC50	0.2 nM	US-20240109917: PYRAZOLOTHIAZOLE CARBOXAMIDES AND THEIR USES AS PDGFR INHIBITORS
N-(5-((2-(2- azabicyclo[2.2.2]octan-2- yl)ethyl)carbamoyl)-2- methylpyridin-3-yl)-2-(2-oxo- 2,3-dihydrobenzo[d]oxazol-5- yl)pyrazolo[5,1-b]thiazole-7- carboxamide	IC50	0.2 nM	US-20240109917: PYRAZOLOTHIAZOLE CARBOXAMIDES AND THEIR USES AS PDGFR INHIBITORS
N-(5-((2-(5-azaspiro[2.4]heptan- 5-yl)ethyl)carbamoyl)-2- methylpyridin-3-yl)-2-(pyridin- 2-yl)pyrazolo[5,1-b]thiazole-7- carboxamide	IC50	0.2 nM	US-20240109917: PYRAZOLOTHIAZOLE CARBOXAMIDES AND THEIR USES AS PDGFR INHIBITORS
N-(5-((2-(2- azabicyclo[2.2.2]octan-2- yl)ethyl)carbamoyl)-2- methylpyridin-3-yl)-2-(1,3- dimethyl-1H-pyrazol-4- yl)pyrazolo[5,1-b]thiazole-7- carboxamide	IC50	0.2 nM	US-20240109917: PYRAZOLOTHIAZOLE CARBOXAMIDES AND THEIR USES AS PDGFR INHIBITORS
N-(5-((2-(2- azabicyclo[2.2.2]octan-2- yl)ethyl)carbamoyl)-2- methylpyridin-3-yl)-2-(1- cyclopropyl-1H-pyrazol-4- yl)pyrazolo[5,1-b]thiazole-7- carboxamide	IC50	0.2 nM	US-20240109917: PYRAZOLOTHIAZOLE CARBOXAMIDES AND THEIR USES AS PDGFR INHIBITORS
2-(1,5-Dimethyl-1H-pyrazol-4- yl)-N-(2-methyl-5-((2- (pyrrolidin-1- yl)ethyl)carbamoyl)pyridin-3- yl)pyrazolo[5,1-b]thiazole-7- carboxamide	IC50	0.2 nM	US-20240109917: PYRAZOLOTHIAZOLE CARBOXAMIDES AND THEIR USES AS PDGFR INHIBITORS
N-(5-((2-(2,2- Dimethylpyrrolidin-1- yl)ethyl)carbamoyl)-2- methylpyridin-3-yl)-2-(2- methoxypyridin-3- yl)pyrazolo[5,1-b]thiazole-7- carboxamide	IC50	0.2 nM	US-20240109917: PYRAZOLOTHIAZOLE CARBOXAMIDES AND THEIR USES AS PDGFR INHIBITORS
2-(2-Methoxypyridin-3-yl)-N- (2-methyl-5-((2-(2- methylpyrrolidin-1- yl)ethyl)carbamoyl)pyridin-3- yl)pyrazolo[5,1-b]thiazole-7- carboxamide	IC50	0.2 nM	US-20240109917: PYRAZOLOTHIAZOLE CARBOXAMIDES AND THEIR USES AS PDGFR INHIBITORS
2-(2-Methoxypyridin-3-yl)-N- (2-methyl-5-((2-(pyrrolidin-1- yl)ethyl)carbamoyl)pyridin-3- yl)pyrazolo[5,1-b]thiazole-7- carboxamide	IC50	0.2 nM	US-20240109917: PYRAZOLOTHIAZOLE CARBOXAMIDES AND THEIR USES AS PDGFR INHIBITORS
N-(5-(2-(2,2-dimethylpyrrolidin- 1-yl)acetamido)-2- methylpyridin-3-yl)-2-(2- methoxypyridin-3- yl)pyrazolo[5,1-b]thiazole-7- carboxamide	IC50	0.2 nM	US-20240109917: PYRAZOLOTHIAZOLE CARBOXAMIDES AND THEIR USES AS PDGFR INHIBITORS
(R)-2-(2-methoxypyridin-3-yl)- N-(2-methyl-5-((2-(2- methylpyrrolidin-1- yl)ethyl)carbamoyl)pyridin-3- yl)pyrazolo[5,1-b]thiazole-7- carboxamide	IC50	0.2 nM	US-20240109917: PYRAZOLOTHIAZOLE CARBOXAMIDES AND THEIR USES AS PDGFR INHIBITORS
(S)-(1-methylpyrrolidin-2- yl)methyl (5-(2-(2- methoxypyridin-3- yl)pyrazolo[5,1-b]thiazole-7- carboxamido)-6-methylpyridin- 3-yl)carbamate	IC50	0.2 nM	US-20240109917: PYRAZOLOTHIAZOLE CARBOXAMIDES AND THEIR USES AS PDGFR INHIBITORS
2-(2,2-dimethylpyrrolidin-1- yl)ethyl (5-(2-(2- methoxypyridin-3- yl)pyrazolo[5,1-b]thiazole-7- carboxamido)-6-methylpyridin- 3-yl)carbamate	IC50	0.2 nM	US-20240109917: PYRAZOLOTHIAZOLE CARBOXAMIDES AND THEIR USES AS PDGFR INHIBITORS
2-(pyrrolidin-1-yl)propyl (5-(2- (2-methoxypyridin-3- yl)pyrazolo[5,1-b]thiazole-7- carboxamido)-6-methylpyridin- 3-yl)carbamate	IC50	0.2 nM	US-20240109917: PYRAZOLOTHIAZOLE CARBOXAMIDES AND THEIR USES AS PDGFR INHIBITORS
(S)-(1-methylpyrrolidin-2- yl)methyl (6-methyl-5-(2-(1- methyl-1H-indazol-4- yl)pyrazolo[5,1-b]thiazole-7- carboxamido)pyridin-3- yl)carbamate	IC50	0.2 nM	US-20240109917: PYRAZOLOTHIAZOLE CARBOXAMIDES AND THEIR USES AS PDGFR INHIBITORS
N-(5-(2-(3,3-dimethylazetidin-1- yl)acetamido)-2-methylpyridin- 3-yl)-2-(1H-pyrazol-4- yl)pyrazolo[5,1-b]thiazole-7- carboxamide	IC50	0.2 nM	US-20240109917: PYRAZOLOTHIAZOLE CARBOXAMIDES AND THEIR USES AS PDGFR INHIBITORS
N-(5-(2-(3,3-dimethylazetidin-1- yl)acetamido)-2-methylpyridin- 3-yl)-2-(4-(3-hydroxyoxetan-3- yl)phenyl)pyrazolo[5,1- b]thiazole-7-carboxamide	IC50	0.2 nM	US-20240109917: PYRAZOLOTHIAZOLE CARBOXAMIDES AND THEIR USES AS PDGFR INHIBITORS
2-(2-acetamidopyridin-4-yl)-N- (5-(2-(3,3-dimethylazetidin-1- yl)acetamido)-2-methylpyridin- 3-yl)pyrazolo[5,1-b]thiazole-7- carboxamide	IC50	0.2 nM	US-20240109917: PYRAZOLOTHIAZOLE CARBOXAMIDES AND THEIR USES AS PDGFR INHIBITORS
N-(5-(2-(3,3-dimethylazetidin-1- yl)acetamido)-2-methylpyridin- 3-yl)-2-(1-(methylsulfonyl)-1H- pyrrol-3-yl)pyrazolo[5,1- b]thiazole-7-carboxamide	IC50	0.2 nM	US-20240109917: PYRAZOLOTHIAZOLE CARBOXAMIDES AND THEIR USES AS PDGFR INHIBITORS
N-(5-(2-(3,3-dimethylazetidin-1- yl)acetamido)-2-methylpyridin- 3-yl)-2-(5- (hydroxymethyl)thiophen-2- yl)pyrazolo[5,1-b]thiazole-7- carboxamide	IC50	0.2 nM	US-20240109917: PYRAZOLOTHIAZOLE CARBOXAMIDES AND THEIR USES AS PDGFR INHIBITORS
N-(5-(2-(3,3-dimethylazetidin-1- yl)acetamido)-2-methylpyridin- 3-yl)-2-(2-morpholinopyridin-4- yl)pyrazolo[5,1-b]thiazole-7- carboxamide	IC50	0.2 nM	US-20240109917: PYRAZOLOTHIAZOLE CARBOXAMIDES AND THEIR USES AS PDGFR INHIBITORS
(S)-2-(2-methoxypyridin-3-yl)- N-(2-methyl-5-((2-(2- methylpyrrolidin-1- yl)ethyl)carbamoyl)pyridin-3- yl)pyrazolo[5,1-b]thiazole-7- carboxamide	IC50	0.2 nM	US-20240109917: PYRAZOLOTHIAZOLE CARBOXAMIDES AND THEIR USES AS PDGFR INHIBITORS
(R)-N-(5-(2-(1- isopropylpyrrolidin-2- yl)acetamido)-2-methylpyridin- 3-yl)-2-(2-methoxypyridin-3- yl)pyrazolo[5,1-b]thiazole-7- carboxamide	IC50	0.2 nM	US-20240109917: PYRAZOLOTHIAZOLE CARBOXAMIDES AND THEIR USES AS PDGFR INHIBITORS
(S)-N-(5-(2-(2- ethylmorpholino)acetamido)-2- methylpyridin-3-yl)-2-(2- methoxypyridin-3- yl)pyrazolo[5,1-b]thiazole-7- carboxamide	IC50	0.2 nM	US-20240109917: PYRAZOLOTHIAZOLE CARBOXAMIDES AND THEIR USES AS PDGFR INHIBITORS
2-(2-methoxypyridin-3-yl)-N-(2- methyl-5-(2-(pyrrolidin-1- yl)acetamido)pyridin-3- yl)pyrazolo[5,1-b]thiazole-7- carboxamide	IC50	0.2 nM	US-20240109917: PYRAZOLOTHIAZOLE CARBOXAMIDES AND THEIR USES AS PDGFR INHIBITORS
N-(5-(2-(2-oxa-7- azaspiro[4.4]nonan-7- yl)acetamido)-2-methylpyridin- 3-yl)-2-(2-methoxypyridin-3- yl)pyrazolo[5,1-b]thiazole-7- carboxamide	IC50	0.2 nM	US-20240109917: PYRAZOLOTHIAZOLE CARBOXAMIDES AND THEIR USES AS PDGFR INHIBITORS
N-(5-(2-(5-azaspiro[2.5]octan-5- yl)acetamido)-2-methylpyridin- 3-yl)-2-(2-methoxypyridin-3- yl)pyrazolo[5,1-b]thiazole-7- carboxamide	IC50	0.2 nM	US-20240109917: PYRAZOLOTHIAZOLE CARBOXAMIDES AND THEIR USES AS PDGFR INHIBITORS
(S)-N-(5-(2-(1- isopropylpyrrolidin-2- yl)acetamido)-2-methylpyridin- 3-yl)-2-(2-methoxypyridin-3- yl)pyrazolo[5,1-b]thiazole-7- carboxamide	IC50	0.2 nM	US-20240109917: PYRAZOLOTHIAZOLE CARBOXAMIDES AND THEIR USES AS PDGFR INHIBITORS

ChEMBL bioactivities

2882 potent at pChembl≥5 of 3076 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
10.12	Kd	0.075	nM	SUNITINIB
10.05	Kd	0.089	nM	CHEMBL3752910
10.00	IC50	0.1	nM	CHEMBL526507
10.00	IC50	0.1	nM	CHEMBL495749
9.99	ED50	0.102	nM	CHEMBL3752910
9.90	Ki	0.1259	nM	CHEMBL196363
9.85	IC50	0.14	nM	CHEMBL5977738
9.70	IC50	0.2	nM	CHEMBL2023477
9.70	IC50	0.2	nM	CHEMBL2023485
9.70	Kd	0.2	nM	SUNITINIB
9.70	IC50	0.2	nM	CHEMBL495984
9.68	Kd	0.21	nM	SUNITINIB
9.59	IC50	0.26	nM	SORAFENIB
9.54	Kd	0.29	nM	SU-014813
9.54	Kd	0.29	nM	CHEMBL1908396
9.52	IC50	0.3	nM	CHEMBL2023476
9.52	IC50	0.3	nM	CHEMBL495762
9.52	IC50	0.3	nM	CHEMBL498551
9.52	IC50	0.3	nM	CHEMBL1940109
9.50	Ki	0.3162	nM	CHEMBL1999414
9.49	Kd	0.32	nM	CEDIRANIB
9.40	IC50	0.4	nM	CHEMBL2023482
9.40	IC50	0.4	nM	CHEMBL2347053
9.40	IC50	0.4	nM	CHEMBL498013
9.40	IC50	0.4	nM	CHEMBL1940273
9.40	IC50	0.4	nM	CHEMBL340284
9.40	IC50	0.4	nM	CHEMBL123928
9.40	Ki	0.3981	nM	CHEMBL1996649
9.38	IC50	0.42	nM	CHEMBL5881155
9.32	IC50	0.475	nM	CHEMBL5758096
9.31	IC50	0.487	nM	CHEMBL6052352
9.30	IC50	0.5	nM	CHEMBL2023486
9.30	IC50	0.5	nM	CHEMBL6028045
9.30	IC50	0.5	nM	CHEMBL13976
9.30	Ki	0.5012	nM	CHEMBL1965170
9.30	Ki	0.5012	nM	ILORASERTIB
9.24	Kd	0.57	nM	AXITINIB
9.22	IC50	0.6	nM	STAUROSPORINE
9.22	IC50	0.6	nM	CHEMBL495735
9.20	IC50	0.626	nM	CHEMBL5857889
9.20	Kd	0.63	nM	DASATINIB
9.20	Ki	0.631	nM	CHEMBL1988437
9.17	IC50	0.68	nM	CHEMBL5936239
9.15	IC50	0.7	nM	CHEMBL2023118
9.15	IC50	0.7	nM	CHEMBL495763
9.14	IC50	0.727	nM	CHEMBL5888997
9.13	IC50	0.739	nM	CHEMBL5990952
9.12	IC50	0.76	nM	STAUROSPORINE
9.10	IC50	0.793	nM	CHEMBL6007247
9.10	IC50	0.8	nM	CHEMBL1940108

PubChem BioAssay actives

2128 with measured affinity, of 4819 total; 50 most potent distinct compounds. Largely complementary to BindingDB; screening values are coarse (µM, 4 dp), so sub-nM hits tie at the floor.

Compound	Assay	Type	Value	Unit
4-amino-3-(1H-benzimidazol-2-yl)-5-(1-methylpiperidin-3-yl)oxy-1H-quinolin-2-one	411861: Inhibition of human recombinant PDGFRbeta	ic50	0.0001	uM
4-amino-N-benzyl-3-[6-(4-methylpiperazin-1-yl)-1H-benzimidazol-2-yl]-2-oxo-1H-quinoline-6-carboxamide	411861: Inhibition of human recombinant PDGFRbeta	ic50	0.0001	uM
4-methyl-3-[(1-methyl-6-pyridin-3-ylpyrazolo[3,4-d]pyrimidin-4-yl)amino]-N-[3-(trifluoromethyl)phenyl]benzamide	2148958: Binding affinity to human PDGFRB incubated for 45 mins by Kinobead based pull down assay	kd	0.0001	uM
Sunitinib	435926: Binding constant for PDGFRB kinase domain	kd	0.0001	uM
3-(1H-benzimidazol-2-yl)-4-[(4-ethyl-1-methylpiperidin-2-yl)amino]-1H-quinolin-2-one	411861: Inhibition of human recombinant PDGFRbeta	ic50	0.0002	uM
2-[4-(6,7-dimethoxyquinolin-4-yl)oxy-2-methoxyphenyl]-N-(4,5-dimethyl-1,2-oxazol-3-yl)acetamide	660685: Inhibition of PDGFRbeta	ic50	0.0002	uM
2-[4-(6,7-dimethoxyquinolin-4-yl)oxy-2-methoxyphenyl]-N-(5-ethyl-1H-pyrazol-3-yl)acetamide	660685: Inhibition of PDGFRbeta	ic50	0.0002	uM
5-[(Z)-(5-fluoro-2-oxo-1H-indol-3-ylidene)methyl]-N-[(2S)-2-hydroxy-3-morpholin-4-ylpropyl]-2,4-dimethyl-1H-pyrrole-3-carboxamide	435926: Binding constant for PDGFRB kinase domain	kd	0.0003	uM
4-amino-3-(1H-benzimidazol-2-yl)-5-(4-methylpiperazin-1-yl)-1H-quinolin-2-one	411861: Inhibition of human recombinant PDGFRbeta	ic50	0.0003	uM
4-amino-5-chloro-3-[6-(4-methylpiperazin-1-yl)-1H-benzimidazol-2-yl]-1H-quinolin-2-one	411861: Inhibition of human recombinant PDGFRbeta	ic50	0.0003	uM
2-[4-[6-methoxy-7-(2-methoxyethoxy)quinazolin-4-yl]oxypyrazol-1-yl]-N-(3-methoxyphenyl)acetamide	639905: Inhibition of PDGFRbeta phosphorylation by cell based assay	ic50	0.0003	uM
2-[2-methoxy-4-(7-methoxyquinolin-4-yl)oxyphenyl]-N-(5-methyl-1,3-thiazol-2-yl)acetamide	660685: Inhibition of PDGFRbeta	ic50	0.0003	uM
1-[4-(6,7-dimethoxyquinolin-4-yl)oxy-2-methoxyphenyl]-3-[1-(1,3-thiazol-2-yl)ethyl]urea	624875: Binding constant for PDGFRB kinase domain	kd	0.0003	uM
4-[(4-fluoro-2-methyl-1H-indol-5-yl)oxy]-6-methoxy-7-(3-pyrrolidin-1-ylpropoxy)quinazoline	624875: Binding constant for PDGFRB kinase domain	kd	0.0003	uM
4-[6,7-bis(2-methoxyethoxy)quinazolin-4-yl]-N-(4-isoquinolin-5-yloxyphenyl)piperazine-1-carboxamide	161392: Inhibition of platelet-derived growth factor receptor beta phosphorylation in MG63 cells in the absence of plasma	ic50	0.0004	uM
4-[6,7-bis(2-methoxyethoxy)quinazolin-4-yl]-N-(4-naphthalen-2-yloxyphenyl)piperazine-1-carboxamide	161392: Inhibition of platelet-derived growth factor receptor beta phosphorylation in MG63 cells in the absence of plasma	ic50	0.0004	uM
4-amino-7-fluoro-3-[6-(4-methylpiperazin-1-yl)-1H-benzimidazol-2-yl]-1H-quinolin-2-one	411861: Inhibition of human recombinant PDGFRbeta	ic50	0.0004	uM
(3Z)-3-[[5-(2-nitrophenyl)-1H-pyrazol-4-yl]methylidene]-1H-indol-2-one	739577: Inhibition of PDGFRbeta (unknown origin) after 10 mins by mobility shift assay	ic50	0.0004	uM
2-[4-(6,7-dimethoxyquinolin-4-yl)oxyphenyl]-N-(1-ethylpyrazol-4-yl)acetamide	639905: Inhibition of PDGFRbeta phosphorylation by cell based assay	ic50	0.0004	uM
N-(5-ethyl-1,2-oxazol-3-yl)-2-[2-methoxy-4-(7-methoxyquinolin-4-yl)oxyphenyl]acetamide	660685: Inhibition of PDGFRbeta	ic50	0.0004	uM
N-[2-(dimethylamino)ethyl]-5-[(Z)-(5-fluoro-2-oxo-1H-indol-3-ylidene)methyl]-2,4-dimethyl-1H-pyrrole-3-carboxamide	161263: Inhibition of Platelet-derived growth factor receptor beta (PDGF-Rbeta)	ic50	0.0005	uM
N-(5-ethyl-1H-pyrazol-3-yl)-2-[2-methoxy-4-(7-methoxyquinolin-4-yl)oxyphenyl]acetamide	660685: Inhibition of PDGFRbeta	ic50	0.0005	uM
N-(2-chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)piperazin-1-yl]-2-methylpyrimidin-4-yl]amino]-1,3-thiazole-5-carboxamide;hydrate	435926: Binding constant for PDGFRB kinase domain	kd	0.0006	uM
4-amino-6-(benzylamino)-3-[6-(4-methylpiperazin-1-yl)-1H-benzimidazol-2-yl]-1H-quinolin-2-one	411861: Inhibition of human recombinant PDGFRbeta	ic50	0.0006	uM
(2S,3R,4R,6R)-3-methoxy-2-methyl-4-(methylamino)-29-oxa-1,7,17-triazaoctacyclo[12.12.2.12,6.07,28.08,13.015,19.020,27.021,26]nonacosa-8,10,12,14,19,21,23,25,27-nonaen-16-one	1308973: Inhibition of PDGFRbeta (unknown origin) incubated for 1 hr by spectrophotometric analysis	ic50	0.0006	uM
Axitinib	624875: Binding constant for PDGFRB kinase domain	kd	0.0006	uM
4-amino-5-methyl-3-[6-(4-methylpiperazin-1-yl)-1H-benzimidazol-2-yl]-1H-quinolin-2-one	411861: Inhibition of human recombinant PDGFRbeta	ic50	0.0007	uM
N-(1-ethylpyrazol-4-yl)-2-[2-methoxy-4-(7-methoxyquinolin-4-yl)oxyphenyl]acetamide	660685: Inhibition of PDGFRbeta	ic50	0.0007	uM
trans-(1S,2S)-2-[[6-[(2-amino-3-chloro-4-pyridinyl)methoxy]-1,3-benzothiazol-2-yl]amino]cyclohexan-1-ol	1723265: Binding affinity to human wild type PDGFRbeta (V582 to Y1009 residues) expressed in bacterial expression system by kinome scan assay	kd	0.0008	uM
2-[4-(6,7-dimethoxyquinazolin-4-yl)oxypyrazol-1-yl]-N-(3-methoxyphenyl)acetamide	639905: Inhibition of PDGFRbeta phosphorylation by cell based assay	ic50	0.0008	uM
3-(1H-benzimidazol-2-yl)-4-(piperidin-4-ylmethylamino)-1H-quinolin-2-one	411861: Inhibition of human recombinant PDGFRbeta	ic50	0.0009	uM
4-amino-3-[6-(4-methylpiperazine-1-carbonyl)-1H-benzimidazol-2-yl]-1H-quinolin-2-one	411861: Inhibition of human recombinant PDGFRbeta	ic50	0.0009	uM
2-N-[4-(4-ethylpiperazin-1-yl)-3-methoxyphenyl]-4-N-(1H-indazol-6-yl)-5-methylpyrimidine-2,4-diamine	1903975: Inhibition of PDGFRbeta (unknown origin) by caliper mobility shift assay	ic50	0.0009	uM
N-(3-tert-butyl-1,2-oxazol-5-yl)-2-[4-[5-(1H-pyrazol-4-yl)benzimidazol-1-yl]phenyl]acetamide	2214734: Inhibition of PDGFR-beta (unknown origin)	ic50	0.0009	uM
2-[4-(6,7-dimethoxyquinazolin-4-yl)oxyphenyl]-N-(3-methoxyphenyl)acetamide	639905: Inhibition of PDGFRbeta phosphorylation by cell based assay	ic50	0.0009	uM
2-[4-(6,7-dimethoxyquinolin-4-yl)oxy-2-methoxyphenyl]-N-(1-ethylpyrazol-4-yl)acetamide	660685: Inhibition of PDGFRbeta	ic50	0.0009	uM
4-[6,7-bis(2-methoxyethoxy)quinazolin-4-yl]-N-[4-(1H-indol-4-yloxy)phenyl]piperazine-1-carboxamide	161392: Inhibition of platelet-derived growth factor receptor beta phosphorylation in MG63 cells in the absence of plasma	ic50	0.0010	uM
6,7-dimethoxy-N-[3-(trifluoromethyl)phenyl]-1,4-dihydroindeno[2,1-d]pyrazol-3-amine	256697: Antiproliferative activity against PDGF-BB stimulated HCASMC	ic50	0.0010	uM
1-(3-methyl-4-morpholin-4-ylphenyl)-3-[4-(3-methyl-2H-pyrazolo[3,4-b]pyridin-4-yl)phenyl]urea	1444973: Inhibition of human His-tagged PDGFRbeta (558 to 1106 residues) expressed in baculovirus by ELISA	ic50	0.0010	uM
4-amino-5-fluoro-3-[6-(4-methylpiperazin-1-yl)-1H-benzimidazol-2-yl]-1H-quinolin-2-one	1431275: Inhibition of recombinant PDGFRbeta (unknown origin) expressed in baculovirus infected insect cells using biotinylated peptide substrate GGLFDDPSYVNVQNL in presence of ATP incubated for 1 to 4 hrs by time resolved fluorescence assay	ic50	0.0010	uM
N-[2-(4-amino-2-oxo-1H-quinolin-3-yl)-3H-benzimidazol-5-yl]-2-(dimethylamino)-N-methylacetamide	411861: Inhibition of human recombinant PDGFRbeta	ic50	0.0010	uM
4-amino-6-fluoro-3-[6-(4-methylpiperazin-1-yl)-1H-benzimidazol-2-yl]-1H-quinolin-2-one	411861: Inhibition of human recombinant PDGFRbeta	ic50	0.0010	uM
4-chloro-2-[5-[[(1R)-2-hydroxy-1-phenylethyl]amino]-3-isoquinolin-6-yl-2-pyridinyl]phenol	1450719: Inhibition of recombinant PDGFR-beta (unknown origin) using poly (Glu,Tyr) 4:1 as substrate after 60 mins by ELISA	ic50	0.0010	uM
5-fluoro-2-[5-[[(1R)-2-hydroxy-1-phenylethyl]amino]-3-(3-methyl-2H-indazol-5-yl)-2-pyridinyl]phenol	1450719: Inhibition of recombinant PDGFR-beta (unknown origin) using poly (Glu,Tyr) 4:1 as substrate after 60 mins by ELISA	ic50	0.0010	uM
N-(3-tert-butylphenyl)-1-methyl-5-[[2-[5-(trifluoromethyl)-1H-imidazol-2-yl]-4-pyridinyl]oxy]benzimidazol-2-amine	1255119: Inhibition of PDGFRbeta (unknown origin)	ic50	0.0010	uM
N-(4-chlorophenyl)-6-(6,7-dimethoxyquinolin-4-yl)oxynaphthalene-1-carboxamide	326901: Inhibition of PDGFRbeta	ic50	0.0010	uM
N-(4,5-dimethyl-1,2-oxazol-3-yl)-2-[2-methoxy-4-(7-methoxyquinolin-4-yl)oxyphenyl]acetamide	660685: Inhibition of PDGFRbeta	ic50	0.0010	uM
1-N’-[3-fluoro-4-[6-methoxy-7-(3-morpholin-4-ylpropoxy)quinolin-4-yl]oxyphenyl]-1-N-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide	624875: Binding constant for PDGFRB kinase domain	kd	0.0010	uM
Toceranib	161263: Inhibition of Platelet-derived growth factor receptor beta (PDGF-Rbeta)	ic50	0.0010	uM
5-[(Z)-(5-fluoro-2-oxo-1H-indol-3-ylidene)methyl]-2,4-dimethyl-N-(pyridin-4-ylmethyl)-1H-pyrrole-3-carboxamide	161263: Inhibition of Platelet-derived growth factor receptor beta (PDGF-Rbeta)	ic50	0.0010	uM

CTD chemical–gene interactions

126 total (human), top 30 by PubMed support.

Chemical	Actions (top 5)	PubMed papers
(+)-JQ1 compound	decreases reaction, increases expression, decreases expression	5
Benzo(a)pyrene	decreases methylation, increases expression, increases methylation, affects methylation, decreases expression	5
Tetrachlorodibenzodioxin	affects expression, decreases expression	4
Sorafenib	affects cotreatment, decreases phosphorylation, decreases activity	3
Particulate Matter	decreases expression, increases abundance, affects expression	3
lipoxin A4	affects reaction, increases phosphorylation, decreases reaction, increases activity, decreases phosphorylation (+1 more)	2
perfluorooctane sulfonic acid	affects expression, affects cotreatment, decreases expression	2
6,7-dimethoxy-2-phenylquinoxaline	decreases reaction, increases expression, increases phosphorylation	2
CP-673,451	decreases reaction, increases phosphorylation, decreases activity, decreases phosphorylation	2
ponatinib	decreases activity	2
Imatinib Mesylate	decreases expression, decreases phosphorylation	2
Dasatinib	decreases phosphorylation, increases expression	2
Resveratrol	affects binding, decreases reaction, increases phosphorylation	2
Aldrin	affects cotreatment, increases expression	2
Arsenic	affects expression, affects cotreatment, decreases expression, increases abundance	2
Cadmium	decreases expression, increases abundance	2
Copper	affects binding, decreases expression, increases expression	2
Dichlorodiphenyldichloroethane	affects cotreatment, increases expression	2
Dichlorodiphenyl Dichloroethylene	affects cotreatment, increases expression	2
Dieldrin	affects cotreatment, increases expression	2
Cyclosporine	decreases expression, increases expression	2
Copper Sulfate	decreases reaction, increases expression, decreases expression	2
Genistein	increases phosphorylation, increases reaction, decreases expression, decreases reaction, increases activity	2
GSK-J4	decreases expression	1
ammonium 2,3,3,3-tetrafluoro-2-(heptafluoropropoxy)-propanoate	affects expression, affects cotreatment	1
Baizhu	decreases expression	1
Fangfeng	decreases expression	1
dicrotophos	increases expression	1
methylmercuric chloride	increases expression	1
triphenyl phosphate	affects expression	1

ChEMBL screening assays

1237 unique, capped per target: 1213 binding, 16 functional, 8 admet

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL1005541	Binding	Inhibition of Tel-fused PDGFRb kinase-mediated mouse BaF3 cell proliferation	Identification of NVP-TAE684, a potent, selective, and efficacious inhibitor of NPM-ALK. — *Proc Natl Acad Sci U S A*
CHEMBL1963778	Functional	PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member name: PDGFRB	PubChem BioAssay data set
CHEMBL4044107	ADMET	Inhibition of wild-type human partial length PDGFRB (V582 to Y1009 residues) expressed in Escherichia coli BL21 assessed as residual activity at 1000 nM after 30 mins by Kinomescan method relative to control	2-Oxo-3, 4-dihydropyrimido[4, 5-d]pyrimidinyl derivatives as new irreversible pan fibroblast growth factor receptor (FGFR) inhibitors. — *Eur J Med Chem*

Cellosaurus cell lines

27 cell lines: 18 spontaneously immortalized cell line, 9 cancer cell line

First 10 cell lines (id-ordered, not curated):

Cellosaurus	Name	Category	Sex
CVCL_1150	CTV-1	Cancer cell line	Male
CVCL_1326	Karpas-45	Cancer cell line	Male
CVCL_8150	MOLT-15	Cancer cell line	Male
CVCL_B0YI	Abcam SH-SY5Y PDGFRB KO	Cancer cell line	Female
CVCL_B8MA	Abcam HCT 116 PDGFRB KO	Cancer cell line	Male
CVCL_B9A5	Abcam MCF-7 PDGFRB KO	Cancer cell line	Female
CVCL_B9PH	Abcam A-549 PDGFRB KO	Cancer cell line	Male
CVCL_E0JT	Ubigene HeLa PDGFRB KO	Cancer cell line	Female
CVCL_E4X4	ZR-75-1 PDGFRA clone 30	Cancer cell line	Female
CVCL_XG30	TRMP PDGFRB-p.Arg634	Spontaneously immortalized cell line	Female

Clinical trials (associated diseases)

Via MONDO — disease-level, not drug-specific.

showing 60 of 301 trials:

NCT	Phase	Status	Title
NCT00154830	Phase 4	COMPLETED	Alterations of Functional Activities and Leg Stiffness After Hamstring Lengthening in Cerebral Palsy Children
NCT00432055	Phase 4	COMPLETED	Effects of Botulinum Toxin Type A in Adults With Cerebral Palsy
NCT00549471	Phase 4	TERMINATED	Improvement After Botulinum Toxin Injections to the Arms in Children With Cerebral Palsy
NCT00752934	Phase 4	TERMINATED	Does Oral Baclofen Improve Care and Comfort in Spastic Children in Nursing Homes?
NCT00964639	Phase 4	COMPLETED	Postoperative Pain in Children With Cerebral Palsy After Pelvic and Femoral Osteotomies
NCT01386255	Phase 4	WITHDRAWN	Placebo Controlled Study of Baclofen for GERD in Children With Cerebral Palsy
NCT02546999	Phase 4	COMPLETED	Does Botulinum Toxin A Make Walking Easier in Children With Cerebral Palsy?
NCT02633241	Phase 4	COMPLETED	A Pilot Study of Dexmedetomidine-Propofol in Children Undergoing Magnetic Resonance Imaging
NCT03117322	Phase 4	COMPLETED	Synbiotic, Prebiotics and Probiotics in Children With Cerebral Palsy and Constipation
NCT03648658	Phase 4	UNKNOWN	Paracetamol Study in Patients With Low Muscle Mass
NCT04074265	Phase 4	COMPLETED	Peri-operative Use of a Pain Injection in Pediatric Patients With Cerebral Palsy
NCT04273737	Phase 4	TERMINATED	Amantadine in Treating Cognitive & Motor Impairments in Adolescents and Adults With Cerebral Palsy
NCT04523935	Phase 4	COMPLETED	Excessive Crying in Children With Cerebral Palsy and Communication Deficits
NCT05887765	Phase 4	COMPLETED	Effect of Systematic Dexamethasone on the Duration of Popliteal Nerve Block for Anesthesia After Pediatric Ankle Surgery
NCT06176430	Phase 4	UNKNOWN	Comparison of Twice Weekly Versus Daily Iron Therapy in Treating Anemia in Children With Cerebral Palsy
NCT06189781	Phase 4	RECRUITING	Pain Injection Versus Epidural Anesthesia for Hip Surgery in Pediatric Patients With Cerebral Palsy
NCT00014989	Phase 3	COMPLETED	Beneficial Effects of Antenatal Magnesium Sulfate (BEAM Trial)
NCT00065949	Phase 3	UNKNOWN	Magnesium Sulfate to Prevent Brain Injury in Premature Infants
NCT00367068	Phase 3	COMPLETED	Dutch National ITB Study in Children With Cerebral Palsy
NCT00491894	Phase 3	COMPLETED	Safety and Efficacy Study of Oral Glycopyrrolate Liquid for the Treatment of Pathologic (Chronic Moderate to Severe) Drooling in Pediatric Patients 3 to 18 Years of Age With Cerebral Palsy or Other Neurologic Conditions
NCT00632528	Phase 3	COMPLETED	MEOPA to Improve Physical Therapy Results After Multilevel Surgery
NCT00822029	Phase 3	TERMINATED	Use of Oral Bisphosphonates in the Treatment of Osteoporosis of Non-walking Children With Cerebral Palsy
NCT00922077	Phase 3	COMPLETED	Individualized Neurodevelopmental Treatment
NCT01249417	Phase 3	COMPLETED	Dysport® Pediatric Lower Limb Spasticity Study
NCT01251380	Phase 3	COMPLETED	Dysport® Pediatric Lower Limb Spasticity Follow-on Study
NCT01437644	Phase 3	COMPLETED	The Post-Operative Pain in Cerebral Palsy (POPPIES) Trial
NCT01492608	Phase 3	COMPLETED	Magnesium Sulphate for Preterm Birth (MASP Study)
NCT01603602	Phase 3	COMPLETED	BOTOX® Treatment in Pediatric Upper Limb Spasticity
NCT01603615	Phase 3	COMPLETED	BOTOX® Open-Label Treatment in Pediatric Upper Limb Spasticity
NCT01603628	Phase 3	COMPLETED	BOTOX® Treatment in Pediatric Lower Limb Spasticity
NCT01603641	Phase 3	COMPLETED	BOTOX® Open-Label Treatment in Pediatric Lower Limb Spasticity
NCT01633736	Phase 3	UNKNOWN	Targeted Hip Strength Training in Children With Cerebral Palsy (CP)
NCT01898520	Phase 3	COMPLETED	A Safety, Efficacy and Tolerability Study of Sativex for the Treatment of Spasticity in Children Aged 8 to 18 Years
NCT01929434	Phase 3	COMPLETED	Efficacy of Stem Cell Transplantation Compared to Rehabilitation Treatment of Patients With Cerebral Paralysis
NCT02002884	Phase 3	COMPLETED	Dose-response Study of Efficacy and Safety of Botulinum Toxin Type A to Treat Spasticity of the Arm(s) or of Arm(s) and Leg(s) in Cerebral Palsy
NCT02270736	Phase 3	COMPLETED	Clinical Study to Investigate the Efficacy and Safety of NT 201 Compared to Placebo in the Treatment of Chronic Troublesome Drooling Associated With Neurological Disorders and/or Intellectual Disability
NCT02839785	Phase 3	TERMINATED	Analgesia and Physiotherapy in Children With Cerebral Palsy (ANTALKINECP)
NCT03110341	Phase 3	UNKNOWN	Effect of Erythropoietin in Premature Infants on White Matter Lesions and Neurodevelopmental Outcome
NCT03302871	Phase 3	COMPLETED	Integrated Management Enhances Functional Gains in Children With Cerebral Palsy Treated by BoNT-A
NCT03306212	Phase 3	COMPLETED	Efficacy of Intermittent Serial Casting on Spastic Wrist Flexion Deformity
NCT03469999	Phase 3	COMPLETED	Effect of Dysport Injections on Energy Expenditure and Walking Efficiency in Children With Cerebral Palsy
NCT03472261	Phase 3	COMPLETED	Integrated Management of Pronation Deformity in Cerebral Palsy
NCT03616067	Phase 3	TERMINATED	Evaluation of the Efficacy of the Injection of Botulinum Toxin A vs Scopolamine Patches in the Treatment of Drooling in Children With Cerebral Palsy
NCT05206513	Phase 3	COMPLETED	Study to Assess the Efficacy, Safety, and Tolerability of Valbenazine for the Treatment of Dyskinesia Due to Cerebral Palsy
NCT06128616	Phase 3	UNKNOWN	Efficacy of Extracorporeal Shock Wave Therapy in Children With Cerebral Palsy
NCT06840158	Phase 3	COMPLETED	Double-blind Comparative Randomized Multicenter
NCT07524972	Phase 3	RECRUITING	Antenatal Magnesium Sulphate in High-Risk Preterm Patients
NCT07672158	Phase 3	NOT_YET_RECRUITING	Tranexamic Acid to Reduce Blood Loss After Varus Derotation Osteotomy
NCT05662111	Phase 2	RECRUITING	Treatment of Ectopic Calcification in Fahr’s Disease or Syndrome
NCT00060957	Phase 2	COMPLETED	Botulinum Toxin (BOTOX) for Cerebral Palsy
NCT00061139	Phase 2	UNKNOWN	Constraint-Based Therapy to Improve Motor Function in Children With Cerebral Palsy
NCT00114075	Phase 2	COMPLETED	Effects of Walking Analysis on Surgical Outcomes
NCT00221247	Phase 2	COMPLETED	Acupuncture as Complementary Therapy for Cerebral Palsy
NCT00221611	Phase 2	COMPLETED	Intrathecal Administration of Baclofen (ITB) to Cerebral Palsy Patients With Therapy-Resistant Spasticity
NCT00295295	Phase 2	COMPLETED	Vibration Intervention to Improve Bone and Muscle in Children With Cerebral Palsy
NCT00413946	Phase 2	COMPLETED	Does Erythropoietin Improve Outcome in Very Preterm Infants?
NCT00455637	Phase 2	TERMINATED	Which is the Best Dose of Dysport in Helping With Hip Pain for Children With Cerebral Palsy?
NCT00467207	Phase 2	COMPLETED	Intensive Strength Training in Children With Cerebral Palsy - Effect on Hand Function
NCT01028833	Phase 2	COMPLETED	Effects of Power Mobility on Young Children With Severe Motor Impairments
NCT01115998	Phase 2	COMPLETED	Effect of Power Wheelchairs on the Development and Function of Young Children With Severe Physical Disabilities

Predicted chemistry — Sugi Predict

The predicted patent-compound landscape for PDGFRB across ~30M SureChEMBL compounds — explore on Sugi Predict.