General Information of the Protein
Protein ID
PT00844
Protein Name
Platelet-derived growth factor receptor beta
Secondarily
Protein Name
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
Gene Name
PDGFRB
Secondarily
Gene Name
PDGFR
PDGFR1
Sequence
MRLPGAMPALALKGELLLLSLLLLLEPQISQGLVVTPPGPELVLNVSSTFVLTCSGSAPVVWERMSQEPPQEMAKAQDGTFSSVLTLTNLTGLDTGEYFCTHNDSRGLETDERKRLYIFVPDPTVGFLPNDAEELFIFLTEITEITIPCRVTDPQLVVTLHEKKGDVALPVPYDHQRGFSGIFEDRSYICKTTIGDREVDSDAYYVYRLQVSSINVSVNAVQTVVRQGENITLMCIVIGNEVVNFEWTYPRKESGRLVEPVTDFLLDMPYHIRSILHIPSAELEDSGTYTCNVTESVNDHQDEKAINITVVESGYVRLLGEVGTLQFAELHRSRTLQVVFEAYPPPTVLWFKDNRTLGDSSAGEIALSTRNVSETRYVSELTLVRVKVAEAGHYTMRAFHEDAEVQLSFQLQINVPVRVLELSESHPDSGEQTVRCRGRGMPQPNIIWSACRDLKRCPRELPPTLLGNSSEEESQLETNVTYWEEEQEFEVVSTLRLQHVDRPLSVRCTLRNAVGQDTQEVIVVPHSLPFKVVVISAILALVVLTIISLIILIMLWQKKPRYEIRWKVIESVSSDGHEYIYVDPMQLPYDSTWELPRDQLVLGRTLGSGAFGQVVEATAHGLSHSQATMKVAVKMLKSTARSSEKQALMSELKIMSHLGPHLNVVNLLGACTKGGPIYIITEYCRYGDLVDYLHRNKHTFLQHHSDKRRPPSAELYSNALPVGLPLPSHVSLTGESDGGYMDMSKDESVDYVPMLDMKGDVKYADIESSNYMAPYDNYVPSAPERTCRATLINESPVLSYMDLVGFSYQVANGMEFLASKNCVHRDLAARNVLICEGKLVKICDFGLARDIMRDSNYISKGSTFLPLKWMAPESIFNSLYTTLSDVWSFGILLWEIFTLGGTPYPELPMNEQFYNAIKRGYRMAQPAHASDEIYEIMQKCWEEKFEIRPPFSQLVLLLERLLGEGYKKKYQQVDEEFLRSDHPAILRSQARLPGFHGLRSPLDTSSVLYTAVQPNEGDNDYIIPLPDPKPEVADEGPLEGSPSLASSTLNEVNTSSTISCDSPLEPQDEPEPEPQLELQVEPEPELEQLPDSGCPAPRAEAEDSFL
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Organism
Homo sapiens, Human
Protein Classification
Enzyme
>
Kinase
>
Protein Kinase
>
TK protein kinase group
>
Tyrosine protein kinase PDGFR family
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.
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Uniprot ID
Primary ID:
P09619

Secondarily ID:
B5A957
Q8N5L4
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Ensembl ID
ENSG00000113721
HGNC ID
HGNC:8804
Subcellular Location
Cell membrane
Cytoplasmic vesicle
Lysosome lumen
Map of Molecular Bioactivity Related to the Protein
Map of Molecular Bioactivity Related to the Protein

Protein
Cell Line
Compound

Bioactivity Value:

<= 0.1 μM
> 0.1 μM and <= 10 μM
> 10 μM
Imprecise Activity
Table of Molecular Bioactivities Related to the Protein
Cell Line ID: CL000052 , A-431
Compound ID Compound Name Compound Formula
CP0371872
2-Amino-4-(N-methyl-m-bromoanilino)-6-(2,5-dimethoxybenzyl)-pyrrolo[2,3-d]pyrimidine
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C22H22BrN5O2
 1
1
IC50 = 1300 nM
   TI
   LI
   LO
   TS
CP0376206
2-Amino-4-(m-bromoanilino)-6-benzyl-7-methyl-pyrrolo-[2,3-d]pyrimidine
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C20H18BrN5
 1
1
IC50 = 2800 nM
   TI
   LI
   LO
   TS
CP0016245
(3Z)-3-{[4-(dimethylamino)phenyl]methylidene}-2,3-dihydro-1H-indol-2-one
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C17H16N2O
 1
1
IC50 = 3750 nM
   TI
   LI
   LO
   TS
CP0096083
4-N-(3-bromophenyl)-6-[(2,5-dimethoxyphenyl)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamine
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C21H20BrN5O2
 1
1
IC50 = 8920 nM
   TI
   LI
   LO
   TS
CP0002211
N-[2-(diethylamino)ethyl]-5-[(Z)-(5-fluoro-2-oxo-1H-indol-3-ylidene)methyl]-2,4-dimethyl-1H-pyrrole-3-carboxamide
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C22H27FN4O2
 1
1
IC50 = 12200 nM
   TI
   LI
   LO
   TS
CP0428721
2-Amino-4-(N-methyl-m-bromoanilino)-6-(2-methylbenzyl)-pyrrolo[2,3-d]pyrimidine
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C21H20BrN5
 1
1
IC50 = 34800 nM
   TI
   LI
   LO
   TS
CP0091116
2-benzyl-N4-(3-bromophenyl)-1H-indole-4,6-diamine
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C19H16BrN5
 1
1
IC50 > 50000 nM
   TI
   LI
   LO
   TS
CP0167979
4-N-(3-bromophenyl)-6-[(2-methylphenyl)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamine
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C20H18BrN5
 1
1
IC50 > 50000 nM
   TI
   LI
   LO
   TS
CP0428464
2-Amino-4-(N-methyl-m-bromoanilino)-6-benzyl-7-methyl-pyrrolo[2,3-d]pyrimidine
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C21H20BrN5
 1
1
IC50 = 71700 nM
   TI
   LI
   LO
   TS
CP0037987
N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)quinazolin-4-amine
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C22H23N3O4
 1
1
IC50 = 83100 nM
   TI
   LI
   LO
   TS
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0043225
4-[4-[[4-chloro-3-(trifluoromethyl)phenyl]carbamoylamino]-3-fluorophenoxy]-N-methylpyridine-2-carboxamide
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C21H15ClF4N4O3
 1
1 IC50 = 1.5 nM
CP0002211
N-[2-(diethylamino)ethyl]-5-[(Z)-(5-fluoro-2-oxo-1H-indol-3-ylidene)methyl]-2,4-dimethyl-1H-pyrrole-3-carboxamide
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C22H27FN4O2
 10
1 IC50 = 2 nM
2 IC50 = 3.9 nM
3 IC50 = 9 nM
4 IC50 = 10.5 nM
5 IC50 = 10.6 nM
6 IC50 = 55 nM
7 Kd = 0.075 nM
8 Kd = 0.2 nM
9 Kd = 0.21 nM
10 Ki = 8 nM
CP0033861
(3Z)-4-amino-5-fluoro-3-[5-(4-methylpiperazino)-1,3-dihydrobenzimidazol-2-ylidene]carbostyril
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C21H21FN6O
 2
1 IC50 = 5 nM
2 Kd = 3.8 nM
CP0006946
2-(1H-indol-2-ylcarbonyl)-1H-indol-5-yl 2-methoxyacetate
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C20H16N2O4
 1
1 IC50 = 20 nM
CP0313546
US9233968, 27
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C21H14N4O
 1
1 IC50 = 27 nM
CP0263705
US9233968, 2
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C22H14F3N5O
 1
1 IC50 = 32 nM
CP0243759
US9233968, 1
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C22H18N6O
 1
1 IC50 = 34 nM
CP0000999
(Z)-3-[2,4-dimethyl-5-(2-oxo-1,2-dihydro-indol-3-ylidenemethyl)-1H-pyrrol-3-yl]-propionic acid
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C18H18N2O3
 2
1 IC50 = 50 nM
2 IC50 = 60 nM
CP0243760
US9233968, 4
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C22H14F4N6O
 1
1 IC50 = 55 nM
CP0002230
4-methyl-N-[3-(4-methyl-1H-imidazol-1-yl)-5-(trifluoromethyl)phenyl]-3-[(4-pyridin-3-ylpyrimidin-2-yl)amino]benzamide
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C28H22F3N7O
 3
1 IC50 = 60.11 nM
2 Kd = 16 nM
3 Kd = 73 nM
CP0008706
(3Z)-3-[(3,5-dimethyl-1H-pyrrol-2-yl)methylidene]-2,3-dihydro-1H-indol-2-one
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C15H14N2O
 7
1 IC50 = 68 nM
2 IC50 = 400 nM
3 IC50 = 680 nM
4 IC50 = 10100 nM
5 IC50 = 10500 nM
6 IC50 = 20260 nM
7 IC50 = 22900 nM
CP0001168
4-(6,7-Dimethoxy-quinazolin-4-yl)-piperazine-1-carboxylic acid (4-phenoxy-phenyl)-amide
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C27H27N5O4
 2
1 IC50 = 80 nM
2 IC50 = 130 nM
CP0098354
US9233968, 3
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C22H17N5O
 1
1 IC50 = 80 nM
CP0010647
(5-Hydroxy-1H-2-indolyl)(1H-2-indolyl)-methanone
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C17H12N2O2
 1
1 IC50 = 90 nM
CP0137907
2-(4-methylpiperazin-1-yl)-N-[4-methyl-5-[3-[(E)-2-pyridin-2-ylethenyl]-1H-indazol-6-yl]-1,3-thiazol-2-yl]acetamide
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C25H27N7OS
 1
1 IC50 = 95.7 nM
CP0006894
2-(1H-indol-2-ylcarbonyl)-1H-indol-5-yl 2-(dimethylamino)acetate
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C21H19N3O3
 1
1 IC50 = 100 nM
CP0034949
4-[6-methoxy-7-(3-piperidin-1-ylpropoxy)quinazolin-4-yl]-N-(4-propan-2-yloxyphenyl)piperazine-1-carboxamide
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C31H42N6O4
 4
1 IC50 = 170 nM
2 IC50 = 200 nM
3 Kd = 4.5 nM
4 Kd = 7.8 nM
CP0007946
4-(6,7-Dimethoxy-quinazolin-4-yl)-piperazine-1-carboxylic acid (4-nitro-phenyl)-amide
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C21H22N6O5
 2
1 IC50 = 240 nM
2 IC50 = 700 nM
CP0002778
4-[(4-methylpiperazin-1-yl)methyl]-N-[4-methyl-3-[(4-pyridin-3-ylpyrimidin-2-yl)amino]phenyl]benzamide
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C29H31N7O
 5
1 IC50 = 240 nM
2 IC50 = 386 nM
3 IC50 = 607 nM
4 Kd = 14 nM
5 Kd = 28 nM
CP0006715
2-(1H-indol-2-ylcarbonyl)-1H-indol-5-yl acetate
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C19H14N2O3
 1
1 IC50 = 300 nM
CP0241515
US9233968, 22
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C22H13F3N4O
 1
1 IC50 = 628 nM
CP0132656
US9233968, 21
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C22H16FN5O
 1
1 IC50 = 767 nM
CP0091315
US9422297, AAG145-136
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C17H13ClN4
 1
1 IC50 = 800 nM
CP0187571
US9233968, 24
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C21H12ClFN4O
 1
1 IC50 = 938 nM
CP0037987
N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)quinazolin-4-amine
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C22H23N3O4
 2
1 IC50 = 2300 nM
2 Kd = 1400 nM
CP0132717
US9233968, 25
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C23H14N4O2
 1
1 IC50 = 2715 nM
CP0040335
5-(phenylthio)-9H-pyrimido[4,5-b]indole-2,4-diamine
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C16H13N5S
 1
1 IC50 = 2800 nM
CP0015507
2-(4-(6-methoxy-7-(3-(4-methylpiperazin-1-yl)propoxy)quinazolin-4-yloxy)phenyl)benzo[d]thiazole
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C30H31N5O3S
 1
1 IC50 = 3500 nM
CP0050064
US9422297, AAG145-135
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C17H12ClFN4
 1
1 IC50 = 3600 nM
CP0419891
US9233968, 15
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C28H17Cl2F2N7O2
 1
1 IC50 = 3610 nM
CP0132657
US9233968, 28
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C22H16N4O
 1
1 IC50 = 4313 nM
CP0313513
US9233968, 26
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C22H15FN4O
 1
1 IC50 = 6083 nM
CP0080859
N-[2-(dimethylamino)ethyl]-N-[[4-[[4-methyl-3-[(4-pyridin-3-ylpyrimidin-2-yl)amino]phenyl]carbamoyl]phenyl]methyl]pyridine-3-carboxamide
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C34H34N8O2
 1
1 IC50 = 6115 nM
CP0093436
US9422297, AAG145-164
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C17H12ClFN4
 1
1 IC50 = 6400 nM
CP0011624
AG1295
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C16H14N2
 1
1 IC50 = 6500 nM
CP0129193
US9233968, 14
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C21H14ClFN6O
 1
1 IC50 = 6574 nM
CP0093435
US9422297, AAG145-161
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C17H13FN4
 1
1 IC50 = 7100 nM
CP0016366
2-(4-(6-methoxy-7-(3-(pyrrolidin-1-yl)propoxy)quinazolin-4-yloxy)phenyl)benzo[d]thiazole
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C29H28N4O3S
 1
1 IC50 = 7700 nM
CP0160645
US9422297, AAG145-126
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C20H20N4
 1
1 IC50 = 7800 nM
CP0096083
4-N-(3-bromophenyl)-6-[(2,5-dimethoxyphenyl)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamine
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C21H20BrN5O2
 1
1 IC50 = 8920 nM
CP0275218
4-N-(3-bromophenyl)-6-[(2,4-dichlorophenyl)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamine
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C19H14BrCl2N5
 1
1 IC50 = 17000 nM
CP0016245
(3Z)-3-{[4-(dimethylamino)phenyl]methylidene}-2,3-dihydro-1H-indol-2-one
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C17H16N2O
 1
1 IC50 = 19400 nM
CP0416275
US9422297, AAG145-124
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C20H20N4
 1
1 IC50 = 21700 nM
CP0093434
US9422297, AAG145-158
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C17H14N4
 1
1 IC50 = 43100 nM
CP0250195
US9422297, AAG145-159
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C18H16N4O
 1
1 IC50 = 75500 nM
CP0274117
US9233968, 10
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C30H17F8N7O2
 1
1 IC50 > 10000 nM
CP0323840
US9233968, 19
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C21H15N5O
 1
1 IC50 > 10000 nM
CP0331532
US9233968, 20
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C22H16FN5O
 1
1 IC50 > 10000 nM
CP0091116
2-benzyl-N4-(3-bromophenyl)-1H-indole-4,6-diamine
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C19H16BrN5
 1
1 IC50 > 50000 nM
CP0126790
4-N-(3-bromophenyl)-6-(naphthalen-1-ylmethyl)-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamine
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C23H18BrN5
 1
1 IC50 > 50000 nM
CP0167979
4-N-(3-bromophenyl)-6-[(2-methylphenyl)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamine
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C20H18BrN5
 1
1 IC50 > 50000 nM
CP0015519
(Z )-3-[(2,4-dimethyl-3-(ethoxycarbonyl)pyrrol-5-yl)methylidenyl]indolin-2-one
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C18H18N2O3
 1
1 IC50 > 100000 nM
Clinical Information about the Protein
Target 1 ( Platelet-derived growth factor receptor beta (PDGFRB) )
Target Type Successful Target
Disease 5 Target-related Diseases  5
1 Thrombocytopenia [ICD-11: 3B64]
2 Renal cell carcinoma [ICD-11: 2C90]
3 Solid tumour/cancer [ICD-11: 2A00-2F9Z]
4 Alzheimer disease [ICD-11: 8A20]
5 Gram-positive bacterial infection [ICD-11: 1B74-1G40]
Approved Drug(s) 2 Approved Drugs  2
1 Romiplostim Approved
Thrombocytopenia
2 Sorafenib Approved
Renal cell carcinoma
Clinical Trial Drug(s) 4 Clinical Trial Drugs  4
1 E-3810 Phase 3
Solid tumour/cancer
2 Famitinib Phase 2
Solid tumour/cancer
3 MK-2461 Phase 1/2
Alzheimer disease
4 TAK-593 Phase 1
Solid tumour/cancer
Investigative Drug(s) 1 Investigative Drug  1
1 HKI-9924129 Investigative
Gram-positive bacterial infection
Target 2 ( PDGFR beta messenger RNA (PDGFRB mRNA) )
Target Type Literature-reported Target
Similar Protein(s) and Bioactivity Statistics
50% Identity
Protein ID Protein Name Protein Organism
PT00832 Platelet-derived growth factor receptor beta Mus musculus, Mouse
PT05989 Platelet-derived growth factor receptor beta Rattus norvegicus, Rat