General Information of the Protein
Protein ID
PT01092
Protein Name
Platelet-derived growth factor receptor alpha
Secondarily
Protein Name
Alpha platelet-derived growth factor receptor
Alpha-type platelet-derived growth factor receptor
CD140 antigen-like family member A
CD140a antigen
Platelet-derived growth factor alpha receptor
Platelet-derived growth factor receptor 2
Gene Name
PDGFRA
Secondarily
Gene Name
PDGFR2
RHEPDGFRA
Sequence
MGTSHPAFLVLGCLLTGLSLILCQLSLPSILPNENEKVVQLNSSFSLRCFGESEVSWQYPMSEEESSDVEIRNEENNSGLFVTVLEVSSASAAHTGLYTCYYNHTQTEENELEGRHIYIYVPDPDVAFVPLGMTDYLVIVEDDDSAIIPCRTTDPETPVTLHNSEGVVPASYDSRQGFNGTFTVGPYICEATVKGKKFQTIPFNVYALKATSELDLEMEALKTVYKSGETIVVTCAVFNNEVVDLQWTYPGEVKGKGITMLEEIKVPSIKLVYTLTVPEATVKDSGDYECAARQATREVKEMKKVTISVHEKGFIEIKPTFSQLEAVNLHEVKHFVVEVRAYPPPRISWLKNNLTLIENLTEITTDVEKIQEIRYRSKLKLIRAKEEDSGHYTIVAQNEDAVKSYTFELLTQVPSSILDLVDDHHGSTGGQTVRCTAEGTPLPDIEWMICKDIKKCNNETSWTILANNVSNIITEIHSRDRSTVEGRVTFAKVEETIAVRCLAKNLLGAENRELKLVAPTLRSELTVAAAVLVLLVIVIISLIVLVVIWKQKPRYEIRWRVIESISPDGHEYIYVDPMQLPYDSRWEFPRDGLVLGRVLGSGAFGKVVEGTAYGLSRSQPVMKVAVKMLKPTARSSEKQALMSELKIMTHLGPHLNIVNLLGACTKSGPIYIITEYCFYGDLVNYLHKNRDSFLSHHPEKPKKELDIFGLNPADESTRSYVILSFENNGDYMDMKQADTTQYVPMLERKEVSKYSDIQRSLYDRPASYKKKSMLDSEVKNLLSDDNSEGLTLLDLLSFTYQVARGMEFLASKNCVHRDLAARNVLLAQGKIVKICDFGLARDIMHDSNYVSKGSTFLPVKWMAPESIFDNLYTTLSDVWSYGILLWEIFSLGGTPYPGMMVDSTFYNKIKSGYRMAKPDHATSEVYEIMVKCWNSEPEKRPSFYHLSEIVENLLPGQYKKSYEKIHLDFLKSDHPAVARMRVDSDNAYIGVTYKNEEDKLKDWEGGLDEQRLSADSGYIIPLPDIDPVPEEEDLGKRNRHSSQTSEESAIETGSSSSTFIKREDETIEDIDMMDDIGIDSSDLVEDSFL
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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 PDGFA, PDGFB and PDGFC and plays an essential role in the regulation of embryonic development, cell proliferation, survival and chemotaxis. Depending on the context, promotes or inhibits cell proliferation and cell migration. Plays an important role in the differentiation of bone marrow-derived mesenchymal stem cells. Required for normal skeleton development and cephalic closure during embryonic development. Required for normal development of the mucosa lining the gastrointestinal tract, and for recruitment of mesenchymal cells and normal development of intestinal villi. Plays a role in cell migration and chemotaxis in wound healing. Plays a role in platelet activation, secretion of agonists from platelet granules, and in thrombin-induced platelet aggregation. Binding of its cognate ligands - homodimeric PDGFA, homodimeric PDGFB, heterodimers formed by PDGFA and PDGFB or homodimeric PDGFC -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 PIK3R1, PLCG1, and PTPN11. 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. Phosphorylates PIK3R1, the regulatory subunit of phosphatidylinositol 3-kinase, and thereby mediates activation of the AKT1 signaling pathway. Mediates activation of HRAS and of the MAP kinases MAPK1/ERK2 and/or MAPK3/ERK1. Promotes activation of STAT family members STAT1, STAT3 and STAT5A and/or STAT5B. 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:
P16234

Secondarily ID:
B2RE69
E9PBH0
Q6P4H5
Q96KZ7
Q9UD28
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Ensembl ID
ENSG00000134853
HGNC ID
HGNC:8803
Subcellular Location
Cell membrane
Cell projection
Cilium
Golgi apparatus
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: CL000077 , Ba/F3
Compound ID Compound Name Compound Formula
CP0394288
N-[4-[[5-fluoro-7-(2-methoxyethoxy)quinazolin-4-yl]amino]phenyl]-2-(4-propan-2-yltriazol-1-yl)acetamide
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C24H26FN7O3
 2
1
GI50 = 1 nM
   TI
   LI
   LO
   TS
2
GI50 = 22 nM
   TI
   LI
   LO
   TS
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
GI50 = 1.7 nM
   TI
   LI
   LO
   TS
CP0441015
N-[4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl]-3-[[3-[(E)-2-pyridin-2-ylethenyl]-1H-indazol-6-yl]sulfanyl]propanamide
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C30H31F3N6OS
 1
1
GI50 = 2 nM
   TI
   LI
   LO
   TS
CP0899400
N-(4-((4-Methyl-3-((4-(pyridin-3-yl)pyrimidin-2-yl)amino)phenyl)carbamoyl)-2-(trifluoromethyl)benzyl)nicotinamide
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C31H24F3N7O2
 1
1
GI50 = 5 nM
   TI
   LI
   LO
   TS
CP0854605
3-Acrylamido-N-(4-methyl-3-((4-(pyridin-3-yl)pyrimidin-2-yl)amino)phenyl)benzamide
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C26H22N6O2
 1
1
GI50 = 8 nM
   TI
   LI
   LO
   TS
CP0410995
US10807985, Compound 44
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C26H27FN10
 2
1
GI50 = 10 nM
   TI
   LI
   LO
   TS
2
GI50 = 34 nM
   TI
   LI
   LO
   TS
CP0036099
1-[4-(3-amino-1H-indazol-4-yl)phenyl]-3-(2-fluoro-5-methyl-phenyl)urea
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C21H18FN5O
 2
1
GI50 = 10.4 nM
   TI
   LI
   LO
   TS
2
GI50 = 104.1 nM
   TI
   LI
   LO
   TS
CP0184289
1-(3-methyl-4-morpholin-4-ylphenyl)-3-[4-(3-methyl-2H-pyrazolo[3,4-b]pyridin-4-yl)phenyl]urea
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C25H26N6O2
 2
1
GI50 = 10.4 nM
   TI
   LI
   LO
   TS
2
GI50 = 134.8 nM
   TI
   LI
   LO
   TS
CP0203048
1-[4-(3-methyl-2H-pyrazolo[3,4-b]pyridin-4-yl)phenyl]-3-(3-phenylpropyl)urea
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C23H23N5O
 2
1
GI50 = 10.4 nM
   TI
   LI
   LO
   TS
2
GI50 = 2054 nM
   TI
   LI
   LO
   TS
CP0203090
1-hexyl-3-[4-(3-methyl-2H-pyrazolo[3,4-b]pyridin-4-yl)phenyl]urea
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C20H25N5O
 2
1
GI50 = 10.4 nM
   TI
   LI
   LO
   TS
2
GI50 = 3178 nM
   TI
   LI
   LO
   TS
CP0205730
1-[4-(3-methyl-2H-pyrazolo[3,4-b]pyridin-4-yl)phenyl]-3-quinolin-3-ylurea
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C23H18N6O
 2
1
GI50 = 10.4 nM
   TI
   LI
   LO
   TS
2
GI50 = 1513 nM
   TI
   LI
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   TS
CP0229003
1-(3-methylphenyl)-3-[4-(3-methyl-2H-pyrazolo[3,4-b]pyridin-4-yl)phenyl]urea
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C21H19N5O
 2
1
GI50 = 10.4 nM
   TI
   LI
   LO
   TS
2
GI50 = 1171 nM
   TI
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   TS
CP0368507
1-[4-[3-(hydroxymethyl)-2H-pyrazolo[3,4-b]pyridin-4-yl]phenyl]-3-(3-methylphenyl)urea
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C21H19N5O2
 2
1
GI50 = 10.4 nM
   TI
   LI
   LO
   TS
2
GI50 = 4996 nM
   TI
   LI
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   TS
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
GI50 = 10.7 nM
   TI
   LI
   LO
   TS
2
GI50 = 34 nM
   TI
   LI
   LO
   TS
3
GI50 = 46 nM
   TI
   LI
   LO
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4
GI50 = 567 nM
   TI
   LI
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   TS
5
GI50 > 10000 nM
   TI
   LI
   LO
   TS
CP0891169
4-((N-(2-(Dimethylamino)ethyl)acrylamido)methyl)-N-(4-methyl-3-((4-(pyridin-3-yl)pyrimidin-2-yl)amino)phenyl)benzamide
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C31H33N7O2
 1
1
GI50 = 11 nM
   TI
   LI
   LO
   TS
CP0190068
N-[4-methyl-3-[1-(6-methylpyridine-3-carbonyl)piperidin-4-yl]oxyphenyl]-4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)benzamide
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C33H38F3N5O3
 1
1
GI50 = 12 nM
   TI
   LI
   LO
   TS
CP0867480
N-(4-Methyl-3-((4-(pyridin-3-yl)pyrimidin-2-yl)amino)phenyl)-4-propionamidobenzamide
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C26H24N6O2
 1
1
GI50 = 12 nM
   TI
   LI
   LO
   TS
CP0854595
3-Acrylamido-N-(4-methyl-3-((4-(pyridin-3-yl)pyrimidin-2-yl)amino)phenyl)-5-(trifluoromethyl)benzamide
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C27H21F3N6O2
 1
1
GI50 = 13 nM
   TI
   LI
   LO
   TS
CP0860664
N-(4-Methyl-3-((4-(pyridin-3-yl)pyrimidin-2-yl)amino)phenyl)-4-(vinylsulfonamidomethyl)benzamide
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C26H24N6O3S
 1
1
GI50 = 13 nM
   TI
   LI
   LO
   TS
CP0891179
N-(4-((4-Methyl-3-((4-(pyridin-3-yl)pyrimidin-2-yl)amino)phenyl)carbamoyl)phenyl)nicotinamide
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C29H23N7O2
 1
1
GI50 = 13 nM
   TI
   LI
   LO
   TS
CP0226713
1-cyclopentyl-3-[4-(3-methyl-2H-pyrazolo[3,4-b]pyridin-4-yl)phenyl]urea
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C19H21N5O
 2
1
GI50 = 13.3 nM
   TI
   LI
   LO
   TS
2
GI50 > 10000 nM
   TI
   LI
   LO
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CP0875440
N-(4-methyl-3-((4-(pyridin-3-yl)pyrimidin-2-yl)amino)phenyl)-4-(propionamidomethyl)benzamide
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C27H26N6O2
 1
1
GI50 = 14 nM
   TI
   LI
   LO
   TS
CP0902838
N-(4-((4-Methyl-3-((4-(pyridin-3-yl)pyrimidin-2-yl)amino)phenyl)carbamoyl)benzyl)nicotinamide
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C30H25N7O2
 1
1
GI50 = 14 nM
   TI
   LI
   LO
   TS
CP0948271
N-(4-Methyl-3-((4-(pyridin-3-yl)pyrimidin-2-yl)amino)phenyl)-3-(propionamidomethyl)benzamide
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C27H26N6O2
 1
1
GI50 = 15 nM
   TI
   LI
   LO
   TS
CP0891184
4-((N-(2-(Dimethylamino)ethyl)pivalamido)methyl)-N-(4-methyl-3-((4-(pyridin-3-yl)pyrimidin-2-yl)amino)phenyl)benzamide
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C33H39N7O2
 1
1
GI50 = 17 nM
   TI
   LI
   LO
   TS
CP0864071
4-((N-Isopentylacrylamido)methyl)-N-(4-methyl-3-((4-(pyridin-3-yl)pyrimidin-2-yl)amino)phenyl)benzamide
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C32H34N6O2
 1
1
GI50 = 19 nM
   TI
   LI
   LO
   TS
CP0883780
4-(((2-(Dimethylamino)ethyl)amino)methyl)-N-(4-methyl-3-((4-(pyridin-3-yl)pyrimidin-2-yl)amino)phenyl)benzamide
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C28H31N7O
 1
1
GI50 = 24 nM
   TI
   LI
   LO
   TS
CP0941817
4-((N-(2-(Dimethylamino)ethyl)butyramido)methyl)-N-(4-methyl-3-((4-(pyridin-3-yl)pyrimidin-2-yl)amino)phenyl)benzamide
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C32H37N7O2
 1
1
GI50 = 25 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
 2
1
GI50 = 30 nM
   TI
   LI
   LO
   TS
2
GI50 = 631 nM
   TI
   LI
   LO
   TS
CP0906649
N-(2-(Diethylamino)ethyl)-N-(4-((4-methyl-3-((4-(pyridin-3-yl)pyrimidin-2-yl)amino)phenyl)carbamoyl)benzyl)nicotinamide
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C36H38N8O2
 1
1
GI50 = 33 nM
   TI
   LI
   LO
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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
 2
1
GI50 = 34 nM
   TI
   LI
   LO
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2
GI50 > 10000 nM
   TI
   LI
   LO
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CP0218115
US8586600, II-6
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C27H24N6O2
 1
1
GI50 = 34 nM
   TI
   LI
   LO
   TS
CP0942328
4-((N-(2-(Dimethylamino)ethyl)propionamido)methyl)-N-(4-methyl-3-((4-(pyridin-3-yl)pyrimidin-2-yl)amino)phenyl)benzamide
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C31H35N7O2
 1
1
GI50 = 36 nM
   TI
   LI
   LO
   TS
CP0875470
N-(4-((4-Methyl-3-((4-(pyridin-3-yl)pyrimidin-2-yl)amino)phenyl)carbamoyl)benzyl)-N-(2-(pyrrolidin-1-yl)ethyl)nicotinamide
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C36H36N8O2
 1
1
GI50 = 39 nM
   TI
   LI
   LO
   TS
CP0899401
N-(4-Methyl-3-((4-(pyridin-3-yl)pyrimidin-2-yl)amino)phenyl)-3-propionamido-5-(trifluoromethyl)benzamide
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C27H23F3N6O2
 1
1
GI50 = 39 nM
   TI
   LI
   LO
   TS
CP0911799
4-((N-(2-(Dimethylamino)ethyl)isobutyramido)methyl)-N-(4-methyl-3-((4-(pyridin-3-yl)pyrimidin-2-yl)amino)phenyl)benzamide
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C32H37N7O2
 1
1
GI50 = 39 nM
   TI
   LI
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   TS
CP0851621
Ripretinib
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C24H21BrFN5O2
 2
1
GI50 = 40 nM
   TI
   LI
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2
GI50 = 188 nM
   TI
   LI
   LO
   TS
CP0064831
US8586600, II-1
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C26H22N6O2
 1
1
GI50 = 44 nM
   TI
   LI
   LO
   TS
CP0387299
4-(methylamino)-2-[4-methyl-3-(propanoylamino)anilino]-N-[2-methyl-5-[[3-(trifluoromethyl)benzoyl]amino]phenyl]pyrimidine-5-carboxamide
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C31H30F3N7O3
 1
1
GI50 = 45 nM
   TI
   LI
   LO
   TS
CP0043225
4-[4-[[4-chloro-3-(trifluoromethyl)phenyl]carbamoylamino]-3-fluorophenoxy]-N-methylpyridine-2-carboxamide
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C21H15ClF4N4O3
 2
1
GI50 = 51 nM
   TI
   LI
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2
GI50 = 522 nM
   TI
   LI
   LO
   TS
CP0891178
(E)-4-((N-(2-(Dimethylamino)ethyl)but-2-enamido)methyl)-N-(4-methyl-3-((4-(pyridin-3-yl)pyrimidin-2-yl)amino)phenyl)benzamide
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C32H35N7O2
 1
1
GI50 = 54 nM
   TI
   LI
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   TS
CP0887639
N-(2-(Dimethylamino)ethyl)-N-(4-((4-methyl-3-((4-(pyridin-3-yl)pyrimidin-2-yl)amino)phenyl)carbamoyl)benzyl)thiophene-2-carboxamide
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C33H33N7O2S
 1
1
GI50 = 56 nM
   TI
   LI
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   TS
CP0906653
4-(Acrylamidomethyl)-N-(4-methyl-3-((4-(pyridin-3-yl)pyrimidin-2-yl)amino)phenyl)-3-(trifluoromethyl)benzamide
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C28H23F3N6O2
 1
1
GI50 = 59 nM
   TI
   LI
   LO
   TS
CP0389976
4-(methylamino)-2-[4-methyl-3-(prop-2-enoylamino)anilino]-N-[2-methyl-5-[[3-(trifluoromethyl)benzoyl]amino]phenyl]pyrimidine-5-carboxamide
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C31H28F3N7O3
 1
1
GI50 = 99 nM
   TI
   LI
   LO
   TS
CP0955464
N-(2-(Dimethylamino)ethyl)-4-methyl-N-(4-((4-methyl-3-((4-(pyridin-3-yl)pyrimidin-2-yl)amino)phenyl)carbamoyl)benzyl)benzamide
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C36H37N7O2
 1
1
GI50 = 100 nM
   TI
   LI
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   TS
CP0911792
4-((N-(2-(Dimethylamino)ethyl)cyclopropanecarboxamido)methyl)-N-(4-methyl-3-((4-(pyridin-3-yl)pyrimidin-2-yl)amino)phenyl)benzamide
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C32H35N7O2
 1
1
GI50 = 112 nM
   TI
   LI
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   TS
CP0874420
4-((2-(Dimethylamino)-N-(2-(dimethylamino)ethyl)acetamido)methyl)-N-(4-methyl-3-((4-(pyridin-3-yl)pyrimidin-2-yl)amino)phenyl)benzamide
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C32H38N8O2
 1
1
GI50 = 120 nM
   TI
   LI
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   TS
CP0899397
3-(Acrylamidomethyl)-N-(4-methyl-3-((4-(pyridin-3-yl)pyrimidin-2-yl)amino)phenyl)benzamide
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C27H24N6O2
 1
1
GI50 = 160 nM
   TI
   LI
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   TS
CP0867482
N-(2-(Dimethylamino)ethyl)-N-(4-((4-methyl-3-((4-(pyridin-3-yl)pyrimidin-2-yl)amino)phenyl)carbamoyl)benzyl)isoxazole-5-carboxamide
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C32H32N8O3
 1
1
GI50 = 166 nM
   TI
   LI
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   TS
CP0228997
1-(2-fluoro-5-methylphenyl)-3-[4-(3-methyl-6-oxo-2,7-dihydropyrazolo[3,4-b]pyridin-4-yl)phenyl]urea
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C21H18FN5O2
 2
1
GI50 = 204.5 nM
   TI
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2
GI50 > 10000 nM
   TI
   LI
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CP0953406
4-((N-(2-(Diethylamino)ethyl)acrylamido)methyl)-N-(4-methyl-3-((4-(pyridin-3-yl)pyrimidin-2-yl)amino)phenyl)benzamide
   Show/Hide
C33H37N7O2
 1
1
GI50 = 344 nM
   TI
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   TS
CP0867481
N-(2-Hydroxyethyl)-N-(4-((4-methyl-3-((4-(pyridin-3-yl)pyrimidin-2-yl)amino)phenyl)carbamoyl)benzyl)nicotinamide
   Show/Hide
C32H29N7O3
 1
1
GI50 = 353 nM
   TI
   LI
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   TS
CP0899399
4-((2-(Dimethylamino)-N-(2-hydroxyethyl)acetamido)methyl)-N-(4-methyl-3-((4-(pyridin-3-yl)pyrimidin-2-yl)amino)phenyl)benzamide
   Show/Hide
C30H33N7O3
 1
1
GI50 = 363 nM
   TI
   LI
   LO
   TS
CP0387298
4-(methylamino)-2-[4-methyl-3-(propanoylamino)anilino]-N-[2-methyl-5-[(3,4,5-trimethoxybenzoyl)amino]phenyl]pyrimidine-5-carboxamide
   Show/Hide
C33H37N7O6
 1
1
GI50 = 370 nM
   TI
   LI
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   TS
CP0226718
1-(3-methylphenyl)-3-[4-[3-(trifluoromethyl)-2H-pyrazolo[3,4-b]pyridin-4-yl]phenyl]urea
   Show/Hide
C21H16F3N5O
 2
1
GI50 = 465.2 nM
   TI
   LI
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   TS
2
GI50 > 10000 nM
   TI
   LI
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   TS
CP0224766
4-(methylamino)-2-[4-methyl-3-(prop-2-enoylamino)anilino]-N-[2-methyl-5-[(3,4,5-trimethoxybenzoyl)amino]phenyl]pyrimidine-5-carboxamide
   Show/Hide
C33H35N7O6
 1
1
GI50 = 670 nM
   TI
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CP0326453
1-(2-fluoro-5-methylphenyl)-3-[4-(3-methyl-6-oxo-2,4,5,7-tetrahydropyrazolo[3,4-b]pyridin-4-yl)phenyl]urea
   Show/Hide
C21H20FN5O2
 2
1
GI50 = 4254 nM
   TI
   LI
   LO
   TS
2
GI50 > 10000 nM
   TI
   LI
   LO
   TS
CP0388615
3-(3,4-dimethoxyphenyl)-5-(1-methylpiperidin-4-yl)oxy-6-(1,3-thiazol-2-yl)pyrazolo[1,5-a]pyrimidin-7-amine
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C23H26N6O3S
 1
1
IC50 = 9 nM
   TI
   LI
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CP0388620
methyl N-[4-[7-amino-3-(3,4-dimethoxyphenyl)-5-(1-methylpiperidin-4-yl)oxypyrazolo[1,5-a]pyrimidin-6-yl]phenyl]carbamate
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C28H32N6O5
 1
1
IC50 = 17 nM
   TI
   LI
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   TS
CP0388616
3-(3,4-dimethoxyphenyl)-5-(1-methylpiperidin-4-yl)oxy-6-phenylpyrazolo[1,5-a]pyrimidin-7-amine
   Show/Hide
C26H29N5O3
 1
1
IC50 = 93 nM
   TI
   LI
   LO
   TS
CP0061016
3-(4-Amino-7-cyclopentyl-7H-pyrrolo[2,3-d]pyrimidin-5-yl)-phenol
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C17H18N4O
 1
1
IC50 = 180 nM
   TI
   LI
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CP0418567
3-[4-amino-7-[3-(hydroxymethyl)cyclobutyl]pyrrolo[2,3-d]pyrimidin-5-yl]phenol
   Show/Hide
C17H18N4O2
 1
1
IC50 = 340 nM
   TI
   LI
   LO
   TS
CP0661487
3-(2,6-Dichloro-3,5-dimethoxy-phenyl)-1-{6-[4-(4-ethyl-piperazin-1-yl)-phenylamino]-pyrimidin-4-yl}-1-methyl-urea monophosphate
   Show/Hide
C26H34Cl2N7O7P
 1
1
IC50 = 2718 nM
   TI
   LI
   LO
   TS
CP0138866
1-[4-[3-[4-amino-5-(2-fluoro-5-hydroxyphenyl)pyrrolo[2,3-d]pyrimidin-7-yl]cyclobutyl]piperazin-1-yl]ethanone
   Show/Hide
C22H25FN6O2
 1
1
IC50 > 10000 nM
   TI
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   TS
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0002778
4-[(4-methylpiperazin-1-yl)methyl]-N-[4-methyl-3-[(4-pyridin-3-ylpyrimidin-2-yl)amino]phenyl]benzamide
   Show/Hide
C29H31N7O
 7
1 EC50 = 90 nM
2 IC50 = 1.995 nM
3 IC50 = 4.6 nM
4 IC50 = 18 nM
5 IC50 = 71 nM
6 IC50 = 160 nM
7 Kd = 31 nM
CP0690323
N-(benzo[d][1,3]dioxol-5-ylmethyl)-4-(6,7-dimethoxy-9H-pyrimido[4,5-b]indol-4-yl)piperazine-1-carbothioamide
   Show/Hide
C25H26N6O4S
 1
1 EC50 = 428.75 nM
CP0639448
Imatinib mesilate
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C30H35N7O4S
 1
1 EC50 = 680.24 nM
CP0085333
Amuvatinib
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C23H21N5O3S
 1
1 EC50 = 27163 nM
CP0002230
4-methyl-N-[3-(4-methyl-1H-imidazol-1-yl)-5-(trifluoromethyl)phenyl]-3-[(4-pyridin-3-ylpyrimidin-2-yl)amino]benzamide
   Show/Hide
C28H22F3N7O
 3
1 IC50 < 2.54 nM
2 Kd = 74 nM
3 Kd = 180 nM
CP0002211
N-[2-(diethylamino)ethyl]-5-[(Z)-(5-fluoro-2-oxo-1H-indol-3-ylidene)methyl]-2,4-dimethyl-1H-pyrrole-3-carboxamide
   Show/Hide
C22H27FN4O2
 4
1 IC50 = 6.9 nM
2 IC50 = 27.3 nM
3 IC50 = 130 nM
4 Kd = 0.79 nM
CP0184289
1-(3-methyl-4-morpholin-4-ylphenyl)-3-[4-(3-methyl-2H-pyrazolo[3,4-b]pyridin-4-yl)phenyl]urea
   Show/Hide
C25H26N6O2
 1
1 IC50 = 7.2 nM
CP0036099
1-[4-(3-amino-1H-indazol-4-yl)phenyl]-3-(2-fluoro-5-methyl-phenyl)urea
   Show/Hide
C21H18FN5O
 2
1 IC50 = 15 nM
2 Kd = 4.2 nM
CP0205730
1-[4-(3-methyl-2H-pyrazolo[3,4-b]pyridin-4-yl)phenyl]-3-quinolin-3-ylurea
   Show/Hide
C23H18N6O
 1
1 IC50 = 22 nM
CP0203048
1-[4-(3-methyl-2H-pyrazolo[3,4-b]pyridin-4-yl)phenyl]-3-(3-phenylpropyl)urea
   Show/Hide
C23H23N5O
 1
1 IC50 = 24 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
   Show/Hide
C25H27N7OS
 1
1 IC50 = 24.2 nM
CP0203090
1-hexyl-3-[4-(3-methyl-2H-pyrazolo[3,4-b]pyridin-4-yl)phenyl]urea
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C20H25N5O
 1
1 IC50 = 27 nM
CP0218115
US8586600, II-6
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C27H24N6O2
 1
1 IC50 = 29.8 nM
CP0229003
1-(3-methylphenyl)-3-[4-(3-methyl-2H-pyrazolo[3,4-b]pyridin-4-yl)phenyl]urea
   Show/Hide
C21H19N5O
 1
1 IC50 = 40 nM
CP0030740
1-(5-Tert-Butyl-1,2-Oxazol-3-Yl)-3-(4-{7-[2-(Morpholin-4-Yl)ethoxy]imidazo[2,1-B][1,3]benzothiazol-2-Yl}phenyl)urea
   Show/Hide
C29H32N6O4S
 3
1 IC50 = 42 nM
2 Kd = 1.6 nM
3 Kd = 11 nM
CP0368507
1-[4-[3-(hydroxymethyl)-2H-pyrazolo[3,4-b]pyridin-4-yl]phenyl]-3-(3-methylphenyl)urea
   Show/Hide
C21H19N5O2
 1
1 IC50 = 87 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
   Show/Hide
C34H34N8O2
 1
1 IC50 = 132 nM
CP0064831
US8586600, II-1
   Show/Hide
C26H22N6O2
 1
1 IC50 = 172.94 nM
CP0006232
4-(6,7-Dimethoxy-quinazolin-4-yl)-piperazine-1-carbothioic acid (benzo[1,3]dioxol-5-ylmethyl)-amide
   Show/Hide
C23H25N5O4S
 1
1 IC50 = 210 nM
CP0226713
1-cyclopentyl-3-[4-(3-methyl-2H-pyrazolo[3,4-b]pyridin-4-yl)phenyl]urea
   Show/Hide
C19H21N5O
 1
1 IC50 = 576 nM
CP0228997
1-(2-fluoro-5-methylphenyl)-3-[4-(3-methyl-6-oxo-2,7-dihydropyrazolo[3,4-b]pyridin-4-yl)phenyl]urea
   Show/Hide
C21H18FN5O2
 1
1 IC50 = 1179 nM
CP0226718
1-(3-methylphenyl)-3-[4-[3-(trifluoromethyl)-2H-pyrazolo[3,4-b]pyridin-4-yl]phenyl]urea
   Show/Hide
C21H16F3N5O
 1
1 IC50 > 5000 nM
CP0661487
3-(2,6-Dichloro-3,5-dimethoxy-phenyl)-1-{6-[4-(4-ethyl-piperazin-1-yl)-phenylamino]-pyrimidin-4-yl}-1-methyl-urea monophosphate
   Show/Hide
C26H34Cl2N7O7P
 1
1 IC50 > 10000 nM
CP0326453
1-(2-fluoro-5-methylphenyl)-3-[4-(3-methyl-6-oxo-2,4,5,7-tetrahydropyrazolo[3,4-b]pyridin-4-yl)phenyl]urea
   Show/Hide
C21H20FN5O2
 1
1 IC50 > 50000 nM
CP0037987
N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)quinazolin-4-amine
   Show/Hide
C22H23N3O4
 1
1 Kd = 1800 nM
CP0007142
N-[3-chloro-4-[(3-fluorophenyl)methoxy]phenyl]-6-[5-[(2-methylsulfonylethylamino)methyl]furan-2-yl]quinazolin-4-amine
   Show/Hide
C29H26ClFN4O4S
 1
1 Kd > 10000 nM
Clinical Information about the Protein
Target 1 ( Platelet-derived growth factor receptor alpha (PDGFRA) )
Target Type Successful Target
Disease 5 Target-related Diseases  5
1 Thrombocytopenia [ICD-11: 3B64]
2 Gastrointestinal cancer [ICD-11: 2C11]
3 Solid tumour/cancer [ICD-11: 2A00-2F9Z]
4 Gastrointestinal stromal tumour [ICD-11: 2B5B]
5 Gram-positive bacterial infection [ICD-11: 1B74-1G40]
Approved Drug(s) 3 Approved Drugs  3
1 Romiplostim Approved
Thrombocytopenia
2 Avapritinib Approved
Gastrointestinal stromal tumour
3 Ripretinib Approved
Gastrointestinal stromal tumour
Clinical Trial Drug(s) 4 Clinical Trial Drugs  4
1 CP-868596 Phase 3
Gastrointestinal cancer
2 E-3810 Phase 3
Solid tumour/cancer
3 Famitinib Phase 2
Solid tumour/cancer
4 MP470 Phase 2
Solid tumour/cancer
Investigative Drug(s) 1 Investigative Drug  1
1 HKI-9924129 Investigative
Gram-positive bacterial infection