General Information of the Protein
Protein ID
PT01867
Protein Name
TGF-beta receptor type-2
Secondarily
Protein Name
TGF-beta type II receptor
Transforming growth factor-beta receptor type II
Gene Name
TGFBR2
Sequence
MGRGLLRGLWPLHIVLWTRIASTIPPHVQKSVNNDMIVTDNNGAVKFPQLCKFCDVRFSTCDNQKSCMSNCSITSICEKPQEVCVAVWRKNDENITLETVCHDPKLPYHDFILEDAASPKCIMKEKKKPGETFFMCSCSSDECNDNIIFSEEYNTSNPDLLLVIFQVTGISLLPPLGVAISVIIIFYCYRVNRQQKLSSTWETGKTRKLMEFSEHCAIILEDDRSDISSTCANNINHNTELLPIELDTLVGKGRFAEVYKAKLKQNTSEQFETVAVKIFPYEEYASWKTEKDIFSDINLKHENILQFLTAEERKTELGKQYWLITAFHAKGNLQEYLTRHVISWEDLRKLGSSLARGIAHLHSDHTPCGRPKMPIVHRDLKSSNILVKNDLTCCLCDFGLSLRLDPTLSVDDLANSGQVGTARYMAPEVLESRMNLENVESFKQTDVYSMALVLWEMTSRCNAVGEVKDYEPPFGSKVREHPCVESMKDNVLRDRGRPEIPSFWLNHQGIQMVCETLTECWDHDPEARLTAQCVAERFSELEHLDRLSGRSCSEEKIPEDGSLNTTK
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Organism
Homo sapiens, Human
Protein Classification
Enzyme
>
Kinase
>
Protein Kinase
>
TKL protein kinase group
>
TKL protein kinase STKR family
>
TKL protein kinase STKR Type 2 subfamily
Function
Transmembrane serine/threonine kinase forming with the TGF-beta type I serine/threonine kinase receptor, TGFBR1, the non-promiscuous receptor for the TGF-beta cytokines TGFB1, TGFB2 and TGFB3. Transduces the TGFB1, TGFB2 and TGFB3 signal from the cell surface to the cytoplasm and thus regulates a plethora of physiological and pathological processes including cell cycle arrest in epithelial and hematopoietic cells, control of mesenchymal cell proliferation and differentiation, wound healing, extracellular matrix production, immunosuppression and carcinogenesis. The formation of the receptor complex composed of 2 TGFBR1 and 2 TGFBR2 molecules symmetrically bound to the cytokine dimer results in the phosphorylation and activation of TGFBR1 by the constitutively active TGFBR2. Activated TGFBR1 phosphorylates SMAD2 which dissociates from the receptor and interacts with SMAD4. The SMAD2-SMAD4 complex is subsequently translocated to the nucleus where it modulates the transcription of the TGF-beta-regulated genes. This constitutes the canonical SMAD-dependent TGF-beta signaling cascade. Also involved in non-canonical, SMAD-independent TGF-beta signaling pathways.
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Uniprot ID
Primary ID:
P37173

Secondarily ID:
B4DTV5
Q15580
Q6DKT6
Q99474
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HGNC ID
HGNC:11773
Subcellular Location
Cell membrane
Membrane raft
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: CL000025 , HEK-293T
 Cell Line Info 
Compound ID Compound Name Compound Formula
CP0036041
 Compound Info 
4-(4-(benzo[d][1,3]dioxol-5-yl)-5-(pyridin-2-yl)-1H-imidazol-2-yl)benzamide
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C22H16N4O3
  1
1
IC50 = 66 nM
 Bioactivity Info 
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CP0885517
 Compound Info 
rac-Ethyl 4-(4-tert-Butylphenyl)-2-methyl-5-oxo-7-(n-propyl)-1,4,5,6,7,8-hexahydroquinoline-3-carboxylate
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C26H35NO3
  1
1
IC50 = 170 nM
 Bioactivity Info 
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CP0888623
 Compound Info 
rac-Isobutyl 4-(4-tert-Butylphenyl)-2-methyl-5-oxo-7-(n-propyl)-1,4,5,6,7,8-hexahydroquinoline-3-carboxylate
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C28H39NO3
  1
1
IC50 = 170 nM
 Bioactivity Info 
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CP0918260
 Compound Info 
rac-Isobutyl 4-(Biphenyl-4-yl)-2,7,7-trimethyl-5-oxo-1,4,5,6,7,8-hexahydroquinoline-3-carboxylate
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C29H33NO3
  1
1
IC50 = 530 nM
 Bioactivity Info 
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CP0905445
 Compound Info 
rac-Methyl 4-(4-tert-Butylphenyl)-2,7,7-trimethyl-5-oxo-1,4,5,6,7,8-hexahydroquinoline-3-carboxylate
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C24H31NO3
  1
1
IC50 = 560 nM
 Bioactivity Info 
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CP0852407
 Compound Info 
rac-Methyl 4-(4-Cyclohexylphenyl)-2,7,7-trimethyl-5-oxo-1,4,5,6,7,8-hexahydroquinoline-3-carboxylate
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C26H33NO3
  1
1
IC50 = 590 nM
 Bioactivity Info 
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CP0902350
 Compound Info 
rac-Methyl 4-(Biphenyl-4-yl)-7-isobutyl-2-methyl-5-oxo-1,4,5,6,7,8-hexahydroquinoline-3-carboxylate
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C28H31NO3
  1
1
IC50 = 590 nM
 Bioactivity Info 
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CP0865574
 Compound Info 
rac-Methyl 2,7,7-Trimethyl-5-oxo-4-(4'-(trifluoromethyl)biphenyl-4-yl)-1,4,5,6,7,8-hexahydroquinoline-3-carboxylate
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C27H26F3NO3
  1
1
IC50 = 730 nM
 Bioactivity Info 
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CP0885521
 Compound Info 
rac-2,2,2-Trifluoroethyl 4-(Biphenyl-4-yl)-2,7,7-trimethyl-5-oxo-1,4,5,6,7,8-hexahydroquinoline-3-carboxylate
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C27H26F3NO3
  1
1
IC50 = 760 nM
 Bioactivity Info 
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CP0866033
 Compound Info 
rac-Methyl 4-(Biphenyl-4-yl)-7-ethyl-2-methyl-5-oxo-1,4,5,6,7,8-hexahydroquinoline-3-carboxylate
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C26H27NO3
  1
1
IC50 = 790 nM
 Bioactivity Info 
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CP0885522
 Compound Info 
rac-Ethyl 4-(Biphenyl-4-yl)-7,7-dimethyl-5-oxo-2-(n-propyl)-1,4,5,6,7,8-hexahydroquinoline-3-carboxylate
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C29H33NO3
  1
1
IC50 = 830 nM
 Bioactivity Info 
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CP0889540
 Compound Info 
rac-4-Methoxybenzyl 4-(Biphenyl-4-yl)-2,7,7-trimethyl-5-oxo-1,4,5,6,7,8-hexahydroquinoline-3-carboxylate
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C33H33NO4
  1
1
IC50 = 830 nM
 Bioactivity Info 
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CP0891186
 Compound Info 
rac-Methyl 2,7,7-Trimethyl-4-(4'-methylbiphenyl-4-yl)-5-oxo-1,4,5,6,7,8-hexahydroquinoline-3-carboxylate
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C27H29NO3
  1
1
IC50 = 860 nM
 Bioactivity Info 
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CP0891185
 Compound Info 
rac-Methyl 2,7,7-Trimethyl-4-(2'-methylbiphenyl-4-yl)-5-oxo-1,4,5,6,7,8-hexahydroquinoline-3-carboxylate
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C27H29NO3
  1
1
IC50 = 890 nM
 Bioactivity Info 
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CP0902349
 Compound Info 
rac-Methyl 4-(Biphenyl-4-yl)-7-isopropyl-2-methyl-5-oxo-1,4,5,6,7,8-hexahydroquinoline-3-carboxylate
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C27H29NO3
  1
1
IC50 = 940 nM
 Bioactivity Info 
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CP0865571
 Compound Info 
rac-Methyl 4-(4'-(Methoxycarbonyl)biphenyl-4-yl)-2,7,7-trimethyl-5-oxo-1,4,5,6,7,8-hexahydroquinoline-3-carboxylate
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C28H29NO5
  1
1
IC50 = 1350 nM
 Bioactivity Info 
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CP0885523
 Compound Info 
rac-Isopentyl 4-(Biphenyl-4-yl)-2,7,7-trimethyl-5-oxo-1,4,5,6,7,8-hexahydroquinoline-3-carboxylate
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C30H35NO3
  1
1
IC50 = 1460 nM
 Bioactivity Info 
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CP0906851
 Compound Info 
rac-Methyl 4-(Biphenyl-4-yl)-2,7,7-trimethyl-5-oxo-1,4,5,6,7,8-hexahydroquinoline-3-carboxylate
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C26H27NO3
  1
1
IC50 = 1490 nM
 Bioactivity Info 
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CP0906849
 Compound Info 
rac-Methyl 4-(3'-Chlorobiphenyl-4-yl)-2,7,7-trimethyl-5-oxo-1,4,5,6,7,8-hexahydroquinoline-3-carboxylate
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C26H26ClNO3
  1
1
IC50 = 1520 nM
 Bioactivity Info 
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CP0891187
 Compound Info 
rac-Methyl 4-(2-Fluorobiphenyl-4-yl)-2,7,7-trimethyl-5-oxo-1,4,5,6,7,8-hexahydroquinoline-3-carboxylate
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C26H26FNO3
  1
1
IC50 = 1840 nM
 Bioactivity Info 
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CP0885519
 Compound Info 
rac-Methyl 4-(Biphenyl-4-yl)-2-methyl-5-oxo-7-phenyl-1,4,5,6,7,8-hexahydroquinoline-3-carboxylate
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C30H27NO3
  1
1
IC50 = 1920 nM
 Bioactivity Info 
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CP0882252
 Compound Info 
rac-Methyl 4-(2'-Fluorobiphenyl-4-yl)-2,7,7-trimethyl-5-oxo-1,4,5,6,7,8-hexahydroquinoline-3-carboxylate
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C26H26FNO3
  1
1
IC50 = 2060 nM
 Bioactivity Info 
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CP0889539
 Compound Info 
rac-Methyl 4-(Biphenyl-4-yl)-2,7-dimethyl-5-oxo-1,4,5,6,7,8-hexahydroquinoline-3-carboxylate
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C25H25NO3
  1
1
IC50 = 2730 nM
 Bioactivity Info 
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CP0905444
 Compound Info 
rac-Ethyl 2-Ethyl-7,7-dimethyl-5-oxo-4-(4-(pyridin-2-yl)phenyl)-1,4,5,6,7,8-hexahydroquinoline-3-carboxylate
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C27H30N2O3
  1
1
IC50 = 3570 nM
 Bioactivity Info 
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CP0902348
 Compound Info 
rac-Methyl 4-(Biphenyl-4-yl)-7-(4-(dimethylamino)phenyl)-2-methyl-5-oxo-1,4,5,6,7,8-hexahydroquinoline-3-carboxylate
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C32H32N2O3
  1
1
IC50 = 3970 nM
 Bioactivity Info 
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CP0911676
 Compound Info 
rac-Methyl 4-(4-(1H-Indol-5-yl)phenyl)-2,7,7-trimethyl-5-oxo-1,4,5,6,7,8-hexahydroquinoline-3-carboxylate
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C28H28N2O3
  1
1
IC50 = 4050 nM
 Bioactivity Info 
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CP0916711
 Compound Info 
rac-4-(Biphenyl-4-yl)-N-(4-methoxybenzyl)-2,7,7-trimethyl-5-oxo-1,4,5,6,7,8-hexahydroquinoline-3-carboxamide
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C33H34N2O3
  1
1
IC50 = 4060 nM
 Bioactivity Info 
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CP0906850
 Compound Info 
rac-Methyl 4-(4-(1H-Pyrazol-1-yl)phenyl)-2,7,7-trimethyl-5-oxo-1,4,5,6,7,8-hexahydroquinoline-3-carboxylate
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C23H25N3O3
  1
1
IC50 = 8800 nM
 Bioactivity Info 
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CP0856420
 Compound Info 
rac-Methyl 4-(4'-Methoxybiphenyl-3-yl)-2,7,7-trimethyl-5-oxo-1,4,5,6,7,8-hexahydroquinoline-3-carboxylate
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C27H29NO4
  1
1
IC50 > 10000 nM
 Bioactivity Info 
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CP0865572
 Compound Info 
rac-Methyl 2,7,7-Trimethyl-5-oxo-4-(3-(pyridin-3-yl)phenyl)-1,4,5,6,7,8-hexahydroquinoline-3-carboxylate
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C25H26N2O3
  1
1
IC50 > 10000 nM
 Bioactivity Info 
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CP0889541
 Compound Info 
rac-Methyl 4-(3'-Chlorobiphenyl-3-yl)-2,7,7-trimethyl-5-oxo-1,4,5,6,7,8-hexahydroquinoline-3-carboxylate
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C26H26ClNO3
  1
1
IC50 > 10000 nM
 Bioactivity Info 
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CP0902351
 Compound Info 
rac-Methyl 4-(Biphenyl-3-yl)-2,7,7-trimethyl-5-oxo-1,4,5,6,7,8-hexahydroquinoline-3-carboxylate
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C26H27NO3
  1
1
IC50 > 10000 nM
 Bioactivity Info 
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CP0911565
 Compound Info 
rac-Methyl 4-(4-Fluorophenyl)-2,7,7-trimethyl-5-oxo-1,4,5,6,7,8-hexahydroquinoline-3-carboxylate
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C20H22FNO3
  1
1
IC50 > 10000 nM
 Bioactivity Info 
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CP0911677
 Compound Info 
rac-Methyl 2,7,7-Trimethyl-5-oxo-4-phenyl-1,4,5,6,7,8-hexahydroquinoline-3-carboxylate
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C20H23NO3
  1
1
IC50 > 10000 nM
 Bioactivity Info 
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CP0917613
 Compound Info 
rac-4-(Biphenyl-4-yl)-2,7,7-trimethyl-5-oxo-1,4,5,6,7,8-hexahydroquinoline-3-carboxylic Acid
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C25H25NO3
  1
1
IC50 > 10000 nM
 Bioactivity Info 
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Cell Line ID: CL000013 , Sf9
 Cell Line Info 
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0036041
 Compound Info 
4-(4-(benzo[d][1,3]dioxol-5-yl)-5-(pyridin-2-yl)-1H-imidazol-2-yl)benzamide
   Show/Hide
C22H16N4O3
  1
1 Kd > 10000 nM
Clinical Information about the Protein
Target 1 ( TGF-beta receptor type II (TGFBR2) )
Target Type Clinical trial Target