Co-Target(s) Information

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Target General Information
Co-Targets of This Target
References
Target General Information  Top
Target ID T53389 Target Info
Target Name TGF-beta receptor type I (TGFBR1)
Synonyms
Type I TGFbeta receptor kinase; Transforming growth factor-beta receptor type I; TbetaRI; TbetaR-I; TGFR-1; TGF-beta type I receptor; TGF-beta receptor type-1; Serine/threonine-protein kinase receptor R4; SKR4; Activin receptor-like kinase 5; Activin A receptor type II-like protein kinase of 53kD; ALK5; ALK-5
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Target Type Clinical trial Target
Gene Name TGFBR1
Biochemical Class Kinase
UniProt ID
TGFR1_HUMAN
Co-Targets of This Target  Top
Co-Target Name Vascular endothelial growth factor receptor 2 (KDR) Successful Target
UniProt ID VGFR2_HUMAN
Gene Name KDR
Synonyms
VEGFR2; VEGFR-2; VEGF-2 receptor; Protein-tyrosine kinase receptor flk-1; Kinase insert domain receptor; Fetal liver kinase 1; FLK1; FLK-1; CD309
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Representative Drug(s) TEW-7197 Drug Info IC50 = 97 nM Click to Show More [1]
2 LY2157299 Drug Info IC50 = 442 nM [1]
Co-Target Name Stress-activated protein kinase 2a (p38 alpha) Clinical trial Target
UniProt ID MK14_HUMAN
Gene Name MAPK14
Synonyms
SAPK2A; P38 mitogen activatedprotein kinase; P38 Mitogen-activatedprotein kinase alpha; Mitogen-activated protein kinase p38 alpha; Mitogen-activated protein kinase 14; MXI2; MAX-interacting protein 2; MAPK 14; MAP kinase p38alpha; MAP kinase p38 alpha; MAP kinase MXI2; MAP kinase 14; Cytokine suppressive anti-inflammatory drug-binding protein; Cytokine suppressive anti-inflammatory drug binding protein; CSPB1; CSBP2; CSBP1; CSBP; CSAID-binding protein; CSAID binding protein; CRK1
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Representative Drug(s) LY2157299 Drug Info IC50 = 405 nM [2]
Co-Target Name Activin receptor type IB (ACVR1B) Patented-recorded Target
UniProt ID ACV1B_HUMAN
Gene Name ACVR1B
Synonyms
Serine/threonine-protein kinase receptor R2; SKR2; Activin receptor-like kinase 4; Activin receptor type-1B; ALK4; ALK-4; ACVRLK4; ACTR-IB
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Representative Drug(s) TEW-7197 Drug Info IC50 = 13 nM Click to Show More [1]
2 LY2157299 Drug Info IC50 = 199 nM [1]
Co-Target Name Serine/threonine-protein kinase RIPK2 (RIPK2) Co-Target
UniProt ID RIPK2_HUMAN
Gene Name RIPK2
Synonyms
Receptor-interacting serine/threonine-protein kinase 2; CARD-containing interleukin-1 beta-converting enzyme-associated kinase; CARD-containing IL-1 beta ICE-kinase; RIP-like-interacting CLARP kinase; Receptor-interacting protein 2; RIP-2; Tyrosine-protein kinase RIPK2
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Representative Drug(s) LY2157299 Drug Info IC50 = 44 nM Click to Show More [1]
2 TEW-7197 Drug Info IC50 = 54 nM [1]
References  Top
REF 1 Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-beta type I receptor kinase as cancer immunotherapeutic/antifibrotic agent. J Med Chem. 2014 May 22;57(10):4213-38.
REF 2 Synthesis and biological evaluation of 5-(fluoro-substituted-6-methylpyridin-2-yl)-4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)imidazoles as inhibitors of transforming growth factor-beta type I receptor kinase. Bioorg Med Chem Lett. 2015 Nov 15;25(22):5228-31.

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