ChEMBL logo


ChEMBL Statistics
  Loading Statistics...

Target Report Card

Target Name and Classification

Target ID CHEMBL4439
Preferred Name TGF-beta receptor type I
Synonyms ALK-5 | ALK5 | ALK5 | Activin A receptor type II-like protein kinase of 53kD | Activin receptor-like kinase 5 | SKR4 | SKR4 | Serine/threonine-protein kinase receptor R4 | TGF-beta receptor type I | TGF-beta receptor type-1 | TGF-beta type I receptor | TGFBR1 | TGFR-1 | TbetaR-I | Transforming growth factor-beta receptor type I
Organism Homo sapiens
Species Group No
Protein Target Classification
  • enzyme > kinase > protein kinase > tkl protein kinase group > tkl protein kinase stkr family > tkl protein kinase stkr type 1 subfamily

Target Components

Component Description Relationship Accession
TGF-beta receptor type-1 SINGLE PROTEIN P36897

Approved Drugs and Clinical Candidates

ChEMBL ID Name Mechanism of Action Max Phase References
CHEMBL2364611 GALUNISERTIB TGF-beta receptor type I inhibitor 2 Other PubMed PubMed

Target Associated Bioactivities

Target Associated Assays

Target Ligand Efficiencies

Target Associated Compound Properties

Target Cross References - Gene

Array Express ENSG00000106799
Ensembl ENSG00000106799
GO Cellular Component GO:0005622 (intracellular)
GO:0005623 (cell)
GO:0005768 (endosome)
GO:0005886 (plasma membrane)
GO:0005923 (bicellular tight junction)
GO:0009986 (cell surface)
GO:0016020 (membrane)
GO:0016021 (integral component of membrane)
GO:0030054 (cell junction)
GO:0043231 (intracellular membrane-bounded organelle)
GO:0043235 (receptor complex)
GO:0045121 (membrane raft)
GO:0070022 (transforming growth factor beta receptor homodimeric complex)
GO Molecular Function GO:0000166 (nucleotide binding)
GO:0004672 (protein kinase activity)
GO:0004674 (protein serine/threonine kinase activity)
GO:0004675 (transmembrane receptor protein serine/threonine kinase activity)
GO:0004702 (receptor signaling protein serine/threonine kinase activity)
GO:0005024 (transforming growth factor beta-activated receptor activity)
GO:0005025 (transforming growth factor beta receptor activity, type I)
GO:0005057 (receptor signaling protein activity)
GO:0005102 (receptor binding)
GO:0005114 (type II transforming growth factor beta receptor binding)
GO:0005515 (protein binding)
GO:0005524 (ATP binding)
GO:0016301 (kinase activity)
GO:0016740 (transferase activity)
GO:0019838 (growth factor binding)
GO:0046332 (SMAD binding)
GO:0046872 (metal ion binding)
GO:0050431 (transforming growth factor beta binding)
GO:0070411 (I-SMAD binding)
GO Biological Process GO:0000186 (activation of MAPKK activity)
GO:0001501 (skeletal system development)
GO:0001525 (angiogenesis)
GO:0001701 (in utero embryonic development)
GO:0001822 (kidney development)
GO:0001824 (blastocyst development)
GO:0001837 (epithelial to mesenchymal transition)
GO:0001937 (negative regulation of endothelial cell proliferation)
GO:0001938 (positive regulation of endothelial cell proliferation)
GO:0002088 (lens development in camera-type eye)
GO:0003222 (ventricular trabecula myocardium morphogenesis)
GO:0003223 (ventricular compact myocardium morphogenesis)
GO:0003342 (proepicardium development)
GO:0006355 (regulation of transcription, DNA-templated)
GO:0006468 (protein phosphorylation)
GO:0006915 (apoptotic process)
GO:0007050 (cell cycle arrest)
GO:0007165 (signal transduction)
GO:0007178 (transmembrane receptor protein serine/threonine kinase signaling pathway)
GO:0007179 (transforming growth factor beta receptor signaling pathway)
GO:0007507 (heart development)
GO:0008284 (positive regulation of cell proliferation)
GO:0008354 (germ cell migration)
GO:0008584 (male gonad development)
GO:0009791 (post-embryonic development)
GO:0009952 (anterior/posterior pattern specification)
GO:0010468 (regulation of gene expression)
GO:0010628 (positive regulation of gene expression)
GO:0010717 (regulation of epithelial to mesenchymal transition)
GO:0010718 (positive regulation of epithelial to mesenchymal transition)
GO:0010862 (positive regulation of pathway-restricted SMAD protein phosphorylation)
GO:0016310 (phosphorylation)
GO:0016579 (protein deubiquitination)
GO:0018105 (peptidyl-serine phosphorylation)
GO:0018107 (peptidyl-threonine phosphorylation)
GO:0023014 (signal transduction by protein phosphorylation)
GO:0030154 (cell differentiation)
GO:0030199 (collagen fibril organization)
GO:0030307 (positive regulation of cell growth)
GO:0030335 (positive regulation of cell migration)
GO:0030512 (negative regulation of transforming growth factor beta receptor signaling pathway)
GO:0031396 (regulation of protein ubiquitination)
GO:0032331 (negative regulation of chondrocyte differentiation)
GO:0032924 (activin receptor signaling pathway)
GO:0035556 (intracellular signal transduction)
GO:0040008 (regulation of growth)
GO:0042060 (wound healing)
GO:0042118 (endothelial cell activation)
GO:0043062 (extracellular structure organization)
GO:0043065 (positive regulation of apoptotic process)
GO:0043066 (negative regulation of apoptotic process)
GO:0043393 (regulation of protein binding)
GO:0043542 (endothelial cell migration)
GO:0045893 (positive regulation of transcription, DNA-templated)
GO:0048538 (thymus development)
GO:0048663 (neuron fate commitment)
GO:0048701 (embryonic cranial skeleton morphogenesis)
GO:0048705 (skeletal system morphogenesis)
GO:0048762 (mesenchymal cell differentiation)
GO:0048844 (artery morphogenesis)
GO:0048870 (cell motility)
GO:0051272 (positive regulation of cellular component movement)
GO:0051491 (positive regulation of filopodium assembly)
GO:0051496 (positive regulation of stress fiber assembly)
GO:0051897 (positive regulation of protein kinase B signaling)
GO:0060017 (parathyroid gland development)
GO:0060021 (palate development)
GO:0060037 (pharyngeal system development)
GO:0060043 (regulation of cardiac muscle cell proliferation)
GO:0060317 (cardiac epithelial to mesenchymal transition)
GO:0060389 (pathway-restricted SMAD protein phosphorylation)
GO:0060391 (positive regulation of SMAD protein import into nucleus)
GO:0060412 (ventricular septum morphogenesis)
GO:0060978 (angiogenesis involved in coronary vascular morphogenesis)
GO:0060982 (coronary artery morphogenesis)
GO:0070723 (response to cholesterol)
GO:0071560 (cellular response to transforming growth factor beta stimulus)
GO:1905007 (positive regulation of epithelial to mesenchymal transition involved in endocardial cushion formation)
GO:1905075 (positive regulation of occluding junction disassembly)
GO:1905223 (epicardium morphogenesis)
GO:2001235 (positive regulation of apoptotic signaling pathway)
GO:2001237 (negative regulation of extrinsic apoptotic signaling pathway)
Wikipedia TGF_beta_receptor_1

Target Cross References - Protein

canSAR P36897
CGD Loeys-Dietz syndrome, type 1A; Loeys-Dietz sydnrome, type 2A
Human Protein Atlas ENSG00000106799
IntAct P36897
Guide to Pharmacology 1788
Open Targets ENSG00000106799
PharmGKB PA36485
Pharos P36897 (Tchem)
Reactome R-HSA-2173788 (Downregulation of TGF-beta receptor signaling.)
R-HSA-2173789 (TGF-beta receptor signaling activates SMADs.)
R-HSA-2173791 (TGF-beta receptor signaling in EMT (epithelial to mesenchymal transition).)
R-HSA-3304356 (SMAD2/3 Phosphorylation Motif Mutants in Cancer.)
R-HSA-3315487 (SMAD2/3 MH2 Domain Mutants in Cancer.)
R-HSA-3645790 (TGFBR2 Kinase Domain Mutants in Cancer.)
R-HSA-3656532 (TGFBR1 KD Mutants in Cancer.)
R-HSA-3656535 (TGFBR1 LBD Mutants in Cancer.)
R-HSA-5689603 (UCH proteinases.)
R-HSA-5689880 (Ub-specific processing proteases.)
UniProt P36897 Q6IR47 Q706C0 Q706C1

Target Cross References - Domain

InterPro IPR000333 (TGFB_receptor.)
IPR000472 (Activin_recp.)
IPR000719 (Prot_kinase_dom.)
IPR003605 (GS_dom.)
IPR008271 (Ser/Thr_kinase_AS.)
IPR011009 (Kinase-like_dom_sf.)
IPR017441 (Protein_kinase_ATP_BS.)
Pfam PF00069 (Pkinase)
PF01064 (Activin_recp)
PF08515 (TGF_beta_GS)

Target Cross References - Structure

PDBe 1B6C 1IAS 1PY5 1RW8 1VJY 2PJY 2WOT 2WOU 2X7O 3FAA 3GXL 3HMM 3KCF 3KFD 3TZM 4X0M 4X2F 4X2G 4X2J 4X2K 4X2N 5E8S 5E8T 5E8U More...
CREDO 1B6C 1IAS 1PY5 1RW8 1VJY 2PJY 2WOT 2WOU 2X7O 3FAA 3GXL 3HMM 3KCF 3KFD 3TZM 4X0M 4X2F 4X2G 4X2J 4X2K 4X2N 5E8S 5E8T 5E8U More...