General Information of Target

Target ID LDTP03833
Target Name Serine/threonine-protein kinase receptor R3 (ACVRL1)
Gene Name ACVRL1
Gene ID 94
Synonyms
ACVRLK1; ALK1; Serine/threonine-protein kinase receptor R3; SKR3; EC 2.7.11.30; Activin receptor-like kinase 1; ALK-1; TGF-B superfamily receptor type I; TSR-I
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MTLGSPRKGLLMLLMALVTQGDPVKPSRGPLVTCTCESPHCKGPTCRGAWCTVVLVREEG
RHPQEHRGCGNLHRELCRGRPTEFVNHYCCDSHLCNHNVSLVLEATQPPSEQPGTDGQLA
LILGPVLALLALVALGVLGLWHVRRRQEKQRGLHSELGESSLILKASEQGDSMLGDLLDS
DCTTGSGSGLPFLVQRTVARQVALVECVGKGRYGEVWRGLWHGESVAVKIFSSRDEQSWF
RETEIYNTVLLRHDNILGFIASDMTSRNSSTQLWLITHYHEHGSLYDFLQRQTLEPHLAL
RLAVSAACGLAHLHVEIFGTQGKPAIAHRDFKSRNVLVKSNLQCCIADLGLAVMHSQGSD
YLDIGNNPRVGTKRYMAPEVLDEQIRTDCFESYKWTDIWAFGLVLWEIARRTIVNGIVED
YRPPFYDVVPNDPSFEDMKKVVCVDQQTPTIPNRLAADPVLSGLAQMMRECWYPNPSARL
TALRIKKTLQKISNSPEKPKVIQ
Target Type
Clinical trial
Target Bioclass
Enzyme
Family
Protein kinase superfamily, TKL Ser/Thr protein kinase family, TGFB receptor subfamily
Subcellular location
Cell membrane
Function
Type I receptor for TGF-beta family ligands BMP9/GDF2 and BMP10 and important regulator of normal blood vessel development. On ligand binding, forms a receptor complex consisting of two type II and two type I transmembrane serine/threonine kinases. Type II receptors phosphorylate and activate type I receptors which autophosphorylate, then bind and activate SMAD transcriptional regulators. May bind activin as well.
TTD ID
T36959
Uniprot ID
P37023
DrugMap ID
TTGYPTC
Ensemble ID
ENST00000388922.9
HGNC ID
HGNC:175
ChEMBL ID
CHEMBL5311

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 1 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
DBIA
 Probe Info 
C389(1.17)  LDD3380  [1]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0022  KB02 A2780 C389(1.25)  LDD2254  [1]
 LDCM0023  KB03 A2780 C389(1.53)  LDD2671  [1]
 LDCM0024  KB05 OV-90 C389(1.17)  LDD3380  [1]

References

1 DrugMap: A quantitative pan-cancer analysis of cysteine ligandability. Cell. 2024 May 9;187(10):2536-2556.e30. doi: 10.1016/j.cell.2024.03.027. Epub 2024 Apr 22.
Mass spectrometry data entry: PXD047840