activin A receptor type IL | Type I receptor serine/threonine kinases | IUPHAR/BPS Guide to PHARMACOLOGY

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activin A receptor type IL

Target not currently curated in GtoImmuPdb

Target id: 1784

Nomenclature: activin A receptor type IL

Abbreviated Name: ALK1

Family: Type I receptor serine/threonine kinases

Annotation status:  image of an orange circle Annotated and awaiting review. Please contact us if you can help with reviewing.  » Email us

Quaternary Structure: Complexes
Bone morphogenetic protein receptors
Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 1 503 12q13.13 ACVRL1 activin A receptor like type 1
Mouse 1 502 15 F3 Acvrl1 activin A receptor, type II-like 1
Rat 1 504 7q36 Acvrl1 activin A receptor like type 1
Previous and Unofficial Names
SKR3 | ACVRLK1 | HHT | HHT2 | ORW2 | SETHKIR | TGF-B superfamily receptor type I | TSR-I | activin receptor-like kinase-1 | Serine/threonine-protein kinase receptor R3 | activin A receptor, type II-like 1 | activin A receptor
Database Links
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
RefSeq Nucleotide
RefSeq Protein
Selected 3D Structures
Image of receptor 3D structure from RCSB PDB
Description:  Crystal structure of the ACVRL1 (ALK1) kinase domain bound to LDN-193189
PDB Id:  3MY0
Resolution:  2.65Å
Species:  Human
Enzyme Reaction
EC Number:

Download all structure-activity data for this target as a CSV file

Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
compound 13d [PMID: 23639540] Hs Inhibition >8.3 pIC50 3
pIC50 >8.3 (IC50 <5x10-9 M) [3]
compound 13r [PMID: 23639540] Hs Inhibition >8.3 pIC50 3
pIC50 >8.3 (IC50 <5x10-9 M) [3]
LDN-214117 Hs Inhibition 7.6 pIC50 5
pIC50 7.6 (IC50 2.7x10-8 M) [5]
compound 13a [PMID: 23639540] Hs Inhibition 7.4 pIC50 3
pIC50 7.4 (IC50 4.21x10-8 M) [3]
ML347 Hs Inhibition 7.3 pIC50 3
pIC50 7.3 (IC50 4.6x10-8 M) [3]
panulisib Hs Inhibition 7.3 pIC50 4
pIC50 7.3 (IC50 4.7x10-8 M) [4]
Description: Using a radiometric protein kinase (33PanQinase activity) assay.
DiscoveRx KINOMEscan® screen
A screen of 72 inhibitors against 456 human kinases. Quantitative data were derived using DiscoveRx KINOMEscan® platform.
Reference: 2,6

Key to terms and symbols Click column headers to sort
Target used in screen: ACVRL1
Ligand Sp. Type Action Value Parameter
PP-242 Hs Inhibitor Inhibition 8.5 pKd
NVP-TAE684 Hs Inhibitor Inhibition 7.2 pKd
PD-173955 Hs Inhibitor Inhibition 7.2 pKd
dasatinib Hs Inhibitor Inhibition 6.3 pKd
vandetanib Hs Inhibitor Inhibition 6.3 pKd
JNJ-28312141 Hs Inhibitor Inhibition 5.7 pKd
lestaurtinib Hs Inhibitor Inhibition 5.7 pKd
fedratinib Hs Inhibitor Inhibition 5.6 pKd
SB203580 Hs Inhibitor Inhibition <5.5 pKd
ruboxistaurin Hs Inhibitor Inhibition <5.5 pKd
Displaying the top 10 most potent ligands  View all ligands in screen »
EMD Millipore KinaseProfilerTM screen/Reaction Biology Kinase HotspotSM screen
A screen profiling 158 kinase inhibitors (Calbiochem Protein Kinase Inhibitor Library I and II, catalogue numbers 539744 and 539745) for their inhibitory activity at 1µM and 10µM against 234 human recombinant kinases using the EMD Millipore KinaseProfilerTM service.

A screen profiling the inhibitory activity of 178 commercially available kinase inhibitors at 0.5µM against a panel of 300 recombinant protein kinases using the Reaction Biology Corporation Kinase HotspotSM platform.

Reference: ...1

Key to terms and symbols Click column headers to sort
Target used in screen: nd/ALK1(ACVRL1)
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
Cdk1/2 inhibitor III Hs Inhibitor Inhibition 15.1
dasatinib Hs Inhibitor Inhibition 15.9
dorsomorphin Hs Inhibitor Inhibition 21.6
alsterpaullone 2-cyanoethyl Hs Inhibitor Inhibition 53.6
bosutinib Hs Inhibitor Inhibition 67.6
TWS119 Hs Inhibitor Inhibition 70.3
Gö 6976 Hs Inhibitor Inhibition 73.6
alsterpaullone Hs Inhibitor Inhibition 76.2
aloisine A Hs Inhibitor Inhibition 76.2
VEGF receptor 2 kinase inhibitor IV Hs Inhibitor Inhibition 76.4
Displaying the top 10 most potent ligands  View all ligands in screen »
Clinically-Relevant Mutations and Pathophysiology
Disease:  Heritable pulmonary arterial hypertension
Orphanet: ORPHA275777
Disease:  Telangiectasia, hereditary hemorrhagic, type 2
Synonyms: Hereditary hemorrhagic telangiectasia [Orphanet: ORPHA774] [Disease Ontology: DOID:1270]
Disease Ontology: DOID:1270
OMIM: 600376
Orphanet: ORPHA774


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1. Anastassiadis T, Deacon SW, Devarajan K, Ma H, Peterson JR. (2011) Comprehensive assay of kinase catalytic activity reveals features of kinase inhibitor selectivity. Nat. Biotechnol., 29 (11): 1039-45. [PMID:22037377]

2. Davis MI, Hunt JP, Herrgard S, Ciceri P, Wodicka LM, Pallares G, Hocker M, Treiber DK, Zarrinkar PP. (2011) Comprehensive analysis of kinase inhibitor selectivity. Nat. Biotechnol., 29 (11): 1046-51. [PMID:22037378]

3. Engers DW, Frist AY, Lindsley CW, Hong CC, Hopkins CR. (2013) Synthesis and structure-activity relationships of a novel and selective bone morphogenetic protein receptor (BMP) inhibitor derived from the pyrazolo[1.5-a]pyrimidine scaffold of dorsomorphin: the discovery of ML347 as an ALK2 versus ALK3 selective MLPCN probe. Bioorg. Med. Chem. Lett., 23 (11): 3248-52. [PMID:23639540]

4. Jalota-Badhwar A, Bhatia DR, Boreddy S, Joshi A, Venkatraman M, Desai N, Chaudhari S, Bose J, Kolla LS, Deore V et al.. (2015) P7170: A Novel Molecule with Unique Profile of mTORC1/C2 and Activin Receptor-like Kinase 1 Inhibition Leading to Antitumor and Antiangiogenic Activity. Mol. Cancer Ther., 14 (5): 1095-106. [PMID:25700704]

5. Mohedas AH, Wang Y, Sanvitale CE, Canning P, Choi S, Xing X, Bullock AN, Cuny GD, Yu PB. (2014) Structure-activity relationship of 3,5-diaryl-2-aminopyridine ALK2 inhibitors reveals unaltered binding affinity for fibrodysplasia ossificans progressiva causing mutants. J. Med. Chem., 57 (19): 7900-15. [PMID:25101911]

6. Wodicka LM, Ciceri P, Davis MI, Hunt JP, Floyd M, Salerno S, Hua XH, Ford JM, Armstrong RC, Zarrinkar PP et al.. (2010) Activation state-dependent binding of small molecule kinase inhibitors: structural insights from biochemistry. Chem. Biol., 17 (11): 1241-9. [PMID:21095574]

How to cite this page

Type I receptor serine/threonine kinases: activin A receptor type IL. Last modified on 10/07/2018. Accessed on 17/11/2019. IUPHAR/BPS Guide to PHARMACOLOGY,