Angiotensin-converting enzyme 2 | M2: Angiotensin-converting (ACE and ACE2) | IUPHAR/BPS Guide to PHARMACOLOGY

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Angiotensin-converting enzyme 2

Target not currently curated in GtoImmuPdb

Target id: 1614

Nomenclature: Angiotensin-converting enzyme 2

Abbreviated Name: ACE2

Family: M2: Angiotensin-converting (ACE and ACE2)

Annotation status:  image of a green circle Annotated and expert reviewed. Please contact us if you can help with updates.  » Email us

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 1 788 Xp22 ACE2 angiotensin I converting enzyme 2
Mouse 1 788 X 76.12 cM Ace2 angiotensin I converting enzyme (peptidyl-dipeptidase A) 2
Rat 1 788 Xq21 Ace2 angiotensin I converting enzyme 2
Previous and Unofficial Names
ACE-related carboxypeptidase | renal angiotensin-converting enzyme 2 | angiotensin I converting enzyme (peptidyl-dipeptidase A) 2
Database Links
Specialist databases
MEROPS M02.006 (Hs)
Other databases
ChEMBL Target
DrugBank Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
Enzyme Reaction
EC Number:
Binding dissociation constants for SARS-CoVs (Kd) (Human)
SARS-CoV-2 (1.2 nM); SARS-CoV (5 nM); Binding of hACE2 ectodomain to immobilised SB domains of the viral strains in a biolayer interferometry assay.  [12]
Endogenous substrates (Human)
angiotensin I (AGT, P01019) > angiotensin-(1-9) (AGT, P01019)  [1]

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
XNT [PMID: 18391097] Hs Activation 4.7 pEC50 3
pEC50 4.7 (EC50 2.01x10-5 M) [3]
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
compound 28 [PMID: 18324760] Hs Inhibition 9.9 pKi 9
pKi 9.9 (Ki 1.3x10-10 M) [9]
MLN-4760 Hs Inhibition 9.4 pIC50 9
pIC50 9.4 (IC50 4.4x10-10 M) [9]
Other Binding Ligands
Key to terms and symbols Click column headers to sort
Ligand Sp. Action Value Parameter Reference
Abz-Ser-Pro-Tyr(NO2)-OH Hs Binding - - 13
Immuno Process Associations
Immuno Process:  Barrier integrity
GO Annotations:  Associated to 2 GO processes
GO:0001618 virus receptor activity IDA
GO:0046718 viral entry into host cell TAS
Immuno Process:  Inflammation
GO Annotations:  Associated to 1 GO processes
GO:0050727 regulation of inflammatory response IC
Immuno Process:  Immune regulation
GO Annotations:  Associated to 1 GO processes
GO:0050727 regulation of inflammatory response IC
Immuno Process:  Cytokine production & signalling
GO Annotations:  Associated to 1 GO processes
GO:0001817 regulation of cytokine production IC
General Comments
Accumulating preliminary data suggest ACE2 as a receptor for the novel coronavirus (officially named SARS-CoV-2) that was identified as the cause of the respiratory disease outbreak in Wuhan in late 2019 [2,4,6-7,10,12]. SARS-CoV-2 was referred to as 2019-nCoV, or Wuhan coronavirus prior to formal naming by the WHO. SARS-CoV-2 is a betacoronavirus, and in common with the original SARS-CoV the viral spike protein has been shown to engage ACE2 [8,11-12] for viral entry.

GSK have already completed a Phase 2 study of their recombinant human ACE2 protein (GSK2586881) to determine its effects in patients with acute lung injury (ALI) or acute respiratory distress syndrome (ARDS) [5]. GSK2586881 modulated the renin-angiotensin system (RAS) as expected, but the trial was terminated following a planned futility analysis. A clinical trial (NCT04287686) is planned to gather preliminary biologic, physiologic, and clinical data on the effects of using recombinant human ACE2 protein as a decoy for SARS-CoV-2 in patients with COVID-19.


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1. Donoghue M, Hsieh F, Baronas E, Godbout K, Gosselin M, Stagliano N, Donovan M, Woolf B, Robison K, Jeyaseelan R et al.. (2000) A novel angiotensin-converting enzyme-related carboxypeptidase (ACE2) converts angiotensin I to angiotensin 1-9. Circ. Res., 87 (5): E1-9. [PMID:10969042]

2. Gralinski LE, Menachery VD. (2020) Return of the Coronavirus: 2019-nCoV. Viruses, 12 (2). DOI: 10.3390/v12020135 [PMID:31991541]

3. Hernández Prada JA, Ferreira AJ, Katovich MJ, Shenoy V, Qi Y, Santos RA, Castellano RK, Lampkins AJ, Gubala V, Ostrov DA et al.. (2008) Structure-based identification of small-molecule angiotensin-converting enzyme 2 activators as novel antihypertensive agents. Hypertension, 51 (5): 1312-7. [PMID:18391097]

4. Hoffmann M, Kleine-Weber H, Krüger N, Müller M, Drosten C, Pöhlmann S. (2020) The novel coronavirus 2019 (2019-nCoV) uses the SARS-coronavirus receptor ACE2 and the cellular protease TMPRSS2 for entry into target cells. BioRxiv,: 929042. DOI: 10.1101/2020.01.31.929042

5. Khan A, Benthin C, Zeno B, Albertson TE, Boyd J, Christie JD, Hall R, Poirier G, Ronco JJ, Tidswell M et al.. (2017) A pilot clinical trial of recombinant human angiotensin-converting enzyme 2 in acute respiratory distress syndrome. Crit Care, 21 (1): 234. [PMID:28877748]

6. Lei C, Fu W, Qian K, Li T, Zhang S, Ding M, Hu S. (2020) Potent neutralization of 2019 novel coronavirus by recombinant ACE2-Ig. BioRxiv,: 929976. DOI: 10.1101/2020.02.01.929976

7. Letko M, Munzter V. (2020) Functional assessment of cell entry and receptor usage for lineage B β-coronaviruses, including 2019-nCoV. BiorXiv, (22 January). DOI: 10.1101/2020.01.22.915660

8. Li F, Li W, Farzan M, Harrison SC. (2005) Structure of SARS coronavirus spike receptor-binding domain complexed with receptor. Science, 309 (5742): 1864-8. [PMID:16166518]

9. Mores A, Matziari M, Beau F, Cuniasse P, Yiotakis A, Dive V. (2008) Development of potent and selective phosphinic peptide inhibitors of angiotensin-converting enzyme 2. J. Med. Chem., 51 (7): 2216-26. [PMID:18324760]

10. Peng Z, Shi Z-L. (2020) Discovery of a novel coronavirus associated with the recent pneumonia outbreak in humans and its potential bat origin. BiorXiv, (23 January). DOI: 10.1101/2020.01.22.914952

11. Song W, Gui M, Wang X, Xiang Y. (2018) Cryo-EM structure of the SARS coronavirus spike glycoprotein in complex with its host cell receptor ACE2. PLoS Pathog., 14 (8): e1007236. [PMID:30102747]

12. Walls AC, Park YJ, Tortorici MA, Wall A, McGuire AT, Veesler D. (2020) Structure, Function, and Antigenicity of the SARS-CoV-2 Spike Glycoprotein. Cell, [Epub ahead of print]. DOI: 10.1016/j.cell.2020.02.058 [PMID:32155444]

13. Yan ZH, Ren KJ, Wang Y, Chen S, Brock TA, Rege AA. (2003) Development of intramolecularly quenched fluorescent peptides as substrates of angiotensin-converting enzyme 2. Anal. Biochem., 312 (2): 141-7. [PMID:12531198]

How to cite this page

M2: Angiotensin-converting (ACE and ACE2): Angiotensin-converting enzyme 2. Last modified on 12/03/2020. Accessed on 06/04/2020. IUPHAR/BPS Guide to PHARMACOLOGY,