General Information of the Protein
Protein ID
PT01813
Protein Name
Angiotensin-converting enzyme 2
Secondarily
Protein Name
Angiotensin-converting enzyme homolog
Angiotensin-converting enzyme-related carboxypeptidase
Metalloprotease MPROT15
Gene Name
ACE2
Secondarily
Gene Name
UNQ868/PRO1885
Sequence
MSSSSWLLLSLVAVTAAQSTIEEQAKTFLDKFNHEAEDLFYQSSLASWNYNTNITEENVQNMNNAGDKWSAFLKEQSTLAQMYPLQEIQNLTVKLQLQALQQNGSSVLSEDKSKRLNTILNTMSTIYSTGKVCNPDNPQECLLLEPGLNEIMANSLDYNERLWAWESWRSEVGKQLRPLYEEYVVLKNEMARANHYEDYGDYWRGDYEVNGVDGYDYSRGQLIEDVEHTFEEIKPLYEHLHAYVRAKLMNAYPSYISPIGCLPAHLLGDMWGRFWTNLYSLTVPFGQKPNIDVTDAMVDQAWDAQRIFKEAEKFFVSVGLPNMTQGFWENSMLTDPGNVQKAVCHPTAWDLGKGDFRILMCTKVTMDDFLTAHHEMGHIQYDMAYAAQPFLLRNGANEGFHEAVGEIMSLSAATPKHLKSIGLLSPDFQEDNETEINFLLKQALTIVGTLPFTYMLEKWRWMVFKGEIPKDQWMKKWWEMKREIVGVVEPVPHDETYCDPASLFHVSNDYSFIRYYTRTLYQFQFQEALCQAAKHEGPLHKCDISNSTEAGQKLFNMLRLGKSEPWTLALENVVGAKNMNVRPLLNYFEPLFTWLKDQNKNSFVGWSTDWSPYADQSIKVRISLKSALGDKAYEWNDNEMYLFRSSVAYAMRQYFLKVKNQMILFGEEDVRVANLKPRISFNFFVTAPKNVSDIIPRTEVEKAIRMSRSRINDAFRLNDNSLEFLGIQPTLGPPNQPPVSIWLIVFGVVMGVIVVGIVILIFTGIRDRKKKNKARSGENPYASIDISKGENNPGFQNTDDVQTSF
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Organism
Homo sapiens, Human
Protein Classification
Enzyme
>
Protease
>
Metallo protease
>
Metallo protease MAE clan
>
Metallo protease M2 family
Function
Essential counter-regulatory carboxypeptidase of the renin-angiotensin hormone system that is a critical regulator of blood volume, systemic vascular resistance, and thus cardiovascular homeostasis (PubMed:27217402). Converts angiotensin I to angiotensin 1-9, a nine-amino acid peptide with anti-hypertrophic effects in cardiomyocytes, and angiotensin II to angiotensin 1-7, which then acts as a beneficial vasodilator and anti-proliferation agent, counterbalancing the actions of the vasoconstrictor angiotensin II (PubMed:10969042, PubMed:10924499, PubMed:11815627, PubMed:19021774, PubMed:14504186). Also removes the C-terminal residue from three other vasoactive peptides, neurotensin, kinetensin, and des-Arg bradykinin, but is not active on bradykinin (PubMed:10969042, PubMed:11815627). Also cleaves other biological peptides, such as apelins (apelin-13, [Pyr1]apelin-13, apelin-17, apelin-36), casomorphins (beta-casomorphin-7, neocasomorphin) and dynorphin A with high efficiency (PubMed:11815627, PubMed:27217402, PubMed:28293165). In addition, ACE2 C-terminus is homologous to collectrin and is responsible for the trafficking of the neutral amino acid transporter SL6A19 to the plasma membrane of gut epithelial cells via direct interaction, regulating its expression on the cell surface and its catalytic activity (PubMed:18424768, PubMed:19185582).
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Uniprot ID
Primary ID:
Q9BYF1

Secondarily ID:
A0A7D6JAD5
C7ECU1
Q6UWP0
Q86WT0
Q9NRA7
Q9UFZ6
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Ensembl ID
ENSG00000130234
HGNC ID
HGNC:13557
Subcellular Location
Secreted
Map of Molecular Bioactivity Related to the Protein
Map of Molecular Bioactivity Related to the Protein

Protein
Cell Line
Compound

Bioactivity Value:

<= 0.1 μM
> 0.1 μM and <= 10 μM
> 10 μM
Imprecise Activity
Table of Molecular Bioactivities Related to the Protein
Cell Line ID: CL000025 , HEK-293T
Compound ID Compound Name Compound Formula
CP0967446
(4S)-5-[[(1S)-2-[[(1S)-1-[[(1S)-2-[[(1S)-2-[[(1S)-4-amino-1-[[(1S)-2-[[(1S)-2-[[(1S)-1-[[(1S)-2-[[(1S)-2-[[(1S)-2-[[(1S)-3-amino-1-[[(1S)-2-[[(1S)-3-amino-1-[[(1S,2R)-1-carbamoyl-2-hydroxy-propyl]carbamoyl]-3-oxo-propyl]amino]-1-[(4-hydroxyphenyl)methyl]-2-oxo-ethyl]carbamoyl]-3-oxo-propyl]amino]-1-(1H-indol-3-ylmethyl)-2-oxo-ethyl]amino]-1-(hydroxymethyl)-2-oxo-ethyl]amino]-1-methyl-2-oxo-ethyl]carbamoyl]-3-methyl-butyl]amino]-1-(hydroxymethyl)-2-oxo-ethyl]amino]-1-(hydroxymethyl)-2-oxo-ethyl]carbamoyl]-4-oxo-butyl]amino]-1-[(4-hydroxyphenyl)methyl]-2-oxo-ethyl]amino]-1-benzyl-2-oxo-ethyl]carbamoyl]-3-methyl-butyl]amino]-1-(carboxymethyl)-2-oxo-ethyl]amino]-4-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-4-amino-2-[[(2S)-2-[[(2S)-6-amino-2-[[(2S)-2-amino-3-carboxy-propanoyl]amino]hexanoyl]amino]-3-phenyl-propanoyl]amino]-4-oxo-butanoyl]amino]-3-(1H-imidazol-4-yl)propanoyl]amino]-4-carboxy-butanoyl]amino]propanoyl]amino]-5-oxo-pentanoic acid
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C125H172N32O41
 1
1
IC50 = 6 nM
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CP0574187
(4S)-4-[[(2S)-2-[[(2S)-4-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S,3S)-2-amino-3-methylpentanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]propanoyl]amino]-4-methylpentanoyl]amino]-4-methylpentanoyl]amino]-4-carboxybutanoyl]amino]-4-oxobutanoyl]amino]propanoyl]amino]-5-[[(2S)-1-[[(2S)-1-[[(2S)-4-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-1,4-diamino-1,4-dioxobutan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-5-oxopentanoic acid
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C79H121N19O26
 1
1
IC50 = 9 nM
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CP0967448
(4S)-5-[[(1S)-2-[[(1S)-1-[[(1S)-5-amino-1-[[(1S)-1-[[(1S)-3-amino-1-[[(1S)-2-[[(1S)-1-[[2-[[(1S)-4-amino-1-carbamoyl-4-oxo-butyl]amino]-2-oxo-ethyl]carbamoyl]-4-guanidino-butyl]amino]-1-(carboxymethyl)-2-oxo-ethyl]carbamoyl]-3-oxo-propyl]carbamoyl]-3-carboxy-propyl]carbamoyl]pentyl]carbamoyl]-3-carboxy-propyl]amino]-1-(1H-imidazol-4-ylmethyl)-2-oxo-ethyl]amino]-4-[[(2S)-2-[[(2S)-2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-amino-3-hydroxy-propanoyl]amino]-5-guanidino-pentanoyl]amino]-3-carboxy-propanoyl]amino]hexanoyl]amino]-3-(1H-imidazol-4-yl)propanoyl]amino]-4-carboxy-butanoyl]amino]-5-oxo-pentanoic acid
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C78H125N31O31
 1
1
IC50 = 10 nM
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CP0968194
(4S)-5-[[(1S)-4-amino-1-[[(1S)-2-[[(1S)-5-amino-1-[[(1S,2R)-1-[[(1S)-2-[[(1S)-1-[[(1S)-2-[[(1S)-5-amino-1-[[(1S)-2-[[(1S)-4-amino-1-[[(1S)-2-[[(1S)-1-[[(1S)-1-[[(1S)-1-[[(1S)-1-[[(1S,2S)-1-[[(1S)-2-[[(1S)-2-[[(1S)-4-amino-1-[[(1S)-2-amino-1-(hydroxymethyl)-2-oxo-ethyl]carbamoyl]-4-oxo-butyl]amino]-1-(1H-indol-3-ylmethyl)-2-oxo-ethyl]amino]-1-[(4-hydroxyphenyl)methyl]-2-oxo-ethyl]carbamoyl]-2-methyl-butyl]carbamoyl]-3-carboxy-propyl]carbamoyl]-3-carboxy-propyl]carbamoyl]-2-methyl-propyl]carbamoyl]-3-carboxy-propyl]amino]-1-(1H-imidazol-4-ylmethyl)-2-oxo-ethyl]carbamoyl]-4-oxo-butyl]amino]-1-benzyl-2-oxo-ethyl]carbamoyl]pentyl]amino]-1-(carboxymethyl)-2-oxo-ethyl]carbamoyl]-3-methyl-butyl]amino]-1-benzyl-2-oxo-ethyl]carbamoyl]-2-hydroxy-propyl]carbamoyl]pentyl]amino]-1-methyl-2-oxo-ethyl]carbamoyl]-4-oxo-butyl]amino]-4-[[(2S)-2-[[(2S,3S)-2-amino-3-methyl-pentanoyl]amino]-4-carboxy-butanoyl]amino]-5-oxo-pentanoic acid
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C133H194N32O41
 1
1
IC50 = 11 nM
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CP0964090
(4S)-4-[[(2S)-6-amino-2-[[(2S)-2-[[2-[[(2S)-6-amino-2-[[(2S)-4-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-5-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-6-amino-2-[[(2S)-3-carboxy-2-[[(2S)-2,5-diamino-5-oxo-pentanoyl]amino]propanoyl]amino]hexanoyl]amino]-3-(1H-imidazol-4-yl)propanoyl]amino]-4-carboxy-butanoyl]amino]-4-carboxy-butanoyl]amino]-3-carboxy-propanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-5-oxo-pentanoyl]amino]-4-methylsulfanyl-butanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-4-oxo-butanoyl]amino]hexanoyl]amino]acetyl]amino]-3-carboxy-propanoyl]amino]hexanoyl]amino]-5-[[(1S)-2-amino-1-(carboxymethyl)-2-oxo-ethyl]amino]-5-oxo-pentanoic acid
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C94H139N27O37S
 1
1
IC50 = 18 nM
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CP0967447
(4S)-4-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-5-amino-2-[[(2S)-2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-4-amino-2-[[(2S)-2-[[(2S)-2-[[(2S,3S)-2-amino-3-methyl-pentanoyl]amino]-3-carboxy-propanoyl]amino]-4-carboxy-butanoyl]amino]-4-oxo-butanoyl]amino]propanoyl]amino]-5-guanidino-pentanoyl]amino]-3-hydroxy-propanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-methyl-pentanoyl]amino]-3-carboxy-propanoyl]amino]hexanoyl]amino]-3-phenyl-propanoyl]amino]-5-oxo-pentanoyl]amino]-3-(1H-imidazol-4-yl)propanoyl]amino]-3-carboxy-propanoyl]amino]propanoyl]amino]-5-[[(1S)-1-[[(1S)-1-[[(1S)-2-[[(1S)-2-[[(1S)-4-amino-1-carbamoyl-4-oxo-butyl]amino]-1-[(4-hydroxyphenyl)methyl]-2-oxo-ethyl]amino]-1-(1H-indol-3-ylmethyl)-2-oxo-ethyl]carbamoyl]-3-methylsulfanyl-propyl]carbamoyl]-3-carboxy-propyl]amino]-5-oxo-pentanoic acid
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C123H175N33O40S
 1
1
IC50 = 32 nM
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Biochemical Assays
Compound ID Compound Name Compound Formula
CP0574187
(4S)-4-[[(2S)-2-[[(2S)-4-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S,3S)-2-amino-3-methylpentanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]propanoyl]amino]-4-methylpentanoyl]amino]-4-methylpentanoyl]amino]-4-carboxybutanoyl]amino]-4-oxobutanoyl]amino]propanoyl]amino]-5-[[(2S)-1-[[(2S)-1-[[(2S)-4-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-1,4-diamino-1,4-dioxobutan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-5-oxopentanoic acid
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C79H121N19O26
 1
1 IC50 = 94 nM
CP0967448
(4S)-5-[[(1S)-2-[[(1S)-1-[[(1S)-5-amino-1-[[(1S)-1-[[(1S)-3-amino-1-[[(1S)-2-[[(1S)-1-[[2-[[(1S)-4-amino-1-carbamoyl-4-oxo-butyl]amino]-2-oxo-ethyl]carbamoyl]-4-guanidino-butyl]amino]-1-(carboxymethyl)-2-oxo-ethyl]carbamoyl]-3-oxo-propyl]carbamoyl]-3-carboxy-propyl]carbamoyl]pentyl]carbamoyl]-3-carboxy-propyl]amino]-1-(1H-imidazol-4-ylmethyl)-2-oxo-ethyl]amino]-4-[[(2S)-2-[[(2S)-2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-amino-3-hydroxy-propanoyl]amino]-5-guanidino-pentanoyl]amino]-3-carboxy-propanoyl]amino]hexanoyl]amino]-3-(1H-imidazol-4-yl)propanoyl]amino]-4-carboxy-butanoyl]amino]-5-oxo-pentanoic acid
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C78H125N31O31
 1
1 IC50 = 94 nM
Clinical Information about the Protein
Target 1 ( Angiotensin-converting enzyme 2 (ACE2) )
Target Type Clinical trial Target
Disease 1 Target-related Disease  1
1 Diabetic complication [ICD-11: 5A2Y]
Clinical Trial Drug(s) 1 Clinical Trial Drug  1
1 ORE-1001 Phase 1/2
Diabetic complication
Target 2 ( HUMAN angiotensin-converting enzyme 2 (ACE2) )
Target Type Unknown Type Target
Disease 1 Target-related Disease  1
1 Severe acute respiratory syndrome (SARS) [ICD-11: 1D65]
Investigative Drug(s) 1 Investigative Drug  1
1 N-(2-aminoethyl)-1-aziridine-ethanamine Investigative
Severe acute respiratory syndrome (SARS)