General Information of the Protein
Protein ID
PT01982
Protein Name
Endothelin-converting enzyme 1
Gene Name
ECE1
Sequence
MRGVWPPPVSALLSALGMSTYKRATLDEEDLVDSLSEGDAYPNGLQVNFHSPRSGQRCWAARTQVEKRLVVLVVLLAAGLVACLAALGIQYQTRSPSVCLSEACVSVTSSILSSMDPTVDPCHDFFSYACGGWIKANPVPDGHSRWGTFSNLWEHNQAIIKHLLENSTASVSEAERKAQVYYRACMNETRIEELRAKPLMELIERLGGWNITGPWAKDNFQDTLQVVTAHYRTSPFFSVYVSADSKNSNSNVIQVDQSGLGLPSRDYYLNKTENEKVLTGYLNYMVQLGKLLGGGDEEAIRPQMQQILDFETALANITIPQEKRRDEELIYHKVTAAELQTLAPAINWLPFLNTIFYPVEINESEPIVVYDKEYLEQISTLINTTDRCLLNNYMIWNLVRKTSSFLDQRFQDADEKFMEVMYGTKKTCLPRWKFCVSDTENNLGFALGPMFVKATFAEDSKSIATEIILEIKKAFEESLSTLKWMDEETRKSAKEKADAIYNMIGYPNFIMDPKELDKVFNDYTAVPDLYFENAMRFFNFSWRVTADQLRKAPNRDQWSMTPPMVNAYYSPTKNEIVFPAGILQAPFYTRSSPKALNFGGIGVVVGHELTHAFDDQGREYDKDGNLRPWWKNSSVEAFKRQTECMVEQYSNYSVNGEPVNGRHTLGENIADNGGLKAAYRAYQNWVKKNGAEHSLPTLGLTNNQLFFLGFAQVWCSVRTPESSHEGLITDPHSPSRFRVIGSLSNSKEFSEHFRCPPGSPMNPPHKCEVW
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Organism
Homo sapiens, Human
Protein Classification
Enzyme
>
Protease
>
Metallo protease
>
Metallo protease MAE clan
>
Metallo protease M13 family
Function
Converts big endothelin-1 to endothelin-1.
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Uniprot ID
Primary ID:
P42892

Secondarily ID:
A8K3P1
B4E291
Q14217
Q17RN5
Q2Z2K8
Q58GE7
Q5THM5
Q5THM7
Q5THM8
Q9UJQ6
Q9UPF4
Q9UPM4
Q9Y501
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Ensembl ID
ENSG00000117298
HGNC ID
HGNC:3146
Subcellular Location
Cell membrane
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: CL000011 , CHO
 Cell Line Info 
Compound ID Compound Name Compound Formula
CP0190261
 Compound Info 
2-{2-[(S)-5-(2,4-Difluoro-phenyl)-2-(phosphonomethyl-amino)-pent-4-ynoylamino]-4-methyl-pentanoylamino}-propionic acid
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C21H28F2N3O7P
  1
1
IC50 = 8 nM
 Bioactivity Info 
   TI
   LI
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CP0133532
 Compound Info 
(S)-3-Biphenyl-4-yl-2-[(S)-5-(2-fluoro-phenyl)-2-(phosphonomethyl-amino)-pent-4-ynoylamino]-propionic acid
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C27H26FN2O6P
  1
1
IC50 = 13 nM
 Bioactivity Info 
   TI
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CP0182802
 Compound Info 
(S)-3-Cyclohexyl-2-[(S)-5-(2,4-difluoro-phenyl)-2-(phosphonomethyl-amino)-pent-4-ynoylamino]-propionic acid
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C21H27F2N2O6P
  1
1
IC50 = 14 nM
 Bioactivity Info 
   TI
   LI
   LO
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CP0101004
 Compound Info 
CGS-31,447
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C28H28N5O3P
  1
1
IC50 = 17 nM
 Bioactivity Info 
   TI
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CP0448711
 Compound Info 
(S)-2-[(S)-5-(2-Fluoro-phenyl)-2-(phosphonomethyl-amino)-pent-4-ynoylamino]-3-naphthalen-2-yl-propionic acid
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C25H24FN2O6P
  1
1
IC50 = 25 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0107342
 Compound Info 
[[(2S)-5-(2,4-difluorophenyl)-1-oxo-1-[2-(4-phenylphenyl)ethylamino]pent-4-yn-2-yl]amino]methylphosphonic acid
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C26H25F2N2O4P
  1
1
IC50 = 28 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0336734
 Compound Info 
(S)-5-(2-Fluoro-phenyl)-2-[(S)-5-(2-fluoro-phenyl)-2-(phosphonomethyl-amino)-pent-4-ynoylamino]-pent-4-ynoic acid
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C23H21F2N2O6P
  1
1
IC50 = 28 nM
 Bioactivity Info 
   TI
   LI
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CP0362349
 Compound Info 
[[(2S)-5-(2-fluorophenyl)-1-oxo-1-[2-(4-phenylphenyl)ethylamino]pent-4-yn-2-yl]amino]methylphosphonic acid
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C26H26FN2O4P
  1
1
IC50 = 33 nM
 Bioactivity Info 
   TI
   LI
   LO
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CP0286476
 Compound Info 
[[(2S)-5-(2,4-difluorophenyl)-1-(2-naphthalen-1-ylethylamino)-1-oxopent-4-yn-2-yl]amino]methylphosphonic acid
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C24H23F2N2O4P
  1
1
IC50 = 34 nM
 Bioactivity Info 
   TI
   LI
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CP0357578
 Compound Info 
[[(2S)-1-[2-(4-bromophenyl)ethylamino]-5-(2,4-difluorophenyl)-1-oxopent-4-yn-2-yl]amino]methylphosphonic acid
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C20H20BrF2N2O4P
  1
1
IC50 = 43 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0037872
 Compound Info 
(S)-2-[(S)-5-(2,4-Difluoro-phenyl)-2-(phosphonomethyl-amino)-pent-4-ynoylamino]-4-methyl-pentanoic acid
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C18H23F2N2O6P
  1
1
IC50 = 51 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0217898
 Compound Info 
[[(2S)-5-(2,4-difluorophenyl)-1-(2-naphthalen-2-ylethylamino)-1-oxopent-4-yn-2-yl]amino]methylphosphonic acid
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C24H23F2N2O4P
  1
1
IC50 = 53 nM
 Bioactivity Info 
   TI
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CP0167269
 Compound Info 
(S)-2-[(S)-5-(2-Fluoro-phenyl)-2-(phosphonomethyl-amino)-pent-4-ynoylamino]-3-phenyl-propionic acid
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C21H22FN2O6P
  1
1
IC50 = 56 nM
 Bioactivity Info 
   TI
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CP0309874
 Compound Info 
[[(2S)-1-[[3-(2-aminoethyl)-1H-indol-2-yl]amino]-5-(2-fluorophenyl)-1-oxopent-4-yn-2-yl]amino]methylphosphonic acid
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C22H24FN4O4P
  1
1
IC50 = 76 nM
 Bioactivity Info 
   TI
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CP0357542
 Compound Info 
2-[(3S)-3-[[(2S)-5-(2,4-difluorophenyl)-2-(phosphonomethylamino)pent-4-ynoyl]amino]-2-oxo-4,5-dihydro-3H-1-benzazepin-1-yl]acetic acid
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C24H24F2N3O7P
  1
1
IC50 = 82 nM
 Bioactivity Info 
   TI
   LI
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CP0183199
 Compound Info 
(S)-2-[(S)-5-(2-Fluoro-phenyl)-2-(phosphonomethyl-amino)-pent-4-ynoylamino]-3-methyl-butyric acid
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C17H22FN2O6P
  1
1
IC50 = 110 nM
 Bioactivity Info 
   TI
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CP0183200
 Compound Info 
[[(2S)-1-[2-(4-bromophenyl)ethylamino]-5-(2-fluorophenyl)-1-oxopent-4-yn-2-yl]amino]methylphosphonic acid
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C20H21BrFN2O4P
  1
1
IC50 = 110 nM
 Bioactivity Info 
   TI
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CP0184322
 Compound Info 
[[(2S)-5-(2,4-difluorophenyl)-1-oxo-1-(2-phenylethylamino)pent-4-yn-2-yl]amino]methylphosphonic acid
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C20H21F2N2O4P
  1
1
IC50 = 110 nM
 Bioactivity Info 
   TI
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CP0285033
 Compound Info 
[[(2S)-1-[[3-(2-aminoethyl)-1H-indol-2-yl]amino]-5-(2,4-difluorophenyl)-1-oxopent-4-yn-2-yl]amino]methylphosphonic acid
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C22H23F2N4O4P
  1
1
IC50 = 111 nM
 Bioactivity Info 
   TI
   LI
   LO
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CP0037870
 Compound Info 
(S)-2-[(S)-5-(2-Fluoro-phenyl)-2-(phosphonomethyl-amino)-pent-4-ynoylamino]-4-methyl-pentanoic acid
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C18H24FN2O6P
  1
1
IC50 = 120 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0048197
 Compound Info 
[[(2S)-5-(2-fluorophenyl)-1-(2-naphthalen-1-ylethylamino)-1-oxopent-4-yn-2-yl]amino]methylphosphonic acid
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C24H24FN2O4P
  1
1
IC50 = 130 nM
 Bioactivity Info 
   TI
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CP0167270
 Compound Info 
[[(2S)-5-(2,4-difluorophenyl)-1-(3-methylbutylamino)-1-oxopent-4-yn-2-yl]amino]methylphosphonic acid
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C17H23F2N2O4P
  1
1
IC50 = 140 nM
 Bioactivity Info 
   TI
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CP0284970
 Compound Info 
[[(2S)-5-(2,4-difluorophenyl)-1-oxo-1-(3-phenylpropylamino)pent-4-yn-2-yl]amino]methylphosphonic acid
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C21H23F2N2O4P
  1
1
IC50 = 150 nM
 Bioactivity Info 
   TI
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CP0301536
 Compound Info 
[[(1S)-4-(2-fluorophenyl)-1-(2H-tetrazol-5-yl)but-3-ynyl]amino]methylphosphonic acid
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C12H13FN5O3P
  1
1
IC50 = 150 nM
 Bioactivity Info 
   TI
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CP0175778
 Compound Info 
({(S)-4-(2,4-Difluoro-phenyl)-1-[2-(3,4-dimethoxy-phenyl)-ethylcarbamoyl]-but-3-ynylamino}-methyl)-phosphonic acid
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C22H25F2N2O6P
  1
1
IC50 = 160 nM
 Bioactivity Info 
   TI
   LI
   LO
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CP0133531
 Compound Info 
(S)-5-(2,4-Difluoro-phenyl)-2-(phosphonomethyl-amino)-pent-4-ynoic acid
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C12H12F2NO5P
  1
1
IC50 = 170 nM
 Bioactivity Info 
   TI
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CP0208567
 Compound Info 
[[(2S)-5-(2-fluorophenyl)-1-oxo-1-(2-phenylethylamino)pent-4-yn-2-yl]amino]methylphosphonic acid
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C20H22FN2O4P
  1
1
IC50 = 230 nM
 Bioactivity Info 
   TI
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CP0349167
 Compound Info 
(S)-2-[(S)-5-(2-Fluoro-phenyl)-2-(phosphonomethyl-amino)-pent-4-ynoylamino]-4-methylsulfanyl-butyric acid
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C17H22FN2O6PS
  1
1
IC50 = 230 nM
 Bioactivity Info 
   TI
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CP0255899
 Compound Info 
(S)-5-(2-Fluoro-phenyl)-2-(phosphonomethyl-amino)-pent-4-ynoic acid
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C12H13FNO5P
  1
1
IC50 = 240 nM
 Bioactivity Info 
   TI
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CP0228833
 Compound Info 
[[(2S)-1-(benzylamino)-5-(2-fluorophenyl)-1-oxopent-4-yn-2-yl]amino]methylphosphonic acid
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C19H20FN2O4P
  1
1
IC50 = 250 nM
 Bioactivity Info 
   TI
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CP0286276
 Compound Info 
[[(2S)-5-(2,4-difluorophenyl)-1-oxo-1-(2-pyridin-2-ylethylamino)pent-4-yn-2-yl]amino]methylphosphonic acid
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C19H20F2N3O4P
  1
1
IC50 = 310 nM
 Bioactivity Info 
   TI
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CP0037918
 Compound Info 
(S)-2-[(S)-5-(3-Fluoro-phenyl)-2-(phosphonomethyl-amino)-pent-4-ynoylamino]-4-methyl-pentanoic acid
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C18H24FN2O6P
  1
1
IC50 = 400 nM
 Bioactivity Info 
   TI
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CP0087775
 Compound Info 
CGS-26303
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C16H18N5O3P
  1
1
IC50 = 410 nM
 Bioactivity Info 
   TI
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CP0358558
 Compound Info 
(S)-4-Methyl-2-[(S)-5-phenyl-2-(phosphonomethyl-amino)-pent-4-ynoylamino]-pentanoic acid
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C18H25N2O6P
  1
1
IC50 = 510 nM
 Bioactivity Info 
   TI
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CP0062600
 Compound Info 
[[(1S)-4-phenyl-1-(2H-tetrazol-5-yl)but-3-ynyl]amino]methylphosphonic acid
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C12H14N5O3P
  1
1
IC50 = 590 nM
 Bioactivity Info 
   TI
   LI
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CP0044595
 Compound Info 
(3R,4R,5R,6S)-3,4,5-trihydroxy-6-methyl-tetrahydro-2H-pyran-2-yl hydrogen (S)-1-((S)-1-(1H-indol-3-yl)-3-oxobutan-2-ylamino)-4-methyl-1-oxopentan-2-ylphosphoramidate
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C23H34N3O10P
  1
1
IC50 = 1200 nM
 Bioactivity Info 
   TI
   LI
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CP0189925
 Compound Info 
(S)-2-[(S)-5-(2-Chloro-phenyl)-2-(phosphonomethyl-amino)-pent-4-ynoylamino]-4-methyl-pentanoic acid
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C18H24ClN2O6P
  1
1
IC50 = 4300 nM
 Bioactivity Info 
   TI
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Cell Line ID: CL000053 , COS-7
 Cell Line Info 
Cell Line ID: CL000749 , HUVEC-C
 Cell Line Info 
Cell Line ID: CL000031 , MDCK
 Cell Line Info 
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0102761
 Compound Info 
(2S,4R)-4-Acetylsulfanyl-2-(2,4,5-trifluoro-benzyloxymethyl)-pyrrolidine-1-carboxylic acid 2,3-dihydro-benzo[1,4]dioxin-5-yl ester
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C23H22F3NO6S
  1
1 IC50 = 6.9 nM
CP0190261
 Compound Info 
2-{2-[(S)-5-(2,4-Difluoro-phenyl)-2-(phosphonomethyl-amino)-pent-4-ynoylamino]-4-methyl-pentanoylamino}-propionic acid
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C21H28F2N3O7P
  1
1 IC50 = 8 nM
CP0051845
 Compound Info 
(3R,5S)-5-{[(2,5-difluorobenzyl)amino]methyl}-1-(5-propylpyrimidin-2-yl)pyrrolidine-3-thiol
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C19H24F2N4S
  1
1 IC50 = 10.4 nM
CP0057474
 Compound Info 
(2S,4R)-4-Mercapto-2-(2,4,5-trifluoro-benzyloxymethyl)-pyrrolidine-1-carboxylic acid 2-methoxycarbonyl-phenyl ester
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C13H13NO3
  1
1 IC50 = 12 nM
CP0102763
 Compound Info 
propan-2-yl (4R)-2-[[(2,5-difluorophenyl)methylamino]methyl]-4-sulfanylpyrrolidine-1-carboxylate
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C16H22F2N2O2S
  1
1 IC50 = 16 nM
CP0101004
 Compound Info 
CGS-31,447
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C28H28N5O3P
  2
1 IC50 = 17 nM
2 Ki = 10.8 nM
CP0044595
 Compound Info 
(3R,4R,5R,6S)-3,4,5-trihydroxy-6-methyl-tetrahydro-2H-pyran-2-yl hydrogen (S)-1-((S)-1-(1H-indol-3-yl)-3-oxobutan-2-ylamino)-4-methyl-1-oxopentan-2-ylphosphoramidate
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C23H34N3O10P
  4
1 IC50 = 17 nM
2 IC50 = 800 nM
3 IC50 = 1200 nM
4 IC50 = 2000 nM
CP0102762
 Compound Info 
(2S,4R)-4-Benzoylsulfanyl-2-(2,4,5-trifluoro-benzyloxymethyl)-pyrrolidine-1-carboxylic acid 2,3-dihydro-benzo[1,4]dioxin-5-yl ester
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C28H24F3NO6S
  1
1 IC50 = 49.7 nM
CP0037872
 Compound Info 
(S)-2-[(S)-5-(2,4-Difluoro-phenyl)-2-(phosphonomethyl-amino)-pent-4-ynoylamino]-4-methyl-pentanoic acid
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C18H23F2N2O6P
  1
1 IC50 = 51 nM
CP0146486
 Compound Info 
(4R)-N'-methyl-N'-[(4-methylbenzene)sulfonyl]-1-(naphthalene-2-sulfonyl)-4-sulfanylpyrrolidine-2-carbohydrazide
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C23H25N3O5S3
  1
1 IC50 = 61.3 nM
CP0057472
 Compound Info 
methyl 2-[[2-[methyl-[(4R)-1-naphthalen-2-ylsulfonyl-4-sulfanylpyrrolidine-2-carbonyl]amino]acetyl]amino]benzoate
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C26H27N3O6S2
  1
1 IC50 = 80.8 nM
CP0301536
 Compound Info 
[[(1S)-4-(2-fluorophenyl)-1-(2H-tetrazol-5-yl)but-3-ynyl]amino]methylphosphonic acid
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C12H13FN5O3P
  1
1 IC50 = 150 nM
CP0087775
 Compound Info 
CGS-26303
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C16H18N5O3P
  1
1 IC50 = 410 nM
CP0092092
 Compound Info 
(2S)-2-[(2R)-2-[(1R)-2,3-dihydro-1H-inden-1-yl]-3-sulfanylpropanamido]-3-(1H-indol-3-yl)propanoic acid
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C23H24N2O3S
  1
1 Ki = 26 nM
CP0197969
 Compound Info 
2-(2-Indan-1-yl-3-mercapto-propionylamino)-3-(1H-indol-3-yl)-propionic acid
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C23H24N2O3S
  1
1 Ki = 100 nM
Clinical Information about the Protein
Target 1 ( Endothelin-converting enzyme 1 (ECE1) )
Target Type Literature-reported Target