General Information of the Protein
Protein ID
PT02017
Protein Name
KiSS-1 receptor
Secondarily
Protein Name
G-protein coupled receptor 54
G-protein coupled receptor OT7T175
Hypogonadotropin-1
Kisspeptins receptor
Metastin receptor
Gene Name
KISS1R
Secondarily
Gene Name
AXOR12
GPR54
Sequence
MHTVATSGPNASWGAPANASGCPGCGANASDGPVPSPRAVDAWLVPLFFAALMLLGLVGNSLVIYVICRHKPMRTVTNFYIANLAATDVTFLLCCVPFTALLYPLPGWVLGDFMCKFVNYIQQVSVQATCATLTAMSVDRWYVTVFPLRALHRRTPRLALAVSLSIWVGSAAVSAPVLALHRLSPGPRAYCSEAFPSRALERAFALYNLLALYLLPLLATCACYAAMLRHLGRVAVRPAPADSALQGQVLAERAGAVRAKVSRLVAAVVLLFAACWGPIQLFLVLQALGPAGSWHPRSYAAYALKTWAHCMSYSNSALNPLLYAFLGSHFRQAFRRVCPCAPRRPRRPRRPGPSDPAAPHAELLRLGSHPAPARAQKPGSSGLAARGLCVLGEDNAPL
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Organism
Homo sapiens, Human
Protein Classification
Membrane receptor
>
Family A G protein-coupled receptor
>
Peptide receptor (family A GPCR)
>
Short peptide receptor (family A GPCR)
>
RF amide receptor
Function
Receptor for metastin (kisspeptin-54 or kp-54), a C-terminally amidated peptide of KiSS1. KiSS1 is a metastasis suppressor protein that suppresses metastases in malignant melanomas and in some breast carcinomas without affecting tumorigenicity. The metastasis suppressor properties may be mediated in part by cell cycle arrest and induction of apoptosis in malignant cells. The receptor is essential for normal gonadotropin-released hormone physiology and for puberty. The hypothalamic KiSS1/KISS1R system is a pivotal factor in central regulation of the gonadotropic axis at puberty and in adulthood. The receptor is also probably involved in the regulation and fine-tuning of trophoblast invasion generated by the trophoblast itself. Analysis of the transduction pathways activated by the receptor identifies coupling to phospholipase C and intracellular calcium release through pertussis toxin-insensitive G(q) proteins.
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Uniprot ID
Primary ID:
Q969F8

Secondarily ID:
A5D8U2
B2RTV1
Q96QG0
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Ensembl ID
ENSG00000116014
HGNC ID
HGNC:4510
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
Compound ID Compound Name Compound Formula
CP0567389
(2S)-N-[(2S)-1-[[(2S)-1-amino-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-5-[(N'-methylcarbamimidoyl)amino]-1-oxopentan-2-yl]-2-[[[(2S)-2-[3-(1H-indol-3-yl)propanoylamino]-3-phenylpropanoyl]amino]carbamoylamino]-4-methylpentanamide
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C45H58N12O6
 1
1
EC50 = 0.022 nM
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CP0474394
N-[(2S)-1-[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-5-[(N'-methylcarbamimidoyl)amino]-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]carbamoyl]hydrazinyl]-1-oxo-3-phenylpropan-2-yl]benzamide
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C41H53N11O6
 1
1
EC50 = 0.024 nM
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CP0571054
N-[(2S)-1-[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-5-[(N'-methylcarbamimidoyl)amino]-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]carbamoyl]hydrazinyl]-1-oxo-3-phenylpropan-2-yl]cyclopropanecarboxamide
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C38H53N11O6
 1
1
EC50 = 0.028 nM
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CP0438590
N-[(2S)-1-[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-5-[(N'-methylcarbamimidoyl)amino]-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]carbamoyl]hydrazinyl]-1-oxo-3-phenylpropan-2-yl]pyridine-2-carboxamide
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C40H52N12O6
 1
1
EC50 = 0.037 nM
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CP0367958
(2S)-2-[[(2S)-2-[[(2R)-2-amino-3-(4-hydroxyphenyl)propanoyl]amino]-3-(1H-indol-3-yl)propanoyl]amino]-N-[(2S)-1-[[(2S)-1-[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]amino]-5-[(N'-methylcarbamimidoyl)amino]-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]carbamoyl]hydrazinyl]-1-oxo-3-phenylpropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]butanediamide
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C59H78N16O12
 2
1
EC50 = 0.057 nM
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2
Ki = 0.044 nM
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CP0534680
(2S)-N-[(2S)-1-[[(2S)-1-amino-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-5-[(N'-methylcarbamimidoyl)amino]-1-oxopentan-2-yl]-4-methyl-2-[[[(2S)-2-(2-methylpropanoylamino)-3-phenylpropanoyl]amino]carbamoylamino]pentanamide
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C38H55N11O6
 1
1
EC50 = 0.058 nM
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CP0352243
N-[(2S)-1-[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-5-[(N'-methylcarbamimidoyl)amino]-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]carbamoyl]hydrazinyl]-1-oxo-3-phenylpropan-2-yl]pyridine-4-carboxamide
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C40H52N12O6
 1
1
EC50 = 0.068 nM
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CP0039237
(2S)-2-[(2S)-2-[(2S)-2-[(2S)-2-amino-3-(4-hydroxyphenyl)propanamido]butanediamido]-3-(1H-indol-3-yl)propanamido]-N-[(1S)-1-{[(1S)-1-[({[(1S)-1-{[(1S)-4-carbamimidamido-1-{[(1S)-1-carbamoyl-2-phenylethyl]carbamoyl}butyl]carbamoyl}-3-methylbutyl]carbamoyl}methyl)carbamoyl]-2-phenylethyl]carbamoyl}-2-hydroxyethyl]butanediamide
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C63H83N17O14
 7
1
EC50 = 0.087 nM
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2
EC50 = 0.24 nM
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3
EC50 = 0.96 nM
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4
IC50 = 0.07 nM
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5
IC50 = 8510 nM
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6
Ki = 0.035 nM
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7
Ki = 0.039 nM
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CP0474393
N-[(2S)-1-[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-5-[(N'-methylcarbamimidoyl)amino]-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]carbamoyl]hydrazinyl]-1-oxo-3-phenylpropan-2-yl]furan-3-carboxamide
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C39H51N11O7
 1
1
EC50 = 0.11 nM
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CP0477053
N-[(2S)-1-[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-5-[(N'-methylcarbamimidoyl)amino]-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]carbamoyl]hydrazinyl]-1-oxo-3-phenylpropan-2-yl]cyclohexanecarboxamide
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C41H59N11O6
 1
1
EC50 = 0.12 nM
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CP0474396
(2S)-N-[(2S)-1-[[(2S)-1-[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]amino]-5-[(N'-methylcarbamimidoyl)amino]-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]carbamoyl]hydrazinyl]-1-oxo-3-phenylpropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]-2-[3-(1H-indol-3-yl)propanoylamino]butanediamide
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C50H68N14O10
 1
1
EC50 = 0.13 nM
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CP0477052
(2S)-N-[(2S)-1-[[(2S)-1-amino-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-5-[(N'-methylcarbamimidoyl)amino]-1-oxopentan-2-yl]-4-methyl-2-[[[(2S)-3-phenyl-2-(propanoylamino)propanoyl]amino]carbamoylamino]pentanamide
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C37H53N11O6
 1
1
EC50 = 0.13 nM
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CP0533850
N-[(2S)-1-[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-5-[(N'-methylcarbamimidoyl)amino]-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]carbamoyl]hydrazinyl]-1-oxo-3-phenylpropan-2-yl]pyridine-3-carboxamide
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C40H52N12O6
 1
1
EC50 = 0.16 nM
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CP0575492
(2S)-N-[(2S)-1-[[(2S)-1-[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]amino]-5-[(N'-methylcarbamimidoyl)amino]-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]carbamoyl]hydrazinyl]-1-oxo-3-phenylpropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]-2-(3-phenylpropanoylamino)butanediamide
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C48H67N13O10
 1
1
EC50 = 0.17 nM
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CP0557278
N-[(2S)-1-[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-5-[(N'-methylcarbamimidoyl)amino]-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]carbamoyl]hydrazinyl]-1-oxo-3-phenylpropan-2-yl]-1H-pyrrole-2-carboxamide
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C39H52N12O6
 1
1
EC50 = 0.23 nM
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CP0477055
N-[(2S)-1-[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-5-[(N'-methylcarbamimidoyl)amino]-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]carbamoyl]hydrazinyl]-1-oxo-3-phenylpropan-2-yl]-1H-imidazole-5-carboxamide
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C38H51N13O6
 1
1
EC50 = 0.24 nM
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CP0083577
(2S)-2-[[(2R)-2-[[(2R)-2-amino-3-(4-hydroxyphenyl)propanoyl]amino]-3-pyridin-4-ylpropanoyl]amino]-N-[(2S)-1-[[(2S)-1-[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]amino]-5-[(N'-methylcarbamimidoyl)amino]-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]carbamoyl]hydrazinyl]-1-oxo-3-phenylpropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]butanediamide
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C56H76N16O12
 5
1
EC50 = 0.27 nM
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2
EC50 = 2.6 nM
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3
IC50 = 8.94 nM
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4
Ki = 0.089 nM
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5
Ki = 0.11 nM
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CP0477054
(2S)-N-[(2S)-1-[[(2S)-1-amino-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-5-[(N'-methylcarbamimidoyl)amino]-1-oxopentan-2-yl]-4-methyl-2-[[[(2S)-3-phenyl-2-[(2-phenylacetyl)amino]propanoyl]amino]carbamoylamino]pentanamide
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C42H55N11O6
 1
1
EC50 = 0.27 nM
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CP0158503
(2R,3E)-N-[(1S)-4-carbamimidamido-1-{[(1S)-1-carbamoyl-2-(1H-indol-3-yl)ethyl]carbamoyl}butyl]-5-[(2S)-2-[(4-fluorophenyl)formamido]-3-phenylpropanamido]-2-(2-methylpropyl)pent-3-enamide
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C42H52FN9O5
 2
1
EC50 = 0.3 nM
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2
IC50 = 0.12 nM
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CP0908452
(S)-N1-((8S,11S,17S,20S,21R)-8-((S)-1-amino-3-(1H-indol-3-yl)-1-oxopropan-2-ylcarbamoyl)-17-benzyl-21-hydroxy-3-imino-11-isobutyl-10,13,16,19-tetraoxo-2,4,9,12,14,15,18-heptaazadocosan-20-yl)-2-((R)-2-(3-(4-hydroxyphenyl)propanamido)-3-(1H-indol-3-yl)propanamido)succinamide
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C62H80N16O12
 2
1
EC50 = 0.3 nM
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2
Ki = 0.039 nM
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CP0920598
(S)-N1-((8S,11S,17S,20S)-8-((S)-1-amino-3-(1H-indol-3-yl)-1-oxopropan-2-ylcarbamoyl)-17-benzyl-3-imino-11-isobutyl-21-methyl-10,13,16,19-tetraoxo-2,4,9,12,14,15,18-heptaazadocosan-20-yl)-2-((R)-2-((R)-2-amino-3-(4-hydroxyphenyl)propanamido)-3-(1H-indol-3-yl)propanamido)succinamide
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C63H83N17O11
 2
1
EC50 = 0.31 nM
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2
Ki = 0.028 nM
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CP0875171
(S)-2-((R)-2-((R)-2-acetamido-3-(4-hydroxyphenyl)propanamido)-3-(1H-indol-3-yl)propanamido)-N1-((8S,11S,17S,20S,21R)-8-((S)-1-amino-3-(1H-indol-3-yl)-1-oxopropan-2-ylcarbamoyl)-17-benzyl-21-hydroxy-3-imino-11-isobutyl-10,13,16,19-tetraoxo-2,4,9,12,14,15,18-heptaazadocosan-20-yl)succinamide
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C64H83N17O13
 2
1
EC50 = 0.33 nM
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2
Ki = 0.036 nM
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CP0485519
(2S)-2-[[[(2S)-2-acetamido-3-phenylpropanoyl]amino]carbamoylamino]-N-[(2S)-1-[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]amino]-5-[(N'-methylcarbamimidoyl)amino]-1-oxopentan-2-yl]-4-methylpentanamide
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C34H50N10O6
 1
1
EC50 = 0.33 nM
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CP0158502
(2R,4S)-N-[(1S)-4-carbamimidamido-1-{[(1S)-1-carbamoyl-2-(1H-indol-3-yl)ethyl]carbamoyl}butyl]-5-[(2S)-2-[(4-fluorophenyl)formamido]-3-phenylpropanamido]-4-hydroxy-2-(2-methylpropyl)pentanamide
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C42H54FN9O6
 2
1
EC50 = 0.36 nM
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2
IC50 = 0.24 nM
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CP0851167
(S)-N1-((8S,11S,17S,20S,21R)-8-((S)-1-amino-3-(1H-indol-3-yl)-1-oxopropan-2-ylcarbamoyl)-17-benzyl-21-hydroxy-3-imino-11-isobutyl-10,13,16,19-tetraoxo-2,4,9,12,14,15,18-heptaazadocosan-20-yl)-2-((R)-2-((R)-2-benzamido-3-(4-hydroxyphenyl)propanamido)-3-(1H-indol-3-yl)propanamido)succinamide
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C69H85N17O13
 2
1
EC50 = 0.44 nM
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2
Ki = 0.027 nM
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CP0868247
(S)-2-((S)-2-((S)-4-amino-2-((S)-2-amino-3-(4-hydroxyphenyl)propanamido)-4-oxobutanamido)-3-(1H-indol-3-yl)propanamido)-N1-((6S,9S,15S,18S)-1-amino-6-((S)-1-amino-3-(1H-indol-3-yl)-1-oxopropan-2-ylcarbamoyl)-15-benzyl-19-hydroxy-1-imino-9-isobutyl-8,11,14,17-tetraoxo-2,7,10,13,16-pentaazanonadecan-18-yl)succinamide
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C65H84N18O14
 2
1
EC50 = 0.44 nM
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2
Ki = 0.026 nM
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CP0210913
(2S)-N-[(1S)-4-carbamimidamido-1-{[(1S)-1-carbamoyl-2-(1H-indol-3-yl)ethyl]carbamoyl}butyl]-2-{2-[(2S)-2-[(4-fluorophenyl)formamido]-3-phenylpropanamido]acetamido}-4-methylpentanamide
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C41H51FN10O6
 3
1
EC50 = 0.45 nM
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2
EC50 = 0.69 nM
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3
IC50 = 0.71 nM
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CP0851170
2-((2S,5S,8S,11R,14R)-11-((1H-indol-3-yl)methyl)-14-amino-2-benzyl-5-(hydroxymethyl)-15-(4-hydroxyphenyl)-8-methyl-4,7,10,13-tetraoxo-3,6,9,12-tetraazapentadecane)-N-((S)-1-((S)-1-((S)-1-amino-3-(1H-indol-3-yl)-1-oxopropan-2-ylamino)-5-(3-methylguanidino)-1-oxopentan-2-ylamino)-4-methyl-1-oxopentan-2-yl)hydrazinecarboxamide
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C60H78N16O11
 1
1
EC50 = 0.49 nM
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CP0868245
(S)-N1-((8S,11S,17S,20S)-8-((S)-1-amino-3-(1H-indol-3-yl)-1-oxopropan-2-ylcarbamoyl)-17-benzyl-21-hydroxy-3-imino-11-isobutyl-10,13,16,19-tetraoxo-2,4,9,12,14,15,18-heptaazahenicosan-20-yl)-2-((R)-2-((R)-2-amino-3-(4-hydroxyphenyl)propanamido)-3-(1H-indol-3-yl)propanamido)succinamide
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C61H79N17O12
 2
1
EC50 = 0.51 nM
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2
Ki = 0.037 nM
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CP0865107
(S)-N1-((8S,11S,17S,20S)-8-((S)-1-amino-3-(1H-indol-3-yl)-1-oxopropan-2-ylcarbamoyl)-17-benzyl-3-imino-21-(1H-indol-3-yl)-11-isobutyl-10,13,16,19-tetraoxo-2,4,9,12,14,15,18-heptaazahenicosan-20-yl)-2-((R)-2-((R)-2-amino-3-(4-hydroxyphenyl)propanamido)-3-(pyridin-4-yl)propanamido)succinamide
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C66H82N18O11
 1
1
EC50 = 0.59 nM
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CP0533851
N-[(2S)-1-[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]amino]-5-[(N'-methylcarbamimidoyl)amino]-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]carbamoyl]hydrazinyl]-1-oxo-3-phenylpropan-2-yl]benzamide
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C39H52N10O6
 1
1
EC50 = 0.6 nM
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CP0578237
(2S)-N-[(2S)-1-[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]amino]-5-[(N'-methylcarbamimidoyl)amino]-1-oxopentan-2-yl]-2-[[[(2S)-2-[3-(1H-indol-3-yl)propanoylamino]-3-phenylpropanoyl]amino]carbamoylamino]-4-methylpentanamide
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C43H57N11O6
 1
1
EC50 = 0.62 nM
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CP0848309
2-((2S,5S,8S,11R,14R)-11-((1H-indol-3-yl)methyl)-14-amino-2-benzyl-5-((R)-1-hydroxyethyl)-15-(4-hydroxyphenyl)-8-methyl-4,7,10,13-tetraoxo-3,6,9,12-tetraazapentadecane)-N-((S)-1-((S)-1-((S)-1-amino-3-(1H-indol-3-yl)-1-oxopropan-2-ylamino)-5-(3-methylguanidino)-1-oxopentan-2-ylamino)-4-methyl-1-oxopentan-2-yl)hydrazinecarboxamide
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C61H80N16O11
 1
1
EC50 = 0.63 nM
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CP0922198
2-((2S,5S,8S,11R,14R)-11-((1H-indol-3-yl)methyl)-14-amino-2-benzyl-8-ethyl-5-(hydroxymethyl)-15-(4-hydroxyphenyl)-4,7,10,13-tetraoxo-3,6,9,12-tetraazapentadecane)-N-((S)-1-((S)-1-((S)-1-amino-3-(1H-indol-3-yl)-1-oxopropan-2-ylamino)-5-(3-methylguanidino)-1-oxopentan-2-ylamino)-4-methyl-1-oxopentan-2-yl)hydrazinecarboxamide
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C61H80N16O11
 2
1
EC50 = 0.64 nM
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2
Ki = 0.12 nM
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CP0868246
(2S)-2-({N'-[(2S)-2-[(2S)-2-[(2S)-2-[(2R)-2-[(2R)-2-amino-3-(4-hydroxyphenyl)propanamido]-3-(pyridin-4-yl)propanamido]propanamido]-3-hydroxypropanamido]-3-phenylpropanoyl]hydrazinecarbonyl}amino)-N-[(1S)-1-{[(1S)-1-carbamoyl-2-(1H-indol-3-yl)ethyl]carbamoyl}-4-(1-methylcarbamimidamido)butyl]-4-methylpentanamide
   Show/Hide
C57H76N16O11
 2
1
EC50 = 0.7 nM
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2
Ki = 0.2 nM
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CP0913533
(S)-2-((R)-2-((R)-2-acetamido-3-(4-hydroxyphenyl)propanamido)-3-(pyridin-4-yl)propanamido)-N1-((8S,11S,17S,20S,21R)-8-((S)-1-amino-3-(1H-indol-3-yl)-1-oxopropan-2-ylcarbamoyl)-17-benzyl-21-hydroxy-3-imino-11-isobutyl-10,13,16,19-tetraoxo-2,4,9,12,14,15,18-heptaazadocosan-20-yl)succinamide
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C61H81N17O13
 2
1
EC50 = 0.75 nM
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2
Ki = 0.089 nM
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CP0435595
(2S)-N-[(1S)-4-carbamimidamido-1-{[(1S)-1-carbamoyl-2-(1H-indol-3-yl)ethyl]carbamoyl}butyl]-4-methyl-2-{2-[(2S)-3-phenyl-2-(pyridin-2-ylformamido)propanamido]acetamido}pentanamide
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C40H51N11O6
 1
1
EC50 = 0.8 nM
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CP0871691
(S)-N1-((8S,11S,17S,20S,21R)-8-((S)-1-amino-3-(1H-indol-3-yl)-1-oxopropan-2-ylcarbamoyl)-17-benzyl-21-hydroxy-3-imino-11-isobutyl-10,13,16,19-tetraoxo-2,4,9,12,14,15,18-heptaazadocosan-20-yl)-2-((R)-2-((R)-2-butyramido-3-(4-hydroxyphenyl)propanamido)-3-(1H-indol-3-yl)propanamido)succinamide
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C66H87N17O13
 1
1
EC50 = 0.8 nM
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CP0908491
(S)-N1-((8S,11S,17S,20S,21R)-8-((S)-1-amino-3-(1H-indol-3-yl)-1-oxopropan-2-ylcarbamoyl)-17-benzyl-21-hydroxy-3-imino-11-isobutyl-10,13,16,19-tetraoxo-2,4,9,12,14,15,18-heptaazadocosan-20-yl)-2-((R)-2-((R)-2-(cyclopropanecarboxamido)-3-(4-hydroxyphenyl)propanamido)-3-(1H-indol-3-yl)propanamido)succinamide
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C66H85N17O13
 2
1
EC50 = 0.82 nM
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2
Ki = 0.034 nM
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CP0858417
(S)-N1-((8S,11S,17S,20S)-8-((S)-1-amino-3-(1H-indol-3-yl)-1-oxopropan-2-ylcarbamoyl)-17-benzyl-21-hydroxy-3-imino-11-isobutyl-10,13,16,19-tetraoxo-2,4,9,12,14,15,18-heptaazahenicosan-20-yl)-2-((R)-2-((R)-2-amino-3-(4-hydroxyphenyl)propanamido)-3-(pyridin-4-yl)propanamido)succinamide
   Show/Hide
C58H77N17O12
 2
1
EC50 = 0.87 nM
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2
Ki = 0.074 nM
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CP0557279
(2S)-N-[(2S)-1-[[(2S)-1-amino-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-5-[(N'-methylcarbamimidoyl)amino]-1-oxopentan-2-yl]-2-[[[(2S)-2-(benzylamino)-3-phenylpropanoyl]amino]carbamoylamino]-4-methylpentanamide
   Show/Hide
C41H55N11O5
 1
1
EC50 = 0.89 nM
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CP0908453
(S)-2-((R)-2-((R)-2-acetamido-3-(4-hydroxyphenyl)propanamido)-3-(1H-indol-3-yl)propanamido)-N1-((8S,11S,17S,20S,21R)-8-((S)-1-amino-1-oxo-3-phenylpropan-2-ylcarbamoyl)-17-benzyl-21-hydroxy-3-imino-11-isobutyl-10,13,16,19-tetraoxo-2,4,9,12,14,15,18-heptaazadocosan-20-yl)succinamide
   Show/Hide
C62H82N16O13
 2
1
EC50 = 0.94 nM
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2
Ki = 0.038 nM
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CP0445746
(2S)-N-[(1S)-4-carbamimidamido-1-{[(1S)-1-carbamoyl-2-(1H-indol-3-yl)ethyl]carbamoyl}butyl]-2-{2-[(2S)-2-{[4-(acetamidomethyl)phenyl]formamido}-3-phenylpropanamido]acetamido}-4-methylpentanamide
   Show/Hide
C44H57N11O7
 1
1
EC50 = 0.99 nM
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CP0463211
(2S)-N-[(1S)-4-carbamimidamido-1-{[(1S)-1-carbamoyl-2-(1H-indol-3-yl)ethyl]carbamoyl}butyl]-4-methyl-2-{2-[(2S)-3-phenyl-2-(phenylformamido)propanamido]acetamido}pentanamide
   Show/Hide
C41H52N10O6
 1
1
EC50 = 0.99 nM
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CP0898490
(2S)-N-[(1S)-4-carbamimidamido-1-{[(1S)-1-carbamoyl-2-(1H-indol-3-yl)ethyl]carbamoyl}butyl]-4-methyl-2-{2-[(2S)-2-[(4-nitrophenyl)formamido]-3-phenylpropanamido]acetamido}pentanamide
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C41H51N11O8
 1
1
EC50 = 1 nM
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CP0848308
(S)-N1-((8S,11S,17S,20S,21R)-8-((S)-1-amino-3-(1H-indol-3-yl)-1-oxopropan-2-ylcarbamoyl)-17-benzyl-21-hydroxy-3-imino-11-isobutyl-10,13,16,19-tetraoxo-2,4,9,12,14,15,18-heptaazadocosan-20-yl)-2-((R)-2-((R)-2-amino-3-(4-hydroxyphenyl)propanamido)-3-(1H-indol-3-yl)propanamido)succinamide
   Show/Hide
C62H81N17O12
 2
1
EC50 = 1 nM
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2
Ki = 0.036 nM
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CP0399987
(2S)-N-[(1S)-4-carbamimidamido-1-{[(1S)-1-carbamoyl-2-(1H-indol-3-yl)ethyl]carbamoyl}butyl]-2-{2-[(2S)-2-[(3-hydroxyphenyl)formamido]-3-phenylpropanamido]acetamido}-4-methylpentanamide
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C41H52N10O7
 1
1
EC50 = 1.2 nM
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CP0524534
(2S)-N-[(1S)-4-carbamimidamido-1-{[(1S)-1-carbamoyl-2-(1H-indol-3-yl)ethyl]carbamoyl}butyl]-2-{2-[(2S)-2-[(4-methoxyphenyl)formamido]-3-phenylpropanamido]acetamido}-4-methylpentanamide
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C42H54N10O7
 1
1
EC50 = 1.2 nM
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CP0865108
(S)-1-((S)-4-amino-2-((R)-2-((R)-2-amino-3-(4-hydroxyphenyl)propanamido)-3-(pyridin-4-yl)propanamido)-4-oxobutanoyl)-N-((8S,11S,17S)-8-((S)-1-amino-3-(1H-indol-3-yl)-1-oxopropan-2-ylcarbamoyl)-3-imino-11-isobutyl-10,13,16-trioxo-18-phenyl-2,4,9,12,14,15-hexaazaoctadecan-17-yl)pyrrolidine-2-carboxamide
   Show/Hide
C60H79N17O11
 2
1
EC50 = 1.2 nM
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2
Ki = 0.096 nM
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CP0445744
(2S)-N-[(1S)-4-carbamimidamido-1-{[(1S)-1-carbamoyl-2-(1H-indol-3-yl)ethyl]carbamoyl}butyl]-2-{2-[(2S)-2-[(4-chlorophenyl)formamido]-3-phenylpropanamido]acetamido}-4-methylpentanamide
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C41H51ClN10O6
 1
1
EC50 = 1.3 nM
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CP0907777
2-((2S,5S,8S,11R,14R)-14-amino-2-benzyl-8-((R)-1-hydroxyethyl)-5-(hydroxymethyl)-15-(4-hydroxyphenyl)-4,7,10,13-tetraoxo-11-(pyridin-4-ylmethyl)-3,6,9,12-tetraazapentadecane)-N-((S)-1-((S)-1-((S)-1-amino-3-(1H-indol-3-yl)-1-oxopropan-2-ylamino)-5-(3-methylguanidino)-1-oxopentan-2-ylamino)-4-methyl-1-oxopentan-2-yl)hydrazinecarboxamide
   Show/Hide
C58H78N16O12
 1
1
EC50 = 1.3 nM
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CP0406559
(2S)-N-[(1S)-4-carbamimidamido-1-{[(1S)-1-carbamoyl-2-(1H-indol-3-yl)ethyl]carbamoyl}butyl]-2-{2-[(2S)-2-{[4-(carbamimidamidomethyl)phenyl]formamido}-3-phenylpropanamido]acetamido}-4-methylpentanamide
   Show/Hide
C43H57N13O6
 1
1
EC50 = 1.4 nM
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CP0438591
(2S)-N-[(2S)-1-[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]amino]-5-[(N'-methylcarbamimidoyl)amino]-1-oxopentan-2-yl]-2-[[[(2S)-2-(hexanoylamino)-3-phenylpropanoyl]amino]carbamoylamino]-4-methylpentanamide
   Show/Hide
C38H58N10O6
 1
1
EC50 = 1.4 nM
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CP0922192
(S)-N1-((8S,11S,17S,20S)-8-((S)-1-amino-3-(1H-indol-3-yl)-1-oxopropan-2-ylcarbamoyl)-17-benzyl-3-imino-11-isobutyl-21,21-dimethyl-10,13,16,19-tetraoxo-2,4,9,12,14,15,18-heptaazadocosan-20-yl)-2-((R)-2-((R)-2-amino-3-(4-hydroxyphenyl)propanamido)-3-(pyridin-4-yl)propanamido)succinamide
   Show/Hide
C61H83N17O11
 1
1
EC50 = 1.5 nM
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CP0474395
(2S)-N-[(2S)-1-[[(2S)-1-[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]amino]-5-[(N'-methylcarbamimidoyl)amino]-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]carbamoyl]hydrazinyl]-1-oxo-3-phenylpropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]-2-(3-pyridin-4-ylpropanoylamino)butanediamide
   Show/Hide
C47H66N14O10
 1
1
EC50 = 1.5 nM
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CP0457949
(2S)-2-{2-[(2S)-2-[(4-aminophenyl)formamido]-3-phenylpropanamido]acetamido}-N-[(1S)-4-carbamimidamido-1-{[(1S)-1-carbamoyl-2-(1H-indol-3-yl)ethyl]carbamoyl}butyl]-4-methylpentanamide
   Show/Hide
C41H53N11O6
 1
1
EC50 = 1.6 nM
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CP0922184
(S)-N1-((8S,11S,17S,20S,21R)-8-((S)-1-amino-3-(1H-indol-3-yl)-1-oxopropan-2-ylcarbamoyl)-17-benzyl-21-hydroxy-3-imino-11-isobutyl-10,13,16,19-tetraoxo-2,4,9,12,14,15,18-heptaazadocosan-20-yl)-2-((R)-2-((R)-2-amino-3-(4-hydroxyphenyl)propanamido)-3-(pyridin-4-yl)propanamido)succinamide
   Show/Hide
C59H79N17O12
 2
1
EC50 = 1.6 nM
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2
Ki = 0.086 nM
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CP0406555
(2S)-N-[(1S)-4-carbamimidamido-1-{[(1S)-1-carbamoyl-2-(1H-indol-3-yl)ethyl]carbamoyl}butyl]-4-methyl-2-{2-[(2S)-3-phenyl-2-(pyridin-4-ylformamido)propanamido]acetamido}pentanamide
   Show/Hide
C40H51N11O6
 1
1
EC50 = 1.7 nM
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CP0435594
(2S)-N-[(1S)-4-carbamimidamido-1-{[(1S)-1-carbamoyl-2-(1H-indol-3-yl)ethyl]carbamoyl}butyl]-2-{2-[(2S)-2-(1H-imidazol-4-ylformamido)-3-phenylpropanamido]acetamido}-4-methylpentanamide
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C38H50N12O6
 1
1
EC50 = 1.7 nM
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CP0445749
(2S)-N-[(1S)-4-carbamimidamido-1-{[(1S)-1-carbamoyl-2-(1H-indol-3-yl)ethyl]carbamoyl}butyl]-2-{2-[(2S)-2-[(4-carbamimidamidophenyl)formamido]-3-phenylpropanamido]acetamido}-4-methylpentanamide
   Show/Hide
C42H55N13O6
 1
1
EC50 = 1.7 nM
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CP0858419
(S)-N1-((8S,11S,17S,20S)-8-((S)-1-amino-3-(1H-indol-3-yl)-1-oxopropan-2-ylcarbamoyl)-17-benzyl-3-imino-11-isobutyl-21-methyl-10,13,16,19-tetraoxo-2,4,9,12,14,15,18-heptaazadocosan-20-yl)-2-((R)-2-((R)-2-amino-3-(4-hydroxyphenyl)propanamido)-3-(pyridin-4-yl)propanamido)succinamide
   Show/Hide
C60H81N17O11
 2
1
EC50 = 1.8 nM
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2
Ki = 0.052 nM
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CP0445747
(2S)-N-[(1S)-4-carbamimidamido-1-{[(1S)-1-carbamoyl-2-(1H-indol-3-yl)ethyl]carbamoyl}butyl]-4-methyl-2-{2-[(2S)-3-phenyl-2-(1H-pyrrol-2-ylformamido)propanamido]acetamido}pentanamide
   Show/Hide
C39H51N11O6
 1
1
EC50 = 2 nM
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CP0463212
(2S)-N-[(1S)-4-carbamimidamido-1-{[(1S)-1-carbamoyl-2-(1H-indol-3-yl)ethyl]carbamoyl}butyl]-2-{2-[(2S)-2-[(4-hydroxyphenyl)formamido]-3-phenylpropanamido]acetamido}-4-methylpentanamide
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C41H52N10O7
 1
1
EC50 = 2.1 nM
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CP0575493
(2S)-2-[[(2S)-2-acetamido-3-(1H-indol-3-yl)propanoyl]amino]-N-[(2S)-1-[[(2S)-1-[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]amino]-5-[(N'-methylcarbamimidoyl)amino]-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]carbamoyl]hydrazinyl]-1-oxo-3-phenylpropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]butanediamide
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C52H71N15O11
 1
1
EC50 = 2.1 nM
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CP0270121
(2S)-N-[(1S)-4-carbamimidamido-1-{[(1S)-1-carbamoyl-2-(1H-indol-3-yl)ethyl]carbamoyl}butyl]-2-{3-[(2S)-2-[(4-fluorophenyl)formamido]-3-phenylpropanamido]propyl}-4-methylpentanamide
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C42H54FN9O5
 2
1
EC50 = 2.5 nM
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2
IC50 = 1.2 nM
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CP0445750
(2S)-N-[(1S)-4-carbamimidamido-1-{[(1S)-1-carbamoyl-2-(1H-indol-3-yl)ethyl]carbamoyl}butyl]-4-methyl-2-{2-[(2S)-3-phenyl-2-[(4-{[(pyridin-2-ylmethyl)amino]methyl}phenyl)formamido]propanamido]acetamido}pentanamide
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C48H60N12O6
 1
1
EC50 = 2.7 nM
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CP0850851
(2S)-1-((S)-4-amino-2-((R)-2-((R)-2-amino-3-(4-hydroxyphenyl)propanamido)-3-(pyridin-4-yl)propanamido)-4-oxobutanoyl)-N-((8S,11S,17S)-8-((S)-1-amino-3-(1H-indol-3-yl)-1-oxopropan-2-ylcarbamoyl)-3-imino-11-isobutyl-10,13,16-trioxo-18-phenyl-2,4,9,12,14,15-hexaazaoctadecan-17-yl)-4-hydroxypyrrolidine-2-carboxamide
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C60H79N17O12
 1
1
EC50 = 2.8 nM
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CP0406554
2-{[(1S)-1-[({[(1S)-1-{[(1S)-4-carbamimidamido-1-{[(1S)-1-carbamoyl-2-(1H-indol-3-yl)ethyl]carbamoyl}butyl]carbamoyl}-3-methylbutyl]carbamoyl}methyl)carbamoyl]-2-phenylethyl]carbamoyl}phenyl 2-hydroxybenzoate
   Show/Hide
C48H56N10O9
 1
1
EC50 = 3 nM
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CP0427902
(2S)-N-[(1S)-4-carbamimidamido-1-{[(1S)-1-carbamoyl-2-(1H-indol-3-yl)ethyl]carbamoyl}butyl]-4-methyl-2-{2-[(2S)-3-phenyl-2-(pyridin-3-ylformamido)propanamido]acetamido}pentanamide
   Show/Hide
C40H51N11O6
 1
1
EC50 = 3 nM
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CP0505374
(2S)-N-[(1S)-4-carbamimidamido-1-{[(1S)-1-carbamoyl-2-(1H-indol-3-yl)ethyl]carbamoyl}butyl]-2-{2-[(2S)-2-{[4-(hydroxymethyl)phenyl]formamido}-3-phenylpropanamido]acetamido}-4-methylpentanamide
   Show/Hide
C42H54N10O7
 1
1
EC50 = 3 nM
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CP0406558
(2S)-2-{2-[(2S)-2-{[4-(aminomethyl)phenyl]formamido}-3-phenylpropanamido]acetamido}-N-[(1S)-4-carbamimidamido-1-{[(1S)-1-carbamoyl-2-(1H-indol-3-yl)ethyl]carbamoyl}butyl]-4-methylpentanamide
   Show/Hide
C42H55N11O6
 1
1
EC50 = 3.1 nM
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CP0475215
(2S)-2-{2-[(2S)-2-[(2-aminophenyl)formamido]-3-phenylpropanamido]acetamido}-N-[(1S)-4-carbamimidamido-1-{[(1S)-1-carbamoyl-2-(1H-indol-3-yl)ethyl]carbamoyl}butyl]-4-methylpentanamide
   Show/Hide
C41H53N11O6
 1
1
EC50 = 3.1 nM
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CP0406552
(2S)-2-{2-[(2S)-2-[(4-{[bis(pyridin-2-ylmethyl)amino]methyl}phenyl)formamido]-3-phenylpropanamido]acetamido}-N-[(1S)-4-carbamimidamido-1-{[(1S)-1-carbamoyl-2-(1H-indol-3-yl)ethyl]carbamoyl}butyl]-4-methylpentanamide
   Show/Hide
C54H65N13O6
 1
1
EC50 = 3.3 nM
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CP0406557
(2S)-2-{2-[(2S)-2-({4-[(benzylamino)methyl]phenyl}formamido)-3-phenylpropanamido]acetamido}-N-[(1S)-4-carbamimidamido-1-{[(1S)-1-carbamoyl-2-(1H-indol-3-yl)ethyl]carbamoyl}butyl]-4-methylpentanamide
   Show/Hide
C49H61N11O6
 1
1
EC50 = 3.3 nM
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CP0158366
(2R,4R)-N-[(1S)-4-carbamimidamido-1-{[(1S)-1-carbamoyl-2-(1H-indol-3-yl)ethyl]carbamoyl}butyl]-5-[(2S)-2-[(4-fluorophenyl)formamido]-3-phenylpropanamido]-4-hydroxy-2-(2-methylpropyl)pentanamide
   Show/Hide
C42H54FN9O6
 2
1
EC50 = 4.3 nM
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2
IC50 = 5.7 nM
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CP0848307
(S)-N1-((8S,11S,17S,20S)-8-((S)-1-amino-3-(1H-indol-3-yl)-1-oxopropan-2-ylcarbamoyl)-17-benzyl-3-imino-11-isobutyl-10,13,16,19-tetraoxo-20-phenyl-2,4,9,12,14,15,18-heptaazaicosan-20-yl)-2-((R)-2-((R)-2-amino-3-(4-hydroxyphenyl)propanamido)-3-(pyridin-4-yl)propanamido)succinamide
   Show/Hide
C63H79N17O11
 1
1
EC50 = 4.4 nM
   TI
   LI
   LO
   TS
CP0406556
(2S)-2-{2-[(2S)-2-[(3-aminophenyl)formamido]-3-phenylpropanamido]acetamido}-N-[(1S)-4-carbamimidamido-1-{[(1S)-1-carbamoyl-2-(1H-indol-3-yl)ethyl]carbamoyl}butyl]-4-methylpentanamide
   Show/Hide
C41H53N11O6
 1
1
EC50 = 4.7 nM
   TI
   LI
   LO
   TS
CP0445745
(2S)-N-[(1S)-4-carbamimidamido-1-{[(1S)-1-carbamoyl-2-(1H-indol-3-yl)ethyl]carbamoyl}butyl]-2-{2-[(2S)-2-[(2-hydroxyphenyl)formamido]-3-phenylpropanamido]acetamido}-4-methylpentanamide
   Show/Hide
C41H52N10O7
 1
1
EC50 = 5 nM
   TI
   LI
   LO
   TS
CP0267258
(2E)-N-[(1S)-4-carbamimidamido-1-{[(1S)-1-carbamoyl-2-(1H-indol-3-yl)ethyl]carbamoyl}butyl]-5-[(2S)-2-[(4-fluorophenyl)formamido]-3-phenylpropanamido]-2-(2-methylpropyl)pent-2-enamide
   Show/Hide
C42H52FN9O5
 2
1
EC50 = 5.4 nM
   TI
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   TS
2
IC50 = 4.6 nM
   TI
   LI
   LO
   TS
CP0477082
(2S)-2-[[(2S)-2-amino-3-(1H-indol-3-yl)propanoyl]amino]-N-[(2S)-1-[[(2S)-1-[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]amino]-5-[(N'-methylcarbamimidoyl)amino]-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]carbamoyl]hydrazinyl]-1-oxo-3-phenylpropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]butanediamide
   Show/Hide
C50H69N15O10
 1
1
EC50 = 7.7 nM
   TI
   LI
   LO
   TS
CP0575491
(2S)-N-[(2S)-1-[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]amino]-5-[(N'-methylcarbamimidoyl)amino]-1-oxopentan-2-yl]-2-[[[(2S)-2-[[(2S)-3-hydroxy-2-[3-(1H-indol-3-yl)propanoylamino]propanoyl]amino]-3-phenylpropanoyl]amino]carbamoylamino]-4-methylpentanamide
   Show/Hide
C46H62N12O8
 1
1
EC50 = 8.2 nM
   TI
   LI
   LO
   TS
CP0520456
(2S)-N-[(2S)-1-[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]amino]-5-[(N'-methylcarbamimidoyl)amino]-1-oxopentan-2-yl]-2-[[[(2S)-2-amino-3-phenylpropanoyl]amino]carbamoylamino]-4-methylpentanamide
   Show/Hide
C32H48N10O5
 1
1
EC50 = 130 nM
   TI
   LI
   LO
   TS
CP0406553
(2S)-N-[(1S)-4-carbamimidamido-1-{[(1S)-1-carbamoyl-2-(1H-indol-3-yl)ethyl]carbamoyl}butyl]-4-methyl-2-{2-[(2S)-2-[(2,3,4,5,6-pentafluorophenyl)formamido]-3-phenylpropanamido]acetamido}pentanamide
   Show/Hide
C41H47F5N10O6
 1
1
EC50 > 100 nM
   TI
   LI
   LO
   TS
CP0475214
(2S)-N-[(1S)-4-carbamimidamido-1-{[(1S)-1-carbamoyl-2-(1H-indol-3-yl)ethyl]carbamoyl}butyl]-4-methyl-2-{2-[(2S)-3-phenyl-2-[(3,4,5-trihydroxyphenyl)formamido]propanamido]acetamido}pentanamide
   Show/Hide
C41H52N10O9
 1
1
EC50 > 100 nM
   TI
   LI
   LO
   TS
CP0487760
N-[3-cyano-6-(4-fluoro-2-hydroxyphenyl)-4-(3-piperazin-1-ylphenyl)pyridin-2-yl]furan-2-carboxamide
   Show/Hide
C27H22FN5O3
 1
1
IC50 = 3.6 nM
   TI
   LI
   LO
   TS
CP0454298
N-[4-[3-(3-aminopropanoylamino)phenyl]-3-cyano-6-(4-fluoro-2-hydroxyphenyl)pyridin-2-yl]furan-2-carboxamide
   Show/Hide
C26H20FN5O4
 2
1
IC50 = 3.7 nM
   TI
   LI
   LO
   TS
2
IC50 = 460 nM
   TI
   LI
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   TS
CP0438744
N-[4-[3-[(2-aminoacetyl)amino]phenyl]-3-cyano-6-(4-fluoro-2-hydroxyphenyl)pyridin-2-yl]furan-2-carboxamide
   Show/Hide
C25H18FN5O4
 1
1
IC50 = 4.1 nM
   TI
   LI
   LO
   TS
CP0373020
N-[3-cyano-6-(4-fluoro-2-hydroxyphenyl)-4-[3-[3-(methylamino)propanoylamino]phenyl]pyridin-2-yl]furan-2-carboxamide
   Show/Hide
C27H22FN5O4
 1
1
IC50 = 4.6 nM
   TI
   LI
   LO
   TS
CP0514912
N-[3-cyano-4-[3-(1,4-diazepan-1-yl)phenyl]-6-(4-fluoro-2-hydroxyphenyl)pyridin-2-yl]furan-2-carboxamide
   Show/Hide
C28H24FN5O3
 1
1
IC50 = 7.3 nM
   TI
   LI
   LO
   TS
CP0446441
N-[4-[3-(3-aminopropanoylamino)phenyl]-3-cyano-6-(4-fluoro-2-hydroxyphenyl)pyridin-2-yl]thiophene-2-carboxamide
   Show/Hide
C26H20FN5O3S
 2
1
IC50 = 7.4 nM
   TI
   LI
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   TS
2
IC50 = 3600 nM
   TI
   LI
   LO
   TS
CP0487759
N-[3-cyano-6-(4-fluoro-2-hydroxyphenyl)-4-[3-[[2-[(2S)-pyrrolidin-2-yl]acetyl]amino]phenyl]pyridin-2-yl]furan-2-carboxamide
   Show/Hide
C29H24FN5O4
 1
1
IC50 = 7.9 nM
   TI
   LI
   LO
   TS
CP0446442
N-[4-[3-(2-aminoethylcarbamoyl)phenyl]-3-cyano-6-(4-fluoro-2-hydroxyphenyl)pyridin-2-yl]furan-2-carboxamide
   Show/Hide
C26H20FN5O4
 2
1
IC50 = 8 nM
   TI
   LI
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   TS
2
IC50 = 660 nM
   TI
   LI
   LO
   TS
CP0448306
N-[3-cyano-4-[3-[3-(ethylamino)pentanoylamino]phenyl]-6-(4-fluoro-2-hydroxyphenyl)pyridin-2-yl]furan-2-carboxamide
   Show/Hide
C30H28FN5O4
 1
1
IC50 = 8 nM
   TI
   LI
   LO
   TS
CP0430721
N-[3-cyano-6-(4-fluoro-2-hydroxyphenyl)-4-[3-[[2-(methylamino)acetyl]amino]phenyl]pyridin-2-yl]furan-2-carboxamide
   Show/Hide
C26H20FN5O4
 1
1
IC50 = 8.4 nM
   TI
   LI
   LO
   TS
CP0180522
(2S)-N-[(2S)-1-[[(2S)-4-amino-1-[[(2S)-1-[[(2S)-1-[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]amino]-5-[(N'-methylcarbamimidoyl)amino]-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]carbamoyl]hydrazinyl]-1-oxo-3-phenylpropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]-2-[[(2R)-2-amino-3-(4-hydroxyphenyl)propanoyl]amino]butanediamide
   Show/Hide
C63H84N18O14
 2
1
IC50 = 9.67 nM
   TI
   LI
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   TS
2
Ki = 0.051 nM
   TI
   LI
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   TS
CP0491036
N-[3-cyano-6-(4-fluoro-2-hydroxyphenyl)-4-[3-[3-(propan-2-ylamino)butanoylamino]phenyl]pyridin-2-yl]furan-2-carboxamide
   Show/Hide
C30H28FN5O4
 1
1
IC50 = 9.7 nM
   TI
   LI
   LO
   TS
CP0931001
N-{3-Cyano-6-(4-fluoro-2-hydroxyphenyl)-4-[3-(piperazin-1-ylmethyl)phenyl]pyridin-2-yl}furan-2-carbox-amide trifluoroacetate
   Show/Hide
C30H25F4N5O5
 1
1
IC50 = 9.7 nM
   TI
   LI
   LO
   TS
CP0388158
N-[4-[3-(3-aminopropanoylamino)phenyl]-6-(4-chloro-2-hydroxyphenyl)-3-cyanopyridin-2-yl]thiophene-2-carboxamide
   Show/Hide
C26H20ClN5O3S
 2
1
IC50 = 9.8 nM
   TI
   LI
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   TS
2
IC50 = 4100 nM
   TI
   LI
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   TS
CP0448305
N-[3-cyano-4-[3-[3-(ethylamino)butanoylamino]phenyl]-6-(4-fluoro-2-hydroxyphenyl)pyridin-2-yl]furan-2-carboxamide
   Show/Hide
C29H26FN5O4
 1
1
IC50 = 10 nM
   TI
   LI
   LO
   TS
CP0487758
N-[3-cyano-4-[3-[3-(dimethylamino)propanoylamino]phenyl]-6-(4-fluoro-2-hydroxyphenyl)pyridin-2-yl]furan-2-carboxamide
   Show/Hide
C28H24FN5O4
 1
1
IC50 = 10 nM
   TI
   LI
   LO
   TS
CP0504184
N-[3-cyano-6-(4-fluoro-2-hydroxyphenyl)-4-[3-[[2-[(2R)-pyrrolidin-2-yl]acetyl]amino]phenyl]pyridin-2-yl]furan-2-carboxamide
   Show/Hide
C29H24FN5O4
 1
1
IC50 = 10 nM
   TI
   LI
   LO
   TS
CP0504282
N-[3-cyano-4-[3-[3-[ethyl(methyl)amino]propanoylamino]phenyl]-6-(4-fluoro-2-hydroxyphenyl)pyridin-2-yl]furan-2-carboxamide
   Show/Hide
C29H26FN5O4
 1
1
IC50 = 10 nM
   TI
   LI
   LO
   TS
CP0505819
N-[4-[3-[(3-amino-2,2-dimethylpropyl)carbamoyl]phenyl]-3-cyano-6-(4-fluoro-2-hydroxyphenyl)pyridin-2-yl]furan-2-carboxamide
   Show/Hide
C29H26FN5O4
 2
1
IC50 = 11 nM
   TI
   LI
   LO
   TS
2
IC50 = 2500 nM
   TI
   LI
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   TS
CP0520918
N-[3-cyano-4-[3-(4-ethylpiperazin-1-yl)phenyl]-6-(4-fluoro-2-hydroxyphenyl)pyridin-2-yl]furan-2-carboxamide
   Show/Hide
C29H26FN5O3
 1
1
IC50 = 11 nM
   TI
   LI
   LO
   TS
CP0472475
N-[4-[3-(3-aminopropanoylamino)phenyl]-3-cyano-6-(2-hydroxy-4-methylphenyl)pyridin-2-yl]thiophene-2-carboxamide
   Show/Hide
C27H23N5O3S
 2
1
IC50 = 12 nM
   TI
   LI
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   TS
2
IC50 = 910 nM
   TI
   LI
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   TS
CP0438701
N-[3-cyano-4-[3-[[2-(dimethylamino)acetyl]amino]phenyl]-6-(4-fluoro-2-hydroxyphenyl)pyridin-2-yl]furan-2-carboxamide
   Show/Hide
C27H22FN5O4
 1
1
IC50 = 12 nM
   TI
   LI
   LO
   TS
CP0446437
N-[4-[3-(2-aminoethylcarbamoyl)phenyl]-3-cyano-6-(2-hydroxyphenyl)pyridin-2-yl]furan-2-carboxamide
   Show/Hide
C26H21N5O4
 1
1
IC50 = 14 nM
   TI
   LI
   LO
   TS
CP0504243
N-[3-cyano-6-(4-fluoro-2-hydroxyphenyl)-4-[3-[(2-piperidin-2-ylacetyl)amino]phenyl]pyridin-2-yl]furan-2-carboxamide
   Show/Hide
C30H26FN5O4
 1
1
IC50 = 14 nM
   TI
   LI
   LO
   TS
CP0487863
N-[4-[3-[(1-amino-2-methylpropan-2-yl)carbamoyl]phenyl]-3-cyano-6-(2-hydroxyphenyl)pyridin-2-yl]furan-2-carboxamide
   Show/Hide
C28H25N5O4
 1
1
IC50 = 15 nM
   TI
   LI
   LO
   TS
CP0516512
N-[3-cyano-6-(4-fluoro-2-hydroxyphenyl)-4-[3-(4-methylpiperazin-1-yl)phenyl]pyridin-2-yl]furan-2-carboxamide
   Show/Hide
C28H24FN5O3
 1
1
IC50 = 15 nM
   TI
   LI
   LO
   TS
CP0543066
N-[3-cyano-6-(4-fluoro-2-hydroxyphenyl)-4-[3-[(2-piperidin-1-ylacetyl)amino]phenyl]pyridin-2-yl]furan-2-carboxamide
   Show/Hide
C30H26FN5O4
 1
1
IC50 = 15 nM
   TI
   LI
   LO
   TS
CP0491035
N-[3-cyano-4-[3-[3-(diethylamino)propanoylamino]phenyl]-6-(4-fluoro-2-hydroxyphenyl)pyridin-2-yl]furan-2-carboxamide
   Show/Hide
C30H28FN5O4
 1
1
IC50 = 16 nM
   TI
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   LO
   TS
CP0509612
(2R)-N-[3-[3-cyano-6-(4-fluoro-2-hydroxyphenyl)-2-(furan-2-carbonylamino)pyridin-4-yl]phenyl]pyrrolidine-2-carboxamide
   Show/Hide
C28H22FN5O4
 1
1
IC50 = 16 nM
   TI
   LI
   LO
   TS
CP0400806
N-[3-cyano-4-[3-[3-(diethylamino)butanoylamino]phenyl]-6-(4-fluoro-2-hydroxyphenyl)pyridin-2-yl]furan-2-carboxamide
   Show/Hide
C31H30FN5O4
 1
1
IC50 = 17 nM
   TI
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   TS
CP0487756
N-[3-cyano-6-(4-fluoro-2-hydroxyphenyl)-4-[3-[[2-[(2S)-1-methylpyrrolidin-2-yl]acetyl]amino]phenyl]pyridin-2-yl]furan-2-carboxamide
   Show/Hide
C30H26FN5O4
 1
1
IC50 = 18 nM
   TI
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   LO
   TS
CP0504244
N-[3-cyano-6-(4-fluoro-2-hydroxyphenyl)-4-[3-[(4-methylpiperazin-1-yl)methyl]phenyl]pyridin-2-yl]furan-2-carboxamide
   Show/Hide
C29H26FN5O3
 1
1
IC50 = 18 nM
   TI
   LI
   LO
   TS
CP0543054
N-[3-cyano-4-[3-[3-(dimethylamino)butanoylamino]phenyl]-6-(4-fluoro-2-hydroxyphenyl)pyridin-2-yl]furan-2-carboxamide
   Show/Hide
C29H26FN5O4
 1
1
IC50 = 18 nM
   TI
   LI
   LO
   TS
CP0225128
(2S)-N-[(2S)-1-[[(2S)-4-amino-1-[[(2S)-1-[[(2S)-1-[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]amino]-5-[(N'-methylcarbamimidoyl)amino]-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]carbamoyl]hydrazinyl]-1-oxo-3-phenylpropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-1-oxo-3-pyridin-4-ylpropan-2-yl]-2-[[(2R)-2-amino-3-(4-hydroxyphenyl)propanoyl]amino]butanediamide
   Show/Hide
C60H82N18O14
 2
1
IC50 = 18.3 nM
   TI
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   TS
2
Ki = 0.12 nM
   TI
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   TS
CP0472474
N-[4-[3-(3-aminopropanoylamino)phenyl]-6-(4-bromo-2-hydroxyphenyl)-3-cyanopyridin-2-yl]thiophene-2-carboxamide
   Show/Hide
C26H20BrN5O3S
 2
1
IC50 = 19 nM
   TI
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   TS
2
IC50 = 6300 nM
   TI
   LI
   LO
   TS
CP0471032
N-[3-cyano-4-[3-[(4-ethylpiperazin-1-yl)methyl]phenyl]-6-(4-fluoro-2-hydroxyphenyl)pyridin-2-yl]furan-2-carboxamide
   Show/Hide
C30H28FN5O3
 1
1
IC50 = 20 nM
   TI
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   LO
   TS
CP0943905
N-[3-Cyano-4-(3-{[2-(dimethylamino)ethyl]carbamoyl}phenyl)-6-(4-fluoro-2-hydroxyphenyl)pyridin-2-yl]furan-2-carboxamide hydrochloride
   Show/Hide
C28H25ClFN5O4
 1
1
IC50 = 20 nM
   TI
   LI
   LO
   TS
CP0446434
N-[4-[3-(3-aminopropanoylamino)phenyl]-3-cyano-6-(2-hydroxyphenyl)pyridin-2-yl]thiophene-2-carboxamide
   Show/Hide
C26H21N5O3S
 2
1
IC50 = 21 nM
   TI
   LI
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   TS
2
IC50 = 1100 nM
   TI
   LI
   LO
   TS
CP0504183
N-[3-cyano-4-[3-[3-(diethylamino)pentanoylamino]phenyl]-6-(4-fluoro-2-hydroxyphenyl)pyridin-2-yl]furan-2-carboxamide
   Show/Hide
C32H32FN5O4
 1
1
IC50 = 22 nM
   TI
   LI
   LO
   TS
CP0912126
N-{3-Cyano-4-[3-(1,4-diazepan-1-ylmethyl)phenyl]-6-(4-fluoro-2-hydroxyphenyl)pyridin-2-yl}furan-2-carboxamide dihydrochloride
   Show/Hide
C29H28Cl2FN5O3
 1
1
IC50 = 25 nM
   TI
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   TS
CP0388164
N-[4-[3-(2-aminoethylcarbamoyl)phenyl]-3-cyano-6-(2-hydroxyphenyl)pyridin-2-yl]thiophene-2-carboxamide
   Show/Hide
C26H21N5O3S
 2
1
IC50 = 30 nM
   TI
   LI
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   TS
2
IC50 = 5100 nM
   TI
   LI
   LO
   TS
CP0471031
N-[3-cyano-4-[3-[2-(dimethylamino)ethyl-methylamino]phenyl]-6-(4-fluoro-2-hydroxyphenyl)pyridin-2-yl]furan-2-carboxamide
   Show/Hide
C28H26FN5O3
 1
1
IC50 = 30 nM
   TI
   LI
   LO
   TS
CP0487757
N-[3-cyano-4-[3-[2-(ethylamino)butanoylamino]phenyl]-6-(4-fluoro-2-hydroxyphenyl)pyridin-2-yl]furan-2-carboxamide
   Show/Hide
C29H26FN5O4
 1
1
IC50 = 30 nM
   TI
   LI
   LO
   TS
CP0388160
N-(2-aminoethyl)-3-[3-cyano-6-(2-hydroxyphenyl)-2-[(4-methoxybenzoyl)amino]pyridin-4-yl]benzamide
   Show/Hide
C29H25N5O4
 1
1
IC50 = 31 nM
   TI
   LI
   LO
   TS
CP0123124
(2S,4S)-N-[(1S)-4-carbamimidamido-1-{[(1S)-1-carbamoyl-2-(1H-indol-3-yl)ethyl]carbamoyl}butyl]-5-[(2S)-2-[(4-fluorophenyl)formamido]-3-phenylpropanamido]-4-hydroxy-2-(2-methylpropyl)pentanamide
   Show/Hide
C42H54FN9O6
 1
1
IC50 = 32 nM
   TI
   LI
   LO
   TS
CP0166625
(2E,4R)-N-[(1S)-4-carbamimidamido-1-{[(1S)-1-carbamoyl-2-(1H-indol-3-yl)ethyl]carbamoyl}butyl]-5-[(2S)-2-[(4-fluorophenyl)formamido]-3-phenylpropanamido]-4-hydroxy-2-(2-methylpropyl)pent-2-enamide
   Show/Hide
C42H52FN9O6
 1
1
IC50 = 32 nM
   TI
   LI
   LO
   TS
CP0388161
N-[4-[3-[(1-amino-2-methylpropan-2-yl)carbamoyl]phenyl]-3-cyano-6-(2-hydroxyphenyl)pyridin-2-yl]-2-methoxybenzamide
   Show/Hide
C31H29N5O4
 1
1
IC50 = 32 nM
   TI
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   TS
CP0506194
N-(1-amino-2-methylpropan-2-yl)-3-[3-cyano-6-(2-hydroxyphenyl)-2-[(4-methoxybenzoyl)amino]pyridin-4-yl]benzamide
   Show/Hide
C31H29N5O4
 1
1
IC50 = 32 nM
   TI
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   TS
CP0446438
N-[4-[3-(4-aminobutanoylamino)phenyl]-3-cyano-6-(2-hydroxyphenyl)pyridin-2-yl]thiophene-2-carboxamide
   Show/Hide
C27H23N5O3S
 2
1
IC50 = 34 nM
   TI
   LI
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   TS
2
IC50 = 1400 nM
   TI
   LI
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   TS
CP0334235
(2R)-N-[(2S)-1-[[(2S)-4-amino-1-[[(2S)-1-[[(2S)-1-[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]amino]-5-[(N'-methylcarbamimidoyl)amino]-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]carbamoyl]hydrazinyl]-1-oxo-3-phenylpropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-1-oxo-3-pyridin-4-ylpropan-2-yl]-2-[[(2R)-2-amino-3-(4-hydroxyphenyl)propanoyl]amino]butanediamide
   Show/Hide
C60H82N18O14
 2
1
IC50 = 41.2 nM
   TI
   LI
   LO
   TS
2
Ki = 0.11 nM
   TI
   LI
   LO
   TS
CP0388159
N-[4-[3-(2-aminoethylcarbamoyl)phenyl]-3-cyano-6-(2-hydroxyphenyl)pyridin-2-yl]-2-methoxybenzamide
   Show/Hide
C29H25N5O4
 1
1
IC50 = 45 nM
   TI
   LI
   LO
   TS
CP0388163
N-[4-[3-[(2-aminoacetyl)amino]phenyl]-3-cyano-6-(2-hydroxyphenyl)pyridin-2-yl]thiophene-2-carboxamide
   Show/Hide
C25H19N5O3S
 2
1
IC50 = 51 nM
   TI
   LI
   LO
   TS
2
IC50 = 2800 nM
   TI
   LI
   LO
   TS
CP0520842
N-[4-[3-(3-aminopropanoylamino)phenyl]-3-cyano-6-(2-hydroxyphenyl)pyridin-2-yl]benzamide
   Show/Hide
C28H23N5O3
 2
1
IC50 = 51 nM
   TI
   LI
   LO
   TS
2
IC50 = 24000 nM
   TI
   LI
   LO
   TS
CP0083575
(2S)-N-[(2S)-1-[[(2S)-4-amino-1-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]amino]-5-[(N'-methylcarbamimidoyl)amino]-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-2-oxoethyl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]-2-[[(2R)-2-amino-3-(4-hydroxyphenyl)propanoyl]amino]butanediamide
   Show/Hide
C64H85N17O14
 2
1
IC50 = 87 nM
   TI
   LI
   LO
   TS
2
Ki = 0.046 nM
   TI
   LI
   LO
   TS
CP0504405
N-[4-[4-(2-aminoethylcarbamoyl)phenyl]-3-cyano-6-(2-hydroxyphenyl)pyridin-2-yl]thiophene-2-carboxamide
   Show/Hide
C26H21N5O3S
 1
1
IC50 = 120 nM
   TI
   LI
   LO
   TS
CP0506196
N-[4-[3-(3-aminopropanoylamino)phenyl]-3-cyano-6-(2-hydroxy-4-methoxyphenyl)pyridin-2-yl]benzamide
   Show/Hide
C29H25N5O4
 1
1
IC50 = 120 nM
   TI
   LI
   LO
   TS
CP0460356
N-[3-cyano-4-[3-[[2-(dimethylamino)acetyl]amino]phenyl]-6-(2-hydroxyphenyl)pyridin-2-yl]thiophene-2-carboxamide
   Show/Hide
C27H23N5O3S
 1
1
IC50 = 180 nM
   TI
   LI
   LO
   TS
CP0270119
(2R)-N-[(1S)-4-carbamimidamido-1-{[(1S)-1-carbamoyl-2-(1H-indol-3-yl)ethyl]carbamoyl}butyl]-2-{2-[(2S)-2-[(4-fluorophenyl)formamido]-3-phenylpropanamido]acetamido}-4-methylpentanamide
   Show/Hide
C41H51FN10O6
 1
1
IC50 = 240 nM
   TI
   LI
   LO
   TS
CP0123122
(2S,4R)-N-[(1S)-4-carbamimidamido-1-{[(1S)-1-carbamoyl-2-(1H-indol-3-yl)ethyl]carbamoyl}butyl]-5-[(2S)-2-[(4-fluorophenyl)formamido]-3-phenylpropanamido]-4-hydroxy-2-(2-methylpropyl)pentanamide
   Show/Hide
C42H54FN9O6
 1
1
IC50 = 380 nM
   TI
   LI
   LO
   TS
CP0137856
(2E,4S)-N-[(1S)-4-carbamimidamido-1-{[(1S)-1-carbamoyl-2-(1H-indol-3-yl)ethyl]carbamoyl}butyl]-5-[(2S)-2-[(4-fluorophenyl)formamido]-3-phenylpropanamido]-4-hydroxy-2-(2-methylpropyl)pent-2-enamide
   Show/Hide
C42H52FN9O6
 1
1
IC50 = 460 nM
   TI
   LI
   LO
   TS
CP0506195
N-[4-[3-(3-aminopropanoylamino)phenyl]-3-cyano-6-(2-hydroxy-5-methoxyphenyl)pyridin-2-yl]thiophene-2-carboxamide
   Show/Hide
C27H23N5O4S
 1
1
IC50 = 480 nM
   TI
   LI
   LO
   TS
CP0446440
N-[4-[3-(3-aminopropanoylamino)phenyl]-6-(5-chloro-2-hydroxyphenyl)-3-cyanopyridin-2-yl]thiophene-2-carboxamide
   Show/Hide
C26H20ClN5O3S
 1
1
IC50 = 490 nM
   TI
   LI
   LO
   TS
CP0446433
N-[4-[3-(aminomethyl)phenyl]-3-cyano-6-(2-hydroxyphenyl)pyridin-2-yl]thiophene-2-carboxamide
   Show/Hide
C24H18N4O2S
 1
1
IC50 = 570 nM
   TI
   LI
   LO
   TS
CP0388165
N-[6-(2-aminophenyl)-4-[3-(3-aminopropanoylamino)phenyl]-3-cyanopyridin-2-yl]benzamide
   Show/Hide
C28H24N6O2
 1
1
IC50 = 890 nM
   TI
   LI
   LO
   TS
CP0504406
N-[4-[3-(3-aminopropanoylamino)phenyl]-3-cyano-6-(2-hydroxyphenyl)-5-methylpyridin-2-yl]furan-2-carboxamide
   Show/Hide
C27H23N5O4
 1
1
IC50 = 1200 nM
   TI
   LI
   LO
   TS
CP0506193
N-[3-cyano-4-[3-(hydroxymethyl)phenyl]-6-(2-hydroxyphenyl)pyridin-2-yl]thiophene-2-carboxamide
   Show/Hide
C24H17N3O3S
 1
1
IC50 = 1500 nM
   TI
   LI
   LO
   TS
CP0388162
N-[4-(3-aminophenyl)-3-cyano-6-(2-hydroxyphenyl)pyridin-2-yl]thiophene-2-carboxamide
   Show/Hide
C23H16N4O2S
 1
1
IC50 = 2100 nM
   TI
   LI
   LO
   TS
CP0520841
3-{3-Cyano-6-(2-hydroxyphenyl)-2-[(thiophen-2-ylcarbonyl)amino]pyridin-4-yl}benzoic acid
   Show/Hide
C24H15N3O4S
 1
1
IC50 = 9900 nM
   TI
   LI
   LO
   TS
CP0446436
N-[4-(3-aminophenyl)-3-cyano-6-(2-methoxyphenyl)pyridin-2-yl]thiophene-2-carboxamide
   Show/Hide
C24H18N4O2S
 1
1
IC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0446435
N-[4-[2-(2-aminoethylcarbamoyl)phenyl]-3-cyano-6-(2-hydroxyphenyl)pyridin-2-yl]thiophene-2-carboxamide
   Show/Hide
C26H21N5O3S
 1
1
IC50 = 33000 nM
   TI
   LI
   LO
   TS
CP0366655
(2S)-2-[[(2S)-2-[[(2R)-2-amino-3-(4-hydroxyphenyl)propanoyl]amino]-3-naphthalen-2-ylpropanoyl]amino]-N-[(2S)-1-[[(2S)-1-[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]amino]-5-[(N'-methylcarbamimidoyl)amino]-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]carbamoyl]hydrazinyl]-1-oxo-3-phenylpropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]butanediamide
   Show/Hide
C61H79N15O12
 1
1
Ki = 0.032 nM
   TI
   LI
   LO
   TS
CP0523493
(2S)-2-[[(2S)-2-[[(2R)-2-[[(2R)-2-amino-3-(4-hydroxyphenyl)propanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]-3-(1H-indol-3-yl)propanoyl]amino]-N-[(2S)-1-[[(2S)-1-[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]amino]-5-[(N-methylcarbamimidoyl)amino]-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]carbamoyl]hydrazinyl]-1-oxo-3-phenylpropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]butanediamide
   Show/Hide
C65H85N19O13
 1
1
Ki = 0.033 nM
   TI
   LI
   LO
   TS
CP0366656
(2S)-N-[(2S)-1-[[(2S)-4-amino-1-[[(2S)-1-[[(2S)-1-[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]carbamoyl]hydrazinyl]-1-oxo-3-phenylpropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]-2-[[(2S)-2-amino-3-(4-hydroxyphenyl)propanoyl]amino]butanediamide
   Show/Hide
C62H82N18O14
 1
1
Ki = 0.045 nM
   TI
   LI
   LO
   TS
CP0339422
(2R)-N-[(2R)-1-[[(2S)-4-amino-1-[[(2S)-1-[[(2S)-1-[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]amino]-5-[(N'-methylcarbamimidoyl)amino]-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]carbamoyl]hydrazinyl]-1-oxo-3-phenylpropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]-2-[[(2R)-2-amino-3-(4-hydroxyphenyl)propanoyl]amino]butanediamide
   Show/Hide
C63H84N18O14
 1
1
Ki = 0.052 nM
   TI
   LI
   LO
   TS
CP0367957
(2S)-2-[[(2S)-2-[[(2R)-4-amino-2-[[(2R)-2-amino-3-(4-hydroxyphenyl)propanoyl]amino]-4-oxobutanoyl]amino]-3-cyclohexylpropanoyl]amino]-N-[(2S)-1-[[(2S)-1-[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]amino]-5-[(N'-methylcarbamimidoyl)amino]-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]carbamoyl]hydrazinyl]-1-oxo-3-phenylpropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]butanediamide
   Show/Hide
C61H89N17O14
 1
1
Ki = 0.055 nM
   TI
   LI
   LO
   TS
CP0350370
(2R)-N-[(2S)-1-[[(2S)-4-amino-1-[[(2S)-1-[[(2S)-1-[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]amino]-5-[(N'-methylcarbamimidoyl)amino]-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]carbamoyl]hydrazinyl]-1-oxo-3-phenylpropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]-2-[[(2R)-2-amino-3-(4-hydroxyphenyl)propanoyl]amino]butanediamide
   Show/Hide
C63H84N18O14
 1
1
Ki = 0.062 nM
   TI
   LI
   LO
   TS
CP0071237
(2S)-2-[[(2R)-2-[[(2R)-2-amino-3-(4-hydroxyphenyl)propanoyl]amino]-3-(1H-indol-3-yl)propanoyl]amino]-N-[(2S)-1-[[(2S)-1-[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]amino]-5-[(N'-methylcarbamimidoyl)amino]-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]carbamoyl]hydrazinyl]-1-oxo-3-phenylpropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]butanediamide
   Show/Hide
C59H78N16O12
 1
1
Ki = 0.065 nM
   TI
   LI
   LO
   TS
CP0260603
(2S)-N-[(2R)-1-[[(2S)-4-amino-1-[[(2S)-1-[[(2S)-1-[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]amino]-5-[(N'-methylcarbamimidoyl)amino]-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]carbamoyl]hydrazinyl]-1-oxo-3-phenylpropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]-2-[[(2R)-2-amino-3-(4-hydroxyphenyl)propanoyl]amino]butanediamide
   Show/Hide
C63H84N18O14
 1
1
Ki = 0.078 nM
   TI
   LI
   LO
   TS
CP0150085
(2S)-2-[[(2S)-2-[[(2R)-2-amino-3-(4-hydroxyphenyl)propanoyl]amino]-3-phenylpropanoyl]amino]-N-[(2S)-1-[[(2S)-1-[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]amino]-5-[(N'-methylcarbamimidoyl)amino]-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]carbamoyl]hydrazinyl]-1-oxo-3-phenylpropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]butanediamide
   Show/Hide
C57H77N15O12
 1
1
Ki = 0.086 nM
   TI
   LI
   LO
   TS
CP0366654
(2S)-2-[[(2S)-2-[[(2R)-2-[[(2R)-2-amino-3-(4-hydroxyphenyl)propanoyl]amino]-3-hydroxypropanoyl]amino]-3-(1H-indol-3-yl)propanoyl]amino]-N-[(2S)-1-[[(2S)-1-[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]amino]-5-[(N'-methylcarbamimidoyl)amino]-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]carbamoyl]hydrazinyl]-1-oxo-3-phenylpropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]butanediamide
   Show/Hide
C62H83N17O14
 1
1
Ki = 0.086 nM
   TI
   LI
   LO
   TS
CP0258966
(2S)-N-[(2S)-1-[[(2S)-1-[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]amino]-5-[(N'-methylcarbamimidoyl)amino]-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]carbamoyl]hydrazinyl]-1-oxo-3-phenylpropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]-2-[[(2S)-2-[[(2R)-2-amino-3-pyridin-3-ylpropanoyl]amino]-3-(1H-indol-3-yl)propanoyl]amino]butanediamide
   Show/Hide
C58H77N17O11
 1
1
Ki = 0.11 nM
   TI
   LI
   LO
   TS
CP0071236
(2S)-2-[[(2S,3S)-2-[[(2R)-2-amino-3-(4-hydroxyphenyl)propanoyl]amino]-3-methylpentanoyl]amino]-N-[(2S)-1-[[(2S)-1-[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]amino]-5-[(N'-methylcarbamimidoyl)amino]-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]carbamoyl]hydrazinyl]-1-oxo-3-phenylpropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]butanediamide
   Show/Hide
C54H79N15O12
 1
1
Ki = 0.12 nM
   TI
   LI
   LO
   TS
CP0247747
(2S)-N-[(2R)-1-[[(2S)-4-amino-1-[[(2S)-1-[[(2S)-1-[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]amino]-5-[(N'-methylcarbamimidoyl)amino]-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]carbamoyl]hydrazinyl]-1-oxo-3-phenylpropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-1-oxo-3-pyridin-4-ylpropan-2-yl]-2-[[(2R)-2-amino-3-(4-hydroxyphenyl)propanoyl]amino]butanediamide
   Show/Hide
C60H82N18O14
 1
1
Ki = 0.12 nM
   TI
   LI
   LO
   TS
CP0258965
(2S)-N-[(2S)-1-[[(2S)-4-amino-1-[[(2S)-1-[[(2S)-1-[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]amino]-5-[(N'-methylcarbamimidoyl)amino]-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]carbamoyl]hydrazinyl]-1-oxo-3-phenylpropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]-2-[[(2R)-2-amino-3-pyridin-3-ylpropanoyl]amino]butanediamide
   Show/Hide
C62H83N19O13
 1
1
Ki = 0.12 nM
   TI
   LI
   LO
   TS
CP0366653
(2R)-N-[(2S)-1-[[(2S)-4-amino-1-[[(2S)-1-[[(2S)-1-[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]amino]-5-[(N'-methylcarbamimidoyl)amino]-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]carbamoyl]hydrazinyl]-1-oxo-3-phenylpropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]-2-[[(2R)-2-amino-3-(4-hydroxyphenyl)propanoyl]amino]butanediamide
   Show/Hide
C61H83N17O14
 1
1
Ki = 0.12 nM
   TI
   LI
   LO
   TS
CP0258832
(2S)-2-[[(2S,3R)-2-[[(2R)-2-amino-3-(4-hydroxyphenyl)propanoyl]amino]-3-hydroxybutanoyl]amino]-N-[(2S)-1-[[(2S)-1-[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]amino]-5-[(N'-methylcarbamimidoyl)amino]-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]carbamoyl]hydrazinyl]-1-oxo-3-phenylpropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]butanediamide
   Show/Hide
C52H75N15O13
 1
1
Ki = 0.2 nM
   TI
   LI
   LO
   TS
CP0258833
(2S)-2-[[(2S)-2-[[(2R)-4-amino-2-[[(2R)-2-amino-3-pyridin-3-ylpropanoyl]amino]-4-oxobutanoyl]amino]-3-cyclohexylpropanoyl]amino]-N-[(2S)-1-[[(2S)-1-[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]amino]-5-[(N'-methylcarbamimidoyl)amino]-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]carbamoyl]hydrazinyl]-1-oxo-3-phenylpropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]butanediamide
   Show/Hide
C60H88N18O13
 1
1
Ki = 0.2 nM
   TI
   LI
   LO
   TS
CP0336463
(2S)-N-[(2S)-1-[[(2S)-1-[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]amino]-5-[(N'-methylcarbamimidoyl)amino]-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]carbamoyl]hydrazinyl]-1-oxo-3-phenylpropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]-2-[[(2S)-2-[[(2R)-2-amino-3-pyridin-3-ylpropanoyl]amino]-3-phenylpropanoyl]amino]butanediamide
   Show/Hide
C56H76N16O11
 1
1
Ki = 0.2 nM
   TI
   LI
   LO
   TS
CP0134996
(2S)-2-[[(2S)-2-[[(2R)-2-amino-3-(4-hydroxyphenyl)propanoyl]amino]-3-hydroxypropanoyl]amino]-N-[(2S)-1-[[(2S)-1-[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]amino]-5-[(N'-methylcarbamimidoyl)amino]-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]carbamoyl]hydrazinyl]-1-oxo-3-phenylpropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]butanediamide
   Show/Hide
C51H73N15O13
 1
1
Ki = 0.21 nM
   TI
   LI
   LO
   TS
CP0334234
(2R)-N-[(2S)-1-[[(2S)-4-amino-1-[[(2S)-1-[[(2S)-1-[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]amino]-5-[(N'-methylcarbamimidoyl)amino]-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]carbamoyl]hydrazinyl]-1-oxo-3-phenylpropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-1-oxo-3-pyridin-4-ylpropan-2-yl]-2-[[(2S)-2-amino-3-(4-hydroxyphenyl)propanoyl]amino]butanediamide
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C60H82N18O14
 1
1
Ki = 0.21 nM
   TI
   LI
   LO
   TS
CP0105322
(2R)-N-[(2S,3R)-1-[[(2S)-4-amino-1-[[(2S)-1-[[(2S)-1-[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]amino]-5-[(N'-methylcarbamimidoyl)amino]-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]carbamoyl]hydrazinyl]-1-oxo-3-phenylpropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]-2-[[(2R)-2-amino-3-(4-hydroxyphenyl)propanoyl]amino]butanediamide
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C56H81N17O15
 1
1
Ki = 0.29 nM
   TI
   LI
   LO
   TS
CP0242406
(2S)-N-[(2S)-1-[[(2S)-4-amino-1-[[(2S)-1-[[(2S)-1-[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]amino]-5-[(N'-methylcarbamimidoyl)amino]-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]carbamoyl]hydrazinyl]-1-oxo-3-phenylpropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]-2-[[(2R)-2-aminopropanoyl]amino]butanediamide
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C57H80N18O13
 1
1
Ki = 0.51 nM
   TI
   LI
   LO
   TS
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0039237
(2S)-2-[(2S)-2-[(2S)-2-[(2S)-2-amino-3-(4-hydroxyphenyl)propanamido]butanediamido]-3-(1H-indol-3-yl)propanamido]-N-[(1S)-1-{[(1S)-1-[({[(1S)-1-{[(1S)-4-carbamimidamido-1-{[(1S)-1-carbamoyl-2-phenylethyl]carbamoyl}butyl]carbamoyl}-3-methylbutyl]carbamoyl}methyl)carbamoyl]-2-phenylethyl]carbamoyl}-2-hydroxyethyl]butanediamide
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C63H83N17O14
 4
1 IC50 = 0.082 nM
2 IC50 = 0.12 nM
3 Ki = 0.062 nM
4 Ki = 1.3 nM
CP0083575
(2S)-N-[(2S)-1-[[(2S)-4-amino-1-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]amino]-5-[(N'-methylcarbamimidoyl)amino]-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-2-oxoethyl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]-2-[[(2R)-2-amino-3-(4-hydroxyphenyl)propanoyl]amino]butanediamide
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C64H85N17O14
 1
1 IC50 = 0.11 nM
CP0158503
(2R,3E)-N-[(1S)-4-carbamimidamido-1-{[(1S)-1-carbamoyl-2-(1H-indol-3-yl)ethyl]carbamoyl}butyl]-5-[(2S)-2-[(4-fluorophenyl)formamido]-3-phenylpropanamido]-2-(2-methylpropyl)pent-3-enamide
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C42H52FN9O5
 1
1 IC50 = 0.12 nM
CP0180522
(2S)-N-[(2S)-1-[[(2S)-4-amino-1-[[(2S)-1-[[(2S)-1-[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]amino]-5-[(N'-methylcarbamimidoyl)amino]-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]carbamoyl]hydrazinyl]-1-oxo-3-phenylpropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]-2-[[(2R)-2-amino-3-(4-hydroxyphenyl)propanoyl]amino]butanediamide
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C63H84N18O14
 1
1 IC50 = 0.16 nM
CP0260603
(2S)-N-[(2R)-1-[[(2S)-4-amino-1-[[(2S)-1-[[(2S)-1-[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]amino]-5-[(N'-methylcarbamimidoyl)amino]-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]carbamoyl]hydrazinyl]-1-oxo-3-phenylpropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]-2-[[(2R)-2-amino-3-(4-hydroxyphenyl)propanoyl]amino]butanediamide
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C63H84N18O14
 1
1 IC50 = 0.19 nM
CP0247747
(2S)-N-[(2R)-1-[[(2S)-4-amino-1-[[(2S)-1-[[(2S)-1-[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]amino]-5-[(N'-methylcarbamimidoyl)amino]-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]carbamoyl]hydrazinyl]-1-oxo-3-phenylpropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-1-oxo-3-pyridin-4-ylpropan-2-yl]-2-[[(2R)-2-amino-3-(4-hydroxyphenyl)propanoyl]amino]butanediamide
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C60H82N18O14
 1
1 IC50 = 0.28 nM
CP0225128
(2S)-N-[(2S)-1-[[(2S)-4-amino-1-[[(2S)-1-[[(2S)-1-[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]amino]-5-[(N'-methylcarbamimidoyl)amino]-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]carbamoyl]hydrazinyl]-1-oxo-3-phenylpropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-1-oxo-3-pyridin-4-ylpropan-2-yl]-2-[[(2R)-2-amino-3-(4-hydroxyphenyl)propanoyl]amino]butanediamide
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C60H82N18O14
 1
1 IC50 = 0.3 nM
CP0210913
(2S)-N-[(1S)-4-carbamimidamido-1-{[(1S)-1-carbamoyl-2-(1H-indol-3-yl)ethyl]carbamoyl}butyl]-2-{2-[(2S)-2-[(4-fluorophenyl)formamido]-3-phenylpropanamido]acetamido}-4-methylpentanamide
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C41H51FN10O6
 1
1 IC50 = 0.71 nM
CP0083577
(2S)-2-[[(2R)-2-[[(2R)-2-amino-3-(4-hydroxyphenyl)propanoyl]amino]-3-pyridin-4-ylpropanoyl]amino]-N-[(2S)-1-[[(2S)-1-[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]amino]-5-[(N'-methylcarbamimidoyl)amino]-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]carbamoyl]hydrazinyl]-1-oxo-3-phenylpropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]butanediamide
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C56H76N16O12
 2
1 IC50 ~ 8.94 nM
2 Ki ~ 0.089 nM
CP0263412
(2S)-2-{[(2S)-1-[(2S)-2-amino-4-methylpentanoyl]pyrrolidin-2-yl]formamido}-N-[(1S)-1-{[(1S)-1-{[(1S)-1-{[(1S)-1-{[(1S)-1-{[(1S)-1-[({[(1S)-1-{[(1S)-4-carbamimidamido-1-{[(1S)-1-carbamoyl-2-phenylethyl]carbamoyl}butyl]carbamoyl}-3-methylbutyl]carbamoyl}methyl)carbamoyl]-2-phenylethyl]carbamoyl}ethyl]carbamoyl}-2-carbamoylethyl]carbamoyl}-2-(1H-indol-3-yl)ethyl]carbamoyl}-2-carbamoylethyl]carbamoyl}-2-(4-hydroxyphenyl)ethyl]butanediamide
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C78H107N21O17
 1
1 Ki = 0.8 nM
CP0263411
(2S)-2-{[(2S)-1-[(2S)-2-amino-4-methylpentanoyl]pyrrolidin-2-yl]formamido}-N-[(1S)-1-{[(1S)-1-{[(1S)-1-{[(1S)-1-{[(1S)-1-{[(1S)-1-[({[(1S)-1-{[(1S)-4-carbamimidamido-1-{[(1S)-1-carbamoyl-2-(1H-indol-3-yl)ethyl]carbamoyl}butyl]carbamoyl}-3-methylbutyl]carbamoyl}methyl)carbamoyl]-2-phenylethyl]carbamoyl}-2-hydroxyethyl]carbamoyl}-2-carbamoylethyl]carbamoyl}-2-(1H-indol-3-yl)ethyl]carbamoyl}-2-carbamoylethyl]carbamoyl}-2-(4-hydroxyphenyl)ethyl]butanediamide
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C80H108N22O18
 1
1 Ki = 1.6 nM
CP0311596
(2S)-2-{[(2S)-1-[(2S)-2-amino-4-methylpentanoyl]pyrrolidin-2-yl]formamido}-N-[(1S)-1-{[(1S)-1-{[(1S)-1-{[(1S)-1-{[(1S)-1-{[(1S)-1-[({[(1S)-1-{[(1S)-4-carbamimidamido-1-{[(1S)-1-carbamoyl-2-phenylethyl]carbamoyl}butyl]carbamoyl}-3-methylbutyl]carbamoyl}methyl)carbamoyl]-2-phenylethyl]carbamoyl}-2-hydroxyethyl]carbamoyl}-2-carbamoylethyl]carbamoyl}ethyl]carbamoyl}-2-carbamoylethyl]carbamoyl}-2-(4-hydroxyphenyl)ethyl]butanediamide
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C70H102N20O18
 1
1 Ki = 1.8 nM
CP0307952
(2S)-2-{[(2S)-1-[(2S)-2-amino-4-methylpentanoyl]pyrrolidin-2-yl]formamido}-N-[(1S)-1-{[(1S)-1-{[(1S)-1-{[(1S)-1-{[(1S)-1-{[(1S)-1-[({[(1S)-1-{[(1S)-4-carbamimidamido-1-{[(1S)-1-carbamoyl-2-phenylethyl]carbamoyl}butyl]carbamoyl}-3-methylbutyl]carbamoyl}methyl)carbamoyl]-2-cyclohexylethyl]carbamoyl}-2-hydroxyethyl]carbamoyl}-2-carbamoylethyl]carbamoyl}-2-(1H-indol-3-yl)ethyl]carbamoyl}-2-carbamoylethyl]carbamoyl}-2-(4-hydroxyphenyl)ethyl]butanediamide
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C78H113N21O18
 1
1 Ki = 2 nM
CP0289489
(2S)-2-{[(2S)-1-[(2S)-2-amino-4-methylpentanoyl]pyrrolidin-2-yl]formamido}-N-[(1S)-1-{[(1S)-1-{[(1S)-1-{[(1S)-1-{[(1S)-1-{[(1S)-1-[({[(1S)-1-{[(1S)-4-carbamimidamido-1-{[(1S)-1-carbamoyl-2-phenylethyl]carbamoyl}butyl]carbamoyl}-3-methylbutyl]carbamoyl}methyl)carbamoyl]-2-(pyridin-3-yl)ethyl]carbamoyl}-2-hydroxyethyl]carbamoyl}-2-carbamoylethyl]carbamoyl}-2-(1H-indol-3-yl)ethyl]carbamoyl}-2-carbamoylethyl]carbamoyl}-2-(4-hydroxyphenyl)ethyl]butanediamide
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C77H106N22O18
 1
1 Ki = 4.7 nM
CP0311595
(2S)-2-{[(2S)-1-[(2S)-2-amino-4-methylpentanoyl]pyrrolidin-2-yl]formamido}-N-[(1S)-1-{[(1S)-1-{[(1S)-1-{[(1S)-1-{[(1S)-1-{[(1S)-1-{[(1S)-1-{[(1S)-1-{[(1S)-4-carbamimidamido-1-{[(1S)-1-carbamoyl-2-phenylethyl]carbamoyl}butyl]carbamoyl}-3-methylbutyl]carbamoyl}ethyl]carbamoyl}-2-phenylethyl]carbamoyl}-2-hydroxyethyl]carbamoyl}-2-carbamoylethyl]carbamoyl}-2-(1H-indol-3-yl)ethyl]carbamoyl}-2-carbamoylethyl]carbamoyl}-2-(4-hydroxyphenyl)ethyl]butanediamide
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C79H109N21O18
 1
1 Ki = 5 nM
CP0172588
(2S)-2-{[(2S)-1-[(2S)-2-amino-4-methylpentanoyl]pyrrolidin-2-yl]formamido}-N-[(1S)-1-{[(1S)-1-{[(1S)-1-{[(1S)-1-{[(1S)-1-{[(1S)-1-[({[(1S)-1-{[(1S)-4-carbamimidamido-1-{[(1S)-1-carbamoyl-2-phenylethyl]carbamoyl}butyl]carbamoyl}-3-methylbutyl]carbamoyl}methyl)carbamoyl]-2-(1H-indol-3-yl)ethyl]carbamoyl}-2-hydroxyethyl]carbamoyl}-2-carbamoylethyl]carbamoyl}-2-(1H-indol-3-yl)ethyl]carbamoyl}-2-carbamoylethyl]carbamoyl}-2-(4-hydroxyphenyl)ethyl]butanediamide
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C80H108N22O18
 1
1 Ki = 7.7 nM
CP0160204
(2S)-2-{[(2S)-1-[(2S)-2-amino-4-methylpentanoyl]pyrrolidin-2-yl]formamido}-N-[(1S)-1-{[(1S)-1-{[(1S)-1-{[(1S)-1-{[(1S)-1-{[(1S)-1-[({[(1S)-1-{[(1S)-4-carbamimidamido-1-{[(1S)-1-carbamoyl-2-(pyridin-3-yl)ethyl]carbamoyl}butyl]carbamoyl}-3-methylbutyl]carbamoyl}methyl)carbamoyl]-2-phenylethyl]carbamoyl}-2-hydroxyethyl]carbamoyl}-2-carbamoylethyl]carbamoyl}-2-(1H-indol-3-yl)ethyl]carbamoyl}-2-carbamoylethyl]carbamoyl}-2-(4-hydroxyphenyl)ethyl]butanediamide
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C77H106N22O18
 1
1 Ki = 9.3 nM
CP0039239
(2S)-N-[(1S)-1-{[(1S)-1-{[(1S)-1-{[(1S)-1-{[(1S)-1-{[(1S)-1-[({[(1S)-1-{[(1S)-5-amino-1-{[(1S)-1-carbamoyl-2-phenylethyl]carbamoyl}pentyl]carbamoyl}-3-methylbutyl]carbamoyl}methyl)carbamoyl]-2-phenylethyl]carbamoyl}-2-hydroxyethyl]carbamoyl}-2-carbamoylethyl]carbamoyl}-2-(1H-indol-3-yl)ethyl]carbamoyl}-2-carbamoylethyl]carbamoyl}-2-(4-hydroxyphenyl)ethyl]-2-{[(2S)-1-[(2S)-2-amino-4-methylpentanoyl]pyrrolidin-2-yl]formamido}butanediamide
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C78H107N19O18
 1
1 Ki = 9.4 nM
CP0039241
(2S)-2-{[(2S)-1-[(2S)-2-amino-4-methylpentanoyl]pyrrolidin-2-yl]formamido}-N-[(1S)-1-{[(1S)-1-{[(1S)-1-{[(1S)-1-{[(1S)-1-{[(1S)-1-[({[(1S)-1-{[(1S)-4-carbamimidamido-1-{[(1S)-1-carbamoyl-2-cyclohexylethyl]carbamoyl}butyl]carbamoyl}-3-methylbutyl]carbamoyl}methyl)carbamoyl]-2-phenylethyl]carbamoyl}-2-hydroxyethyl]carbamoyl}-2-carbamoylethyl]carbamoyl}-2-(1H-indol-3-yl)ethyl]carbamoyl}-2-carbamoylethyl]carbamoyl}-2-(4-hydroxyphenyl)ethyl]butanediamide
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C78H113N21O18
 1
1 Ki = 11.1 nM
CP0192813
(2S)-2-{[(2S)-1-[(2S)-2-amino-4-methylpentanoyl]pyrrolidin-2-yl]formamido}-N-[(1S)-1-{[(1S)-1-{[(1S)-1-{[(1S)-1-{[(1S)-1-{[(1S)-1-[({[(1S)-1-{[(1S)-4-carbamimidamido-1-{[(1S)-1-carbamoyl-2-phenylethyl]carbamoyl}butyl]carbamoyl}pentyl]carbamoyl}methyl)carbamoyl]-2-phenylethyl]carbamoyl}-2-hydroxyethyl]carbamoyl}-2-carbamoylethyl]carbamoyl}-2-(1H-indol-3-yl)ethyl]carbamoyl}-2-carbamoylethyl]carbamoyl}-2-(4-hydroxyphenyl)ethyl]butanediamide
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C78H107N21O18
 1
1 Ki = 15.8 nM
CP0360703
(2S)-2-{[(2S)-1-[(2S)-2-amino-4-methylpentanoyl]pyrrolidin-2-yl]formamido}-N-[(1S)-1-{[(1S)-1-{[(1S)-1-{[(1S)-1-{[(1S)-1-{[(1S)-1-[({[(1S)-1-{[(1S)-4-carbamimidamido-1-{[(1S)-1-carbamoyl-2-phenylethyl]carbamoyl}butyl]carbamoyl}-3-methylbutyl]carbamoyl}methyl)carbamoyl]-2-(4-hydroxyphenyl)ethyl]carbamoyl}-2-hydroxyethyl]carbamoyl}-2-carbamoylethyl]carbamoyl}-2-(1H-indol-3-yl)ethyl]carbamoyl}-2-carbamoylethyl]carbamoyl}-2-(4-hydroxyphenyl)ethyl]butanediamide
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C78H107N21O19
 1
1 Ki = 16.2 nM
CP0192815
(2S)-2-{[(2S)-1-[(2S)-2-amino-4-methylpentanoyl]pyrrolidin-2-yl]formamido}-N-[(1S)-1-{[(1S)-1-{[(1S)-1-{[(1S)-1-{[(1S)-1-{[(1S)-1-[({[(1S)-1-{[(1S)-4-carbamimidamido-1-{[(1S)-1-carbamoyl-2-phenylethyl]carbamoyl}butyl]carbamoyl}-3-methylbutyl]carbamoyl}methyl)carbamoyl]-2-phenylethyl]carbamoyl}-2-hydroxyethyl]carbamoyl}-2-carbamoylethyl]carbamoyl}-2-(1H-indol-3-yl)ethyl]carbamoyl}ethyl]carbamoyl}-2-(4-hydroxyphenyl)ethyl]butanediamide
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C77H106N20O17
 1
1 Ki = 21.1 nM
CP0347616
(2S)-2-{[(2S)-1-[(2S)-2-amino-4-methylpentanoyl]pyrrolidin-2-yl]formamido}-N-[(1S)-1-{[(1S)-1-{[(1S)-1-{[(1S)-1-{[(1S)-1-{[(1S)-1-[({[(1S)-1-{[(1S)-4-carbamimidamido-1-{[(1S)-1-carbamoyl-2-phenylethyl]carbamoyl}butyl]carbamoyl}ethyl]carbamoyl}methyl)carbamoyl]-2-phenylethyl]carbamoyl}-2-hydroxyethyl]carbamoyl}-2-carbamoylethyl]carbamoyl}-2-(1H-indol-3-yl)ethyl]carbamoyl}-2-carbamoylethyl]carbamoyl}-2-(4-hydroxyphenyl)ethyl]butanediamide
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C75H101N21O18
 1
1 Ki = 29.5 nM
CP0171873
(2S)-2-{[(2S)-1-[(2S)-2-amino-4-methylpentanoyl]pyrrolidin-2-yl]formamido}-N-[(1S)-1-{[(1S)-1-{[(1S)-1-{[(1S)-1-{[(1S)-1-{[(1S)-1-[({[(1S)-1-{[(1S)-4-carbamimidamido-1-{[(1S)-1-carbamoyl-2-phenylethyl]carbamoyl}butyl]carbamoyl}-3-methylbutyl]carbamoyl}methyl)carbamoyl]-2-phenylethyl]carbamoyl}-2-hydroxyethyl]carbamoyl}ethyl]carbamoyl}-2-(1H-indol-3-yl)ethyl]carbamoyl}-2-carbamoylethyl]carbamoyl}-2-(4-hydroxyphenyl)ethyl]butanediamide
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C77H106N20O17
 1
1 Ki = 33.4 nM
CP0336559
(2S)-2-{[(2S)-1-[(2S)-2-amino-4-methylpentanoyl]pyrrolidin-2-yl]formamido}-N-[(1S)-1-{[(1S)-1-{[(1S)-1-{[(1S)-1-{[(1S)-1-{[(1S)-1-[({[(1S,2S)-1-{[(1S)-4-carbamimidamido-1-{[(1S)-1-carbamoyl-2-phenylethyl]carbamoyl}butyl]carbamoyl}-2-methylbutyl]carbamoyl}methyl)carbamoyl]-2-phenylethyl]carbamoyl}-2-hydroxyethyl]carbamoyl}-2-carbamoylethyl]carbamoyl}-2-(1H-indol-3-yl)ethyl]carbamoyl}-2-carbamoylethyl]carbamoyl}-2-(4-hydroxyphenyl)ethyl]butanediamide
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C78H107N21O18
 1
1 Ki = 51.5 nM
CP0360704
(2S)-2-[(2S)-2-[(2S)-2-{[(2S)-1-[(2S)-2-amino-4-methylpentanoyl]pyrrolidin-2-yl]formamido}-3-carbamoylpropanamido]-3-(4-hydroxyphenyl)propanamido]-N-[(1S)-1-{[(1S)-2-carbamoyl-1-{[(1S)-1-{[(1S)-1-[({[(1S)-1-{[(1S)-1-{[(1S)-1-carbamoyl-2-phenylethyl]carbamoyl}ethyl]carbamoyl}-3-methylbutyl]carbamoyl}methyl)carbamoyl]-2-phenylethyl]carbamoyl}-2-hydroxyethyl]carbamoyl}ethyl]carbamoyl}-2-(1H-indol-3-yl)ethyl]butanediamide
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C75H100N18O18
 1
1 Ki = 82.7 nM
CP0192812
(2S)-2-[(2S)-2-[(2S)-2-{[(2S)-1-[(2S)-2-amino-4-methylpentanoyl]pyrrolidin-2-yl]formamido}-3-carbamoylpropanamido]-3-(4-hydroxyphenyl)propanamido]-N-[(1S)-1-{[(1S)-2-carbamoyl-1-{[(1S)-1-{[(1S)-1-[({[(1S)-1-{[(1S)-1-{[(1S)-1-carbamoyl-2-phenylethyl]carbamoyl}-4-(carbamoylamino)butyl]carbamoyl}-3-methylbutyl]carbamoyl}methyl)carbamoyl]-2-phenylethyl]carbamoyl}-2-hydroxyethyl]carbamoyl}ethyl]carbamoyl}-2-(1H-indol-3-yl)ethyl]butanediamide
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C78H106N20O19
 1
1 Ki = 88.1 nM
CP0296459
(2S)-N-[(2S)-1-[[(2S)-4-amino-1-[[(2S)-1-[[(2S)-4-amino-1-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]-2-[[(2S)-1-[(2S)-2-amino-4-methylpentanoyl]pyrrolidine-2-carbonyl]amino]butanediamide
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C81H112N22O19
 1
1 Ki = 94.8 nM
CP0172585
(2S)-2-{[(2S)-1-[(2S)-2-amino-4-methylpentanoyl]pyrrolidin-2-yl]formamido}-N-[(1S)-1-{[(1S)-1-{[(1S)-1-{[(1S)-1-{[(1S)-1-{[(1S)-1-[({[(1S)-1-{[(1S)-4-carbamimidamido-1-{[(1S)-1-carbamoyl-2-phenylethyl]carbamoyl}butyl]carbamoyl}-3-methylbutyl]carbamoyl}methyl)carbamoyl]-2-(1H-imidazol-5-yl)ethyl]carbamoyl}-2-hydroxyethyl]carbamoyl}-2-carbamoylethyl]carbamoyl}-2-(1H-indol-3-yl)ethyl]carbamoyl}-2-carbamoylethyl]carbamoyl}-2-(4-hydroxyphenyl)ethyl]butanediamide
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C75H105N23O18
 1
1 Ki = 109.6 nM
CP0171871
(2S)-2-{[(2S)-1-[(2S)-2-amino-4-methylpentanoyl]pyrrolidin-2-yl]formamido}-N-[(1S)-1-{[(1S)-1-{[(1S)-1-{[(1S)-1-{[(1S)-1-{[(1S)-1-[({[(1S)-1-{[(1S)-4-carbamimidamido-1-{[(1S)-1-carbamoyl-2-phenylethyl]carbamoyl}butyl]carbamoyl}-3-methylbutyl]carbamoyl}methyl)carbamoyl]-3-methylbutyl]carbamoyl}-2-hydroxyethyl]carbamoyl}-2-carbamoylethyl]carbamoyl}-2-(1H-indol-3-yl)ethyl]carbamoyl}-2-carbamoylethyl]carbamoyl}-2-(4-hydroxyphenyl)ethyl]butanediamide
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C75H109N21O18
 1
1 Ki = 141.8 nM
CP0363148
(2S)-2-{[(2S)-1-[(2S)-2-amino-4-methylpentanoyl]pyrrolidin-2-yl]formamido}-N-[(1S)-1-{[(1S)-1-{[(1S)-1-{[(1S)-1-{[(1S)-1-{[(1S)-1-[({[(1S)-1-{[(1S)-4-carbamimidamido-1-{[(1S)-1-carbamoyl-2-(1H-imidazol-4-yl)ethyl]carbamoyl}butyl]carbamoyl}-3-methylbutyl]carbamoyl}methyl)carbamoyl]-2-phenylethyl]carbamoyl}-2-hydroxyethyl]carbamoyl}-2-carbamoylethyl]carbamoyl}-2-(1H-indol-3-yl)ethyl]carbamoyl}-2-carbamoylethyl]carbamoyl}-2-(4-hydroxyphenyl)ethyl]butanediamide
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C75H105N23O18
 1
1 Ki = 161.8 nM
CP0160205
(2S)-2-{[(2S)-1-[(2S)-2-amino-4-methylpentanoyl]pyrrolidin-2-yl]formamido}-N-[(1S)-1-{[(1S)-1-{[(1S)-1-{[(1S)-1-{[(1S)-1-{[(1S)-4-carbamimidamido-1-[({[(1S)-1-{[(1S)-4-carbamimidamido-1-{[(1S)-1-carbamoyl-2-phenylethyl]carbamoyl}butyl]carbamoyl}-3-methylbutyl]carbamoyl}methyl)carbamoyl]butyl]carbamoyl}-2-hydroxyethyl]carbamoyl}-2-carbamoylethyl]carbamoyl}-2-(1H-indol-3-yl)ethyl]carbamoyl}-2-carbamoylethyl]carbamoyl}-2-(4-hydroxyphenyl)ethyl]butanediamide
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C75H110N24O18
 1
1 Ki = 196.7 nM
CP0363155
(2S)-2-{[(2S)-1-[(2S)-2-amino-4-methylpentanoyl]pyrrolidin-2-yl]formamido}-N-[(1S)-1-{[(1S)-1-{[(1S)-1-{[(1S)-1-{[(1S)-1-{[(1S)-1-[({[(1S)-1-{[(1S)-4-carbamimidamido-1-{[(1S)-1-carbamoyl-2-phenylethyl]carbamoyl}butyl]carbamoyl}-3-methylbutyl]carbamoyl}methyl)carbamoyl]ethyl]carbamoyl}-2-hydroxyethyl]carbamoyl}-2-carbamoylethyl]carbamoyl}-2-(1H-indol-3-yl)ethyl]carbamoyl}-2-carbamoylethyl]carbamoyl}-2-(4-hydroxyphenyl)ethyl]butanediamide
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C72H103N21O18
 1
1 Ki = 198.3 nM
CP0171872
(2S)-2-{[(2S)-1-[(2S)-2-amino-4-methylpentanoyl]pyrrolidin-2-yl]formamido}-N-[(1S)-1-{[(1S)-1-{[(1S)-1-{[(1S)-1-{[(1S)-1-{[(1S)-1-[({[(1S)-1-{[(1S)-4-carbamimidamido-1-{[(1S)-1-carbamoylethyl]carbamoyl}butyl]carbamoyl}-3-methylbutyl]carbamoyl}methyl)carbamoyl]-2-phenylethyl]carbamoyl}-2-hydroxyethyl]carbamoyl}-2-carbamoylethyl]carbamoyl}-2-(1H-indol-3-yl)ethyl]carbamoyl}-2-carbamoylethyl]carbamoyl}-2-(4-hydroxyphenyl)ethyl]butanediamide
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C72H103N21O18
 1
1 Ki = 240.2 nM
CP0160206
(2S)-2-[(2S)-2-[(2S)-2-[(2S)-2-[(2S)-2-[(2S)-2-[(2S)-2-{[(2S)-1-[(2S)-2-amino-4-methylpentanoyl]pyrrolidin-2-yl]formamido}-3-carbamoylpropanamido]-3-(4-hydroxyphenyl)propanamido]-3-carbamoylpropanamido]-3-(1H-indol-3-yl)propanamido]-3-carbamoylpropanamido]-3-hydroxypropanamido]-N-({[(1S)-1-{[(1S)-4-carbamimidamido-1-{[(1S)-1-carbamoyl-2-phenylethyl]carbamoyl}butyl]carbamoyl}-3-methylbutyl]carbamoyl}methyl)pentanediamide
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C74H106N22O19
 1
1 Ki = 298.2 nM
CP0263410
(2S)-2-[(2S)-2-[(2S)-2-{2-[(2S)-2-[(2S)-2-[(2S)-2-[(2S)-2-[(2S)-2-[(2S)-2-[(2S)-2-{[(2S)-1-[(2S)-2-amino-4-methylpentanoyl]pyrrolidin-2-yl]formamido}-3-carbamoylpropanamido]-3-(4-hydroxyphenyl)propanamido]-3-carbamoylpropanamido]-3-(1H-indol-3-yl)propanamido]-3-carbamoylpropanamido]-3-hydroxypropanamido]-3-phenylpropanamido]acetamido}-4-methylpentanamido]-5-carbamimidamidopentanamido]pentanediamide
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C74H106N22O19
 1
1 Ki = 494.9 nM
CP0160202
(2S)-2-[[(2S)-2-[[(2S)-2-[[2-[[(2S)-2-[[(2S)-2-[[(2S)-4-amino-2-[[(2S)-2-[[(2S)-4-amino-2-[[(2S)-2-[[(2S)-4-amino-2-[[(2S)-1-[(2S)-2-amino-4-methylpentanoyl]pyrrolidine-2-carbonyl]amino]-4-oxobutanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-4-oxobutanoyl]amino]-3-(1H-indol-3-yl)propanoyl]amino]-4-oxobutanoyl]amino]-3-hydroxypropanoyl]amino]-3-phenylpropanoyl]amino]acetyl]amino]-4-methylpentanoyl]amino]-5-carbamimidamidopentanoyl]amino]-3-phenylpropanoic acid
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C78H106N20O19
 1
1 Ki = 551.8 nM
CP0171867
(2S)-2-{[(2S)-1-[(2S)-2-amino-4-methylpentanoyl]pyrrolidin-2-yl]formamido}-N-[(1S)-1-{[(1S)-1-{[(1S)-1-{[(1S)-1-{[(1S)-1-{[(1S)-1-{[(1S)-1-{[(1S)-1-{[(1S)-4-carbamimidamido-1-{[(1S)-1-carbamoyl-2-phenylethyl]carbamoyl}butyl]carbamoyl}-3-methylbutyl]carbamoyl}-3-methylbutyl]carbamoyl}-2-phenylethyl]carbamoyl}-2-hydroxyethyl]carbamoyl}-2-carbamoylethyl]carbamoyl}-2-(1H-indol-3-yl)ethyl]carbamoyl}-2-carbamoylethyl]carbamoyl}-2-(4-hydroxyphenyl)ethyl]butanediamide
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C82H115N21O18
 1
1 Ki = 775.2 nM
CP0039240
(2S)-2-{[(2S)-1-[(2S)-2-amino-4-methylpentanoyl]pyrrolidin-2-yl]formamido}-N-[(1S)-1-{[(1S)-1-{[(1S)-1-{[(1S)-1-{[(1S)-1-{[(2S)-1-[(2S)-2-{[(1S)-1-{[(1S)-4-carbamimidamido-1-{[(1S)-1-carbamoyl-2-phenylethyl]carbamoyl}butyl]carbamoyl}-3-methylbutyl]carbamoyl}pyrrolidin-1-yl]-1-oxo-3-phenylpropan-2-yl]carbamoyl}-2-hydroxyethyl]carbamoyl}-2-carbamoylethyl]carbamoyl}-2-(1H-indol-3-yl)ethyl]carbamoyl}-2-carbamoylethyl]carbamoyl}-2-(4-hydroxyphenyl)ethyl]butanediamide
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C81H111N21O18
 1
1 Ki = 10000 nM
CP0160203
(2S)-2-{[(2S)-1-[(2S)-2-amino-4-methylpentanoyl]pyrrolidin-2-yl]formamido}-N-[(1S)-1-{[(1S)-1-{[(1S)-1-{[(1S)-1-{[(1S)-1-{[(1S)-1-[({[(1S)-1-{[(1S)-4-carbamimidamido-1-{[(1S)-4-carbamimidamido-1-carbamoylbutyl]carbamoyl}butyl]carbamoyl}-3-methylbutyl]carbamoyl}methyl)carbamoyl]-2-phenylethyl]carbamoyl}-2-hydroxyethyl]carbamoyl}-2-carbamoylethyl]carbamoyl}-2-(1H-indol-3-yl)ethyl]carbamoyl}-2-carbamoylethyl]carbamoyl}-2-(4-hydroxyphenyl)ethyl]butanediamide
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C75H110N24O18
 1
1 Ki = 10000 nM
CP0171869
(2S)-N-[(2S)-1-[[(2S)-4-amino-1-[[(2S)-1-[[(2S)-4-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]-2-[[(2S)-1-[(2S)-2-amino-4-methylpentanoyl]pyrrolidine-2-carbonyl]amino]butanediamide
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C76H104N20O17
 1
1 Ki = 10000 nM
CP0171870
(2S)-2-{[(2S)-1-[(2S)-2-amino-4-methylpentanoyl]pyrrolidin-2-yl]formamido}-N-[(1S)-1-{[(1S)-1-{[(1S)-1-{[(1S)-1-{[(1S)-1-{[(1S)-1-[({[(1S)-1-{[(1S)-4-carbamimidamido-1-{[(1S)-4-carbamimidamido-1-carbamoylbutyl]carbamoyl}butyl]carbamoyl}-3-methylbutyl]carbamoyl}methyl)carbamoyl]ethyl]carbamoyl}-2-hydroxyethyl]carbamoyl}-2-carbamoylethyl]carbamoyl}-2-(1H-indol-3-yl)ethyl]carbamoyl}-2-carbamoylethyl]carbamoyl}-2-(4-hydroxyphenyl)ethyl]butanediamide
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C69H106N24O18
 1
1 Ki = 10000 nM
CP0172583
(2S)-2-{[(2S)-1-[(2S)-2-amino-4-methylpentanoyl]pyrrolidin-2-yl]formamido}-N-[(1S)-1-{[(1S)-1-{[(1S)-1-{[(1S)-1-{[(1S)-1-{[(1S)-1-[({[(1S)-1-{[(1S)-4-carbamimidamido-1-{[(1S)-1-carbamoylethyl]carbamoyl}butyl]carbamoyl}-3-methylbutyl]carbamoyl}methyl)carbamoyl]ethyl]carbamoyl}-2-hydroxyethyl]carbamoyl}-2-carbamoylethyl]carbamoyl}-2-(1H-indol-3-yl)ethyl]carbamoyl}-2-carbamoylethyl]carbamoyl}-2-(4-hydroxyphenyl)ethyl]butanediamide
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C66H99N21O18
 1
1 Ki = 10000 nM
CP0360772
(2S)-2-{[(2S)-1-[(2S)-2-amino-4-methylpentanoyl]pyrrolidin-2-yl]formamido}-N-[(1S)-1-{[(1S)-1-{[(1S)-1-{[(1S)-1-{[(1S)-1-{[(1S)-1-({2-[(2S)-2-{[(1S)-4-carbamimidamido-1-{[(1S)-1-carbamoyl-2-phenylethyl]carbamoyl}butyl]carbamoyl}pyrrolidin-1-yl]-2-oxoethyl}carbamoyl)-2-phenylethyl]carbamoyl}-2-hydroxyethyl]carbamoyl}-2-carbamoylethyl]carbamoyl}-2-(1H-indol-3-yl)ethyl]carbamoyl}-2-carbamoylethyl]carbamoyl}-2-(4-hydroxyphenyl)ethyl]butanediamide
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C77H103N21O18
 1
1 Ki = 10000 nM
CP0363147
(2S)-2-[(2S)-2-[(2S)-2-{[(2S)-1-[(2S)-2-amino-4-methylpentanoyl]pyrrolidin-2-yl]formamido}-3-carbamoylpropanamido]-3-(4-hydroxyphenyl)propanamido]-N-[(1S)-1-{[(1S)-2-carbamoyl-1-{[(1S)-1-{[(1S)-1-[({[(1S)-1-{[(1S)-1-{[(1S)-1-carbamoyl-2-phenylethyl]carbamoyl}-3-phenylpropyl]carbamoyl}-3-methylbutyl]carbamoyl}methyl)carbamoyl]-2-phenylethyl]carbamoyl}-2-hydroxyethyl]carbamoyl}ethyl]carbamoyl}-2-(1H-indol-3-yl)ethyl]butanediamide
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C82H106N18O18
 1
1 Ki = 10000 nM
Clinical Information about the Protein
Target 1 ( G-protein coupled receptor 54 (KISS1R) )
Target Type Discontinued Target
Disease 1 Target-related Disease  1
1 Prostate cancer [ICD-11: 2C82.0]
Discontinued Drug(s) 1 Discontinued Drug  1
1 TAK-683 Discontinued in Phase 1
Prostate cancer