Brief Information of the Cell Line and Protein
Cell Line ID: CL000011 , CHO
Synonyms
Chinese Hamster Ovary
CHO-ori
Category Spontaneously immortalized cell line
Organism
Cricetulus griseus (Chinese hamster)
Cellosaurus ID
CVCL_0213
Protein ID: PT01804 , Melanocortin receptor 5
Gene Name MC5R
Organism Homo sapiens, Human
Protein Classification Membrane receptor
Uniprot ID P33032
Table of Molecular Bioactivities Related to the Cell Line and Protein
Cell Line ID: CL000011  Protein ID: PT01804
 
Compound ID Compound Name Compound Formula
CP0876125
Ac-Nle4-cyclo(Asp5-Pro6-D-4,4'-Bip7-Pip8-Trp9-Lys10)-NH2
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C55H70N10O9
 2
1
EC50 = 0.031 nM
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2
IC50 = 0.15 nM
   TI
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CP0058748
15-(2-Acetylamino-hexanoylamino)-6-(3-guanidino-propyl)-12-(3H-imidazol-4-ylmethyl)-3-(1H-indol-3-ylmethyl)-9-naphthalen-2-ylmethyl-2,5,8,11,14,17-hexaoxo-1,4,7,10,13,18hexaaza-cyclotricosane-23-carboxylic acid amide
   Show/Hide
C54H71N15O9
 1
1
EC50 = 0.12 nM
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CP0291923
3-[25-Acetylamino-4-carbamoyl-13-(3-guanidino-propyl)-19-(3H-imidazol-4-ylmethyl)-10-(1H-indol-3-ylmethyl)-16-naphthalen-2-ylmethyl-6,9,12,15,18,21,24-heptaoxo-1,2-dithia-5,8,11,14,17,20,23-heptaaza-cyclohexacos-22-yl]-propionic acid
   Show/Hide
C51H63N15O11S2
 1
1
EC50 = 0.22 nM
   TI
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CP0882669
Ac-Nle4-cyclo(Asp5-Val6-D-4,4'-Bip7-Pip8-Trp9-Lys10)-NH2
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C55H72N10O9
 2
1
EC50 = 0.23 nM
   TI
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2
IC50 = 7.3 nM
   TI
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CP0878527
Ac-Nle4-cyclo(Asp5-Phg6-D-4,4'-Bip7-Pip8-Trp9-Lys10)-NH2
   Show/Hide
C58H70N10O9
 2
1
EC50 = 0.29 nM
   TI
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2
IC50 = 2.1 nM
   TI
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CP0844893
Ac-Nle4-cyclo(Asp5-His6-D-4,4'-Bip7-Pip8-Trp9-Lys10)-NH2
   Show/Hide
C56H70N12O9
 2
1
EC50 = 0.37 nM
   TI
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2
IC50 = 0.72 nM
   TI
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CP0876424
c-Nle4-cyclo(Asp5-Tic6-D-4,4'-Bip7-Pip8-Trp9-Lys10)-NH2
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C60H72N10O9
 2
1
EC50 = 0.45 nM
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2
IC50 = 2.7 nM
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CP0411217
(3S,11S,14S,17S,20R,23S)-3-[[(2S)-2-acetamidohexanoyl]amino]-20-benzyl-17-[3-(diaminomethylideneamino)propyl]-14-(1H-indol-3-ylmethyl)-2,5,13,16,19,22-hexaoxo-1,6,12,15,18,21-hexazabicyclo[21.3.0]hexacosane-11-carboxamide
   Show/Hide
C49H69N13O9
 1
1
EC50 = 0.93 nM
   TI
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   TS
CP0844894
Ac-Nle4-cyclo(Asp5-Oic6-D-4,4'-Bip7-Pip8-Trp9-Lys10)-NH2
   Show/Hide
C59H76N10O9
 2
1
EC50 = 0.99 nM
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2
IC50 = 0.95 nM
   TI
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CP0855105
Ac-Nle4-cyclo(Asp5-Chg6-D-4,4'-Bip7-Pip8-Trp9-Lys10)-NH2
   Show/Hide
C58H76N10O9
 2
1
EC50 = 1 nM
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2
IC50 = 50 nM
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CP0878544
Ac-Nle4-cyclo(Asp5-Pro6-D-4,4'-Bip7-Pro8-Trp9-Lys10)-NH2
   Show/Hide
C54H68N10O9
 2
1
EC50 = 1.6 nM
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2
IC50 = 2.9 nM
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CP0394757
Ac-Nle4-cyclo(Asp5-His6-D-4,4'-Bip-Pro8-Trp9-Lys10)-NH2
   Show/Hide
C56H69N11O9
 2
1
EC50 = 2.5 nM
   TI
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2
IC50 = 4.1 nM
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CP0274905
15-Acetylamino-6-(3-guanidino-propyl)-12-(3H-imidazol-4-ylmethyl)-3-(1H-indol-3-ylmethyl)-9-naphthalen-2-ylmethyl-2,5,8,11,14,17-hexaoxo-1,4,7,10,13,18hexaaza-cyclotricosane-23-carboxylic acid
   Show/Hide
C48H60N14O8
 1
1
EC50 = 4.2 nM
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CP0855549
Ac-Nle4-cyclo(Asp5-Oic6-D-4,4'-Bip7-Pro8-Trp9-Lys10)-NH2
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C58H74N10O9
 2
1
EC50 = 17 nM
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2
IC50 = 10 nM
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CP0045108
(4S)-4-{[(1S)-1-{[(1S)-1-{[(1S)-1-{[(1S)-1-[({[(2S)-6-amino-1-[(2S)-2-{[(1S)-1-carbamoyl-2-methylpropyl]carbamoyl}pyrrolidin-1-yl]-1-oxohexan-2-yl]carbamoyl}methyl)carbamoyl]-2-(1H-indol-3-yl)ethyl]carbamoyl}-4-carbamimidamidobutyl]carbamoyl}-2-phenylethyl]carbamoyl}-2-(1H-imidazol-5-yl)ethyl]carbamoyl}-4-[(2S)-2-[(2S)-2-[(2S)-2-[(2S)-2-acetamido-3-hydroxypropanamido]-3-(4-hydroxyphenyl)propanamido]-3-hydroxypropanamido]-4-(methylsulfanyl)butanamido]butanoic acid
   Show/Hide
C77H109N21O19S
 2
1
EC50 = 17 nM
   TI
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2
IC50 = 118 nM
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CP0201251
15-Amino-6-(3-guanidino-propyl)-12-(3H-imidazol-4-ylmethyl)-3-(1H-indol-3-ylmethyl)-9-naphthalen-2-ylmethyl-2,5,8,11,14,17-hexaoxo-1,4,7,10,13,18hexaaza-cyclotricosane-23-carboxylic acid
   Show/Hide
C46H58N14O7
 1
1
EC50 = 18 nM
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CP0137537
16-(2-Acetylamino-hexanoylamino)-6-(3-guanidino-propyl)-12-(3H-imidazol-4-ylmethyl)-3-(1H-indol-3-ylmethyl)-9-naphthalen-2-ylmethyl-2,5,8,11,14,17-hexaoxo-1,4,7,10,13,18hexaaza-cyclotricosane-23-carboxylic acid
   Show/Hide
C54H71N15O9
 1
1
EC50 = 19 nM
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CP0281018
(3R,6S,9R,12S,15S,23R)-15-((S)-2-Acetylamino-hexanoylamino)-6-(3-guanidino-propyl)-12-(3H-imidazol-4-ylmethyl)-3-(1H-indol-3-ylmethyl)-9-naphthalen-2-ylmethyl-2,5,8,11,14,17-hexaoxo-1,4,7,10,13,18hexaaza-cyclotricosane-23-carboxylic acid amide
   Show/Hide
C54H71N15O9
 1
1
EC50 = 28 nM
   TI
   LI
   LO
   TS
CP0879920
Ac-Nle4-cyclo(Asp5-Oic6-D-D-pBzlPhe7-Pip8-Trp9-Lys10)-NH2
   Show/Hide
C60H78N10O9
 2
1
EC50 = 31 nM
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2
IC50 = 24 nM
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CP0685081
Cyclo Ac-Cys-Glu-His-D-(2')Nal-Arg-Trp-Gly-Cys-Pro-Pro-Lys-Asp-NH2
   Show/Hide
C70H93N19O16S2
 1
1
EC50 = 42 nM
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CP0425206
Ac-Nle4-cyclo(Asp5-His6-D-Nal(2)-Pro8-Trp9-Lys10)-NH2
   Show/Hide
C53H66N12O9
 2
1
EC50 = 50 nM
   TI
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2
IC50 = 50 nM
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CP0793638
Cyclo Ac-Cys-Glu-His-D-Phe-(3,4-di-Cl)-Arg-Trp-Gly-Cys-Pro-Pro-Lys-Asp-NH2
   Show/Hide
C66H89Cl2N19O16S2
 1
1
EC50 = 73 nM
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CP0394150
Ac-Nle4-cyclo(Asp5-His6-D-Phe(4-Cl)-Pro8-Trp9-Lys10)-NH2
   Show/Hide
C49H63ClN12O9
 2
1
EC50 = 82 nM
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2
IC50 = 1300 nM
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CP0061104
12-(2-Acetylamino-hexanoylamino)-6-(3-guanidino-propyl)-3-(1H-indol-3-ylmethyl)-9-naphthalen-2-ylmethyl-2,5,8,11,14-pentaoxo-1,4,7,10,15pentaaza-cycloicosane-20-carboxylic acid
   Show/Hide
C48H64N12O8
 1
1
EC50 = 87 nM
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CP0083436
N-[(1S)-1-[2-[1-[(3S,4R)-4-(4-bromo-2-fluorophenyl)-1-tert-butylpyrrolidine-3-carbonyl]piperidin-4-yl]-5-chlorophenyl]propyl]acetamide
   Show/Hide
C31H40BrClFN3O2
 1
1
EC50 = 101.6 nM
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CP0161427
N-[(1S)-1-[2-[1-[(3S,4R)-1-tert-butyl-4-(2-fluoro-4-methoxyphenyl)pyrrolidine-3-carbonyl]piperidin-4-yl]-5-chlorophenyl]propyl]acetamide
   Show/Hide
C32H43ClFN3O3
 1
1
EC50 = 166.7 nM
   TI
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CP0168805
6-(3-Guanidino-propyl)-12-(3H-imidazol-4-ylmethyl)-3-(1H-indol-3-ylmethyl)-9-naphthalen-2-ylmethyl-2,5,8,11,14,17-hexaoxo-1,4,7,10,13,18hexaaza-cyclotricosane-23-carboxylic acid
   Show/Hide
C46H57N13O7
 1
1
EC50 = 170 nM
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CP0047335
12-Amino-6-(3-guanidino-propyl)-3-(1H-indol-3-ylmethyl)-9-naphthalen-2-ylmethyl-2,5,8,11,14-pentaoxo-1,4,7,10,15pentaaza-cycloicosane-20-carboxylic acid
   Show/Hide
C40H51N11O6
 1
1
EC50 = 200 nM
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CP0110629
9-(3-Guanidino-propyl)-15-(3H-imidazol-4-ylmethyl)-6-(1H-indol-3-ylmethyl)-12-naphthalen-2-ylmethyl-5,8,11,14,17,20-hexaoxo-1,4,7,10,13,16hexaaza-cycloicosane-3-carboxylic acid
   Show/Hide
C43H51N13O7
 1
1
EC50 = 210 nM
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CP0378160
(3S,5R)-N-[(2R)-1-[4-(tert-butylcarbamoyl)-4-cyclohexylpiperidin-1-yl]-3-(4-chlorophenyl)-1-oxopropan-2-yl]-3,5-dimethylpiperazine-1-carboxamide
   Show/Hide
C32H50ClN5O3
 2
1
EC50 = 210 nM
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2
IC50 = 54 nM
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CP0425195
Ac-Nle4-cyclo(Asp5-His6-D-Tyr(Et)-Pro8-Trp9-Lys10)-NH2
   Show/Hide
C51H68N12O10
 2
1
EC50 = 270 nM
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2
IC50 = 340 nM
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CP0167616
5-(3-Guanidino-propyl)-8-(1H-indol-3-ylmethyl)-2-naphthalen-2-ylmethyl-3,6,9,16,19-pentaoxo-1,4,7,10,15pentaaza-cyclononadecane-11-carboxylic acid
   Show/Hide
C39H48N10O6
 1
1
EC50 = 300 nM
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CP0853375
(S)-4-Isobutyl-piperazine-2-carboxylic acid [(R)-2-(4-tert-butylcarbamoyl-4-cyclohexyl-piperidin-1-yl)-1-(4-fluoro-benzyl)-2-oxo-ethyl]-amide; compound with 2 TFA
   Show/Hide
C38H56F7N5O7
 1
1
EC50 = 340 nM
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CP0422262
Ac-Nle4-cyclo(Asp5-His6-D-Phe-Pro8-Trp9-Lys10)-NH2
   Show/Hide
C49H64N12O9
 2
1
EC50 = 360 nM
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2
IC50 = 250 nM
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CP0202447
N-[(1S)-1-[2-[1-[(3S,4R)-1-tert-butyl-4-(4-chloro-2-fluorophenyl)pyrrolidine-3-carbonyl]piperidin-4-yl]-5-chlorophenyl]propyl]acetamide
   Show/Hide
C31H40Cl2FN3O2
 1
1
EC50 = 372 nM
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CP0162604
N-[(1S)-1-[2-[1-[(3R,4S)-4-(4-bromo-2-fluorophenyl)-1-tert-butylpyrrolidine-3-carbonyl]piperidin-4-yl]-5-chlorophenyl]propyl]acetamide
   Show/Hide
C31H40BrClFN3O2
 1
1
EC50 = 455 nM
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CP0382832
N-[2-[4-[(3S,4R)-1-tert-butyl-4-(2,4-difluorophenyl)pyrrolidine-3-carbonyl]piperazin-1-yl]-2-cyclohexylethyl]-N-propan-2-ylpyridazine-3-carboxamide
   Show/Hide
C35H50F2N6O2
 2
1
EC50 = 490 nM
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2
IC50 = 130 nM
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CP0869660
(S)-4-(2,2-Difluoro-ethyl)-piperazine-2-carboxylic acid [(R)-2-(4-tert-butylcarbamoyl-4-cyclohexyl-piperidin-1-yl)-1-(4-fluoro-benzyl)-2-oxo-ethyl]-amide; compound with 2 TFA
   Show/Hide
C36H50F9N5O7
 1
1
EC50 = 510 nM
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CP0129840
6-(3-Guanidino-propyl)-3-(1H-indol-3-ylmethyl)-9-naphthalen-2-ylmethyl-2,5,8,11,14-pentaoxo-1,4,7,10,15pentaaza-cycloicosane-20-carboxylic acid
   Show/Hide
C40H51N11O6
 1
1
EC50 = 530 nM
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CP0394113
Ac-Nle4-cyclo(Asp5-His6-D-Bth-Pro8-Trp9-Lys10)-NH2
   Show/Hide
C53H68N12O9S
 2
1
EC50 = 670 nM
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2
IC50 = 360 nM
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CP0394111
Ac-Nle4-cyclo(Asp5-His6-D-Phe(No2)-Pro8-Trp9-Lys10)-NH2
   Show/Hide
C49H63N13O11
 2
1
EC50 = 770 nM
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2
IC50 = 780 nM
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CP0895694
(S)-4-Ethyl-piperazine-2-carboxylic acid [(R)-2-(4-tert-butylcarbamoyl-4-cyclohexyl-piperidin-1-yl)-1-(4-fluoro-benzyl)-2-oxo-ethyl]-amide; compound with 2 TFA
   Show/Hide
C36H52F7N5O7
 1
1
EC50 = 840 nM
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CP0391988
(1R,4S,6S)-2-Methyl-2-aza-bicyclo[2.2.2]octane-6-carboxylic acid [(R)-2-(4-tert-butylcarbamoyl-4-cyclohexyl-piperidin-1-yl)-1-(4-fluoro-benzyl)-2-oxo-ethyl]-amide
   Show/Hide
C34H51FN4O3
 2
1
EC50 = 850 nM
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2
IC50 = 6460 nM
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CP0039210
12-Acetylamino-6-(3-guanidino-propyl)-3-(1H-indol-3-ylmethyl)-9-naphthalen-2-ylmethyl-2,5,8,11,14-pentaoxo-1,4,7,10,15pentaaza-cycloicosane-20-carboxylic acid
   Show/Hide
C42H53N11O7
 1
1
EC50 = 1000 nM
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   TS
CP0400320
N-[2-[4-[(3S,4R)-1-tert-butyl-4-(2,4-difluorophenyl)pyrrolidine-3-carbonyl]piperazin-1-yl]-2-cyclohexylethyl]-N,1-di(propan-2-yl)pyrazole-4-carboxamide
   Show/Hide
C37H56F2N6O2
 2
1
EC50 = 1000 nM
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2
IC50 = 620 nM
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CP0378158
(3R,5R)-N-[(2R)-1-[4-(tert-butylcarbamoyl)-4-cyclohexylpiperidin-1-yl]-3-(4-fluorophenyl)-1-oxopropan-2-yl]-3,5-dimethylpiperazine-1-carboxamide
   Show/Hide
C32H50FN5O3
 2
1
EC50 = 1000 nM
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2
IC50 = 1400 nM
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CP0156912
N-[(1S)-1-[2-[1-[(3S,4R)-1-tert-butyl-4-naphthalen-2-ylpyrrolidine-3-carbonyl]piperidin-4-yl]-5-chlorophenyl]propyl]acetamide
   Show/Hide
C35H44ClN3O2
 1
1
EC50 = 1233 nM
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CP0422856
(3S,5S)-N-[(2R)-1-[4-(tert-butylcarbamoyl)-4-cyclohexylpiperidin-1-yl]-3-(4-fluorophenyl)-1-oxopropan-2-yl]-3,5-dimethylpiperazine-1-carboxamide
   Show/Hide
C32H50FN5O3
 2
1
EC50 = 1400 nM
   TI
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2
IC50 = 1400 nM
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CP0394108
Ac-Nle4-cyclo(Asp5-His6-D-Tyr(Me)-Pro8-Trp9-Lys10)-NH2
   Show/Hide
C50H66N12O10
 2
1
EC50 = 1500 nM
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2
IC50 = 2600 nM
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CP0083437
N-[(1S)-1-[2-[1-[(3R,4S)-1-tert-butyl-4-(2,4-dichlorophenyl)pyrrolidine-3-carbonyl]piperidin-4-yl]-5-chlorophenyl]propyl]acetamide
   Show/Hide
C31H40Cl3N3O2
 1
1
EC50 = 1600 nM
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CP0853376
(S)-2-[(R)-2-(4-tert-Butylcarbamoyl-4-cyclohexyl-piperidin-1-yl)-1-(4-fluoro-benzyl)-2-oxo-ethylcarbamoyl]-4-methyl-piperazine-1-carboxylic acid tert-butyl ester
   Show/Hide
C35H54FN5O5
 1
1
EC50 = 1800 nM
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CP0378171
(S)-4-Methyl-piperazine-2-carboxylic acid [(R)-2-(4-tert-butylcarbamoyl-4-cyclohexyl-piperidin-1-yl)-1-(4-fluoro-benzyl)-2-oxo-ethyl]-amide
   Show/Hide
C31H48FN5O3
 1
1
EC50 = 1900 nM
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   TS
CP0391989
(1S,4R,6S)-2-Aza-bicyclo[2.2.2]octane-6-carboxylic acid [(R)-2-(4-tert-butylcarbamoyl-4-cyclohexyl-piperidin-1-yl)-1-(4-fluoro-benzyl)-2-oxo-ethyl]-amide
   Show/Hide
C33H49FN4O3
 2
1
EC50 = 1980 nM
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2
IC50 = 9870 nM
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CP0432989
Ac-Nle4-cyclo(Asp5-His6-L-Phe-Pro8-Trp9-Lys10)-NH2
   Show/Hide
C49H64N12O9
 2
1
EC50 = 2000 nM
   TI
   LI
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2
IC50 = 390 nM
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CP0918363
(S)-4-(2-Amino-propionyl)-piperazine-2-carboxylic acid [(R)-2-(4-tert-butylcarbamoyl-4-cyclohexyl-piperidin-1-yl)-1-(4-fluoro-benzyl)-2-oxo-ethyl]-amide; compound with 2 TFA
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C37H53F7N6O8
 1
1
EC50 = 2000 nM
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CP0918361
(R)-4-Methyl-piperazine-2-carboxylic acid [(R)-2-(4-tert-butylcarbamoyl-4-cyclohexyl-piperidin-1-yl)-1-(4-fluoro-benzyl)-2-oxo-ethyl]-amide dihydrochloride
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C31H50Cl2FN5O3
 1
1
EC50 = 2700 nM
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CP0400322
N-[2-[4-[(3S,4R)-1-tert-butyl-4-(2,4-difluorophenyl)pyrrolidine-3-carbonyl]piperazin-1-yl]-2-cyclohexylethyl]-N-propan-2-ylacetamide
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C32H50F2N4O2
 2
1
EC50 = 2800 nM
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2
IC50 = 660 nM
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CP0877838
(S)-1-Methyl-piperazine-2-carboxylic acid [(R)-2-(4-tert-butylcarbamoyl-4-cyclohexyl-piperidin-1-yl)-1-(4-fluoro-benzyl)-2-oxo-ethyl]-amide dihydrochloride
   Show/Hide
C31H50Cl2FN5O3
 1
1
EC50 = 3300 nM
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CP0876570
Ac-Nle4-cyclo(Asp5-Oic6-D-4,4'-Bic7-Pip8-Trp9-Lys10)-NH2
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C59H88N10O9
 2
1
EC50 > 500 nM
   TI
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2
IC50 = 700 nM
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CP0431963
Ac-Nle4-cyclo(Asp5-His6-D-2-Thi-Pro8-Trp9-Lys10)-NH2
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C47H62N12O9S
 2
1
EC50 > 1500 nM
   TI
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2
IC50 > 5000 nM
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CP0315803
(3S,5R)-N-[(2R)-1-[4-(tert-butylcarbamoyl)-4-cyclohexylpiperidin-1-yl]-3-(4-fluorophenyl)-1-oxopropan-2-yl]-3,5-dimethylpiperazine-1-carboxamide
   Show/Hide
C32H50FN5O3
 2
1
EC50 > 3000 nM
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2
IC50 = 850 nM
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CP0039213
8-(3-Guanidino-propyl)-2-(3H-imidazol-4-ylmethyl)-11-(1H-indol-3-ylmethyl)-5-naphthalen-2-ylmethyl-3,6,9,12,17-pentaoxo-1,4,7,10,13pentaaza-cyclooctadecane-14-carboxylic acid amide
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C42H50N12O6
 1
1
EC50 > 5000 nM
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CP0201349
9-(3-Guanidino-propyl)-6-(1H-indol-3-ylmethyl)-12-naphthalen-2-ylmethyl-5,8,11,14,17-pentaoxo-1,4,7,10,13pentaaza-cycloheptadecane-3-carboxylic acid
   Show/Hide
C37H44N10O6
 1
1
EC50 > 5000 nM
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CP0425204
Ac-Nle4-cyclo(Asp5-His6-D-Tyr-Pro8-Trp9-Lys10)-NH2
   Show/Hide
C51H65N13O9
 2
1
EC50 > 5000 nM
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2
IC50 = 2700 nM
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CP0382833
N-[2-[4-[(3S,4R)-1-tert-butyl-4-(2,4-difluorophenyl)pyrrolidine-3-carbonyl]piperazin-1-yl]-2-cyclohexylethyl]-N-propan-2-ylmethanesulfonamide
   Show/Hide
C31H50F2N4O3S
 2
1
EC50 > 5000 nM
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2
IC50 = 250 nM
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CP0400321
N-[2-[4-[(3S,4R)-1-tert-butyl-4-(2,4-difluorophenyl)pyrrolidine-3-carbonyl]piperazin-1-yl]-4-methylpentyl]-N-propan-2-ylacetamide
   Show/Hide
C30H48F2N4O2
 2
1
EC50 > 5000 nM
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2
IC50 = 1100 nM
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CP0400328
N-[2-[4-[(3S,4R)-1-tert-butyl-4-(2,4-difluorophenyl)pyrrolidine-3-carbonyl]piperazin-1-yl]-4-methylpentyl]-N-propan-2-ylmethanesulfonamide
   Show/Hide
C29H48F2N4O3S
 2
1
EC50 > 5000 nM
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2
IC50 = 2800 nM
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CP0405831
1-[(R)-2-[((1R,2R)-1-Amino-1,2,3,4-tetrahydro-naphthalene-2-carbonyl)-amino]-3-(4-chloro-phenyl)-propionyl]-4-cyclohexyl-piperidine-4-carboxylic acid tert-butylamide
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C36H49ClN4O3
 1
1
IC50 = 24 nM
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CP0466894
1-[(R)-2-[((1S,2S)-1-Amino-1-methyl-1,2,3,4-tetrahydro-naphthalene-2-carbonyl)-amino]-3-(4-chloro-phenyl)-propionyl]-4-cyclohexyl-piperidine-4-carboxylic acid tert-butylamide
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C37H51ClN4O3
 1
1
IC50 = 31 nM
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   TS
CP0490759
1-[2-[((R)-1-Amino-indane-2-carbonyl)-amino]-3-(4-chloro-phenyl)-propionyl]-4-cyclohexyl-piperidine-4-carboxylic acid tert-butylamide
   Show/Hide
C35H47ClN4O3
 1
1
IC50 = 34 nM
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   TS
CP0497448
1-[2-[((R)-3-Amino-1,2,3,4-tetrahydro-naphthalene-2-carbonyl)-amino]-3-(4-chloro-phenyl)-propionyl]-4-cyclohexyl-piperidine-4-carboxylic acid tert-butylamide
   Show/Hide
C36H49ClN4O3
 1
1
IC50 = 40 nM
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CP0493433
1-[(2R)-2-[(5-amino-6,7,8,9-tetrahydro-5H-benzo[7]annulene-6-carbonyl)amino]-3-(4-chlorophenyl)propanoyl]-N-tert-butyl-4-cyclohexylpiperidine-4-carboxamide
   Show/Hide
C37H51ClN4O3
 1
1
IC50 = 54 nM
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   TS
CP0150320
1-[(R)-2-[((1S,2S)-1-Amino-1,2,3,4-tetrahydro-naphthalene-2-carbonyl)-amino]-3-(4-chloro-phenyl)-propionyl]-4-cyclohexyl-piperidine-4-carboxylic acid tert-butylamide
   Show/Hide
C36H49ClN4O3
 1
1
IC50 = 64 nM
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CP0451850
(R)-N-((R)-3-(4-chlorophenyl)-1-(4-cyclohexyl-4-((4,4-dimethyl-2-oxooxazolidin-3-yl)methyl)piperidin-1-yl)-1-oxopropan-2-yl)-1,2,3,4-tetrahydroisoquinoline-3-carboxamide
   Show/Hide
C36H47ClN4O4
 1
1
IC50 = 80 nM
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CP0376350
(R)-N-((R)-3-(4-chlorophenyl)-1-(4-cyclohexyl-4-(((R)-4-methyl-2-oxooxazolidin-3-yl)methyl)piperidin-1-yl)-1-oxopropan-2-yl)-1,2,3,4-tetrahydroisoquinoline-3-carboxamide
   Show/Hide
C35H45ClN4O4
 1
1
IC50 = 110 nM
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CP0495900
(R)-N-((R)-3-(4-chlorophenyl)-1-(4-cyclohexyl-4-((2-oxoimidazolidin-1-yl)methyl)piperidin-1-yl)-1-oxopropan-2-yl)-1,2,3,4-tetrahydroisoquinoline-3-carboxamide
   Show/Hide
C34H44ClN5O3
 1
1
IC50 = 150 nM
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CP0376351
(R)-N-((R)-3-(4-chlorophenyl)-1-(4-cyclohexyl-4-((3-methyl-2-oxoimidazolidin-1-yl)methyl)piperidin-1-yl)-1-oxopropan-2-yl)-1,2,3,4-tetrahydroisoquinoline-3-carboxamide
   Show/Hide
C35H46ClN5O3
 1
1
IC50 = 160 nM
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CP0382075
(R)-1,2,3,4-tetrahydro-isoquinoline-3-carboxylic acid {(R)-1-(4-chloro-benzyl)-2-[4-cyclohexyl-4-(5-oxo-6-oxa-4-aza-spiro[2.4]hept-4-ylmethyl)-piperidin-1-yl]-2-oxo-ethyl}-amide
   Show/Hide
C36H45ClN4O4
 1
1
IC50 = 170 nM
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CP0432760
(R)-1,2,3,4-tetrahydro-isoquinoline-3-carboxylic acid {(R)-1-(4-chloro-benzyl)-2-[4-cyclohexyl-4-(1,1-dioxo-1lambda*6*-isothiazolidin-2-ylmethyl)-piperidin-1-yl]-2-oxo-ethyl}-amide
   Show/Hide
C34H45ClN4O4S
 1
1
IC50 = 170 nM
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CP0501131
(R)-N-((R)-3-(4-chlorophenyl)-1-(4-cyclohexyl-4-((2-oxooxazolidin-3-yl)methyl)piperidin-1-yl)-1-oxopropan-2-yl)-1,2,3,4-tetrahydroisoquinoline-3-carboxamide
   Show/Hide
C34H43ClN4O4
 1
1
IC50 = 180 nM
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CP0376413
(R)-1,2,3,4-tetrahydro-isoquinoline-3-carboxylic acid {(R)-1-(4-chloro-benzyl)-2-[4-cyclohexyl-4-(5,5-dimethyl-1,1-dioxo-1lambda*6*-isothiazolidin-2-ylmethyl)-piperidin-1-yl]-2-oxo-ethyl}-amide
   Show/Hide
C36H49ClN4O4S
 1
1
IC50 = 190 nM
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CP0376349
(R)-N-((R)-3-(4-chlorophenyl)-1-(4-cyclohexyl-4-((N-isopropylmethan-2-ylsulfonamido)methyl)piperidin-1-yl)-1-oxopropan-2-yl)-1,2,3,4-tetrahydroisoquinoline-3-carboxamide
   Show/Hide
C35H49ClN4O4S
 1
1
IC50 = 200 nM
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CP0497207
(R)-1,2,3,4-tetrahydro-isoquinoline-3-carboxylic acid {(R)-1-(4-chloro-benzyl)-2-[4-cyclohexyl-4-(6-oxo-7-oxa-5-aza-spiro[3.4]oct-5-ylmethyl)-piperidin-1-yl]-2-oxo-ethyl}-amide
   Show/Hide
C37H47ClN4O4
 1
1
IC50 = 210 nM
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CP0451849
(R)-N-((R)-3-(4-chlorophenyl)-1-(4-cyclohexyl-4-(((S)-4-methyl-2-oxooxazolidin-3-yl)methyl)piperidin-1-yl)-1-oxopropan-2-yl)-1,2,3,4-tetrahydroisoquinoline-3-carboxamide
   Show/Hide
C35H45ClN4O4
 1
1
IC50 = 220 nM
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CP0149367
(R)-1,2,3,4-Tetrahydro-isoquinoline-3-carboxylic acid [(R)-1-(4-chloro-benzyl)-2-(4-cyclohexyl-4-[1,2,4]triazol-1-ylmethyl-piperidin-1-yl)-2-oxo-ethyl]-amide
   Show/Hide
C33H41ClN6O2
 1
1
IC50 = 326 nM
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CP0462980
(3R,5S)-N-[(2R)-1-[4-(tert-butylcarbamoyl)-4-cyclohexylpiperidin-1-yl]-3-(4-fluorophenyl)-1-oxopropan-2-yl]-3,5-diethylpiperazine-1-carboxamide
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C34H54FN5O3
 1
1
IC50 = 430 nM
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CP0376348
ethyl N-[[1-[(2R)-3-(4-chlorophenyl)-2-[[(3R)-1,2,3,4-tetrahydroisoquinoline-3-carbonyl]amino]propanoyl]-4-cyclohexylpiperidin-4-yl]methyl]-N-propan-2-ylcarbamate
   Show/Hide
C37H51ClN4O4
 1
1
IC50 = 630 nM
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CP0445633
(4R,5S)-4-(4-Fluoro-phenyl)-piperidine-3-carboxylic acid {(R)-3-[6-(4-chloro-phenylsulfanyl)-2-(4-methoxy-phenyl)-3-oxo-2,3-dihydro-pyridazin-4-yl]-1-methyl-propyl}-amide
   Show/Hide
C33H34ClFN4O3S
 1
1
IC50 = 840 nM
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CP0378167
(1S,4R,6R)-N-[(2R)-1-[4-(tert-butylcarbamoyl)-4-cyclohexylpiperidin-1-yl]-3-(4-fluorophenyl)-1-oxopropan-2-yl]-2-azabicyclo[2.2.2]octane-6-carboxamide
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C33H49FN4O3
 1
1
IC50 = 940 nM
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CP0406608
(1S,4S,6S)-2-Aza-bicyclo[2.2.2]octane-6-carboxylic acid [(R)-2-(4-tert-butylcarbamoyl-4-cyclohexyl-piperidin-1-yl)-1-(4-fluoro-benzyl)-2-oxo-ethyl]-amide
   Show/Hide
C33H49FN4O3
 1
1
IC50 = 1020 nM
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CP0406610
(1S,4R,6S)-2-Methyl-2-aza-bicyclo[2.2.2]octane-6-carboxylic acid [(R)-2-(4-tert-butylcarbamoyl-4-cyclohexyl-piperidin-1-yl)-1-(4-fluoro-benzyl)-2-oxo-ethyl]-amide
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C34H51FN4O3
 1
1
IC50 = 1080 nM
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CP0466535
(2S,3S)-3-(4-Fluoro-phenyl)-piperidine-4-carboxylic acid {(R)-3-[6-(4-chloro-phenylsulfanyl)-2-(4-methoxy-phenyl)-3-oxo-2,3-dihydro-pyridazin-4-yl]-1-methyl-propyl}-amide
   Show/Hide
C33H34ClFN4O3S
 1
1
IC50 = 1200 nM
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CP0378159
(3R,5R)-N-[(2R)-1-[4-(tert-butylcarbamoyl)-4-cyclohexylpiperidin-1-yl]-3-(4-fluorophenyl)-1-oxopropan-2-yl]-3,5-diethylpiperazine-1-carboxamide
   Show/Hide
C34H54FN5O3
 1
1
IC50 = 1300 nM
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CP0390508
(4R,5S)-4-(4-Fluoro-phenyl)-pyrrolidine-3-carboxylic acid {(R)-3-[6-(4-chloro-phenylsulfanyl)-2-(4-methoxy-phenyl)-3-oxo-2,3-dihydro-pyridazin-4-yl]-1-methyl-propyl}-amide
   Show/Hide
C32H32ClFN4O3S
 1
1
IC50 = 1400 nM
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CP0438966
(3R,5S)-N-[(2R)-1-[4-(tert-butylcarbamoyl)-4-cyclohexylpiperidin-1-yl]-3-(4-fluorophenyl)-1-oxopropan-2-yl]-3,4,5-trimethylpiperazine-1-carboxamide
   Show/Hide
C33H52FN5O3
 1
1
IC50 = 1400 nM
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CP0897048
(3R,4S)-4-Phenyl-piperidine-3-carboxylic acid {(R)-3-[6-(4-chloro-phenylsulfanyl)-2-(4-methoxy-phenyl)-3-oxo-2,3-dihydro-pyridazin-4-yl]-1-methyl-propyl}-amide hydrochloride
   Show/Hide
C33H36Cl2N4O3S
 1
1
IC50 = 1410 nM
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CP0876124
Ac-Nle4-cyclo(Asp5-His6-D-4-Dip-Pro8-Trp9-Lys10)-NH2
   Show/Hide
C55H68N12O9
 1
1
IC50 = 1500 nM
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CP0394112
Ac-Nle4-cyclo(Asp5-His6-D-Cha-Pro8-Trp9-Lys10)-NH2
   Show/Hide
C49H70N12O9
 1
1
IC50 > 10000 nM
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CP0394115
Ac-Nle4-cyclo(Asp5-His6-D-Nle-Pro8-Trp9-Lys10)-NH2
   Show/Hide
C46H66N12O9
 1
1
IC50 > 10000 nM
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   TS
CP0394119
Ac-Nle4-cyclo(Asp5-His6-D-Glu-Pro8-Trp9-Lys10)-NH2
   Show/Hide
C45H62N12O11
 1
1
IC50 > 10000 nM
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CP0394120
Ac-Nle4-cyclo(Asp5-His6-D-Tic-Pro8-Trp9-Lys10)-NH2
   Show/Hide
C51H66N12O9
 1
1
IC50 > 10000 nM
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CP0432988
Ac-Nle4-cyclo(Asp5-His6-D-Tyr-Pro8-Trp9-Lys10)-NH2
   Show/Hide
C49H64N12O10
 1
1
IC50 > 10000 nM
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   TS
CP0433726
Ac-Nle4-cyclo(Asp5-His6-D-Gln-Pro8-Trp9-Lys10)-NH2
   Show/Hide
C45H63N13O10
 1
1
IC50 > 10000 nM
   TI
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   TS
CP0434012
Ac-Nle4-cyclo(Asp5-His6-D-His-Pro8-Trp9-Lys10)-NH2
   Show/Hide
C46H62N14O9
 1
1
IC50 > 10000 nM
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   TS
CP0434038
Ac-Nle4-cyclo(Asp5-His6-D-Lys-Pro8-Trp9-Lys10)-NH2
   Show/Hide
C46H67N13O9
 1
1
IC50 > 10000 nM
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   TS
CP0433731
Ac-Nle4-cyclo(Asp5-His6-L-Tyr(Me)-Pro8-Trp9-Lys10)-NH2
   Show/Hide
C50H66N12O10
 1
1
IC50 > 2000 nM
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   TS
CP0855016
Ac-Nle4-cyclo(Asp5-His6-D-4-Thz-Pro8-Trp9-Lys10)-NH2
   Show/Hide
C44H60N12O9S
 1
1
IC50 > 5000 nM
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   TS
CP0964966
(2S)-1-[(2S)-1-[(2S)-2-[[(2S)-2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-5-amino-5-oxo-2-[[(3S,9S,12S,15S,18S,21R,26R,29S,32S,38S,41S,47S)-9,15,32,38-tetrakis(4-aminobutyl)-21-[[(2R)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-amino-4-methylpentanoyl]amino]-3-phenylpropanoyl]amino]-3-(1H-imidazol-4-yl)propanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-12,18-bis(3-amino-3-oxopropyl)-29,41-dibenzyl-2,8,11,14,17,20,28,31,34,37,40,43,46-tridecaoxo-23,24-dithia-1,7,10,13,16,19,27,30,33,36,39,42,45-tridecazatricyclo[45.3.0.03,7]pentacontane-26-carbonyl]amino]pentanoyl]amino]-3-phenylpropanoyl]amino]hexanoyl]amino]-4-methylpentanoyl]amino]-5-carbamimidamidopentanoyl]pyrrolidine-2-carbonyl]pyrrolidine-2-carboxylic acid
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C144H214N38O30S2
 1
1
Ki = 25.7 nM
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CP0961059
(2S)-1-[(2S)-1-[(2S)-2-[[(2S)-2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-5-amino-2-[[(3S,9S,12S,15S,18S,21R,26R,29S,32S,38S,41S,47S)-32,38-bis(4-aminobutyl)-21-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-amino-4-methylpentanoyl]amino]-3-phenylpropanoyl]amino]-3-(1H-imidazol-4-yl)propanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-12,18-bis(3-amino-3-oxopropyl)-29,41-dibenzyl-9,15-bis(2-methylpropyl)-2,8,11,14,17,20,28,31,34,37,40,43,46-tridecaoxo-23,24-dithia-1,7,10,13,16,19,27,30,33,36,39,42,45-tridecazatricyclo[45.3.0.03,7]pentacontane-26-carbonyl]amino]-5-oxopentanoyl]amino]-3-phenylpropanoyl]amino]hexanoyl]amino]-4-methylpentanoyl]amino]-5-carbamimidamidopentanoyl]pyrrolidine-2-carbonyl]pyrrolidine-2-carboxylic acid
   Show/Hide
C144H212N36O30S2
 1
1
Ki = 117.49 nM
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CP0961058
(S)-1-((S)-1-((6S,9S,15S,18S,21R,24S,27S,30S,33S,36S)-1-((S)-1-((S)-1-((2S,5S,8S,11S,14R,17S,20S,23S,26S)-20-((1H-imidazol-5-yl)methyl)-26-amino-5,11-bis(3-amino-3-oxopropyl)-2,8-bis(4-aminobutyl)-23-benzyl-14-(carbamoylthiomethyl)-17-(4-hydroxybenzyl)-28-methyl-4,7,10,13,16,19,22,25-octaoxo-3,6,9,12,15,18,21,24-octaazanonacosane)pyrrolidine-2-carbonyl)pyrrolidin-2-yl)-24-(3-amino-3-oxopropyl)-9,15,30-tris(4-aminobutyl)-6,18,27-tribenzyl-21-(carbamoylthiomethyl)-36-(3-guanidinopropyl)-33-isobutyl-1,4,7,10,13,16,19,22,25,28,31,34-dodecaoxo-2,5,8,11,14,17,20,23,26,29,32,35-dodecaazaheptatriacontane)pyrrolidine-2-carbonyl)pyrrolidine-2-carboxylic acid
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C146H218N40O32S2
 1
1
Ki = 134.9 nM
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CP0964152
(2S)-1-[(2S)-1-[(2S)-2-[[(2S)-2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-5-amino-2-[[(3S,9S,12S,15S,18S,21R,26R,29S,32S,38S,41S,47S)-32,38-bis(4-aminobutyl)-21-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-amino-4-methylpentanoyl]amino]-3-phenylpropanoyl]amino]-3-(1H-imidazol-4-yl)propanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-12,18-bis(3-amino-3-oxopropyl)-29,41-dibenzyl-9,15-dimethyl-2,8,11,14,17,20,28,31,34,37,40,43,46-tridecaoxo-23,24-dithia-1,7,10,13,16,19,27,30,33,36,39,42,45-tridecazatricyclo[45.3.0.03,7]pentacontane-26-carbonyl]amino]-5-oxopentanoyl]amino]-3-phenylpropanoyl]amino]hexanoyl]amino]-4-methylpentanoyl]amino]-5-carbamimidamidopentanoyl]pyrrolidine-2-carbonyl]pyrrolidine-2-carboxylic acid
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C138H200N36O30S2
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1
Ki = 194.98 nM
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CP0944118
(2S)-1-[(2S)-1-[(2S)-2-[[(2S)-2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-5-amino-2-[[(3S,9S,12S,15S,18S,21R,26R,29S,32S,38S,41S,47S)-32,38-bis(4-aminobutyl)-21-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-amino-4-methylpentanoyl]amino]-3-phenylpropanoyl]amino]-3-(1H-imidazol-4-yl)propanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-12,18-bis(3-amino-3-oxopropyl)-29,41-dibenzyl-2,8,11,14,17,20,28,31,34,37,40,43,46-tridecaoxo-9,15-di(propan-2-yl)-23,24-dithia-1,7,10,13,16,19,27,30,33,36,39,42,45-tridecazatricyclo[45.3.0.03,7]pentacontane-26-carbonyl]amino]-5-oxopentanoyl]amino]-3-phenylpropanoyl]amino]hexanoyl]amino]-4-methylpentanoyl]amino]-5-carbamimidamidopentanoyl]pyrrolidine-2-carbonyl]pyrrolidine-2-carboxylic acid
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C142H208N36O30S2
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1
Ki = 223.87 nM
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CP0944134
(2S)-1-[(2S)-1-[(2S)-2-[[(2S)-2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-5-amino-2-[[(3S,9S,12S,15S,18S,21R,26R,29S,32S,38S,41S,47S)-32,38-bis(4-aminobutyl)-21-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-amino-4-methylpentanoyl]amino]-3-phenylpropanoyl]amino]-3-(1H-imidazol-4-yl)propanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-12,18-bis(3-amino-3-oxopropyl)-29,41-dibenzyl-9,15-bis(hydroxymethyl)-2,8,11,14,17,20,28,31,34,37,40,43,46-tridecaoxo-23,24-dithia-1,7,10,13,16,19,27,30,33,36,39,42,45-tridecazatricyclo[45.3.0.03,7]pentacontane-26-carbonyl]amino]-5-oxopentanoyl]amino]-3-phenylpropanoyl]amino]hexanoyl]amino]-4-methylpentanoyl]amino]-5-carbamimidamidopentanoyl]pyrrolidine-2-carbonyl]pyrrolidine-2-carboxylic acid
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C138H200N36O32S2
 1
1
Ki = 229.09 nM
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