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: PT00911 , Melanocyte-stimulating hormone receptor
Gene Name MC1R
Organism Homo sapiens, Human
Protein Classification Membrane receptor
Uniprot ID Q01726
Table of Molecular Bioactivities Related to the Cell Line and Protein
Cell Line ID: CL000011  Protein ID: PT00911
 
Compound ID Compound Name Compound Formula
CP0861760
(+/-)-3-(6-Fluoro-1H-indazol-3-ylmethylene)-1-[2-oxoethyl-2-(2,3,4,5-tetrahydro-1H-1-benzazepin-1-yl)]-5-phenyl-1H-1,5-diazepine-2,4-dione
   Show/Hide
C31H28FN5O3
 1
1
EC50 = 1.585 nM
   TI
   LI
   LO
   TS
CP0874344
(+/-)-2-[2,4-Dioxo-3-(6-fluoro-1H-indazol-3-ylmethylene)-5-phenyl-2,3,4,5-tetrahydro-1H-1,5-diazepin-1-yl]-N-isopropyl-N-(4-methoxyphenyl)acetamide
   Show/Hide
C31H30FN5O4
 1
1
EC50 = 1.585 nM
   TI
   LI
   LO
   TS
CP0874693
(+/-)-3-(1H-Indazol-3-ylmethylene)-1-[2-oxoethyl-2-(2,3,4,5-tetrahydro-1H-1-benzazepin-1-yl)]-5-phenyl-1H-1,5-diazepine-2,4-dione
   Show/Hide
C31H29N5O3
 1
1
EC50 = 1.585 nM
   TI
   LI
   LO
   TS
CP0885254
(R)-3-(1H-Indazol-3-ylmethylene)-1-[2-oxoethyl-2-(2,3,4,5-tetrahydro-1H-1-benzazepin-1-yl)]-5-phenyl-1H-1,5-diazepine-2,4-dione
   Show/Hide
C31H29N5O3
 1
1
EC50 = 1.585 nM
   TI
   LI
   LO
   TS
CP0844893
Ac-Nle4-cyclo(Asp5-His6-D-4,4'-Bip7-Pip8-Trp9-Lys10)-NH2
   Show/Hide
C56H70N12O9
 2
1
EC50 = 3.3 nM
   TI
   LI
   LO
   TS
2
IC50 = 5.9 nM
   TI
   LI
   LO
   TS
CP0394757
Ac-Nle4-cyclo(Asp5-His6-D-4,4'-Bip-Pro8-Trp9-Lys10)-NH2
   Show/Hide
C56H69N11O9
 2
1
EC50 = 5.3 nM
   TI
   LI
   LO
   TS
2
IC50 = 45 nM
   TI
   LI
   LO
   TS
CP0847012
(+/-)-2-[6-(6-Fluoro-1H-indazol-3-ylmethylene)-5,7-dioxo-4-(3-pyridinyl)-4,5,6,7-tetrahydro-1H-1,4-diazepin-1-yl]-N-(1-methylethyl)-N-[4-(methyloxy)phenyl]acetamide
   Show/Hide
C30H29FN6O4
 1
1
EC50 = 12.59 nM
   TI
   LI
   LO
   TS
CP0846974
(+/-)-2-[2,4-Dioxo-3-(6-fluoro-1H-indazol-3-ylmethylene)-5-phenyl-2,3,4,5-tetrahydro-1H-1,5-diazepin-1-yl]-N-(4-fluorophenyl)-N-isopropylacetamide
   Show/Hide
C30H27F2N5O3
 1
1
EC50 = 14.13 nM
   TI
   LI
   LO
   TS
CP0897229
(R)-2-[2,4-Dioxo-3-(1H-indazol-3-ylmethylene)-5-phenyl-2,3,4,5-tetrahydro-1H-1,5-diazepin-1-yl]-N-isopropyl-N-(4-methoxyphenyl)acetamide
   Show/Hide
C31H31N5O4
 1
1
EC50 = 15.85 nM
   TI
   LI
   LO
   TS
CP0873909
(+/-)-2-[2,4-Dioxo-3-(1H-indazol-3-ylmethylene)-5-phenyl-2,3,4,5-tetrahydro-1H-1,5-diazepin-1-yl]-N-isopropyl-N-(2-methyl-4-trifluoromethoxy)phenyl)acetamide
   Show/Hide
C31H28F3N5O4
 1
1
EC50 = 22.39 nM
   TI
   LI
   LO
   TS
CP0876125
Ac-Nle4-cyclo(Asp5-Pro6-D-4,4'-Bip7-Pip8-Trp9-Lys10)-NH2
   Show/Hide
C55H70N10O9
 2
1
EC50 = 28 nM
   TI
   LI
   LO
   TS
2
IC50 = 65 nM
   TI
   LI
   LO
   TS
CP0885253
(+/-)-2-[2,4-Dioxo-3-(1H-indazol-3-ylmethylene)-5-phenyl-2,3,4,5-tetrahydro-1H-1,5-diazepin-1-yl]-N-isopropyl-N-(4-methoxyphenyl)acetamide
   Show/Hide
C31H31N5O4
 1
1
EC50 = 29.51 nM
   TI
   LI
   LO
   TS
CP0921840
(R)-2-[2,4-Dioxo-3-(6-fluoro-1H-indazol-3-ylmethylene)-5-phenyl-2,3,4,5-tetrahydro-1H-1,5-diazepin-1-yl]-N-isopropyl-N-phenylacetamide
   Show/Hide
C30H28FN5O3
 1
1
EC50 = 35.48 nM
   TI
   LI
   LO
   TS
CP0394108
Ac-Nle4-cyclo(Asp5-His6-D-Tyr(Me)-Pro8-Trp9-Lys10)-NH2
   Show/Hide
C50H66N12O10
 2
1
EC50 = 50 nM
   TI
   LI
   LO
   TS
2
IC50 = 500 nM
   TI
   LI
   LO
   TS
CP0874312
(+/-)-2-[2,4-Dioxo-3-(1H-indazol-3-ylmethylene)-5-phenyl-2,3,4,5-tetrahydro-1H-1,5-diazepin-1-yl]-N-(4-fluorophenyl)-Nisopropylacetamide
   Show/Hide
C30H28FN5O3
 1
1
EC50 = 50.12 nM
   TI
   LI
   LO
   TS
CP0853038
(2-[2,4-Dioxo-3-(1H-indazol-3-ylmethylene)-5-phenyl-2,3.4.5-tetrahydro-1H-1,5-diazepin-1-yl]-N-(4-hydroxyphenyl)-N-isopropylacetamide hydrobromide
   Show/Hide
C30H30BrN5O4
 1
1
EC50 = 52.48 nM
   TI
   LI
   LO
   TS
CP0425195
Ac-Nle4-cyclo(Asp5-His6-D-Tyr(Et)-Pro8-Trp9-Lys10)-NH2
   Show/Hide
C51H68N12O10
 2
1
EC50 = 60 nM
   TI
   LI
   LO
   TS
2
IC50 = 430 nM
   TI
   LI
   LO
   TS
CP0873910
(S)-3-(1H-Indazol-3-ylmethylene)-1-[2-oxoethyl-2-(2,3,4,5-tetrahydro-1H-1-benzazepin-1-yl)]-5-phenyl-1H-1,5-diazepine-2,4-dione
   Show/Hide
C31H29N5O3
 1
1
EC50 = 61.66 nM
   TI
   LI
   LO
   TS
CP0394150
Ac-Nle4-cyclo(Asp5-His6-D-Phe(4-Cl)-Pro8-Trp9-Lys10)-NH2
   Show/Hide
C49H63ClN12O9
 2
1
EC50 = 63 nM
   TI
   LI
   LO
   TS
2
IC50 = 560 nM
   TI
   LI
   LO
   TS
CP0425206
Ac-Nle4-cyclo(Asp5-His6-D-Nal(2)-Pro8-Trp9-Lys10)-NH2
   Show/Hide
C53H66N12O9
 2
1
EC50 = 89 nM
   TI
   LI
   LO
   TS
2
IC50 = 880 nM
   TI
   LI
   LO
   TS
CP0876424
c-Nle4-cyclo(Asp5-Tic6-D-4,4'-Bip7-Pip8-Trp9-Lys10)-NH2
   Show/Hide
C60H72N10O9
 2
1
EC50 = 130 nM
   TI
   LI
   LO
   TS
2
IC50 = 710 nM
   TI
   LI
   LO
   TS
CP0874311
2-[2,4-Dioxo-3-(1H-indazol-3-ylmethylene)-5-phenyl-2,3.4.5-tetrahydro-1H-1,5-diazepin-1-yl]-N-(4-hydroxyphenyl)-N-isopropylacetamide hydrochloride
   Show/Hide
C30H30ClN5O4
 1
1
EC50 = 158.49 nM
   TI
   LI
   LO
   TS
CP0873848
(+/-)-2-[6-(1H-Indazol-3-ylmethyl)-5,7-dioxo-4-(3-pyridinyl)-4,5,6,7-tetrahydro-1H-1,4-diazepin-1-yl]-N-(1-methylethyl)-N-[4-(methyloxy)phenyl]acetamide
   Show/Hide
C30H30N6O4
 1
1
EC50 = 177.83 nM
   TI
   LI
   LO
   TS
CP0847013
(+/-)-2-[2,4-Dioxo-3-(6-fluoro-1H-indazol-3-ylmethylene)-5-phenyl-2,3,4,5-tetrahydro-1H-1,5-diazepin-1-yl]-N-isopropyl-N-phenylacetamide
   Show/Hide
C30H28FN5O3
 1
1
EC50 = 186.21 nM
   TI
   LI
   LO
   TS
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 = 250 nM
   TI
   LI
   LO
   TS
2
IC50 = 3300 nM
   TI
   LI
   LO
   TS
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 = 260 nM
   TI
   LI
   LO
   TS
2
IC50 = 2100 nM
   TI
   LI
   LO
   TS
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 = 280 nM
   TI
   LI
   LO
   TS
2
IC50 = 1500 nM
   TI
   LI
   LO
   TS
CP0848954
(R)-2-[2,4-Dioxo-3-(1H-indazol-3-ylmethylene)-5-phenyl-2,3,4,5-tetrahydro-1H-1,5-diazepin-1-yl]-N-isopropyl-Nphenylacetamide
   Show/Hide
C30H29N5O3
 1
1
EC50 = 295.12 nM
   TI
   LI
   LO
   TS
CP0394113
Ac-Nle4-cyclo(Asp5-His6-D-Bth-Pro8-Trp9-Lys10)-NH2
   Show/Hide
C53H68N12O9S
 2
1
EC50 = 300 nM
   TI
   LI
   LO
   TS
2
IC50 = 2200 nM
   TI
   LI
   LO
   TS
CP0882669
Ac-Nle4-cyclo(Asp5-Val6-D-4,4'-Bip7-Pip8-Trp9-Lys10)-NH2
   Show/Hide
C55H72N10O9
 2
1
EC50 = 330 nM
   TI
   LI
   LO
   TS
2
IC50 = 4900 nM
   TI
   LI
   LO
   TS
CP0878544
Ac-Nle4-cyclo(Asp5-Pro6-D-4,4'-Bip7-Pro8-Trp9-Lys10)-NH2
   Show/Hide
C54H68N10O9
 2
1
EC50 = 350 nM
   TI
   LI
   LO
   TS
2
IC50 = 2100 nM
   TI
   LI
   LO
   TS
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
 2
1
EC50 = 350 nM
   TI
   LI
   LO
   TS
2
IC50 = 1700 nM
   TI
   LI
   LO
   TS
CP0885306
(+/-)-2-(6-((1H-indazol-3-yl)methyl)-6-((1H-pyrazol-3-yl)methyl)-5,7-dioxo-4-phenyl-4,5,6,7-tetrahydro-1H-1,4-diazepin-1-yl)-N-isopropyl-N-(4-methoxyphenyl)acetamide
   Show/Hide
C35H35N7O4
 1
1
EC50 = 398.11 nM
   TI
   LI
   LO
   TS
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
 2
1
EC50 = 400 nM
   TI
   LI
   LO
   TS
2
IC50 = 2800 nM
   TI
   LI
   LO
   TS
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
   Show/Hide
C34H54FN5O3
 2
1
EC50 = 420 nM
   TI
   LI
   LO
   TS
2
IC50 = 2100 nM
   TI
   LI
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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 = 520 nM
   TI
   LI
   LO
   TS
2
IC50 = 730 nM
   TI
   LI
   LO
   TS
CP0431963
Ac-Nle4-cyclo(Asp5-His6-D-2-Thi-Pro8-Trp9-Lys10)-NH2
   Show/Hide
C47H62N12O9S
 2
1
EC50 = 540 nM
   TI
   LI
   LO
   TS
2
IC50 > 5000 nM
   TI
   LI
   LO
   TS
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 = 540 nM
   TI
   LI
   LO
   TS
2
IC50 = 1000 nM
   TI
   LI
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   TS
CP0381200
N-(4-hydroxyphenyl)-2-[6-(2H-indazol-3-ylmethyl)-5,7-dioxo-4-phenyl-1,4-diazepin-1-yl]-N-propan-2-ylacetamide
   Show/Hide
C30H29N5O4
 1
1
EC50 = 549.54 nM
   TI
   LI
   LO
   TS
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 = 560 nM
   TI
   LI
   LO
   TS
2
IC50 = 3600 nM
   TI
   LI
   LO
   TS
CP0874694
(+/-)-2-[2,4-Dioxo-3-(1H-indazol-3-ylmethylene)-5-phenyl-2,3,4,5-tetrahydro-1H-1,5-diazepin-1-yl]-N-isopropyl-Nphenylacetamide
   Show/Hide
C30H29N5O3
 1
1
EC50 = 707.95 nM
   TI
   LI
   LO
   TS
CP0462697
(+/-)-2-[6-(1H-Indazol-3-ylmethyl)-5,7-dioxo-4-(phenylmethyl)-4,5,6,7-tetrahydro-1H-1,4-diazepin-1-yl]-N-(1-methylethyl)-N-[4-(methyloxy)phenyl]acetamide
   Show/Hide
C32H33N5O4
 1
1
EC50 = 794.33 nM
   TI
   LI
   LO
   TS
CP0407464
(+/-)-2-[6-(1H-Indazol-3-ylmethyl)-5,7-dioxo-4-phenyl-4,5,6,7-tetrahydro-1H-1,4-diazepin-1-yl]-N-(1-methylethyl)-N-[4-(4-morpholinyl)phenyl]acetamide
   Show/Hide
C34H36N6O4
 1
1
EC50 = 831.76 nM
   TI
   LI
   LO
   TS
CP0425204
Ac-Nle4-cyclo(Asp5-His6-D-Tyr-Pro8-Trp9-Lys10)-NH2
   Show/Hide
C51H65N13O9
 2
1
EC50 = 880 nM
   TI
   LI
   LO
   TS
2
IC50 > 5000 nM
   TI
   LI
   LO
   TS
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
   Show/Hide
C32H50F2N4O2
 2
1
EC50 = 890 nM
   TI
   LI
   LO
   TS
2
IC50 = 1800 nM
   TI
   LI
   LO
   TS
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
 2
1
EC50 = 910 nM
   TI
   LI
   LO
   TS
2
IC50 = 7800 nM
   TI
   LI
   LO
   TS
CP0438920
(+/-)-2-(6-((1H-indazol-3-yl)methyl)-6-methoxy-5,7-dioxo-4-(thiophen-2-ylmethyl)-4,5,6,7-tetrahydro-1H-1,4-diazepin-1-yl)-N-isopropyl-N-(4-methoxyphenyl)acetamide
   Show/Hide
C31H33N5O5S
 1
1
EC50 = 1174.9 nM
   TI
   LI
   LO
   TS
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 = 1200 nM
   TI
   LI
   LO
   TS
2
IC50 = 1900 nM
   TI
   LI
   LO
   TS
CP0422262
Ac-Nle4-cyclo(Asp5-His6-D-Phe-Pro8-Trp9-Lys10)-NH2
   Show/Hide
C49H64N12O9
 2
1
EC50 = 1300 nM
   TI
   LI
   LO
   TS
2
IC50 = 2500 nM
   TI
   LI
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   TS
CP0846176
(+/-)-2-[2,4-Dioxo-3-(1H-indazol-3-ylmethylene)-3-methoxy-5-phenyl-2,3,4,5-tetrahydro-1H-1,5-diazepin-1-yl]-N-(4-methoxyphenyl)N-isopropylacetamide
   Show/Hide
C32H33N5O5
 1
1
EC50 = 1380.38 nM
   TI
   LI
   LO
   TS
CP0429199
(S)-2-[2,4-Dioxo-3-(1H-indazol-3-ylmethylene)-5-phenyl-2,3,4,5-tetrahydro-1H-1,5-diazepin-1-yl]-N-isopropyl-N-(4-methoxyphenyl)acetamide
   Show/Hide
C31H31N5O4
 1
1
EC50 = 1548.82 nM
   TI
   LI
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   TS
CP0874910
(+/-)-2-[2,4-Dioxo-3-(1H-indazol-3-ylmethylene)-3-methoxy-5-phenyl-2,3,4,5-tetrahydro-1H-1,5-diazepin-1-yl]-N-(4-fluorophenyl)N-isopropylacetamide
   Show/Hide
C31H30FN5O4
 1
1
EC50 = 2951.21 nM
   TI
   LI
   LO
   TS
CP0381199
(+/-)-2-{6-[(6-Fluoro-1H-indazol-3-yl)methyl]-4-methyl-5,7-dioxo-4,5,6,7-tetrahydro-1H-1,4-diazepin-1-yl}-N-(4-fluorophenyl)-N-(1-methylethyl)acetamide
   Show/Hide
C25H25F2N5O3
 1
1
EC50 = 3715.35 nM
   TI
   LI
   LO
   TS
CP0394111
Ac-Nle4-cyclo(Asp5-His6-D-Phe(No2)-Pro8-Trp9-Lys10)-NH2
   Show/Hide
C49H63N13O11
 2
1
EC50 > 500 nM
   TI
   LI
   LO
   TS
2
IC50 > 2000 nM
   TI
   LI
   LO
   TS
CP0855105
Ac-Nle4-cyclo(Asp5-Chg6-D-4,4'-Bip7-Pip8-Trp9-Lys10)-NH2
   Show/Hide
C58H76N10O9
 2
1
EC50 > 500 nM
   TI
   LI
   LO
   TS
2
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0432989
Ac-Nle4-cyclo(Asp5-His6-L-Phe-Pro8-Trp9-Lys10)-NH2
   Show/Hide
C49H64N12O9
 2
1
EC50 > 1000 nM
   TI
   LI
   LO
   TS
2
IC50 = 980 nM
   TI
   LI
   LO
   TS
CP0394112
Ac-Nle4-cyclo(Asp5-His6-D-Cha-Pro8-Trp9-Lys10)-NH2
   Show/Hide
C49H70N12O9
 2
1
EC50 > 2500 nM
   TI
   LI
   LO
   TS
2
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0432988
Ac-Nle4-cyclo(Asp5-His6-D-Tyr-Pro8-Trp9-Lys10)-NH2
   Show/Hide
C49H64N12O10
 2
1
EC50 > 2500 nM
   TI
   LI
   LO
   TS
2
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0855549
Ac-Nle4-cyclo(Asp5-Oic6-D-4,4'-Bip7-Pro8-Trp9-Lys10)-NH2
   Show/Hide
C58H74N10O9
 2
1
EC50 > 2500 nM
   TI
   LI
   LO
   TS
2
IC50 = 7800 nM
   TI
   LI
   LO
   TS
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
   TI
   LI
   LO
   TS
2
IC50 = 5000 nM
   TI
   LI
   LO
   TS
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 = 220 nM
   TI
   LI
   LO
   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 = 530 nM
   TI
   LI
   LO
   TS
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
   Show/Hide
C37H51ClN4O3
 1
1
IC50 = 620 nM
   TI
   LI
   LO
   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 = 940 nM
   TI
   LI
   LO
   TS
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
   Show/Hide
C36H49ClN4O3
 1
1
IC50 = 980 nM
   TI
   LI
   LO
   TS
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 = 1100 nM
   TI
   LI
   LO
   TS
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 = 1100 nM
   TI
   LI
   LO
   TS
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 = 1100 nM
   TI
   LI
   LO
   TS
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 = 1200 nM
   TI
   LI
   LO
   TS
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 = 1300 nM
   TI
   LI
   LO
   TS
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 = 1300 nM
   TI
   LI
   LO
   TS
CP0876570
Ac-Nle4-cyclo(Asp5-Oic6-D-4,4'-Bic7-Pip8-Trp9-Lys10)-NH2
   Show/Hide
C59H88N10O9
 1
1
IC50 = 1300 nM
   TI
   LI
   LO
   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 = 1400 nM
   TI
   LI
   LO
   TS
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 = 1700 nM
   TI
   LI
   LO
   TS
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 = 1800 nM
   TI
   LI
   LO
   TS
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 = 2000 nM
   TI
   LI
   LO
   TS
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
 2
1
IC50 = 2063 nM
   TI
   LI
   LO
   TS
2
IC50 = 2067 nM
   TI
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   LO
   TS
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 = 2100 nM
   TI
   LI
   LO
   TS
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 = 2400 nM
   TI
   LI
   LO
   TS
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 = 2400 nM
   TI
   LI
   LO
   TS
CP0876124
Ac-Nle4-cyclo(Asp5-His6-D-4-Dip-Pro8-Trp9-Lys10)-NH2
   Show/Hide
C55H68N12O9
 1
1
IC50 = 2900 nM
   TI
   LI
   LO
   TS
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
 1
1
IC50 = 5100 nM
   TI
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   LO
   TS
CP0394115
Ac-Nle4-cyclo(Asp5-His6-D-Nle-Pro8-Trp9-Lys10)-NH2
   Show/Hide
C46H66N12O9
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0394119
Ac-Nle4-cyclo(Asp5-His6-D-Glu-Pro8-Trp9-Lys10)-NH2
   Show/Hide
C45H62N12O11
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0394120
Ac-Nle4-cyclo(Asp5-His6-D-Tic-Pro8-Trp9-Lys10)-NH2
   Show/Hide
C51H66N12O9
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0433726
Ac-Nle4-cyclo(Asp5-His6-D-Gln-Pro8-Trp9-Lys10)-NH2
   Show/Hide
C45H63N13O10
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0434012
Ac-Nle4-cyclo(Asp5-His6-D-His-Pro8-Trp9-Lys10)-NH2
   Show/Hide
C46H62N14O9
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0434038
Ac-Nle4-cyclo(Asp5-His6-D-Lys-Pro8-Trp9-Lys10)-NH2
   Show/Hide
C46H67N13O9
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0878527
Ac-Nle4-cyclo(Asp5-Phg6-D-4,4'-Bip7-Pip8-Trp9-Lys10)-NH2
   Show/Hide
C58H70N10O9
 1
1
IC50 > 1000 nM
   TI
   LI
   LO
   TS
CP0879920
Ac-Nle4-cyclo(Asp5-Oic6-D-D-pBzlPhe7-Pip8-Trp9-Lys10)-NH2
   Show/Hide
C60H78N10O9
 1
1
IC50 > 1000 nM
   TI
   LI
   LO
   TS
CP0433731
Ac-Nle4-cyclo(Asp5-His6-L-Tyr(Me)-Pro8-Trp9-Lys10)-NH2
   Show/Hide
C50H66N12O10
 1
1
IC50 > 2000 nM
   TI
   LI
   LO
   TS
CP0844894
Ac-Nle4-cyclo(Asp5-Oic6-D-4,4'-Bip7-Pip8-Trp9-Lys10)-NH2
   Show/Hide
C59H76N10O9
 1
1
IC50 > 5000 nM
   TI
   LI
   LO
   TS
CP0855016
Ac-Nle4-cyclo(Asp5-His6-D-4-Thz-Pro8-Trp9-Lys10)-NH2
   Show/Hide
C44H60N12O9S
 1
1
IC50 > 5000 nM
   TI
   LI
   LO
   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
   Show/Hide
C144H214N38O30S2
 1
1
Ki = 85.11 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
   Show/Hide
C146H218N40O32S2
 1
1
Ki = 109.65 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 = 398.11 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
   Show/Hide
C142H208N36O30S2
 1
1
Ki = 724.44 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
   Show/Hide
C138H200N36O32S2
 1
1
Ki = 776.25 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
   Show/Hide
C138H200N36O30S2
 1
1
Ki = 912.01 nM
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