General Information of the Protein
Protein ID
PT01155
Protein Name
Growth hormone secretagogue receptor type 1
Secondarily
Protein Name
GH-releasing peptide receptor
Ghrelin receptor
Gene Name
GHSR
Sequence
MWNATPSEEPGFNLTLADLDWDASPGNDSLGDELLQLFPAPLLAGVTATCVALFVVGIAGNLLTMLVVSRFRELRTTTNLYLSSMAFSDLLIFLCMPLDLVRLWQYRPWNFGDLLCKLFQFVSESCTYATVLTITALSVERYFAICFPLRAKVVVTKGRVKLVIFVIWAVAFCSAGPIFVLVGVEHENGTDPWDTNECRPTEFAVRSGLLTVMVWVSSIFFFLPVFCLTVLYSLIGRKLWRRRRGDAVVGASLRDQNHKQTVKMLAVVVFAFILCWLPFHVGRYLFSKSFEPGSLEIAQISQYCNLVSFVLFYLSAAINPILYNIMSKKYRVAVFRLLGFEPFSQRKLSTLKDESSRAWTESSINT
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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)
>
GRP-related receptor
Function
Receptor for ghrelin, coupled to G-alpha-11 proteins. Stimulates growth hormone secretion. Binds also other growth hormone releasing peptides (GHRP) (e.g. Met-enkephalin and GHRP-6) as well as non-peptide, low molecular weight secretagogues (e.g. L-692,429, MK-0677, adenosine).
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Uniprot ID
Primary ID:
Q92847

Secondarily ID:
Q14D12
Q6ISR8
Q92848
Q96RJ7
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HGNC ID
HGNC:4267
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: CL000051 , BHK-21
Compound ID Compound Name Compound Formula
CP0885533
(S)-5-Phenethyl-3-(3-piperidin-1-yl-propyl)-1-[2'-(2H-tetrazol-5-yl)-biphenyl-4-ylmethyl]-imidazolidine-2,4-dione
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C33H37N7O2
 1
1
IC50 = 600 nM
   TI
   LI
   LO
   TS
CP0854017
(S)-5-Phenethyl-3-(3-pyrrolidin-1-yl-propyl)-1-[2'-(2H-tetrazol-5-yl)-biphenyl-4-ylmethyl]-imidazolidine-2,4-dione
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C32H35N7O2
 1
1
IC50 = 1100 nM
   TI
   LI
   LO
   TS
CP0885520
(S)-5-Phenethyl-3-(3-piperidin-1-yl-propyl)-1-{4-[2-(2H-tetrazol-5-yl)-phenyl]-thiophen-2-ylmethyl}-imidazolidine-2,4-dione
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C31H35N7O2S
 1
1
IC50 = 1300 nM
   TI
   LI
   LO
   TS
CP0914989
(S)-1-[3-Fluoro-2'-(2H-tetrazol-5-yl)-biphenyl-4-ylmethyl]-5-phenethyl-3-(3-piperidin-1-yl-propyl)-imidazolidine-2,4-dione
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C33H36FN7O2
 1
1
IC50 = 1600 nM
   TI
   LI
   LO
   TS
CP0907730
(S)-3-(3-Dimethylamino-propyl)-5-phenethyl-1-[2'-(2H-tetrazol-5-yl)-biphenyl-4-ylmethyl]-imidazolidine-2,4-dione
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C30H33N7O2
 1
1
IC50 = 4000 nM
   TI
   LI
   LO
   TS
CP0945109
(S)-3-(3-Dimethylamino-propyl)-5-phenethyl-1-[2'-(2H-tetrazol-5-yl)-biphenyl-4-ylmethyl]-2-thioxo-imidazolidin-4-one
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C30H33N7OS
 1
1
IC50 = 8200 nM
   TI
   LI
   LO
   TS
CP0950536
(S)-5-Phenethyl-3-(3-piperidin-1-yl-propyl)-1-{5-[2-(2H-tetrazol-5-yl)-phenyl]-thiophen-2-ylmethyl}-imidazolidine-2,4-dione
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C31H35N7O2S
 1
1
IC50 = 15000 nM
   TI
   LI
   LO
   TS
CP0854272
(S)-5-Benzyl-3-(3-dimethylamino-propyl)-1-[2'-(2H-tetrazol-5-yl)-biphenyl-4-ylmethyl]-2-thioxo-imidazolidin-4-one
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C29H31N7OS
 1
1
IC50 = 35000 nM
   TI
   LI
   LO
   TS
CP0925503
(S)-3-(3-Dimethylamino-propyl)-5-phenyl-1-[2'-(2H-tetrazol-5-yl)-biphenyl-4-ylmethyl]-2-thioxo-imidazolidin-4-one
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C28H29N7OS
 1
1
IC50 = 35000 nM
   TI
   LI
   LO
   TS
CP0917651
(S)-3-(3-Morpholin-4-yl-propyl)-5-phenethyl-1-[2'-(2H-tetrazol-5-yl)-biphenyl-4-ylmethyl]-2-thioxo-imidazolidin-4-one
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C32H35N7O2S
 1
1
IC50 = 45000 nM
   TI
   LI
   LO
   TS
CP0845400
(S)-5-(1H-Indol-3-ylmethyl)-3-piperidin-4-yl-1-[2'-(2H-tetrazol-5-yl)-biphenyl-4-ylmethyl]-imidazolidine-2,4-dione
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C31H30N8O2
 1
1
IC50 = 50000 nM
   TI
   LI
   LO
   TS
CP0845325
3-{(S)-2,5-Dioxo-4-phenethyl-3-[2'-(2H-tetrazol-5-yl)-biphenyl-4-ylmethyl]-imidazolidin-1-yl}-N,N-dimethyl-propionamide
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C30H31N7O3
 1
1
IC50 > 100000 nM
   TI
   LI
   LO
   TS
CP0896728
(S)-3-(3-Amino-propyl)-5-phenethyl-1-[2'-(2H-tetrazol-5-yl)-biphenyl-4-ylmethyl]-imidazolidine-2,4-dione
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C28H29N7O2
 1
1
IC50 > 100000 nM
   TI
   LI
   LO
   TS
CP0906746
(S)-3-(4-Dimethylamino-phenyl)-5-phenethyl-1-[2'-(2H-tetrazol-5-yl)-biphenyl-4-ylmethyl]-2-thioxo-imidazolidin-4-one
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C33H31N7OS
 1
1
IC50 > 100000 nM
   TI
   LI
   LO
   TS
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0037119
1-{[(2R)-3-(benzyloxy)-1-{1-methanesulfonyl-1,2-dihydrospiro[indole-3,4'-piperidine]-1'-yl}-1-oxopropan-2-yl]carbamoyl}-1-methylethan-1-aminium
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C27H36N4O5S
 8
1 Activity = 0.3 nM
2 EC50 = 0.1995 nM
3 IC50 = 0.4 nM
4 IC50 = 0.63 nM
5 IC50 = 32 nM
6 IC50 = 300 nM
7 Kd = 0.14 nM
8 Ki = 0.24 nM
CP0048653
2-(2-methylimidazo[2,1-b][1,3]thiazol-6-yl)-1-[2-[(1R)-5-(6-methylpyrimidin-4-yl)-2,3-dihydro-1H-inden-1-yl]-2,7-diazaspiro[3.5]nonan-7-yl]ethanone
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C29H32N6OS
 1
1 Activity = 11200000 nM
CP0280449
Ghrelin
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C149H249N47O42
 1
1 IC50 = 0.25 nM
CP0263325
2,4-diaminopyrimidine derivative, 8c
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C26H27N5O3S
 1
1 IC50 = 0.3 nM
CP0419825
US8546435, 3
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C38H36N8O3
 1
1 IC50 = 0.6 nM
CP0663159
5-((1R,5S)-8-acetyl-8-azabicyclo[3.2.1]oct-3-en-3-yl)-N-(((S)-2,3-dihydrobenzo[b][1,4]dioxin-2-yl)methyl)-2-((2,3-dihydrobenzofuran-6-yl)methylamino)nicotinamide
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C33H34N4O5
 1
1 IC50 = 0.96 nM
CP0284845
US8546435, 4
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C36H35N7O3
 1
1 IC50 = 1.3 nM
CP0510760
US8546435, 8
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C36H40N8O3
 1
1 IC50 = 1.4 nM
CP0229128
US8546435, 6
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C32H34N6O4
 1
1 IC50 = 3 nM
CP0327955
US8546435, 9
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C35H38N8O3
 1
1 IC50 = 3.2 nM
CP0126988
US8546435, 5
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C35H33N7O3
 1
1 IC50 = 3.4 nM
CP0475496
US8546435, 7
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C35H39N7O4
 1
1 IC50 = 3.4 nM
CP0171189
3-(2,6-Dichloro-phenyl)-5-(2-[1,3]dioxan-2-yl-ethyl)-isoxazole-4-carboxylic acid (4-diethylamino-phenyl)-amide
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C26H29Cl2N3O4
 1
1 IC50 = 6 nM
CP0722711
2-(1-amino-1-methylethylcarboxamido)-3-[1-methylsulfonylspiro[2,3-dihydro-1H-indole-3,4'-(hexahydropyridine)]-1-yl]-3-oxo-(2R)-propyl octanoate; Trifluoroacetate
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C30H45F3N4O8S
 1
1 IC50 = 8.12 nM
CP0370138
3-(2,6-Dichloro-phenyl)-5-(2-[1,3]dioxan-2-yl-ethyl)-isoxazole-4-carboxylic acid (4-diethylamino-2-methyl-phenyl)-amide
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C27H31Cl2N3O4
 1
1 IC50 = 9 nM
CP0135116
2,4-diaminopyrimidine-based antagonist, 4c
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C20H23N5O2S
 1
1 IC50 = 9.7 nM
CP0134612
GHRELIN
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C147H245N45O42
 2
1 IC50 = 9.8 nM
2 IC50 = 250 nM
CP0702454
Tyr-Ala-hexarelin
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C59H72N14O9
 1
1 IC50 = 12 nM
CP0306681
(S)-4-(3-hexylureido)-N-(4-(2-(2-hydroxy-3-(4-hydroxyphenoxy)propylamino)-2-methylpropyl)phenyl)benzenesulfonamide
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C32H44N4O6S
 1
1 IC50 = 13 nM
CP0202154
(+/-)isobutyl 2-((4-(diethylamino)phenyl)carbamoyl)-8-methoxy-1,2,3,4-tetrahydronaphthalen-2-yl(methyl)carbamate
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C28H39N3O4
 1
1 IC50 = 16 nM
CP0112074
ethyl N-[(1S)-1-[[(2R)-2-[(2-amino-2-methylpropanoyl)amino]-3-(1H-indol-3-yl)propanoyl]amino]-2-(1H-indol-3-yl)ethyl]carbamate
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C28H34N6O4
 1
1 IC50 = 16.2 nM
CP0310947
2-Amino-N-[1-[(R)-(S)-1-(3-ethyl-ureido)-2-(1H-indol-3-yl)-ethylcarbamoyl]-2-(1H-indol-3-yl)-ethyl]-2-methyl-propionamide
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C28H35N7O3
 1
1 IC50 = 16.9 nM
CP0310354
Examorelin
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C47H58N12O6
 1
1 IC50 = 18 nM
CP0268289
N-[(2R)-1-[[(1R)-1-acetamido-2-(1H-indol-3-yl)ethyl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]-2-(dimethylamino)-2-methylpropanamide
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C29H36N6O3
 1
1 IC50 = 20.1 nM
CP0235411
N-[(1R)-1-[[(2R)-2-[(2-amino-2-methylpropanoyl)amino]-3-(1H-indol-3-yl)propanoyl]amino]-2-(1H-indol-3-yl)ethyl]piperidine-2-carboxamide
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C31H39N7O3
 1
1 IC50 = 21.5 nM
CP0303771
2-Amino-N-{(R)-1-[(R)-1-formylamino-2-(1H-indol-3-yl)-ethylcarbamoyl]-2-1H-indol-3-yl-ethyl}-2-methyl-propionamide
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C26H30N6O3
 1
1 IC50 = 22.9 nM
CP0102070
N-[(2R)-1-[[(1R)-1-acetamido-2-(1H-indol-3-yl)ethyl]-methylamino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]-2-methyl-2-(methylamino)propanamide
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C29H36N6O3
 1
1 IC50 = 25.6 nM
CP0686858
1N-[1-benzyloxymethyl-2-[1-methylsulfonylspiro[2,3-dihydro-1H-indole-3,4'-(hexahydropyridine)]-1-yl]-2-oxo-(1R)-ethyl]-2-aminomethylcarboxamido-3-hydroxy-(2S)-propanamide; Trifluoroacetate
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C30H38F3N5O9S
 1
1 IC50 = 36.2 nM
CP0367518
3-(2,6-Dichloro-phenyl)-5-methyl-isoxazole-4-carboxylic acid (4-diethylamino-2-methyl-phenyl)-amide
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C22H23Cl2N3O2
 1
1 IC50 = 37 nM
CP0112161
N-[(2R)-1-[[(1R)-1-formamido-2-(1H-indol-3-yl)ethyl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]-2-methyl-2-(methylamino)propanamide
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C27H32N6O3
 1
1 IC50 = 39 nM
CP0090232
N-[(1R)-1-[[(2R)-2-[(2-amino-2-methylpropanoyl)amino]-3-(1H-indol-3-yl)propanoyl]amino]-2-(1H-indol-3-yl)ethyl]-3-methylbutanamide
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C30H38N6O3
 1
1 IC50 = 59.8 nM
CP0160317
N-[(2R)-1-[[(1R)-1-acetamido-2-(1H-indol-3-yl)ethyl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]-2-methyl-2-(methylamino)propanamide
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C28H34N6O3
 1
1 IC50 = 74 nM
CP0773560
2-[1-aminomethylcarboxamido-2-hydroxy-(1S)-ethylcarboxamido]-3-[1-methylsulfonylspiro[2,3-dihydro-1H-indole-3,4'-(hexahydropyridine)]-1-yl]-3-oxo-(2R)-propyl octanoate; Trifluoroacatate
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C31H46F3N5O10S
 1
1 IC50 = 128 nM
CP0006991
3-(2,6-Dichloro-phenyl)-5-methyl-isoxazole-4-carboxylic acid (4-diethylamino-phenyl)-amide
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C21H21Cl2N3O2
 1
1 IC50 = 130 nM
CP0193125
2-Amino-N-{2-(1H-indol-3-yl)-1-[(R)-(R)-2-(1H-indol-3-yl)-1-propionylamino-ethylcarbamoyl]-ethyl}-2-methyl-propionamide
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C28H34N6O3
 1
1 IC50 = 185 nM
CP0735614
1N-[1-benzyloxymethyl-2-[1-methylsulfonylspiro[2,3-dihydro-1H-indole-3,4'-(hexahydropyridine)]-1-yl]-2-oxo-(1R)-ethyl]-2-amino-3-hydroxy-(2S)-propanamide; Trifluoroacetate
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C28H35F3N4O8S
 1
1 IC50 = 209 nM
CP0509277
N-[(1R)-2-(1H-indol-3-yl)-1-[[(2R)-3-(1H-indol-3-yl)-2-[[2-methyl-2-(methylamino)propanoyl]amino]propanoyl]amino]ethyl]-3-methylbutanamide
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C31H40N6O3
 1
1 IC50 = 213 nM
CP0111596
3-(2-Bromo-phenyl)-5-methyl-isoxazole-4-carboxylic acid (4-diethylamino-phenyl)-amide
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C21H22BrN3O2
 1
1 IC50 = 340 nM
CP0370122
3-(2,6-Dichloro-phenyl)-5-methyl-isoxazole-4-carboxylic acid {2-[(benzo[1,3]dioxol-5-ylmethyl)-carbamoyl]-phenyl}-amide
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C26H19Cl2N3O5
 1
1 IC50 = 350 nM
CP0152858
3-(2,6-Dichloro-phenyl)-5-methyl-isoxazole-4-carboxylic acid (4-diethylamino-2-ethyl-phenyl)-amide
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C23H25Cl2N3O2
 1
1 IC50 = 370 nM
CP0316950
N-[(2R)-1-[[(1R)-1-formamido-2-(1H-indol-3-yl)ethyl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]piperidine-4-carboxamide
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C28H32N6O3
 1
1 IC50 = 391 nM
CP0083621
3-(2,6-Dichloro-phenyl)-5-methyl-isoxazole-4-carboxylic acid [4-(ethyl-propyl-amino)-phenyl]-amide
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C22H23Cl2N3O2
 1
1 IC50 = 410 nM
CP0013808
5-Methyl-3-(2-nitro-phenyl)-isoxazole-4-carboxylic acid (4-diethylamino-phenyl)-amide
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C21H22N4O4
 1
1 IC50 = 550 nM
CP0727184
2-(1-amino-1-methylethylcarboxamido)-3-[1-methylsulfonylspiro[2,3-dihydro-1H-indole-3,4'-(hexahydropyridine)]-1-yl]-3-oxo-(2S)-propyl octanoate; trifluoroacetate
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C30H45F3N4O8S
 1
1 IC50 = 590.5 nM
CP0061848
3-(2,6-Dichloro-phenyl)-5-methyl-isoxazole-4-carboxylic acid (4-diethylamino-2-ethyl-phenyl)-amide
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C22H23Cl2N3O3
 1
1 IC50 = 600 nM
CP0005801
3-(2-Chloro-phenyl)-5-methyl-isoxazole-4-carboxylic acid (4-diethylamino-phenyl)-amide
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C21H22ClN3O2
 1
1 IC50 = 690 nM
CP0677986
2-[1-amino-2-hydroxy-(1S)-ethylcarboxamido]-3-[1-methylsulfonylspiro[2,3-dihydro-1H-indole-3,4'-(hexahydropyridine)]-1-yl]-3-oxo-(2R)-propyl octanoate; Trifluoroacetate
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C29H43F3N4O9S
 1
1 IC50 = 828.5 nM
CP0082096
3-(2,6-Dichloro-phenyl)-5-methyl-isoxazole-4-carboxylic acid [2-(azepane-1-carbonyl)-phenyl]-amide
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C24H23Cl2N3O3
 1
1 IC50 = 860 nM
CP0310709
2-[1-[1-aminomethylcarboxamido-2-heptylcarbonyloxy-(1S)-ethylcarboxamido]-2-hydroxy-(1S)-ethylcarboxamido]-3-phenyl-(2S)-propanoic acid
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C25H38N4O8
 1
1 IC50 = 889 nM
CP0370121
3-(2,6-Dichloro-phenyl)-5-methyl-isoxazole-4-carboxylic acid [2-(2-methyl-1,2,3,4-tetrahydro-isoquinolin-1-ylmethyl)-phenyl]-amide
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C28H25Cl2N3O2
 1
1 IC50 = 980 nM
CP0040929
3-(2,6-Dichloro-phenyl)-5-methyl-isoxazole-4-carboxylic acid (2-benzylcarbamoyl-phenyl)-amide
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C25H19Cl2N3O3
 1
1 IC50 = 1200 nM
CP0184651
3-Biphenyl-2-yl-5-methyl-isoxazole-4-carboxylic acid (4-diethylamino-phenyl)-amide
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C27H27N3O2
 1
1 IC50 = 1300 nM
CP0270411
4-Amino-piperidine-4-carboxylic acid [1-[(R)-(R)-1-formylamino-2-(1H-indol-3-yl)-ethylcarbamoyl]-2-(1H-indol-3-yl)-ethyl]-amide
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C28H33N7O3
 1
1 IC50 = 1791 nM
CP0333137
3-(2,6-Dichloro-phenyl)-5-methyl-isoxazole-4-carboxylic acid (2-diethylcarbamoyl-phenyl)-amide
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C22H21Cl2N3O3
 1
1 IC50 = 1900 nM
CP0250114
3-(2,6-Dichloro-phenyl)-5-methyl-isoxazole-4-carboxylic acid [2-(piperidine-1-carbonyl)-phenyl]-amide
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C23H21Cl2N3O3
 1
1 IC50 = 2200 nM
CP0650732
2-[1-aminomethylcarboxamido-2-hydroxy-(1S)-ethylcarboxamido]-3-[1-methylsulfonylspiro[2,3-dihydro-1H-indole-3,4'-(hexahydropyridine)]-1-yl]-3-oxo-(2S)-propyl octanoate; trifluoroactate
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C31H46F3N5O10S
 1
1 IC50 = 2670 nM
CP0302498
N-[(2R)-1-[[(1R)-1-acetamido-2-(1H-indol-3-yl)ethyl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]-2-amino-2-methylpropanamide
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C27H32N6O3
 1
1 IC50 = 3852 nM
CP0111597
3-(2-Methoxy-phenyl)-5-methyl-isoxazole-4-carboxylic acid (4-diethylamino-phenyl)-amide
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C22H25N3O3
 1
1 IC50 = 4000 nM
CP0225215
3-(2,6-Dichloro-phenyl)-5-methyl-isoxazole-4-carboxylic acid (4-diethylamino-2-trifluoromethyl-phenyl)-amide
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C22H20Cl2F3N3O2
 1
1 IC50 = 4100 nM
CP0152861
3-(2,6-Dichloro-phenyl)-5-methyl-isoxazole-4-carboxylic acid [4-(ethyl-methyl-amino)-phenyl]-amide
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C20H19Cl2N3O2
 1
1 IC50 = 5500 nM
CP0219009
US9708370, GHRP-6
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C46H56N12O6
 2
1 IC50 = 6000 nM
2 Ki = 6 nM
CP0180252
3-(4-Chloro-phenyl)-5-methyl-isoxazole-4-carboxylic acid (4-diethylamino-phenyl)-amide
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C21H22ClN3O2
 1
1 IC50 = 7100 nM
CP0137589
3-(2,6-Dichloro-phenyl)-5-(2-[1,3]dioxan-2-yl-ethyl)-isoxazole-4-carboxylic acid [2-(piperidine-1-carbonyl)-phenyl]-amide
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C28H29Cl2N3O5
 1
1 IC50 = 7500 nM
CP0003133
5-Methyl-3-phenyl-isoxazole-4-carboxylic acid (4-diethylamino-phenyl)-amide
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C21H23N3O2
 1
1 IC50 = 8200 nM
CP0225214
3-(2,6-Dichloro-phenyl)-5-methyl-isoxazole-4-carboxylic acid (2-cyano-4-diethylamino-phenyl)-amide
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C22H20Cl2N4O2
 1
1 IC50 = 9000 nM
CP0225195
3-(2,6-Dichloro-phenyl)-5-methyl-isoxazole-4-carboxylic acid {4-[ethyl-(2-hydroxy-ethyl)-amino]-phenyl}-amide
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C21H21Cl2N3O3
 1
1 IC50 = 9200 nM
CP0152859
3-(2,6-Dichloro-phenyl)-5-methyl-isoxazole-4-carboxylic acid (4-diethylamino-3-methyl-phenyl)-amide
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C22H23Cl2N3O2
 1
1 IC50 > 100 nM
CP0258518
N-[(2R)-1-[[(1R)-1-acetamido-2-(1H-indol-3-yl)ethyl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]piperidine-4-carboxamide
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C29H34N6O3
 1
1 IC50 > 10000 nM
CP0272419
N-[(2R)-3-(1H-indol-3-yl)-1-[[(1R)-2-(1H-indol-3-yl)-1-(propanoylamino)ethyl]amino]-1-oxopropan-2-yl]-2-methyl-2-(methylamino)propanamide
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C29H36N6O3
 1
1 IC50 > 10000 nM
CP0238556
(6S,9R,12R)-6-[(2S)-butan-2-yl]-12-[(4-chlorophenyl)methyl]-8,9-dimethyl-2-oxa-5,8,11,14-tetrazabicyclo[16.4.0]docosa-1(22),18,20-triene-7,10,13-trione
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C30H41ClN4O4
 1
1 Ki = 0.35 nM
CP0260069
(3R,6S,9R,12R)-6-cyclohexyl-12-[(4-fluorophenyl)methyl]-3,8,9-trimethyl-2-oxa-5,8,11,14-tetrazabicyclo[16.4.0]docosa-1(22),18,20-triene-7,10,13-trione
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C33H45FN4O4
 1
1 Ki = 0.38 nM
CP0260072
(7R,10R,13S,16R)-13-cyclopropyl-7-[(4-fluorophenyl)methyl]-10,11-dimethyl-24-oxa-5,8,11,14-tetrazatricyclo[14.6.2.019,23]tetracosa-1(23),19,21-triene-6,9,12-trione
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C31H39FN4O4
 1
1 Ki = 0.9 nM
CP0213761
(6S,9R,12R)-6-cyclopropyl-21-fluoro-12-[(4-fluorophenyl)methyl]-8,9-dimethyl-2-oxa-5,8,11,14-tetrazabicyclo[16.4.0]docosa-1(18),19,21-triene-7,10,13-trione
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C29H36F2N4O4
 1
1 Ki = 2.6 nM
CP0444784
(2S)-N-[(1R)-1-[5-[(1R)-1-[[(2S)-2-[[(2S)-2-acetamido-4-methylpentanoyl]amino]-4-methylpentanoyl]amino]-2-(1H-indol-3-yl)ethyl]-4-[(4-methoxyphenyl)methyl]-1,2,4-triazol-3-yl]-2-(1H-indol-3-yl)ethyl]-2,6-diaminohexanamide
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C50H67N11O5
 1
1 Ki = 3 nM
CP0504852
(2S)-2-acetamido-N-[(2S)-1-[[(1R)-1-[5-[(1R)-1-[(2-hydroxyacetyl)amino]-2-(1H-indol-3-yl)ethyl]-4-[(4-methoxyphenyl)methyl]-1,2,4-triazol-3-yl]-2-(1H-indol-3-yl)ethyl]amino]-4-methyl-1-oxopentan-2-yl]-4-methylpentanamide
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C46H57N9O6
 1
1 Ki = 3 nM
CP0213740
(6S,9R,12R)-12-benzyl-6-cyclopropyl-8,9-dimethyl-2-oxa-5,8,11,14-tetrazabicyclo[16.4.0]docosa-1(22),18,20-triene-7,10,13-trione
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C29H38N4O4
 1
1 Ki = 4.4 nM
CP0079401
(6S,9R,12R)-6-cyclopropyl-8,9-dimethyl-12-[(4-methylphenyl)methyl]-2-oxa-5,8,11,14-tetrazabicyclo[16.4.0]docosa-1(22),18,20-triene-7,10,13-trione
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C30H40N4O4
 1
1 Ki = 5 nM
CP0332150
(6S,9R,12R)-6-cyclopropyl-12-[(2-fluorophenyl)methyl]-8,9-dimethyl-2-oxa-5,8,11,14-tetrazabicyclo[16.4.0]docosa-1(22),18,20-triene-7,10,13-trione
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C29H37FN4O4
 1
1 Ki = 6.2 nM
CP0260064
(6S,9R,12R)-12-benzyl-6-[(2S)-butan-2-yl]-8,9-dimethyl-2-oxa-5,8,11,14-tetrazabicyclo[16.4.0]docosa-1(22),18,20-triene-7,10,13-trione
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C30H42N4O4
 1
1 Ki = 6.4 nM
CP0284752
(6S,9R,12R)-6-cyclopropyl-8,9-dimethyl-12-[[4-(trifluoromethyl)phenyl]methyl]-2-oxa-5,8,11,14-tetrazabicyclo[16.4.0]docosa-1(22),18,20-triene-7,10,13-trione
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C30H37F3N4O4
 1
1 Ki = 7 nM
CP0260068
(6S,9R,12R)-6-cyclopropyl-12-[(4-fluorophenyl)methyl]-8,9-dimethyl-2-oxa-5,8,11,14-tetrazabicyclo[16.4.0]docosa-1(22),18,20-triene-7,10,13-trione
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C29H37FN4O4
 1
1 Ki = 7.3 nM
CP0084691
(6S,9R,12R)-6-cyclopropyl-12-[(4-fluorophenyl)methyl]-4,8,9-trimethyl-2-oxa-5,8,11,14-tetrazabicyclo[16.4.0]docosa-1(22),18,20-triene-7,10,13-trione
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C30H39FN4O4
 1
1 Ki = 9 nM
CP0260067
(3R,6S,9R,12R)-12-[(4-chlorophenyl)methyl]-6-cyclopropyl-3,8,9-trimethyl-2-oxa-5,8,11,14-tetrazabicyclo[16.4.0]docosa-1(22),18,20-triene-7,10,13-trione
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C30H39ClN4O4
 1
1 Ki = 15 nM
CP0191601
(6S,9R,12R)-12-benzyl-8,9-dimethyl-6-propyl-2-oxa-5,8,11,14-tetrazabicyclo[16.4.0]docosa-1(22),18,20-triene-7,10,13-trione
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C29H40N4O4
 1
1 Ki = 16 nM
CP0726922
(2R,5S,8R,11R)-5-cyclopropyl-11-(4-fluorobenzyl)-2,7,8-trimethyl-4,5,7,8,10,11,13,14,15,16-decahydro-2H-benzo[q][1,4,7,10,13]oxatetraazacyclooctadecine-6,9,12(3H)-trione hydrochloride hydrate
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C30H42ClFN4O5
 1
1 Ki = 16 nM
CP0151998
(6S,9R,12R)-6-cyclopropyl-12-[(3-fluorophenyl)methyl]-8,9-dimethyl-2-oxa-5,8,11,14-tetrazabicyclo[16.4.0]docosa-1(22),18,20-triene-7,10,13-trione
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C29H37FN4O4
 1
1 Ki = 21 nM
CP0260123
(6S,9R,12R)-12-benzyl-8,9-dimethyl-6-(2-methylpropyl)-2-oxa-5,8,11,14-tetrazabicyclo[16.4.0]docosa-1(22),18,20-triene-7,10,13-trione
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C30H42N4O4
 1
1 Ki = 25 nM
CP0151997
(6S,9R,12R)-6-[(2S)-butan-2-yl]-8,9-dimethyl-12-(2-phenylethyl)-2-oxa-5,8,11,14-tetrazabicyclo[16.4.0]docosa-1(22),18,20-triene-7,10,13-trione
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C31H44N4O4
 1
1 Ki = 43 nM
CP0238497
(3S,6S,9R,12R)-6-cyclopropyl-12-[(4-fluorophenyl)methyl]-3,8,9-trimethyl-2-oxa-5,8,11,14-tetrazabicyclo[16.4.0]docosa-1(22),18,20-triene-7,10,13-trione
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C30H39FN4O4
 1
1 Ki = 56 nM
CP0213743
(6S,9R,12R)-6-cyclopropyl-20-fluoro-12-[(4-fluorophenyl)methyl]-8,9-dimethyl-2-oxa-5,8,11,14-tetrazabicyclo[16.4.0]docosa-1(18),19,21-triene-7,10,13-trione
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C29H36F2N4O4
 1
1 Ki = 58 nM
CP0205852
(6S,12R)-12-benzyl-8-methyl-6-propyl-2-oxa-5,8,11,14-tetrazabicyclo[16.4.0]docosa-1(22),18,20-triene-7,10,13-trione
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C28H38N4O4
 1
1 Ki = 68 nM
CP0354581
(6S,9R,12R)-12-benzyl-6-[(2S)-butan-2-yl]-8,9-dimethyl-5,8,11,14-tetrazabicyclo[17.4.0]tricosa-1(23),19,21-triene-7,10,13-trione
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C32H46N4O3
 1
1 Ki = 78 nM
CP0274269
(7R,10R,13S)-7-benzyl-13-[(2S)-butan-2-yl]-10,11-dimethyl-5,8,11,14-tetrazabicyclo[16.4.0]docosa-1(22),18,20-triene-6,9,12-trione
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C31H44N4O3
 1
1 Ki = 81 nM
CP0354578
(6S,12R,16E)-12-benzyl-8-methyl-6-propyl-2-oxa-5,8,11,14-tetrazabicyclo[16.4.0]docosa-1(22),16,18,20-tetraene-7,10,13-trione
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C28H36N4O4
 1
1 Ki = 86 nM
CP0151994
(6S,12R)-12-[(4-hydroxyphenyl)methyl]-8-methyl-6-propyl-2-oxa-5,8,11,14-tetrazabicyclo[16.4.0]docosa-1(22),18,20-triene-7,10,13-trione
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C28H38N4O5
 1
1 Ki = 120 nM
CP0084690
(3R,6R,9S,15E)-3-benzyl-9-[(2S)-butan-2-yl]-6,7-dimethyl-1,4,7,10-tetrazacyclooctadec-15-ene-2,5,8-trione
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C27H42N4O3
 1
1 Ki = 160 nM
CP0051354
(S,E)-2-amino-N-(2-(benzyloxy)-1-(1-cinnamyl-1H-tetrazol-5-yl)ethyl)-2-methylpropanamide
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C23H28N6O2
 1
1 Ki = 190 nM
CP0261719
(S)-2-amino-N-(2-(benzyloxy)-1-(1-(3-phenylpropyl)-1H-tetrazol-5-yl)ethyl)-2-methylpropanamide
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C23H30N6O2
 1
1 Ki = 200 nM
CP0094817
(6S,9R,12R)-12-benzyl-6-[(2S)-butan-2-yl]-8,9-dimethyl-2-oxa-5,8,11,14-tetrazabicyclo[15.4.0]henicosa-1(21),17,19-triene-7,10,13-trione
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C29H40N4O4
 1
1 Ki = 210 nM
CP0379087
(2S)-2,6-diamino-N-[(2R)-1-[[(2S)-1-[[(2R)-1-[[(2S)-1-[[(2S)-1-amino-4-methyl-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]hexanamide
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C49H66N10O6
 1
1 Ki = 255 nM
CP0332885
(S)-benzyl 5-(5-(1-(2-amino-2-methylpropanamido)-2-(benzyloxy)ethyl)-1H-tetrazol-1-yl)pentylcarbamate
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C27H37N7O4
 1
1 Ki = 320 nM
CP0155470
(6S,12S)-12-benzyl-8-methyl-6-propyl-2-oxa-5,8,11,14-tetrazabicyclo[16.4.0]docosa-1(22),18,20-triene-7,10,13-trione
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C28H38N4O4
 1
1 Ki = 380 nM
CP0238558
(6R,9R,12S)-6-benzyl-12-[(2S)-butan-2-yl]-9,10-dimethyl-4,7,10,13-tetrazabicyclo[15.4.0]henicosa-1(21),17,19-triene-5,8,11-trione
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C30H42N4O3
 1
1 Ki = 400 nM
CP0284751
(6S,12R)-12-butyl-8-methyl-6-propyl-2-oxa-5,8,11,14-tetrazabicyclo[16.4.0]docosa-1(22),18,20-triene-7,10,13-trione
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C25H40N4O4
 1
1 Ki = 400 nM
CP0051292
methyl 2-[5-[(1S)-1-[(2-amino-2-methylpropanoyl)amino]-2-phenylmethoxyethyl]tetrazol-1-yl]-2-phenylacetate
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C23H28N6O4
 1
1 Ki = 470 nM
CP0260065
(6S,9R,12R)-12-benzyl-9-methyl-6-propyl-2-oxa-5,8,11,14-tetrazabicyclo[16.4.0]docosa-1(22),18,20-triene-7,10,13-trione
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C28H38N4O4
 1
1 Ki = 500 nM
CP0329376
(6S,9S,12R)-12-benzyl-8,9-dimethyl-6-propyl-2-oxa-5,8,11,14-tetrazabicyclo[16.4.0]docosa-1(22),18,20-triene-7,10,13-trione
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C29H40N4O4
 1
1 Ki = 580 nM
CP0284750
(6S,12R)-6,12-dibenzyl-8-methyl-2-oxa-5,8,11,14-tetrazabicyclo[16.4.0]docosa-1(22),18,20-triene-7,10,13-trione
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C32H38N4O4
 1
1 Ki = 670 nM
CP0035111
2-amino-N-{(S)-2-benzyloxy-1-[1-(2-phenethylcarbamoyl-ethyl)-1H-tetrazol-5-yl]-ethyl}-2-methyl-propionamide
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C25H33N7O3
 1
1 Ki = 780 nM
CP0165849
2-amino-N-((S)-2-benzyloxy-1-{1-[2-(3-phenyl-propylcarbamoyl)-ethyl]-1H-tetrazol-5-yl}-ethyl)-2-methyl-propionamide
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C26H35N7O3
 1
1 Ki = 820 nM
CP0165860
(S)-2-amino-N-(2-(benzyloxy)-1-(1-(2-(1-(methylsulfonyl)-1H-indol-2-yl)ethyl)-1H-tetrazol-5-yl)ethyl)-2-methylpropanamide
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C25H31N7O4S
 1
1 Ki = 970 nM
CP0370661
2-amino-N-{(S)-1-[1-(2-benzylcarbamoyl-ethyl)-1H-tetrazol-5-yl]-2-benzyloxy-ethyl}-2-methyl-propionamide
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C24H31N7O3
 1
1 Ki = 1070 nM
CP0084688
(6S,12R)-6-(4-aminobutyl)-12-benzyl-8-methyl-2-oxa-5,8,11,14-tetrazabicyclo[16.4.0]docosa-1(22),18,20-triene-7,10,13-trione
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C29H41N5O4
 1
1 Ki = 1100 nM
CP0151993
(6R,12R)-12-benzyl-8-methyl-6-propyl-2-oxa-5,8,11,14-tetrazabicyclo[16.4.0]docosa-1(22),18,20-triene-7,10,13-trione
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C28H38N4O4
 1
1 Ki = 1200 nM
CP0079826
(S)-2-amino-N-(2-(benzyloxy)-1-(2-(2-(1-(methylsulfonyl)-1H-indol-2-yl)ethyl)-2H-tetrazol-5-yl)ethyl)-2-methylpropanamide
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C25H31N7O4S
 1
1 Ki = 1270 nM
CP0370660
2-amino-N-{(R)-1-[1-(2-butylcarbamoyl-ethyl)-1H-tetrazol-5-yl]-3-phenyl-propyl}-2-methyl-propionamide
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C21H33N7O2
 1
1 Ki = 1370 nM
CP0274331
(3R,6R,9S)-3-benzyl-9-[(2S)-butan-2-yl]-6,7-dimethyl-1,4,7,10-tetrazacyclooctadecane-2,5,8-trione
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C27H44N4O3
 1
1 Ki = 1500 nM
CP0500552
2-amino-N-((S)-2-(benzyloxy)-1-(1-((1-(methylsulfonyl)indolin-3-yl)methyl)-1H-tetrazol-5-yl)ethyl)-2-methylpropanamide
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C24H31N7O4S
 1
1 Ki = 1590 nM
CP0145444
(S)-2-amino-N-(2-(benzyloxy)-1-(1-(3-(2-(N-methylmethan-4-ylsulfonamido)phenyl)propyl)-1H-tetrazol-5-yl)ethyl)-2-methylpropanamide
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C25H35N7O4S
 1
1 Ki = 1720 nM
CP0370662
(S)-4-(5-(1-(2-amino-2-methylpropanamido)-2-(benzyloxy)ethyl)-1H-tetrazol-1-yl)-N-butylbutanamide
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C22H35N7O3
 1
1 Ki = 1780 nM
CP0051352
(S)-2-amino-N-(1-(1-benzyl-1H-tetrazol-5-yl)-2-(benzyloxy)ethyl)-2-methylpropanamide
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C21H26N6O2
 1
1 Ki = 1900 nM
CP0541779
2-amino-N-{(S)-2-benzyloxy-1-[1-(2-butylcarbamoyl-ethyl)-1H-tetrazol-5-yl]-ethyl}-2-methyl-propionamide
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C21H33N7O3
 1
1 Ki = 2190 nM
CP0165856
(S)-N-(1-(1-(2-(methylsulfonamido)phenethyl)-1H-tetrazol-5-yl)-2-(benzyloxy)ethyl)-2-amino-2-methylpropanamide
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C23H31N7O4S
 1
1 Ki = 2200 nM
CP0165851
(S)-methyl 4-(5-(1-(2-amino-2-methylpropanamido)-2-(benzyloxy)ethyl)-1H-tetrazol-1-yl)butanoate
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C19H28N6O4
 1
1 Ki = 2380 nM
CP0079827
(S)-2-amino-N-(2-(benzyloxy)-1-(2-(3-(2-(methylsulfonamido)phenyl)propyl)-2H-tetrazol-5-yl)ethyl)-2-methylpropanamide
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C24H33N7O4S
 1
1 Ki = 2390 nM
CP0215202
(S)-N-(1-(2-(2-(methylsulfonamido)phenethyl)-2H-tetrazol-5-yl)-2-(benzyloxy)ethyl)-2-amino-2-methylpropanamide
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C23H31N7O4S
 1
1 Ki = 2660 nM
CP0285233
(S)-2-amino-N-(2-(benzyloxy)-1-(1-(2-cyanoethyl)-1H-tetrazol-5-yl)ethyl)-2-methylpropanamide
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C17H23N7O2
 1
1 Ki = 2940 nM
CP0051294
(S)-2-amino-N-(2-(benzyloxy)-1-(1-(4-cyanobutyl)-1H-tetrazol-5-yl)ethyl)-2-methylpropanamide
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C19H27N7O2
 1
1 Ki = 3120 nM
CP0222631
(S)-methyl 3-(5-(1-(2-amino-2-methylpropanamido)-2-(benzyloxy)ethyl)-1H-tetrazol-1-yl)propanoate
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C18H26N6O4
 1
1 Ki = 3380 nM
CP0145445
(S)-2-amino-N-(2-(benzyloxy)-1-(1-(cyanomethyl)-1H-tetrazol-5-yl)ethyl)-2-methylpropanamide
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C16H21N7O2
 1
1 Ki = 4170 nM
CP0296915
(S)-N-(1-(1-(2-(methylsulfonamido)benzyl)-1H-tetrazol-5-yl)-2-(benzyloxy)ethyl)-2-amino-2-methylpropanamide
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C22H29N7O4S
 1
1 Ki = 4450 nM
CP0296917
(S)-2-amino-N-(1-(2-benzyl-2H-tetrazol-5-yl)-2-(benzyloxy)ethyl)-2-methylpropanamide
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C21H26N6O2
 1
1 Ki = 4750 nM
CP0241192
(S)-N-(1-(1-(2-(1H-tetrazol-5-yl)ethyl)-1H-tetrazol-5-yl)-2-(benzyloxy)ethyl)-2-amino-2-methylpropanamide
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C17H24N10O2
 1
1 Ki = 5000 nM
CP0051349
(R)-methyl 3-(5-(1-(2-amino-2-methylpropanamido)-2-(1H-indol-3-yl)ethyl)-1H-tetrazol-1-yl)propanoate
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C19H25N7O3
 1
1 Ki > 5000 nM
CP0075566
(S)-2-amino-N-(2-(benzyloxy)-1-(2-(cyanomethyl)-2H-tetrazol-5-yl)ethyl)-2-methylpropanamide
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C16H21N7O2
 1
1 Ki > 5000 nM
CP0075567
(S)-2-amino-N-(2-(benzyloxy)-1-(2-(4-cyanobutyl)-2H-tetrazol-5-yl)ethyl)-2-methylpropanamide
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C19H27N7O2
 1
1 Ki > 5000 nM
CP0075568
(S)-2-amino-N-(2-(benzyloxy)-1-(1-(5-(methylsulfonamido)pentyl)-1H-tetrazol-5-yl)ethyl)-2-methylpropanamide
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C20H33N7O4S
 1
1 Ki > 5000 nM
CP0103666
(S)-N-(1-(2-(2-(methylsulfonamido)benzyl)-2H-tetrazol-5-yl)-2-(benzyloxy)ethyl)-2-amino-2-methylpropanamide
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C22H29N7O4S
 1
1 Ki > 5000 nM
CP0165853
(S)-N-(1-(2-(4-(methylsulfonamido)benzyl)-2H-tetrazol-5-yl)-2-(benzyloxy)ethyl)-2-amino-2-methylpropanamide
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C22H29N7O4S
 1
1 Ki > 5000 nM
CP0241188
(S,E)-2-amino-N-(2-(benzyloxy)-1-(2-cinnamyl-2H-tetrazol-5-yl)ethyl)-2-methylpropanamide
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C23H28N6O2
 1
1 Ki > 5000 nM
CP0241189
2-amino-N-((S)-2-(benzyloxy)-1-(2-((1-(methylsulfonyl)indolin-2-yl)methyl)-2H-tetrazol-5-yl)ethyl)-2-methylpropanamide
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C24H31N7O4S
 1
1 Ki > 5000 nM
CP0241190
methyl 2-[5-[(1S)-1-[(2-amino-2-methylpropanoyl)amino]-2-phenylmethoxyethyl]tetrazol-2-yl]-2-phenylacetate
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C23H28N6O4
 1
1 Ki > 5000 nM
CP0261718
(S)-N-(1-(1-(3-(methylsulfonamido)benzyl)-1H-tetrazol-5-yl)-2-(benzyloxy)ethyl)-2-amino-2-methylpropanamide
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C22H29N7O4S
 1
1 Ki > 5000 nM
CP0296916
(S)-N-(1-(2-(3-(methylsulfonamido)benzyl)-2H-tetrazol-5-yl)-2-(benzyloxy)ethyl)-2-amino-2-methylpropanamide
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C22H29N7O4S
 1
1 Ki > 5000 nM
CP0332882
(S)-N-(1-(1-(4-(methylsulfonamido)benzyl)-1H-tetrazol-5-yl)-2-(benzyloxy)ethyl)-2-amino-2-methylpropanamide
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C22H29N7O4S
 1
1 Ki > 5000 nM
CP0084689
(6S,12R)-12-(3-aminopropyl)-8-methyl-6-propyl-2-oxa-5,8,11,14-tetrazabicyclo[16.4.0]docosa-1(22),18,20-triene-7,10,13-trione
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C24H39N5O4
 1
1 Ki > 10000 nM
CP0205853
3-[(6S,12R)-12-benzyl-8-methyl-7,10,13-trioxo-2-oxa-5,8,11,14-tetrazabicyclo[16.4.0]docosa-1(22),18,20-trien-6-yl]propanoic acid
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C28H36N4O6
 1
1 Ki > 10000 nM
CP0205854
(6S,12R)-12-(hydroxymethyl)-8-methyl-6-propyl-2-oxa-5,8,11,14-tetrazabicyclo[16.4.0]docosa-1(22),18,20-triene-7,10,13-trione
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C22H34N4O5
 1
1 Ki > 10000 nM
CP0238495
3-[(6S,12R)-8-methyl-7,10,13-trioxo-6-propyl-2-oxa-5,8,11,14-tetrazabicyclo[16.4.0]docosa-1(22),18,20-trien-12-yl]propanoic acid
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C24H36N4O6
 1
1 Ki > 10000 nM
CP0238530
(6S,12R)-12-benzyl-6-(hydroxymethyl)-8-methyl-2-oxa-5,8,11,14-tetrazabicyclo[16.4.0]docosa-1(22),18,20-triene-7,10,13-trione
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C26H34N4O5
 1
1 Ki > 10000 nM
CP0260071
(3R,6R,9S)-3-benzyl-9-[(2S)-butan-2-yl]-6,7-dimethyl-1,4,7,10-tetrazacycloheptadecane-2,5,8-trione
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C26H42N4O3
 1
1 Ki > 10000 nM
Clinical Information about the Protein
Target 1 ( Growth hormone secretagogue receptor 1 (GHSR) )
Target Type Successful Target
Disease 7 Target-related Diseases  7
1 Fibromyalgia [ICD-11: MG30.01]
2 Somatotropin deficiency [ICD-11: 5A61.0]
3 Gastrointestinal disease [ICD-11: DE2Z]
4 Growth hormone deficiency [ICD-11: 5A61.3]
5 Frailty [ICD-11: MG2A]
6 Postoperative ileus [ICD-11: DA91-DB30]
7 Type-2 diabetes [ICD-11: 5A11]
Approved Drug(s) 2 Approved Drugs  2
1 Ibutamoren Approved
Fibromyalgia
2 Macimorelin Approved
Somatotropin deficiency
Clinical Trial Drug(s) 6 Clinical Trial Drugs  6
1 TZP-101 Phase 2b
Gastrointestinal disease
2 Ibutamoren mesylate Phase 2
Growth hormone deficiency
3 RQ-00000005 Phase 2
Frailty
4 Tabimorelin Phase 2
Growth hormone deficiency
5 Ipamorelin Phase 1/2
Postoperative ileus
6 PF-05190457 Phase 1
Type-2 diabetes
Similar Protein(s) and Bioactivity Statistics
50% Identity
Protein ID Protein Name Protein Organism
PT04369 Mas-related G-protein coupled receptor member X1 Homo sapiens, Human