General Information of the Protein
Protein ID
PT06127
Protein Name
Gastrin-releasing peptide receptor
Secondarily
Protein Name
GRP-preferring bombesin receptor
Gene Name
GRPR
Sequence
MAPNNCSHLNLDVDPFLSCNDTFNQSLSPPKMDNWFHPGFIYVIPAVYGLIIVIGLIGNITLIKIFCTVKSMRNVPNLFISSLALGDLLLLVTCAPVDASKYLADRWLFGRIGCKLIPFIQLTSVGVSVFTLTALSADRYKAIVRPMDIQASHALMKICLKAALIWIVSMLLAIPEAVFSDLHPFHVKDTNQTFISCAPYPHSNELHPKIHSMASFLVFYVIPLAIISVYYYFIARNLIQSAYNLPVEGNIHVKKQIESRKRLAKTVLVFVGLFAFCWLPNHVIYLYRSYHYSEVDTSMLHFVTSICARLLAFTNSCVNPFALYLLSKSFRKQFNTQLLCCQPGLMNRSHSTGRSTTCMTSFKSTNPSATFSLINRNICHEGYV
    Show/Hide
Organism
Mus musculus, Mouse
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 gastrin-releasing peptide (GRP) (PubMed:1671171, PubMed:1707129, PubMed:9345264, PubMed:12526815, PubMed:26658875). Signals via association with G proteins that activate a phosphatidylinositol-calcium second messenger system, resulting in Akt phosphorylation (PubMed:26658875). Contributes to the regulation of food intake (PubMed:12176666). Contributes to the perception of prurient stimuli and transmission of itch signals in the spinal cord that promote scratching behavior, but does not play a role in the perception of pain (PubMed:28280205, PubMed:17653196, PubMed:26658875). Contributes primarily to nonhistaminergic itch sensation (PubMed:28280205). In one study, shown to act in the amygdala as part of an inhibitory network which inhibits memory specifically related to learned fear (PubMed:12526815). In another study, shown to contribute to disinhibition of glutamatergic cells in the auditory cortex via signaling on vasoactive intestinal peptide-expressing cells which leads to enhanced auditory fear memories (PubMed:34610277). Contributes to the induction of sighing through signaling in the pre-Botzinger complex, a cluster of several thousand neurons in the ventrolateral medulla responsible for inspiration during respiratory activity (PubMed:26855425).
    Show/Hide
Uniprot ID
Primary ID:
P21729

Secondarily ID:
Q53WV4
    Show/Hide
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: CL000035 , NIH 3T3
Compound ID Compound Name Compound Formula
CP0409836
(2S)-N-[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2R)-1-[[(2S)-1-[(2R)-2-[[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]amino]methyl]pyrrolidin-1-yl]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]-2-phenylcyclopropane-1-carboxamide
   Show/Hide
C58H72N14O8
 2
1
IC50 = 0.03 nM
   TI
   LI
   LO
   TS
2
IC50 = 0.049 nM
   TI
   LI
   LO
   TS
CP0441769
(2S)-N-[(2R)-1-[[(2S)-1-[(2R)-2-[[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]amino]methyl]pyrrolidin-1-yl]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]-2-[[(2S)-2-[[(2S)-2-[[(2S)-3-(1H-imidazol-5-yl)-2-(3-phenylpropanoylamino)propanoyl]amino]-3-(1H-indol-3-yl)propanoyl]amino]propanoyl]amino]-3-methylbutanamide
   Show/Hide
C57H72N14O8
 1
1
IC50 = 0.038 nM
   TI
   LI
   LO
   TS
CP0451514
1-naphthyl(CO)His-Trp-Ala-Val-DAla-His-DPro(psi)Phe-NH2
   Show/Hide
C59H70N14O8
 1
1
IC50 = 0.05 nM
   TI
   LI
   LO
   TS
CP0448646
4-OHPhCH2CH2(CO)His-Trp-Ala-Val-DAla-His-DPro(psi)Phe-NH2
   Show/Hide
C57H72N14O9
 2
1
IC50 = 0.05 nM
   TI
   LI
   LO
   TS
2
IC50 = 0.23 nM
   TI
   LI
   LO
   TS
CP0459367
2-tetrahydronaphthyl(CO)His-Trp-Ala-Val-DAla-His-DPro(psi)Phe-NH2
   Show/Hide
C59H74N14O8
 2
1
IC50 = 0.079 nM
   TI
   LI
   LO
   TS
2
IC50 = 0.3 nM
   TI
   LI
   LO
   TS
CP0377335
(2S)-N-[2-[[(2S)-1-[(2S)-2-[[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]amino]methyl]pyrrolidin-1-yl]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-2-oxoethyl]-2-[[(2S)-2-[[(2S)-2-[[(2S)-3-(1H-imidazol-5-yl)-2-(3-phenylpropanoylamino)propanoyl]amino]-3-(1H-indol-3-yl)propanoyl]amino]propanoyl]amino]-N,3-dimethylbutanamide
   Show/Hide
C57H72N14O8
 2
1
IC50 = 0.1 nM
   TI
   LI
   LO
   TS
2
IC50 = 21 nM
   TI
   LI
   LO
   TS
CP0451264
2-aminoPhCH2(CO)His-Trp-Ala-Val-DAla-His-DPro(psi)Phe-NH2
   Show/Hide
C56H71N15O8
 2
1
IC50 = 0.1 nM
   TI
   LI
   LO
   TS
2
IC50 = 2 nM
   TI
   LI
   LO
   TS
CP0459359
N-[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]-3-hydroxy-4-[[(2S)-3-(1H-imidazol-5-yl)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-3-(1H-imidazol-5-yl)-2-(3-phenylpropanoylamino)propanoyl]amino]-3-(1H-indol-3-yl)propanoyl]amino]propanoyl]amino]-3-methylbutanoyl]amino]propanoyl]amino]propanoyl]amino]-6-methylheptanamide
   Show/Hide
C60H78N14O10
 2
1
IC50 = 0.1 nM
   TI
   LI
   LO
   TS
2
IC50 = 7.3 nM
   TI
   LI
   LO
   TS
CP0406764
3-CF3PhCH2CH2(CO)His-Trp-Ala-Val-DAla-His-DPro(psi)Phe-NH2
   Show/Hide
C58H71F3N14O8
 2
1
IC50 = 0.16 nM
   TI
   LI
   LO
   TS
2
IC50 = 1 nM
   TI
   LI
   LO
   TS
CP0432964
(CH3)2PhC(CO)His-Trp-Ala-Val-DAla-His-DPro(psi)Phe-NH2
   Show/Hide
C58H74N14O8
 1
1
IC50 = 0.18 nM
   TI
   LI
   LO
   TS
CP0395492
(2S)-N-[(2R)-1-[[(2S)-1-[(2R)-2-[[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]amino]methyl]pyrrolidin-1-yl]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]-2-[[(2S)-2-[[(2S)-2-[[(2S)-3-(1H-imidazol-5-yl)-2-[[(3S)-3-phenylbutanoyl]amino]propanoyl]amino]-3-(1H-indol-3-yl)propanoyl]amino]propanoyl]amino]-3-methylbutanamide
   Show/Hide
C58H74N14O8
 2
1
IC50 = 0.21 nM
   TI
   LI
   LO
   TS
2
IC50 = 1 nM
   TI
   LI
   LO
   TS
CP0377334
(2S)-N-[(2S)-1-[[(2S)-1-[(2S)-2-[[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]amino]methyl]pyrrolidin-1-yl]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]-2-[[(2S)-2-[[(2S)-2-[[(2S)-3-(1H-imidazol-5-yl)-2-(3-phenylpropanoylamino)propanoyl]amino]-3-(1H-indol-3-yl)propanoyl]amino]propanoyl]amino]-3-methylbutanamide
   Show/Hide
C57H72N14O8
 1
1
IC50 = 0.22 nM
   TI
   LI
   LO
   TS
CP0409762
(2S)-N-[(2R)-1-[[(2S)-1-[(2R)-2-[[[(2S)-1-amino-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]methyl]pyrrolidin-1-yl]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]-2-[[(2S)-2-[[(2S)-2-[[(2S)-3-(1H-imidazol-5-yl)-2-(3-phenylpropanoylamino)propanoyl]amino]-3-(1H-indol-3-yl)propanoyl]amino]propanoyl]amino]-3-methylbutanamide
   Show/Hide
C57H72N14O9
 1
1
IC50 = 0.33 nM
   TI
   LI
   LO
   TS
CP0448849
(2S)-N-[(2R)-1-[[(2S)-1-[(2R)-2-[[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]amino]methyl]pyrrolidin-1-yl]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]-2-[[(2S)-2-[[(2S)-2-[[(2S)-3-(1H-imidazol-5-yl)-2-[[(3R)-3-phenylbutanoyl]amino]propanoyl]amino]-3-(1H-indol-3-yl)propanoyl]amino]propanoyl]amino]-3-methylbutanamide
   Show/Hide
C58H74N14O8
 1
1
IC50 = 0.49 nM
   TI
   LI
   LO
   TS
CP0482730
3-isoquinolyl(CO)His-Trp-Ala-Val-DAla-His-DPro(psi)Phe-NH2
   Show/Hide
C58H69N15O8
 1
1
IC50 = 0.57 nM
   TI
   LI
   LO
   TS
CP0527749
2-{2-[2-[2-(2,2-Dimethyl-propionylamino)-3-(3H-imidazol-4-yl)-propionylamino]-3-(1H-indol-3-yl)-propionylamino]-propionylamino}-N-{[2-(3H-imidazol-4-yl)-1-(1-isobutyl-hexylcarbamoyl)-ethylcarbamoyl]-methyl}-3-methyl-butyramide
   Show/Hide
C48H72N12O7
 2
1
IC50 = 0.6 nM
   TI
   LI
   LO
   TS
2
IC50 = 1.8 nM
   TI
   LI
   LO
   TS
CP0514967
(2S)-N-[(2S)-1-[[(2S)-1-[(2R)-2-[[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]amino]methyl]pyrrolidin-1-yl]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]-2-[[(2S)-2-[[(2S)-3-(1-benzothiophen-3-yl)-2-[[(2S)-3-(1H-imidazol-5-yl)-2-(3-phenylpropanoylamino)propanoyl]amino]propanoyl]amino]propanoyl]amino]-3-methylbutanamide
   Show/Hide
C57H71N13O8S
 1
1
IC50 = 0.75 nM
   TI
   LI
   LO
   TS
CP0406766
(2S)-N-[(2R)-1-[[(2S)-1-[(2R)-2-[[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]amino]methyl]pyrrolidin-1-yl]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]-2-[[(2S)-2-[[(2S)-2-[[(2S)-3-(1H-imidazol-5-yl)-2-[[(2R)-2-phenylpropanoyl]amino]propanoyl]amino]-3-(1H-indol-3-yl)propanoyl]amino]propanoyl]amino]-3-methylbutanamide
   Show/Hide
C57H72N14O8
 2
1
IC50 = 0.95 nM
   TI
   LI
   LO
   TS
2
IC50 = 3 nM
   TI
   LI
   LO
   TS
CP0409649
(2S)-N-[(2S)-1-[[(2S)-1-[(2S)-2-[[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]amino]methyl]pyrrolidin-1-yl]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]-2-[[(2S)-2-[[(2S)-3-(1H-indol-3-yl)-2-[[(2S)-2-(3-phenylpropanoylamino)-3-thiophen-2-ylpropanoyl]amino]propanoyl]amino]propanoyl]amino]-3-methylbutanamide
   Show/Hide
C58H72N12O8S
 2
1
IC50 = 1 nM
   TI
   LI
   LO
   TS
2
IC50 = 5.6 nM
   TI
   LI
   LO
   TS
CP0461143
(2S)-N-[(2R)-1-[[(2S)-1-[(2R)-2-[[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]amino]methyl]pyrrolidin-1-yl]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]-2-[[(2S)-2-[[(2S)-2-[[(2S)-3-(1H-imidazol-5-yl)-2-[[(2S)-2-phenylpropanoyl]amino]propanoyl]amino]-3-(1H-indol-3-yl)propanoyl]amino]propanoyl]amino]-3-methylbutanamide
   Show/Hide
C57H72N14O8
 2
1
IC50 = 1 nM
   TI
   LI
   LO
   TS
2
IC50 = 1.3 nM
   TI
   LI
   LO
   TS
CP0375748
2-{2-[2-[2-Acetylamino-3-(3H-imidazol-4-yl)-propionylamino]-3-(1H-indol-3-yl)-propionylamino]-propionylamino}-N-{[2-(3H-imidazol-4-yl)-1-(1-isobutyl-3-methyl-butylcarbamoyl)-ethylcarbamoyl]-methyl}-3-methyl-butyramide
   Show/Hide
C44H64N12O7
 2
1
IC50 = 1.2 nM
   TI
   LI
   LO
   TS
2
IC50 = 8 nM
   TI
   LI
   LO
   TS
CP0463151
(CH3)2PhCCH2(CO)His-Trp-Ala-Val-DAla-His-DPro(psi)Phe-NH2
   Show/Hide
C59H76N14O8
 2
1
IC50 = 1.2 nM
   TI
   LI
   LO
   TS
2
IC50 = 10 nM
   TI
   LI
   LO
   TS
CP0414805
2-{2-[2-[2-Acetylamino-3-(3H-imidazol-4-yl)-propionylamino]-3-(1H-indol-3-yl)-propionylamino]-propionylamino}-N-{[2-(3H-imidazol-4-yl)-1-(1-isobutyl-pentylcarbamoyl)-ethylcarbamoyl]-methyl}-3-methyl-butyramide
   Show/Hide
C44H64N12O7
 2
1
IC50 = 1.4 nM
   TI
   LI
   LO
   TS
2
IC50 = 3 nM
   TI
   LI
   LO
   TS
CP0505280
Ac-His-Trp-Ala-Val-Gly-His-Leu-Met-NH2
   Show/Hide
C46H66N14O9S
 1
1
IC50 = 1.8 nM
   TI
   LI
   LO
   TS
CP0440473
(2S)-N-[(2R)-1-[[(2S)-1-[(2R)-2-[[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]amino]methyl]pyrrolidin-1-yl]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]-2-[[(2S)-2-[[(2S)-2-[[(2S)-3-(1H-imidazol-5-yl)-2-(3-phenothiazin-10-ylpropanoylamino)propanoyl]amino]-3-(1H-indol-3-yl)propanoyl]amino]propanoyl]amino]-3-methylbutanamide
   Show/Hide
C63H75N15O8S
 1
1
IC50 = 1.9 nM
   TI
   LI
   LO
   TS
CP0509126
2-{2-[2-[2-Acetylamino-3-(3H-imidazol-4-yl)-propionylamino]-3-(1H-indol-3-yl)-propionylamino]-propionylamino}-N-{[2-(3H-imidazol-4-yl)-1-(1-isobutyl-hexylcarbamoyl)-ethylcarbamoyl]-methyl}-3-methyl-butyramide
   Show/Hide
C45H66N12O7
 2
1
IC50 = 2 nM
   TI
   LI
   LO
   TS
2
IC50 = 4 nM
   TI
   LI
   LO
   TS
CP0407203
(2S)-N-[(2R)-1-[[(2S)-1-[(2R)-2-[[[(2S)-1-amino-3-naphthalen-2-yl-1-oxopropan-2-yl]amino]methyl]pyrrolidin-1-yl]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]-2-[[(2S)-2-[[(2S)-2-[[(2S)-3-(1H-imidazol-5-yl)-2-(3-phenylpropanoylamino)propanoyl]amino]-3-(1H-indol-3-yl)propanoyl]amino]propanoyl]amino]-3-methylbutanamide
   Show/Hide
C61H74N14O8
 2
1
IC50 = 2 nM
   TI
   LI
   LO
   TS
2
IC50 = 5 nM
   TI
   LI
   LO
   TS
CP0400004
2-{2-[2-[2-Acetylamino-3-(3H-imidazol-4-yl)-propionylamino]-3-(1H-indol-3-yl)-propionylamino]-propionylamino}-N-{[2-(3H-imidazol-4-yl)-1-(1-isobutyl-pentylcarbamoyl)-ethylcarbamoyl]-methyl}-3-methyl-butyramide
   Show/Hide
C44H64N12O7
 2
1
IC50 = 2.4 nM
   TI
   LI
   LO
   TS
2
IC50 = 6 nM
   TI
   LI
   LO
   TS
CP0404545
2-{2-[2-[2-Acetylamino-3-(3H-imidazol-4-yl)-propionylamino]-3-(1H-indol-3-yl)-propionylamino]-propionylamino}-N-{[2-(3H-imidazol-4-yl)-1-(3-methyl-1-propyl-butylcarbamoyl)-ethylcarbamoyl]-methyl}-3-methyl-butyramide
   Show/Hide
C43H62N12O7
 2
1
IC50 = 2.6 nM
   TI
   LI
   LO
   TS
2
IC50 = 10 nM
   TI
   LI
   LO
   TS
CP0384171
2-{2-[2-[2-Acetylamino-3-(3H-imidazol-4-yl)-propionylamino]-3-(1H-indol-3-yl)-propionylamino]-propionylamino}-N-{[2-(3H-imidazol-4-yl)-1-(1-isobutyl-heptylcarbamoyl)-ethylcarbamoyl]-methyl}-3-methyl-butyramide
   Show/Hide
C46H68N12O7
 2
1
IC50 = 2.8 nM
   TI
   LI
   LO
   TS
2
IC50 = 7 nM
   TI
   LI
   LO
   TS
CP0406141
2-{2-[2-[2-Acetylamino-3-(3H-imidazol-4-yl)-propionylamino]-3-(1H-indol-3-yl)-propionylamino]-propionylamino}-N-{[2-(3H-imidazol-4-yl)-1-(3-methyl-1-propoxymethyl-butylcarbamoyl)-ethylcarbamoyl]-methyl}-3-methyl-butyramide
   Show/Hide
C44H64N12O8
 2
1
IC50 = 3.2 nM
   TI
   LI
   LO
   TS
2
IC50 = 18 nM
   TI
   LI
   LO
   TS
CP0504857
Ac-His-Trp-Ala-Val-D-Ala-His-Leu-Met-NH2
   Show/Hide
C47H68N14O9S
 1
1
IC50 = 3.2 nM
   TI
   LI
   LO
   TS
CP0399869
2-{2-[2-[2-Acetylamino-3-(3H-imidazol-4-yl)-propionylamino]-3-(1H-indol-3-yl)-propionylamino]-propionylamino}-N-{[1-(1-butyl-pentylcarbamoyl)-2-(3H-imidazol-4-yl)-ethylcarbamoyl]-methyl}-3-methyl-butyramide
   Show/Hide
C44H64N12O7
 2
1
IC50 = 3.3 nM
   TI
   LI
   LO
   TS
2
IC50 = 11 nM
   TI
   LI
   LO
   TS
CP0448036
4-CF3PhCH2(CO)His-Trp-Ala-Val-DAla-His-DPro(psi)Phe-NH2
   Show/Hide
C57H69F3N14O8
 1
1
IC50 = 3.7 nM
   TI
   LI
   LO
   TS
CP0447980
2-[2-[2-(2-{2-[2-[2-Acetylamino-3-(3H-imidazol-4-yl)-propionylamino]-3-(1H-indol-3-yl)-propionylamino]-propionylamino}-3-methyl-butyrylamino)-acetylamino]-3-(3H-imidazol-4-yl)-propionylamino]-4-methyl-pentanoic acid ethyl ester
   Show/Hide
C43H60N12O9
 2
1
IC50 = 3.9 nM
   TI
   LI
   LO
   TS
2
IC50 = 20 nM
   TI
   LI
   LO
   TS
CP0503457
(CH3)CCO-His-Trp-Ala-Val-Gly-His-Leu-Met-NH2
   Show/Hide
C49H72N14O9S
 1
1
IC50 = 4.1 nM
   TI
   LI
   LO
   TS
CP0380786
2-{2-[2-[2-Acetylamino-3-(3H-imidazol-4-yl)-propionylamino]-3-(1H-indol-3-yl)-propionylamino]-propionylamino}-N-{[2-(3H-imidazol-4-yl)-1-(3-methyl-1-propyl-butylcarbamoyl)-ethylcarbamoyl]-methyl}-3-methyl-butyramide
   Show/Hide
C43H62N12O7
 2
1
IC50 = 4.9 nM
   TI
   LI
   LO
   TS
2
IC50 = 35 nM
   TI
   LI
   LO
   TS
CP0497940
2-{2-[2-[2-Acetylamino-3-(3H-imidazol-4-yl)-propionylamino]-3-(1H-indol-3-yl)-propionylamino]-propionylamino}-N-{[1-(1-ethoxymethyl-3-methyl-butylcarbamoyl)-2-(3H-imidazol-4-yl)-ethylcarbamoyl]-methyl}-3-methyl-butyramide
   Show/Hide
C44H64N12O8
 2
1
IC50 = 5 nM
   TI
   LI
   LO
   TS
2
IC50 = 35 nM
   TI
   LI
   LO
   TS
CP0449423
2-{2-[2-[2-Acetylamino-3-(3H-imidazol-4-yl)-propionylamino]-3-(1H-indol-3-yl)-propionylamino]-propionylamino}-N-{1-[1-(1-ethoxymethyl-3-methyl-butylcarbamoyl)-2-(3H-imidazol-4-yl)-ethylcarbamoyl]-ethyl}-3-methyl-butyramide
   Show/Hide
C43H62N12O8
 2
1
IC50 = 6.2 nM
   TI
   LI
   LO
   TS
2
IC50 = 31 nM
   TI
   LI
   LO
   TS
CP0453558
(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-amino-3-naphthalen-2-ylpropanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]-3-(1H-indol-3-yl)propanoyl]amino]propanoyl]amino]-N-[(2R)-1-[[(2S)-1-[(2R)-2-[[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]amino]methyl]pyrrolidin-1-yl]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]-3-methylbutanamide
   Show/Hide
C61H75N15O8
 1
1
IC50 = 7.7 nM
   TI
   LI
   LO
   TS
CP0437445
2-{2-[2-[2-Acetylamino-3-(3H-imidazol-4-yl)-propionylamino]-3-(1H-indol-3-yl)-propionylamino]-propionylamino}-N-{[2-(3H-imidazol-4-yl)-1-(1-methoxymethyl-3-methyl-butylcarbamoyl)-ethylcarbamoyl]-methyl}-3-methyl-butyramide
   Show/Hide
C42H60N12O8
 2
1
IC50 = 8.3 nM
   TI
   LI
   LO
   TS
2
IC50 = 91 nM
   TI
   LI
   LO
   TS
CP0451570
3-CF3PhCH2(CO)His-Trp-Ala-Val-DAla-His-DPro(psi)Phe-NH2
   Show/Hide
C57H69F3N14O8
 1
1
IC50 = 8.4 nM
   TI
   LI
   LO
   TS
CP0406381
2-{2-[2-[2-Acetylamino-3-(3H-imidazol-4-yl)-propionylamino]-3-(1H-indol-3-yl)-propionylamino]-propionylamino}-N-({2-(3H-imidazol-4-yl)-1-[3-methyl-1-(3-methyl-butoxymethyl)-butylcarbamoyl]-ethylcarbamoyl}-methyl)-3-methyl-butyramide
   Show/Hide
C46H68N12O8
 2
1
IC50 = 11 nM
   TI
   LI
   LO
   TS
2
IC50 = 32 nM
   TI
   LI
   LO
   TS
CP0437371
2-{2-[2-[2-Acetylamino-3-(3H-imidazol-4-yl)-propionylamino]-3-(1H-indol-3-yl)-propionylamino]-propionylamino}-N-{[2-(3H-imidazol-4-yl)-1-(1-isobutyl-hexylcarbamoyl)-ethylcarbamoyl]-methyl}-3-methyl-butyramide
   Show/Hide
C45H66N12O7
 2
1
IC50 = 11 nM
   TI
   LI
   LO
   TS
2
IC50 = 22 nM
   TI
   LI
   LO
   TS
CP0453631
2-CF3PhCH2CH2(CO)His-Trp-Ala-Val-DAla-His-DPro(psi)Phe-NH2
   Show/Hide
C57H69F3N14O8
 1
1
IC50 = 12 nM
   TI
   LI
   LO
   TS
CP0430287
2-{2-[2-[2-Acetylamino-3-(3H-imidazol-4-yl)-propionylamino]-3-(1H-indol-3-yl)-propionylamino]-propionylamino}-N-{[2-(3H-imidazol-4-yl)-1-(1-propyl-butylcarbamoyl)-ethylcarbamoyl]-methyl}-3-methyl-butyramide
   Show/Hide
C42H60N12O7
 2
1
IC50 = 18 nM
   TI
   LI
   LO
   TS
2
IC50 = 80 nM
   TI
   LI
   LO
   TS
CP0459222
(2S)-N-[(2S)-1-[[(2S)-1-[(2S)-2-[3-[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]amino]-1-hydroxy-3-oxopropyl]pyrrolidin-1-yl]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]-2-[[(2S)-2-[[(2S)-2-[[(2S)-3-(1H-imidazol-5-yl)-2-(3-phenylpropanoylamino)propanoyl]amino]-3-(1H-indol-3-yl)propanoyl]amino]propanoyl]amino]-3-methylbutanamide
   Show/Hide
C59H74N14O10
 2
1
IC50 = 31 nM
   TI
   LI
   LO
   TS
2
IC50 = 50 nM
   TI
   LI
   LO
   TS
CP0496398
(2S)-N-[(2S)-1-[[(2S)-1-[(2R)-2-[3-[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]amino]-1-hydroxy-3-oxopropyl]pyrrolidin-1-yl]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]-2-[[(2S)-2-[[(2S)-2-[[(2S)-3-(1H-imidazol-5-yl)-2-(3-phenylpropanoylamino)propanoyl]amino]-3-(1H-indol-3-yl)propanoyl]amino]propanoyl]amino]-3-methylbutanamide
   Show/Hide
C59H74N14O10
 2
1
IC50 = 60 nM
   TI
   LI
   LO
   TS
2
IC50 = 140 nM
   TI
   LI
   LO
   TS
CP0448760
2-{2-[2-[2-Acetylamino-3-(3H-imidazol-4-yl)-propionylamino]-3-(1H-indol-3-yl)-propionylamino]-propionylamino}-N-{[1-(1-hydroxymethyl-3-methyl-butylcarbamoyl)-2-(3H-imidazol-4-yl)-ethylcarbamoyl]-methyl}-3-methyl-butyramide
   Show/Hide
C41H58N12O8
 2
1
IC50 = 81 nM
   TI
   LI
   LO
   TS
2
IC50 = 300 nM
   TI
   LI
   LO
   TS
CP0469362
Ac-His-Trp-Ala-Val-Ala-His-Leu-Met-NH2
   Show/Hide
C47H68N14O9S
 1
1
IC50 = 180 nM
   TI
   LI
   LO
   TS
CP0441706
2-{2-[2-[2-Acetylamino-3-(3H-imidazol-4-yl)-propionylamino]-3-(1H-indol-3-yl)-propionylamino]-propionylamino}-N-{1-[1-(1-ethoxymethyl-3-methyl-butylcarbamoyl)-2-(3H-imidazol-4-yl)-ethylcarbamoyl]-ethyl}-3-methyl-butyramide
   Show/Hide
C44H64N12O8
 2
1
IC50 = 410 nM
   TI
   LI
   LO
   TS
2
IC50 > 300 nM
   TI
   LI
   LO
   TS
CP0448848
(2S)-N-[(2S)-1-[[(2S)-1-[(2S)-2-[[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]amino]methyl]pyrrolidin-1-yl]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]-2-[[(2S)-2-[[(2S)-2-[[(2S)-3-(1H-imidazol-5-yl)-2-(3-phenylpropanoylamino)propanoyl]amino]-3-(1H-indol-3-yl)propanoyl]amino]propyl]amino]-3-methylbutanamide
   Show/Hide
C57H74N14O7
 1
1
IC50 > 1000 nM
   TI
   LI
   LO
   TS