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Pyroglutamylated RFamide peptide receptor Inhibitors (IC50, Ki)

Structure
Compound Name
Standard Type
Standard Values (in nM)
N-(4,6,7-Trimethylquinazolin-2-yl)guanidineIC502511.89 [1], 5011.87 [2]
(5-Bromo-1-methylpyrrolo[2,3-c]pyridin-2-yl)-[6-[(dimethylamino)methyl]-3,4-dihydro-1H-isoquinolin-2-yl]methanoneIC50240.0 [1], 280.0 [2]
(5-Chloro-1-methylindol-2-yl)-[6-[(dimethylamino)methyl]-7-methyl-3,4-dihydro-1H-isoquinolin-2-yl]methanoneIC5040.0 [1], 46.0 [2]
(6R)-N-(5-Chloro-2-methoxyphenyl)-6-(dimethylamino)-4-methoxy-5,6,7,8-tetrahydronaphthalene-1-sulfonamideIC5079.43 [1]
(5-Chloro-1-methylindol-2-yl)-[6-[(dimethylamino)methyl]-3,4-dihydro-1H-isoquinolin-2-yl]methanoneIC5070.0 [1]
N'-[3-(Cyclopentylsulfanylmethyl)-4-methoxyphenyl]benzenecarboximidamideIC5019.95 [1], 25.12 [2]
N-[3-(Cyclopentylsulfanylmethyl)-4-methoxyphenyl]pyridin-2-amineIC5012589.25 [1], 31622.78 [2]
3-(Cyclopentylsulfanylmethyl)-4-methoxy-N'-phenylbenzenecarboximidamideIC501000.0 [1], 3981.07 [2]
N'-[3-(Cyclopentylsulfanylmethyl)phenyl]thiophene-2-carboximidamideIC50794.33 [1], 2511.89 [2]
N'-[3-(Cyclopentylsulfanylmethyl)-4-methylphenyl]thiophene-2-carboximidamideIC501584.89 [1], 10000.0 [2]
N'-[3-(Cyclopentylsulfanylmethyl)-4-fluorophenyl]thiophene-2-carboximidamideIC50501.19 [1], 1258.93 [2]
N'-[4-Chloro-3-(cyclopentylsulfanylmethyl)phenyl]thiophene-2-carboximidamideIC501000.0 [1], 3981.07 [2]
N'-[3-(Cyclopentyloxymethyl)-4-methoxyphenyl]thiophene-2-carboximidamideIC502511.89 [1], 10000.0 [2]
N'-[3-(2-Cyclopentylethyl)-4-methoxyphenyl]benzenecarboximidamideIC50199.53 [1], 316.23 [2]
N'-[4-Methoxy-3-(phenylsulfanylmethyl)phenyl]benzenecarboximidamideIC501584.89 [1], 7943.28 [2]
N-[[5-[[Amino(phenyl)methylidene]amino]-2-methoxyphenyl]methyl]cyclopentanecarboxamideIC502511.89 [1], 7943.28 [2]
N'-[3-(Cyclopentylsulfanylmethyl)-4-methoxyphenyl]thiophene-2-carboximidamideIC5050.12 [1], 158.49 [2]
N'-[3-(Cyclopentylsulfanylmethyl)-4-methoxyphenyl]thiophene-3-carboximidamideIC50100.0 [1], 125.89 [2]
N'-[3-(Cyclopentylsulfanylmethyl)-4-methoxyphenyl]-4-methylthiophene-2-carboximidamideIC5063.1 [1], 100.0 [2]
5-Bromo-N'-[3-(cyclopentylsulfanylmethyl)-4-methoxyphenyl]thiophene-2-carboximidamideIC5019.95 [1], 125.89 [2]
4-Chloro-N'-[3-(cyclopentylsulfanylmethyl)-4-methoxyphenyl]benzenecarboximidamideIC5012.59 [1], 39.81 [2]
N'-[3-(Cyclopentylsulfanylmethyl)-4-methoxyphenyl]-1,3-thiazole-2-carboximidamideIC502511.89 [1], 25118.86 [2]
N'-[3-(Cyclopentylsulfanylmethyl)-4-methoxyphenyl]pyridine-3-carboximidamideIC50251.19 [1], 501.19 [2]
N-[3-(Cyclopentylsulfanylmethyl)-4-methoxyphenyl]thiophene-2-carboxamideIC507943.28 [1], 31622.78 [2]
N-[3-(Cyclopentylsulfanylmethyl)-4-methoxyphenyl]-N'-methylthiophene-2-carboximidamideIC50251.19 [1], 630.96 [2]
(5-Bromo-1-methylpyrrolo[2,3-c]pyridin-2-yl)-[6-[(dimethylamino)methyl]-4-methyl-3,4-dihydro-1H-isoquinolin-2-yl]methanoneIC50110.0 [1]
(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[2-[(2-Aminoacetyl)amino]acetyl]amino]-3-phenylpropanoyl]amino]-3-hydroxypropanoyl]amino]-3-phenylpropanoyl]amino]-N-[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]-5-(diaminomethylideneamino)pentanamideIC508730.0 [1]
CID 56659503IC501.26 [1]
(5-Chloro-1-methylpyrrolo[2,3-c]pyridin-2-yl)-[6-[(dimethylamino)methyl]-3,4-dihydro-1H-isoquinolin-2-yl]methanoneIC50570.0 [1]
[6-[(Dimethylamino)methyl]-3,4-dihydro-1H-isoquinolin-2-yl]-(1-methylpyrrolo[2,3-c]pyridin-2-yl)methanoneIC502900.0 [1]
[6-[(Dimethylamino)methyl]-3,4-dihydro-1H-isoquinolin-2-yl]-(1,5-dimethylpyrrolo[2,3-c]pyridin-2-yl)methanoneIC5018900.0 [1]
[6-[(Dimethylamino)methyl]-3,4-dihydro-1H-isoquinolin-2-yl]-(5-iodo-1-methylpyrrolo[2,3-c]pyridin-2-yl)methanoneIC50130.0 [1]
[6-[(Dimethylamino)methyl]-3,4-dihydro-1H-isoquinolin-2-yl]-(5-ethynyl-1-methylpyrrolo[2,3-c]pyridin-2-yl)methanoneIC506000.0 [1]
[6-[(Dimethylamino)methyl]-3,4-dihydro-1H-isoquinolin-2-yl]-[1-methyl-5-(trifluoromethyl)pyrrolo[2,3-c]pyridin-2-yl]methanoneIC503300.0 [1]
[6-[(Dimethylamino)methyl]-3,4-dihydro-1H-isoquinolin-2-yl]-(1-methyl-5-phenylpyrrolo[2,3-c]pyridin-2-yl)methanoneIC5041000.0 [1]
(5-Chloro-1-methylpyrrolo[2,3-c]pyridin-2-yl)-[6-[(dimethylamino)methyl]-1-methyl-3,4-dihydro-1H-isoquinolin-2-yl]methanoneIC50500.0 [1]
(5-Chloro-1-methylpyrrolo[2,3-c]pyridin-2-yl)-[6-[(dimethylamino)methyl]-3-methyl-3,4-dihydro-1H-isoquinolin-2-yl]methanoneIC50710.0 [1]
(5-Chloro-1-methylpyrrolo[2,3-c]pyridin-2-yl)-[6-[1-(dimethylamino)ethyl]-3,4-dihydro-1H-isoquinolin-2-yl]methanoneIC50460.0 [1]
(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[2-[(2-Aminoacetyl)amino]acetyl]amino]-3-phenylpropanoyl]amino]-3-hydroxypropanoyl]amino]-3-phenylpropanoyl]amino]-4-[[amino(diethylamino)methylidene]amino]-N-[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]butanamideIC50100000.0 [1]
(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[2-[(2-Aminoacetyl)amino]acetyl]amino]-3-phenylpropanoyl]amino]-3-hydroxypropanoyl]amino]-3-phenylpropanoyl]amino]-5-[[amino(dimethylamino)methylidene]amino]-N-[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]pentanamideIC506060.0 [1]
(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[2-[(2-Aminoacetyl)amino]acetyl]amino]-3-phenylpropanoyl]amino]-3-hydroxypropanoyl]amino]-3-phenylpropanoyl]amino]-4-[[amino(ethylamino)methylidene]amino]-N-[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]butanamideIC50100000.0 [1]
(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[2-[(2-Aminoacetyl)amino]acetyl]amino]-3-phenylpropanoyl]amino]-3-hydroxypropanoyl]amino]-3-phenylpropanoyl]amino]-N-[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]-5-[(N,N,N'-trimethylcarbamimidoyl)amino]pentanamideIC508250.0 [1]
(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[2-[(2-Aminoacetyl)amino]acetyl]amino]-3-phenylpropanoyl]amino]-3-hydroxypropanoyl]amino]-3-phenylpropanoyl]amino]-6-[[amino(dimethylamino)methylidene]amino]-N-[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]hexanamideIC50100000.0 [1]
(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[2-[(2-Aminoacetyl)amino]acetyl]amino]-3-phenylpropanoyl]amino]-3-hydroxypropanoyl]amino]-3-phenylpropanoyl]amino]-4-[[amino(azetidin-1-yl)methylidene]amino]-N-[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]butanamideIC50100000.0 [1]
(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[2-[(2-Aminoacetyl)amino]acetyl]amino]-3-phenylpropanoyl]amino]-3-hydroxypropanoyl]amino]-3-phenylpropanoyl]amino]-6-[[amino(ethylamino)methylidene]amino]-N-[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]hexanamideIC50100000.0 [1]
(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[2-[(2-Aminoacetyl)amino]acetyl]amino]-3-phenylpropanoyl]amino]-3-hydroxypropanoyl]amino]-3-phenylpropanoyl]amino]-6-[[amino(diethylamino)methylidene]amino]-N-[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]hexanamideIC50100000.0 [1]
(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[2-[(2-Aminoacetyl)amino]acetyl]amino]-3-phenylpropanoyl]amino]-3-hydroxypropanoyl]amino]-3-phenylpropanoyl]amino]-5-[[amino(diethylamino)methylidene]amino]-N-[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]pentanamideIC50100000.0 [1]
(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[2-[(2-Aminoacetyl)amino]acetyl]amino]-3-phenylpropanoyl]amino]-3-hydroxypropanoyl]amino]-3-phenylpropanoyl]amino]-N-[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]-6-[(N'-methylcarbamimidoyl)amino]hexanamideIC50100000.0 [1]
(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[2-[(2-Aminoacetyl)amino]acetyl]amino]-3-phenylpropanoyl]amino]-3-hydroxypropanoyl]amino]-3-phenylpropanoyl]amino]-N-[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]-6-[(N,N,N'-trimethylcarbamimidoyl)amino]hexanamideIC50100000.0 [1]
(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[2-[(2-Aminoacetyl)amino]acetyl]amino]-3-phenylpropanoyl]amino]-3-hydroxypropanoyl]amino]-3-phenylpropanoyl]amino]-N-[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]-4-[(N,N,N'-trimethylcarbamimidoyl)amino]butanamideIC50100000.0 [1]
(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[2-[(2-Aminoacetyl)amino]acetyl]amino]-3-phenylpropanoyl]amino]-3-hydroxypropanoyl]amino]-3-phenylpropanoyl]amino]-5-[[amino-[ethyl(methyl)amino]methylidene]amino]-N-[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]pentanamideIC50100000.0 [1]
(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[2-[(2-Aminoacetyl)amino]acetyl]amino]-3-phenylpropanoyl]amino]-3-hydroxypropanoyl]amino]-3-phenylpropanoyl]amino]-N-[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]-4-[(N'-propylcarbamimidoyl)amino]butanamideIC50100000.0 [1]
(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[2-[(2-Aminoacetyl)amino]acetyl]amino]-3-phenylpropanoyl]amino]-3-hydroxypropanoyl]amino]-3-phenylpropanoyl]amino]-N-[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]-4-[(N,N'-dimethylcarbamimidoyl)amino]butanamideIC50100000.0 [1]
(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[2-[(2-Aminoacetyl)amino]acetyl]amino]-3-phenylpropanoyl]amino]-3-hydroxypropanoyl]amino]-3-phenylpropanoyl]amino]-4-[[amino(dimethylamino)methylidene]amino]-N-[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]butanamideIC50100000.0 [1]
(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[2-[(2-Aminoacetyl)amino]acetyl]amino]-3-phenylpropanoyl]amino]-3-hydroxypropanoyl]amino]-3-phenylpropanoyl]amino]-6-[[amino-[ethyl(methyl)amino]methylidene]amino]-N-[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]hexanamideIC50100000.0 [1]
(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[2-[(2-Aminoacetyl)amino]acetyl]amino]-3-phenylpropanoyl]amino]-3-hydroxypropanoyl]amino]-3-phenylpropanoyl]amino]-6-[[amino(azetidin-1-yl)methylidene]amino]-N-[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]hexanamideIC50100000.0 [1]
(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[2-[(2-Aminoacetyl)amino]acetyl]amino]-3-phenylpropanoyl]amino]-3-hydroxypropanoyl]amino]-3-phenylpropanoyl]amino]-4-[[amino-[ethyl(methyl)amino]methylidene]amino]-N-[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]butanamideIC50100000.0 [1]
(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[2-[(2-Aminoacetyl)amino]acetyl]amino]-3-phenylpropanoyl]amino]-3-hydroxypropanoyl]amino]-3-phenylpropanoyl]amino]-N-[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]-4-[[N'-(2-methylpropyl)carbamimidoyl]amino]butanamideIC50100000.0 [1]
(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[2-[(2-Aminoacetyl)amino]acetyl]amino]-3-phenylpropanoyl]amino]-3-hydroxypropanoyl]amino]-3-phenylpropanoyl]amino]-N-[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]-4-[(N'-methylcarbamimidoyl)amino]butanamideIC50100000.0 [1]
(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[2-[(2-Aminoacetyl)amino]acetyl]amino]-3-phenylpropanoyl]amino]-3-hydroxypropanoyl]amino]-3-phenylpropanoyl]amino]-N-[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]-5-[(N,N'-dimethylcarbamimidoyl)amino]pentanamideIC50100000.0 [1]
(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[2-[(2-Aminoacetyl)amino]acetyl]amino]-3-phenylpropanoyl]amino]-3-hydroxypropanoyl]amino]-3-phenylpropanoyl]amino]-N-[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]-4-(diaminomethylideneamino)butanamideIC50100000.0 [1]
(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[2-[(2-Aminoacetyl)amino]acetyl]amino]-3-phenylpropanoyl]amino]-3-hydroxypropanoyl]amino]-3-phenylpropanoyl]amino]-5-[[amino(azetidin-1-yl)methylidene]amino]-N-[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]pentanamideIC50100000.0 [1]
(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[2-[(2-Aminoacetyl)amino]acetyl]amino]-3-phenylpropanoyl]amino]-3-hydroxypropanoyl]amino]-3-phenylpropanoyl]amino]-N-[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]-6-[(N,N'-dimethylcarbamimidoyl)amino]hexanamideIC50100000.0 [1]
(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[2-[(2-Aminoacetyl)amino]acetyl]amino]-3-phenylpropanoyl]amino]-3-hydroxypropanoyl]amino]-3-phenylpropanoyl]amino]-N-[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]-6-[(N'-propylcarbamimidoyl)amino]hexanamideIC50100000.0 [1]
(2S)-2-[[2-[[[(2S)-2-[[(2S)-2-[[2-[(2-Aminoacetyl)amino]acetyl]amino]-3-phenylpropanoyl]amino]-3-hydroxypropanoyl]amino]-benzylamino]acetyl]amino]-N-[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]-5-(diaminomethylideneamino)pentanamideIC5010000.0 [1]
(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[2-[2-(2-Aminoacetyl)hydrazinyl]acetyl]amino]-3-phenylpropanoyl]amino]-3-hydroxypropanoyl]amino]-3-phenylpropanoyl]amino]-N-[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]-5-(diaminomethylideneamino)pentanamideIC502987.0 [1]
(2S)-2-[[2-[(2-Aminoacetyl)amino]acetyl]amino]-N-[(2S)-1-[[(2S)-1-[[(2S)-1-[2-(2-amino-2-oxoethyl)-2-benzylhydrazinyl]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]-3-phenylpropanamideIC5010000.0 [1]
(2S)-2-[[2-[[[(2S)-2-[[(2S)-2-[[(2S)-2-[[2-[(2-Aminoacetyl)amino]acetyl]amino]-3-phenylpropanoyl]amino]-3-hydroxypropanoyl]amino]-3-phenylpropanoyl]amino]-[3-(diaminomethylideneamino)propyl]amino]acetyl]amino]-3-phenylpropanamideIC5010000.0 [1]
(2S)-2-[[(2S)-2-[[2-[[[(2S)-2-[[2-[(2-Aminoacetyl)amino]acetyl]amino]-3-phenylpropanoyl]amino]-propylamino]acetyl]amino]-3-phenylpropanoyl]amino]-N-[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]-5-(diaminomethylideneamino)pentanamideIC5010000.0 [1]
(2S)-N-[(2S)-1-Amino-1-oxo-3-phenylpropan-2-yl]-5-(diaminomethylideneamino)-2-[[(2S)-2-[[2-[2,3-dihydroxypropyl-[[(2S)-3-phenyl-2-[(2-piperazin-1-ylacetyl)amino]propanoyl]amino]amino]acetyl]amino]-3-phenylpropanoyl]amino]pentanamideIC501994.0 [1]
4-Bromo-N'-[3-(cyclopentylsulfanylmethyl)-4-methoxyphenyl]thiophene-2-carboximidamideIC50158.49 [1]
N'-[3-(Cyclopentylsulfanylmethyl)-4-methoxyphenyl]-2-phenylethanimidamideIC506309.57 [1]
N'-[3-(Cyclopentylsulfanylmethyl)-4-methoxyphenyl]propanimidamideIC5039810.72 [1]
N'-[3-(Cyclopentylsulfanylmethyl)-4-methoxyphenyl]pyridine-4-carboximidamideIC501584.89 [1]
N-[3-(Cyclopentylsulfanylmethyl)-4-methoxyphenyl]-N,N'-dimethylthiophene-2-carboximidamideIC5039810.72 [1]
N'-[3-(Cyclopentylsulfanylmethyl)-4-(trifluoromethoxy)phenyl]thiophene-2-carboximidamideIC501995.26 [1]
N'-[3-(Cyclopentylsulfinylmethyl)-4-methoxyphenyl]benzenecarboximidamideIC5039810.72 [1]
N'-[3-(Cyclopentylsulfonylmethyl)-4-methoxyphenyl]benzenecarboximidamideIC5031622.78 [1]



References

This online tool may be cited as follows

MLA

"Quest Database™ Pyroglutamylated RFamide peptide receptor Inhibitors (IC50, Ki)." AAT Bioquest, Inc.9 May2024https://www.aatbio.com/data-sets/pyroglutamylated-rfamide-peptide-receptor-inhibitors-ic50-ki.

APA

AAT Bioquest, Inc. (2024May 9). Quest Database™ Pyroglutamylated RFamide peptide receptor Inhibitors (IC50, Ki). AAT Bioquest. https://www.aatbio.com/data-sets/pyroglutamylated-rfamide-peptide-receptor-inhibitors-ic50-ki.
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