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Glucose-dependent insulinotropic receptor Inhibitors (IC50, Ki)

Structure
Compound Name
Standard Type
Standard Values (in nM)
Isopropyl 4-(5-methyl-6-(2-methylpyridin-3-yloxy)pyrimidin-4-yloxy)piperidine-1-carboxylateKi23.0 [1]
4-[[2-[(2R)-2-Methyl-4-(5-propan-2-yl-1,2,4-oxadiazol-3-yl)piperazin-1-yl]pyrimidin-5-yl]oxymethyl]pyridine-3-carbonitrileIC503.0 [1]
Propan-2-yl 4-[6-(2-fluoro-4-methylsulfonylphenoxy)-5-methylpyrimidin-4-yl]oxypiperidine-1-carboxylateKi53.0 [1]
Tert-butyl 4-(5-(4-(methylsulfonyl)-benzyloxy)pyrimidin-2-yl)piperazine-1-carboxylateIC50351.0 [1]
(R)-Tert-butyl 3-methyl-4-(5-(4-(methylsulfonyl)benzyloxy)pyrimidin-2-yl)piperazine-1-carboxylateIC5017.0 [1]
Tert-butyl 4-(5-((3-cyanopyridin-4-yl)methoxy)pyrimidin-2-yl)piperazine-1-carboxylateIC5010.0 [1]
Tert-butyl (3R)-4-[5-[(3-cyanopyridin-4-yl)methoxy]pyrimidin-2-yl]-3-methylpiperazine-1-carboxylateIC501.0 [1]
2,2,2-Trifluoroethyl (3R)-4-[5-[(3-cyanopyridin-4-yl)methoxy]pyrimidin-2-yl]-3-methylpiperazine-1-carboxylateIC5031.0 [1]
Propan-2-yl 8-[5-methyl-6-(2-methylpyridin-3-yl)oxypyrimidin-4-yl]oxy-6-oxa-3-azabicyclo[3.2.1]octane-3-carboxylateKi1599.0 [1]
Propan-2-yl 9-[5-methyl-6-(2-methylpyridin-3-yl)oxypyrimidin-4-yl]oxy-3-oxa-7-azabicyclo[3.3.1]nonane-7-carboxylateKi20.0 [1]
Ethyl 1-(6-(4-bromophenoxy)-5-nitropyrimidin-4-yl)piperidine-4-carboxylateIC5050.0 [1]
Ethyl 1-[6-[4-(2-methoxyethoxy)phenoxy]-5-nitropyrimidin-4-yl]piperidine-4-carboxylateIC50500.0 [1]
Ethyl 1-[6-[2-methyl-5-(trifluoromethyl)pyrazol-3-yl]oxy-5-nitropyrimidin-4-yl]piperidine-4-carboxylateIC5084.0 [1]
Propan-2-yl (1S,5R)-9-[5-methyl-6-(2-methylpyridin-3-yl)oxypyrimidin-4-yl]oxy-3-oxa-7-azabicyclo[3.3.1]nonane-7-carboxylateKi20.0 [1]
4-((2-(4-(5-Isopropyl-1,2,4-oxadiazol-3-yl)piperazin-1-yl)pyrimidin-5-yloxy)methyl)nicotinonitrileIC5012.0 [1]
2,2,2-Trifluoroethyl 4-[5-[(3-cyanopyridin-4-yl)methoxy]pyrimidin-2-yl]piperazine-1-carboxylateIC5018.0 [1]
Propan-2-yl (1R,5R,8R)-8-[5-methyl-6-(2-methylpyridin-3-yl)oxypyrimidin-4-yl]oxy-6-oxa-3-azabicyclo[3.2.1]octane-3-carboxylateKi1176.0 [1]
Propan-2-yl (1S,5S,8S)-8-[5-methyl-6-(2-methylpyridin-3-yl)oxypyrimidin-4-yl]oxy-6-oxa-3-azabicyclo[3.2.1]octane-3-carboxylateKi2270.0 [1]
(1-Methylcyclopropyl) 4-[5-cyano-4-[[2-fluoro-4-(1-methyltetrazol-5-yl)phenoxy]methyl]pyrazol-1-yl]piperidine-1-carboxylateKi99.0 [1]
(1-Methylcyclopropyl) 4-[5-cyano-4-[(4-cyano-2-fluorophenoxy)methyl]pyrazol-1-yl]piperidine-1-carboxylateKi36.5 [1]
(1-Methylcyclopropyl) 4-[5-cyano-4-[[4-(tetrazol-1-yl)phenoxy]methyl]pyrazol-1-yl]piperidine-1-carboxylateKi29.8 [1]
4-[(4-Cyano-2-fluorophenoxy)methyl]-2-[1-(5-ethylpyrimidin-2-yl)piperidin-4-yl]pyrazole-3-carbonitrileKi9.25 [1]
2-[1-(5-Ethylpyrimidin-2-yl)piperidin-4-yl]-4-[[4-(tetrazol-1-yl)phenoxy]methyl]pyrazole-3-carbonitrileKi14.9 [1]
Propan-2-yl 6-[5-methyl-6-(2-methylpyridin-3-yl)oxypyrimidin-4-yl]-2,6-diazatricyclo[3.3.1.13,7]decane-2-carboxylateKi2233.0 [1]
Ethyl 6-[5-methyl-6-(2-methylpyridin-3-yl)oxypyrimidin-4-yl]-2,6-diazatricyclo[3.3.1.13,7]decane-2-carboxylateKi1970.0 [1]
(1-Methylcyclopropyl) 6-[5-methyl-6-(2-methylpyridin-3-yl)oxypyrimidin-4-yl]-2,6-diazatricyclo[3.3.1.13,7]decane-2-carboxylateKi586.0 [1]
Cyclobutyl 6-[5-methyl-6-(2-methylpyridin-3-yl)oxypyrimidin-4-yl]-2,6-diazatricyclo[3.3.1.13,7]decane-2-carboxylateKi682.0 [1]
Tert-butyl 6-[5-methyl-6-(2-methylpyridin-3-yl)oxypyrimidin-4-yl]-2,6-diazatricyclo[3.3.1.13,7]decane-2-carboxylateKi486.0 [1]
2-Methylpropyl 6-[5-methyl-6-(2-methylpyridin-3-yl)oxypyrimidin-4-yl]-2,6-diazatricyclo[3.3.1.13,7]decane-2-carboxylateKi231.0 [1]
[(2R)-Butan-2-yl] 6-[5-methyl-6-(2-methylpyridin-3-yl)oxypyrimidin-4-yl]-2,6-diazatricyclo[3.3.1.13,7]decane-2-carboxylateKi290.0 [1]
[(2S)-Butan-2-yl] 6-[5-methyl-6-(2-methylpyridin-3-yl)oxypyrimidin-4-yl]-2,6-diazatricyclo[3.3.1.13,7]decane-2-carboxylateKi493.0 [1]
(1-Methylcyclobutyl) 6-[5-methyl-6-(2-methylpyridin-3-yl)oxypyrimidin-4-yl]-2,6-diazatricyclo[3.3.1.13,7]decane-2-carboxylateKi136.0 [1]
Tert-butyl 6-[6-(2-fluoro-4-methylsulfonylphenoxy)-5-methylpyrimidin-4-yl]-2,6-diazatricyclo[3.3.1.13,7]decane-2-carboxylateKi41.0 [1]
Propan-2-yl 6-[6-(2-fluoro-4-methylsulfonylphenoxy)-5-methylpyrimidin-4-yl]-2,6-diazatricyclo[3.3.1.13,7]decane-2-carboxylateKi141.0 [1]
(1-Methylcyclopropyl) 6-[6-(2-fluoro-4-methylsulfonylphenoxy)-5-methylpyrimidin-4-yl]-2,6-diazatricyclo[3.3.1.13,7]decane-2-carboxylateKi131.0 [1]
(1-Methylcyclopropyl) 6-[6-(2-methylpyridin-3-yl)oxypyrimidin-4-yl]-2,6-diazatricyclo[3.3.1.13,7]decane-2-carboxylateKi8148.0 [1]
Tert-butyl 6-[6-(2-methylpyridin-3-yl)oxypyrimidin-4-yl]-2,6-diazatricyclo[3.3.1.13,7]decane-2-carboxylateKi8148.0 [1]
Propan-2-yl 6-[5-ethyl-6-(2-methylpyridin-3-yl)oxypyrimidin-4-yl]-2,6-diazatricyclo[3.3.1.13,7]decane-2-carboxylateKi197.0 [1]
(1-Methylcyclopropyl) 6-[5-ethyl-6-(2-methylpyridin-3-yl)oxypyrimidin-4-yl]-2,6-diazatricyclo[3.3.1.13,7]decane-2-carboxylateKi123.0 [1]
Tert-butyl 6-[5-ethyl-6-(2-methylpyridin-3-yl)oxypyrimidin-4-yl]-2,6-diazatricyclo[3.3.1.13,7]decane-2-carboxylateKi18.0 [1]
(1-Methylcyclopropyl) 6-[5-fluoro-6-(2-methylpyridin-3-yl)oxypyrimidin-4-yl]-2,6-diazatricyclo[3.3.1.13,7]decane-2-carboxylateKi7318.0 [1]
Tert-butyl 6-[5-fluoro-6-(2-methylpyridin-3-yl)oxypyrimidin-4-yl]-2,6-diazatricyclo[3.3.1.13,7]decane-2-carboxylateKi814.0 [1]
Propan-2-yl 6-[5-methoxy-6-(2-methylpyridin-3-yl)oxypyrimidin-4-yl]-2,6-diazatricyclo[3.3.1.13,7]decane-2-carboxylateKi1496.0 [1]
(1-Methylcyclopropyl) 6-[5-methoxy-6-(2-methylpyridin-3-yl)oxypyrimidin-4-yl]-2,6-diazatricyclo[3.3.1.13,7]decane-2-carboxylateKi3123.0 [1]
Tert-butyl 6-[5-methoxy-6-(2-methylpyridin-3-yl)oxypyrimidin-4-yl]-2,6-diazatricyclo[3.3.1.13,7]decane-2-carboxylateKi163.0 [1]
Propan-2-yl 6-[6-(4-cyano-2-fluorophenoxy)-5-methylpyrimidin-4-yl]-2,6-diazatricyclo[3.3.1.13,7]decane-2-carboxylateKi912.0 [1]
Tert-butyl 6-[6-(4-cyano-2-fluorophenoxy)-5-methylpyrimidin-4-yl]-2,6-diazatricyclo[3.3.1.13,7]decane-2-carboxylateKi133.0 [1]
Propan-2-yl 6-[5-methyl-6-[4-(triazol-1-yl)phenoxy]pyrimidin-4-yl]-2,6-diazatricyclo[3.3.1.13,7]decane-2-carboxylateKi294.0 [1]
Propan-2-yl 6-[5-methyl-6-[4-(tetrazol-1-yl)phenoxy]pyrimidin-4-yl]-2,6-diazatricyclo[3.3.1.13,7]decane-2-carboxylateKi94.0 [1]
(1-Methylcyclopropyl) 6-[5-methyl-6-[4-(tetrazol-1-yl)phenoxy]pyrimidin-4-yl]-2,6-diazatricyclo[3.3.1.13,7]decane-2-carboxylateKi48.0 [1]
Tert-butyl 6-[5-methyl-6-[4-(tetrazol-1-yl)phenoxy]pyrimidin-4-yl]-2,6-diazatricyclo[3.3.1.13,7]decane-2-carboxylateKi21.0 [1]
Propan-2-yl 6-[6-[2-fluoro-4-(tetrazol-1-yl)phenoxy]-5-methylpyrimidin-4-yl]-2,6-diazatricyclo[3.3.1.13,7]decane-2-carboxylateKi18.0 [1]
(1-Methylcyclopropyl) 6-[6-[2-fluoro-4-(tetrazol-1-yl)phenoxy]-5-methylpyrimidin-4-yl]-2,6-diazatricyclo[3.3.1.13,7]decane-2-carboxylateKi15.0 [1]
Tert-butyl 6-[6-[2-fluoro-4-(tetrazol-1-yl)phenoxy]-5-methylpyrimidin-4-yl]-2,6-diazatricyclo[3.3.1.13,7]decane-2-carboxylateKi7.0 [1]
Propan-2-yl 6-[6-[4-(dimethylcarbamoyl)-2-fluorophenoxy]-5-methylpyrimidin-4-yl]-2,6-diazatricyclo[3.3.1.13,7]decane-2-carboxylateKi1148.0 [1]
Tert-butyl 6-[6-[2-fluoro-4-(1,2,4-triazol-1-yl)phenoxy]-5-methylpyrimidin-4-yl]-2,6-diazatricyclo[3.3.1.13,7]decane-2-carboxylateKi33.0 [1]
Tert-butyl 6-[5-methyl-6-[4-(1,2,4-triazol-1-yl)phenoxy]pyrimidin-4-yl]-2,6-diazatricyclo[3.3.1.13,7]decane-2-carboxylateKi125.0 [1]
Tert-butyl 6-[6-[2-fluoro-4-(3-methyl-1,2,4-triazol-1-yl)phenoxy]-5-methylpyrimidin-4-yl]-2,6-diazatricyclo[3.3.1.13,7]decane-2-carboxylateKi507.0 [1]
Tert-butyl 6-[5-methyl-6-[4-(3-methyl-1,2,4-triazol-1-yl)phenoxy]pyrimidin-4-yl]-2,6-diazatricyclo[3.3.1.13,7]decane-2-carboxylateKi948.0 [1]
(2,2,3,3-Tetrafluorocyclobutyl) 4-[5-[(3-cyanopyridin-4-yl)methoxy]pyrimidin-2-yl]piperazine-1-carboxylateIC5025.0 [1]
(2,2,3,3-Tetrafluorocyclobutyl) 3-[5-[(3-cyanopyridin-4-yl)methoxy]pyrimidin-2-yl]-3,8-diazabicyclo[3.2.1]octane-8-carboxylateIC509.0 [1]
Tert-butyl 3-[5-[(3-cyanopyridin-4-yl)methoxy]pyrimidin-2-yl]-3,8-diazabicyclo[3.2.1]octane-8-carboxylateIC501.0 [1]
4-[[2-[8-(5-Propan-2-yl-1,2,4-oxadiazol-3-yl)-3,8-diazabicyclo[3.2.1]octan-3-yl]pyrimidin-5-yl]oxymethyl]pyridine-3-carbonitrileIC504.0 [1]
(2,2,3,3-Tetrafluorocyclobutyl) (3R)-4-[5-[(3-cyanopyridin-4-yl)methoxy]pyrimidin-2-yl]-3-methylpiperazine-1-carboxylateIC506.0 [1]
2,2,2-Trifluoroethyl 3-[5-[(3-cyanopyridin-4-yl)methoxy]pyrimidin-2-yl]-3,8-diazabicyclo[3.2.1]octane-8-carboxylateIC508.0 [1]
Tert-butyl 8-[5-[(4-methylsulfonylphenyl)methoxy]pyrimidin-2-yl]-3,8-diazabicyclo[3.2.1]octane-3-carboxylateIC5092.0 [1]
Tert-butyl 3-[5-[(4-methylsulfonylphenyl)methoxy]pyrimidin-2-yl]-3,8-diazabicyclo[3.2.1]octane-8-carboxylateIC503.0 [1]



References

This online tool may be cited as follows

MLA

"Quest Database™ Glucose-dependent insulinotropic receptor Inhibitors (IC50, Ki)." AAT Bioquest, Inc.20 Dec2024https://www.aatbio.com/data-sets/glucose-dependent-insulinotropic-receptor-inhibitors-ic50-ki.

APA

AAT Bioquest, Inc. (2024December 20). Quest Database™ Glucose-dependent insulinotropic receptor Inhibitors (IC50, Ki). AAT Bioquest. https://www.aatbio.com/data-sets/glucose-dependent-insulinotropic-receptor-inhibitors-ic50-ki.
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