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Phosphodiesterase 4A Inhibitors (IC50, Ki)

Structure
Compound Name
Standard Type
Standard Values (in nM)
RolipramIC50162.0 [1]
RolipramKi7940.0 [1]
4-(2-(3-(Cyclopentyloxy)-4-methoxyphenyl)-2-phenylethyl)pyridineIC504.2 [1]
4-(2-(3-(Cyclopentyloxy)-4-methoxyphenyl)-2-phenylethyl)pyridineKi4.0 [1]
CilomilastIC50150.0 [1]
Unii-G6gso9sdnjIC501.0 [1], 1.4 [2]
2-[5-[(1S)-1-[3-Cyclopropyloxy-4-(difluoromethoxy)phenyl]-2-(1-oxidopyridin-1-ium-3-yl)ethyl]-1,3-thiazol-2-yl]-1,1,1,3,3,3-hexafluoropropan-2-olIC500.4 [1], 0.5 [2]
2-[5-[(1S)-1-[3-Cyclopropyloxy-4-(difluoromethoxy)phenyl]-2-(1-oxidopyridin-1-ium-3-yl)ethyl]-1,3-thiazol-2-yl]-1,1,1,3,3,3-hexafluoropropan-2-olKi0.43 [1]
2-[4-[1-[3,4-Bis(difluoromethoxy)phenyl]-2-(1-oxidopyridin-1-ium-4-yl)ethyl]phenyl]-1,1,1,3,3,3-hexafluoropropan-2-olIC504.2 [1], 670.0 [2]
4-[8-(2,1,3-Benzoxadiazol-5-yl)-1,7-naphthyridin-6-yl]benzoic acidIC50290.0 [1], 602.0 [2]
(R)-(-)-RolipramIC50162.0 [1], 550.0 [2], 4000.0 [3]
2-[4-[1-[3,4-Bis(difluoromethoxy)phenyl]-2-(3-methyl-1-oxidopyridin-1-ium-4-yl)ethyl]phenyl]-1,1,1,3,3,3-hexafluoropropan-2-olIC501.3 [1], 23.0 [2]
4-[8-(3-Nitrophenyl)-1,7-naphthyridin-6-yl]benzoic AcidIC5029.0 [1], 88.0 [2]
RoflumilastIC500.35 [1], 0.59 [2]
IbudilastIC5054.0 [1], 1300.0 [2]
PiclamilastIC501.6 [1], 4.0 [2]
Unii-K4kac9xccoIC505.1 [1], 6.7 [2]
2-Methoxy-6,7-dimethyl-9-propylimidazo[1,5-a]pyrido[3,2-e]pyrazineIC505000.0 [1]
4-Imino-7-methyl-5,6,7,8-tetrahydro[1]benzothieno[2,3-d]pyrimidin-3(4H)-amineIC50757000.0 [1], 1760000.0 [2]
8-(3-Methoxyphenyl)-6-(pyridin-4-ylmethyl)quinolineIC501.5 [1]
6-(3,4-Dimethoxyphenyl)-3-(2-methoxyphenyl)-7H-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazineIC5024.0 [1], 46.0 [2]
2-[5-[(1R)-1-[3-Cyclopropyloxy-4-(difluoromethoxy)phenyl]-2-(1-oxidopyridin-1-ium-3-yl)ethyl]-1,3-thiazol-2-yl]-1,1,1,3,3,3-hexafluoropropan-2-olIC5048.0 [1], 56.0 [2]
5,5-Dimethyl-3-(piperazin-1-ylmethyl)imidazolidine-2,4-dioneIC501380000.0 [1], 4269000.0 [2]
2-[5-[1-[3,4-Bis(difluoromethoxy)phenyl]-2-(1-oxidopyridin-1-ium-4-yl)ethyl]pyridin-2-yl]propan-2-olIC5040.0 [1], 520.0 [2]
1-[5-[1-[3,4-Bis(difluoromethoxy)phenyl]-2-(1-oxidopyridin-1-ium-4-yl)ethyl]pyridin-2-yl]-1-phenylethanolIC501.0 [1], 2.1 [2]
4-[8-(3-Fluorophenyl)-1,7-naphthyridin-6-yl]cyclohexane-1-carboxylic AcidIC50123.0 [1]
N-(3,4-Dimethoxyphenyl)-4-morpholin-4-yl-2-(trifluoromethyl)pyrimidine-5-carboxamideIC50100.0 [1], 678.0 [2]
4-(3,4-Dimethoxyphenyl)-N-pyridin-4-yl-2-(trifluoromethyl)pyrimidine-5-carboxamideIC5098.0 [1], 152.0 [2]
N-(3,5-Dichloropyridin-4-yl)-4-(3,4-dimethoxyphenyl)-2-(trifluoromethyl)pyrimidine-5-carboxamideIC5089.0 [1], 281.0 [2]
N-(3,4-Dimethoxyphenyl)-2-methylsulfanyl-4-morpholin-4-ylpyrimidine-5-carboxamideIC5045.0 [1], 756.0 [2]
4-[2-(4-Chlorophenyl)-2-[3-(cyclopentyloxy)-4-methoxyphenyl]ethyl]pyridineIC502.8 [1], 12000.0 [2]
4-[2-(4-Chlorophenyl)-2-[2-fluoro-4-methoxy-5-(cyclopentyloxy)phenyl]ethyl]pyridineIC5013.0 [1], 25000.0 [2]
4-[2-(4-Chlorophenyl)-2-[2-fluoro-3-(cyclopentyloxy)-4-methoxyphenyl]ethyl]pyridineIC50110.0 [1], 98000.0 [2]
4-[2-(4-Chlorophenyl)-2-[3,4-bis(difluoromethoxy)phenyl]ethyl]pyridineIC5011.0 [1], 4500.0 [2]
N-[4-[1-[3,4-Bis(difluoromethoxy)phenyl]-2-(1-oxidopyridin-1-ium-4-yl)ethyl]phenyl]sulfonyl-2-methylbenzamideIC503.1 [1], 75000.0 [2]
4-[2-(4-Carboxyphenyl)-2-[3,4-bis(difluoromethoxy)phenyl]ethyl]pyridine 1-oxideIC5024.0 [1], 77000.0 [2]
4-[2-[4-(1-Hydroxycyclopropyl)phenyl]-2-[3,4-bis(difluoromethoxy)phenyl]ethyl]pyridine 1-oxideIC5016.0 [1], 1700.0 [2]
4-[2-[4-(1-Hydroxycyclobutyl)phenyl]-2-[3,4-bis(difluoromethoxy)phenyl]ethyl]pyridine 1-oxideIC507.5 [1], 380.0 [2]
4-[2-[4-(1-Hydroxy-1-methylethyl)phenyl]-2-[3,4-bis(difluoromethoxy)phenyl]ethyl]pyridine 1-oxideIC509.6 [1], 360.0 [2]
4-[2-[4-(1-Hydroxyethyl)phenyl]-2-[3,4-bis(difluoromethoxy)phenyl]ethyl]pyridine 1-oxideIC5045.0 [1], 510.0 [2]
2-[3-[4-[1-[3,4-Bis(difluoromethoxy)phenyl]-2-(1-oxidopyridin-1-ium-4-yl)ethyl]phenyl]phenyl]-2-methylpropanoic acidIC502.2 [1], 6500.0 [2]
4-[2-[4-(Hydroxymethyl)phenyl]-2-[3,4-bis(difluoromethoxy)phenyl]ethyl]pyridine 1-oxideIC5044.0 [1], 470.0 [2]
4-[2-[4-(Dimethylaminocarbonyl)phenyl]-2-[3,4-bis(difluoromethoxy)phenyl]ethyl]pyridine 1-oxideIC508.6 [1], 1000.0 [2]
4-[2-[4-(2-Oxo-2-hydroxyethyl)phenyl]-2-[3,4-bis(difluoromethoxy)phenyl]ethyl]pyridine 1-oxideIC5053.0 [1], 58000.0 [2]
[4-[1-[3,4-Bis(difluoromethoxy)phenyl]-2-(1-oxidopyridin-1-ium-4-yl)ethyl]phenyl]methyl N-ethylcarbamateIC504.6 [1], 410.0 [2]
4-[2-[4-(4-Fluorophenoxymethyl)phenyl]-2-[3,4-bis(difluoromethoxy)phenyl]ethyl]pyridine 1-oxideIC500.5 [1], 1900.0 [2]
5-[1-(4-Chlorophenyl)-2-pyridin-4-ylethyl]-2,3-bis(difluoromethoxy)-1-oxidopyridin-1-iumIC5032.0 [1], 3800.0 [2]
4-[2-(4-Chlorophenyl)-2-[3-(cyclopentyloxy)-4-(difluoromethoxy)phenyl]ethyl]pyridineIC5013.0 [1], 8700.0 [2]
4-[2-[4-(5-Methyl-2-pyridylcarbonyl)phenyl]-2-[3,4-bis(difluoromethoxy)phenyl]ethyl]pyridine 1-oxideIC507.3 [1], 890.0 [2]
Acetic acid;2-[(Z)-1-(3,3-dimethylcyclohexen-1-yl)ethylideneamino]guanidineIC50790000.0 [1], 1460000.0 [2]
2-[4-[(3R)-3-Methyl-2-oxo-1,3-dihydroindol-5-yl]-1,3-thiazol-2-yl]guanidineIC501320000.0 [1], 2650000.0 [2]
SildenafilIC505000.0 [1]
ChlortetracyclineIC50100000.0 [1]
TadalafilIC5010000.0 [1]
ZaprinastKi50000.0 [1]
4-(3-Butoxy-4-methoxybenzyl)-2-imidazolidinoneIC504300.0 [1]
CrisaboroleIC5055.0 [1]
SibenadetIC5038.0 [1]
4,5-Dihydro-6-(4-(imidazol-1-yl)phenyl)-5-methyl-3(2H)-pyridazinoneKi50000.0 [1]
2-(Cyclopentyloxy)-4-[alpha-(4-pyridylmethyl)benzyl]anisoleIC5017.5 [1]
(S)-(+)-RolipramIC504300.0 [1]
(2S,3R)-3-(6-Amino-9H-purin-9-yl)nonan-2-olIC5016000.0 [1]
2,5-DiphenylfuranIC5010000.0 [1]
1-(3-Nitrophenyl)-3-(pyridin-4-ylmethyl)pyrido[2,3-d]pyrimidine-2,4(1H,3H)-dioneIC5022.0 [1]
(R)-5-(6-Cyclohexyl-1-(hydroxyamino)-1-oxohexan-3-yl)-1,2,4-oxadiazole-3-carboxamideIC501800.0 [1]
CipamfyllineIC501600.0 [1]
3-(2,5-Dimethoxyphenyl)-6-[4-methoxy-3-[(3R)-oxolan-3-yl]oxyphenyl]-[1,2,4]triazolo[4,3-b]pyridazineIC501.5 [1]
4-(4-((8-(3-(Difluoromethoxy)phenyl)quinolin-6-yl)methoxy)phenyl)-2-methylbutan-2-olIC5063.7 [1]
8-(3-Nitrophenyl)-6-(pyridin-4-ylmethyl)quinolineIC500.07 [1]
3-(2,5-Dimethoxyphenyl)-6-(3,4-dimethoxyphenyl)-7H-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazineIC506.7 [1]
3-[4-(2-Hydroxyethyl)piperazin-1-yl]-7-(6-methoxypyridin-3-yl)-1-(2-propoxyethyl)pyrido[3,4-b]pyrazin-2-oneIC502000.0 [1]
6-(3-Cyclopentyloxy-4-methoxyphenyl)-3-(2-methoxyphenyl)-7H-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazineIC5032.0 [1]
3-(2-Chlorophenyl)-6-(3-cyclopentyloxy-4-methoxyphenyl)-7H-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazineIC5026.0 [1]
CID 44142091IC5035.0 [1]
6-[4-Methoxy-3-(oxolan-3-yloxy)phenyl]-3-(2-methoxyphenyl)-7H-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazineIC5020.0 [1]
3-(2-Chlorophenyl)-6-[4-methoxy-3-(3-oxolanyloxy)phenyl]-7H-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazineIC509.8 [1]
6-[4-Methoxy-3-(oxolan-3-yloxy)phenyl]-3-[2-(trifluoromethyl)phenyl]-7H-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazineIC507.1 [1]
3-(2,5-Dimethoxyphenyl)-6-[4-methoxy-3-(oxolan-3-yloxy)phenyl]-7H-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazineIC503.4 [1]
N-Tert-Butyl-6-chloro-N'-methyl-[1,3,5]triazine-2,4-diamineIC50245.0 [1]
6-(3-Cyclopentyloxy-4-methoxyphenyl)-3-(2-fluorophenyl)-7H-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazineIC5033.0 [1]
CID 44142090IC5013.0 [1]
CID 44142093IC5021.0 [1]
Triazolothiadiazine, 7IC506.1 [1]
CID 44142095IC5035.0 [1]
CID 44142096IC5037.0 [1]
CID 44142097IC5053.0 [1]
CID 44142098IC5011.0 [1]
3-(2-Fluorophenyl)-6-[4-methoxy-3-(3-oxolanyloxy)phenyl]-7H-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazineIC5011.0 [1]
8-(3-Nitrophenyl)-6-(4-pyridylmethyl)pyrido(2,3-d)pyridazin-5-oneIC50340.0 [1]
4-(3,4-Dimethoxy-phenyl)-4a,5,8,8a-tetrahydro-2H-phthalazin-1-oneKi1000.0 [1]
ITI214 (free base)Ki62.0 [1]
TofimilastIC5023.0 [1]
N-[4-[5-(4-Fluorophenyl)-3-methyl-2-methylsulfinylimidazol-4-yl]pyridin-2-yl]acetamideIC502900.0 [1]
3-[(4-Hydroxycyclohexyl)amino]-7-(6-methoxypyridin-3-yl)-1-(2-propoxyethyl)pyrido[3,4-b]pyrazin-2-oneIC502000.0 [1]
7-(6-Methoxypyridin-3-yl)-3-(2-morpholin-4-ylethylamino)-1-(2-propoxyethyl)pyrido[3,4-b]pyrazin-2-oneIC502000.0 [1]
3-Phenyl-2-(propylthio)-6,7-dihydrothieno[3,2-d]pyrimidin-4(3H)-oneIC50100000.0 [1]
3-Phenyl-[1,3,5]triazino[2,1-b][1,3]benzothiazole-2,4-dioneIC50100000.0 [1]
4-[[1-(2-Chlorophenyl)-4-methyl-[1,2,4]triazolo[4,3-a]quinoxalin-8-yl]methyl]morpholineIC5010000.0 [1]
4-ChloroquinazolineIC50162.0 [1]
N-(3-(6-(Pyridin-4-ylmethyl)quinolin-8-yl)phenyl)benzenesulfonamideIC505.6 [1]



References

This online tool may be cited as follows

MLA

"Quest Database™ Phosphodiesterase 4A Inhibitors (IC50, Ki)." AAT Bioquest, Inc.9 May2024https://www.aatbio.com/data-sets/phosphodiesterase-4a-inhibitors-ic50-ki.

APA

AAT Bioquest, Inc. (2024May 9). Quest Database™ Phosphodiesterase 4A Inhibitors (IC50, Ki). AAT Bioquest. https://www.aatbio.com/data-sets/phosphodiesterase-4a-inhibitors-ic50-ki.
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