3.1.4.39 0.0000061 - cyclohexanaminium hydrogen [[4-(decanoylamino)phenyl](fluoro)methyl]phosphonate pH and temperature not specified in the publication 714443 3.1.4.39 0.000009 - cyclohexanaminium hydrogen [4-(tetradecanoylamino)benzyl]phosphonate pH and temperature not specified in the publication 714443 3.1.4.39 0.00001 - PF8380 pH and temperature not specified in the publication 729701 3.1.4.39 0.000018 - cyclohexanaminium hydrogen [4-(decanoylamino)benzyl]phosphonate pH and temperature not specified in the publication 714443 3.1.4.39 0.000024 - cyclohexanaminium hydrogen [[4-(decanoylamino)phenyl](hydroxy)methyl]phosphonate pH and temperature not specified in the publication 714443 3.1.4.39 0.0000242 - cyclohexanaminium hydrogen [[4-(decanoylamino)phenyl](hydroxy)methyl]phosphonate pH and temperature not specified in the publication 714443 3.1.4.39 0.000072 - cyclohexanaminium hydrogen [[4-(decanoylamino)phenyl](fluoro)methyl]phosphonate pH and temperature not specified in the publication 714443 3.1.4.39 0.0001 - 1-acyl glycerol 3-phosphate CPF4 FRET assay (change of fluorescence intensity), inihibition involves both a reduction in vmax and an increase in km, binding affinity is 1000fold stronger than to 1-alkyl-sn-glycero-3-phosphoethanolamine and analogue substrates 697490 3.1.4.39 0.00011 - lysophosphatidic acid - 665628 3.1.4.39 0.0002 - 2-amino-2-(2-(4-octylphenyl) ethyl)propan-1,3-diol substrate p-nitrophenyl thymidine 5-monophosphate, pH 8.0, 30 min of incubation at 37°C, measuring absorbance at 405 nm, twofold higher KI compared to inhibitor S1P 697080 3.1.4.39 0.00021 - 1-linoleoyl-lysophosphatidic acid most potent in the inhibition of lysoPLD activity, based on fluoresecent assay, same order of inhibitory potency among lysophosphatidic acid analogs with different acyl chains in the spectrophotometric assay 680318 3.1.4.39 0.00021 - sphingosine-1-phosphate SIP, inhibition of lysoPLD activity, fluorometric assay 680318 3.1.4.39 0.000512 - cyclohexanaminium hydrogen [4-(heptanoylamino)benzyl]phosphonate pH and temperature not specified in the publication 714443 3.1.4.39 0.00055 - 1-arachidonoyl-lysophosphatidic acid inhibition of lysoPLD activity, based on fluoresecent assay, same order of inhibitory potency among lysophosphatidic acid analogs with different acyl chains in the spectrophotometric assay 680318 3.1.4.39 0.0007 - 2-(4-[[(3-trifluoromethylphenyl)amino]carbonothioyl]-1-piperazinyl)-8-ethyl-5-oxo-5,8-dihydropyrido[2,3-d]pyrimidine-6-carboxylic acid 1 mM each CaCl2 and MgCl2, 5 mM KCl, and 140 mM NaCl, in 50 mM Tris, pH 8.0, at 37°C 705057 3.1.4.39 0.000834 - cyclohexanaminium hydrogen [fluoro[4-(heptanoylamino)phenyl]methyl]phosphonate pH and temperature not specified in the publication 714443 3.1.4.39 0.001 - [(2R,3S)-3-(hexadecanoylamino)-2-hydroxy-4-[4-[(4-methoxy-3,5-dimethylpyridin-2-yl)methoxy]phenyl]butyl]phosphonic acid syn configuration, pH and temperature not specified in the publication 714422 3.1.4.39 0.001009 - cyclohexanaminium hydrogen [[4-(heptanoylamino)phenyl](hydroxy)methyl]phosphonate pH and temperature not specified in the publication 714443 3.1.4.39 0.0012 - 1-oleoyl-lysophosphatidic acid inhibition of lysoPLD activity, based on fluoresecent assay, same order of inhibitory potency among lysophosphatidic acid analogs with different acyl chains in the spectrophotometric assay 680318 3.1.4.39 0.00141 - 1-palmitoyl-lysophosphatidic acid inhibition of lysoPLD activity,size of acyl chain is crucial for the maximal inhibitory action, fluorometric assay 680318 3.1.4.39 0.0015 - [(2R,3S)-4-[4-[(3,5-dimethyl-4-propoxypyridin-2-yl)methoxy]phenyl]-3-(hexadecanoylamino)-2-hydroxybutyl]phosphonic acid syn configuration, pH and temperature not specified in the publication 714422 3.1.4.39 0.0016 - [(2R,3S)-4-(4-[[3,5-dimethyl-4-(2,2,2-trifluoroethoxy)pyridin-2-yl]methoxy]phenyl)-3-(hexadecanoylamino)-2-hydroxybutyl]phosphonic acid syn configuration, pH and temperature not specified in the publication 714422 3.1.4.39 0.0018 - 1-linoleoyl-lysophosphatidic acid competitive inhibition, spectrophotometric assay 680318 3.1.4.39 0.0018 - sphingosine-1-phosphate SIP, inhibition of lysoPLD activity, spectrophotometric assay 680318 3.1.4.39 0.0019 - H2L 7905958 1 mM each CaCl2 and MgCl2, 5 mM KCl, and 140 mM NaCl, in 50 mM Tris, pH 8.0, at 37°C 705057 3.1.4.39 0.0019 - H2L 7905958 with respect to ATX-mediated FS-3 hydrolysis 702693 3.1.4.39 0.002 - H2L 5761473 with respect to ATX-mediated FS-3 hydrolysis 702693 3.1.4.39 0.00209 - 1-stearoyl-lysophosphatidic acid inhibition of lysoPLD activity,size of acyl chain is crucial for the maximal inhibitory action, fluorometric assay 680318 3.1.4.39 0.0026 - 2-(4-[[(3-chlorophenyl)amino]carbonothioyl]-1-piperazinyl)-8-ethyl-5-oxo-5,8-dihydropyrido[2,3-d]pyrimidine-6-carboxylic acid 1 mM each CaCl2 and MgCl2, 5 mM KCl, and 140 mM NaCl, in 50 mM Tris, pH 8.0, at 37°C 705057 3.1.4.39 0.0027 - H2L 7839888 with respect to ATX-mediated FS-3 hydrolysis 702693 3.1.4.39 0.0034 - 1-arachidonoyl-lysophosphatidic acid inhibition of lysoPLD activity, spectrophotometric assay 680318 3.1.4.39 0.0034 - 2-(4-[[(2,5-dichlorophenyl)amino]carbonothioyl]-1-piperazinyl)-8-ethyl-5-oxo-5,8-dihydropyrido[2,3-d]pyrimidine-6-carboxylic acid 1 mM each CaCl2 and MgCl2, 5 mM KCl, and 140 mM NaCl, in 50 mM Tris, pH 8.0, at 37°C 705057 3.1.4.39 0.0035 - [(2R,3S)-4-(4-[[3,5-dimethyl-4-(2,2,2-trifluoroethoxy)pyridin-2-yl]methoxy]phenyl)-3-(hexadecanoylamino)-2-hydroxybutyl]phosphonic acid anti configuration, pH and temperature not specified in the publication 714422 3.1.4.39 0.0039 - [(2R,3S)-4-[4-(benzyloxy)phenyl]-3-(hexadecanoylamino)-2-hydroxybutyl]phosphonic acid anti configuration, pH and temperature not specified in the publication 714422 3.1.4.39 0.004 - 2-(4-[[(3,5-bis(trifluoromethyl)phenyl)amino]carbonothioyl]-1-piperazinyl)-8-ethyl-5-oxo-5,8-dihydropyrido[2,3-d]pyrimidine-6-carboxylic acid 1 mM each CaCl2 and MgCl2, 5 mM KCl, and 140 mM NaCl, in 50 mM Tris, pH 8.0, at 37°C 705057 3.1.4.39 0.0042 - 2-(4-[[(3,5-dimethylphenyl)amino]carbonothioyl]-1-piperazinyl)-8-ethyl-5-oxo-5,8-dihydropyrido[2,3-d]pyrimidine-6-carboxylic acid 1 mM each CaCl2 and MgCl2, 5 mM KCl, and 140 mM NaCl, in 50 mM Tris, pH 8.0, at 37°C 705057 3.1.4.39 0.0043 - [(2R,3S)-4-[4-[(3,5-dimethylbenzyl)oxy]phenyl]-3-(hexadecanoylamino)-2-hydroxybutyl]phosphonic acid syn configuration, pH and temperature not specified in the publication 714422 3.1.4.39 0.0044 - [(2R,3S)-4-[4-[(3,5-dimethylpyridin-2-yl)methoxy]phenyl]-3-(hexadecanoylamino)-2-hydroxybutyl]phosphonic acid syn configuration, pH and temperature not specified in the publication 714422 3.1.4.39 0.0045 - 2-(4-[[(3-methylphenyl)amino]carbonothioyl]-1-piperazinyl)-8-ethyl-5-oxo-5,8-dihydropyrido[2,3-d]pyrimidine-6-carboxylic acid 1 mM each CaCl2 and MgCl2, 5 mM KCl, and 140 mM NaCl, in 50 mM Tris, pH 8.0, at 37°C 705057 3.1.4.39 0.0047 - [(2R,3S)-3-(hexadecanoylamino)-2-hydroxy-4-[4-[(4-methoxy-3,5-dimethylbenzyl)oxy]phenyl]butyl]phosphonic acid syn configuration, pH and temperature not specified in the publication 714422 3.1.4.39 0.005 - 1-myristoyl-lysophosphatidic acid most potent in inhibiting lysoPLD activity, spectrophotometric assay 680318 3.1.4.39 0.0057 - 2-(4-[[(4-chlorophenyl)amino]carbonothioyl]-1-piperazinyl)-8-ethyl-5-oxo-5,8-dihydropyrido[2,3-d]pyrimidine-6-carboxylic acid 1 mM each CaCl2 and MgCl2, 5 mM KCl, and 140 mM NaCl, in 50 mM Tris, pH 8.0, at 37°C 705057 3.1.4.39 0.0062 - [(2R,3S)-4-[4-[(3,5-dimethylbenzyl)oxy]phenyl]-3-(hexadecanoylamino)-2-hydroxybutyl]phosphonic acid anti configuration, pH and temperature not specified in the publication 714422 3.1.4.39 0.0065 - 1-myristoyl-lysophosphatidic acid most potent in inhibiting lysoPLD activity, fluorometric assay 680318 3.1.4.39 0.0065 - H2L 7905958 with respect to ATX-mediated 4-nitrophenyl-TMP hydrolysis 702693 3.1.4.39 0.0071 - 2-(4-[[(3-benzothiadiazolphenyl)amino]carbonothioyl]-1-piperazinyl)-8-ethyl-5-oxo-5,8-dihydropyrido[2,3-d]pyrimidine-6-carboxylic acid 1 mM each CaCl2 and MgCl2, 5 mM KCl, and 140 mM NaCl, in 50 mM Tris, pH 8.0, at 37°C 705057 3.1.4.39 0.0074 - 2-(4-[[(3-iodophenyl)amino]carbonothioyl]-1-piperazinyl)-8-ethyl-5-oxo-5,8-dihydropyrido[2,3-d]pyrimidine-6-carboxylic acid 1 mM each CaCl2 and MgCl2, 5 mM KCl, and 140 mM NaCl, in 50 mM Tris, pH 8.0, at 37°C 705057 3.1.4.39 0.0088 - [(2R,3S)-3-(hexadecanoylamino)-2-hydroxy-4-[4-[(4-methoxy-3-methylbenzyl)oxy]phenyl]butyl]phosphonic acid syn configuration, pH and temperature not specified in the publication 714422 3.1.4.39 0.0093 - H2L 7921385 with respect to ATX-mediated FS-3 hydrolysis 702693 3.1.4.39 0.0096 - 1-oleoyl-lysophosphatidic acid inhibition of lysoPLD activity, spectrophotometric assay 680318 3.1.4.39 0.01031 - 1-arachidoyl-lysophosphatidic acid inhibition of lysoPLD activity, fluorometric assay 680318 3.1.4.39 0.0104 - 1-palmitoyl-lysophosphatidic acid inhibition of lysoPLD activity,size of acyl chain is crucial for the maximal inhibitory action, spectrophotometric assay 680318 3.1.4.39 0.011 - [(2R,3S)-4-[4-[(4-ethoxy-3,5-dimethylpyridin-2-yl)methoxy]phenyl]-3-(hexadecanoylamino)-2-hydroxybutyl]phosphonic acid anti configuration, pH and temperature not specified in the publication 714422 3.1.4.39 0.0111 - [(2R,3S)-3-(hexadecanoylamino)-2-hydroxy-4-[4-[(4-methoxy-3,5-dimethylpyridin-2-yl)methoxy]phenyl]butyl]phosphonic acid anti configuration, pH and temperature not specified in the publication 714422 3.1.4.39 0.0116 - [(2R,3S)-4-[4-(benzyloxy)phenyl]-3-(hexadecanoylamino)-2-hydroxybutyl]phosphonic acid syn configuration, pH and temperature not specified in the publication 714422 3.1.4.39 0.01299 - 1-hexanoyl-lysophosphatidic acid inhibition of lysoPLD activity, fluorometric assay 680318 3.1.4.39 0.0132 - 2-(4-[[(4-iodophenyl)amino]carbonothioyl]-1-piperazinyl)-8-ethyl-5-oxo-5,8-dihydropyrido[2,3-d]pyrimidine-6-carboxylic acid 1 mM each CaCl2 and MgCl2, 5 mM KCl, and 140 mM NaCl, in 50 mM Tris, pH 8.0, at 37°C 705057 3.1.4.39 0.0132 - 2-(4-[[(4-trifluoromethylphenyl)amino]carbonothioyl]-1-piperazinyl)-8-ethyl-5-oxo-5,8-dihydropyrido[2,3-d]pyrimidine-6-carboxylic acid 1 mM each CaCl2 and MgCl2, 5 mM KCl, and 140 mM NaCl, in 50 mM Tris, pH 8.0, at 37°C 705057 3.1.4.39 0.0151 - H2L 5564949 with respect to ATX-mediated FS-3 hydrolysis 702693 3.1.4.39 0.0225 - [(2R,3S)-3-(hexadecanoylamino)-2-hydroxy-4-[4-(pyridin-2-ylmethoxy)phenyl]butyl]phosphonic acid anti configuration, pH and temperature not specified in the publication 714422 3.1.4.39 0.0258 - 1-stearoyl-lysophosphatidic acid inhibition of lysoPLD activity,size of acyl chain is crucial for the maximal inhibitory action, spectrophotometric assay 680318 3.1.4.39 0.0265 - [(2R,3S)-3-(hexadecanoylamino)-2-hydroxy-4-[4-[(4-methoxy-3-methylbenzyl)oxy]phenyl]butyl]phosphonic acid anti configuration, pH and temperature not specified in the publication 714422 3.1.4.39 0.027 - [(2R,3S)-3-(hexadecanoylamino)-2-hydroxy-4-[4-(pyridin-2-ylmethoxy)phenyl]butyl]phosphonic acid syn configuration, pH and temperature not specified in the publication 714422 3.1.4.39 0.06 - 1-arachidoyl-lysophosphatidic acid > 60 microM, inhibition of lysoPLD activity, spectrophotometric assay 680318 3.1.4.39 0.06 - 1-hexanoyl-lysophosphatidic acid inhibition of lysoPLD activity, > 60 microM, size of acyl chain is crucial for the maximal inhibitory action, spectrophotometric assay 680318 3.1.4.39 0.083 - [(2R,3S)-3-(hexadecanoylamino)-2-hydroxy-4-[4-[(4-methoxypyridin-2-yl)methoxy]phenyl]butyl]phosphonic acid anti configuration, pH and temperature not specified in the publication 714422 3.1.4.39 0.0889 - [(2R,3S)-4-[4-[(2,4-dichlorobenzyl)oxy]phenyl]-3-(hexadecanoylamino)-2-hydroxybutyl]phosphonic acid syn configuration, pH and temperature not specified in the publication 714422 3.1.4.39 0.2175 - [(2R,3S)-3-(hexadecanoylamino)-2-hydroxy-4-[4-[(4-methoxy-3,5-dimethylbenzyl)oxy]phenyl]butyl]phosphonic acid anti configuration, pH and temperature not specified in the publication 714422 3.1.4.39 0.399 - [(2R,3S)-4-[4-[(2,4-dichlorobenzyl)oxy]phenyl]-3-(hexadecanoylamino)-2-hydroxybutyl]phosphonic acid anti configuration, pH and temperature not specified in the publication 714422 3.1.4.39 0.5841 - [(2R,3S)-4-[4-[(4-ethoxy-3,5-dimethylpyridin-2-yl)methoxy]phenyl]-3-(hexadecanoylamino)-2-hydroxybutyl]phosphonic acid syn configuration, pH and temperature not specified in the publication 714422 3.1.4.39 1.059 - [(2R,3S)-4-[4-[(3,5-dimethyl-4-propoxypyridin-2-yl)methoxy]phenyl]-3-(hexadecanoylamino)-2-hydroxybutyl]phosphonic acid anti configuration, pH and temperature not specified in the publication 714422