Inhibitors | Comment | Organism | Structure |
---|---|---|---|
2-(4-[[(2,3-dichlorophenyl)amino]carbonothioyl]-1-piperazinyl)-8-ethyl-5-oxo-5,8-dihydropyrido[2,3-d]pyrimidine-6-carboxylic acid | 72.3% residual activity at 0.001 mM using FS-3 as substrate | Homo sapiens | |
2-(4-[[(2,4,6-mesitylphenyl)amino]carbonothioyl]-1-piperazinyl)-8-ethyl-5-oxo-5,8-dihydropyrido[2,3-d]pyrimidine-6-carboxylic acid | 53.5% residual activity at 0.001 mM using FS-3 as substrate | Homo sapiens | |
2-(4-[[(2,5-dichlorophenyl)amino]carbonothioyl]-1-piperazinyl)-8-ethyl-5-oxo-5,8-dihydropyrido[2,3-d]pyrimidine-6-carboxylic acid | mixed inhibition, 5.4% residual activity at 0.001 mM using FS-3 as substrate | Homo sapiens | |
2-(4-[[(2-benzothiadiazolphenyl)amino]carbonothioyl]-1-piperazinyl)-8-ethyl-5-oxo-5,8-dihydropyrido[2,3-d]pyrimidine-6-carboxylic acid | 63.2% residual activity at 0.001 mM using FS-3 as substrate | Homo sapiens | |
2-(4-[[(2-chlorophenyl)amino]carbonothioyl]-1-piperazinyl)-8-ethyl-5-oxo-5,8-dihydropyrido[2,3-d]pyrimidine-6-carboxylic acid | 83.5% residual activity at 0.001 mM using FS-3 as substrate | Homo sapiens | |
2-(4-[[(2-fluorophenyl)amino]carbonothioyl]-1-piperazinyl)-8-ethyl-5-oxo-5,8-dihydropyrido[2,3-d]pyrimidine-6-carboxylic acid | 77.3% residual activity at 0.001 mM using FS-3 as substrate | Homo sapiens | |
2-(4-[[(2-iodophenyl)amino]carbonothioyl]-1-piperazinyl)-8-ethyl-5-oxo-5,8-dihydropyrido[2,3-d]pyrimidine-6-carboxylic acid | 68.4% residual activity at 0.001 mM using FS-3 as substrate | Homo sapiens | |
2-(4-[[(2-methoxyphenyl)amino]carbonothioyl]-1-piperazinyl)-8-ethyl-5-oxo-5,8-dihydropyrido[2,3-d]pyrimidine-6-carboxylic acid | 97.6% residual activity at 0.001 mM using FS-3 as substrate | Homo sapiens | |
2-(4-[[(2-methylesterphenyl)amino]carbonothioyl]-1-piperazinyl)-8-ethyl-5-oxo-5,8-dihydropyrido[2,3-d]pyrimidine-6-carboxylic acid | 51.2% residual activity at 0.001 mM using FS-3 as substrate | Homo sapiens | |
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 | competitive inhibition, 34.1% residual activity at 0.001 mM using FS-3 as substrate | Homo sapiens | |
2-(4-[[(3,5-dimethylphenyl)amino]carbonothioyl]-1-piperazinyl)-8-ethyl-5-oxo-5,8-dihydropyrido[2,3-d]pyrimidine-6-carboxylic acid | competitive inhibition, 30.4% residual activity at 0.001 mM using FS-3 as substrate | Homo sapiens | |
2-(4-[[(3-benzothiadiazolphenyl)amino]carbonothioyl]-1-piperazinyl)-8-ethyl-5-oxo-5,8-dihydropyrido[2,3-d]pyrimidine-6-carboxylic acid | competitive inhibition, 28.6% residual activity at 0.001 mM using FS-3 as substrate | Homo sapiens | |
2-(4-[[(3-chlorophenyl)amino]carbonothioyl]-1-piperazinyl)-8-ethyl-5-oxo-5,8-dihydropyrido[2,3-d]pyrimidine-6-carboxylic acid | mixed inhibition, 9.7% residual activity at 0.001 mM using FS-3 as substrate | Homo sapiens | |
2-(4-[[(3-fluorophenyl)amino]carbonothioyl]-1-piperazinyl)-8-ethyl-5-oxo-5,8-dihydropyrido[2,3-d]pyrimidine-6-carboxylic acid | 40.5% residual activity at 0.001 mM using FS-3 as substrate | Homo sapiens | |
2-(4-[[(3-iodophenyl)amino]carbonothioyl]-1-piperazinyl)-8-ethyl-5-oxo-5,8-dihydropyrido[2,3-d]pyrimidine-6-carboxylic acid | mixed inhibition, 8.6% residual activity at 0.001 mM using FS-3 as substrate | Homo sapiens | |
2-(4-[[(3-methoxyphenyl)amino]carbonothioyl]-1-piperazinyl)-8-ethyl-5-oxo-5,8-dihydropyrido[2,3-d]pyrimidine-6-carboxylic acid | 40.9% residual activity at 0.001 mM using FS-3 as substrate | Homo sapiens | |
2-(4-[[(3-methylphenyl)amino]carbonothioyl]-1-piperazinyl)-8-ethyl-5-oxo-5,8-dihydropyrido[2,3-d]pyrimidine-6-carboxylic acid | competitive inhibition, 41.9% residual activity at 0.001 mM using FS-3 as substrate | Homo sapiens | |
2-(4-[[(3-trifluoromethylphenyl)amino]carbonothioyl]-1-piperazinyl)-8-ethyl-5-oxo-5,8-dihydropyrido[2,3-d]pyrimidine-6-carboxylic acid | competitive inhibition, 0.3% residual activity at 0.001 mM using FS-3 as substrate | Homo sapiens | |
2-(4-[[(4-carboxylphenyl)amino]carbonothioyl]-1-piperazinyl)-8-ethyl-5-oxo-5,8-dihydropyrido[2,3-d]pyrimidine-6-carboxylic acid | 72.7% residual activity at 0.001 mM using FS-3 as substrate | Homo sapiens | |
2-(4-[[(4-chlorophenyl)amino]carbonothioyl]-1-piperazinyl)-8-ethyl-5-oxo-5,8-dihydropyrido[2,3-d]pyrimidine-6-carboxylic acid | competitive inhibition, 42.4% residual activity at 0.001 mM using FS-3 as substrate | Homo sapiens | |
2-(4-[[(4-dimethylaminonaphthylphenyl)amino]carbonothioyl]-1-piperazinyl)-8-ethyl-5-oxo-5,8-dihydropyrido[2,3-d]pyrimidine-6-carboxylic acid | 59.9% residual activity at 0.001 mM using FS-3 as substrate | Homo sapiens | |
2-(4-[[(4-fluorophenyl)amino]carbonothioyl]-1-piperazinyl)-8-ethyl-5-oxo-5,8-dihydropyrido[2,3-d]pyrimidine-6-carboxylic acid | 48.9% residual activity at 0.001 mM using FS-3 as substrate | Homo sapiens | |
2-(4-[[(4-iodophenyl)amino]carbonothioyl]-1-piperazinyl)-8-ethyl-5-oxo-5,8-dihydropyrido[2,3-d]pyrimidine-6-carboxylic acid | mixed inhibition, 32.7% residual activity at 0.001 mM using FS-3 as substrate | Homo sapiens | |
2-(4-[[(4-methoxyphenyl)amino]carbonothioyl]-1-piperazinyl)-8-ethyl-5-oxo-5,8-dihydropyrido[2,3-d]pyrimidine-6-carboxylic acid | 79.7% residual activity at 0.001 mM using FS-3 as substrate | Homo sapiens | |
2-(4-[[(4-methylphenyl)amino]carbonothioyl]-1-piperazinyl)-8-ethyl-5-oxo-5,8-dihydropyrido[2,3-d]pyrimidine-6-carboxylic acid | 49.9% residual activity at 0.001 mM using FS-3 as substrate | Homo sapiens | |
2-(4-[[(4-morpholinosulfonylphenyl)amino]carbonothioyl]-1-piperazinyl)-8-ethyl-5-oxo-5,8-dihydropyrido[2,3-d]pyrimidine-6-carboxylic acid | 64.1% residual activity at 0.001 mM using FS-3 as substrate | Homo sapiens | |
2-(4-[[(4-pyrazolephenyl)amino]carbonothioyl]-1-piperazinyl)-8-ethyl-5-oxo-5,8-dihydropyrido[2,3-d]pyrimidine-6-carboxylic acid | 68.6% residual activity at 0.001 mM using FS-3 as substrate | Homo sapiens | |
2-(4-[[(4-trifluoromethylphenyl)amino]carbonothioyl]-1-piperazinyl)-8-ethyl-5-oxo-5,8-dihydropyrido[2,3-d]pyrimidine-6-carboxylic acid | noncompetitive inhibition, 36.2% residual activity at 0.001 mM using FS-3 as substrate | Homo sapiens | |
2-(4-[[(phenyl)amino]carbonothioyl]-1-piperazinyl)-8-ethyl-5-oxo-5,8-dihydropyrido[2,3-d]pyrimidine-6-carboxylic acid phenyl | 56.4% residual activity at 0.001 mM using FS-3 as substrate | Homo sapiens | |
2-carba cyclic phosphatidic acid | - |
Homo sapiens | |
3-carba cyclic phosphatidic acid | - |
Homo sapiens | |
fatty alkyl phosphonate | - |
Homo sapiens | |
fatty alkyl thiophosphate | - |
Homo sapiens | |
FTY720-phosphate | - |
Homo sapiens | |
H2L 7905958 | potent ATX inhibitor, complete inhibition of FS-3 hydrolysis at 0.01 mM, competitive inhibitor | Homo sapiens | |
lysophosphatidic acid | - |
Homo sapiens | |
additional information | not inhibited by 2-(4-[[(2-trifluoromethylphenyl)amino]carbonothioyl]-1-piperazinyl)-8-ethyl-5-oxo-5,8-dihydropyrido[2,3-d]pyrimidine-6-carboxylic acid | Homo sapiens | |
sphingosine 1-phosphate | - |
Homo sapiens | |
[4-(tetradecanoylamino)benzyl]phosphonic acid | S32826 | Homo sapiens |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | - |
- |
- |
Source Tissue | Comment | Organism | Textmining |
---|---|---|---|
MDA-MB-435 cell | - |
Homo sapiens | - |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
FS-3 + H2O | fluorogenic lysoPLD substrate | Homo sapiens | 2-(6-hydroxy-3-oxo-9a,10a-dihydro-3H-xanthen-9-yl)-5-[(18-hydroxy-15-oxo-3,6,9,12-tetraoxa-16-azaoctadec-1-yl)carbamoyl]benzoic acid + (2R)-2-hydroxy-3-(phosphonooxy)propyl 6-[(4-[(E)-[4-(dimethylamino)phenyl]diazenyl]benzoyl)amino]hexanoate | - |
? | |
lysophosphatidylcholine + H2O | - |
Homo sapiens | lysophosphatidic acid + choline | - |
? |
Synonyms | Comment | Organism |
---|---|---|
ATX | - |
Homo sapiens |
autotaxin | - |
Homo sapiens |
lysophospholipase D | - |
Homo sapiens |
NPP2 | - |
Homo sapiens |
Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
---|---|---|---|---|---|
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 | Homo sapiens | |
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 | Homo sapiens | |
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 | Homo sapiens | |
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 | Homo sapiens | |
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 | Homo sapiens | |
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 | Homo sapiens | |
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 | Homo sapiens | |
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 | Homo sapiens | |
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 | Homo sapiens | |
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 | Homo sapiens | |
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 | Homo sapiens | |
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 | Homo sapiens |
IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
---|---|---|---|---|---|
0.0009 | - |
1 mM each CaCl2 and MgCl2, 5 mM KCl, and 140 mM NaCl, in 50 mM Tris, pH 8.0, at 37°C | Homo sapiens | 2-(4-[[(3-trifluoromethylphenyl)amino]carbonothioyl]-1-piperazinyl)-8-ethyl-5-oxo-5,8-dihydropyrido[2,3-d]pyrimidine-6-carboxylic acid | |
0.0013 | - |
1 mM each CaCl2 and MgCl2, 5 mM KCl, and 140 mM NaCl, in 50 mM Tris, pH 8.0, at 37°C | Homo sapiens | 2-(4-[[(2,5-dichlorophenyl)amino]carbonothioyl]-1-piperazinyl)-8-ethyl-5-oxo-5,8-dihydropyrido[2,3-d]pyrimidine-6-carboxylic acid | |
0.0015 | - |
1 mM each CaCl2 and MgCl2, 5 mM KCl, and 140 mM NaCl, in 50 mM Tris, pH 8.0, at 37°C | Homo sapiens | 2-(4-[[(4-iodophenyl)amino]carbonothioyl]-1-piperazinyl)-8-ethyl-5-oxo-5,8-dihydropyrido[2,3-d]pyrimidine-6-carboxylic acid | |
0.0016 | - |
- |
Homo sapiens | H2L 7905958 | |
0.0016 | - |
1 mM each CaCl2 and MgCl2, 5 mM KCl, and 140 mM NaCl, in 50 mM Tris, pH 8.0, at 37°C | Homo sapiens | 2-(4-[[(3-iodophenyl)amino]carbonothioyl]-1-piperazinyl)-8-ethyl-5-oxo-5,8-dihydropyrido[2,3-d]pyrimidine-6-carboxylic acid | |
0.0097 | - |
1 mM each CaCl2 and MgCl2, 5 mM KCl, and 140 mM NaCl, in 50 mM Tris, pH 8.0, at 37°C | Homo sapiens | 2-(4-[[(3-chlorophenyl)amino]carbonothioyl]-1-piperazinyl)-8-ethyl-5-oxo-5,8-dihydropyrido[2,3-d]pyrimidine-6-carboxylic acid | |
0.0107 | - |
1 mM each CaCl2 and MgCl2, 5 mM KCl, and 140 mM NaCl, in 50 mM Tris, pH 8.0, at 37°C | Homo sapiens | 2-(4-[[(4-chlorophenyl)amino]carbonothioyl]-1-piperazinyl)-8-ethyl-5-oxo-5,8-dihydropyrido[2,3-d]pyrimidine-6-carboxylic acid | |
0.0135 | - |
1 mM each CaCl2 and MgCl2, 5 mM KCl, and 140 mM NaCl, in 50 mM Tris, pH 8.0, at 37°C | Homo sapiens | 2-(4-[[(3-methylphenyl)amino]carbonothioyl]-1-piperazinyl)-8-ethyl-5-oxo-5,8-dihydropyrido[2,3-d]pyrimidine-6-carboxylic acid | |
0.0161 | - |
1 mM each CaCl2 and MgCl2, 5 mM KCl, and 140 mM NaCl, in 50 mM Tris, pH 8.0, at 37°C | Homo sapiens | 2-(4-[[(3-fluorophenyl)amino]carbonothioyl]-1-piperazinyl)-8-ethyl-5-oxo-5,8-dihydropyrido[2,3-d]pyrimidine-6-carboxylic acid | |
0.0161 | - |
1 mM each CaCl2 and MgCl2, 5 mM KCl, and 140 mM NaCl, in 50 mM Tris, pH 8.0, at 37°C | Homo sapiens | 2-(4-[[(4-methylphenyl)amino]carbonothioyl]-1-piperazinyl)-8-ethyl-5-oxo-5,8-dihydropyrido[2,3-d]pyrimidine-6-carboxylic acid | |
0.0177 | - |
1 mM each CaCl2 and MgCl2, 5 mM KCl, and 140 mM NaCl, in 50 mM Tris, pH 8.0, at 37°C | Homo sapiens | 2-(4-[[(3-methoxyphenyl)amino]carbonothioyl]-1-piperazinyl)-8-ethyl-5-oxo-5,8-dihydropyrido[2,3-d]pyrimidine-6-carboxylic acid | |
0.0177 | - |
1 mM each CaCl2 and MgCl2, 5 mM KCl, and 140 mM NaCl, in 50 mM Tris, pH 8.0, at 37°C | Homo sapiens | 2-(4-[[(4-fluorophenyl)amino]carbonothioyl]-1-piperazinyl)-8-ethyl-5-oxo-5,8-dihydropyrido[2,3-d]pyrimidine-6-carboxylic acid | |
0.0286 | - |
1 mM each CaCl2 and MgCl2, 5 mM KCl, and 140 mM NaCl, in 50 mM Tris, pH 8.0, at 37°C | Homo sapiens | 2-(4-[[(3-benzothiadiazolphenyl)amino]carbonothioyl]-1-piperazinyl)-8-ethyl-5-oxo-5,8-dihydropyrido[2,3-d]pyrimidine-6-carboxylic acid | |
0.0304 | - |
1 mM each CaCl2 and MgCl2, 5 mM KCl, and 140 mM NaCl, in 50 mM Tris, pH 8.0, at 37°C | Homo sapiens | 2-(4-[[(3,5-dimethylphenyl)amino]carbonothioyl]-1-piperazinyl)-8-ethyl-5-oxo-5,8-dihydropyrido[2,3-d]pyrimidine-6-carboxylic acid | |
0.0327 | - |
1 mM each CaCl2 and MgCl2, 5 mM KCl, and 140 mM NaCl, in 50 mM Tris, pH 8.0, at 37°C | Homo sapiens | 2-(4-[[(4-trifluoromethylphenyl)amino]carbonothioyl]-1-piperazinyl)-8-ethyl-5-oxo-5,8-dihydropyrido[2,3-d]pyrimidine-6-carboxylic acid | |
0.0341 | - |
1 mM each CaCl2 and MgCl2, 5 mM KCl, and 140 mM NaCl, in 50 mM Tris, pH 8.0, at 37°C | Homo sapiens | 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 |