Activating Compound | Comment | Organism | Structure |
---|---|---|---|
rhodamine derivatives | enhancement of calcein uptake into MDCK-MDR1 cells by diverse rhodamine analogues, detailed overview | Homo sapiens | |
rosamine derivatives | enhancement of calcein uptake into MDCK-MDR1 cells by diverse rosamine analogues, detailed overview | Homo sapiens | |
verapamil | the substrate is one of the most potent activators of P-gp ATPase activity, but inhibits calcein uptake | Homo sapiens |
Cloned (Comment) | Organism |
---|---|
expression of gene MDR1 in MDCK II cells, expression of His10-tagged P-gp in BHK cells | Homo sapiens |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
N-methyl-N-(9-phenyl-2,3,6,7-tetrahydro-1H,5H,12H-pyrido[3,2,1-ij]selenochromeno[2,3-f]quinolin-12-ylidene)methanaminium hexafluorophosphate | - |
Homo sapiens | |
N-[6-(dimethylamino)-9-[5-(piperidin-1-ylcarbonyl)thiophen-2-yl]-3H-selenoxanthen-3-ylidene]-N-methylmethanaminium hexafluorophosphate | - |
Homo sapiens | |
N-[6-(dimethylamino)-9-[5-(piperidin-1-ylcarbonyl)thiophen-2-yl]-3H-telluroxanthen-3-ylidene]-N-methylmethanaminium hexafluorophosphate | - |
Homo sapiens | |
N-[6-(dimethylamino)-9-[5-(piperidin-1-ylcarbonyl)thiophen-2-yl]-3H-thioxanthen-3-ylidene]-N-methylmethanaminium hexafluorophosphate | - |
Homo sapiens | |
N-[9-[3-(dimethylamino)phenyl]-2,3,6,7-tetrahydro-1H,5H,12H-pyrido[3,2,1-ij]selenochromeno[2,3-f]quinolin-12-ylidene]-N-methylmethanaminium bromide | - |
Homo sapiens | |
N-[9-[4-(dimethylamino)phenyl]-2,3,6,7-tetrahydro-1H,5H,12H-pyrido[3,2,1-ij]selenochromeno[2,3-f]quinolin-12-ylidene]-N-methylmethanaminium bromide | - |
Homo sapiens | |
verapamil | the substrate is one of the most potent activators of P-gp ATPase activity, but inhibits calcein uptake | Homo sapiens |
KM Value [mM] | KM Value Maximum [mM] | Substrate | Comment | Organism | Structure |
---|---|---|---|---|---|
additional information | - |
additional information | Km values for stimulating rhodamine and rosamine derivatives, overview | Homo sapiens |
Metals/Ions | Comment | Organism | Structure |
---|---|---|---|
Mg2+ | - |
Homo sapiens |
Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
---|---|---|---|---|---|---|
ATP + H2O + xenobiotic/in | Homo sapiens | - |
ADP + phosphate + xenobiotic/out | - |
? |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | - |
gene MDR1 encodes P-gp | - |
Purification (Comment) | Organism |
---|---|
recombinant His10-tagged P-gp from BHK cells by nickel affinity chromatography | Homo sapiens |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
ATP + H2O + calcein/in | - |
Homo sapiens | ADP + phosphate + calcein/out | - |
? | |
ATP + H2O + verapamil/in | - |
Homo sapiens | ADP + phosphate + verapamil/out | - |
? | |
ATP + H2O + vinblastine/in | - |
Homo sapiens | ADP + phosphate + vinblastine/out | - |
? | |
ATP + H2O + xenobiotic/in | - |
Homo sapiens | ADP + phosphate + xenobiotic/out | - |
? | |
additional information | Pgp transport studies across recombinant MDCK-MDR1 monolayers, overview | Homo sapiens | ? | - |
? |
Synonyms | Comment | Organism |
---|---|---|
ABCB1 | - |
Homo sapiens |
MDR1 | - |
Homo sapiens |
P-glycoprotein | - |
Homo sapiens |
P-gp | - |
Homo sapiens |
Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
---|---|---|---|
37 | - |
assay at | Homo sapiens |
pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
---|---|---|---|
7.4 | - |
assay at | Homo sapiens |
Cofactor | Comment | Organism | Structure |
---|---|---|---|
ATP | - |
Homo sapiens |
IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
---|---|---|---|---|---|
0.0023 | - |
pH 7.4, 37°C, recombinant enzyme | Homo sapiens | N-methyl-N-(9-phenyl-2,3,6,7-tetrahydro-1H,5H,12H-pyrido[3,2,1-ij]selenochromeno[2,3-f]quinolin-12-ylidene)methanaminium hexafluorophosphate | |
0.0053 | - |
pH 7.4, 37°C, recombinant enzyme | Homo sapiens | N-[6-(dimethylamino)-9-[5-(piperidin-1-ylcarbonyl)thiophen-2-yl]-3H-telluroxanthen-3-ylidene]-N-methylmethanaminium hexafluorophosphate | |
0.0068 | - |
pH 7.4, 37°C, recombinant enzyme | Homo sapiens | N-[9-[4-(dimethylamino)phenyl]-2,3,6,7-tetrahydro-1H,5H,12H-pyrido[3,2,1-ij]selenochromeno[2,3-f]quinolin-12-ylidene]-N-methylmethanaminium bromide | |
0.0079 | - |
pH 7.4, 37°C, recombinant enzyme | Homo sapiens | N-[6-(dimethylamino)-9-[5-(piperidin-1-ylcarbonyl)thiophen-2-yl]-3H-thioxanthen-3-ylidene]-N-methylmethanaminium hexafluorophosphate | |
0.009 | - |
pH 7.4, 37°C, recombinant enzyme | Homo sapiens | N-[6-(dimethylamino)-9-[5-(piperidin-1-ylcarbonyl)thiophen-2-yl]-3H-telluroxanthen-3-ylidene]-N-methylmethanaminium hexafluorophosphate | |
0.0236 | - |
pH 7.4, 37°C, recombinant enzyme | Homo sapiens | N-[9-[3-(dimethylamino)phenyl]-2,3,6,7-tetrahydro-1H,5H,12H-pyrido[3,2,1-ij]selenochromeno[2,3-f]quinolin-12-ylidene]-N-methylmethanaminium bromide |