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Literature summary extracted from

  • Gannon, M.K.; Holt, J.J.; Bennett, S.M.; Wetzel, B.R.; Loo, T.W.; Bartlett, M.C.; Clarke, D.M.; Sawada, G.A.; Higgins, J.W.; Tombline, G.; Raub, T.J.; Detty, M.R.
    Rhodamine inhibitors of P-glycoprotein: an amide/thioamide switch for ATPase activity (2009), J. Med. Chem., 52, 3328-3341.
    View publication on PubMedView publication on EuropePMC

Activating Compound

EC Number Activating Compound Comment Organism Structure
7.6.2.2 rhodamine derivatives enhancement of calcein uptake into MDCK-MDR1 cells by diverse rhodamine analogues, detailed overview Homo sapiens
7.6.2.2 rosamine derivatives enhancement of calcein uptake into MDCK-MDR1 cells by diverse rosamine analogues, detailed overview Homo sapiens
7.6.2.2 verapamil the substrate is one of the most potent activators of P-gp ATPase activity, but inhibits calcein uptake Homo sapiens

Cloned(Commentary)

EC Number Cloned (Comment) Organism
7.6.2.2 expression of gene MDR1 in MDCK II cells, expression of His10-tagged P-gp in BHK cells Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
7.6.2.2 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
7.6.2.2 N-[6-(dimethylamino)-9-[5-(piperidin-1-ylcarbonyl)thiophen-2-yl]-3H-selenoxanthen-3-ylidene]-N-methylmethanaminium hexafluorophosphate
-
 Homo sapiens
7.6.2.2 N-[6-(dimethylamino)-9-[5-(piperidin-1-ylcarbonyl)thiophen-2-yl]-3H-telluroxanthen-3-ylidene]-N-methylmethanaminium hexafluorophosphate
-
 Homo sapiens
7.6.2.2 N-[6-(dimethylamino)-9-[5-(piperidin-1-ylcarbonyl)thiophen-2-yl]-3H-thioxanthen-3-ylidene]-N-methylmethanaminium hexafluorophosphate
-
 Homo sapiens
7.6.2.2 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
7.6.2.2 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
7.6.2.2 verapamil the substrate is one of the most potent activators of P-gp ATPase activity, but inhibits calcein uptake Homo sapiens

KM Value [mM]

EC Number KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
7.6.2.2 additional information
-
 additional information Km values for stimulating rhodamine and rosamine derivatives, overview Homo sapiens

Metals/Ions

EC Number Metals/Ions Comment Organism Structure
7.6.2.2 Mg2+
-
 Homo sapiens

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
7.6.2.2 ATP + H2O + xenobiotic/in Homo sapiens
-
 ADP + phosphate + xenobiotic/out
-
 ?

Organism

EC Number Organism UniProt Comment Textmining
7.6.2.2 Homo sapiens
-
 gene MDR1 encodes P-gp
-

Purification (Commentary)

EC Number Purification (Comment) Organism
7.6.2.2 recombinant His10-tagged P-gp from BHK cells by nickel affinity chromatography Homo sapiens

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
7.6.2.2 ATP + H2O + calcein/in
-
 Homo sapiens ADP + phosphate + calcein/out
-
 ?
7.6.2.2 ATP + H2O + verapamil/in
-
 Homo sapiens ADP + phosphate + verapamil/out
-
 ?
7.6.2.2 ATP + H2O + vinblastine/in
-
 Homo sapiens ADP + phosphate + vinblastine/out
-
 ?
7.6.2.2 ATP + H2O + xenobiotic/in
-
 Homo sapiens ADP + phosphate + xenobiotic/out
-
 ?
7.6.2.2 additional information Pgp transport studies across recombinant MDCK-MDR1 monolayers, overview Homo sapiens ?
-
 ?

Synonyms

EC Number Synonyms Comment Organism
7.6.2.2 ABCB1
-
 Homo sapiens
7.6.2.2 MDR1
-
 Homo sapiens
7.6.2.2 P-glycoprotein
-
 Homo sapiens
7.6.2.2 P-gp
-
 Homo sapiens

Temperature Optimum [°C]

EC Number Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
7.6.2.2 37
-
 assay at Homo sapiens

pH Optimum

EC Number pH Optimum Minimum pH Optimum Maximum Comment Organism
7.6.2.2 7.4
-
 assay at Homo sapiens

Cofactor

EC Number Cofactor Comment Organism Structure
7.6.2.2 ATP
-
 Homo sapiens

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
7.6.2.2 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
7.6.2.2 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
7.6.2.2 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
7.6.2.2 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
7.6.2.2 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
7.6.2.2 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