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Literature summary for 7.6.2.2 extracted from

  • Tombline, G.; Holt, J.J.; Gannon, M.K.; Donnelly, D.J.; Wetzel, B.; Sawada, G.A.; Raub, T.J.; Detty, M.R.
    ATP occlusion by P-glycoprotein as a surrogate measure for drug coupling (2008), Biochemistry, 47, 3294-3307.
    View publication on PubMed
Search for more literature for 7.6.2.2

Cloned(Commentary)

Cloned (Comment) Organism
expression in Pichia pastoris Mus musculus

Inhibitors

Inhibitors Comment Organism Structure
3,6-bis(dimethylamino)-9-(4-dimethylaminophenyl)-thioxanthylium hexafluorophosphate competitive inhibition of verapamil-dependent ATPase-activity Mus musculus
3,6-bis(dimethylamino)-9-phenyl-selenoxanthylium bromide i.e. selenium-derivative of tetramethylrosamine, competitive inhibition of verapamil-dependent ATPase-activity Mus musculus
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 competitive inhibition of verapamil-dependent ATPase-activity Mus musculus
N-methyl-N-(9-phenyl-2,3,6,7-tetrahydro-1H,5H,12H-pyrido[3,2,1-ij]thiochromeno[2,3-f]quinolin-12-ylidene)methanaminium hexafluorophosphate competitive inhibition of verapamil-dependent ATPase-activity Mus musculus

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.074
-
 3,6-bis(dimethylamino)-9-phenyl-selenoxanthylium bromide pH 7.4, 37°C Mus musculus
0.078
-
 N-methyl-N-(9-phenyl-2,3,6,7-tetrahydro-1H,5H,12H-pyrido[3,2,1-ij]thiochromeno[2,3-f]quinolin-12-ylidene)methanaminium hexafluorophosphate pH 7.4, 37°C Mus musculus

Organism

Organism UniProt Comment Textmining
Mus musculus
-
 isoform Mdr3
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
3,6-bis(dimethylamino)-9-phenyl-selenoxanthylium bromide/in + ATP + H2O
-
 Mus musculus 3,6-bis(dimethylamino)-9-phenyl-selenoxanthylium bromide/out + ADP + phosphate
-
 ?
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/in + ATP + H2O
-
 Mus musculus N-methyl-N-(9-phenyl-2,3,6,7-tetrahydro-1H,5H,12H-pyrido[3,2,1-ij]thiochromeno[2,3-f]quinolin-12-ylidene)methanaminium hexafluorophosphate/out + ADP + phosphate
-
 ?

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.002
-
 N-methyl-N-(9-phenyl-2,3,6,7-tetrahydro-1H,5H,12H-pyrido[3,2,1-ij]thiochromeno[2,3-f]quinolin-12-ylidene)methanaminium hexafluorophosphate pH 7.4, 37°C Mus musculus
0.007
-
 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 pH 7.4, 37°C Mus musculus
0.008
-
 3,6-bis(dimethylamino)-9-(4-dimethylaminophenyl)-thioxanthylium hexafluorophosphate pH 7.4, 37°C Mus musculus