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Literature summary extracted from

  • Ebert, S.P.; Wetzel, B.; Myette, R.L.; Conseil, G.; Cole, S.P.; Sawada, G.A.; Loo, T.W.; Bartlett, M.C.; Clarke, D.M.; Detty, M.R.
    Chalcogenopyrylium compounds as modulators of the ATP-binding cassette transporters P-glycoprotein (P-gp/ABCB1) and multidrug resistance protein 1 (MRP1/ABCC1) (2012), J. Med. Chem., 55, 4683-4699.
    View publication on PubMed

Inhibitors

EC Number Inhibitors Comment Organism Structure
7.6.2.2 (R)-4-[(1a,6,10b)-1,1-dichloro-1,1a,6,10b-tetrahydrodibenzo[a,e]cyclopropa[c]cyclohepten-6-yl]-[(5-quinolinyloxy)methyl]-1-piperazineethanol complete inhibition of P-glycoprotein at 0.005 mM Homo sapiens
7.6.2.2 (R)-4-[(1a,6,10b)-1,1-difluoro-1,1a,6,10btetrahydrodibenzo[a,e]cyclopropa[c]cyclohepten-6-yl]-[(5-quin-olinyloxy)methyl]-1-piperazineethanol LSN 335979, P-glycoprotein-specific inhibitor Homo sapiens
7.6.2.2 2,6-bis(4-(dimethylamino)phenyl)-4-(5-(piperidine-1-carbonothioyl)thien-2-yl)thiopyrylium chloride 81% inhibition of MRP1 at 0.01 mM Homo sapiens
7.6.2.2 2,6-bis(4-(dimethylamino)phenyl)-4-(5-(piperidine-1-carbonyl)thien-2-yl)thiopyrylium hexafluorophosphate 78% inhibition of MRP1 at 0.01 mM Homo sapiens
7.6.2.2 2,6-di-tert-butyl-4-(5-(piperidine-1-carbonothioyl)thien-2-yl)thiopyrylium hexafluorophosphate 11% inhibition of MRP1 at 0.01 mM Homo sapiens
7.6.2.2 2,6-di-tert-butyl-4-(5-(piperidine-1-carbonothioyl)thiophen-2-yl)thiopyrylium chloride 32% inhibition of MRP1 at 0.01 mM Homo sapiens
7.6.2.2 2-tert-butyl-6-(4-(dimethylamino)phenyl)-4-(5-(piperidine-1-carbonothioyl)thiophen-2-yl)thiopyrylium chloride 93% inhibition of MRP1 at 0.01 mM Homo sapiens
7.6.2.2 2-tert-butyl-6-(4-(dimethylamino)phenyl)-4-(5-(piperidine-1-carbonyl)thien-2-yl)thiopyrylium hexafluorophosphate 59% inhibition of MRP1 at 0.01 mM Homo sapiens
7.6.2.2 verapamil
-
 Homo sapiens

Localization

EC Number Localization Comment Organism GeneOntology No. Textmining

Molecular Weight [Da]

EC Number Molecular Weight [Da] Molecular Weight Maximum [Da] Comment Organism
7.6.2.2 190000
-
 x * 190000, MRP1, SDS-PAGE 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
-
-
-

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 + estradiol glucuronide/in
-
 Homo sapiens ADP + phosphate + estradiol glucuronide/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
-
 ?

Subunits

EC Number Subunits Comment Organism
7.6.2.2 ? x * 190000, MRP1, SDS-PAGE Homo sapiens

Synonyms

EC Number Synonyms Comment Organism
7.6.2.2 ABCB1
-
 Homo sapiens
7.6.2.2 ABCC1
-
 Homo sapiens
7.6.2.2 MRP1
-
 Homo sapiens
7.6.2.2 multidrug resistance protein 1
-
 Homo sapiens
7.6.2.2 P-glycoprotein
-
 Homo sapiens
7.6.2.2 P-gp
-
 Homo sapiens