Literature summary for 7.6.2.3 extracted from

Schmitt, S.M.; Stefan, K.; Wiese, M.
Pyrrolopyrimidine derivatives and purine analogs as novel activators of multidrug resistance-associated protein 1 (MRP1, ABCC1) (2017), Biochim. Biophys. Acta, 1859, 69-79 .

Activating Compound

Activating Compound	Comment	Organism
4,5-bis(benzylamino)-5H-pyrrolo[3,2-d]pyrimidine-7-carbonitrile	about 15% increase of activity at 10 nM	Homo sapiens
4,5-bis(benzylamino)-5H-pyrrolo[3,2-d]pyrimidine-7-carbonitrile	about 30% increase of activity at 10 nM	Canis lupus familiaris
4-(benzylamino)-5-[(3-phenylpropyl)amino]-5H-pyrrolo[3,2-d]pyrimidine-7-carbonitrile	about 15% increase of activity at 10 nM	Homo sapiens
4-(benzylamino)-5-[(3-phenylpropyl)amino]-5H-pyrrolo[3,2-d]pyrimidine-7-carbonitrile	about 30% increase of activity at 10 nM	Canis lupus familiaris
4-(benzylamino)-6,7,8,9-tetrahydropyrimido[4,5-b]indolizine-10-carbonitrile	-	Homo sapiens
4-(benzylamino)-6,7,8,9-tetrahydropyrimido[4,5-b]indolizine-10-carbonitrile	-	Canis lupus familiaris
4-anilino-5-(benzylamino)-5H-pyrrolo[3,2-d]pyrimidine-7-carbonitrile	15% increase of activity at 10 nM	Homo sapiens
4-anilino-5-(benzylamino)-5H-pyrrolo[3,2-d]pyrimidine-7-carbonitrile	25% increase of activity at 10 nM	Canis lupus familiaris
4-anilino-6,7,8,9-tetrahydropyrimido[4,5-b]indolizine-10-carbonitrile	-	Homo sapiens
4-anilino-6,7,8,9-tetrahydropyrimido[4,5-b]indolizine-10-carbonitrile	-	Canis lupus familiaris
4-[(2-phenylethyl)amino]-6,7,8,9-tetrahydropyrimido[4,5-b]indolizine-10-carbonitrile	-	Homo sapiens
4-[(2-phenylethyl)amino]-6,7,8,9-tetrahydropyrimido[4,5-b]indolizine-10-carbonitrile	-	Canis lupus familiaris
4-[(3-phenylpropyl)amino]-6,7,8,9-tetrahydropyrimido[4,5-b]indolizine-10-carbonitrile	-	Homo sapiens
4-[(3-phenylpropyl)amino]-6,7,8,9-tetrahydropyrimido[4,5-b]indolizine-10-carbonitrile	-	Canis lupus familiaris
5-(2-phenylethyl)-4-[(2-phenylethyl)amino]-5H-pyrrolo[3,2-d]pyrimidine-7-carbonitrile	about 20% increase of activity at 10 nM	Homo sapiens
5-(2-phenylethyl)-4-[(2-phenylethyl)amino]-5H-pyrrolo[3,2-d]pyrimidine-7-carbonitrile	about 43% increase of activity at 10 nM	Canis lupus familiaris
5-(2-phenylethyl)-4-[(3-phenylpropyl)amino]-5H-pyrrolo[3,2-d]pyrimidine-7-carbonitrile	about 20% increase of activity at 10 nM	Homo sapiens
5-(2-phenylethyl)-4-[(3-phenylpropyl)amino]-5H-pyrrolo[3,2-d]pyrimidine-7-carbonitrile	about 45% increase of activity at 10 nM	Canis lupus familiaris
5-(benzylamino)-4-(methylamino)-5H-pyrrolo[3,2-d]pyrimidine-7-carbonitrile	about 10% increase of activity at 10 nM	Homo sapiens
5-(benzylamino)-4-(methylamino)-5H-pyrrolo[3,2-d]pyrimidine-7-carbonitrile	about 40% increase of activity at 10 nM	Canis lupus familiaris
6-(4-benzylpiperazin-1-yl)-7H-purine	25% increase of activity at 10 nM	Canis lupus familiaris
6-(4-benzylpiperazin-1-yl)-7H-purine	about 20% increase of activity at 10 nM	Homo sapiens
6-(4-phenylpiperazin-1-yl)-7H-purine	about 35% increase of activity at 10 nM	Canis lupus familiaris
6-(4-phenylpiperazin-1-yl)-7H-purine	about 7% increase of activity at 10 nM	Homo sapiens
6-[4-(2-phenylethyl)piperazin-1-yl]-7H-purine	about 30% increase of activity at 10 nM	Canis lupus familiaris
6-[4-(2-phenylethyl)piperazin-1-yl]-7H-purine	about 7% increase of activity at 10 nM	Homo sapiens
6-[4-(diphenylmethyl)piperazin-1-yl]-7H-purine	25% increase of activity at 10 nM	Homo sapiens
6-[4-(diphenylmethyl)piperazin-1-yl]-7H-purine	more than 50% increase of activity at 10 nM	Canis lupus familiaris

Inhibitors

Inhibitors	Comment	Organism
4-[4-(2-phenylethyl)piperazin-1-yl]-6,7,8,9-tetrahydropyrimido[4,5-b]indolizine-10-carbonitrile	complete inhibition at 10 nM	Canis lupus familiaris
4-[4-(2-phenylethyl)piperazin-1-yl]-6,7,8,9-tetrahydropyrimido[4,5-b]indolizine-10-carbonitrile	complete inhibition at 10 nM	Homo sapiens
cyclosporine A	-	Canis lupus familiaris
cyclosporine A	-	Homo sapiens
Ko143	-	Canis lupus familiaris
Ko143	-	Homo sapiens
verapamil	-	Canis lupus familiaris
verapamil	-	Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates	Organism	Comment (Nat. Sub.)	Natural Products	Comment (Nat. Pro.)	Rev.	Reac.
ATP + H2O + glutathione-S-conjugate[side 1]	Homo sapiens	-	ADP + phosphate + glutathione-S-conjugate[side 2]	-	?
ATP + H2O + glutathione-S-conjugate[side 1]	Canis lupus familiaris	-	ADP + phosphate + glutathione-S-conjugate[side 2]	-	?

Organism

Organism	UniProt	Comment	Textmining
Canis lupus familiaris	Q6UR05	-	-
Homo sapiens	P33527	-	-

Source Tissue

Source Tissue	Comment	Organism	Textmining
H-69AR cell	-	Homo sapiens	-
MDCK II cell	-	Canis lupus familiaris	-

Substrates and Products (Substrate)

Substrates	Comment Substrates	Organism	Products	Comment (Products)	Rev.
ATP + H2O + glutathione-S-conjugate[side 1]	-	Homo sapiens	ADP + phosphate + glutathione-S-conjugate[side 2]	-	?
ATP + H2O + glutathione-S-conjugate[side 1]	-	Canis lupus familiaris	ADP + phosphate + glutathione-S-conjugate[side 2]	-	?
ATP + H2O + S-(calcein acetoxymethyl ester)glutathione[side 1]	-	Homo sapiens	ADP + phosphate + S-(calcein acetoxymethyl ester)glutathione[side 2]	-	?
ATP + H2O + S-(calcein acetoxymethyl ester)glutathione[side 1]	-	Canis lupus familiaris	ADP + phosphate + S-(calcein acetoxymethyl ester)glutathione[side 2]	-	?
ATP + H2O + S-(daunorubicin)glutathione[side 1]	-	Homo sapiens	ADP + phosphate + S-(daunorubicin)glutathione[side 2]	-	?
ATP + H2O + S-(daunorubicin)glutathione[side 1]	-	Canis lupus familiaris	ADP + phosphate + S-(daunorubicin)glutathione[side 2]	-	?

Synonyms

Synonyms	Comment	Organism
ABCC1	-	Homo sapiens
ABCC1	-	Canis lupus familiaris
MRP1	-	Homo sapiens
MRP1	-	Canis lupus familiaris
multidrug resistance-associated protein 1	-	Homo sapiens
multidrug resistance-associated protein 1	-	Canis lupus familiaris