MK-571 [Ligand Id: 10346] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL15177 (L-660711, MK-571)
  • ABCC2/Canalicular multispecific organic anion transporter 1 in Human [ChEMBL: CHEMBL5748] [GtoPdb: 780] [UniProtKB: Q92887]
  • ABCC2/Canalicular multispecific organic anion transporter 1 in Rat [ChEMBL: CHEMBL2073676] [GtoPdb: 780] [UniProtKB: Q63120]
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  • Cysteinyl leukotriene receptor 1 in Guinea pig [ChEMBL: CHEMBL5645] [UniProtKB: Q2NNR5]
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  • ABCC1/Multidrug resistance-associated protein 1 in Human [ChEMBL: CHEMBL3004] [GtoPdb: 779] [UniProtKB: P33527]
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  • ABCC4/Multidrug resistance-associated protein 4 in Human [ChEMBL: CHEMBL1743128] [GtoPdb: 782] [UniProtKB: O15439]
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  • ABCC5/Multidrug resistance-associated protein 5 in Human [ChEMBL: CHEMBL2046258] [GtoPdb: 783] [UniProtKB: O15440]
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  • CysLT1 receptor in Human [GtoPdb: 269] [UniProtKB: Q9Y271]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
ABCC2/Canalicular multispecific organic anion transporter 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5748] [GtoPdb: 780] [UniProtKB: Q92887]
ChEMBL TP_TRANSPORTER: inhibition of Vinblastine transepithelial transport (basal to apical) in MRP2-expressing MDCK cells F 4.58 pKi 26400 nM Ki Pharm. Res. (2002) 19: 773-779 [PMID:12134946]
ChEMBL TP_TRANSPORTER: inhibition of LTC4 uptake in membrane vesicles from MRP2-expressing LLC PK1 cells F 4.88 pKi 13100 nM Ki Mol. Pharmacol. (1999) 56: 1219-1228 [PMID:10570049]
ChEMBL Inhibition of human MRP2-mediated estradiol-17-beta-glucuronide transport in Sf9 cells inverted membrane vesicles B 5 pIC50 10000 nM IC50 J. Med. Chem. (2008) 51: 3275-3287 [PMID:18457386]
ChEMBL TP_TRANSPORTER: inhibition of PAH uptake (PAH: 0.1uM) in membrane vesicles from MRP2-expressing HEK cells F 5.4 pIC50 4000 nM IC50 Kidney Int. (2000) 57: 1636-1642 [PMID:10760098]
ChEMBL Inhibition of ABCC2 overexpressed in MDCK cells at 100 uM by flow cytometric-based chloromethylfluorescein-diacetate accumulation assay B 6 pIC50 >1000 nM IC50 J. Med. Chem. (2009) 52: 1190-1197 [PMID:19170519]
ABCC2/Canalicular multispecific organic anion transporter 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2073676] [GtoPdb: 780] [UniProtKB: Q63120]
ChEMBL TP_TRANSPORTER: inhibition of E217betaG uptake (E217betaG: 0.055 uM) in membrane vesicles from Mrp2-expressing Sf9 cells F 5.58 pIC50 2620 nM IC50 Mol. Pharmacol. (2001) 59: 1077-1085 [PMID:11306690]
Cysteinyl leukotriene receptor 1 in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5645] [UniProtKB: Q2NNR5]
ChEMBL Inhibition of Leukotriene D4 induced contraction of guinea-pig trachea was determined F 8.8 pKd 1.58 nM Kd Bioorg. Med. Chem. Lett. (1992) 2: 1141-1146
ChEMBL Binding affinity against Cysteinyl leukotriene D4 receptor from guinea pig trachea using [3H]LTD4 B 9 pKd 1 nM Kd J. Med. Chem. (1990) 33: 1194-1200 [PMID:2157010]
ChEMBL Compound was evaluated for its ability to displace [3H]LTD4 from Cysteinyl leukotriene D4 receptor in guinea pig lung membranes B 9.7 pKi 0.2 nM Ki J. Med. Chem. (1991) 34: 1235-1242 [PMID:1849993]
ChEMBL Inhibitory concentration against [3H]Leukotriene D4 binding to guinea-pig lung membranes was determined B 8.41 pIC50 3.9 nM IC50 Bioorg. Med. Chem. Lett. (1992) 2: 1141-1146
ChEMBL Inhibitory concentration against [3H]Leukotriene D4 binding to guinea-pig lung membranes was determined B 8.52 pIC50 3 nM IC50 Bioorg. Med. Chem. Lett. (1992) 2: 1141-1146
ChEMBL In vitro inhibition of [3H]LTD4 binding to guinea pig lung membranes B 9.1 pIC50 0.8 nM IC50 J. Med. Chem. (1992) 35: 3832-3844 [PMID:1331447]
ABCC1/Multidrug resistance-associated protein 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3004] [GtoPdb: 779] [UniProtKB: P33527]
ChEMBL Inhibition of MRP1-mediated transport of [3H]LTC4 expressed in human HeLa T5 cells by liquid scintillation counting B 6.22 pKi 600 nM Ki J. Med. Chem. (2009) 52: 4586-4595 [PMID:19580319]
ChEMBL TP_TRANSPORTER: inhibition of GSSG uptake in membrane vesicle from MRP1-expressing HeLa cells F 6.22 pKi 600 nM Ki Biochem. J. (1996) 314: 433-437 [PMID:8670053]
ChEMBL TP_TRANSPORTER: inhibition of LTC4 uptake in membrane vesicle from MRP1-expressing HeLa cells F 6.22 pKi 600 nM Ki Cancer Res. (1996) 56: 988-994 [PMID:8640791]
ChEMBL Inhibition of human ABCC1 transfected in HEK293 cells assessed as potentiation of etoposide-induced cytotoxicity by measuring etoposide IC50 at 25000 nM after 72 hrs by CCK8 assay (Rvb = 38.54 +/- 5.62 nM) B 5.28 pIC50 5220 nM IC50 J Nat Prod (2016) 79: 2135-2142 [PMID:27504669]
ChEMBL Inhibition of recombinant MRP1 expressed in human HeLa T5 cells assessed as ATP-dependent transport of [3H]para-aminohippurate B 5.48 pIC50 3300 nM IC50 J. Med. Chem. (2009) 52: 4586-4595 [PMID:19580319]
ChEMBL TP_TRANSPORTER: inhibition of Daunorubicin uptake (Daunorubicin: 0.6 uM) in membrane vesicles from GLC4/ADR cells F 6.4 pIC50 400 nM IC50 Br. J. Pharmacol. (1999) 126: 681-688 [PMID:10188979]
ChEMBL Inhibition of MRP1 in human 2008/MRP1 cells assessed as potentiation of doxorubicin-induced cytotoxicity by measuring reduction in cell survival after 5 days by MTS assay B 4.72 pEC50 19000 nM EC50 J Med Chem (2018) 61: 9931-9951 [PMID:30351934]
ChEMBL Modulation of MRP1 mediated drug efflux in doxorubicin-resistant human H69 cells assessed as accumulation of calcein AM incubated for 15 mins prior to calcein AM addition measured after 30 mins by fluorescence analysis B 4.91 pEC50 12400 nM EC50 Bioorg. Med. Chem. (2014) 22: 5860-5870 [PMID:25311564]
ChEMBL Inhibition of MRP1 expressed in MDCK cells assessed as calcein AM accumulation by fluorescence assay B 5.55 pEC50 2850 nM EC50 J. Med. Chem. (2010) 53: 5467-5475 [PMID:20684594]
ABCC4/Multidrug resistance-associated protein 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1743128] [GtoPdb: 782] [UniProtKB: O15439]
ChEMBL TP_TRANSPORTER: inhibition of 9-(2-phosphonomethoxyethyl)adenine(PMEA) efflux (PMEA: 1 uM) in MRP4-expressing HEK293 cells F 5 pIC50 10000 nM IC50 Mol. Pharmacol. (2003) 63: 1094-1103 [PMID:12695538]
ABCC5/Multidrug resistance-associated protein 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2046258] [GtoPdb: 783] [UniProtKB: O15440]
ChEMBL TP_TRANSPORTER: inhibition of 9-(2-phosphonomethoxyethyl)adenine(PMEA) efflux (PMEA: 1 uM) in MRP5-expressing HEK293 cells F 4.4 pIC50 40000 nM IC50 Mol. Pharmacol. (2003) 63: 1094-1103 [PMID:12695538]
CysLT1 receptor in Human [GtoPdb: 269] [UniProtKB: Q9Y271]
GtoPdb Antagonism of [3H]LTD4 binding in COS-7 cells. - 8 pIC50 10 nM IC50 Nature (1999) 399: 789-93 [PMID:10391245]

ChEMBL data shown on this page come from version 27:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]