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

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ChEMBL ligand: CHEMBL15177 (L-660711, MK-571)
  • ABCG2/ATP-binding cassette sub-family G member 2 in Human [ChEMBL: CHEMBL5393] [GtoPdb: 792] [UniProtKB: Q9UNQ0]
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  • 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
ABCG2/ATP-binding cassette sub-family G member 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5393] [GtoPdb: 792] [UniProtKB: Q9UNQ0]
ChEMBL Inhibition of human ABCG2 expressed in human SAOS-2 cells mediated mitoxantrone efflux using mitoxantrone as substrate by flow cytometry B 4.3 pIC50 50000 nM IC50 Eur J Med Chem (2022) 237: 114346-114346 [PMID:35483322]
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 Reversal of human ABCC1-mediated multidrug resistance in HEK293/MRP1 cells assessed as effect on etoposide-induced cytotoxicity by measuring etoposide IC50 at 25 uM after 72 hrs by CCK8 assay (Rvb = 63.34 +/- 7.92 uM) B 4.93 pIC50 11870 nM IC50 J Nat Prod (2020) 83: 1461-1472 [PMID:32347726]
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 Inhibition of ABCC1 (unknown origin) overexpressing human KBV cells mediated efflux assessed as cisplatin IC50 using cisplatin as substrate at 25 uM B 5.79 pIC50 1620 nM IC50 J Med Chem (2023) 66: 8628-8642 [PMID:37332162]
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 34:

Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]