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ChEMBL ligand: CHEMBL15177 (L-660711, MK-571) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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 | 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 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]