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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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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]