tariquidar [Ligand Id: 11787] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL348475 (XR-9576, Tariquidar, XR9576)
  • ABCG2/ATP-binding cassette sub-family G member 2 in Human [ChEMBL: CHEMBL5393] [GtoPdb: 792] [UniProtKB: Q9UNQ0]
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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 BCRP expressed in MCF-7 MX cells using Hoechst 33342 staining B 5.82 pIC50 1500 nM IC50 Bioorg. Med. Chem. (2011) 19: 2090-2102 [PMID:21354800]
ChEMBL Inhibition of ABCG2 in human mitoxantrone-resistant MCF7 cells by Hoechst 33342 assay B 5.84 pIC50 1445.44 nM IC50 Bioorg. Med. Chem. (2008) 16: 8224-8236 [PMID:18678495]
ChEMBL Inhibition of BCRP expressed in MDCK cells using Hoechst 33342 staining B 6.03 pIC50 940 nM IC50 Bioorg. Med. Chem. (2011) 19: 2090-2102 [PMID:21354800]
ChEMBL Inhibition of ABCG2 overexpressed in human MCF7/Topo cells by flow cytometric-based mitoxantrone efflux assay B 6.04 pIC50 916 nM IC50 J. Med. Chem. (2009) 52: 1190-1197 [PMID:19170519]
ChEMBL Inhibition of BCRP expressed in MDCK cells by pheophorbide A assay B 6.07 pIC50 850 nM IC50 Bioorg. Med. Chem. Lett. (2010) 20: 180-183 [PMID:19932960]
ChEMBL Inhibition of BCRP expressed in MCF7 MX cells by Hoechst 33342 staining B 6.17 pIC50 680 nM IC50 Bioorg. Med. Chem. Lett. (2010) 20: 180-183 [PMID:19932960]
ChEMBL Inhibition of ABCG2 in human MCF7/Topo cells after 2 hrs by Hoechst 33342 staining based fluorescence assay B 6.28 pIC50 526 nM IC50 ACS Med Chem Lett (2018) 9: 854-859 [PMID:30128080]
ChEMBL Inhibition of ABCG2 expressed in human MCF7/Topo cells by Hoechst microplate assay B 6.28 pIC50 526 nM IC50 Bioorg. Med. Chem. Lett. (2011) 21: 3654-3657 [PMID:21570282]
ChEMBL Inhibition of ABCG2 in human MCF7/Topo cells after 2 hrs by Hoechst 33342 microplate assay B 6.28 pIC50 526 nM IC50 ACS Med. Chem. Lett. (2013) 4: 393-396 [PMID:24900683]
ChEMBL Inhibition of ABCG2 in human MCF7/Topo cells by Hoechst 33342 assay B 6.28 pIC50 520 nM IC50 Eur. J. Med. Chem. (2016) 109: 124-133 [PMID:26774038]
ChEMBL Inhibition of BCRP (unknown origin) B 7 pEC50 100 nM EC50 J Med Chem (2019) 62: 8578-8608 [PMID:31465686]
ChEMBL Activity at BCRP (unknown origin) expressed in MDCK cells using rhodamine 123 as substrate incubated for 30 mins prior to substrate addition measured after 30 mins by fluorometric analysis B 8 pEC50 10 nM EC50 Bioorg. Med. Chem. Lett. (2013) 23: 1370-1374 [PMID:23374872]
ABCB1/P-glycoprotein 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4302] [GtoPdb: 768] [UniProtKB: P08183]
ChEMBL Inhibition of ABCB1 in human K562/A02 cells assessed as potentiation of adriamycin-induced cytotoxicity by measuring ADR IC50 treated for 48 hrs followed by compound washout measured after 24 hrs by MTT assay (Rvb = 51.34 +/- 5.1 uM) B 4.84 pIC50 14390 nM IC50 Bioorg Med Chem (2017) 25: 4194-4202 [PMID:28645831]
ChEMBL Inhibition of ABCB1 in human K562/A02 cells assessed as potentiation of adriamycin-induced cytotoxicity by measuring ADR IC50 treated for 48 hrs followed by compound washout measured after 12 hrs by MTT assay (Rvb = 51.34 +/- 5.1 uM) B 5.08 pIC50 8280 nM IC50 Bioorg Med Chem (2017) 25: 4194-4202 [PMID:28645831]
ChEMBL Reversal of P-gp-mediated drug resistance in human KBV cells assessed as potentiation of paclitaxel-induced cytotoxicity by measuring paclitaxel IC50 at 5 uM after 72 hrs by MTT assay (Rvb = 398.34 +/- 0.58 uM) B 5.28 pIC50 5240 nM IC50 Eur J Med Chem (2019) 161: 364-377 [PMID:30384042]
ChEMBL Inhibition of ABCB1 in human K562/A02 cells assessed as potentiation of adriamycin-induced cytotoxicity by measuring ADR IC50 treated for 48 hrs followed by compound washout measured after 6 hrs by MTT assay (Rvb = 51.34 +/- 5.1 uM) B 5.3 pIC50 4970 nM IC50 Bioorg Med Chem (2017) 25: 4194-4202 [PMID:28645831]
ChEMBL Reversal of P-gp-mediated drug resistance in human KBV cells assessed as potentiation of paclitaxel-induced cytotoxicity by measuring paclitaxel IC50 at 10 uM after 72 hrs by MTT assay (Rvb = 398.34 +/- 0.58 uM) B 5.35 pIC50 4460 nM IC50 Eur J Med Chem (2019) 161: 364-377 [PMID:30384042]
ChEMBL Inhibition of ABCB1 in human K562/A02 cells assessed as potentiation of adriamycin-induced cytotoxicity by measuring ADR IC50 treated for 48 hrs followed by compound washout measured immediately by MTT assay (Rvb = 51.34 +/- 5.1 uM) B 5.52 pIC50 3020 nM IC50 Bioorg Med Chem (2017) 25: 4194-4202 [PMID:28645831]
ChEMBL Inhibition of ABCB1 in human K562/A02 cells assessed as potentiation of adriamycin-induced cytotoxicity by measuring ADR IC50 at 5 uM measured after 48 hrs by MTT assay (Rvb = 43.75 to 96.91 uM) B 5.71 pIC50 1970 nM IC50 Bioorg Med Chem (2017) 25: 4194-4202 [PMID:28645831]
ChEMBL Inhibition of ABCB1 in human K562/A02 cells assessed as potentiation of adriamycin-induced cytotoxicity by measuring ADR IC50 measured after 48 hrs by MTT assay (Rvb = 51.34 +/- 5.1 uM) B 5.8 pIC50 1600 nM IC50 Bioorg Med Chem (2017) 25: 4194-4202 [PMID:28645831]
ChEMBL Inhibition of human ABCB1 expressed in NCI-ADR-RES cells assessed as potentiation of doxorubicin-induced cytotoxicity by measuring doxorubicin IC50 at 1000 nM after 72 hrs by MTT assay (Rvb = 5.54 +/- 0.60 uM) B 6.62 pIC50 240 nM IC50 J Nat Prod (2016) 79: 2135-2142 [PMID:27504669]
ChEMBL Inhibition of ABCB1 in human KBV1 cells after 10 mins by Calcein-AM microplate assay B 6.65 pIC50 223 nM IC50 ACS Med. Chem. Lett. (2013) 4: 393-396 [PMID:24900683]
ChEMBL Inhibition of ABCB1 expressed in Kb-V1 cells after 10 mins by calcein-AM assay B 6.65 pIC50 223 nM IC50 Bioorg. Med. Chem. Lett. (2011) 21: 3654-3657 [PMID:21570282]
ChEMBL Inhibition of ABCB1 overexpressed in human KBv1 cells by flow cytometric-based calcein-AM efflux assay B 6.65 pIC50 223 nM IC50 J. Med. Chem. (2009) 52: 1190-1197 [PMID:19170519]
ChEMBL Inhibition of ABCB1 in human KBV1 cells assessed as inhibition of calcein-AM efflux B 6.66 pIC50 220 nM IC50 Eur. J. Med. Chem. (2016) 109: 124-133 [PMID:26774038]
ChEMBL Inhibition of MDR1 expressed in MDCK cells using rhodamine 123 staining by flow cytometry B 6.68 pIC50 210 nM IC50 Bioorg. Med. Chem. (2011) 19: 2090-2102 [PMID:21354800]
ChEMBL Inhibition of human Pgp in A2780 cells after 30 mins by Hoechst 33342 assay B 6.9 pIC50 125.89 nM IC50 Bioorg. Med. Chem. (2008) 16: 2448-2462 [PMID:18083034]
ChEMBL Inhibition of P-glycoprotein-mediated multidrug resistance in adriamycin-resistant human A2780/ADR cells by calcein AM assay B 7.11 pIC50 78 nM IC50 Bioorg. Med. Chem. (2009) 17: 2524-2535 [PMID:19250834]
ChEMBL Inhibition of P-gp in human adriamycin-resistant A2780 cells by Hoechst 33342 assay B 7.14 pIC50 72.44 nM IC50 Bioorg. Med. Chem. (2008) 16: 8224-8236 [PMID:18678495]
ChEMBL Inhibition of human ABCB1 expressed in KBV1 cells assessed as potentiation of doxorubicin-induced cytotoxicity by measuring doxorubicin IC50 at 1000 nM after 72 hrs by MTT assay (Rvb = 5.07 +/- 0.19 uM) B 7.15 pIC50 70 nM IC50 J Nat Prod (2016) 79: 2135-2142 [PMID:27504669]
ChEMBL Inhibition of Pgp by daunorubicin accumulation assay B 7.42 pIC50 38.02 nM IC50 Bioorg. Med. Chem. (2008) 16: 2448-2462 [PMID:18083034]
ChEMBL Inhibition of Pgp by daunorubicin accumulation assay B 7.42 pIC50 38 nM IC50 Bioorg. Med. Chem. (2008) 16: 2448-2462 [PMID:18083034]
ChEMBL Inhibition of P-glycoprotein-mediated daunorubicin efflux from human CCRF-CEM/VCR1000 cells after 240 secs by FACS flow cytometric analysis B 7.48 pIC50 33.11 nM IC50 J. Med. Chem. (2012) 55: 3261-3273 [PMID:22452412]
ChEMBL Inhibition of human ABCB1 expressed in NCI-ADR-RES cells assessed as potentiation of colchicine-induced cytotoxicity by measuring colchicine IC50 at 1000 nM after 72 hrs by MTT assay (Rvb = 1607.50 +/- 497.42 nM) B 7.6 pIC50 24.97 nM IC50 J Nat Prod (2016) 79: 2135-2142 [PMID:27504669]
ChEMBL Inhibition of human ABCB1 transfected in HEK293 cells assessed as potentiation of doxorubicin-induced cytotoxicity by measuring doxorubicin IC50 at 1000 nM after 72 hrs by CCK8 assay (Rvb = 504.65 +/- 44.94 nM) B 7.61 pIC50 24.77 nM IC50 J Nat Prod (2016) 79: 2135-2142 [PMID:27504669]
ChEMBL Inhibition of human ABCB1 expressed in NCI-ADR-RES cells assessed as potentiation of vincristine-induced cytotoxicity by measuring vincristine IC50 at 1000 nM after 72 hrs by MTT assay (Rvb = 3714.80 +/- 383.58 nM) B 7.73 pIC50 18.51 nM IC50 J Nat Prod (2016) 79: 2135-2142 [PMID:27504669]
ChEMBL Inhibition of human ABCB1 expressed in KBV1 cells assessed as potentiation of colchicine-induced cytotoxicity by measuring colchicine IC50 at 1000 nM after 72 hrs by MTT assay (Rvb = 487.57 +/- 30.54 nM) B 8.04 pIC50 9.05 nM IC50 J Nat Prod (2016) 79: 2135-2142 [PMID:27504669]
ChEMBL Inhibition of human ABCB1 expressed in KBV1 cells assessed as potentiation of vincristine-induced cytotoxicity by measuring vincristine IC50 at 1000 nM after 72 hrs by MTT assay (Rvb = 277.68 +/- 56.61 nM) B 9.18 pIC50 0.66 nM IC50 J Nat Prod (2016) 79: 2135-2142 [PMID:27504669]
ChEMBL Reversal of P-gp-mediated multidrug resistance to vinblastine in human CEM/VLB500 cells after 3 days by resazurin assay B 7.17 pEC50 68 nM EC50 Bioorg. Med. Chem. (2007) 15: 3854-3868 [PMID:17399990]
ChEMBL Activity at MDR1 (unknown origin) expressed in MDCK cells using calcein AM as substrate incubated for 30 mins prior to substrate addition measured after 30 mins by fluorometric analysis B 7.36 pEC50 44 nM EC50 Bioorg. Med. Chem. Lett. (2013) 23: 1370-1374 [PMID:23374872]
ChEMBL Inhibition of P-glycoprotein (unknown origin) expressed in MDCK cells assessed as reduction of calcein-AM transport after 30 mins by fluorescence assay B 7.36 pEC50 44 nM EC50 Eur. J. Med. Chem. (2014) 76: 558-566 [PMID:24607999]
P-glycoprotein 1 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3467] [UniProtKB: P06795]
ChEMBL Inhibition of mouse Pgp in EMT6/AR1.0 cells after 1 hr by daunorubicin accumulation assay B 7.19 pIC50 64.57 nM IC50 Bioorg. Med. Chem. (2008) 16: 2448-2462 [PMID:18083034]
ChEMBL Inhibition of mouse Pgp in EMT6/AR1.0 cells after 1 hr by daunorubicin accumulation assay B 7.19 pIC50 64 nM IC50 Bioorg. Med. Chem. (2008) 16: 2448-2462 [PMID:18083034]

ChEMBL data shown on this page come from version 28:

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]