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ChEMBL ligand: CHEMBL348475 (Tariquidar, XR-9576, XR9576) |
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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 ABCG2 in topotecan-cultured human MCF7 cells using Hoechst 33342 as substrate measured after 2 hrs by fluorescence assay | B | 5.21 | pIC50 | 6223 | nM | IC50 | Eur J Med Chem (2020) 191: 112133-112133 [PMID:32105979] |
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 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 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 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 sulfasalazine-stimulated BCRP ATP ase activity (unknown origin) | B | 6.74 | pIC50 | 183.3 | nM | IC50 | J Med Chem (2021) 64: 3677-3693 [PMID:33729781] |
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] |
ABCC1/Multidrug resistance-associated protein 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3004] [GtoPdb: 779] [UniProtKB: P33527] | ||||||||
ChEMBL | Inhibition of NEM-GS-stimulated MRP1 ATPase activity (unknown origin) in presence of GSH | B | 4.62 | pIC50 | 23780 | nM | IC50 | J Med Chem (2021) 64: 3677-3693 [PMID:33729781] |
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 human ABCB1-mediated multidrug resistance in HEK293/MDR19 cells assessed as effect on colchicine-induced cytotoxicity at 1 uM by measuring colchine IC50 after 72 hrs by CCK8 assay (Rvb = 97.58 +/- 17.62 uM) | B | 5.11 | pIC50 | 7830 | nM | IC50 | J Nat Prod (2020) 83: 1461-1472 [PMID:32347726] |
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 sulfasalazine-stimulated ABCB1 ATPase activity (unknown origin) expressed in baculovirus infected Sf9 insect cells using ATP as substrate measured after 1 hr by colorimetric assay | B | 5.93 | pIC50 | >=1180 | nM | IC50 | Eur J Med Chem (2020) 191: 112133-112133 [PMID:32105979] |
ChEMBL | Reversal of P-gp-mediated multidrug resistance in human K562/A02 cells assessed as potentiation of adriamycin-induced cytotoxicity at 5 uM by measuring adriamycin IC50 after 48 hrs by MTT assay | B | 6.34 | pIC50 | 460 | nM | IC50 | J Med Chem (2021) 64: 6179-6197 [PMID:33938746] |
ChEMBL | Inhibition of ABCB1 in human KB-V1 cells using calcein-AM as substrate measured after 10 mins by fluorescence assay | B | 6.45 | pIC50 | 356 | nM | IC50 | Eur J Med Chem (2020) 191: 112133-112133 [PMID:32105979] |
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 paclitaxel stimulated- P-gp ATPase activity (unknown origin) | B | 7.49 | pIC50 | 32.7 | nM | IC50 | J Med Chem (2021) 64: 3677-3693 [PMID:33729781] |
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 | Reversal of P-glycoprotein mediated multidrug resistance in human KBV cells assessed as reversal of resistance to paclitaxel-induced cytotoxicity by measuring paclitaxel IC50 at 5 uM measured after 72 hrs by MTT assay | B | 8.12 | pIC50 | 7.57 | nM | IC50 | Eur J Med Chem (2021) 211: 113107-113107 [PMID:33360797] |
ChEMBL | Reversal of P-glycoprotein mediated multidrug resistance in human KBV cells assessed as reversal of resistance to paclitaxel-induced cytotoxicity by measuring paclitaxel IC50 at 10 uM measured after 72 hrs by MTT assay | B | 8.35 | pIC50 | 4.46 | nM | IC50 | Eur J Med Chem (2021) 211: 113107-113107 [PMID:33360797] |
ChEMBL | Reversal of P-glycoprotein mediated multidrug resistance in human KBV cells assessed as reversal of resistance to vincristine-induced cytotoxicity by measuring vincristine IC50 at 5 uM measured after 72 hrs by MTT assay | B | 8.48 | pIC50 | 3.34 | nM | IC50 | Eur J Med Chem (2021) 211: 113107-113107 [PMID:33360797] |
ChEMBL | Reversal of P-glycoprotein mediated multidrug resistance in human MCF-7T cells assessed as reversal of resistance to paclitaxel-induced cytotoxicity by measuring paclitaxel IC50 at 5 uM measured after 72 hrs by MTT assay | B | 8.49 | pIC50 | 3.26 | nM | IC50 | Eur J Med Chem (2021) 211: 113107-113107 [PMID:33360797] |
ChEMBL | Reversal of P-glycoprotein mediated multidrug resistance in human KBV cells assessed as reversal of resistance to vincristine-induced cytotoxicity by measuring vincristine IC50 at 10 uM measured after 72 hrs by MTT assay | B | 8.69 | pIC50 | 2.05 | nM | IC50 | Eur J Med Chem (2021) 211: 113107-113107 [PMID:33360797] |
ChEMBL | Reversal of P-glycoprotein mediated multidrug resistance in human MCF-7T cells assessed as reversal of resistance to vincristine-induced cytotoxicity by measuring vincristine IC50 at 5 uM measured after 72 hrs by MTT assay | B | 9.15 | pIC50 | 0.71 | nM | IC50 | Eur J Med Chem (2021) 211: 113107-113107 [PMID:33360797] |
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-glycoprotein mediated multidrug resistance in human MCF-7T cells assessed as reversal of resistance to paclitaxel-induced cytotoxicity by measuring paclitaxel IC50 at 10 uM measured after 72 hrs by MTT assay | B | 9.59 | pIC50 | 0.26 | nM | IC50 | Eur J Med Chem (2021) 211: 113107-113107 [PMID:33360797] |
ChEMBL | Reversal of P-glycoprotein mediated multidrug resistance in human MCF-7T cells assessed as reversal of resistance to vincristine-induced cytotoxicity by measuring vincristine IC50 at 10 uM measured after 72 hrs by MTT assay | B | 9.66 | pIC50 | 0.22 | nM | IC50 | Eur J Med Chem (2021) 211: 113107-113107 [PMID:33360797] |
ChEMBL | Activation of ABCB1 ATPase activity (unknown origin) expressed in baculovirus infected Sf9 insect cells using ATP as substrate measured after 1 hr by colorimetric assay | B | 6.68 | pEC50 | 211 | nM | EC50 | Eur J Med Chem (2020) 191: 112133-112133 [PMID:32105979] |
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] |
ChEMBL | Inhibition of P-gp (unknown origin) expressed in MES-SA/DX5 cells assessed as cell growth inhibition after 3 days in presence of 200 nM paclitaxel by MTT assay | B | 7.8 | pEC50 | 16 | nM | EC50 | J Med Chem (2021) 64: 3677-3693 [PMID:33729781] |
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 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]