ChEMBL ligand: CHEMBL348475 (Tariquidar, XR-9576, XR9576)
ABCG2/ATP-binding cassette sub-family G member 2 in Human [ChEMBL: CHEMBL5393] [GtoPdb: 792] [UniProtKB: Q9UNQ0] There should be some charts here, you may need to enable JavaScript!
ABCC1/Multidrug resistance-associated protein 1 in Human [ChEMBL: CHEMBL3004] [GtoPdb: 779] [UniProtKB: P33527] There should be some charts here, you may need to enable JavaScript!
ABCB1/P-glycoprotein 1 in Human [ChEMBL: CHEMBL4302] [GtoPdb: 768] [UniProtKB: P08183] P-glycoprotein 1 in Mouse [ChEMBL: CHEMBL3467] [UniProtKB: P06795] There should be some charts here, you may need to enable JavaScript!

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 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 P-gp-mediated multidrug resistance in doxorubicin-resistant human MCF7/ADR cells assessed as potentiation of doxorubicin-induced cytotoxicity by measuring doxorubicin IC50 incubated for 48 hrs by CCK-8 assay	B	6.76	pIC50	174	nM	IC50	J Med Chem (2023) 66: 5550-5566 [PMID:37011035]
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 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]