ChEMBL ligand: CHEMBL348475 (XR-9576, Tariquidar, 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!
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 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, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños 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]