ChEMBL ligand: CHEMBL396298 (Elacridar, LY-335979, LY335979)
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] 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 MDCK cells by pheophorbide A assay	B	6.37	pIC50	430	nM	IC50	Bioorg Med Chem Lett (2010) 20: 180-183 [PMID:19932960]
ChEMBL	Inhibition of ABCG2 expressed in HEK293 cells assessed as mitoxantrone-mediated efflux by flow cytometry	B	6.39	pIC50	410	nM	IC50	Bioorg Med Chem (2007) 15: 2892-2897 [PMID:17317193]
ChEMBL	Inhibition of BCRP expressed in MCF7 MX cells by Hoechst 33342 staining	B	6.4	pIC50	400	nM	IC50	Bioorg Med Chem Lett (2010) 20: 180-183 [PMID:19932960]
ChEMBL	Inhibition of sulfasalazine-stimulated BCRP ATP ase activity (unknown origin)	B	6.6	pIC50	252.2	nM	IC50	J Med Chem (2021) 64: 3677-3693 [PMID:33729781]
ChEMBL	Inhibition of ABCG2 overexpressed in human MCF7/Topo cells by flow cytometric-based mitoxantrone efflux assay	B	6.6	pIC50	250	nM	IC50	J Med Chem (2009) 52: 1190-1197 [PMID:19170519]
GtoPdb	-	-	6.71	pIC50	193	nM	IC50	ACS Med Chem Lett (2013) 4: 393-6 [PMID:24900683]
ChEMBL	Inhibition of ABCG2 expressed in human MCF7/Topo cells by Hoechst microplate assay	B	6.9	pIC50	127	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	6.9	pIC50	127	nM	IC50	ACS Med Chem Lett (2013) 4: 393-396 [PMID:24900683]
GtoPdb	-	-	6.9	pIC50	127	nM	IC50	Bioorg Med Chem Lett (2011) 21: 3654-7 [PMID:21570282]
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	5.38	pIC50	>4128	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]
GtoPdb	Inhibition of digoxin transport in Caco-2 cells	-	7.4	pKi	40	nM	Ki	Pharm Res (2003) 20: 161-8 [PMID:12636153]
ChEMBL	Inhibition of ABCB1-mediated [3H]vinblastine transportation in human Caco-2 cells	B	5.7	pIC50	2000	nM	IC50	J Med Chem (2008) 51: 7602-7613 [PMID:19053888]
ChEMBL	Inhibition of ABCB1 overexpressed in human KBv1 cells by flow cytometric-based calcein-AM efflux assay	B	6.71	pIC50	193	nM	IC50	J Med Chem (2009) 52: 1190-1197 [PMID:19170519]
ChEMBL	Inhibition of ABCB1 expressed in Kb-V1 cells after 10 mins by calcein-AM assay	B	6.71	pIC50	193	nM	IC50	Bioorg Med Chem Lett (2011) 21: 3654-3657 [PMID:21570282]
ChEMBL	Inhibition of ABCB1 in human KBV1 cells after 10 mins by Calcein-AM microplate assay	B	6.71	pIC50	193	nM	IC50	ACS Med Chem Lett (2013) 4: 393-396 [PMID:24900683]
ChEMBL	Inhibition of P-glycoprotein-mediated daunorubicin efflux from human CCRF-CEM/VCR1000 cells after 240 secs by FACS flow cytometric analysis	B	7.14	pIC50	72.44	nM	IC50	J Med Chem (2012) 55: 3261-3273 [PMID:22452412]
ChEMBL	Inhibition of paclitaxel stimulated- P-gp ATPase activity (unknown origin)	B	8.31	pIC50	4.9	nM	IC50	J Med Chem (2021) 64: 3677-3693 [PMID:33729781]
ChEMBL	Inhibition of Pgp measured as inhibition of [3H]vinblastine basolateral to apical transport in Caco-2 cells	F	5.7	pEC50	2000	nM	EC50	J Med Chem (2006) 49: 6607-6613 [PMID:17064079]
ChEMBL	Inhibition of human P-glycoprotein mediated [3H]vinblastine transport in human Caco-2 cells	B	5.7	pEC50	2000	nM	EC50	J Med Chem (2008) 51: 1415-1422 [PMID:18257545]
ChEMBL	Inhibition of human Pgp mediated [3H]vinblastine transport in human Caco-2 cells	B	5.7	pEC50	2000	nM	EC50	Bioorg Med Chem (2008) 16: 362-373 [PMID:17936633]

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]