ChEMBL ligand: CHEMBL15177 (L-660711, MK-571)
ABCC2/Canalicular multispecific organic anion transporter 1 in Human [ChEMBL: CHEMBL5748] [GtoPdb: 780] [UniProtKB: Q92887] ABCC2/Canalicular multispecific organic anion transporter 1 in Rat [ChEMBL: CHEMBL2073676] [GtoPdb: 780] [UniProtKB: Q63120] There should be some charts here, you may need to enable JavaScript!
Cysteinyl leukotriene receptor 1 in Guinea pig [ChEMBL: CHEMBL5645] [UniProtKB: Q2NNR5] 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!
ABCC4/Multidrug resistance-associated protein 4 in Human [ChEMBL: CHEMBL1743128] [GtoPdb: 782] [UniProtKB: O15439] There should be some charts here, you may need to enable JavaScript!
ABCC5/Multidrug resistance-associated protein 5 in Human [ChEMBL: CHEMBL2046258] [GtoPdb: 783] [UniProtKB: O15440] There should be some charts here, you may need to enable JavaScript!
CysLT1 receptor in Human [GtoPdb: 269] [UniProtKB: Q9Y271] 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
ABCC2/Canalicular multispecific organic anion transporter 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5748] [GtoPdb: 780] [UniProtKB: Q92887]
ChEMBL	TP_TRANSPORTER: inhibition of Vinblastine transepithelial transport (basal to apical) in MRP2-expressing MDCK cells	F	4.58	pKi	26400	nM	Ki	Pharm Res (2002) 19: 773-779 [PMID:12134946]
ChEMBL	TP_TRANSPORTER: inhibition of LTC4 uptake in membrane vesicles from MRP2-expressing LLC PK1 cells	F	4.88	pKi	13100	nM	Ki	Mol Pharmacol (1999) 56: 1219-1228 [PMID:10570049]
ChEMBL	Inhibition of human MRP2-mediated estradiol-17-beta-glucuronide transport in Sf9 cells inverted membrane vesicles	B	5	pIC50	10000	nM	IC50	J Med Chem (2008) 51: 3275-3287 [PMID:18457386]
ChEMBL	TP_TRANSPORTER: inhibition of PAH uptake (PAH: 0.1uM) in membrane vesicles from MRP2-expressing HEK cells	F	5.4	pIC50	4000	nM	IC50	Kidney Int (2000) 57: 1636-1642 [PMID:10760098]
ChEMBL	Inhibition of ABCC2 overexpressed in MDCK cells at 100 uM by flow cytometric-based chloromethylfluorescein-diacetate accumulation assay	B	6	pIC50	>1000	nM	IC50	J Med Chem (2009) 52: 1190-1197 [PMID:19170519]
ABCC2/Canalicular multispecific organic anion transporter 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2073676] [GtoPdb: 780] [UniProtKB: Q63120]
ChEMBL	TP_TRANSPORTER: inhibition of E217betaG uptake (E217betaG: 0.055 uM) in membrane vesicles from Mrp2-expressing Sf9 cells	F	5.58	pIC50	2620	nM	IC50	Mol Pharmacol (2001) 59: 1077-1085 [PMID:11306690]
Cysteinyl leukotriene receptor 1 in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5645] [UniProtKB: Q2NNR5]
ChEMBL	Inhibition of Leukotriene D4 induced contraction of guinea-pig trachea was determined	F	8.8	pKd	1.58	nM	Kd	Bioorg Med Chem Lett (1992) 2: 1141-1146
ChEMBL	Binding affinity against Cysteinyl leukotriene D4 receptor from guinea pig trachea using [3H]LTD4	B	9	pKd	1	nM	Kd	J Med Chem (1990) 33: 1194-1200 [PMID:2157010]
ChEMBL	Compound was evaluated for its ability to displace [3H]LTD4 from Cysteinyl leukotriene D4 receptor in guinea pig lung membranes	B	9.7	pKi	0.2	nM	Ki	J Med Chem (1991) 34: 1235-1242 [PMID:1849993]
ChEMBL	Inhibitory concentration against [3H]Leukotriene D4 binding to guinea-pig lung membranes was determined	B	8.41	pIC50	3.9	nM	IC50	Bioorg Med Chem Lett (1992) 2: 1141-1146
ChEMBL	Inhibitory concentration against [3H]Leukotriene D4 binding to guinea-pig lung membranes was determined	B	8.52	pIC50	3	nM	IC50	Bioorg Med Chem Lett (1992) 2: 1141-1146
ChEMBL	In vitro inhibition of [3H]LTD4 binding to guinea pig lung membranes	B	9.1	pIC50	0.8	nM	IC50	J Med Chem (1992) 35: 3832-3844 [PMID:1331447]
ABCC1/Multidrug resistance-associated protein 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3004] [GtoPdb: 779] [UniProtKB: P33527]
ChEMBL	Inhibition of MRP1-mediated transport of [3H]LTC4 expressed in human HeLa T5 cells by liquid scintillation counting	B	6.22	pKi	600	nM	Ki	J Med Chem (2009) 52: 4586-4595 [PMID:19580319]
ChEMBL	TP_TRANSPORTER: inhibition of GSSG uptake in membrane vesicle from MRP1-expressing HeLa cells	F	6.22	pKi	600	nM	Ki	Biochem J (1996) 314: 433-437 [PMID:8670053]
ChEMBL	TP_TRANSPORTER: inhibition of LTC4 uptake in membrane vesicle from MRP1-expressing HeLa cells	F	6.22	pKi	600	nM	Ki	Cancer Res (1996) 56: 988-994 [PMID:8640791]
ChEMBL	Reversal of human ABCC1-mediated multidrug resistance in HEK293/MRP1 cells assessed as effect on etoposide-induced cytotoxicity by measuring etoposide IC50 at 25 uM after 72 hrs by CCK8 assay (Rvb = 63.34 +/- 7.92 uM)	B	4.93	pIC50	11870	nM	IC50	J Nat Prod (2020) 83: 1461-1472 [PMID:32347726]
ChEMBL	Inhibition of human ABCC1 transfected in HEK293 cells assessed as potentiation of etoposide-induced cytotoxicity by measuring etoposide IC50 at 25000 nM after 72 hrs by CCK8 assay (Rvb = 38.54 +/- 5.62 nM)	B	5.28	pIC50	5220	nM	IC50	J Nat Prod (2016) 79: 2135-2142 [PMID:27504669]
ChEMBL	Inhibition of recombinant MRP1 expressed in human HeLa T5 cells assessed as ATP-dependent transport of [3H]para-aminohippurate	B	5.48	pIC50	3300	nM	IC50	J Med Chem (2009) 52: 4586-4595 [PMID:19580319]
ChEMBL	TP_TRANSPORTER: inhibition of Daunorubicin uptake (Daunorubicin: 0.6 uM) in membrane vesicles from GLC4/ADR cells	F	6.4	pIC50	400	nM	IC50	Br J Pharmacol (1999) 126: 681-688 [PMID:10188979]
ChEMBL	Inhibition of MRP1 in human 2008/MRP1 cells assessed as potentiation of doxorubicin-induced cytotoxicity by measuring reduction in cell survival after 5 days by MTS assay	B	4.72	pEC50	19000	nM	EC50	J Med Chem (2018) 61: 9931-9951 [PMID:30351934]
ChEMBL	Modulation of MRP1 mediated drug efflux in doxorubicin-resistant human H69 cells assessed as accumulation of calcein AM incubated for 15 mins prior to calcein AM addition measured after 30 mins by fluorescence analysis	B	4.91	pEC50	12400	nM	EC50	Bioorg Med Chem (2014) 22: 5860-5870 [PMID:25311564]
ChEMBL	Inhibition of MRP1 expressed in MDCK cells assessed as calcein AM accumulation by fluorescence assay	B	5.55	pEC50	2850	nM	EC50	J Med Chem (2010) 53: 5467-5475 [PMID:20684594]
ABCC4/Multidrug resistance-associated protein 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1743128] [GtoPdb: 782] [UniProtKB: O15439]
ChEMBL	TP_TRANSPORTER: inhibition of 9-(2-phosphonomethoxyethyl)adenine(PMEA) efflux (PMEA: 1 uM) in MRP4-expressing HEK293 cells	F	5	pIC50	10000	nM	IC50	Mol Pharmacol (2003) 63: 1094-1103 [PMID:12695538]
ABCC5/Multidrug resistance-associated protein 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2046258] [GtoPdb: 783] [UniProtKB: O15440]
ChEMBL	TP_TRANSPORTER: inhibition of 9-(2-phosphonomethoxyethyl)adenine(PMEA) efflux (PMEA: 1 uM) in MRP5-expressing HEK293 cells	F	4.4	pIC50	40000	nM	IC50	Mol Pharmacol (2003) 63: 1094-1103 [PMID:12695538]
CysLT1 receptor in Human [GtoPdb: 269] [UniProtKB: Q9Y271]
GtoPdb	Antagonism of [3H]LTD4 binding in COS-7 cells.	-	8	pIC50	10	nM	IC50	Nature (1999) 399: 789-93 [PMID:10391245]

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]