ChEMBL ligand: CHEMBL1186579 (Methylnaltrexone, Methylnaltrexone cation, Methylnaltrexone ion, MRZ-2663)
δ receptor/Delta opioid receptor in Human [ChEMBL: CHEMBL236] [GtoPdb: 317] [UniProtKB: P41143] There should be some charts here, you may need to enable JavaScript!
κ receptor/Kappa opioid receptor in Human [ChEMBL: CHEMBL237] [GtoPdb: 318] [UniProtKB: P41145] Kappa opioid receptor in Guinea pig [ChEMBL: CHEMBL3952] [UniProtKB: P41144] There should be some charts here, you may need to enable JavaScript!
μ receptor/Mu opioid receptor in Human [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372] 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
δ receptor/Delta opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL236] [GtoPdb: 317] [UniProtKB: P41143]
ChEMBL	Displacement of [3H]-DADLE from human recombinant delta opioid receptor by radioligand binding assay	B	5.46	pKi	3454	nM	Ki	J Med Chem (2022) 65: 4991-5003 [PMID:35255683]
GtoPdb	-	-	6.05	pKi	900	nM	Ki	Bioorg Med Chem Lett (2009) 19: 2289-94 [PMID:19282177]
ChEMBL	Displacement of [3H]DPN from recombinant human delta opioid receptor expressed in CHOK1 cell membranes	B	6.3	pKi	501.19	nM	Ki	Bioorg Med Chem Lett (2017) 27: 2926-2930 [PMID:28499731]
ChEMBL	Antagonist activity at human recombinant delta opioid receptor assessed as reduction in SNC80 induced [3S]-GTPgammaS binding	F	5	pEC50	>10000	nM	EC50	J Med Chem (2022) 65: 4991-5003 [PMID:35255683]
κ receptor/Kappa opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL237] [GtoPdb: 318] [UniProtKB: P41145]
ChEMBL	Displacement of [3H]-U69593 from human recombinant kappa opioid receptor by radioligand binding assay	B	7.49	pKi	32.1	nM	Ki	J Med Chem (2022) 65: 4991-5003 [PMID:35255683]
GtoPdb	-	-	8.2	pKi	6.3	nM	Ki	Bioorg Med Chem Lett (2009) 19: 2289-94 [PMID:19282177]
ChEMBL	Antagonist activity at human recombinant kappa opioid receptor assessed as reduction in U50,488H-induced [3S]-GTPgammaS binding	F	5	pEC50	>10000	nM	EC50	J Med Chem (2022) 65: 4991-5003 [PMID:35255683]
Kappa opioid receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3952] [UniProtKB: P41144]
ChEMBL	Displacement of [3H]DPN from guinea pig kappa opioid receptor expressed in CHOK1 cell membranes	B	7.7	pKi	19.95	nM	Ki	Bioorg Med Chem Lett (2017) 27: 2926-2930 [PMID:28499731]
μ receptor/Mu opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372]
ChEMBL	Displacement of [3H]DPN from recombinant human mu opioid receptor expressed in CHOK1 cell membranes	B	8.1	pKi	7.94	nM	Ki	Bioorg Med Chem Lett (2017) 27: 2926-2930 [PMID:28499731]
ChEMBL	Displacement of [3H]-DAMGO from human recombinant mu opioid receptor by radioligand binding assay	B	8.26	pKi	5.5	nM	Ki	J Med Chem (2022) 65: 4991-5003 [PMID:35255683]
GtoPdb	Displacement of [3H]DAMGO from human μ opioid receptors expressed in CHO cells	-	8.7	pKi	2	nM	Ki	Bioorg Med Chem Lett (2009) 19: 2289-94 [PMID:19282177]
ChEMBL	Antagonist activity at human recombinant mu opioid receptor assessed as reduction in DAMGO-induced [3S]-GTPgammaS binding	F	5	pEC50	>10000	nM	EC50	J Med Chem (2022) 65: 4991-5003 [PMID:35255683]

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]