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 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]