ChEMBL ligand: CHEMBL270190 (ADL 8-2698, ADL-8-2698, Alvimopan, Alvimopan anhydrous, Alvimopan dihydrate, Anhydrous alvimopan, Entereg, LY-246736, LY246736, LY-246736 DIHYDRATE)
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!
Cav1.2/Voltage-gated L-type calcium channel alpha-1C subunit in Human [ChEMBL: CHEMBL1940] [GtoPdb: 529] [UniProtKB: Q13936] There should be some charts here, you may need to enable JavaScript!
Kv7.1/Voltage-gated potassium channel, IKs; KCNQ1(Kv7.1)/KCNE1(MinK) in Human [ChEMBL: CHEMBL2221347] [GtoPdb: 560] [UniProtKB: P15382, P51787] 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]
GtoPdb	-	-	7.92	pKi	12	nM	Ki	Bioorg Med Chem Lett (2008) 18: 2006-12 [PMID:18313920]
ChEMBL	Displacement of [3H]diprenorphine from human cloned delta opioid receptor	B	7.92	pKi	12	nM	Ki	Bioorg Med Chem Lett (2008) 18: 2006-2012 [PMID:18313920]
ChEMBL	Displacement of [3H]DPN from recombinant human delta opioid receptor expressed in CHOK1 cell membranes	B	8.3	pKi	5.01	nM	Ki	Bioorg Med Chem Lett (2017) 27: 2926-2930 [PMID:28499731]
κ receptor/Kappa opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL237] [GtoPdb: 318] [UniProtKB: P41145]
GtoPdb	-	-	7	pKi	100	nM	Ki	Bioorg Med Chem Lett (2008) 18: 2006-12 [PMID:18313920]
ChEMBL	Displacement of [3H]diprenorphine from human cloned kappa opioid receptor	B	7	pKi	100	nM	Ki	Bioorg Med Chem Lett (2008) 18: 2006-2012 [PMID:18313920]
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	8.3	pKi	5.01	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]DAMGO from human cloned mu-opioid receptor by radioligand binding assay	B	9.11	pKi	0.77	nM	Ki	Bioorg Med Chem Lett (2018) 28: 3283-3289 [PMID:30243589]
ChEMBL	Displacement of [3H]diprenorphine from human cloned mu opioid receptor	B	9.33	pKi	0.47	nM	Ki	Bioorg Med Chem Lett (2008) 18: 2006-2012 [PMID:18313920]
GtoPdb	-	-	9.33	pKi	0.47	nM	Ki	Bioorg Med Chem Lett (2008) 18: 2006-12 [PMID:18313920]
ChEMBL	Displacement of [3H]DPN from recombinant human mu opioid receptor expressed in CHOK1 cell membranes	B	9.5	pKi	0.32	nM	Ki	Bioorg Med Chem Lett (2017) 27: 2926-2930 [PMID:28499731]
ChEMBL	Antagonist activity at recombinant human MOR expressed in HEK293T cells assessed as reduction in DAMGO-induced inhibition of forskolin-stimulated cAMP level preincubated for 15 to 20 mins followed by DAMGO and forskolin addition by GloSensor assay	F	8.5	pIC50	3.16	nM	IC50	J Med Chem (2017) 60: 6733-6750 [PMID:28726402]
ChEMBL	Antagonist activity at recombinant human MOR expressed in HEK293T cells assessed as reduction in DAMGO-induced inhibition of forskolin-stimulated cAMP level preincubated for 15 to 20 mins followed by DAMGO and forskolin addition by GloSensor assay	F	8.52	pIC50	3	nM	IC50	J Med Chem (2017) 60: 6733-6750 [PMID:28726402]
ChEMBL	Antagonist activity at human cloned mu opioid receptor assessed as inhibition of loperamide-stimulated [35S]GTP-gamma-S binding	F	8.77	pIC50	1.7	nM	IC50	Bioorg Med Chem Lett (2008) 18: 2006-2012 [PMID:18313920]
Cav1.2/Voltage-gated L-type calcium channel alpha-1C subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1940] [GtoPdb: 529] [UniProtKB: Q13936]
ChEMBL	Inhibition of long-lasting type calcium current (hICa) in Chinese Hamster Ovary (CHO) cells expressing hCav1.2 measured using IonWorks Quattro automated patch clamp platform	F	5.3	pIC50	5011.87	nM	IC50	J Pharmacol Toxicol Methods (2014) 70: 246-254 [PMID:25087753]
Kv7.1/Voltage-gated potassium channel, IKs; KCNQ1(Kv7.1)/KCNE1(MinK) in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2221347] [GtoPdb: 560] [UniProtKB: P15382, P51787]
ChEMBL	Inhibition of slow delayed inward rectifying potassium current (Iks) in Chinese Hamster Ovary (CHO) cells expressing hKvLQT1/hminK measured using IonWorks Quattro automated patch clamp platform	F	4.3	pIC50	50118.72	nM	IC50	J Pharmacol Toxicol Methods (2014) 70: 246-254 [PMID:25087753]

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]