alvimopan [Ligand Id: 7471] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL270190 (Alvimopan dihydrate, LY-246736, Alvimopan, LY246736, Entereg, ADL 8-2698, LY-246736 DIHYDRATE, ADL-8-2698)
  • δ receptor/Delta opioid receptor in Human [ChEMBL: CHEMBL236] [GtoPdb: 317] [UniProtKB: P41143]
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  • κ receptor/Kappa opioid receptor in Human [ChEMBL: CHEMBL237] [GtoPdb: 318] [UniProtKB: P41145]
  • Kappa opioid receptor in Guinea pig [ChEMBL: CHEMBL3952] [UniProtKB: P41144]
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  • μ receptor/Mu opioid receptor in Human [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372]
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  • Cav1.2/Voltage-gated L-type calcium channel alpha-1C subunit in Human [ChEMBL: CHEMBL1940] [GtoPdb: 529] [UniProtKB: Q13936]
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  • Kv7.1/Voltage-gated potassium channel, IKs; KCNQ1(Kv7.1)/KCNE1(MinK) in Human [ChEMBL: CHEMBL2221347] [GtoPdb: 560] [UniProtKB: P15382P51787]
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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]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 B 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 B 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: P15382P51787]
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 27:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]