alvimopan [Ligand Id: 7471] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL270190 (ADL 8-2698, ADL-8-2698, Alvimopan, Alvimopan anhydrous, Alvimopan dihydrate, Anhydrous alvimopan, Entereg, LY-246736, LY246736, LY-246736 DIHYDRATE) |
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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 | 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 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]
