salvinorin A [Ligand Id: 1666] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL445332 (Divinorin a, Salvinorin, (-)-salvinorin a, Salvinorin a) |
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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] | ||||||||
| ChEMBL | Displacement of [3H]DADLE from delta opioid receptor expressed in HEK293 cells | B | 5 | pKi | >10000 | nM | Ki | Bioorg Med Chem Lett (2011) 21: 160-163 [PMID:21115248] |
| ChEMBL | Displacement of [3H]DADLE from delta opioid receptor | B | 5 | pKi | >10000 | nM | Ki | J Nat Prod (2011) 74: 718-726 [PMID:21338114] |
| ChEMBL | Displacement of [3H]DADLE from human recombinant delta opioid receptor expressed in CHO cells after 2 hrs by liquid scintillation counting | B | 5 | pKi | >10000 | nM | Ki | Bioorg Med Chem (2012) 20: 3100-3110 [PMID:22464684] |
| ChEMBL | Displacement of [3H]DADLE from delta opioid receptor (unknown origin) | B | 5 | pKi | >10000 | nM | Ki | Bioorg Med Chem Lett (2013) 23: 2860-2862 [PMID:23587424] |
| ChEMBL | Inhibition of [125I]- IOXY binding to human Opioid receptor delta1 | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2005) 48: 4765-4771 [PMID:16033256] |
| ChEMBL | Displacement of [125]OXY from delta opioid receptor | B | 5.24 | pKi | 5790 | nM | Ki | J Nat Prod (2006) 69: 914-918 [PMID:16792410] |
| ChEMBL | Displacement of [125I]IOXY from human recombinant delta opioid receptor expressed in CHO cells | B | 5.24 | pKi | 5790 | nM | Ki | J Med Chem (2008) 51: 2421-2431 [PMID:18380425] |
| ChEMBL | Inhibition of [125I]- IOXY binding to human Opioid receptor delta1 | B | 5.24 | pKi | 5790 | nM | Ki | J Med Chem (2005) 48: 4765-4771 [PMID:16033256] |
| ChEMBL | Displacement of [125I]IOXY from human recombinant delta opioid receptor expressed in CHO cells | B | 5.4 | pKi | 3990 | nM | Ki | J Med Chem (2008) 51: 2421-2431 [PMID:18380425] |
| ChEMBL | Agonist activity at human delta opiod receptor expressed in CHO-K1 cells assessed as increase in forskolin induced cAMP production measured after 30 mins by HitHunter luminescence based assay | F | 5 | pEC50 | >10000 | nM | EC50 | J Med Chem (2016) 59: 11027-11038 [PMID:27958743] |
| δ receptor/Delta opioid receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3222] [GtoPdb: 317] [UniProtKB: P32300] | ||||||||
| ChEMBL | Displacement of [3H]diprenorphine from mouse delta opioid receptor expressed in HEK293 cells | B | 4.6 | pKi | >25000 | nM | Ki | J Med Chem (2008) 51: 1824-1830 [PMID:18293909] |
| ChEMBL | Displacement of [3H]diprenorphine from mouse delta opioid receptor expressed in CHO cells | B | 6 | pKi | >1000 | nM | Ki | Bioorg Med Chem (2008) 16: 1279-1286 [PMID:17981041] |
| ChEMBL | Binding affinity to mouse DOPR expressed in CHO cells | B | 6 | pKi | >1000 | nM | Ki | Bioorg Med Chem (2009) 17: 1370-1380 [PMID:19147366] |
| ChEMBL | Displacement of [3H]diprenorphine from FLAG-tagged mouse delta opioid receptor expressed in CHO cell membranes | B | 6 | pKi | >1000 | nM | Ki | Bioorg Med Chem Lett (2015) 25: 4689-4692 [PMID:26330078] |
| κ receptor/Kappa opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL237] [GtoPdb: 318] [UniProtKB: P41145] | ||||||||
| ChEMBL | Inhibition of [125I]- IOXY binding to human Opioid receptor kappa1 | B | 7.42 | pKi | 38 | nM | Ki | J Med Chem (2005) 48: 4765-4771 [PMID:16033256] |
| ChEMBL | Binding affinity to kappa opioid receptor (unknown origin) expressed in HEK293 cells by radioligand displacement assay | B | 7.8 | pKi | 16 | nM | Ki | J Nat Prod (2014) 77: 678-689 [PMID:24559070] |
| ChEMBL | Displacement of [3H]U69593 from human recombinant kappa opioid receptor expressed in CHO cells after 2 hrs by liquid scintillation counting | B | 8.13 | pKi | 7.4 | nM | Ki | Bioorg Med Chem (2012) 20: 3100-3110 [PMID:22464684] |
| ChEMBL | Displacement of [3H]U69593 from kappa opioid receptor | B | 8.13 | pKi | 7.4 | nM | Ki | J Nat Prod (2011) 74: 718-726 [PMID:21338114] |
| ChEMBL | Displacement of [3H]U69593 from kappa opioid receptor (unknown origin) | B | 8.21 | pKi | 6.2 | nM | Ki | Bioorg Med Chem Lett (2013) 23: 2860-2862 [PMID:23587424] |
| ChEMBL | Displacement of [125I]IOXY from human recombinant kappa opioid receptor expressed in CHO cells | B | 8.24 | pKi | 5.7 | nM | Ki | J Med Chem (2008) 51: 2421-2431 [PMID:18380425] |
| ChEMBL | Displacement of [3H]U69593 from kappa opioid receptor (unknown origin) | B | 8.49 | pKi | 3.2 | nM | Ki | Bioorg Med Chem Lett (2014) 24: 576-579 [PMID:24365159] |
| ChEMBL | Displacement of [3H]U69593 from kappa opioid receptor (unknown origin) | B | 8.5 | pKi | 3.16 | nM | Ki | Bioorg Med Chem Lett (2014) 24: 576-579 [PMID:24365159] |
| ChEMBL | Displacement of [3H]diprenorphine from human KOPR expressed in CHO cells | B | 8.52 | pKi | 3 | nM | Ki | Bioorg Med Chem Lett (2012) 22: 1023-1026 [PMID:22204910] |
| ChEMBL | Displacement of [3H]U69593 from kappa opioid receptor (unknown origin) expressed in HEK293T cells after 1.5 hrs by radioligand binding assay | B | 8.54 | pKi | 2.9 | nM | Ki | Eur J Med Chem (2014) 85: 818-829 [PMID:25193297] |
| ChEMBL | Inhibition of [3H]diprenorphine binding to human KOR expressed in CHO cells | B | 8.59 | pKi | 2.6 | nM | Ki | Bioorg Med Chem Lett (2006) 16: 4679-4685 [PMID:16777411] |
| ChEMBL | Displacement of [3H]diprenorphine from human KOPR expressed in CHO cells | B | 8.6 | pKi | 2.5 | nM | Ki | Bioorg Med Chem (2009) 17: 1370-1380 [PMID:19147366] |
| ChEMBL | Displacement of [3H]diprenorphine from human kappa opioid receptor expressed in CHO cells | B | 8.62 | pKi | 2.4 | nM | Ki | Bioorg Med Chem (2008) 16: 1279-1286 [PMID:17981041] |
| GtoPdb | - | - | 8.7 | pKi | - | - | - |
Proc Natl Acad Sci USA (2002) 99: 11934-9 [PMID:12192085]; Bioorg Med Chem Lett (2005) 15: 2761-5 [PMID:15869877] |
| ChEMBL | Inhibition of [125I]- IOXY binding to human Opioid receptor kappa1 | B | 8.72 | pKi | 1.9 | nM | Ki | J Med Chem (2005) 48: 4765-4771 [PMID:16033256] |
| ChEMBL | Binding affinity to kappa opioid receptor | B | 8.72 | pKi | 1.9 | nM | Ki | Bioorg Med Chem (2010) 18: 4446-4452 [PMID:20478711] |
| ChEMBL | Displacement of [125]OXY from kappa opioid receptor | B | 8.72 | pKi | 1.9 | nM | Ki | J Nat Prod (2006) 69: 914-918 [PMID:16792410] |
| ChEMBL | Displacement of [125I]IOXY from human recombinant kappa opioid receptor expressed in CHO cells | B | 8.72 | pKi | 1.9 | nM | Ki | J Med Chem (2008) 51: 2421-2431 [PMID:18380425] |
| ChEMBL | Displacement of [3H]diprenorphine from human kappa opioid receptor expressed in CHO cell membranes | B | 8.89 | pKi | 1.3 | nM | Ki | Bioorg Med Chem Lett (2015) 25: 4689-4692 [PMID:26330078] |
| ChEMBL | Inhibition of [3H]diprenorphine binding to human Opioid receptor kappa 1 expressed in chinese hamster ovary cells | B | 8.89 | pKi | 1.3 | nM | Ki | Bioorg Med Chem Lett (2005) 15: 2761-2765 [PMID:15869877] |
| ChEMBL | Inhibition of [3H]diprenorphine binding to human KOR expressed in CHO cells | B | 8.89 | pKi | 1.3 | nM | Ki | Bioorg Med Chem Lett (2006) 16: 4679-4685 [PMID:16777411] |
| ChEMBL | Displacement of [3H]diprenorphine binding from human kappa opioid receptor expressed in CHO cells | B | 8.89 | pKi | 1.3 | nM | Ki | Bioorg Med Chem Lett (2006) 16: 5498-5502 [PMID:16945525] |
| ChEMBL | Displacement of [3H]U69593 from kappa opioid receptor expressed in HEK293 cells by visible spectrophotometry | B | 9.1 | pKi | 0.8 | nM | Ki | Bioorg Med Chem (2009) 17: 6671-6681 [PMID:19683449] |
| ChEMBL | Displacement of [3H]U69593 from kappa opioid receptor expressed in HEK293 cells | B | 9.12 | pKi | 0.75 | nM | Ki | Bioorg Med Chem Lett (2011) 21: 160-163 [PMID:21115248] |
| ChEMBL | Antagonist activity at human kappa opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assay | F | 7.35 | pEC50 | 45 | nM | EC50 | J Med Chem (2007) 50: 3596-3603 [PMID:17580847] |
| ChEMBL | Agonist activity at human kappa opioid receptor expressed in CHO cells by [35S]GTPgammaS binding | F | 7.35 | pEC50 | 45 | nM | EC50 | J Nat Prod (2006) 69: 107-112 [PMID:16441078] |
| ChEMBL | Agonist activity at KOR (unknown origin) | B | 7.4 | pEC50 | 40 | nM | EC50 | Bioorg Med Chem Lett (2014) 24: 4895-4898 [PMID:25248680] |
| ChEMBL | Agonist activity at human recombinant kappa opioid receptor expressed in CHO cells assessed as [35S]GTP-gamma-S binding after 3 hrs by liquid scintillation counting | F | 7.4 | pEC50 | 40 | nM | EC50 | Bioorg Med Chem (2012) 20: 3100-3110 [PMID:22464684] |
| ChEMBL | Stimulation of [35S]GTP-gamma-S, binding to Opioid receptor kappa1 expressed in CHO cells | F | 7.4 | pEC50 | 40 | nM | EC50 | J Med Chem (2005) 48: 4765-4771 [PMID:16033256] |
| ChEMBL | Agonist activity at human recombinant kappa opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assay | F | 7.4 | pEC50 | 40 | nM | EC50 | J Med Chem (2008) 51: 2421-2431 [PMID:18380425] |
| ChEMBL | Agonist activity at human KOPR expressed in U2OS cells assessed as beta-arrestin2 recruitment after 90 mins by DiscoveRx PathHunter assay | F | 7.51 | pEC50 | 31 | nM | EC50 | Bioorg Med Chem Lett (2012) 22: 1023-1026 [PMID:22204910] |
| ChEMBL | Agonist activity at kappa opioid receptor (unknown origin) assessed as increase in venus-tagged N-terminal beta-arrestin-2 recruitment by BRET assay | B | 8 | pEC50 | 10 | nM | EC50 | J Med Chem (2018) 61: 9841-9878 [PMID:29939744] |
| ChEMBL | Agonist activity at human kappa opioid receptor expressed in CHO cells assessed as increase of [35S]GTPgammaS binding | F | 8.12 | pEC50 | 7.5 | nM | EC50 | Bioorg Med Chem Lett (2010) 20: 5749-5752 [PMID:20801035] |
| ChEMBL | Agonist activity at human KOPR expressed in CHO cells assessed as [35S]GTPgammaS binding after 60 mins by liquid scintillation counting | F | 8.16 | pEC50 | 6.9 | nM | EC50 | Bioorg Med Chem Lett (2012) 22: 1023-1026 [PMID:22204910] |
| ChEMBL | Agonist activity at human recombinant kappa opioid receptor expressed in CHO cells assessed as calcium mobilization after 1 hrs by fluorescence analysis | F | 8.21 | pEC50 | 6.11 | nM | EC50 | Bioorg Med Chem (2012) 20: 3100-3110 [PMID:22464684] |
| ChEMBL | Agonist activity at Tango-KOR (unknown origin) expressed in HTLA cells harboring TEV-fused-beta-arrestin 2 assessed as increase in beta arrestin 2 recruitment after overnight incubation by BrightGlo reagent based assay | B | 8.29 | pEC50 | 5.1 | nM | EC50 | J Med Chem (2019) 62: 893-907 [PMID:30543421] |
| ChEMBL | Agonist activity at kappa opioid receptor in human HEK293 cells assessed as stimulation of Galphai signaling by cAMP assay | F | 8.3 | pEC50 | 5 | nM | EC50 | Bioorg Med Chem Lett (2013) 23: 2860-2862 [PMID:23587424] |
| ChEMBL | Activity at human kappa opioid receptor expressed in HEK293 cells as intracellular calcium mobilization | F | 8.32 | pEC50 | 4.77 | nM | EC50 | Bioorg Med Chem Lett (2007) 17: 2229-2232 [PMID:17303418] |
| ChEMBL | Agonist activity at kappa opioid receptor (unknown origin) expressed in HEK cells co-expressing luciferase based cAMP biosensor assessed as increase in cAMP accumulation after 20 to 30 mins by luciferase reporter gene assay | F | 8.33 | pEC50 | 4.7 | nM | EC50 | J Med Chem (2018) 61: 9841-9878 [PMID:29939744] |
| ChEMBL | Enhancement of [35S]GTP-gamma-S binding to human KOR expressed in CHO cells | F | 8.35 | pEC50 | 4.5 | nM | EC50 | Bioorg Med Chem Lett (2006) 16: 4679-4685 [PMID:16777411] |
| ChEMBL | Agonist activity at human kappa opioid receptor expressed in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding | F | 8.35 | pEC50 | 4.5 | nM | EC50 | Bioorg Med Chem Lett (2015) 25: 4689-4692 [PMID:26330078] |
| ChEMBL | Binding potency at human kappa opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay | F | 8.35 | pEC50 | 4.5 | nM | EC50 | Bioorg Med Chem Lett (2006) 16: 5498-5502 [PMID:16945525] |
| ChEMBL | Effective concentration for activation of human Opioid receptor kappa 1 expressed in chinese hamster ovary cells to enhance [35S]GTP-gamma-S, binding | F | 8.35 | pEC50 | 4.5 | nM | EC50 | Bioorg Med Chem Lett (2005) 15: 2761-2765 [PMID:15869877] |
| ChEMBL | Activity at human kappa opioid receptor expressed in HEK293 cells as intracellular calcium mobilization | F | 8.55 | pEC50 | 2.82 | nM | EC50 | Bioorg Med Chem Lett (2007) 17: 2229-2232 [PMID:17303418] |
| ChEMBL | Enhancement of [35S]GTP-gamma-S binding to human KOR expressed in CHO cells | F | 8.66 | pEC50 | 2.2 | nM | EC50 | Bioorg Med Chem Lett (2006) 16: 4679-4685 [PMID:16777411] |
| ChEMBL | Agonist activity at human KOPR expressed in CHO cells assessed as enhancement of [35S]GTPgammaS binding | F | 8.68 | pEC50 | 2.1 | nM | EC50 | Bioorg Med Chem (2009) 17: 1370-1380 [PMID:19147366] |
| ChEMBL | Agonist activity at human kappa opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding | F | 8.74 | pEC50 | 1.8 | nM | EC50 | Bioorg Med Chem (2008) 16: 1279-1286 [PMID:17981041] |
| ChEMBL | Agonist activity at human kappa opioid receptor expressed CHO cells co-expressing Galphaq16 assessed as calcium mobilization by fluorescence assay | F | 8.77 | pEC50 | 1.7 | nM | EC50 | J Nat Prod (2014) 77: 1817-1824 [PMID:25075762] |
| ChEMBL | Agonist activity at human kappa opioid receptor assessed as inhibition of Galpha-16-induced calcium flux | F | 8.91 | pEC50 | 1.24 | nM | EC50 | Bioorg Med Chem Lett (2007) 17: 6111-6115 [PMID:17904842] |
| ChEMBL | Agonist activity at human kappa opioid receptor-Galpha-16 fusion protein expressed in CHO cells by calcium flux assay | F | 9.09 | pEC50 | 0.81 | nM | EC50 | J Nat Prod (2006) 69: 107-112 [PMID:16441078] |
| ChEMBL | Inhibition of human kappa opioid receptor expressed in HEK293T cells assessed as inhibition of cAMP production after 30 mins | F | 9.44 | pEC50 | 0.36 | nM | EC50 | Eur J Med Chem (2014) 85: 818-829 [PMID:25193297] |
| ChEMBL | Agonist activity at human kappa-type opioid receptor expressed in CHO-K1 cells assessed as forskolin-induced cAMP accumulation after 30 mins in presence of forskolin by luminescence-based HitHunter cAMP assay | F | 9.68 | pEC50 | 0.21 | nM | EC50 | J Med Chem (2017) 60: 3866-3878 [PMID:28376298] |
| ChEMBL | Agonist activity at kappa opioid receptor expressed in HEK293 cells by [35S]GTPgammaS binding assay | F | 9.7 | pEC50 | 0.2 | nM | EC50 | Bioorg Med Chem Lett (2011) 21: 160-163 [PMID:21115248] |
| ChEMBL | Agonist activity at human kappa-type opioid receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by luminescence-based assay | F | 10.38 | pEC50 | 0.04 | nM | EC50 | J Nat Prod (2017) 80: 2094-2100 [PMID:28718638] |
| ChEMBL | Agonist activity at human kappa opiod receptor expressed in CHO-K1 cells assessed as increase in forskolin induced cAMP production measured after 30 mins by HitHunter luminescence based assay | F | 10.4 | pEC50 | 0.04 | nM | EC50 | J Med Chem (2016) 59: 11027-11038 [PMID:27958743] |
| ChEMBL | Agonist activity at human KOR expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by luminescence assay | F | 10.52 | pEC50 | 0.03 | nM | EC50 | J Med Chem (2014) 57: 10464-10475 [PMID:25426797] |
| ChEMBL | Agonist activity at human KOR expressed in CHOK1 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by luminescence assay | F | 10.52 | pEC50 | 0.03 | nM | EC50 | RSC Med Chem (2020) 11: 896-904 [PMID:33479684] |
| ChEMBL | Agonist activity at human KOR expressed in HEK293T cells assessed as inhibition of Galphai-mediated cAMP accumulation after 15 mins by microbeta counting assay | F | 10.82 | pEC50 | 0.01 | nM | EC50 | J Med Chem (2019) 62: 893-907 [PMID:30543421] |
| κ receptor/Kappa opioid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3614] [GtoPdb: 318] [UniProtKB: P34975] | ||||||||
| ChEMBL | Displacement of [3H]diprenorphine from rat kappa opioid receptor I316A mutant expressed in HEK293 cells | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2008) 51: 1824-1830 [PMID:18293909] |
| ChEMBL | Displacement of [3H]diprenorphine from rat kappa opioid receptor Y320A mutant expressed in HEK293 cells | B | 6.25 | pKi | 565 | nM | Ki | J Med Chem (2008) 51: 1824-1830 [PMID:18293909] |
| ChEMBL | Displacement of [3H]diprenorphine from rat kappa opioid receptor Q115A mutant expressed in HEK293 cells | B | 6.83 | pKi | 147 | nM | Ki | J Med Chem (2008) 51: 1824-1830 [PMID:18293909] |
| ChEMBL | Displacement of [3H]diprenorphine from rat kappa opioid receptor Y313A mutant expressed in HEK293 cells | B | 6.9 | pKi | 126 | nM | Ki | J Med Chem (2008) 51: 1824-1830 [PMID:18293909] |
| ChEMBL | Displacement of [3H]diprenorphine from rat kappa opioid receptor Y312A mutant expressed in HEK293 cells | B | 7.1 | pKi | 79 | nM | Ki | J Med Chem (2008) 51: 1824-1830 [PMID:18293909] |
| ChEMBL | Displacement of [3H]diprenorphine from rat kappa opioid receptor Y320F mutant expressed in HEK293 cells | B | 7.15 | pKi | 71 | nM | Ki | J Med Chem (2008) 51: 1824-1830 [PMID:18293909] |
| ChEMBL | Displacement of [3H]diprenorphine from rat kappa opioid receptor Y119A mutant expressed in HEK293 cells | B | 7.17 | pKi | 67 | nM | Ki | J Med Chem (2008) 51: 1824-1830 [PMID:18293909] |
| ChEMBL | Displacement of [3H]diprenorphine from rat kappa opioid receptor Y313F mutant expressed in HEK293 cells | B | 7.43 | pKi | 37 | nM | Ki | J Med Chem (2008) 51: 1824-1830 [PMID:18293909] |
| ChEMBL | Displacement of [3H]diprenorphine from rat kappa opioid receptor I290A mutant expressed in HEK293 cells | B | 7.53 | pKi | 29.6 | nM | Ki | J Med Chem (2008) 51: 1824-1830 [PMID:18293909] |
| ChEMBL | Displacement of [3H]diprenorphine from rat kappa opioid receptor K227A mutant expressed in HEK293 cells | B | 7.6 | pKi | 25.3 | nM | Ki | J Med Chem (2008) 51: 1824-1830 [PMID:18293909] |
| ChEMBL | Displacement of [3H]diprenorphine from rat kappa opioid receptor I62A mutant expressed in HEK293 cells | B | 7.66 | pKi | 22 | nM | Ki | J Med Chem (2008) 51: 1824-1830 [PMID:18293909] |
| ChEMBL | Displacement of [3H]diprenorphine from rat kappa opioid receptor E297A mutant expressed in HEK293 cells | B | 7.71 | pKi | 19.5 | nM | Ki | J Med Chem (2008) 51: 1824-1830 [PMID:18293909] |
| ChEMBL | Displacement of [3H]U-69593 from rat cloned KOR | B | 7.74 | pKi | 18.4 | nM | Ki | Bioorg Med Chem Lett (2007) 17: 2229-2232 [PMID:17303418] |
| ChEMBL | Displacement of [3H]diprenorphine from rat kappa opioid receptor Y66A mutant expressed in HEK293 cells | B | 7.74 | pKi | 18.1 | nM | Ki | J Med Chem (2008) 51: 1824-1830 [PMID:18293909] |
| ChEMBL | Displacement of [3H]diprenorphine from rat kappa opioid receptor Y119F mutant expressed in HEK293 cells | B | 7.75 | pKi | 17.7 | nM | Ki | J Med Chem (2008) 51: 1824-1830 [PMID:18293909] |
| ChEMBL | Displacement of [3H]diprenorphine from rat kappa opioid receptor expressed in HEK293 cells | B | 7.76 | pKi | 17.5 | nM | Ki | J Med Chem (2008) 51: 1824-1830 [PMID:18293909] |
| ChEMBL | Displacement of [3H]diprenorphine from rat kappa opioid receptor D138A mutant expressed in HEK293 cells | B | 7.76 | pKi | 17.5 | nM | Ki | J Med Chem (2008) 51: 1824-1830 [PMID:18293909] |
| ChEMBL | Displacement of [3H]diprenorphine from rat kappa opioid receptor Y312F mutant expressed in HEK293 cells | B | 7.8 | pKi | 16 | nM | Ki | J Med Chem (2008) 51: 1824-1830 [PMID:18293909] |
| ChEMBL | Displacement of [3H]diprenorphine from rat kappa opioid receptor Y139F mutant expressed in HEK293 cells | B | 8.02 | pKi | 9.5 | nM | Ki | J Med Chem (2008) 51: 1824-1830 [PMID:18293909] |
| ChEMBL | Displacement of [3H]diprenorphine from rat kappa opioid receptor Y66F mutant expressed in HEK293 cells | B | 8.17 | pKi | 6.8 | nM | Ki | J Med Chem (2008) 51: 1824-1830 [PMID:18293909] |
| ChEMBL | Inhibition of [3H]U-69593 binding to rat opioid receptor kappa 1 expressed in HEK 293 cells | B | 8.4 | pKi | 4 | nM | Ki | J Med Chem (2005) 48: 345-348 [PMID:15658846] |
| ChEMBL | Displacement of [3H]diprenorphine from rat kappa opioid receptor I294A mutant expressed in HEK293 cells | B | 8.54 | pKi | 2.9 | nM | Ki | J Med Chem (2008) 51: 1824-1830 [PMID:18293909] |
| ChEMBL | Displacement of [3H]U-69593 from rat cloned KOR | B | 9.12 | pKi | 0.75 | nM | Ki | Bioorg Med Chem Lett (2007) 17: 2229-2232 [PMID:17303418] |
| μ receptor/Mu opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372] | ||||||||
| ChEMBL | Displacement of [3H]DAMGO from mu opioid receptor expressed in HEK293 cells | B | 5 | pKi | >10000 | nM | Ki | Bioorg Med Chem Lett (2011) 21: 160-163 [PMID:21115248] |
| ChEMBL | Displacement of [3H]DAMGO from mu opioid receptor (unknown origin) | B | 5 | pKi | >10000 | nM | Ki | Bioorg Med Chem Lett (2013) 23: 2860-2862 [PMID:23587424] |
| ChEMBL | Inhibition of [125I]- IOXY binding to human Opioid receptor mu1 | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2005) 48: 4765-4771 [PMID:16033256] |
| ChEMBL | Displacement of [125I]IOXY from human recombinant mu opioid receptor expressed in CHO cells | B | 5.36 | pKi | 4370 | nM | Ki | J Med Chem (2008) 51: 2421-2431 [PMID:18380425] |
| ChEMBL | Displacement of [3H]DAMGO from human recombinant mu opioid receptor expressed in CHO cells after 2 hrs by liquid scintillation counting | B | 5.86 | pKi | 1370 | nM | Ki | Bioorg Med Chem (2012) 20: 3100-3110 [PMID:22464684] |
| ChEMBL | Displacement of [125]OXY from mu opioid receptor | B | 6 | pKi | >1000 | nM | Ki | J Nat Prod (2006) 69: 914-918 [PMID:16792410] |
| ChEMBL | Displacement of [125I]IOXY from human recombinant mu opioid receptor expressed in CHO cells | B | 6 | pKi | >1000 | nM | Ki | J Med Chem (2008) 51: 2421-2431 [PMID:18380425] |
| ChEMBL | Inhibition of [125I]- IOXY binding to human Opioid receptor mu1 | B | 6 | pKi | >1000 | nM | Ki | J Med Chem (2005) 48: 4765-4771 [PMID:16033256] |
| ChEMBL | Agonist activity at human MOR expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by luminescence assay | F | 5 | pEC50 | >=10000 | nM | EC50 | J Med Chem (2014) 57: 10464-10475 [PMID:25426797] |
| ChEMBL | Agonist activity at human mu opiod receptor expressed in CHO-K1 cells assessed as increase in forskolin induced cAMP production measured after 30 mins by HitHunter luminescence based assay | F | 5 | pEC50 | >10000 | nM | EC50 | J Med Chem (2016) 59: 11027-11038 [PMID:27958743] |
| ChEMBL | Agonist activity at mu opioid receptor assessed as stimulation of [35S]GTPgammaS binding | F | 5.54 | pEC50 | 2860 | nM | EC50 | J Nat Prod (2011) 74: 718-726 [PMID:21338114] |
| μ receptor/Mu opioid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL270] [GtoPdb: 319] [UniProtKB: P33535] | ||||||||
| ChEMBL | Displacement of [3H]diprenorphine from rat mu opioid receptor expressed in HEK293 cells | B | 4.6 | pKi | >25000 | nM | Ki | J Med Chem (2008) 51: 1824-1830 [PMID:18293909] |
| ChEMBL | Displacement of [3H]diprenorphine from rat mu opioid receptor expressed in CHO cells | B | 6 | pKi | >1000 | nM | Ki | Bioorg Med Chem (2008) 16: 1279-1286 [PMID:17981041] |
| ChEMBL | Binding affinity to rat MOPR expressed in CHO cells | B | 6 | pKi | >1000 | nM | Ki | Bioorg Med Chem (2009) 17: 1370-1380 [PMID:19147366] |
| ChEMBL | Displacement of [3H]diprenorphine from rat mu opioid receptor expressed in CHO cell membranes | B | 6 | pKi | >1000 | nM | Ki | Bioorg Med Chem Lett (2015) 25: 4689-4692 [PMID:26330078] |
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]
