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 | Binding affinity to DOP (unknown origin) | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2022) 65: 1612-1661 [PMID:34995453] |
| 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 [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 | 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 | 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 | 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 | Binding affinity to wild type human KOR assessed as inhibition constant | B | 7.4 | pKi | 40 | nM | Ki | Eur J Med Chem (2022) 243: 114785-114785 [PMID:36179400] |
| 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 | Binding affinity to KOR (unknown origin) expressed in HEK293 cells assessed as inhibition constant | B | 7.8 | pKi | 16 | nM | Ki | Eur J Med Chem (2022) 243: 114785-114785 [PMID:36179400] |
| 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 | Binding affinity to KOR (unknown origin) | B | 8.4 | pKi | 4 | nM | Ki | Eur J Med Chem (2022) 243: 114785-114785 [PMID:36179400] |
| 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 | 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 [125]OXY from kappa opioid receptor | B | 8.72 | pKi | 1.9 | nM | Ki | J Nat Prod (2006) 69: 914-918 [PMID:16792410] |
| 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 [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 | 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 | 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 | 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 | 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 | 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 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 | 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 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 KOR (unknown origin) assessed as beta-arrestin recruitment by TANGO assay | F | 7.98 | pEC50 | 10.5 | nM | EC50 | Eur J Med Chem (2022) 243: 114785-114785 [PMID:36179400] |
| 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 KOR (unknown origin) by beta-arrestin recruitment assay | F | 8.33 | pEC50 | 4.73 | nM | EC50 | Eur J Med Chem (2022) 243: 114785-114785 [PMID:36179400] |
| 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 | 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 | 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 | 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 | 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 | 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 | Displacement of [35S]GTPgammaS binding from human KOR assessed as inhibition constant | B | 8.66 | pEC50 | 2.2 | nM | EC50 | Eur J Med Chem (2022) 243: 114785-114785 [PMID:36179400] |
| 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 wild type human KOR receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding measured after 30 mins by scintillation counting assay | F | 9.7 | pEC50 | 0.2 | nM | EC50 | Eur J Med Chem (2022) 243: 114785-114785 [PMID:36179400] |
| 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 Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4329] [GtoPdb: 318] [UniProtKB: P33534] | ||||||||
| ChEMBL | Displacement of [3H]U69593 from C57BL6/J mouse brain KOP | B | 7.73 | pKi | 18.7 | nM | Ki | J Med Chem (2022) 65: 1612-1661 [PMID:34995453] |
| ChEMBL | Agonist activity at C57BL6/J mouse brain KOP by calcium mobilization assay | F | 6.98 | pEC50 | 104 | nM | EC50 | J Med Chem (2022) 65: 1612-1661 [PMID:34995453] |
| ChEMBL | Agonist activity at C57BL6/J mouse brain KOP | F | 8.16 | pEC50 | 6.9 | nM | EC50 | J Med Chem (2022) 65: 1612-1661 [PMID:34995453] |
| 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] |
| Kappa opioid receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3952] [UniProtKB: P41144] | ||||||||
| ChEMBL | Agonist activity at KOR in guinea pig brain membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hr by liquid scintillation counting analysis | F | 5.3 | pKi | >5000 | nM | Ki | Eur J Med Chem (2022) 243: 114785-114785 [PMID:36179400] |
| ChEMBL | Binding affinity to KOR in Guinea pig brain assessed as inhibition constant | B | 8.37 | pKi | 4.3 | nM | Ki | Eur J Med Chem (2022) 243: 114785-114785 [PMID:36179400] |
| 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 (unknown origin) | B | 5 | pKi | >10000 | nM | Ki | Bioorg Med Chem Lett (2013) 23: 2860-2862 [PMID:23587424] |
| ChEMBL | Binding affinity to MOP (unknown origin) | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2022) 65: 1612-1661 [PMID:34995453] |
| 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 [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 [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 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]
