BW373U86 [Ligand Id: 9002] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL25230 (BW-373U86, SNC-86)
  • δ receptor/Delta opioid receptor in Human [ChEMBL: CHEMBL236] [GtoPdb: 317] [UniProtKB: P41143]
  • δ receptor/Delta opioid receptor in Mouse [ChEMBL: CHEMBL3222] [GtoPdb: 317] [UniProtKB: P32300]
  • δ receptor/Delta opioid receptor in Rat [ChEMBL: CHEMBL269] [GtoPdb: 317] [UniProtKB: P33533]
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  • κ receptor/Kappa opioid receptor in Human [ChEMBL: CHEMBL237] [GtoPdb: 318] [UniProtKB: P41145]
  • κ receptor in Rat [GtoPdb: 318] [UniProtKB: P34975]
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  • μ receptor/Mu opioid receptor in Human [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372]
  • μ receptor/Mu opioid receptor in Rat [ChEMBL: CHEMBL270] [GtoPdb: 319] [UniProtKB: P33535]
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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 - - 9.49 pKi 0.32 nM Ki J Med Chem (2008) 51: 5893-6 [PMID:18788723]
ChEMBL Displacement of [3H]diprenorphine from human delta opioid receptor in CHO cells B 9.49 pKi 0.32 nM Ki J Med Chem (2008) 51: 5893-5896 [PMID:18788723]
ChEMBL Binding affinity against human opioid receptor delta 1 using [125I]-[D-Ala2]-deltorphin II as radioligand B 9.64 pIC50 0.23 nM IC50 J Med Chem (2000) 43: 3878-3894 [PMID:11052793]
ChEMBL Agonist activity at human delta opioid receptor in CHO cells assessed as stimulation of [35S]GTPgammaS binding F 9.4 pEC50 0.4 nM EC50 J Med Chem (2008) 51: 5893-5896 [PMID:18788723]
ChEMBL Agonist potency was measured using GTP gamma-[35S] binding assay B 9.92 pEC50 0.12 nM EC50 J Med Chem (2000) 43: 3878-3894 [PMID:11052793]
δ receptor/Delta opioid receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3222] [GtoPdb: 317] [UniProtKB: P32300]
ChEMBL Binding affinity towards opioid Delta receptor using [3H]DADLE as radioligand B 9.04 pKi 0.91 nM Ki Bioorg Med Chem Lett (1999) 9: 3053-3056 [PMID:10571174]
ChEMBL Binding affinity towards opioid Delta receptor using [3H]DADLE as radioligand B 9.04 pKi 0.91 nM Ki Bioorg Med Chem Lett (1999) 9: 3347-3350 [PMID:10612597]
ChEMBL Agonist activity at delta opioid receptor in mouse vas deferens F 9.2 pIC50 0.63 nM IC50 Bioorg Med Chem Lett (2006) 16: 905-910 [PMID:16290934]
ChEMBL Tested for inhibition of binding of [3H]DADLE to mouse brain membranes depleted of mu binding sites by pretreatment with irreversible ligand BIT for delta opioid receptor B 9.51 pIC50 0.31 nM IC50 J Med Chem (1994) 37: 2125-2128 [PMID:8035418]
δ receptor/Delta opioid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL269] [GtoPdb: 317] [UniProtKB: P33533]
GtoPdb - - 8.74 pKi 1.8 nM Ki J Pharmacol Exp Ther (1993) 267: 852-7 [PMID:8246159]
ChEMBL Binding affinity of compound evaluated for Opioid receptor delta 1 isolated from rat brain B 8.74 pKi 1.8 nM Ki J Med Chem (2003) 46: 623-633 [PMID:12570383]
ChEMBL Affinity of [H]DADLE to the delta opioid receptor from rat brain B 9.04 pKi 0.91 nM Ki J Med Chem (2001) 44: 972-987 [PMID:11300879]
ChEMBL Inhibition of radioligand [3H]DADLE binding to rat brain Opioid receptor delta 1 B 7.23 pIC50 58.3 nM IC50 J Med Chem (1997) 40: 695-704 [PMID:9057856]
ChEMBL Inhibition of radioligand [3H]DADLE binding to rat brain Opioid receptor delta 1 B 8.83 pIC50 1.49 nM IC50 J Med Chem (1997) 40: 695-704 [PMID:9057856]
ChEMBL Binding affinity was measured against Opioid receptor delta 1 using [3H]p-Cl-DPDPE as radioligand. B 9.51 pIC50 0.31 nM IC50 J Med Chem (1998) 41: 4767-4776 [PMID:9822547]
κ receptor/Kappa opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL237] [GtoPdb: 318] [UniProtKB: P41145]
ChEMBL Displacement of [3H]diprenorphine from human kappa opioid receptor in CHO cells B 5.47 pKi 3400 nM Ki J Med Chem (2008) 51: 5893-5896 [PMID:18788723]
ChEMBL Displacement of [3H]diprenorphine from human kappa opioid receptor in CHO cells at 10 uM B 6.89 pKi 130 nM Ki J Med Chem (2008) 51: 5893-5896 [PMID:18788723]
GtoPdb - - 6.89 pKi 130 nM Ki J Med Chem (2008) 51: 5893-6 [PMID:18788723]
ChEMBL Binding affinity against cloned human Opioid receptor kappa 1 using [125I]-D-Pro10-dynorphin A[1-11] as radioligand B 7.7 pIC50 20 nM IC50 J Med Chem (2000) 43: 3878-3894 [PMID:11052793]
κ receptor in Rat [GtoPdb: 318] [UniProtKB: P34975]
GtoPdb - - 7.47 pKi 34 nM Ki J Pharmacol Exp Ther (1993) 267: 852-7 [PMID:8246159]
μ receptor/Mu opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372]
ChEMBL Displacement of [3H]diprenorphine from human mu opioid receptor in CHO cells B 6.59 pKi 260 nM Ki J Med Chem (2008) 51: 5893-5896 [PMID:18788723]
GtoPdb - - 6.59 pKi 260 nM Ki J Med Chem (2008) 51: 5893-6 [PMID:18788723]
ChEMBL Binding affinity against cloned human Opioid receptor mu 1 using [125I]FK33824 as radioligand B 8.68 pIC50 2.1 nM IC50 J Med Chem (2000) 43: 3878-3894 [PMID:11052793]
μ receptor/Mu opioid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL270] [GtoPdb: 319] [UniProtKB: P33535]
ChEMBL Affinity of [3H]DAMGO to the mu opioid receptor from rat brain B 7.44 pKi 36 nM Ki J Med Chem (2001) 44: 972-987 [PMID:11300879]
ChEMBL Binding affinity towards opioid Mu receptor using [3H]DAMGO as radioligand B 7.44 pKi 36 nM Ki Bioorg Med Chem Lett (1999) 9: 3053-3056 [PMID:10571174]
ChEMBL Binding affinity towards opioid Mu receptor using [3H]DAMGO as radioligand B 7.44 pKi 36 nM Ki Bioorg Med Chem Lett (1999) 9: 3347-3350 [PMID:10612597]
GtoPdb - - 7.82 pKi 15 nM Ki J Pharmacol Exp Ther (1993) 267: 852-7 [PMID:8246159]
ChEMBL Inhibition of [3H]DAMGO binding to mu opioid receptor of rat brain membranes B 7.82 pKi 15 nM Ki J Med Chem (2003) 46: 623-633 [PMID:12570383]
ChEMBL Inhibition of radioligand [3H]DAMGO binding to rat brain Opioid receptor mu 1 using 100 nM DAMGO B 5.63 pIC50 2322 nM IC50 J Med Chem (1997) 40: 695-704 [PMID:9057856]
ChEMBL Inhibition of radioligand [3H]DAMGO binding to rat brain Opioid receptor mu 1 using 100 nM DAMGO B 8.01 pIC50 9.71 nM IC50 J Med Chem (1997) 40: 695-704 [PMID:9057856]
ChEMBL Evaluated for inhibition of [3H]DAMGO binding from mu receptor in rat brain membranes B 8.01 pIC50 9.71 nM IC50 J Med Chem (1994) 37: 2125-2128 [PMID:8035418]
ChEMBL Binding affinity was measured against Opioid receptor mu 1 using [3H]-DAMGO as radioligand. B 8.01 pIC50 9.7 nM IC50 J Med Chem (1998) 41: 4767-4776 [PMID:9822547]

ChEMBL data shown on this page come from version 32:

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]