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 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]