(-)-pentazocine [Ligand Id: 1606] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL560
  • δ receptor/Delta-type opioid receptor in Human [ChEMBL: CHEMBL236] [GtoPdb: 317] [UniProtKB: P41143]
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  • κ receptor/Kappa-type opioid receptor in Human [ChEMBL: CHEMBL237] [GtoPdb: 318] [UniProtKB: P41145]
  • Kappa-type opioid receptor in Guinea pig [ChEMBL: CHEMBL3952] [UniProtKB: P41144]
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  • μ receptor/Mu-type opioid receptor in Human [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372]
  • μ receptor/Mu-type opioid receptor in Rat [ChEMBL: CHEMBL270] [GtoPdb: 319] [UniProtKB: P33535]
  • Mu-type opioid receptor in Guinea pig [ChEMBL: CHEMBL4354] [UniProtKB: P97266]
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  • sigma non-opioid intracellular receptor 1/Sigma non-opioid intracellular receptor 1 in Human [ChEMBL: CHEMBL287] [GtoPdb: 2552] [UniProtKB: Q99720]
  • sigma non-opioid intracellular receptor 1/Sigma non-opioid intracellular receptor 1 in Rat [ChEMBL: CHEMBL3602] [GtoPdb: 2552] [UniProtKB: Q9R0C9]
  • Sigma non-opioid intracellular receptor 1 in Guinea pig [ChEMBL: CHEMBL4153] [UniProtKB: Q60492]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
δ receptor/Delta-type opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL236] [GtoPdb: 317] [UniProtKB: P41143]
ChEMBL Displacement of [3H]Naltrindole form human delta opioid receptor expressed in CHO cells B 6.74 pKi 180 nM Ki Bioorg Med Chem Lett (2009) 19: 203-208 [PMID:19027293]
GtoPdb - - 7.3 pKi - - - NIDA Res Monogr (1998) 178: 440-66 [PMID:9686407]
ChEMBL Displacement of [125I]OXY from human delta opioid receptor expressed in CHO cells B 7.31 pKi 49 nM Ki J Med Chem (2010) 53: 1392-1396 [PMID:20055417]
κ receptor/Kappa-type opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL237] [GtoPdb: 318] [UniProtKB: P41145]
ChEMBL Displacement of [3H]U69593 form human kappa opioid receptor expressed in CHO cells B 8.52 pKi 3 nM Ki Bioorg Med Chem Lett (2009) 19: 203-208 [PMID:19027293]
GtoPdb - - 8.6 pKi - - - NIDA Res Monogr (1998) 178: 440-66 [PMID:9686407];
J Pharmacol Exp Ther (1997) 282: 676-84 [PMID:9262330]
ChEMBL Displacement of [125I]OXY from human kappa opioid receptor expressed in CHO cells B 8.66 pKi 2.2 nM Ki J Med Chem (2010) 53: 1392-1396 [PMID:20055417]
Kappa-type opioid receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3952] [UniProtKB: P41144]
ChEMBL Displacement of [3H]U69593 from kappa opioid receptor in guinea pig cerebellum homogenate by scintillation counting B 8.44 pKi 3.6 nM Ki Bioorg Med Chem Lett (2011) 21: 4104-4107 [PMID:21641798]
μ receptor/Mu-type opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372]
ChEMBL Displacement of [3H]DAMGO form human mu opioid receptor expressed in CHO cells B 8.16 pKi 6.9 nM Ki Bioorg Med Chem Lett (2009) 19: 203-208 [PMID:19027293]
GtoPdb - - 8.4 pKi - - - NIDA Res Monogr (1998) 178: 440-66 [PMID:9686407]
ChEMBL Displacement of [125I]OXY from human mu opioid receptor expressed in CHO cells B 8.41 pKi 3.9 nM Ki J Med Chem (2010) 53: 1392-1396 [PMID:20055417]
μ receptor/Mu-type opioid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL270] [GtoPdb: 319] [UniProtKB: P33535]
ChEMBL Binding affinity against opioid receptor mu using [3H]-DAMGO as radioligand. B 7.89 pKi 13 nM Ki J Med Chem (1992) 35: 2812-2818 [PMID:1322987]
Mu-type opioid receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4354] [UniProtKB: P97266]
ChEMBL Displacement of [3H]DAMGO from mu opioid receptor in guinea pig forebrain homogenate by scintillation counting B 8.34 pKi 4.6 nM Ki Bioorg Med Chem Lett (2011) 21: 4104-4107 [PMID:21641798]
sigma non-opioid intracellular receptor 1/Sigma non-opioid intracellular receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL287] [GtoPdb: 2552] [UniProtKB: Q99720]
ChEMBL Tested for binding affinity against sigma receptors B 6.96 pKi 110 nM Ki J Med Chem (1994) 37: 1214-1219 [PMID:8164264]
ChEMBL Binding affinity measured on Sigma receptor type 1 from guinea pig brain membranes using [3H]pentazocine as radioligand. B 7.08 pKi 83.1 nM Ki J Med Chem (1995) 38: 2978-2985 [PMID:7636860]
ChEMBL Binding affinity was measured on Sigma receptor type 1 using [3H]- pentazocine as radioligand B 7.08 pKi 83.1 nM Ki J Med Chem (1995) 38: 2986-2989 [PMID:7636861]
ChEMBL Affinity against Sigma opioid receptor type 1 using [3H](+)-pentazocine in guinea pig brain membranes B 7.08 pKi 83.1 nM Ki J Med Chem (1999) 42: 4621-4629 [PMID:10579824]
ChEMBL Affinity against Sigma opioid receptor type 2 using [3H]- DTG in rat liver membranes B 7.44 pKi 36.5 nM Ki J Med Chem (1999) 42: 4621-4629 [PMID:10579824]
sigma non-opioid intracellular receptor 1/Sigma non-opioid intracellular receptor 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3602] [GtoPdb: 2552] [UniProtKB: Q9R0C9]
ChEMBL Binding affinity at Sigma receptor type 2 on rat liver membranes receptor by [3H]DTG displacement. B 7.44 pKi 36.5 nM Ki J Med Chem (1995) 38: 2978-2985 [PMID:7636860]
ChEMBL Binding affinity was measured on Sigma receptor type 2 using [3H]- DTG as radioligand B 7.44 pKi 36.5 nM Ki J Med Chem (1995) 38: 2986-2989 [PMID:7636861]
ChEMBL Displacement of [3H](+)-pentazocine from sigma1 receptor in rat brain homogenate B 7.8 pKi 16 nM Ki J Med Chem (2010) 53: 1392-1396 [PMID:20055417]
ChEMBL Displacement of [3H]-pentazocine from sigma 1 opioid receptor in rat liver homogenate by liquid scintillation counting B 7.82 pKi 15 nM Ki ACS Med Chem Lett (2011) 2: 834-839 [PMID:24900272]
ChEMBL Binding affinity for sigma receptor was evaluated by the inhibitory effect on [3H]DTG to rat whole brain membranes B 6.77 pIC50 170 nM IC50 J Med Chem (2000) 43: 177-189 [PMID:10649973]
ChEMBL Binding affinity towards Sigma receptor type 2 in whole rat brain homogenates except cerebellum using radioligand ([3H]DTG) binding assay. B 7.54 pIC50 29 nM IC50 J Med Chem (1995) 38: 2009-2017 [PMID:7783132]
ChEMBL Compound was evaluated for the binding affinity towards Sigma receptor type 1 using radioligand ([3H]-(+)- Pentazocine) binding assay. B 8.05 pIC50 8.9 nM IC50 J Med Chem (1995) 38: 2009-2017 [PMID:7783132]
Sigma non-opioid intracellular receptor 1 in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4153] [UniProtKB: Q60492]
ChEMBL Displacement of [3H](+)-pentazocine from sigma 1 receptor in guinea pig brain membrane B 7.08 pKi 83.4 nM Ki Bioorg Med Chem Lett (2008) 18: 5238-5241 [PMID:18774292]

ChEMBL data shown on this page come from version 36:

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]