TAN-67 [Ligand Id: 9567] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL327745 (SB-213698, TAN-67)
  • 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 Mouse [ChEMBL: CHEMBL4329] [GtoPdb: 318] [UniProtKB: P33534]
  • Kappa opioid receptor in Guinea pig [ChEMBL: CHEMBL3952] [UniProtKB: P41144]
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  • μ receptor/Mu opioid receptor in Mouse [ChEMBL: CHEMBL2858] [GtoPdb: 319] [UniProtKB: P42866]
  • μ receptor/Mu opioid receptor in Rat [ChEMBL: CHEMBL270] [GtoPdb: 319] [UniProtKB: P33535]
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  • MRGPRX2 in Human [GtoPdb: 157] [UniProtKB: Q96LB1]
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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 Agonist activity at human recombinant delta opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay F 8.85 pEC50 1.4 nM EC50 Bioorg Med Chem Lett (2009) 19: 2792-2795 [PMID:19362480]
ChEMBL Agonist activity at human recombinant delta opioid receptor expressed in HEK293 cells by [35S]GTPgammaS binding assay F 9.15 pEC50 0.7 nM EC50 Bioorg Med Chem Lett (2009) 19: 2792-2795 [PMID:19362480]
ChEMBL Agonist activity at human recombinant delta opioid receptor expressed in human HEK293 cells by [35S]GTPgammaS binding assay F 9.15 pEC50 0.7 nM EC50 Bioorg Med Chem (2012) 20: 949-961 [PMID:22197670]
δ receptor/Delta opioid receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3222] [GtoPdb: 317] [UniProtKB: P32300]
ChEMBL Displacement of [3H]DPDPE from delta opioid receptor in mouse whole brain membranes B 8.84 pKi 1.44 nM Ki Bioorg Med Chem Lett (2010) 20: 6302-6305 [PMID:20850307]
ChEMBL inhibition of [3H]DADLE binding to delta-opioid receptor of mouse brain homogenates B 9.64 pKi 0.23 nM Ki Bioorg Med Chem Lett (1997) 7: 2967-2972
GtoPdb Bioassay using mouse vas deferens. - 8.44 pIC50 3.65 nM IC50 Drug Des Discov (2001) 17: 325-30 [PMID:11765135]
δ receptor/Delta opioid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL269] [GtoPdb: 317] [UniProtKB: P33533]
ChEMBL Displacement of [3H]DADLE from delta opioid receptor in rat cerebellum membrane B 8.84 pKi 1.44 nM Ki Bioorg Med Chem Lett (2009) 19: 2792-2795 [PMID:19362480]
ChEMBL Displacement of [3H]DADLE from delta opioid receptor in rat cerebrum membranes B 8.84 pKi 1.44 nM Ki Bioorg Med Chem (2012) 20: 949-961 [PMID:22197670]
κ receptor/Kappa opioid receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4329] [GtoPdb: 318] [UniProtKB: P33534]
ChEMBL Binding affinity against Kappa opioid receptor using [3H]U-69593 radioligand in mouse brain homogenates B 6.51 pKi 312 nM Ki Bioorg Med Chem Lett (1997) 7: 2967-2972
Kappa opioid receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3952] [UniProtKB: P41144]
ChEMBL Displacement of [3H]U-69,593 from kappa opioid receptor in guinea pig cerebrum membranes B 6.14 pKi 732.5 nM Ki Bioorg Med Chem (2012) 20: 949-961 [PMID:22197670]
ChEMBL Displacement of [3H]U-69593 from kappa opioid receptor in guinea pig cerebellum B 6.14 pKi 732.45 nM Ki Bioorg Med Chem Lett (2009) 19: 2792-2795 [PMID:19362480]
ChEMBL Displacement of [3H]U-69,593 from kappa opioid receptor in guinea pig cerebellum membranes B 6.14 pKi 732.45 nM Ki Bioorg Med Chem Lett (2010) 20: 6302-6305 [PMID:20850307]
μ receptor/Mu opioid receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2858] [GtoPdb: 319] [UniProtKB: P42866]
ChEMBL Displacement of [3H]DAMGO from mu opioid receptor in mouse whole brain membranes B 6.55 pKi 284.14 nM Ki Bioorg Med Chem Lett (2010) 20: 6302-6305 [PMID:20850307]
ChEMBL Inhibition of [3H]DAMGO from mouse brain homogenate Mu opioid receptor B 7.22 pKi 59.6 nM Ki Bioorg Med Chem Lett (1997) 7: 2967-2972
μ receptor/Mu opioid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL270] [GtoPdb: 319] [UniProtKB: P33535]
ChEMBL Displacement of [3H]DAMGO from mu opioid receptor in rat cerebellum membrane B 6.55 pKi 284.14 nM Ki Bioorg Med Chem Lett (2009) 19: 2792-2795 [PMID:19362480]
ChEMBL Displacement of [3H]DAMGO from mu opioid receptor in rat cerebrum membranes B 6.55 pKi 284.1 nM Ki Bioorg Med Chem (2012) 20: 949-961 [PMID:22197670]
MRGPRX2 in Human [GtoPdb: 157] [UniProtKB: Q96LB1]
GtoPdb Assayed using racemic TAN-67, the more active stereoisomer is the (4aS,12aR). - 5.74 pEC50 1820 nM EC50 J Biomol Screen (2013) 18: 599-609 [PMID:23396314];
Nat Chem Biol (2017) 13: 529-536 [PMID:28288109];
Drug Des Discov (2001) 17: 325-30 [PMID:11765135]

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]