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 33:

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]