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ChEMBL ligand: CHEMBL327745 (SB-213698, TAN-67) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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]