reboxetine [Ligand Id: 4808] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL180101 (Esreboxetina, Esreboxetine, REBOXETINE, (s,s)-reboxetine, S,s-reboxetine) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| DAT/Dopamine transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL238] [GtoPdb: 927] [UniProtKB: Q01959] | ||||||||
| ChEMBL | Displacement of [3H]WIN35428 from human recombinant DAT transfected in HEK293 cell membrane | B | 4.7 | pKi | 19952.62 | nM | Ki | Bioorg Med Chem Lett (2013) 23: 1456-1461 [PMID:23347683] |
| ChEMBL | Displacement of [125I]RTI-55 from human DAT receptor expressed in canine kidney cells | B | 5.7 | pKi | >2000 | nM | Ki | J Med Chem (2009) 52: 62-73 [PMID:19067522] |
| ChEMBL | Inhibition of dopamine uptake at human DAT expressed in HEK293 cells | B | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem Lett (2008) 18: 4491-4494 [PMID:18672364] |
| DAT/Dopamine transporter in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL338] [GtoPdb: 927] [UniProtKB: P23977] | ||||||||
| ChEMBL | Inhibition of dopamine uptake at cloned DAT in rat brain synaptosome | B | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem Lett (2008) 18: 3682-3686 [PMID:18539031] |
| NET/Norepinephrine transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL222] [GtoPdb: 926] [UniProtKB: P23975] | ||||||||
| GtoPdb | - | - | 8 | pKi | 10 | nM | Ki | Biol Psychiatry (2000) 47: 818-29 [PMID:10812041] |
| ChEMBL | Displacement of [3H]nisoxetine from human NET receptor expressed in HEK293 cells | B | 8.98 | pKi | 1.04 | nM | Ki | J Med Chem (2009) 52: 62-73 [PMID:19067522] |
| ChEMBL | Inhibition of norepinephrine reuptake at NET | B | 9.52 | pKi | 0.3 | nM | Ki | Bioorg Med Chem (2009) 17: 7802-7815 [PMID:19836247] |
| ChEMBL | Inhibition of [3H]norepinephrine uptake at human NET expressed in MDCK-Net6 cells by scintillation counting | B | 8.51 | pIC50 | 3.1 | nM | IC50 | J Med Chem (2009) 52: 5703-5711 [PMID:19722525] |
| ChEMBL | Inhibition of norepinephrine uptake at human NET expressed in HEK293 cells | B | 8.52 | pIC50 | 3 | nM | IC50 | Bioorg Med Chem Lett (2008) 18: 4491-4494 [PMID:18672364] |
| ChEMBL | Inhibition of human recombinant NET expressed in HEK293 cells assessed as inhibition of [3H]NE reuptake | B | 8.7 | pIC50 | 2 | nM | IC50 | Bioorg Med Chem Lett (2013) 23: 1456-1461 [PMID:23347683] |
| SERT/Serotonin transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL228] [GtoPdb: 928] [UniProtKB: P31645] | ||||||||
| ChEMBL | Displacement of [3H]citalopram from human SERT receptor expressed in HEK293 cells | B | 6.18 | pKi | 661 | nM | Ki | J Med Chem (2009) 52: 62-73 [PMID:19067522] |
| ChEMBL | Inhibition of serotonin uptake at human SERT expressed in HEK293 cells | B | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem Lett (2008) 18: 4491-4494 [PMID:18672364] |
| ChEMBL | Inhibition of human recombinant SERT expressed in HEK293 cells assessed as inhibition of [3H]5HT reuptake | B | 5.5 | pIC50 | 3162.28 | nM | IC50 | Bioorg Med Chem Lett (2013) 23: 1456-1461 [PMID:23347683] |
| SERT/Serotonin transporter in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL313] [GtoPdb: 928] [UniProtKB: P31652] | ||||||||
| ChEMBL | Inhibition of serotonin uptake at SERT in rat brain synaptosome | B | 5.28 | pIC50 | 5200 | nM | IC50 | Bioorg Med Chem Lett (2008) 18: 3682-3686 [PMID:18539031] |
| Transporter in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6184] [UniProtKB: Q63380] | ||||||||
| ChEMBL | Inhibition of norepinephrine uptake at NET in rat brain synaptosome | B | 8.51 | pIC50 | 3.1 | nM | IC50 | Bioorg Med Chem Lett (2008) 18: 3682-3686 [PMID:18539031] |
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]
