sibutramine [Ligand Id: 2586] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1419 (Butramin, Cf-alli, Medaria, Racemic sibutramine, Reductil, Sibutramine)
  • α2B-adrenoceptor/Alpha-2b adrenergic receptor in Human [ChEMBL: CHEMBL1942] [GtoPdb: 26] [UniProtKB: P18089]
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  • NET/Norepinephrine transporter in Human [ChEMBL: CHEMBL222] [GtoPdb: 926] [UniProtKB: P23975]
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  • SERT/Serotonin transporter in Human [ChEMBL: CHEMBL228] [GtoPdb: 928] [UniProtKB: P31645]
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  • Kv4.3 in Rat [GtoPdb: 554] [UniProtKB: Q62897]
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  • CYP2B6 in Human [GtoPdb: 1324] [UniProtKB: P20813]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
α2B-adrenoceptor/Alpha-2b adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1942] [GtoPdb: 26] [UniProtKB: P18089]
ChEMBL DRUGMATRIX: Alpha-2B adrenergic receptor radioligand binding (ligand: Rauwolscine) B 5.96 pKi 1091 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Alpha-2B adrenergic receptor radioligand binding (ligand: Rauwolscine) B 5.62 pIC50 2390 nM IC50 DrugMatrix in vitro pharmacology data
DAT/Dopamine transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL238] [GtoPdb: 927] [UniProtKB: Q01959]
ChEMBL DRUGMATRIX: Dopamine Transporter radioligand binding (ligand: [125I] RTI-55) B 6.3 pKi 502 nM Ki DrugMatrix in vitro pharmacology data
GtoPdb - - 6.3 pKi 502 nM Ki National Toxicology Program: Dept of Health and Human Services.. DrugMatrix
ChEMBL DRUGMATRIX: Dopamine Transporter radioligand binding (ligand: [125I] RTI-55) B 6.2 pIC50 632 nM IC50 DrugMatrix in vitro pharmacology data
NET/Norepinephrine transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL222] [GtoPdb: 926] [UniProtKB: P23975]
GtoPdb - - 5.25 pKi 5619 nM Ki National Toxicology Program: Dept of Health and Human Services.. DrugMatrix
ChEMBL DRUGMATRIX: Norepinephrine Transporter radioligand binding (ligand: [125I] RTI-55) B 5.25 pKi 5619 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Norepinephrine Transporter radioligand binding (ligand: [125I] RTI-55) B 5.25 pIC50 5665 nM IC50 DrugMatrix in vitro pharmacology data
SERT/Serotonin transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL228] [GtoPdb: 928] [UniProtKB: P31645]
ChEMBL DRUGMATRIX: Transporter, Serotonin (5-Hydroxytryptamine) (SERT) radioligand binding (ligand: [3H] Paroxetine) B 5.96 pKi 1108 nM Ki DrugMatrix in vitro pharmacology data
GtoPdb - - 5.96 pKi 1108 nM Ki National Toxicology Program: Dept of Health and Human Services.. DrugMatrix
ChEMBL DRUGMATRIX: Transporter, Serotonin (5-Hydroxytryptamine) (SERT) radioligand binding (ligand: [3H] Paroxetine) B 5.68 pIC50 2085 nM IC50 DrugMatrix in vitro pharmacology data
Kv4.3 in Rat [GtoPdb: 554] [UniProtKB: Q62897]
GtoPdb - - 4.7 pIC50 - - - J Pharmacol Exp Ther (2007) 321: 753-62 [PMID:17312186]
CYP2B6 in Human [GtoPdb: 1324] [UniProtKB: P20813]
GtoPdb - - 5.79 pIC50 1610 nM IC50 Chem Biol Interact (2013) 205: 11-9 [PMID:23777987]

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]