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

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ChEMBL ligand: CHEMBL1419 (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 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]