paroxetine [Ligand Id: 4790] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL490 ((-)3s,4r-paroxetine, Arketis, Arotin, Besitram, BRL 29060, BRL-29060, Casbol, Daparox, Fg-7051, Frosinor, Motivan, Parogen, Paroxetina, Paroxetine, Paxil, Paxpar, Pexeva, Xetanor) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| Beta-adrenergic receptor kinase 1 in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3711550] [UniProtKB: P21146] | ||||||||
| ChEMBL | Inhibition of bovine GRK2 S670A mutant after 5 mins in presence of ATP by phosphorimaging assay | B | 5.86 | pIC50 | 1380 | nM | IC50 | J Med Chem (2017) 60: 3052-3069 [PMID:28323425] |
| ChEMBL | Inhibition of bovine GRK2 using porcine brain tubulin as substrate incubated for 3 to 5 mins by [gamma32P]ATP based radiometric assay | B | 6.11 | pIC50 | 780 | nM | IC50 | J Med Chem (2021) 64: 566-585 [PMID:33393767] |
| CYP2D6/Cytochrome P450 2D6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL289] [GtoPdb: 1329] [UniProtKB: P10635] | ||||||||
| ChEMBL | DRUGMATRIX: CYP450, 2D6 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin) | B | 6 | pIC50 | 1000 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| DAT/Dopamine transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL238] [GtoPdb: 927] [UniProtKB: Q01959] | ||||||||
| ChEMBL | Equilibrium dissociation constant (KD) for Competitive binding between [3H]WIN-35428 and the compound at human transporter-hDAT | B | 6.31 | pKd | 490 | nM | Kd | Bioorg Med Chem Lett (1998) 8: 487-492 [PMID:9871604] |
| ChEMBL | DRUGMATRIX: Dopamine Transporter radioligand binding (ligand: [125I] RTI-55) | B | 6.27 | pKi | 534 | nM | Ki | DrugMatrix in vitro pharmacology data |
| ChEMBL | Binding inhibition towards human dopamine transporter | B | 6.4 | pKi | 400 | nM | Ki | J Med Chem (2005) 48: 6023-6034 [PMID:16162005] |
| ChEMBL | DRUGMATRIX: Dopamine Transporter radioligand binding (ligand: [125I] RTI-55) | B | 6.17 | pIC50 | 672 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| DAT/Dopamine transporter in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2799] [GtoPdb: 927] [UniProtKB: Q61327] | ||||||||
| ChEMBL | Tested in vitro for dopamine(DA) neuronal uptake inhibition | B | 6.34 | pKi | 460 | nM | Ki | J Med Chem (1990) 33: 2793-2797 [PMID:2213832] |
| DAT/Dopamine transporter in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL338] [GtoPdb: 927] [UniProtKB: P23977] | ||||||||
| ChEMBL | Inhibition of [3H]- DA reuptake into rat striatal synaptosomes | B | 5.77 | pKi | 1700 | nM | Ki | Bioorg Med Chem Lett (1998) 8: 487-492 [PMID:9871604] |
| ChEMBL | Inhibitory constant towards reuptake of [125I]-12 from dopamine transporter in rat striatal membranes | B | 6.4 | pKi | 400 | nM | Ki | J Med Chem (1994) 37: 1535-1542 [PMID:8182712] |
| ChEMBL | Binding affinity against dopamine transporter (DAT) by displacement of [3H]WIN-35428 in male wistar rats | B | 6 | pIC50 | >1000 | nM | IC50 | J Med Chem (2003) 46: 5512-5532 [PMID:14640559] |
| ChEMBL | Displacement of [3H]WIN-35428(0.5 nM) from Dopamine transporter | B | 6.21 | pIC50 | 623 | nM | IC50 | J Med Chem (1998) 41: 247-257 [PMID:9457247] |
| beta adrenergic receptor kinase 1/G-protein coupled receptor kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4079] [GtoPdb: 1466] [UniProtKB: P25098] | ||||||||
| ChEMBL | Binding affinity to full length human GRK2 by Thermofluor thermal shift assay | B | 5.53 | pKd | 2980 | nM | Kd | Bioorg Med Chem Lett (2020) 30: 127602-127602 [PMID:33038544] |
| ChEMBL | Inhibition of full length C-terminal hexahistidine tagged GRK2 (unknown origin) S670A mutant expressed in High Five cells using Bac to Bac insect cell expression system using tubulin as substrate by SDS-PAGE method | B | 5.86 | pIC50 | 1380 | nM | IC50 | J Med Chem (2016) 59: 3793-3807 [PMID:27050625] |
| ChEMBL | Inhibition of GRK2 (unknown origin) | B | 5.86 | pIC50 | 1380 | nM | IC50 | J Med Chem (2017) 60: 3052-3069 [PMID:28323425] |
| ChEMBL | Inhibition of human GRK2 | B | 5.86 | pIC50 | 1380 | nM | IC50 | Eur J Med Chem (2022) 243: 114668-114668 [PMID:36055000] |
| ChEMBL | Inhibition of human GRK2 S670A mutant preincubated for 30 mins using tubulin as substrate followed by ATP addition | B | 5.96 | pIC50 | 1100 | nM | IC50 | J Med Chem (2016) 59: 3793-3807 [PMID:27050625] |
| ChEMBL | Inhibition of GRK2 (unknown origin) | B | 5.96 | pIC50 | 1100 | nM | IC50 | J Med Chem (2021) 64: 1283-1345 [PMID:33481605] |
| G protein-coupled receptor kinase 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5678] [GtoPdb: 1469] [UniProtKB: P34947] | ||||||||
| ChEMBL | Inhibition of GRK5 (unknown origin) using tubulin as substrate by SDS-PAGE method | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (2016) 59: 3793-3807 [PMID:27050625] |
| ChEMBL | Inhibition of C-terminal his6-tagged human GRK5 | B | 4 | pIC50 | >100000 | nM | IC50 | Eur J Med Chem (2022) 243: 114668-114668 [PMID:36055000] |
| G protein-coupled receptor kinase 5 in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3879830] [UniProtKB: P43249] | ||||||||
| ChEMBL | Inhibition of bovine GRK5 after 5 mins after 5 mins in presence of ATP by phosphorimaging assay | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (2017) 60: 3052-3069 [PMID:28323425] |
| Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809] | ||||||||
| ChEMBL | DRUGMATRIX: Potassium Channel HERG radioligand binding (ligand: [3H] Astemizole) | B | 5.07 | pKi | 8544.5 | nM | Ki | DrugMatrix in vitro pharmacology data |
| ChEMBL | DRUGMATRIX: Potassium Channel HERG radioligand binding (ligand: [3H] Astemizole) | B | 4.98 | pIC50 | 10429.3 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| M1 receptor/Muscarinic acetylcholine receptor M1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL216] [GtoPdb: 13] [UniProtKB: P11229] | ||||||||
| ChEMBL | DRUGMATRIX: Muscarinic M1 radioligand binding (ligand: [3H] N-Methylscopolamine) | B | 7.46 | pKi | 35 | nM | Ki | DrugMatrix in vitro pharmacology data |
| ChEMBL | DRUGMATRIX: Muscarinic M1 radioligand binding (ligand: [3H] N-Methylscopolamine) | B | 6.84 | pIC50 | 145 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| M2 receptor/Muscarinic acetylcholine receptor M2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL211] [GtoPdb: 14] [UniProtKB: P08172] | ||||||||
| ChEMBL | DRUGMATRIX: Muscarinic M2 radioligand binding (ligand: [3H] N-Methylscopolamine) | B | 6.72 | pKi | 189 | nM | Ki | DrugMatrix in vitro pharmacology data |
| ChEMBL | DRUGMATRIX: Muscarinic M2 radioligand binding (ligand: [3H] N-Methylscopolamine) | B | 6.27 | pIC50 | 532 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| M3 receptor/Muscarinic acetylcholine receptor M3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL245] [GtoPdb: 15] [UniProtKB: P20309] | ||||||||
| ChEMBL | DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine) | B | 7.42 | pKi | 38 | nM | Ki | DrugMatrix in vitro pharmacology data |
| ChEMBL | DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine) | B | 6.75 | pIC50 | 179 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| M4 receptor/Muscarinic acetylcholine receptor M4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1821] [GtoPdb: 16] [UniProtKB: P08173] | ||||||||
| ChEMBL | DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine) | B | 7.47 | pKi | 34 | nM | Ki | DrugMatrix in vitro pharmacology data |
| ChEMBL | DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine) | B | 6.61 | pIC50 | 244 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| M5 receptor/Muscarinic acetylcholine receptor M5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2035] [GtoPdb: 17] [UniProtKB: P08912] | ||||||||
| ChEMBL | DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine) | B | 7.05 | pKi | 89 | nM | Ki | DrugMatrix in vitro pharmacology data |
| ChEMBL | DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine) | B | 6.91 | pIC50 | 123 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| myeloperoxidase/Myeloperoxidase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2439] [GtoPdb: 2789] [UniProtKB: P05164] | ||||||||
| ChEMBL | Inhibition of recombinant MPO (unknown origin) assessed as reduction in taurine chloramine production preincubated with enzyme and taurine followed by H2O2 addition measured after 5 mins | B | 7.7 | pIC50 | 20 | nM | IC50 | J Med Chem (2017) 60: 6563-6586 [PMID:28671460] |
| NK1 receptor/Neurokinin 1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL249] [GtoPdb: 360] [UniProtKB: P25103] | ||||||||
| ChEMBL | Displacement of [125I]substance P from human recombinant NK1 receptor expressed in human U373 cells after 1 hr by scintillation counting analysis | B | 6.05 | pIC50 | 900 | nM | IC50 | Bioorg Med Chem (2013) 21: 2217-2228 [PMID:23477943] |
| NET/Norepinephrine transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL222] [GtoPdb: 926] [UniProtKB: P23975] | ||||||||
| ChEMBL | Equilibrium dissociation constant (KD) for Competitive binding between [3H]- nisoxatine and the compound at human Norepinephrine transporter | B | 7.4 | pKd | 40 | nM | Kd | Bioorg Med Chem Lett (1998) 8: 487-492 [PMID:9871604] |
| ChEMBL | Binding inhibition towards human norepinephrine transporter | B | 7.05 | pKi | 90 | nM | Ki | J Med Chem (2005) 48: 6023-6034 [PMID:16162005] |
| ChEMBL | DRUGMATRIX: Norepinephrine Transporter radioligand binding (ligand: [125I] RTI-55) | B | 7.07 | pKi | 86 | nM | Ki | DrugMatrix in vitro pharmacology data |
| ChEMBL | Inhibition of norepinephrine uptake at human NET expressed in MDCK cells | B | 7 | pIC50 | 100 | nM | IC50 | Bioorg Med Chem Lett (2008) 18: 4929-4931 [PMID:18771916] |
| ChEMBL | DRUGMATRIX: Norepinephrine Transporter radioligand binding (ligand: [125I] RTI-55) | B | 7.07 | pIC50 | 86 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| NET/Norepinephrine transporter in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2370] [GtoPdb: 926] [UniProtKB: O55192] | ||||||||
| ChEMBL | Tested in vitro for norepinephrine (NE) neuronal uptake inhibition | B | 7.7 | pKi | 20 | nM | Ki | J Med Chem (1990) 33: 2793-2797 [PMID:2213832] |
| Norepinephrine transporter in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL304] [UniProtKB: Q9WTR4] | ||||||||
| ChEMBL | Binding affinity against norepinephrine transporter (NET) by displacement of [3H]nisoxetine in male wistar rats | B | 6.18 | pKi | 659.6 | nM | Ki | J Med Chem (2003) 46: 5512-5532 [PMID:14640559] |
| ChEMBL | Inhibition of [3H]- NE reuptake into rat hippocampal synaptosomes | B | 7.48 | pKi | 33 | nM | Ki | Bioorg Med Chem Lett (1998) 8: 487-492 [PMID:9871604] |
| ChEMBL | Inhibition of [3H]nisoxetine (0.5 nM) binding to Noradrenaline transporter | B | 6.27 | pIC50 | 535 | nM | IC50 | J Med Chem (1998) 41: 247-257 [PMID:9457247] |
| P2X4/P2X purinoceptor 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2104] [GtoPdb: 481] [UniProtKB: Q99571] | ||||||||
| ChEMBL | Antagonist activity at human P2X4 receptor expressed in human 1321N1 cells assessed as inhibition of ATP-induced cytosolic calcium influx preincubated for 30 mins followed by ATP addition by Fluo-4 AM dye-based fluorescence assay | B | 5.33 | pIC50 | 4680 | nM | IC50 | Bioorg Med Chem (2014) 22: 1077-1088 [PMID:24411477] |
| ChEMBL | Antagonist activity at human P2X4 receptor expressed in 1321N1 cells assessed as inhibition of ATP-induced cytosolic calcium influx compound preincubated for 30 mins before ATP treatment by Fluo-4 AM fluorescence method | F | 5.73 | pIC50 | 1870 | nM | IC50 | J Med Chem (2012) 55: 9576-9588 [PMID:23075067] |
| ChEMBL | Antagonist activity at human P2X4 receptor tranfected in human 1321N1 cells assessed as inhibition of ATP-induced calcium influx incubated for 10 mins by Fluo2-AM staining based inverted fluorescence microscopic method | B | 5.73 | pIC50 | 1870 | nM | IC50 | J Med Chem (2019) 62: 11194-11217 [PMID:31746599] |
| GtoPdb | - | - | 6 | pIC50 | - | - | - |
Mol Pharmacol (2013) 83: 759-69 [PMID:23253448]; Neuropharmacology (2016) 104: 31-49 [PMID:26686393] |
| P2X4/P2X purinoceptor 4 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2818] [GtoPdb: 481] [UniProtKB: P51577] | ||||||||
| ChEMBL | Antagonist activity at rat P2X4 receptor by cell-based calcium influx assay | F | 5.61 | pIC50 | 2450 | nM | IC50 | J Med Chem (2012) 55: 9576-9588 [PMID:23075067] |
| ChEMBL | Antagonist activity at rat P2X4 receptor tranfected in human 1321N1 cells assessed as inhibition of ATP-induced calcium influx incubated for 10 mins by Fluo2-AM staining based inverted fluorescence microscopic method | B | 5.61 | pIC50 | 2450 | nM | IC50 | J Med Chem (2019) 62: 11194-11217 [PMID:31746599] |
| ABCB1/P-glycoprotein 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4302] [GtoPdb: 768] [UniProtKB: P08183] | ||||||||
| ChEMBL | TP_TRANSPORTER: cell accumulation of calcein in L-MDR1 cells | F | 4.53 | pIC50 | 29800 | nM | IC50 | J Pharmacol Exp Ther (2003) 305: 197-204 [PMID:12649369] |
| Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364] | ||||||||
| ChEMBL | DNDI: Malaria in Vitro, 72 hour | F | 5.03 | pIC50 | 9230 | nM | IC50 | Antiprotozoal Activity Profiling of Approved Drugs: A Starting Point toward Drug Repositioning |
| Quinolone resistance protein norA in S.aureus (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5114] [UniProtKB: P0A0J7] | ||||||||
| ChEMBL | Inhibition of NorA in Staphylococcus aureus 1199B assessed as inhibition of ethidium bromide efflux dose response curve based fluorometric assay | B | 5.15 | pIC50 | 7000 | nM | IC50 | J Med Chem (2011) 54: 5722-5736 [PMID:21751791] |
| G protein-coupled receptor kinase 1/Rhodopsin kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5607] [GtoPdb: 1465] [UniProtKB: Q15835] | ||||||||
| ChEMBL | Inhibition of GRK1 (unknown origin) using tubulin as substrate by SDS-PAGE method | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (2016) 59: 3793-3807 [PMID:27050625] |
| ChEMBL | Inhibition of C-terminal his6-tagged human GRK1 | B | 4 | pIC50 | >100000 | nM | IC50 | Eur J Med Chem (2022) 243: 114668-114668 [PMID:36055000] |
| Rhodopsin kinase in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3879860] [UniProtKB: P28327] | ||||||||
| ChEMBL | Inhibition of bovine GRK1 (1 to 535 residues) after 5 mins after 5 mins in presence of ATP by phosphorimaging assay | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (2017) 60: 3052-3069 [PMID:28323425] |
| 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908] | ||||||||
| ChEMBL | Binding affinity to 5HT1A receptor | B | 4.5 | pKd | 31622.78 | nM | Kd | J Med Chem (2009) 52: 6107-6125 [PMID:19754201] |
| ChEMBL | Binding affinity to 5HT1A receptor | B | 4.52 | pKd | 30000 | nM | Kd | J Med Chem (2009) 52: 6107-6125 [PMID:19754201] |
| 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327] | ||||||||
| ChEMBL | Binding affinity against 5-hydroxytryptamine 1A receptor (5-HT1A) by displacement of [3H]8-OH-DPAT from rat hippocampus membranes | B | 6 | pIC50 | >1000 | nM | IC50 | J Med Chem (2003) 46: 5512-5532 [PMID:14640559] |
| 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL322] [GtoPdb: 6] [UniProtKB: P14842] | ||||||||
| ChEMBL | Binding affinity against 5-hydroxytryptamine 2A receptor by displacement of [3H]-ketanserin from rat prefrontal cerebral cortex mambranes | B | 6 | pIC50 | >1000 | nM | IC50 | J Med Chem (2003) 46: 5512-5532 [PMID:14640559] |
| SERT/Serotonin transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL228] [GtoPdb: 928] [UniProtKB: P31645] | ||||||||
| ChEMBL | Equilibrium dissociation constant (KD) for Competitive binding between [3H]- imipramine and the compound at human transporter-hSERT | B | 9.89 | pKd | 0.13 | nM | Kd | Bioorg Med Chem Lett (1998) 8: 487-492 [PMID:9871604] |
| GtoPdb | - | - | 10.1 | pKd | 0.08 | nM | Kd | Nature (2016) 532: 334-9 [PMID:27049939] |
| ChEMBL | Displacement of [3H]citalopram from human SERT expressed in HEK293 cells | B | 9.38 | pKi | 0.42 | nM | Ki | Bioorg Med Chem (2008) 16: 6364-6370 [PMID:18487050] |
| ChEMBL | Displacement of [3H]citalopram from human SERT expressed in HEK293 cells | B | 9.38 | pKi | 0.42 | nM | Ki | Bioorg Med Chem Lett (2008) 18: 4727-4730 [PMID:18644726] |
| ChEMBL | Displacement of [3H]paroxetine from human SERT expressed in HEK293 cells | B | 9.42 | pKi | 0.38 | nM | Ki | Bioorg Med Chem Lett (2008) 18: 4727-4730 [PMID:18644726] |
| ChEMBL | Displacement of [3H]paroxetine from human SERT expressed in HEK293 cells | B | 9.42 | pKi | 0.38 | nM | Ki | Bioorg Med Chem (2008) 16: 6364-6370 [PMID:18487050] |
| GtoPdb | - | - | 9.6 | pKi | 0.25 | nM | Ki | Eur J Pharmacol (1997) 340: 249-58 [PMID:9537821] |
| ChEMBL | Displacement of [3H]citalopram from human SERT expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting method | B | 9.96 | pKi | 0.11 | nM | Ki | Bioorg Med Chem (2017) 25: 293-304 [PMID:27865645] |
| ChEMBL | Displacement of [3H]paroxetine from SERT receptor in human platelet membrane | B | 10.05 | pKi | 0.09 | nM | Ki | Bioorg Med Chem (2007) 15: 7581-7589 [PMID:17900912] |
| ChEMBL | Displacement of [125I]RTI55 binding from human wild type SERT | B | 10.1 | pKi | 0.08 | nM | Ki | Eur J Med Chem (2021) 220: 113533-113533 [PMID:34049262] |
| ChEMBL | Evaluated for affinity at 5-HT uptake site using [3H]paroxetine as radioligand in radioligand binding assay | B | 10.11 | pKi | 0.08 | nM | Ki | Bioorg Med Chem Lett (1995) 5: 2287-2292 |
| ChEMBL | DRUGMATRIX: Transporter, Serotonin (5-Hydroxytryptamine) (SERT) radioligand binding (ligand: [3H] Paroxetine) | B | 10.37 | pKi | 0.04 | nM | Ki | DrugMatrix in vitro pharmacology data |
| ChEMBL | Binding inhibition towards human serotonin transporter | B | 10.4 | pKi | 0.04 | nM | Ki | J Med Chem (2005) 48: 6023-6034 [PMID:16162005] |
| ChEMBL | Inhibition of human SERT | B | 7.7 | pIC50 | 20 | nM | IC50 | Medchemcomm (2016) 7: 1176-1182 |
| ChEMBL | Inhibition of serotonin uptake at human SERT expressed in JAR cells | B | 8.7 | pIC50 | 2 | nM | IC50 | Bioorg Med Chem Lett (2008) 18: 4929-4931 [PMID:18771916] |
| ChEMBL | Inhibition of human SERT expressed in CHO cell membranes assessed as reduction in [3H]serotonin uptake preincubated for 10 mins followed by [3H]serotonin addition measured after 20 mins by liquid scintillation counting method | B | 9.25 | pIC50 | 0.56 | nM | IC50 | Bioorg Med Chem (2017) 25: 293-304 [PMID:27865645] |
| ChEMBL | Displacement of [125I]RTI-55 from human recombinant SERT expressed in HEK293 cells after 1 hr by scintillation counting analysis | B | 9.7 | pIC50 | 0.2 | nM | IC50 | Bioorg Med Chem (2013) 21: 2217-2228 [PMID:23477943] |
| ChEMBL | DRUGMATRIX: Transporter, Serotonin (5-Hydroxytryptamine) (SERT) radioligand binding (ligand: [3H] Paroxetine) | B | 10.1 | pIC50 | 0.08 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| SERT/Serotonin transporter in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4642] [GtoPdb: 928] [UniProtKB: Q60857] | ||||||||
| ChEMBL | Tested in vitro for serotonin(5-HT) neuronal uptake inhibition | B | 9.36 | pKi | 0.44 | nM | Ki | J Med Chem (1990) 33: 2793-2797 [PMID:2213832] |
| SERT/Serotonin transporter in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL313] [GtoPdb: 928] [UniProtKB: P31652] | ||||||||
| ChEMBL | The potency of the [3H]paroxetine for 5-HT transporters | B | 9.82 | pKd | 0.15 | nM | Kd | J Med Chem (1994) 37: 1262-1268 [PMID:8176704] |
| ChEMBL | Inhibition of [3H]5-HT reuptake into rat frontal cortex synaptosomes | B | 9.14 | pKi | 0.73 | nM | Ki | Bioorg Med Chem Lett (1998) 8: 487-492 [PMID:9871604] |
| ChEMBL | Binding affinity to the serotonin transporter (SERT) measured by displacement of [3H]paroxetine in male wistar rats | B | 9.15 | pKi | 0.7 | nM | Ki | J Med Chem (2003) 46: 5512-5532 [PMID:14640559] |
| ChEMBL | Displacement of [3H]citalopram from rat cortical serotonin transporter (SERT) | B | 9.28 | pKi | 0.53 | nM | Ki | Bioorg Med Chem Lett (2002) 12: 811-815 [PMID:11859009] |
| ChEMBL | Inhibition of [3H]citalopram binding to Serotonin transporter of rat cerebral cortex | B | 9.28 | pKi | 0.53 | nM | Ki | Bioorg Med Chem Lett (2000) 10: 1559-1562 [PMID:10915050] |
| ChEMBL | Inhibition of uptake of [3H]5-HT in synaptosomes from rat cortex | F | 8.19 | pIC50 | 6.43 | nM | IC50 | J Med Chem (1997) 40: 1049-1062 [PMID:9089327] |
| ChEMBL | Inhibition of [3H]paroxetine (0.2 nM) binding to 5-HT transporter | B | 9.55 | pIC50 | 0.28 | nM | IC50 | J Med Chem (1998) 41: 247-257 [PMID:9457247] |
| sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL287] [GtoPdb: 2552] [UniProtKB: Q99720] | ||||||||
| ChEMBL | DRUGMATRIX: Sigma1 radioligand binding (ligand: [3H] Haloperidol) | B | 5.65 | pKi | 2255 | nM | Ki | DrugMatrix in vitro pharmacology data |
| ChEMBL | DRUGMATRIX: Sigma1 radioligand binding (ligand: [3H] Haloperidol) | B | 5.27 | pIC50 | 5366 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| Kv1.3/Voltage-gated potassium channel subunit Kv1.3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4633] [GtoPdb: 540] [UniProtKB: P22001] | ||||||||
| ChEMBL | Inhibition of human Kv1.3 expressed in HEK293 cells assessed as inhibition of tetracyclin induced current at holding potential of -80 mV by patch clamp method | B | 4.5 | pIC50 | 31900 | nM | IC50 | J Nat Prod (2022) 85: 815-827 [PMID:35245067] |
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]
