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, Paroxetine, Paxil, Paxil [as hydrochloride], 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 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] |
| 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] |
| 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] |
| 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 |
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]
