[3H]citalopram [Ligand Id: 4621] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL549 (Citalopram, Celexa)
  • α1A-adrenoceptor/Alpha-1a adrenergic receptor in Rat [ChEMBL: CHEMBL319] [GtoPdb: 22] [UniProtKB: P43140]
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  • α1B-adrenoceptor/Alpha-1b adrenergic receptor in Rat [ChEMBL: CHEMBL315] [GtoPdb: 23] [UniProtKB: P15823]
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  • α1D-adrenoceptor/Alpha-1d adrenergic receptor in Human [ChEMBL: CHEMBL223] [GtoPdb: 24] [UniProtKB: P25100]
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  • H1 receptor/Histamine H1 receptor in Human [ChEMBL: CHEMBL231] [GtoPdb: 262] [UniProtKB: P35367]
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  • NET/Norepinephrine transporter in Human [ChEMBL: CHEMBL222] [GtoPdb: 926] [UniProtKB: P23975]
  • NET/Norepinephrine transporter in Mouse [ChEMBL: CHEMBL2370] [GtoPdb: 926] [UniProtKB: O55192]
  • Norepinephrine transporter in Rat [ChEMBL: CHEMBL304] [UniProtKB: Q9WTR4]
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  • 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Rat [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327]
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  • 5-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Human [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595]
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  • 5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335]
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  • sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Human [ChEMBL: CHEMBL287] [GtoPdb: 2552] [UniProtKB: Q99720]
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  • Organic cation transporter 1/Solute carrier family 22 member 1 in Human [ChEMBL: CHEMBL5685] [GtoPdb: 1019] [UniProtKB: O15245]
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  • Cav1.2/Voltage-gated L-type calcium channel alpha-1C subunit in Rat [ChEMBL: CHEMBL3762] [GtoPdb: 529] [UniProtKB: P22002]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
α1A-adrenoceptor/Alpha-1a adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL319] [GtoPdb: 22] [UniProtKB: P43140]
ChEMBL DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin) B 6.15 pKi 711 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin) B 5.76 pIC50 1756 nM IC50 DrugMatrix in vitro pharmacology data
α1B-adrenoceptor/Alpha-1b adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL315] [GtoPdb: 23] [UniProtKB: P15823]
ChEMBL DRUGMATRIX: Alpha-1B adrenergic receptor radioligand binding (ligand: prazosin) B 5.74 pKi 1820 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Alpha-1B adrenergic receptor radioligand binding (ligand: prazosin) B 5.48 pIC50 3288 nM IC50 DrugMatrix in vitro pharmacology data
α1D-adrenoceptor/Alpha-1d adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL223] [GtoPdb: 24] [UniProtKB: P25100]
ChEMBL DRUGMATRIX: Alpha-1D adrenergic receptor radioligand binding (ligand: prazosin) B 5.79 pKi 1617 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Alpha-1D adrenergic receptor radioligand binding (ligand: prazosin) B 5.48 pIC50 3289 nM IC50 DrugMatrix in vitro pharmacology data
DAT/Dopamine transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL238] [GtoPdb: 927] [UniProtKB: Q01959]
ChEMBL In vitro binding affinity against human dopamine transporter in dog kidney cell line by using [125I]RTI-55 radioligand B 4.78 pKi 16540 nM Ki J. Med. Chem. (2004) 47: 1122-1135 [PMID:14971892]
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 5 pKi >10000 nM Ki J. Med. Chem. (1990) 33: 2793-2797 [PMID:2213832]
ChEMBL Tested in vitro for serotonin(5-HT) neuronal uptake inhibition B 8.54 pKi 2.9 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 Displacement of [3H]GBR-12935 from dopamine transporter of rat caudate-putamen B 4.78 pKi 16540 nM Ki Bioorg. Med. Chem. Lett. (2005) 15: 1131-1133 [PMID:15686927]
ChEMBL Displacement of [3H]WIN-35428 from DAT in rat caudate-putamen by scintillation counting B 5.03 pKi 9270 nM Ki J. Med. Chem. (2010) 53: 6112-6121 [PMID:20672825]
ChEMBL Inhibition of dopamine uptake in rat synaptosomal fraction F 4.39 pIC50 41000 nM IC50 J. Med. Chem. (1985) 28: 1817-1828 [PMID:2999402]
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 4.86 pKi 13661.8 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Potassium Channel HERG radioligand binding (ligand: [3H] Astemizole) B 4.78 pIC50 16675.4 nM IC50 DrugMatrix in vitro pharmacology data
ChEMBL Inhibition of human Potassium channel HERG expressed in mammalian cells B 5.4 pIC50 3981.07 nM IC50 Bioorg. Med. Chem. Lett. (2003) 13: 2773-2775 [PMID:12873512]
ChEMBL Inhibitory concentration against potassium channel HERG B 5.4 pIC50 3981.07 nM IC50 Bioorg. Med. Chem. Lett. (2005) 15: 2886-2890 [PMID:15911273]
ChEMBL Inhibition of human ERG expressed in CHO cells by whole cell patch clamp technique B 5.4 pIC50 3981.07 nM IC50 Bioorg. Med. Chem. (2008) 16: 6252-6260 [PMID:18448342]
ChEMBL Inhibition of human ERG B 5.4 pIC50 3981.07 nM IC50 Eur. J. Med. Chem. (2011) 46: 618-630 [PMID:21185626]
ChEMBL Inhibition of human ERG B 8 pIC50 10 nM IC50 J. Med. Chem. (2013) 56: 8955-8971 [PMID:23919353]
H1 receptor/Histamine H1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL231] [GtoPdb: 262] [UniProtKB: P35367]
ChEMBL DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine) B 6.43 pKi 371 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine) B 5.5 pIC50 3194 nM IC50 DrugMatrix in vitro pharmacology data
NET/Norepinephrine transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL222] [GtoPdb: 926] [UniProtKB: P23975]
ChEMBL In vitro binding affinity against human norepinephrine transporter in human embryonic kidney cell line by using [3H]-nisoxatine radioligand B 5.21 pKi 6190 nM Ki J. Med. Chem. (2004) 47: 1122-1135 [PMID:14971892]
ChEMBL DRUGMATRIX: Norepinephrine Transporter radioligand binding (ligand: [125I] RTI-55) B 5.66 pKi 2178 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Norepinephrine Transporter radioligand binding (ligand: [125I] RTI-55) B 5.66 pIC50 2196 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 6 pKi >1000 nM Ki J. Med. Chem. (1990) 33: 2793-2797 [PMID:2213832]
Norepinephrine transporter in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL304] [UniProtKB: Q9WTR4]
ChEMBL Displacement of [3H]nisoxetine from norepinephrine transporter of rat cerebral cortex B 5.21 pKi 6190 nM Ki Bioorg. Med. Chem. Lett. (2005) 15: 1131-1133 [PMID:15686927]
ChEMBL Inhibition of noradrenaline uptake in rat synaptosomal fraction F 5.06 pIC50 8800 nM IC50 J. Med. Chem. (1985) 28: 1817-1828 [PMID:2999402]
5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327]
ChEMBL Binding affinity of a compound to rat brain 5-hydroxytryptamine 1A (serotonin) receptor assayed by radiolabeled [3H]-8-OH-DPAT ligand displacement B 4.3 pKi 50118.72 nM Ki J. Med. Chem. (1996) 39: 126-134 [PMID:8568799]
5-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595]
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide) B 5.93 pKi 1171 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide) B 5.74 pIC50 1839 nM IC50 DrugMatrix in vitro pharmacology data
5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335]
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2C radioligand binding (ligand: [3H] Mesulergine) B 6.81 pKi 156 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2C radioligand binding (ligand: [3H] Mesulergine) B 6.53 pIC50 297 nM IC50 DrugMatrix in vitro pharmacology data
SERT/Serotonin transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL228] [GtoPdb: 928] [UniProtKB: P31645]
GtoPdb - - 8.3 pKd 5 nM Kd
ChEMBL Displacement of [3H]paroxetine from human SERT expressed in HEK293 cells B 7.48 pKi 32.8 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 7.48 pKi 32.8 nM Ki Bioorg. Med. Chem. (2008) 16: 6364-6370 [PMID:18487050]
ChEMBL Inhibition of [3H]5-HT uptake at human SERT expressed in COS7 cells after 3 mins by beta-counting B 7.8 pKi 16 nM Ki Bioorg. Med. Chem. Lett. (2013) 23: 323-326 [PMID:23168018]
ChEMBL Displacement of [3H]citalopram from human SERT expressed in HEK293 cells B 8.36 pKi 4.38 nM Ki Bioorg. Med. Chem. Lett. (2008) 18: 4727-4730 [PMID:18644726]
ChEMBL Displacement of [3H]citalopram from human SERT expressed in HEK293 cells B 8.36 pKi 4.38 nM Ki Bioorg. Med. Chem. (2008) 16: 6364-6370 [PMID:18487050]
ChEMBL Inhibition of [125I]RTI-55 binding to human serotonin transporter expressed in human embryonic kidney cells B 8.8 pKi 1.6 nM Ki J. Med. Chem. (2004) 47: 1122-1135 [PMID:14971892]
ChEMBL DRUGMATRIX: Transporter, Serotonin (5-Hydroxytryptamine) (SERT) radioligand binding (ligand: [3H] Paroxetine) B 9.32 pKi 0.48 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL Inhibition of SERT (unknown origin) assessed as inhibition of serotonin uptake B 4.05 pIC50 90000 nM IC50 J. Med. Chem. (2013) 56: 9709-9724 [PMID:24237160]
ChEMBL Inhibition of [3H]-serotonin reuptake at human SERT expressed in HEK293 cells after 15 to 20 mins by fluorescence neurotransmitter transporter assay B 7.72 pIC50 19 nM IC50 Bioorg. Med. Chem. (2011) 19: 1328-1348 [PMID:21227702]
ChEMBL Inhibition of [3H]5-HT uptake by SERT primary site (S1) (unknown origin) expressed in African green monkey COS1 cells after 10 mins by TopCount scintillation counting method B 8.17 pIC50 6.7 nM IC50 Bioorg Med Chem Lett (2017) 27: 470-478 [PMID:28041833]
ChEMBL Inhibition of SERT (unknown origin) expressed in HEK293 cells assessed as reduction in 5-HT uptake incubated for 30 mins B 8.2 pIC50 6.27 nM IC50 Bioorg Med Chem (2018) 26: 3117-3125 [PMID:29729987]
ChEMBL DRUGMATRIX: Transporter, Serotonin (5-Hydroxytryptamine) (SERT) radioligand binding (ligand: [3H] Paroxetine) B 9.04 pIC50 0.9 nM IC50 DrugMatrix in vitro pharmacology data
ChEMBL Inhibition of [3H]-S-citalopram dissociation from SERT allosteric modulator site (S2) (unknown origin) expressed in African green monkey COS1 cell membranes by scintillation counting method B 5.06 pEC50 8700 nM EC50 Bioorg Med Chem Lett (2017) 27: 470-478 [PMID:28041833]
SERT/Serotonin transporter in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL313] [GtoPdb: 928] [UniProtKB: P31652]
ChEMBL Displacement of [3H]citalopram from SERT in rat brain stem by scintillation counting B 8.71 pKi 1.94 nM Ki J. Med. Chem. (2010) 53: 6112-6121 [PMID:20672825]
ChEMBL Displacement of [3H]paroxetine from serotonin transporter of rat cerebral cortex B 8.8 pKi 1.6 nM Ki Bioorg. Med. Chem. Lett. (2005) 15: 1131-1133 [PMID:15686927]
ChEMBL Inhibition of [3H]citalopram binding to Serotonin transporter of rat cerebral cortex B 8.82 pKi 1.5 nM Ki Bioorg. Med. Chem. Lett. (2000) 10: 1559-1562 [PMID:10915050]
ChEMBL Inhibition of SERT-mediated [3H]5HT uptake in rat synaptosomes by scintillation counting B 8.41 pIC50 3.9 nM IC50 J. Med. Chem. (2011) 54: 3206-3221 [PMID:21486038]
ChEMBL Inhibition of [3H]5-HT reuptake at rat SERT expressed in HEK293 cells after 2 mins by liquid scintillation counting B 8.5 pIC50 3.17 nM IC50 Eur. J. Med. Chem. (2009) 44: 4862-4888 [PMID:19717215]
ChEMBL Displacement of [3H]paroxetine from SERT in rat cortical membranes after 6 mins by liquid scintillation counting B 8.52 pIC50 3 nM IC50 Bioorg. Med. Chem. (2013) 21: 7604-7611 [PMID:24262884]
ChEMBL Inhibition of 5-HT uptake in rat synaptosomal fraction F 8.74 pIC50 1.8 nM IC50 J. Med. Chem. (1985) 28: 1817-1828 [PMID:2999402]
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 6.78 pKi 167 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Sigma1 radioligand binding (ligand: [3H] Haloperidol) B 6.4 pIC50 398 nM IC50 DrugMatrix in vitro pharmacology data
Organic cation transporter 1/Solute carrier family 22 member 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5685] [GtoPdb: 1019] [UniProtKB: O15245]
ChEMBL Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells by confocal microscopy B 4.73 pIC50 18800 nM IC50 J. Med. Chem. (2008) 51: 5932-5942 [PMID:18788725]
Transporter in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6184] [UniProtKB: Q63380]
ChEMBL Displacement of [3H]nisoxetine from NET in rat frontal cortex by scintillation counting B 5.23 pKi 5950 nM Ki J. Med. Chem. (2010) 53: 6112-6121 [PMID:20672825]
Cav1.2/Voltage-gated L-type calcium channel alpha-1C subunit in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3762] [GtoPdb: 529] [UniProtKB: P22002]
ChEMBL Inhibition of L-type calcium channel measured using whole-cell patch clamp in rat ventricular myocytes F 4.19 pIC50 64500 nM IC50 Journal of Applied Toxicology (2012) 32: 858-866 [PMID:22761000]

ChEMBL data shown on this page come from version 27:

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]