imipramine [Ligand Id: 357] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL11 (Antideprin, Berkomine, Cristalia, Imipramine, Janimine, Melipramine, NSC-169866, ORG-2463, Pramine, Presamine, Sermonil, Tofranil, Tofranil-PM, Trimipramine maleate impurity, imipramine-)
  • α1A-adrenoceptor/Alpha-1a adrenergic receptor in Rat [ChEMBL: CHEMBL319] [GtoPdb: 22] [UniProtKB: P43140]
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  • D2 receptor/Dopamine D2 receptor in Human [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
  • D2 receptor/Dopamine D2 receptor in Mouse [ChEMBL: CHEMBL3427] [GtoPdb: 215] [UniProtKB: P61168]
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  • H1 receptor/Histamine H1 receptor in Human [ChEMBL: CHEMBL231] [GtoPdb: 262] [UniProtKB: P35367]
  • H1 receptor/Histamine H1 receptor in Rat [ChEMBL: CHEMBL4701] [GtoPdb: 262] [UniProtKB: P31390]
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  • M5 receptor/Muscarinic acetylcholine receptor M5 in Rat [ChEMBL: CHEMBL277] [GtoPdb: 17] [UniProtKB: P08911]
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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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  • Pleiotropic ABC efflux transporter of multiple drugs in Saccharomyces cerevisiae S288c [ChEMBL: CHEMBL1697658] [UniProtKB: P33302]
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  • 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223]
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  • 5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335]
  • 5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Mouse [ChEMBL: CHEMBL3006] [GtoPdb: 8] [UniProtKB: P34968]
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  • sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Rat [ChEMBL: CHEMBL3602] [GtoPdb: 2552] [UniProtKB: Q9R0C9]
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  • Organic cation transporter 1/Solute carrier family 22 member 1 in Human [ChEMBL: CHEMBL5685] [GtoPdb: 1019] [UniProtKB: O15245]
  • Organic cation transporter 1/Solute carrier family 22 member 1 in Rat [ChEMBL: CHEMBL2073670] [GtoPdb: 1019] [UniProtKB: Q63089]
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  • Organic cation transporter 2/Solute carrier family 22 member 2 in Rat [ChEMBL: CHEMBL1770032] [GtoPdb: 1020] [UniProtKB: Q9R0W2]
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  • Organic cation transporter 3/Solute carrier family 22 member 3 in Human [ChEMBL: CHEMBL2073673] [GtoPdb: 1021] [UniProtKB: O75751]
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  • sphingomyelin phosphodiesterase 1/Sphingomyelin phosphodiesterase in Human [ChEMBL: CHEMBL2760] [GtoPdb: 2514] [UniProtKB: P17405]
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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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  • Cav2.2/Voltage-gated N-type calcium channel alpha-1B subunit in Human [ChEMBL: CHEMBL4478] [GtoPdb: 533] [UniProtKB: Q00975]
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  • M2 receptor in Human [GtoPdb: 14] [UniProtKB: P08172]
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  • Kir3.2 in Mouse [GtoPdb: 435] [UniProtKB: P48542]
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  • Kir3.4 in Mouse [GtoPdb: 437] [UniProtKB: P48545]
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  • Kv10.1 in Human [GtoPdb: 570] [UniProtKB: O95259]
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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 Inhibition of binding of [3H]imipramine to imipramine receptor in rat brain B 8.77 pIC50 1.7 nM IC50 J Med Chem (1990) 33: 2899-2905 [PMID:1976813]
D2 receptor/Dopamine D2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
ChEMBL Binding affinity towards dopamine receptor D2 using [3H]spiperone as radioligand B 6.14 pKi 726 nM Ki Bioorg Med Chem Lett (2004) 14: 2279-2283 [PMID:15081025]
ChEMBL Binding affinity to dopamine D2 receptor (unknown origin) by radioligand binding assay B 6.39 pIC50 410 nM IC50 J Med Chem (2013) 56: 8955-8971 [PMID:23919353]
D2 receptor/Dopamine D2 receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3427] [GtoPdb: 215] [UniProtKB: P61168]
ChEMBL Binding affinity to Dopamine receptor D2 using [3H]spiperone as radioligand in stably transfected NIH3T3 cells B 6.14 pKi 726 nM Ki Bioorg Med Chem Lett (2001) 11: 655-658 [PMID:11266163]
DAT/Dopamine transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL238] [GtoPdb: 927] [UniProtKB: Q01959]
ChEMBL Inhibition of [3H]dopamine uptake at human DAT expressed in HEK293 cells B 4.59 pIC50 25600 nM IC50 Antimicrob Agents Chemother (2007) 51: 4133-4140 [PMID:17846138]
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]
DAT/Dopamine transporter in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL338] [GtoPdb: 927] [UniProtKB: P23977]
ChEMBL Inhibition of the uptake of tritiated dopamine (DA) in rat synaptosomes B 5 pKi >10000 nM Ki J Med Chem (1987) 30: 1433-1454 [PMID:3039136]
ChEMBL Inhibition of dopamine uptake in synaptosomal preparation in rat corpus striatum, using [3H]dopamine F 4.7 pIC50 20000 nM IC50 J Med Chem (1984) 27: 1508-1515 [PMID:6492080]
GluN1/GluN2A/GluN2B/GluN2C/GluN2D/GluN3B/GluN3A/Glutamate NMDA receptor in Rat (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL1907608] [GtoPdb: 455, 456, 457, 458, 459, 461, 460] [UniProtKB: P35439, Q00959, Q00960, Q00961, Q62645, Q8VHN2, Q9R1M7]
ChEMBL Inhibition of [3H]MK-801 binding to NMDA receptor of rat cerebral cortical synaptic membrane B 4.85 pIC50 14000 nM IC50 J Med Chem (1995) 38: 2964-2968 [PMID:7636857]
Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809]
ChEMBL K+ channel blocking activity in Chinese hamster ovary cells expressing HERG Kv11.1 F 5.47 pIC50 3400 nM IC50 J Med Chem (2002) 45: 3844-3853 [PMID:12190308]
ChEMBL Inhibition of hERG K channel F 5.47 pIC50 3400 nM IC50 Cardiovasc Res (2011) 91: 53-61 [PMID:21300721]
ChEMBL Inhibition of partially open human voltage-gated potassium channel subunit Kv11.1 (ERG K+ channel) F 5.47 pIC50 3388.44 nM IC50 Bioorg Med Chem Lett (2005) 15: 1737-1741 [PMID:15745831]
ChEMBL Inhibitory concentration against potassium channel HERG B 5.47 pIC50 3388.44 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 5.47 pIC50 3388.44 nM IC50 Bioorg Med Chem (2008) 16: 6252-6260 [PMID:18448342]
ChEMBL Inhibition of human ERG in MCF7 cells B 5.47 pIC50 3388.44 nM IC50 Eur J Med Chem (2009) 44: 1926-1932 [PMID:19110341]
ChEMBL Inhibition of human ERG B 5.47 pIC50 3388.44 nM IC50 Eur J Med Chem (2011) 46: 618-630 [PMID:21185626]
ChEMBL Inhibition of human Potassium channel HERG expressed in mammalian cells B 5.47 pIC50 3388.44 nM IC50 Bioorg Med Chem Lett (2003) 13: 2773-2775 [PMID:12873512]
H1 receptor/Histamine H1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL231] [GtoPdb: 262] [UniProtKB: P35367]
ChEMBL Binding affinity to H1 receptor (unknown origin) B 8 pKi 10 nM Ki Bioorg Med Chem Lett (2020) 30: 127493-127493 [PMID:32798652]
ChEMBL Binding affinity to histamine H1 receptor (unknown origin) by radioligand binding assay B 7.57 pIC50 27 nM IC50 J Med Chem (2013) 56: 8955-8971 [PMID:23919353]
H1 receptor/Histamine H1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4701] [GtoPdb: 262] [UniProtKB: P31390]
ChEMBL Compound tested for its inhibitory activity against Histamine H1 receptor B 10.22 pIC50 0.06 nM IC50 J Med Chem (1999) 42: 3154-3162 [PMID:10447960]
Histamine H2 receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2882] [UniProtKB: P47747]
ChEMBL Inhibitory activity against brain adenylate cyclase Histamine H2 receptor F 5.72 pIC50 1900 nM IC50 J Med Chem (1999) 42: 3154-3162 [PMID:10447960]
M5 receptor/Muscarinic acetylcholine receptor M5 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL277] [GtoPdb: 17] [UniProtKB: P08911]
ChEMBL Binding affinity towards muscarinic acetylcholine receptor by inhibiting specific binding of [3H]quinuclidinyl benzilate (0.8 nM) in vitro to membranes of rat brain without cerebellum B 6.52 pIC50 300 nM IC50 J Med Chem (1984) 27: 995-1003 [PMID:6747997]
NET/Norepinephrine transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL222] [GtoPdb: 926] [UniProtKB: P23975]
ChEMBL Binding affinity towards Norepinephrine transporter using [3H]nisoxitine as radioligand B 7.8 pKi 16 nM Ki Bioorg Med Chem Lett (2004) 14: 2279-2283 [PMID:15081025]
GtoPdb - - 7.8 pKi 16 nM Ki
ChEMBL Inhibition of [3H]norepinephrine uptake at human NET expressed in HEK293 cells B 7.13 pIC50 74 nM IC50 Antimicrob Agents Chemother (2007) 51: 4133-4140 [PMID:17846138]
NET/Norepinephrine transporter in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2370] [GtoPdb: 926] [UniProtKB: O55192]
ChEMBL Binding affinity to Norepinephrine transporter using [3H]-nisoxatine as radioligand in stably transfected NIH3T3 cells B 7.8 pKi 16 nM Ki Bioorg Med Chem Lett (2001) 11: 655-658 [PMID:11266163]
ChEMBL Tested in vitro for norepinephrine (NE) neuronal uptake inhibition B 7.92 pKi 12 nM Ki J Med Chem (1990) 33: 2793-2797 [PMID:2213832]
Norepinephrine transporter in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL304] [UniProtKB: Q9WTR4]
ChEMBL Inhibition of uptake of tritiated norepinephrine (NE) in rat synaptosomes B 7.92 pKi 12 nM Ki J Med Chem (1987) 30: 1433-1454 [PMID:3039136]
ChEMBL In vitro inhibition of accumulation of (-)-[3H]Norepinephrine (NA) in mouse brain slices F 5.89 pIC50 1300 nM IC50 J Med Chem (1981) 24: 1499-1507 [PMID:6458703]
ChEMBL Inhibition of uptake of tritiated norepinephrine (NE) into rat brain synaptosomes F 6.59 pIC50 260 nM IC50 J Med Chem (1990) 33: 2899-2905 [PMID:1976813]
ChEMBL Inhibition of norepinephrine uptake in synaptosomal preparation fro rat hypothalamus, using [3H]norepinephrine F 7.22 pIC50 60 nM IC50 J Med Chem (1984) 27: 1508-1515 [PMID:6492080]
Pleiotropic ABC efflux transporter of multiple drugs in Saccharomyces cerevisiae S288c (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1697658] [UniProtKB: P33302]
ChEMBL Inhibition of Pdr5p-mediated rhodamine 6G transport in Saccharomyces cerevisiae MKPDR5h plasma membrane by spectrofluorometric assay B 4.66 pIC50 22000 nM IC50 Antimicrob Agents Chemother (2009) 53: 1516-1527 [PMID:19188399]
Prion protein in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4869] [UniProtKB: P04156]
ChEMBL Half maximal inhibition of Prion protein PrPsc formation was assayed in ScN2a cells B 5 pEC50 10000 nM EC50 J Med Chem (2003) 46: 3563-3564 [PMID:12904059]
5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223]
ChEMBL Displacement of [3H]ketanserin from 5-hydroxytryptamine 2A receptor expressed NIH3T3 cells B 6.8 pKi 160 nM Ki Bioorg Med Chem Lett (2001) 11: 655-658 [PMID:11266163]
ChEMBL Binding affinity towards 5-hydroxytryptamine 2A receptor using [3H]ketanserin B 7.03 pKi 94 nM Ki Bioorg Med Chem Lett (2004) 14: 2279-2283 [PMID:15081025]
ChEMBL Binding affinity to 5HT2A receptor (unknown origin) by radioligand binding assay B 6.66 pIC50 220 nM IC50 J Med Chem (2013) 56: 8955-8971 [PMID:23919353]
5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335]
ChEMBL Binding affinity towards 5-hydroxytryptamine 2C receptor using [3H]mesulergine as radioligand B 6.8 pKi 160 nM Ki Bioorg Med Chem Lett (2004) 14: 2279-2283 [PMID:15081025]
5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3006] [GtoPdb: 8] [UniProtKB: P34968]
ChEMBL Binding affinity to 5-hydroxytryptamine 2C receptor using [3H]Mesulergine as radioligand in stably transfected NIH3T3 cells B 6.8 pKi 160 nM Ki Bioorg Med Chem Lett (2001) 11: 655-658 [PMID:11266163]
SERT/Serotonin transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL228] [GtoPdb: 928] [UniProtKB: P31645]
ChEMBL Inhibition of human SERT I172M mutant expressed in HEK293 MSR cells assessed as [3H]-5-HT uptake preincubated for 30 mins followed addition of [3H]-5HT and compound for 10 mins by micro-scintillation counter B 5.89 pKi 1300 nM Ki Bioorg Med Chem (2016) 24: 2725-2738 [PMID:27160055]
ChEMBL Inhibition of wild-type human SERT expressed in HEK293 MSR cells assessed as [3H]-5-HT uptake preincubated for 30 mins followed addition of [3H]-5HT and compound for 10 mins by micro-scintillation counter B 7.51 pKi 31 nM Ki Bioorg Med Chem (2016) 24: 2725-2738 [PMID:27160055]
GtoPdb Displacement of [3H]citalopram from hSERT. - 7.69 pKi 20.3 nM Ki J Nat Prod (1993) 56: 441-55 [PMID:8496700]
ChEMBL Displacement of [3H]citalopram from serotonin transporter B 7.69 pKi 20.3 nM Ki J Nat Prod (1993) 56: 441-455 [PMID:8496700]
ChEMBL Binding affinity to SERT (unknown origin) B 7.7 pKi 20 nM Ki Bioorg Med Chem Lett (2020) 30: 127493-127493 [PMID:32798652]
ChEMBL Inhibition of [3H]serotonin reuptake at serotonin transporter B 8.12 pKi 7.57 nM Ki J Med Chem (2009) 52: 5872-5879 [PMID:19791802]
ChEMBL Inhibition of human SERT I179C mutant expressed in HEK293 MSR cells assessed as [3H]-5-HT uptake preincubated for 30 mins followed addition of [3H]-5HT and compound for 10 mins by micro-scintillation counter B 8.24 pKi 5.7 nM Ki Bioorg Med Chem (2016) 24: 2725-2738 [PMID:27160055]
ChEMBL Binding affinity towards Serotonin transporter using [3H]paroxetine as radioligand B 8.3 pKi 5 nM Ki Bioorg Med Chem Lett (2004) 14: 2279-2283 [PMID:15081025]
ChEMBL Displacement of radiolabeled imipramine from human SERT B 8.49 pKi 3.2 nM Ki J Med Chem (2008) 51: 7094-7098 [PMID:18983139]
ChEMBL Displacement of [3H]-imipramine from human serotonin transporter expressed in HEK293 cells membranes incubated for 30 mins by microbeta scintillation counting analysis B 8.6 pKi 2.5 nM Ki Eur J Med Chem (2019) 183: 111736-111736 [PMID:31586817]
ChEMBL Displacement of [3H]imipramine from human recombinant SERT expressed in CHO cells B 8.68 pKi 2.1 nM Ki J Med Chem (2014) 57: 4543-4557 [PMID:24805037]
ChEMBL Displacement of [3H]imipramine from human SERT expressed in CHO cells B 8.68 pKi 2.1 nM Ki Eur J Med Chem (2015) 92: 221-235 [PMID:25557493]
ChEMBL Displacement of [3H]citalopram from human SERT expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting method B 8.7 pKi 2 nM Ki Bioorg Med Chem (2017) 25: 293-304 [PMID:27865645]
ChEMBL Displacement of [3H] imipramine from human recombinant 5-HT transporter measured after 60 mins by scintillation counter method B 8.72 pKi 1.9 nM Ki Eur J Med Chem (2019) 176: 292-309 [PMID:31112891]
ChEMBL Displacement of [3H]-imipramine from human serotonin transporter expressed in HEK-293 cell membranes after 30 mins by scintillation counting B 9 pKi 1 nM Ki J Med Chem (2017) 60: 7483-7501 [PMID:28763213]
ChEMBL Displacement of [3H]imipramine from human 5HT transporter B 9.11 pKi 0.77 nM Ki J Med Chem (2011) 54: 5320-5334 [PMID:21726069]
ChEMBL Binding affinity to human 5-HT transporter by radioligand displacement assay B 9.28 pKi 0.52 nM Ki Eur J Med Chem (2013) 63: 85-94 [PMID:23466604]
ChEMBL Inhibition of SERT (unknown origin) B 7.54 pIC50 29 nM IC50 J Med Chem (2020) 63: 15187-15217 [PMID:33111525]
ChEMBL Inhibition of human SERT expressed in HEK293-MSR cells by 5-HT uptake assay B 7.54 pIC50 29 nM IC50 Bioorg Med Chem Lett (2013) 23: 1220-1224 [PMID:23385211]
ChEMBL Inhibition of [3H]5HT uptake at human SERT expressed in HEK293 cells B 8.1 pIC50 8 nM IC50 Antimicrob Agents Chemother (2007) 51: 4133-4140 [PMID:17846138]
ChEMBL Inhibition of human 5-HT transporter B 8.14 pIC50 7.3 nM IC50 Bioorg Med Chem (2010) 18: 7675-7699 [PMID:20875743]
ChEMBL Displacement of radiolabeled imipramine from human SERT B 8.16 pIC50 6.9 nM IC50 J Med Chem (2008) 51: 7094-7098 [PMID:18983139]
ChEMBL Displacement of [3H]imipramin from human recombinant SERT over-expressed in HEK293 cells B 8.17 pIC50 6.8 nM IC50 Bioorg Med Chem Lett (2013) 23: 5515-5518 [PMID:24012181]
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 8.29 pIC50 5.1 nM IC50 Bioorg Med Chem (2017) 25: 293-304 [PMID:27865645]
ChEMBL Percent inhibition against 5-hydroxytryptamine transporter at 1 uM nonselective B 8.36 pIC50 4.4 nM IC50 J Med Chem (2005) 48: 6887-6896 [PMID:16250647]
ChEMBL Displacement of [3H] imipramine from human recombinant 5-HT transporter measured after 60 mins by scintillation counter method B 8.39 pIC50 4.1 nM IC50 Eur J Med Chem (2019) 176: 292-309 [PMID:31112891]
ChEMBL Binding affinity to SERT (unknown origin) by radioligand binding assay B 8.46 pIC50 3.5 nM IC50 J Med Chem (2013) 56: 8955-8971 [PMID:23919353]
ChEMBL Inhibition of human SERT W103A mutant expressed in HEK293 MSR cells assessed as [3H]-5-HT uptake preincubated for 30 mins followed addition of [3H]-5HT and compound for 10 mins by micro-scintillation counter B 8.59 pIC50 2.6 nM IC50 Bioorg Med Chem (2016) 24: 2725-2738 [PMID:27160055]
ChEMBL Binding affinity to human serotonin 5-HT transporter by radioligand displacement assay B 8.7 pIC50 2 nM IC50 Bioorg Med Chem (2013) 21: 2764-2771 [PMID:23582449]
ChEMBL Binding affinity to human 5-HT transporter by radioligand displacement assay B 8.96 pIC50 1.1 nM IC50 Eur J Med Chem (2013) 63: 85-94 [PMID:23466604]
ChEMBL Displacement of [3H]imipramine from human recombinant 5HT transporter expressed in CHO cells measured after 60 mins by scintillation counting method B 9.06 pIC50 0.88 nM IC50 Bioorg Med Chem (2017) 25: 471-482 [PMID:27876250]
ChEMBL Displacement of [3H]imipramine from human recombinant 5-HT transporter expressed in CHO cells B 9.06 pIC50 0.88 nM IC50 Bioorg Med Chem (2016) 24: 1793-1810 [PMID:26988801]
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 7.38 pKi 42 nM Ki J Med Chem (1990) 33: 2793-2797 [PMID:2213832]
ChEMBL Binding affinity to Serotonin transporter using [3H]-paroxetine as radioligand in stably transfected NIH3T3 cells B 8.3 pKi 5 nM Ki Bioorg Med Chem Lett (2001) 11: 655-658 [PMID:11266163]
SERT/Serotonin transporter in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL313] [GtoPdb: 928] [UniProtKB: P31652]
ChEMBL Inhibition the uptake of tritiated serotonin (5-HT) by the serotonin transporter SERT in rat synaptosomes B 7.38 pKi 41.8 nM Ki J Med Chem (1987) 30: 1433-1454 [PMID:3039136]
ChEMBL Displacement of [3H]-citalopram from SERT in rat cortex tissue incubated for 60 mins by microbeta scintillation counting method B 7.54 pKi 29 nM Ki Eur J Med Chem (2019) 180: 383-397 [PMID:31325785]
ChEMBL Displacement of [3H]-citalopram from SERT in rat cortex tissue measured after 60 mins by microbeta scintillation counting analysis B 7.54 pKi 29 nM Ki Eur J Med Chem (2019) 166: 144-158 [PMID:30703658]
ChEMBL Inhibition of 5-HT uptake in synaptosomal preparation from rat corpus striatum, using [3H]5-HT F 6.09 pIC50 810 nM IC50 J Med Chem (1984) 27: 1508-1515 [PMID:6492080]
ChEMBL In vitro inhibition of accumulation of [14C]5-HT (5-HT) in mouse brain slices F 6.52 pIC50 300 nM IC50 J Med Chem (1981) 24: 1499-1507 [PMID:6458703]
ChEMBL Inhibition of uptake of tritiated serotonin (5-HT) into rat brain synaptosomes F 6.92 pIC50 120 nM IC50 J Med Chem (1990) 33: 2899-2905 [PMID:1976813]
ChEMBL Inhibition of SERT expressed in rat brain synaptosomes assessed as decrease in incorporation of [3H]serotonin measured after 15 mins by scintillation counting method B 7.21 pIC50 61 nM IC50 J Med Chem (2017) 60: 7483-7501 [PMID:28763213]
σ2/Sigma intracellular receptor 2 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105864] [GtoPdb: 2553] [UniProtKB: Q5U3Y7]
ChEMBL Displacement of [3H]DTG from sigma 2 receptor in Sprague-Dawley rat brain membranes in presence of (+)-pentazocine by scintillation counting method B 5.68 pKi 2107 nM Ki J Med Chem (2020) 63: 15187-15217 [PMID:33111525]
sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3602] [GtoPdb: 2552] [UniProtKB: Q9R0C9]
ChEMBL Displacement of [3H]-(+)-pentazocine from sigma 1 receptor in Sprague-Dawley rat brain membranes by scintillation counting method B 6.46 pKi 343 nM Ki J Med Chem (2020) 63: 15187-15217 [PMID:33111525]
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 4.77 pIC50 17100 nM IC50 J Med Chem (2008) 51: 5932-5942 [PMID:18788725]
ChEMBL Inhibition of human OCT1 expressed in HEK293 cells assessed as decrease in uptake of ASP+ after 2 mins by fluorescence assay B 5.1 pIC50 7950 nM IC50 J Med Chem (2017) 60: 2685-2696 [PMID:28230985]
Organic cation transporter 1/Solute carrier family 22 member 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2073670] [GtoPdb: 1019] [UniProtKB: Q63089]
ChEMBL TP_TRANSPORTER: inhibition of TEA uptake (TEA: 50 uM) in OCT1-expressing MDCK cells F 4.8 pIC50 16000 nM IC50 Pharm Res (2001) 18: 1528-1534 [PMID:11758759]
Organic cation transporter 2/Solute carrier family 22 member 2 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1770032] [GtoPdb: 1020] [UniProtKB: Q9R0W2]
ChEMBL TP_TRANSPORTER: inhibition of TEA uptake (TEA: 50 uM) in OCT2-expressing MDCK cells F 5 pIC50 9900 nM IC50 Pharm Res (2001) 18: 1528-1534 [PMID:11758759]
Organic cation transporter 3/Solute carrier family 22 member 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2073673] [GtoPdb: 1021] [UniProtKB: O75751]
ChEMBL TP_TRANSPORTER: inhibition of MPP+ uptake in OCT3-expressing HRPE cells F 4.38 pKi 42000 nM Ki Am J Physiol Renal Physiol (2000) 279: F449-F458 [PMID:10966924]
sphingomyelin phosphodiesterase 1/Sphingomyelin phosphodiesterase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2760] [GtoPdb: 2514] [UniProtKB: P17405]
ChEMBL Inhibition of mmLDL-stimulated acid sphingomyelinase in human PBMC lysates using 3H-sphingomyelin as substrate preincubated for 30 mins followed by mmLDL stimulation measured after 2 hrs by HPLC method B 5.3 pIC50 5000 nM IC50 Eur J Med Chem (2018) 153: 73-104 [PMID:29031494]
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 5.08 pIC50 8300 nM IC50 J Appl Toxicol (2012) 32: 858-866 [PMID:22761000]
ChEMBL Inhibition of L-type calcium channel measured using whole-cell patch clamp in rat ventricular myocytes F 5.39 pIC50 4050 nM IC50 J Appl Toxicol (2012) 32: 858-866 [PMID:22761000]
Cav2.2/Voltage-gated N-type calcium channel alpha-1B subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4478] [GtoPdb: 533] [UniProtKB: Q00975]
ChEMBL Inhibition of endogenous human CaV2.2 in human SH-SY5Y cells in presence of nifedipine by Calcium 4 dye based calcium influx fluorescence-imaging assay B 4.66 pIC50 22000 nM IC50 RSC Med Chem (2022) 13: 183-195 [PMID:35308021]
M2 receptor in Human [GtoPdb: 14] [UniProtKB: P08172]
GtoPdb - - 6.9 pKi - - - J Pharmacol Exp Ther (1998) 284: 500-7 [PMID:9454790]
Kir3.2 in Mouse [GtoPdb: 435] [UniProtKB: P48542]
GtoPdb - - 4.3 pIC50 - - - Neuropsychopharmacology (2004) 29: 1841-51 [PMID:15150531]
Kir3.4 in Mouse [GtoPdb: 437] [UniProtKB: P48545]
GtoPdb - - 4.5 pEC50 - - - Neuropsychopharmacology (2004) 29: 1841-51 [PMID:15150531]
Kv10.1 in Human [GtoPdb: 570] [UniProtKB: O95259]
GtoPdb - - 5.7 pIC50 - - - J Gen Physiol (2004) 124: 301-17 [PMID:15365094]

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]