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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  • 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]
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]
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]