desipramine [Ligand Id: 2399] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL72 (Desipramine, Imipramine, demethyl-, Monodemethylimipramine, N-desmethylimipramine, Norimipramine)
  • α1A-adrenoceptor/Alpha-1a adrenergic receptor in Rat [ChEMBL: CHEMBL319] [GtoPdb: 22] [UniProtKB: P43140]
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  • H1 receptor/Histamine H1 receptor in Rat [ChEMBL: CHEMBL4701] [GtoPdb: 262] [UniProtKB: P31390]
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  • H3 receptor/Histamine H3 receptor in Human [ChEMBL: CHEMBL264] [GtoPdb: 264] [UniProtKB: Q9Y5N1]
  • H3 receptor/Histamine H3 receptor in Rat [ChEMBL: CHEMBL4124] [GtoPdb: 264] [UniProtKB: Q9QYN8]
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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-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223]
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  • Nav1.5/Sodium channel protein type V alpha subunit in Human [ChEMBL: CHEMBL1980] [GtoPdb: 582] [UniProtKB: Q14524]
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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 Human [ChEMBL: CHEMBL1743122] [GtoPdb: 1020] [UniProtKB: O15244]
  • 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]
  • Organic cation transporter 3/Solute carrier family 22 member 3 in Rat [ChEMBL: CHEMBL1770033] [GtoPdb: 1021] [UniProtKB: O88446]
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  • Organic cation/carnitine transporter 1/Solute carrier family 22 member 4 in Rat [ChEMBL: CHEMBL2073667] [GtoPdb: 1022] [UniProtKB: Q9R141]
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  • Voltage-dependent L-type calcium channel subunit alpha-1C in Guinea pig [ChEMBL: CHEMBL2366456] [UniProtKB: O35505]
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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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  • Kir3.2 in Mouse [GtoPdb: 435] [UniProtKB: P48542]
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  • Kir3.4 in Mouse [GtoPdb: 437] [UniProtKB: P48545]
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  • Plasma membrane monoamine transporter in Human [GtoPdb: 1120] [UniProtKB: Q7RTT9]
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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 6.89 pIC50 130 nM IC50 J Med Chem (1990) 33: 2899-2905 [PMID:1976813]
ChEMBL Compound was tested for its inhibitory activity against Alpha-1 adrenergic receptor B 9.6 pIC50 0.25 nM IC50 J Med Chem (1999) 42: 3154-3162 [PMID:10447960]
DAT/Dopamine transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL238] [GtoPdb: 927] [UniProtKB: Q01959]
ChEMBL Compound was tested for inhibition of [3H]WIN-35428 binding to the human (DAT) dopamine transporter B 5.52 pKi 3000 nM Ki J Med Chem (1999) 42: 2721-2736 [PMID:10425082]
ChEMBL In vitro competitive binding versus [N-methyl-3H]WIN-35428 in murine kidney cells transfected with cDNA for human dopamine transporter (DAT) B 9.31 pKi 0.49 nM Ki J Med Chem (2003) 46: 925-935 [PMID:12620070]
ChEMBL Inhibition of [3H]dopamine uptake at human DAT expressed in HEK293 cells B 4.09 pIC50 82000 nM IC50 Antimicrob Agents Chemother (2007) 51: 4133-4140 [PMID:17846138]
ChEMBL Inhibition of [3H]dopamine uptake in human DAT P387A mutant transfected HEK293 cells B 4.3 pIC50 50500 nM IC50 Science (2007) 317: 1390-1393 [PMID:17690258]
ChEMBL Inhibition of [3H]dopamine uptake in human wild type DAT transfected HEK293 cells B 4.32 pIC50 47900 nM IC50 Science (2007) 317: 1390-1393 [PMID:17690258]
ChEMBL Inhibition of [3H]dopamine uptake in human DAT I390V mutant transfected HEK293 cells B 4.75 pIC50 17700 nM IC50 Science (2007) 317: 1390-1393 [PMID:17690258]
ChEMBL Inhibition of [3H]dopamine uptake in human DAT F472L mutant transfected HEK293 cells B 5 pIC50 9900 nM IC50 Science (2007) 317: 1390-1393 [PMID:17690258]
DAT/Dopamine transporter in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL338] [GtoPdb: 927] [UniProtKB: P23977]
ChEMBL Ability to inhibit reuptake of dopamine ([3H]DA) at dopamine transporter of rat striatum B 5 pKi >10000 nM Ki Bioorg Med Chem Lett (2003) 13: 3565-3569 [PMID:14505672]
ChEMBL Inhibitory constant against reuptake of [3H]-DA at dopamine transporter of rat striatal membranes B 5 pKi >10000 nM Ki Bioorg Med Chem Lett (2005) 15: 2461-2465 [PMID:15863297]
ChEMBL Inhibition of the uptake of tritiated dopamine (DA) in rat synaptosomes B 5.19 pKi 6530 nM Ki J Med Chem (1987) 30: 1433-1454 [PMID:3039136]
ChEMBL Inhibitory constant towards reuptake of [125I]-12 from dopamine transporter in rat striatal membranes B 5.4 pKi >4000 nM Ki J Med Chem (1994) 37: 1535-1542 [PMID:8182712]
ChEMBL Inhibition of the reuptake of dopamine in rat corpora striata. F 5.11 pIC50 7800 nM IC50 J Med Chem (1989) 32: 1805-1813 [PMID:2754707]
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 4.64 pKi 22816.6 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Potassium Channel HERG radioligand binding (ligand: [3H] Astemizole) B 4.56 pIC50 27849.7 nM IC50 DrugMatrix in vitro pharmacology data
ChEMBL Inhibition of human Potassium channel HERG expressed in mammalian cells B 5.82 pIC50 1513.56 nM IC50 Bioorg Med Chem Lett (2003) 13: 2773-2775 [PMID:12873512]
ChEMBL Inhibition of human ERG channel B 5.86 pIC50 1390 nM IC50 J Med Chem (2009) 52: 4266-4276 [PMID:19534531]
ChEMBL Inhibition of hERG K channel F 5.86 pIC50 1390 nM IC50 Cardiovasc Res (2011) 91: 53-61 [PMID:21300721]
ChEMBL Inhibition of human ERG channel B 5.86 pIC50 1390 nM IC50 J Med Chem (2009) 52: 4266-4276 [PMID:19534531]
ChEMBL Inhibition of human ERG B 5.86 pIC50 1380.38 nM IC50 Eur J Med Chem (2011) 46: 618-630 [PMID:21185626]
ChEMBL Inhibition of human ERG expressed in CHO cells by whole cell patch clamp technique B 5.86 pIC50 1380.38 nM IC50 Bioorg Med Chem (2008) 16: 6252-6260 [PMID:18448342]
ChEMBL Inhibitory concentration against potassium channel HERG B 5.86 pIC50 1380.38 nM IC50 Bioorg Med Chem Lett (2005) 15: 2886-2890 [PMID:15911273]
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 9.1 pIC50 0.8 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 5.42 pIC50 3800 nM IC50 J Med Chem (1999) 42: 3154-3162 [PMID:10447960]
H3 receptor/Histamine H3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL264] [GtoPdb: 264] [UniProtKB: Q9Y5N1]
ChEMBL Displacement of [3H]N-R-methylhistamine from human H3 receptor isolated from C6 cells B 5.3 pKi >5000 nM Ki J Med Chem (2010) 53: 7869-7873 [PMID:20945906]
H3 receptor/Histamine H3 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4124] [GtoPdb: 264] [UniProtKB: Q9QYN8]
ChEMBL Displacement of [3H]N-R-methylhistamine from rat H3 receptor B 5.3 pKi >5000 nM Ki J Med Chem (2010) 53: 7869-7873 [PMID:20945906]
NET/Norepinephrine transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL222] [GtoPdb: 926] [UniProtKB: P23975]
ChEMBL Inhibition of human NET B 9.08 pKd 0.83 nM Kd J Med Chem (2010) 53: 7869-7873 [PMID:20945906]
ChEMBL Displacement of [3H]DMI from norepinephrine transporter B 6.24 pKi 580 nM Ki J Nat Prod (1993) 56: 441-455 [PMID:8496700]
ChEMBL Inhibition of [3H]norepinephrine reuptake at norepinephrine transporter B 8.29 pKi 5.11 nM Ki J Med Chem (2009) 52: 5872-5879 [PMID:19791802]
ChEMBL Inhibition of human NET-mediated norepinephrine uptake in MDCK-Net6 cells B 8.47 pKi 3.4 nM Ki J Med Chem (2010) 53: 4511-4521 [PMID:20462211]
ChEMBL Displacement of [3H]-Nisoxetine from human NET expressed in HEK cell membrane assessed as inhibition constant by radioligand binding assay B 8.52 pKi 3 nM Ki Bioorg Med Chem (2021) 51: 116509-116509 [PMID:34798381]
ChEMBL Displacement of [3H]nisoxetine from human NET expressed in HEK293 cells measured after 30 mins B 8.6 pKi 2.5 nM Ki J Med Chem (2016) 59: 6329-6343 [PMID:27309376]
ChEMBL Displacement of [3H]nisoxetine from human NET expressed in MDCK-Net6 cells B 8.68 pKi 2.1 nM Ki J Med Chem (2010) 53: 4511-4521 [PMID:20462211]
ChEMBL Displacement of [3H]nisoxetine from human norepinephrine transporter expressed in MDCK-Net6 cells B 8.68 pKi 2.1 nM Ki J Med Chem (2008) 51: 4038-4049 [PMID:18557608]
ChEMBL Inhibition of [3H]nisoxetine binding to human NET expressed in MDCK-Net6 cells by plate scintillation counting B 8.68 pKi 2.1 nM Ki J Med Chem (2009) 52: 5703-5711 [PMID:19722525]
ChEMBL Displacement of [3H]nisoxetine from human NET expressed in MDCK-Net6 cells B 8.68 pKi 2.1 nM Ki J Med Chem (2011) 54: 6824-6831 [PMID:21916421]
GtoPdb - - 8.68 pKi 2.1 nM Ki J Med Chem (2010) 53: 4511-21 [PMID:20462211]
ChEMBL Displacement of [3H]Nisoxetine from norepinephrine transporter (unknown origin) B 8.94 pKi 1.15 nM Ki Bioorg Med Chem Lett (2014) 24: 576-579 [PMID:24365159]
ChEMBL Displacement of [3H]Nisoxetine from norepinephrine transporter (unknown origin) B 8.96 pKi 1.1 nM Ki Bioorg Med Chem Lett (2014) 24: 576-579 [PMID:24365159]
ChEMBL Binding affinity at NET B 9 pKi 1 nM Ki Bioorg Med Chem (2007) 15: 616-625 [PMID:17123820]
ChEMBL Displacement of [125I]RTI55 from human recombinant norepinephrine transporter expressed in MDCK cells after 3 hrs B 9.04 pKi 0.92 nM Ki Bioorg Med Chem Lett (2013) 23: 1834-1838 [PMID:23403082]
ChEMBL Inhibition of norepinephrine reuptake at NET B 9.22 pKi 0.6 nM Ki Bioorg Med Chem (2009) 17: 7802-7815 [PMID:19836247]
ChEMBL Inhibition of [3H]norepinephrine uptake at human NET expressed in HEK293 cells B 8.38 pIC50 4.2 nM IC50 Antimicrob Agents Chemother (2007) 51: 4133-4140 [PMID:17846138]
ChEMBL Inhibition of norepinephrine transporter (unknown origin) B 8.41 pIC50 3.92 nM IC50 Eur J Med Chem (2022) 229: 114045-114045 [PMID:34922191]
ChEMBL Inhibition of norepinephrine uptake at human NET expressed in MDCK cells B 8.41 pIC50 3.9 nM IC50 Bioorg Med Chem Lett (2008) 18: 4929-4931 [PMID:18771916]
ChEMBL Inhibition of [3H]norepinephrine uptake at human NET expressed in MDCK-Net6 cells by scintillation counting B 8.47 pIC50 3.4 nM IC50 J Med Chem (2009) 52: 5703-5711 [PMID:19722525]
ChEMBL Inhibition of human NET expressed in MDCK-Net6 cells B 8.47 pIC50 3.4 nM IC50 Bioorg Med Chem Lett (2009) 19: 5807-5810 [PMID:19713106]
ChEMBL Inhibition of norepinephrine uptake at human norepinephrine transporter expressed in MDCK-Net6 cells B 8.47 pIC50 3.4 nM IC50 J Med Chem (2008) 51: 4038-4049 [PMID:18557608]
ChEMBL Inhibition of norepinephrine uptake at human NET expressed in MDCK-Net6 cells B 8.47 pIC50 3.4 nM IC50 J Med Chem (2010) 53: 2051-2062 [PMID:20131864]
ChEMBL Inhibition of norepinephrine reuptake at human NET expressed in MDCK-Net6 cells B 8.47 pIC50 3.4 nM IC50 Bioorg Med Chem Lett (2009) 19: 5029-5032 [PMID:19632110]
ChEMBL Inhibition of norepinephrine uptake at human NET expressed in MDCK-Net6 cells B 8.47 pIC50 3.4 nM IC50 Bioorg Med Chem Lett (2009) 19: 2464-2467 [PMID:19329313]
ChEMBL Inhibition of norepinephrine uptake at human NET expressed in MDCK-Net6 cells B 8.47 pIC50 3.4 nM IC50 Bioorg Med Chem Lett (2008) 18: 6067-6070 [PMID:18951020]
ChEMBL Inhibition of human NET transfected in MDCK-Net6 cells B 8.47 pIC50 3.4 nM IC50 Bioorg Med Chem Lett (2010) 20: 2809-2812 [PMID:20378347]
ChEMBL Inhibition of human NET expressed in MDCK-Net6 cells assessed as inhibition of norepinephrine uptake B 8.47 pIC50 3.4 nM IC50 J Med Chem (2011) 54: 6824-6831 [PMID:21916421]
ChEMBL Displacement of [3H]nisoxetine from human NET expressed in MDCK-Net6 cells B 8.48 pIC50 3.3 nM IC50 J Med Chem (2010) 53: 2051-2062 [PMID:20131864]
ChEMBL Displacement of [3H]Nisoxetine from human recombinant NET over-expressed in dog MDCK cells B 8.82 pIC50 1.5 nM IC50 Bioorg Med Chem Lett (2013) 23: 5515-5518 [PMID:24012181]
ChEMBL Displacement of [125I]RTI-55 from human NET expressed in MDCK cell membrane B 9.03 pIC50 0.93 nM IC50 J Nat Prod (2006) 69: 1305-1309 [PMID:16989524]
ChEMBL Displacement of [125I]RTI55 from human recombinant norepinephrine transporter expressed in MDCK cells after 3 hrs B 9.03 pIC50 0.93 nM IC50 Bioorg Med Chem Lett (2013) 23: 1834-1838 [PMID:23403082]
NET/Norepinephrine transporter in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2370] [GtoPdb: 926] [UniProtKB: O55192]
ChEMBL Inhibition of noradrenaline transporter in NMRI albino mouse brain assessed as [3H]NA accumulation in hypothalamus after 5 mins B 5.8 pIC50 1600 nM IC50 J Med Chem (1978) 21: 78-82 [PMID:22757]
Norepinephrine transporter in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL304] [UniProtKB: Q9WTR4]
ChEMBL Ability to inhibit reuptake of norepinephrine ([3H]NE) at norepinephrine transporter of rat parietal/occipital region B 8.13 pKi 7.36 nM Ki Bioorg Med Chem Lett (2003) 13: 3565-3569 [PMID:14505672]
ChEMBL Inhibitory constant against reuptake of [3H]NE at norepinephrine transporter of rat parietal-occipital cortex B 8.13 pKi 7.36 nM Ki Bioorg Med Chem Lett (2005) 15: 2461-2465 [PMID:15863297]
ChEMBL Inhibition of uptake of tritiated norepinephrine (NE) in rat synaptosomes B 9.19 pKi 0.65 nM Ki J Med Chem (1987) 30: 1433-1454 [PMID:3039136]
ChEMBL Inhibition of norepinephrine reuptake in rat whole brains minus cerebellar F 4.87 pIC50 13500 nM IC50 J Med Chem (1989) 32: 1805-1813 [PMID:2754707]
ChEMBL Inhibition of neuronal uptake of Noradrenaline in rat brain homogenate F 5.77 pIC50 1700 nM IC50 J Med Chem (1997) 40: 3516-3523 [PMID:9357518]
ChEMBL Inhibition of uptake of tritiated norepinephrine (NE) into rat brain synaptosomes F 6.82 pIC50 150 nM IC50 J Med Chem (1990) 33: 2899-2905 [PMID:1976813]
ChEMBL In vitro inhibition of accumulation of (-)-[3H]Norepinephrine (NA) in mouse brain slices F 7.15 pIC50 70 nM IC50 J Med Chem (1981) 24: 1499-1507 [PMID:6458703]
Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364]
ChEMBL Antimalarial activity after 72 hrs against chloroquine-resistant Plasmodium falciparum Dd2 infected human erythrocytes by SYBR green assay F 4.78 pIC50 16600 nM IC50 Antimicrob Agents Chemother (2007) 51: 4133-4140 [PMID:17846138]
ChEMBL Antimicrobial activity against Plasmodium falciparum F 4.92 pIC50 12000 nM IC50 Bioorg Med Chem (2010) 18: 2225-2231 [PMID:20185316]
ChEMBL Antimalarial activity after 72 hrs against chloroquine-sensitive Plasmodium falciparum D6 infected human erythrocytes by SYBR green assay F 4.94 pIC50 11400 nM IC50 Antimicrob Agents Chemother (2007) 51: 4133-4140 [PMID:17846138]
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]
SERT/Serotonin transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL228] [GtoPdb: 928] [UniProtKB: P31645]
GtoPdb Assay using HEK-293 cells transfected with hSERT - 6.79 pKi 163 nM Ki J Pharmacol Exp Ther (1997) 283: 1305-22 [PMID:9400006]
ChEMBL Inhibition of SERT B 7.7 pKi 20 nM Ki J Med Chem (2010) 53: 7869-7873 [PMID:20945906]
ChEMBL Inhibition of human SERT expressed in HEK293-MSR cells by 5-HT uptake assay B 6.25 pIC50 560 nM IC50 Bioorg Med Chem Lett (2013) 23: 1220-1224 [PMID:23385211]
ChEMBL Inhibition of [3H]serotonin uptake in human wild type SERT transfected HEK293 cells B 6.97 pIC50 108 nM IC50 Science (2007) 317: 1390-1393 [PMID:17690258]
ChEMBL Inhibition of [3H]5HT uptake at human SERT expressed in HEK293 cells B 7.19 pIC50 64 nM IC50 Antimicrob Agents Chemother (2007) 51: 4133-4140 [PMID:17846138]
ChEMBL Inhibition of [3H]serotonin uptake in human SERT K490T mutant transfected HEK293 cells B 7.28 pIC50 52.4 nM IC50 Science (2007) 317: 1390-1393 [PMID:17690258]
SERT/Serotonin transporter in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4642] [GtoPdb: 928] [UniProtKB: Q60857]
ChEMBL Inhibition of 5-HT transporter in NMRI albino mouse brain assessed as [3H]5-HT accumulation in hypothalamus after 5 mins B 5.03 pIC50 9300 nM IC50 J Med Chem (1978) 21: 78-82 [PMID:22757]
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 6.74 pKi 182 nM Ki J Med Chem (1987) 30: 1433-1454 [PMID:3039136]
ChEMBL Ability to inhibit reuptake of serotonin ([3H]5-HT) at serotonin transporter of rat midbrian B 6.79 pKi 163 nM Ki Bioorg Med Chem Lett (2003) 13: 3565-3569 [PMID:14505672]
ChEMBL Inhibitory constant against reuptake of [3H]5-HT at serotonin transporter of rat midbrain cortex B 6.79 pKi 163 nM Ki Bioorg Med Chem Lett (2005) 15: 2461-2465 [PMID:15863297]
GtoPdb - - 7.7 pKi 20 nM Ki J Med Chem (2010) 53: 7869-73 [PMID:20945906]
ChEMBL Inhibition of serotonin reuptake in rat whole brains without cerebellum