desipramine [Ligand Id: 2399] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL72 (Desipramine, Imipramine, demethyl-, Monodemethylimipramine, N-desmethylimipramine, Norimipramine) |
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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 | F | 4.7 | pIC50 | >20000 | nM | IC50 | J Med Chem (1989) 32: 1805-1813 [PMID:2754707] |
| ChEMBL | In vitro inhibition of accumulation of [14C]5-HT (5-HT) in mouse brain slices | F | 4.92 | pIC50 | 12000 | 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 | 5.52 | pIC50 | 3000 | nM | IC50 | J Med Chem (1990) 33: 2899-2905 [PMID:1976813] |
| Nav1.5/Sodium channel protein type V alpha subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1980] [GtoPdb: 582] [UniProtKB: Q14524] | ||||||||
| ChEMBL | Inhibition of sodium current measured using whole-cell patch clamp experiments in HEK-293 cells stably transfected with hNaV1.5 cDNA | F | 5.82 | pIC50 | 1520 | nM | IC50 | Cardiovasc Res (2011) 91: 53-61 [PMID:21300721] |
| Organic cation transporter 1/Solute carrier family 22 member 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5685] [GtoPdb: 1019] [UniProtKB: O15245] | ||||||||
| ChEMBL | TP_TRANSPORTER: inhibition of TEA uptake in OCT1-expressing HeLa cells | F | 5.27 | pKi | 5360 | nM | Ki | J Pharmacol Exp Ther (1998) 286: 354-361 [PMID:9655880] |
| ChEMBL | Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells by confocal microscopy | B | 4.25 | pIC50 | 56800 | 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 | 5.04 | pIC50 | 9180 | 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 in Xenopus laevis oocytes | F | 5.55 | pKi | 2800 | nM | Ki | Nature (1994) 372: 549-552 [PMID:7990927] |
| ChEMBL | TP_TRANSPORTER: inhibition of TEA uptake (TEA: 10 uM) in Xenopus laevis oocytes | F | 4.76 | pIC50 | 17500 | nM | IC50 | Am J Physiol Renal Physiol (2001) 281: F454-F468 [PMID:11502595] |
| Organic cation transporter 2/Solute carrier family 22 member 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1743122] [GtoPdb: 1020] [UniProtKB: O15244] | ||||||||
| ChEMBL | TP_TRANSPORTER: inhibition of TEA uptake in Xenopus laevis oocytes | F | 4.8 | pKi | 16000 | nM | Ki | DNA Cell Biol (1997) 16: 871-881 [PMID:9260930] |
| 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: 10 uM) in Xenopus laevis oocytes | F | 5 | pIC50 | 10000 | nM | IC50 | Am J Physiol Renal Physiol (2001) 281: F454-F468 [PMID:11502595] |
| 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 | 4.85 | pKi | 14000 | nM | Ki | Am J Physiol Renal Physiol (2000) 279: F449-F458 [PMID:10966924] |
| Organic cation transporter 3/Solute carrier family 22 member 3 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1770033] [GtoPdb: 1021] [UniProtKB: O88446] | ||||||||
| ChEMBL | TP_TRANSPORTER: inhibition of MPP+ uptake (MPP+: 1 uM) in OCT3-expressing HRPE cells | F | 4.17 | pIC50 | 68000 | nM | IC50 | J Biol Chem (1998) 273: 32776-32786 [PMID:9830022] |
| Organic cation/carnitine transporter 1/Solute carrier family 22 member 4 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2073667] [GtoPdb: 1022] [UniProtKB: Q9R141] | ||||||||
| ChEMBL | TP_TRANSPORTER: inhibition of TEA uptake in Octn1-HRPE cells | F | 4.1 | pIC50 | 80000 | nM | IC50 | Biochim Biophys Acta (2000) 1466: 315-327 [PMID:10825452] |
| Transporter in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6184] [UniProtKB: Q63380] | ||||||||
| ChEMBL | Displacement of [3H]nisoxetine from rat NET in rat cerebral cortex | B | 9.11 | pKi | 0.78 | nM | Ki | J Med Chem (2010) 53: 7869-7873 [PMID:20945906] |
| Voltage-dependent L-type calcium channel subunit alpha-1C in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2366456] [UniProtKB: O35505] | ||||||||
| ChEMBL | Inhibition of calcium current (ICaL) measured using whole-cell patch clamp experiments in isolated guinea pig ventricular myocytes | F | 5.77 | pIC50 | 1709 | nM | IC50 | Cardiovasc Res (2011) 91: 53-61 [PMID:21300721] |
| ChEMBL | Inhibition of L-type calcium channel measured using whole-cell patch clamp in guinea pig ventricular myocytes | F | 5.77 | pIC50 | 1709 | nM | IC50 | J Appl Toxicol (2012) 32: 858-866 [PMID:22761000] |
| 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 | 4.93 | pIC50 | 11700 | nM | IC50 | J Appl Toxicol (2012) 32: 858-866 [PMID:22761000] |
| Kir3.2 in Mouse [GtoPdb: 435] [UniProtKB: P48542] | ||||||||
| GtoPdb | - | - | 4.4 | pIC50 | - | - | - | Neuropsychopharmacology (2004) 29: 1841-51 [PMID:15150531] |
| Kir3.4 in Mouse [GtoPdb: 437] [UniProtKB: P48545] | ||||||||
| GtoPdb | - | - | 4.3 | pIC50 | - | - | - | Neuropsychopharmacology (2004) 29: 1841-51 [PMID:15150531] |
| Plasma membrane monoamine transporter in Human [GtoPdb: 1120] [UniProtKB: Q7RTT9] | ||||||||
| GtoPdb | - | - | 4.49 | pKi | 32600 | nM | Ki |
Mol Pharmacol (2005) 68: 1397-407 [PMID:16099839]; Clin Pharmacol Ther (2016) 100: 489-499 [PMID:27506881] |
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]
