clomipramine [Ligand Id: 2398] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL415 (3-chloro-iminodibenzyl, Anafranil, Anapramine, Chlorimipramine, Clomicalm, Clomipramine, NSC-169865)
  • α1A-adrenoceptor in Human [GtoPdb: 22] [UniProtKB: P35348]
  • 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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  • α2A-adrenoceptor/Alpha-2a adrenergic receptor in Human [ChEMBL: CHEMBL1867] [GtoPdb: 25] [UniProtKB: P08913]
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  • α2B-adrenoceptor/Alpha-2b adrenergic receptor in Human [ChEMBL: CHEMBL1942] [GtoPdb: 26] [UniProtKB: P18089]
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  • α2C-adrenoceptor/Alpha-2c adrenergic receptor in Human [ChEMBL: CHEMBL1916] [GtoPdb: 27] [UniProtKB: P18825]
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  • D1 receptor/Dopamine D1 receptor in Human [ChEMBL: CHEMBL2056] [GtoPdb: 214] [UniProtKB: P21728]
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  • D2 receptor/Dopamine D2 receptor in Human [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
  • D2 receptor/Dopamine D2 receptor in Rat [ChEMBL: CHEMBL339] [GtoPdb: 215] [UniProtKB: P61169]
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  • D3 receptor/Dopamine D3 receptor in Human [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462]
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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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  • H2 receptor/Histamine H2 receptor in Human [ChEMBL: CHEMBL1941] [GtoPdb: 263] [UniProtKB: P25021]
  • Histamine H2 receptor in Guinea pig [ChEMBL: CHEMBL2882] [UniProtKB: P47747]
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  • M1 receptor/Muscarinic acetylcholine receptor M1 in Human [ChEMBL: CHEMBL216] [GtoPdb: 13] [UniProtKB: P11229]
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  • M2 receptor/Muscarinic acetylcholine receptor M2 in Human [ChEMBL: CHEMBL211] [GtoPdb: 14] [UniProtKB: P08172]
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  • M3 receptor/Muscarinic acetylcholine receptor M3 in Human [ChEMBL: CHEMBL245] [GtoPdb: 15] [UniProtKB: P20309]
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  • M4 receptor/Muscarinic acetylcholine receptor M4 in Human [ChEMBL: CHEMBL1821] [GtoPdb: 16] [UniProtKB: P08173]
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  • M5 receptor/Muscarinic acetylcholine receptor M5 in Human [ChEMBL: CHEMBL2035] [GtoPdb: 17] [UniProtKB: P08912]
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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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  • 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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  • 5-HT6 receptor/Serotonin 6 (5-HT6) receptor in Human [ChEMBL: CHEMBL3371] [GtoPdb: 11] [UniProtKB: P50406]
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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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  • Trypanothione reductase in Trypanosoma cruzi [ChEMBL: CHEMBL5131] [UniProtKB: P28593]
  • Trypanothione reductase in Trypanosoma brucei brucei [ChEMBL: CHEMBL1837] [UniProtKB: P39051]
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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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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
α1A-adrenoceptor in Human [GtoPdb: 22] [UniProtKB: P35348]
GtoPdb - - 8.1 pKi - - - Pharmacol Res Perspect (2020) 8: e00602 [PMID:32608144]
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 7.4 pKi 40 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin) B 7 pIC50 99 nM IC50 DrugMatrix in vitro pharmacology data
ChEMBL Compound was tested for its inhibitory activity against Alpha-1 adrenergic receptor B 10.4 pIC50 0.04 nM IC50 J Med Chem (1999) 42: 3154-3162 [PMID:10447960]
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 7.14 pKi 73 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Alpha-1B adrenergic receptor radioligand binding (ligand: prazosin) B 6.88 pIC50 132 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 7.06 pKi 88 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Alpha-1D adrenergic receptor radioligand binding (ligand: prazosin) B 6.74 pIC50 180 nM IC50 DrugMatrix in vitro pharmacology data
α2A-adrenoceptor/Alpha-2a adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1867] [GtoPdb: 25] [UniProtKB: P08913]
ChEMBL DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912) B 6.28 pKi 530 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912) B 5.85 pIC50 1414 nM IC50 DrugMatrix in vitro pharmacology data
α2B-adrenoceptor/Alpha-2b adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1942] [GtoPdb: 26] [UniProtKB: P18089]
ChEMBL DRUGMATRIX: Alpha-2B adrenergic receptor radioligand binding (ligand: Rauwolscine) B 7.34 pKi 46 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Alpha-2B adrenergic receptor radioligand binding (ligand: Rauwolscine) B 7 pIC50 101 nM IC50 DrugMatrix in vitro pharmacology data
α2C-adrenoceptor/Alpha-2c adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1916] [GtoPdb: 27] [UniProtKB: P18825]
ChEMBL DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912) B 6.69 pKi 205 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912) B 5.85 pIC50 1413 nM IC50 DrugMatrix in vitro pharmacology data
CYP2D6/Cytochrome P450 2D6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL289] [GtoPdb: 1329] [UniProtKB: P10635]
ChEMBL DRUGMATRIX: CYP450, 2D6 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin) B 5.4 pIC50 3946.5 nM IC50 DrugMatrix in vitro pharmacology data
D1 receptor/Dopamine D1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2056] [GtoPdb: 214] [UniProtKB: P21728]
ChEMBL DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390) B 6.25 pKi 557 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390) B 5.95 pIC50 1113 nM IC50 DrugMatrix in vitro pharmacology data
D2 receptor/Dopamine D2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
ChEMBL DRUGMATRIX: Dopamine D2L radioligand binding (ligand: [3H] Spiperone) B 6.86 pKi 138 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Dopamine D2L radioligand binding (ligand: [3H] Spiperone) B 6.38 pIC50 413 nM IC50 DrugMatrix in vitro pharmacology data
D2 receptor/Dopamine D2 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL339] [GtoPdb: 215] [UniProtKB: P61169]
ChEMBL Binding affinity towards Dopamine receptor D2 B 7.25 pKi 56 nM Ki J Med Chem (1987) 30: 1433-1454 [PMID:3039136]
D3 receptor/Dopamine D3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462]
ChEMBL DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone) B 7.33 pKi 47 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone) B 6.86 pIC50 139 nM IC50 DrugMatrix in vitro pharmacology data
DAT/Dopamine transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL238] [GtoPdb: 927] [UniProtKB: Q01959]
GtoPdb - - 5.66 pKd 2190 nM Kd Eur J Pharmacol (1997) 340: 249-58 [PMID:9537821]
ChEMBL DRUGMATRIX: Dopamine Transporter radioligand binding (ligand: [125I] RTI-55) B 5.66 pKi 2182 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL Displacement of [3H]Win35428 from human recombinant DAT over-expressed in CHOK1 cells B 5.56 pIC50 2777 nM IC50 Bioorg Med Chem Lett (2013) 23: 5515-5518 [PMID:24012181]
ChEMBL DRUGMATRIX: Dopamine Transporter radioligand binding (ligand: [125I] RTI-55) B 5.56 pIC50 2746 nM IC50 DrugMatrix in vitro pharmacology data
DAT/Dopamine transporter in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL338] [GtoPdb: 927] [UniProtKB: P23977]
ChEMBL Inhibition of uptake of dopamine (DA) rat brain striatum F 6 pIC50 1000 nM IC50 J Med Chem (1980) 23: 1306-1310 [PMID:7452682]
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 8.01 pKi 9.83 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine) B 7.07 pIC50 85 nM IC50 DrugMatrix in vitro pharmacology data
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 9.7 pIC50 0.2 nM IC50 J Med Chem (1999) 42: 3154-3162 [PMID:10447960]
H2 receptor/Histamine H2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1941] [GtoPdb: 263] [UniProtKB: P25021]
ChEMBL DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine) B 5.7 pKi 2015 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine) B 5.69 pIC50 2049 nM IC50 DrugMatrix in vitro pharmacology data
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 6.14 pIC50 720 nM IC50 J Med Chem (1999) 42: 3154-3162 [PMID:10447960]
M1 receptor/Muscarinic acetylcholine receptor M1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL216] [GtoPdb: 13] [UniProtKB: P11229]
ChEMBL DRUGMATRIX: Muscarinic M1 radioligand binding (ligand: [3H] N-Methylscopolamine) B 7.66 pKi 22 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Muscarinic M1 radioligand binding (ligand: [3H] N-Methylscopolamine) B 7.04 pIC50 91 nM IC50 DrugMatrix in vitro pharmacology data
M2 receptor/Muscarinic acetylcholine receptor M2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL211] [GtoPdb: 14] [UniProtKB: P08172]
ChEMBL DRUGMATRIX: Muscarinic M2 radioligand binding (ligand: [3H] N-Methylscopolamine) B 7.07 pKi 86 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Muscarinic M2 radioligand binding (ligand: [3H] N-Methylscopolamine) B 6.62 pIC50 241 nM IC50 DrugMatrix in vitro pharmacology data
M3 receptor/Muscarinic acetylcholine receptor M3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL245] [GtoPdb: 15] [UniProtKB: P20309]
ChEMBL DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine) B 7.44 pKi 36 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine) B 6.77 pIC50 170 nM IC50 DrugMatrix in vitro pharmacology data
M4 receptor/Muscarinic acetylcholine receptor M4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1821] [GtoPdb: 16] [UniProtKB: P08173]
ChEMBL DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine) B 7.89 pKi 13 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine) B 7.04 pIC50 91 nM IC50 DrugMatrix in vitro pharmacology data
M5 receptor/Muscarinic acetylcholine receptor M5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2035] [GtoPdb: 17] [UniProtKB: P08912]
ChEMBL DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine) B 7.42 pKi 38 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine) B 7.28 pIC50 53 nM IC50 DrugMatrix in vitro pharmacology data
NET/Norepinephrine transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL222] [GtoPdb: 926] [UniProtKB: P23975]
GtoPdb - - 7.42 pKd 38 nM Kd Eur J Pharmacol (1997) 340: 249-58 [PMID:9537821]
ChEMBL DRUGMATRIX: Norepinephrine Transporter radioligand binding (ligand: [125I] RTI-55) B 7.15 pKi 70 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Norepinephrine Transporter radioligand binding (ligand: [125I] RTI-55) B 7.15 pIC50 71 nM IC50 DrugMatrix in vitro pharmacology data
ChEMBL Displacement of [3H]Nisoxetine from human recombinant NET over-expressed in dog MDCK cells B 7.19 pIC50 64.6 nM IC50 Bioorg Med Chem Lett (2013) 23: 5515-5518 [PMID:24012181]
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 6.05 pIC50 900 nM IC50 J Med Chem (1978) 21: 78-82 [PMID:22757]
Norepinephrine transporter in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL304] [UniProtKB: Q9WTR4]
ChEMBL In vitro inhibition of accumulation of (-)-[3H]Norepinephrine (NA) in mouse brain slices F 6.05 pIC50 900 nM IC50 J Med Chem (1981) 24: 1499-1507 [PMID:6458703]
ChEMBL Inhibition of uptake of noradrenaline in rat brain hypothalamus F 6.15 pIC50 700 nM IC50 J Med Chem (1980) 23: 1306-1310 [PMID:7452682]
Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364]
ChEMBL DNDI: Malaria in Vitro, 72 hour F 5.89 pIC50 1300 nM IC50 Antiprotozoal Activity Profiling of Approved Drugs: A Starting Point toward Drug Repositioning
5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223]
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2A radioligand binding (ligand: [3H] Ketanserin) B 7.72 pKi 19 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2A radioligand binding (ligand: [3H] Ketanserin) B 7.17 pIC50 67 nM IC50 DrugMatrix in vitro pharmacology data
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 6.82 pKi 152 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide) B 6.62 pIC50 239 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 7.74 pKi 18 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2C radioligand binding (ligand: [3H] Mesulergine) B 7.47 pIC50 34 nM IC50 DrugMatrix in vitro pharmacology data
5-HT6 receptor/Serotonin 6 (5-HT6) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3371] [GtoPdb: 11] [UniProtKB: P50406]
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide) B 6.94 pKi 114 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation counting B 6.95 pKi 112 nM Ki J Med Chem (2012) 55: 5704-5719 [PMID:22537153]
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide) B 6.61 pIC50 245 nM IC50 DrugMatrix in vitro pharmacology data
SERT/Serotonin transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL228] [GtoPdb: 928] [UniProtKB: P31645]
GtoPdb - - 9.55 pKd 0.28 nM Kd Eur J Pharmacol (1997) 340: 249-58 [PMID:9537821]
ChEMBL Displacement of [3H]-imipramine from human serotonin transporter expressed in HEK293 cells after 30 mins by liquid scintillation counting analysis B 9.55 pKi 0.28 nM Ki Bioorg Med Chem (2015) 23: 6528-6534 [PMID:26372073]
GtoPdb - - 9.68 pKi 0.21 nM Ki Eur J Pharmacol (1997) 340: 249-58 [PMID:9537821]
ChEMBL DRUGMATRIX: Transporter, Serotonin (5-Hydroxytryptamine) (SERT) radioligand binding (ligand: [3H] Paroxetine) B 10.33 pKi 0.05 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL In vivo inhibition of uptake of 5-HT in human platelets F 7.15 pIC50 70 nM IC50 J Med Chem (1980) 23: 1306-1310 [PMID:7452682]
ChEMBL DRUGMATRIX: Transporter, Serotonin (5-Hydroxytryptamine) (SERT) radioligand binding (ligand: [3H] Paroxetine) B 10.06 pIC50 0.09 nM IC50 DrugMatrix in vitro pharmacology data
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 7.15 pIC50 70 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 In vitro inhibition of accumulation of [14C]5-HT (5-HT) in mouse brain slices F 7.05 pIC50 90 nM IC50 J Med Chem (1981) 24: 1499-1507 [PMID:6458703]
ChEMBL Inhibition of uptake of 5-HT in rat brain cortex F 7.7 pIC50 20 nM IC50 J Med Chem (1980) 23: 1306-1310 [PMID:7452682]
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 6.24 pKi 572 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Sigma1 radioligand binding (ligand: [3H] Haloperidol) B 5.87 pIC50 1362 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 4.71 pIC50 19300 nM IC50 J Med Chem (2008) 51: 5932-5942 [PMID:18788725]
Trypanothione reductase in Trypanosoma cruzi (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5131] [UniProtKB: P28593]
ChEMBL Inhibition of Trypanosoma cruzi recombinant trypanothione reductase B 5.15 pKi 7000 nM Ki Bioorg Med Chem (2008) 16: 6689-6695 [PMID:18558492]
ChEMBL Compound was evaluated for the competitive inhibition of trypanothione reduction by recombinant Trypanothione reductase from Trypanosoma cruzi B 5.19 pKi 6500 nM Ki Bioorg Med Chem Lett (1995) 5: 1957-1960
ChEMBL Inhibition of Trypanosoma cruzi trypanothione reductase expressed in Escherichia coli JM109 cells B 5.19 pKi 6500 nM Ki Bioorg Med Chem Lett (2009) 19: 3031-3035 [PMID:19414258]
ChEMBL Inhibition of Trypanosoma cruzi trypanothione reductase assessed as reduction of trypanothione disulfide by spectrophotometrically B 5.19 pKi 6500 nM Ki Bioorg Med Chem (2015) 23: 996-1010 [PMID:25661449]
ChEMBL Inhibition of Trypanosoma cruzi trypanothione reductase assessed as reduction in NADPH consumption using varying levels of trypanothione disulfide as substrate by Lineweaver-Burk plot analysis B 5.19 pKi 6500 nM Ki Eur J Med Chem (2017) 141: 138-148 [PMID:29031061]
ChEMBL Inhibition of Trypanosoma cruzi trypanothione reductase expressed in Escherichia coli BL21 (DE3) pre-incubated for 30 mins using TS2 substrate in presence of NADPH by colorimetric microplate assay B 4.82 pIC50 15200 nM IC50 Eur J Med Chem (2017) 140: 187-199 [PMID:28926763]
ChEMBL Inhibition of Trypanosoma cruzi trypanothione reductase expressed in Escherichia coli BL21(DE3) assessed as reduction of oxidized trypanothione preincubated for 30 mins measured for 30 mins by spectrophotometric analysis B 4.91 pIC50 12300 nM IC50 Eur J Med Chem (2014) 71: 282-289 [PMID:24321832]
Trypanothione reductase in Trypanosoma brucei brucei (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1837] [UniProtKB: P39051]
ChEMBL Inhibition of recombinant Trypanosoma brucei brucei strain S427 trypanothione reductase assessed as reduction of trypanothione disulphide by 412 nm assay B 5.47 pIC50 3400 nM IC50 Bioorg Med Chem (2015) 23: 996-1010 [PMID:25661449]
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 4.94 pIC50 11600 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 - - 3.6 pIC50 - - - Neuropsychopharmacology (2004) 29: 1841-51 [PMID:15150531]

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]