cisapride [Ligand Id: 240] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1729 (Alimix, Cisaprida, Cisapride, Cisapride monohydrate, Prepulsid, Prepulsid quicklet, Propulsid, Propulsid quicksolv, R-51,619, R-51619)
  • Alpha-1a adrenergic receptor in Bovine [ChEMBL: CHEMBL4892] [UniProtKB: P18130]
  • 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]
  • α2A-adrenoceptor/Alpha-2a adrenergic receptor in Rat [ChEMBL: CHEMBL327] [GtoPdb: 25] [UniProtKB: P22909]
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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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  • β1-adrenoceptor/Beta-1 adrenergic receptor in Human [ChEMBL: CHEMBL213] [GtoPdb: 28] [UniProtKB: P08588]
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  • β2-adrenoceptor/Beta-2 adrenergic receptor in Human [ChEMBL: CHEMBL210] [GtoPdb: 29] [UniProtKB: P07550]
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  • D2 receptor/Dopamine D2 receptor in Human [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
  • Dopamine D2 receptor in Bovine [ChEMBL: CHEMBL3998] [UniProtKB: P20288]
  • 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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  • hydroxymethylglutaryl-CoA reductase/HMG-CoA reductase in Human [ChEMBL: CHEMBL402] [GtoPdb: 639] [UniProtKB: P04035]
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  • 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908]
  • 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Rat [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327]
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  • 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223]
  • Serotonin 2a (5-HT2a) receptor in Bovine [ChEMBL: CHEMBL3446] [UniProtKB: Q75Z89]
  • 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Rat [ChEMBL: CHEMBL322] [GtoPdb: 6] [UniProtKB: P14842]
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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-HT3A/Serotonin 3a (5-HT3a) receptor in Human [ChEMBL: CHEMBL1899] [GtoPdb: 373] [UniProtKB: P46098]
  • 5-HT3A/Serotonin 3a (5-HT3a) receptor in Rat [ChEMBL: CHEMBL2411] [GtoPdb: 373] [UniProtKB: P35563]
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  • 5-HT4 receptor/Serotonin 4 (5-HT4) receptor in Human [ChEMBL: CHEMBL1875] [GtoPdb: 9] [UniProtKB: Q13639]
  • 5-HT4 receptor in Mouse [GtoPdb: 9] [UniProtKB: P97288]
  • 5-HT4 receptor/Serotonin 4 (5-HT4) receptor in Rat [ChEMBL: CHEMBL4317] [GtoPdb: 9] [UniProtKB: Q62758]
  • Serotonin 4 (5-HT4) receptor in Guinea pig [ChEMBL: CHEMBL5017] [UniProtKB: O70528]
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  • 5-HT7 receptor/Serotonin 7 (5-HT7) receptor in Human [ChEMBL: CHEMBL3155] [GtoPdb: 12] [UniProtKB: P34969]
  • 5-HT7 receptor in Mouse [GtoPdb: 12] [UniProtKB: P32304]
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  • SERT/Serotonin transporter in Human [ChEMBL: CHEMBL228] [GtoPdb: 928] [UniProtKB: P31645]
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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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  • Nav1.5/Sodium channel protein type V alpha subunit in Human [ChEMBL: CHEMBL1980] [GtoPdb: 582] [UniProtKB: Q14524]
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  • Voltage-dependent L-type calcium channel subunit alpha-1C in Guinea pig [ChEMBL: CHEMBL2366456] [UniProtKB: O35505]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Alpha-1a adrenergic receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4892] [UniProtKB: P18130]
ChEMBL Binding affinity was evaluated by Alpha-1 adrenergic receptor in calf cortex by displacing prazosin B 7.5 pKd 7.5 - pKD J Med Chem (1995) 38: 2326-2330 [PMID:7608898]
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 7.31 pKi 49 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL The ability to inhibit [3H]prazosin binding to Alpha-1 adrenergic receptor in rat whole brain B 7.52 pKi 30 nM Ki J Med Chem (1992) 35: 1486-1489 [PMID:1573641]
ChEMBL DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin) B 6.92 pIC50 120 nM IC50 DrugMatrix in vitro pharmacology data
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 8.06 pKi 8.65 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Alpha-1B adrenergic receptor radioligand binding (ligand: prazosin) B 7.8 pIC50 16 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 7.03 pKi 93 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Alpha-1D adrenergic receptor radioligand binding (ligand: prazosin) B 6.72 pIC50 189 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 6.18 pKi 666 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912) B 5.75 pIC50 1777 nM IC50 DrugMatrix in vitro pharmacology data
α2A-adrenoceptor/Alpha-2a adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL327] [GtoPdb: 25] [UniProtKB: P22909]
ChEMBL Compound was evaluated for the binding affinity at Alpha adrenergic receptor B 7.52 pKi 30 nM Ki J Med Chem (1995) 38: 2326-2330 [PMID:7608898]
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 6.28 pKi 524 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Alpha-2B adrenergic receptor radioligand binding (ligand: Rauwolscine) B 5.94 pIC50 1148 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 6.95 pKi 113 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912) B 6.11 pIC50 780 nM IC50 DrugMatrix in vitro pharmacology data
β1-adrenoceptor/Beta-1 adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL213] [GtoPdb: 28] [UniProtKB: P08588]
ChEMBL Binding affinity to adrenergic beta-1 receptor B 5 pIC50 >10000 nM IC50 J Med Chem (2006) 49: 1125-1139 [PMID:16451077]
β2-adrenoceptor/Beta-2 adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL210] [GtoPdb: 29] [UniProtKB: P07550]
ChEMBL Binding affinity to adrenergic beta-2 receptor B 5 pIC50 >10000 nM IC50 J Med Chem (2006) 49: 1125-1139 [PMID:16451077]
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 7.15 pIC50 70 nM IC50 DrugMatrix in vitro pharmacology data
CYP3A4/Cytochrome P450 3A4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL340] [GtoPdb: 1337] [UniProtKB: P08684]
ChEMBL DRUGMATRIX: CYP450, 3A4 enzyme inhibition (substrate: 7-Benzyloxy-4-(trifluoromethyl)-coumarin) B 6.52 pIC50 300 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 Binding affinity to dopamine receptor D1 B 5.77 pIC50 1700 nM IC50 J Med Chem (2006) 49: 1125-1139 [PMID:16451077]
Dopamine D1 receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2967] [UniProtKB: Q95136]
ChEMBL Binding affinity was evaluated by Dopamine receptor D1 agonism in the calf striatum by displacing SCH 23390 B 5.2 pKd 5.2 - pKD J Med Chem (1995) 38: 2326-2330 [PMID:7608898]
D1 receptor/Dopamine D1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL265] [GtoPdb: 214] [UniProtKB: P18901]
ChEMBL The ability to inhibit [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striata B 5.77 pKi 1700 nM Ki J Med Chem (1992) 35: 1486-1489 [PMID:1573641]
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 6.8 pKi 158 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Dopamine D2L radioligand binding (ligand: [3H] Spiperone) B 6.33 pIC50 473 nM IC50 DrugMatrix in vitro pharmacology data
ChEMBL Binding affinity to dopamine receptor D2 B 6.64 pIC50 227 nM IC50 J Med Chem (2006) 49: 1125-1139 [PMID:16451077]
Dopamine D2 receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3998] [UniProtKB: P20288]
ChEMBL Binding affinity was evaluated by Dopamine receptor D2 agonism in the calf striatum by displacing spiperone B 6.5 pKd 6.5 - pKD J Med Chem (1995) 38: 2326-2330 [PMID:7608898]
D2 receptor/Dopamine D2 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL339] [GtoPdb: 215] [UniProtKB: P61169]
ChEMBL Affinity towards Dopamine receptor D2 in rat striatum using [3H]spiperone as radioligand B 6.64 pKi 227 nM Ki J Med Chem (2003) 46: 702-715 [PMID:12593651]
ChEMBL The ability to inhibit [3H]domperidone binding to dopamine receptor D2 in rat striata B 6.64 pKi 227 nM Ki J Med Chem (1992) 35: 1486-1489 [PMID:1573641]
ChEMBL Displacement of [3H]spiroperidol from D2 dopamine receptor B 6.17 pIC50 680 nM IC50 J Med Chem (1994) 37: 1320-1325 [PMID:8176710]
ChEMBL Inhibitory activity against dopamine receptor D2 by 3H ligand binding experiments. B 6.41 pIC50 390 nM IC50 J Med Chem (1991) 34: 616-624 [PMID:1995885]
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 7.31 pKi 49 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone) B 6.84 pIC50 144 nM IC50 DrugMatrix in vitro pharmacology data
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 6.86 pKi 139.4 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL Inhibition of human ERG Y652A mutant expressed in HEK293 cells by whole cell patch clamp method B 5.57 pIC50 2690 nM IC50 J Med Chem (2009) 52: 1630-1638 [PMID:19260734]
ChEMBL Inhibition of human ERG F656A mutant expressed in HEK293 cells by whole cell patch clamp method B 5.77 pIC50 1710 nM IC50 J Med Chem (2009) 52: 1630-1638 [PMID:19260734]
ChEMBL DRUGMATRIX: Potassium Channel HERG radioligand binding (ligand: [3H] Astemizole) B 6.77 pIC50 170.1 nM IC50 DrugMatrix in vitro pharmacology data
ChEMBL Inhibition of human ERG expressed in CHO cells by Qpatch assay B 6.82 pIC50 150 nM IC50 Eur J Med Chem (2017) 127: 72-86 [PMID:28038328]
ChEMBL Inhibition of human ERG S624A mutant expressed in HEK293 cells by whole cell patch clamp method B 6.92 pIC50 120 nM IC50 J Med Chem (2009) 52: 1630-1638 [PMID:19260734]
ChEMBL Inhibition of human ERG overexpressed in CHO cells by Qpatch method B 7.01 pIC50 98 nM IC50 Bioorg Med Chem (2015) 23: 5881-5890 [PMID:26211462]
ChEMBL Inhibition of human ERG expressed in CHO cells by whole-cell patch clamp assay B 7.1 pIC50 80 nM IC50 J Med Chem (2014) 57: 3687-3706 [PMID:24564525]
ChEMBL Inhibitory activity against Potassium channel HERG B 7.33 pIC50 47 nM IC50 J Med Chem (2003) 46: 2017-2022 [PMID:12747773]
ChEMBL Inhibition of K+ channel activity in CHO cells expressing HERG Kv11.1 B 7.35 pIC50 45 nM IC50 Bioorg Med Chem Lett (2003) 13: 1829-1835 [PMID:12729675]
ChEMBL Inhibition of human ERG expressed in CHO cells assessed as whole cell current by patch clamp assay B 7.4 pIC50 40 nM IC50 J Med Chem (2015) 58: 4506-4520 [PMID:25992974]
GtoPdb - - 7.4 pIC50 44.5 nM IC50 FEBS Lett (1997) 417: 28-32 [PMID:9395068]
ChEMBL Inhibition of human ERG expressed in CHO cells by whole cell patch clamp technique B 7.4 pIC50 39.81 nM IC50 Bioorg Med Chem (2008) 16: 6252-6260 [PMID:18448342]
ChEMBL Inhibition of human Potassium channel HERG expressed in mammalian cells B 7.4 pIC50 39.81 nM IC50 Bioorg Med Chem Lett (2003) 13: 2773-2775 [PMID:12873512]
ChEMBL Inhibitory concentration against potassium channel HERG B 7.4 pIC50 39.81 nM IC50 Bioorg Med Chem Lett (2005) 15: 2886-2890 [PMID:15911273]
ChEMBL Inhibition of human ERG expressed in CHOK1 cells by patch clamp assay B 7.92 pIC50 12 nM IC50 Bioorg Med Chem Lett (2018) 28: 2477-2480 [PMID:29871847]
ChEMBL Inhibition of wild-type human ERG expressed in HEK293 cells by whole cell patch clamp method B 8 pIC50 10 nM IC50 J Med Chem (2009) 52: 1630-1638 [PMID:19260734]
ChEMBL Inhibition of human ERG B 8.17 pIC50 6.76 nM IC50 Eur J Med Chem (2011) 46: 618-630 [PMID:21185626]
ChEMBL Inhibition of human ERG channel B 8.17 pIC50 6.7 nM IC50 J Med Chem (2009) 52: 4266-4276 [PMID:19534531]
ChEMBL Inhibition of human ERG channel B 8.17 pIC50 6.7 nM IC50 J Med Chem (2009) 52: 4266-4276 [PMID:19534531]
ChEMBL K+ channel blocking activity in human embryonic kidney cells expressing HERG Kv11.1 F 8.19 pIC50 6.5 nM IC50 J Med Chem (2002) 45: 3844-3853 [PMID:12190308]
ChEMBL Inhibition of hERG K channel F 8.19 pIC50 6.5 nM IC50 Cardiovasc Res (2011) 91: 53-61 [PMID:21300721]
ChEMBL Inhibition of human ERG in MCF7 cells B 8.19 pIC50 6.46 nM IC50 Eur J Med Chem (2009) 44: 1926-1932 [PMID:19110341]
ChEMBL Inhibition of partially open human voltage-gated potassium channel subunit Kv11.1 (ERG K+ channel) F 8.19 pIC50 6.46 nM IC50 Bioorg Med Chem Lett (2005) 15: 1737-1741 [PMID:15745831]
hydroxymethylglutaryl-CoA reductase/HMG-CoA reductase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL402] [GtoPdb: 639] [UniProtKB: P04035]
ChEMBL DRUGMATRIX: HMG-CoA Reductase enzyme inhibition (substrate: [14C]HMG-CoA) B 5.47 pIC50 3370 nM IC50 DrugMatrix in vitro pharmacology data
5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908]
ChEMBL Binding affinity was evaluated by 5-hydroxytryptamine 1A receptor agonism in the pig cortex by displacing 8-OH-DPAT B 5.7 pKd 5.7 - pKD J Med Chem (1995) 38: 2326-2330 [PMID:7608898]
ChEMBL Binding affinity to human serotonin 5-HT1A receptor B 6.1 pKi 794.33 nM Ki Bioorg Med Chem Lett (2013) 23: 4210-4215 [PMID:23756062]
5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327]
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1A radioligand binding (ligand: [3H] 8-OH-DPAT) B 5.79 pKi 1617 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1A radioligand binding (ligand: [3H] 8-OH-DPAT) B 5.55 pIC50 2829 nM IC50 DrugMatrix in vitro pharmacology data
5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223]
ChEMBL Binding affinity to human serotonin 5-HT2A receptor B 8.2 pKi 6.31 nM Ki Bioorg Med Chem Lett (2013) 23: 4210-4215 [PMID:23756062]
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2A radioligand binding (ligand: [3H] Ketanserin) B 8.96 pKi 1.1 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2A radioligand binding (ligand: [3H] Ketanserin) B 8.41 pIC50 3.86 nM IC50 DrugMatrix in vitro pharmacology data
Serotonin 2a (5-HT2a) receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3446] [UniProtKB: Q75Z89]
ChEMBL Compound was evaluated for the binding affinity at 5- HT2 receptor B 8.14 pKi 7.2 nM Ki J Med Chem (1995) 38: 2326-2330 [PMID:7608898]
5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL322] [GtoPdb: 6] [UniProtKB: P14842]
ChEMBL Binding affinity was evaluated by 5-hydroxytryptamine 2A receptor agonism in the rat cortex by displacing ketanserin B 8.1 pKd 8.1 - pKD J Med Chem (1995) 38: 2326-2330 [PMID:7608898]
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 7.15 pKi 70 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL Binding affinity to human serotonin 5-HT2B receptor B 7.4 pKi 39.81 nM Ki Bioorg Med Chem Lett (2013) 23: 4210-4215 [PMID:23756062]
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide) B 6.96 pIC50 110 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 6.4 pKi 402 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2C radioligand binding (ligand: [3H] Mesulergine) B 6.12 pIC50 767 nM IC50 DrugMatrix in vitro pharmacology data
5-HT3E/5-HT3B/5-HT3A/5-HT3D/5-HT3C/Serotonin 3 (5-HT3) receptor in Human (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL2094132] [GtoPdb: 377, 374, 373, 376, 375] [UniProtKB: A5X5Y0, O95264, P46098, Q70Z44, Q8WXA8]
ChEMBL Antagonistic activity against Serotonin 5-hydroxytryptamine 3 receptor in isolated rabbit vagus nerve (RVN) F 6.5 pKd 316.23 nM Kd Bioorg Med Chem Lett (1992) 2: 461-466
ChEMBL Evaluated for the antagonistic activity against Serotonin 5-hydroxytryptamine 3 receptor in isolated perfused rabbit heart (RH) F 7.1 pKd 79.43 nM Kd Bioorg Med Chem Lett (1992) 2: 461-466
ChEMBL Antagonistic activity against Serotonin 5-hydroxytryptamine 3 receptor of isolated guinea pig ileum (GPI) F 7.2 pKd 63.1 nM Kd Bioorg Med Chem Lett (1992) 2: 461-466
ChEMBL Compound was tested for 5-hydroxytryptamine 3 receptor binding affinity B 6.82 pKi 152 nM Ki J Med Chem (2003) 46: 319-344 [PMID:12540230]
5-HT3A/5-HT3B/Serotonin 3 (5-HT3) receptor in Rat (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2094116] [GtoPdb: 373, 374] [UniProtKB: P35563, Q9JJ16]
ChEMBL Inhibition of [3H]GR-65630 binding to 5-hydroxytryptamine 3 receptor B 6.87 pKi 134 nM Ki J Med Chem (1992) 35: 1486-1489 [PMID:1573641]
ChEMBL Displacement of [3H]GR65630 from 5HT3 receptor in brain cortex from Wistar rat B 6.87 pKi 134 nM Ki J Med Chem (2006) 49: 1125-1139 [PMID:16451077]
ChEMBL Inhibition of [3H]GR-65630 binding to rat cortical membrane serotonin 5-hydroxytryptamine 3 receptor B 7.02 pKi 94.7 nM Ki J Med Chem (2003) 46: 702-715 [PMID:12593651]
ChEMBL Inhibition of [3H]BRL-43694 binding to rat 5-hydroxytryptamine 3 receptor B 6.05 pIC50 900 nM IC50 J Med Chem (1994) 37: 1320-1325 [PMID:8176710]
5-HT3A/Serotonin 3a (5-HT3a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1899] [GtoPdb: 373] [UniProtKB: P46098]
ChEMBL Binding affinity to serotonin 5-HT3 receptor (unknown origin) B 5.7 pKi 1995.26 nM Ki Bioorg Med Chem Lett (2013) 23: 4210-4215 [PMID:23756062]
ChEMBL Binding affinity to human recombinant 5HT3 receptor B 5.7 pKi 1995.26 nM Ki Bioorg Med Chem Lett (2013) 23: 4210-4215 [PMID:23756062]
5-HT3A/Serotonin 3a (5-HT3a) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2411] [GtoPdb: 373] [UniProtKB: P35563]
ChEMBL Compound was evaluated in vivo for the antagonistic activity towards 5-hydroxytryptamine 3 receptor F 5.82 pKi 1500 nM Ki Bioorg Med Chem Lett (1992) 2: 1613-1618
5-HT4 receptor/Serotonin 4 (5-HT4) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1875] [GtoPdb: 9] [UniProtKB: Q13639]
ChEMBL Binding affinity to serotonin 5-HT4 receptor (unknown origin) B 6.9 pKi 125.89 nM Ki Bioorg Med Chem Lett (2013) 23: 4210-4215 [PMID:23756062]
ChEMBL Binding affinity to human recombinant 5HT4 receptor B 7 pKi 100 nM Ki Bioorg Med Chem Lett (2013) 23: 4210-4215 [PMID:23756062]
GtoPdb - - 7.4 pKi - - - J Neurochem (1997) 69: 1810-9 [PMID:9349523];
EMBO J (1995) 14: 2806-15 [PMID:7796807];
J Neurochem (2000) 74: 478-89 [PMID:10646498];
Naunyn Schmiedebergs Arch Pharmacol (2001) 363: 146-60 [PMID:11218067];
Br J Pharmacol (2000) 129: 771-81 [PMID:10683202];
Br J Pharmacol (2000) 131: 827-35 [PMID:11030734]
ChEMBL Binding affinity towards Serotonin 5-hydroxytryptamine 4 receptor B 7.54 pKi 29 nM Ki J Med Chem (2003) 46: 2017-2022 [PMID:12747773]
ChEMBL Binding Assay: The binding affinity of the compounds for a human 5-HT4 receptor was assayed according to the method as disclosed in the literature [Wyngaert et al., Journal of Neurochemistry, (1997) 69, 1810-1819]. For this purpose, COS-7 cells expressing the human 5-HT4 receptor were constructed and homogenized to obtain membrane homogenates which were then used in binding assay experiments. For the binding assay, the membrane homogenates were respectively mixed and incubated with different concentrations of test materials and [H3]-GR113808 (Amersham Biosciences). The concentrations of the individual test materials were set to 4 uM, 1 uM, 0.25 uM, and 0.0625 uM, respectively, and the concentration of [H3]-GR113808 was set to 0.595 nM. After the incubation was completed, the reaction products were collected in GF/B glass fiber filters using a Packard cell harvester, and the bound radioactivity was then determined using a liquid cell scintillation counter (Packard TopCount NXT). B 9.44 pIC50 0.36 nM IC50 US-9221790-B2. Benzamide derivatives (2015)
ChEMBL Agonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulation F 7.1 pEC50 79.43 nM EC50 Bioorg Med Chem Lett (2013) 23: 4210-4215 [PMID:23756062]
5-HT4 receptor in Mouse [GtoPdb: 9] [UniProtKB: P97288]
GtoPdb - - 7.5 pKi - - - FEBS Lett (1996) 398: 19-25 [PMID:8946946]
5-HT4 receptor/Serotonin 4 (5-HT4) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4317] [GtoPdb: 9] [UniProtKB: Q62758]
GtoPdb - - 8 pKi - - - Eur J Pharmacol (1996) 304: 231-5 [PMID:8813606];
Neuropharmacology (1997) 36: 671-9 [PMID:9225293]
ChEMBL Compound was evaluated for the agonistic activity towards 5-hydroxytryptamine 4 receptor using the rat tunica muscularis mucosae (TMM) esophagus strip assay F 7.26 pEC50 55 nM EC50 Bioorg Med Chem Lett (1992) 2: 1613-1618
ChEMBL Agonism at 5HT4 receptor in rat tunica muscularis mucosa F 7.26 pEC50 54.7 nM EC50 J Med Chem (2006) 49: 1125-1139 [PMID:16451077]
Serotonin 4 (5-HT4) receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5017] [UniProtKB: O70528]
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808) B 7.35 pKi 45 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL Displacement of [3H]GR113808 from Dunkin-Hartley guinea pig brain striatum 5HT4R after 30 mins B 7.7 pKi 20 nM Ki Eur J Med Chem (2014) 82: 36-46 [PMID:24871995]
ChEMBL Displacement of [3H]-GR113808 from 5-HT4R in Dunkin-Hartley guinea pig straitum nuclear membranes after 2 hrs by filter binding method B 7.7 pKi 20 nM Ki Medchemcomm (2018) 9: 1466-1471 [PMID:30288221]
ChEMBL Displacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum B 7.77 pKi 17 nM Ki J Med Chem (2006) 49: 1125-1139 [PMID:16451077]
ChEMBL Inhibition of [3H]GR-113808 binding to guinea pig striatum 5-hydroxytryptamine 4 receptor B 7.84 pKi 14.3 nM Ki J Med Chem (2003) 46: 702-715 [PMID:12593651]
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808) B 6.56 pIC50 273 nM IC50 DrugMatrix in vitro pharmacology data
ChEMBL Induction of 5-HT4 receptor-mediated contraction in guinea pig longitudinal muscle myenteric plexus B 7 pEC50 100 nM EC50 Bioorg Med Chem Lett (2013) 23: 4210-4215 [PMID:23756062]
5-HT7 receptor/Serotonin 7 (5-HT7) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3155] [GtoPdb: 12] [UniProtKB: P34969]
ChEMBL Binding affinity to human serotonin 5-HT7 receptor B 6 pKi 1000 nM Ki Bioorg Med Chem Lett (2013) 23: 4210-4215 [PMID:23756062]
5-HT7 receptor in Mouse [GtoPdb: 12] [UniProtKB: P32304]
GtoPdb - - 5.8 pKi - - - Mol Pharmacol (1993) 44: 229-36 [PMID:8394987]
SERT/Serotonin transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL228] [GtoPdb: 928] [UniProtKB: P31645]
ChEMBL DRUGMATRIX: Transporter, Serotonin (5-Hydroxytryptamine) (SERT) radioligand binding (ligand: [3H] Paroxetine) B 6.69 pKi 204 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Transporter, Serotonin (5-Hydroxytryptamine) (SERT) radioligand binding (ligand: [3H] Paroxetine) B 6.42 pIC50 384 nM IC50 DrugMatrix in vitro pharmacology data
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 6.38 pKi 418 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Sigma1 radioligand binding (ligand: [3H] Haloperidol) B 6 pIC50 994 nM IC50 DrugMatrix in vitro pharmacology data
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 4.83 pIC50 14700 nM IC50 Cardiovasc Res (2011) 91: 53-61 [PMID:21300721]
Voltage-dependent L-type calcium channel subunit alpha-1C in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2366456] [UniProtKB: O35505]
ChEMBL Inhibition of L-type calcium channel measured using whole-cell patch clamp in guinea pig ventricular myocytes F 4.33 pIC50 46900 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 guinea pig ventricular myocytes F 4.8 pIC50 16000 nM IC50 J Appl Toxicol (2012) 32: 858-866 [PMID:22761000]

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]