lisuride [Ligand Id: 43] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL157138 (Lisurida, Lisuride, Lisuride maleate, Lysuride, Lysuride maleate, Revanil 200)
  • 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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  • 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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  • 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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  • D4 receptor/Dopamine D4 receptor in Human [ChEMBL: CHEMBL219] [GtoPdb: 217] [UniProtKB: P21917]
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  • H1 receptor/Histamine H1 receptor in Human [ChEMBL: CHEMBL231] [GtoPdb: 262] [UniProtKB: P35367]
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  • H2 receptor/Histamine H2 receptor in Human [ChEMBL: CHEMBL1941] [GtoPdb: 263] [UniProtKB: P25021]
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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-HT1B receptor in Human [GtoPdb: 2] [UniProtKB: P28222]
  • 5-HT1B receptor/Serotonin 1b (5-HT1b) receptor in Rat [ChEMBL: CHEMBL3459] [GtoPdb: 2] [UniProtKB: P28564]
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  • Serotonin 1d (5-HT1d) receptor in Pig [ChEMBL: CHEMBL4105] [UniProtKB: P79400]
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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]
  • 5-HT6 receptor in Rat [GtoPdb: 11] [UniProtKB: P31388]
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  • 5-HT1D receptor in Human [GtoPdb: 3] [UniProtKB: P28221]
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  • 5-HT7 receptor in Rat [GtoPdb: 12] [UniProtKB: P32305]
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  • D5 receptor in Human [GtoPdb: 218] [UniProtKB: P21918]
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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 - - 8.3 pKi - - - J Pharmacol Exp Ther (2002) 303: 791-804 [PMID:12388666];
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 8.04 pKi 9.19 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin) B 7.64 pIC50 23 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 7.17 pKi 67 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Alpha-1B adrenergic receptor radioligand binding (ligand: prazosin) B 6.92 pIC50 121 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 7.7 pKi 20 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Alpha-1D adrenergic receptor radioligand binding (ligand: prazosin) B 7.39 pIC50 41 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 9.94 pKi 0.12 nM Ki DrugMatrix in vitro pharmacology data
GtoPdb - - 10.3 pKi - - - J Pharmacol Exp Ther (2002) 303: 791-804 [PMID:12388666];
Pharmacol Res Perspect (2022) 10: e00936 [PMID:35224877]
ChEMBL DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912) B 9.51 pIC50 0.31 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 9.63 pKi 0.24 nM Ki DrugMatrix in vitro pharmacology data
GtoPdb - - 9.9 pKi - - - J Pharmacol Exp Ther (2002) 303: 791-804 [PMID:12388666];
Pharmacol Res Perspect (2022) 10: e00936 [PMID:35224877]
ChEMBL DRUGMATRIX: Alpha-2B adrenergic receptor radioligand binding (ligand: Rauwolscine) B 9.29 pIC50 0.52 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 9.2 pKi 0.63 nM Ki DrugMatrix in vitro pharmacology data
GtoPdb - - 9.9 pKi - - - J Pharmacol Exp Ther (2002) 303: 791-804 [PMID:12388666];
Trends Pharmacol Sci (1997) 18: 211-9 [PMID:9227000];
Pharmacol Res Perspect (2022) 10: e00936 [PMID:35224877]
ChEMBL DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912) B 8.37 pIC50 4.31 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 DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol) B 6.49 pKi 323 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol) B 6.25 pIC50 559 nM IC50 DrugMatrix in vitro pharmacology data
β2-adrenoceptor/Beta-2 adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL210] [GtoPdb: 29] [UniProtKB: P07550]
ChEMBL DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177) B 7.54 pKi 29 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177) B 7.39 pIC50 41 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 7.8 pIC50 16 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 7.07 pKi 86 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL Affinity towards Dopamine receptor D1 B 7.11 pKi 77 nM Ki J Med Chem (1998) 41: 4385-4399 [PMID:9784114]
GtoPdb - - 7.2 pKi - - - J Pharmacol Exp Ther (2002) 303: 791-804 [PMID:12388666]
ChEMBL Binding affinity to dopamine D1 receptor (unknown origin) assessed as inhibition constant B 9.47 pKi 0.34 nM Ki RSC Med Chem (2024) 15: 788-808 [PMID:38516587]
ChEMBL DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390) B 6.76 pIC50 173 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 9.02 pKi 0.95 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL Affinity towards Dopamine receptor D2 B 9.1 pKi 0.8 nM Ki J Med Chem (1998) 41: 4385-4399 [PMID:9784114]
ChEMBL Displacement of [125]iodosulpride from human recombinant dopamine D2L receptor expressed in CHO cells after 30 mins B 9.18 pKi 0.66 nM Ki J Med Chem (2014) 57: 5823-5828 [PMID:24878269]
ChEMBL Displacement of [125]iodosulpride from human recombinant dopamine D2L receptor expressed in CHO cells after 30 mins B 9.18 pKi 0.66 nM Ki J Med Chem (2014) 57: 5823-5828 [PMID:24878269]
ChEMBL Binding affinity towards Dopamine receptor D2 by displacement of [3H]U-86170. B 9.3 pKi 0.5 nM Ki J Med Chem (1997) 40: 639-646 [PMID:9057850]
ChEMBL Binding affinity to dopamine D2 receptor (unknown origin) assessed as inhibition constant B 9.47 pKi 0.34 nM Ki RSC Med Chem (2024) 15: 788-808 [PMID:38516587]
GtoPdb - - 9.5 pKi - - - J Pharmacol Exp Ther (2002) 303: 791-804 [PMID:12388666]
ChEMBL DRUGMATRIX: Dopamine D2L radioligand binding (ligand: [3H] Spiperone) B 8.54 pIC50 2.86 nM IC50 DrugMatrix in vitro pharmacology data
ChEMBL Agonist activity at dopamine D2 receptor short isoform (unknown origin) expressed in mouse NIH/3T3 cells by R-SAT assay B 11 pEC50 0.01 nM EC50 US-20040213816-A1. Selective serotonin 2A/2C receptor inverse agonists as therapeutics for neurodegenerative diseases (2004)
D2 receptor/Dopamine D2 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL339] [GtoPdb: 215] [UniProtKB: P61169]
ChEMBL In vitro affinity at mutant D2 receptor (S194A) in C6 (glioma) cell membranes. B 8.64 pKd 2.3 nM Kd J Med Chem (2000) 43: 3005-3019 [PMID:10956209]
ChEMBL In vitro affinity at wild type Dopamine receptor D2 on C6 (glioma) cell membranes. B 9.22 pKd 0.6 nM Kd J Med Chem (2000) 43: 3005-3019 [PMID:10956209]
ChEMBL In vitro affinity at mutant D2 receptor (S197A) in C6 (glioma) cell membranes. B 9.4 pKd 0.4 nM Kd J Med Chem (2000) 43: 3005-3019 [PMID:10956209]
ChEMBL In vitro affinity at mutant D2 receptor (S194A) in C6 (glioma) cell membranes. B 9.52 pKd 0.3 nM Kd J Med Chem (2000) 43: 3005-3019 [PMID:10956209]
D3 receptor/Dopamine D3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462]
ChEMBL Binding affinity towards Dopamine receptor D3 by displacement of [3H](+)-7-OH-DPAT. B 8.77 pKi 1.7 nM Ki J Med Chem (1997) 40: 639-646 [PMID:9057850]
GtoPdb - - 9.6 pKi - - - J Pharmacol Exp Ther (2002) 303: 791-804 [PMID:12388666]
ChEMBL Inhibition constant against [3H]-spiperone binding to human Dopamine receptor D3 expressed in CHO cells B 9.85 pKi 0.14 nM Ki J Med Chem (2005) 48: 2493-2508 [PMID:15801839]
ChEMBL DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone) B 10.23 pKi 0.06 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone) B 9.76 pIC50 0.17 nM IC50 DrugMatrix in vitro pharmacology data
D4 receptor/Dopamine D4 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL219] [GtoPdb: 217] [UniProtKB: P21917]
GtoPdb - - 8.3 pKi - - - J Pharmacol Exp Ther (2002) 303: 791-804 [PMID:12388666]
ChEMBL Agonist activity at recombinant human D4 receptor expressed in CHOK1 cells assessed as induction of beta arrestin2 recruitment measured after 30 mins by coelenterazine-based beta-galactosidase reporter gene assay B 7.05 pEC50 88.5 nM EC50 J Med Chem (2019) 62: 5132-5147 [PMID:31021617]
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 7.72 pKi 19 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine) B 6.8 pIC50 160 nM IC50 DrugMatrix in vitro pharmacology data
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 5.99 pKi 1022 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine) B 5.98 pIC50 1040 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 for 5-hydroxytryptamine 1A receptor in piglet hippocampus using [3H]8-OH-DPAT B 6.3 pKd 6.3 - pKD J Med Chem (1993) 36: 1918-1919 [PMID:8515429]
ChEMBL Binding affinity to 5HT1A receptor B 8.7 pKd 2 nM Kd J Med Chem (2009) 52: 6107-6125 [PMID:19754201]
ChEMBL Binding affinity towards Serotonin 5-hydroxytryptamine 1A receptor by displacement of [3H]-(+)-8-OH-DPAT. B 9.4 pKi 0.4 nM Ki J Med Chem (1997) 40: 639-646 [PMID:9057850]
GtoPdb - - 9.8 pKi - - - Naunyn Schmiedebergs Arch Pharmacol (1998) 357: 205-17 [PMID:9550290];
Naunyn Schmiedebergs Arch Pharmacol (1997) 355: 682-8 [PMID:9205951];
J Pharmacol Exp Ther (2002) 303: 791-804 [PMID:12388666]
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 9.58 pKi 0.27 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1A radioligand binding (ligand: [3H] 8-OH-DPAT) B 9.33 pIC50 0.47 nM IC50 DrugMatrix in vitro pharmacology data
5-HT1B receptor in Human [GtoPdb: 2] [UniProtKB: P28222]
GtoPdb - - 7.7 pKi - - - J Pharmacol Exp Ther (2002) 303: 791-804 [PMID:12388666]
5-HT1B receptor/Serotonin 1b (5-HT1b) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3459] [GtoPdb: 2] [UniProtKB: P28564]
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol) B 8.34 pKi 4.59 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol) B 8 pIC50 10 nM IC50 DrugMatrix in vitro pharmacology data
Serotonin 1d (5-HT1d) receptor in Pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105] [UniProtKB: P79400]
ChEMBL Binding affinity for 5-hydroxytryptamine 1D receptor in piglet caudate using [3H]5-HT B 8 pKd 8 - pKD J Med Chem (1993) 36: 1918-1919 [PMID:8515429]
5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223]
GtoPdb - - 8.6 pKi - - - J Pharmacol Exp Ther (2002) 303: 791-804 [PMID:12388666]
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2A radioligand binding (ligand: [3H] Ketanserin) B 9.06 pKi 0.87 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2A radioligand binding (ligand: [3H] Ketanserin) B 8.52 pIC50 3.04 nM IC50 DrugMatrix in vitro pharmacology data
ChEMBL Agonist activity at 5HT2A receptor (unknown origin) expressed in mouse NIH/3T3 cells by R-SAT assay B 10.65 pEC50 0.02 nM EC50 US-20040213816-A1. Selective serotonin 2A/2C receptor inverse agonists as therapeutics for neurodegenerative diseases (2004)
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 8.49 pKi 3.24 nM Ki DrugMatrix in vitro pharmacology data
GtoPdb - - 8.9 pKi - - - J Pharmacol Exp Ther (2002) 303: 791-804 [PMID:12388666]
ChEMBL Displacement of [3H]-5HT from human 5-HT2B receptor expressed in CHO-K1 cells assessed as inhibition constant B 8.96 pKi 1.1 nM Ki J Med Chem (2023) 66: 11027-11039 [PMID:37584406]
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide) B 8.29 pIC50 5.09 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 Binding affinity for 5-hydroxytryptamine 1C receptor in piglet choroid plexus using [3H]5-HT B 4.3 pKd 4.3 - pKD J Med Chem (1993) 36: 1918-1919 [PMID:8515429]
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2C radioligand binding (ligand: [3H] Mesulergine) B 8 pKi 10 nM Ki DrugMatrix in vitro pharmacology data
GtoPdb - - 8.3 pKi - - - J Pharmacol Exp Ther (2002) 303: 791-804 [PMID:12388666];
J Neurochem (1999) 72: 2127-34 [PMID:10217294];
Synapse (2000) 35: 144-50 [PMID:10611640]
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2C radioligand binding (ligand: [3H] Mesulergine) B 7.7 pIC50 20 nM IC50 DrugMatrix in vitro pharmacology data
ChEMBL Agonist activity at 5HT2C receptor VGV isoform (unknown origin) expressed in mouse NIH/3T3 cells by R-SAT assay B 7.61 pEC50 24.55 nM EC50 US-20040213816-A1. Selective serotonin 2A/2C receptor inverse agonists as therapeutics for neurodegenerative diseases (2004)
5-HT6 receptor/Serotonin 6 (5-HT6) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3371] [GtoPdb: 11] [UniProtKB: P50406]
GtoPdb - - 8.1 pKi - - - Mol Pharmacol (1998) 54: 577-83 [PMID:9730917];
Mol Pharmacol (1997) 52: 515-523 [PMID:9284367]
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide) B 8.26 pKi 5.51 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide) B 7.92 pIC50 12 nM IC50 DrugMatrix in vitro pharmacology data
5-HT6 receptor in Rat [GtoPdb: 11] [UniProtKB: P31388]
GtoPdb - - 8.3 pKi - - - Mol Pharmacol (1993) 43: 320-7 [PMID:7680751];
Neuropharmacology (1997) 36: 713-20 [PMID:9225298];
J Neurochem (1998) 71: 2169-77 [PMID:9798944];
Mol Pharmacol (1998) 54: 577-83 [PMID:9730917]
5-HT1D receptor in Human [GtoPdb: 3] [UniProtKB: P28221]
GtoPdb - - 9 pKi - - - J Pharmacol Exp Ther (2002) 303: 791-804 [PMID:12388666]
5-HT7 receptor in Rat [GtoPdb: 12] [UniProtKB: P32305]
GtoPdb - - 9.3 pKi - - - J Biol Chem (1993) 268: 18200-4 [PMID:8394362];
Proc Natl Acad Sci USA (1993) 90: 8547-51 [PMID:8397408]
D5 receptor in Human [GtoPdb: 218] [UniProtKB: P21918]
GtoPdb - - 8.5 pKi - - - J Pharmacol Exp Ther (2002) 303: 791-804 [PMID:12388666]

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]