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ChEMBL ligand: CHEMBL516 (Ciprovit, Cyproheptadine) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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α1A-adrenoceptor in Human [GtoPdb: 22] [UniProtKB: P35348] | ||||||||
GtoPdb | - | - | 7.4 | pKi | - | - | - | Jpn J Pharmacol (2001) 86: 189-95 [PMID:11459121] |
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 | 7.01 | pKi | 98 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin) | B | 6.62 | pIC50 | 241 | nM | IC50 | DrugMatrix in vitro pharmacology data |
α1B-adrenoceptor in Human [GtoPdb: 23] [UniProtKB: P35368] | ||||||||
GtoPdb | - | - | 7.6 | pKi | - | - | - | Jpn J Pharmacol (2001) 86: 189-95 [PMID:11459121] |
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 | 7.36 | pKi | 44 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Alpha-1B adrenergic receptor radioligand binding (ligand: prazosin) | B | 7.1 | pIC50 | 80 | 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] | ||||||||
GtoPdb | - | - | 6.9 | pKi | - | - | - | Jpn J Pharmacol (2001) 86: 189-95 [PMID:11459121] |
ChEMBL | DRUGMATRIX: Alpha-1D adrenergic receptor radioligand binding (ligand: prazosin) | B | 7.28 | pKi | 53 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Alpha-1D adrenergic receptor radioligand binding (ligand: prazosin) | B | 6.97 | pIC50 | 107 | 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 | 6.97 | pKi | 106 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912) | B | 6.55 | pIC50 | 283 | 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 | 7.77 | pKi | 17 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Alpha-2B adrenergic receptor radioligand binding (ligand: Rauwolscine) | B | 7.42 | pIC50 | 38 | 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 | 6.73 | pKi | 185 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912) | B | 5.89 | pIC50 | 1275 | nM | IC50 | DrugMatrix in vitro pharmacology data |
Cysteinyl leukotriene receptor 1 in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5645] [UniProtKB: Q2NNR5] | ||||||||
ChEMBL | Inhibitory concentration against LTD4-induced contraction of guinea pig ileum at 10 uM concentration | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (2005) 48: 6523-6543 [PMID:16220969] |
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 | 7.1 | pKi | 79 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390) | B | 6.8 | pIC50 | 158 | 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 | Binding affinity towards dopamine receptor D2 using [3H]spiperone as radioligand | B | 6.95 | pKi | 112 | nM | Ki | Bioorg Med Chem Lett (2004) 14: 2279-2283 [PMID:15081025] |
ChEMBL | DRUGMATRIX: Dopamine D2L radioligand binding (ligand: [3H] Spiperone) | B | 7.26 | pKi | 55 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Dopamine D2L radioligand binding (ligand: [3H] Spiperone) | B | 6.79 | pIC50 | 164 | nM | IC50 | DrugMatrix in vitro pharmacology data |
D2 receptor/Dopamine D2 receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3427] [GtoPdb: 215] [UniProtKB: P61168] | ||||||||
ChEMBL | Binding affinity to Dopamine receptor D2 using [3H]spiperone as radioligand in stably transfected NIH3T3 cells | B | 6.95 | pKi | 112 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 655-658 [PMID:11266163] |
D2 receptor/Dopamine D2 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL339] [GtoPdb: 215] [UniProtKB: P61169] | ||||||||
ChEMBL | Binding affinity at dopamine D2 receptor by [3H]spiperone displacement. | B | 6.85 | pIC50 | 140 | nM | IC50 | J Med Chem (1994) 37: 950-962 [PMID:8151622] |
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 | 7.8 | pKi | 16 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone) | B | 7.32 | pIC50 | 48 | 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 | 4.85 | pKi | 13967.9 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Potassium Channel HERG radioligand binding (ligand: [3H] Astemizole) | B | 4.77 | pIC50 | 17049.1 | nM | IC50 | DrugMatrix in vitro pharmacology data |
H1 receptor/Histamine H1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL231] [GtoPdb: 262] [UniProtKB: P35367] | ||||||||
ChEMBL | Dissociation constant against histamine H1 receptor | B | 5.27 | pKd | 5400 | nM | Kd | J Med Chem (2005) 48: 6523-6543 [PMID:16220969] |
ChEMBL | DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine) | B | 9.37 | pKi | 0.43 | nM | Ki | DrugMatrix in vitro pharmacology data |
GtoPdb | - | - | 10.2 | pKi | - | - | - | Eur J Biochem (1994) 224: 489-95 [PMID:7925364] |
ChEMBL | DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine) | B | 8.43 | pIC50 | 3.7 | nM | IC50 | DrugMatrix in vitro pharmacology data |
Histamine H1 receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3943] [UniProtKB: P31389] | ||||||||
ChEMBL | Potency against histamine H1 receptor on guinea pig ileum | B | 9 | pKd | 1 | nM | Kd | J Med Chem (1995) 38: 3351-3360 [PMID:7650688] |
ChEMBL | Inhibition of [3H]mepyramine binding with histamine H1 receptor in guinea pig cerebellum membranes after 30 min | B | 9.27 | pKi | 0.54 | nM | Ki | J Med Chem (1995) 38: 3351-3360 [PMID:7650688] |
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 | 6.71 | pKi | 195 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine) | B | 6.7 | pIC50 | 198 | nM | IC50 | DrugMatrix in vitro pharmacology data |
SET domain containing 7, histone lysine methyltransferase/Histone-lysine N-methyltransferase SETD7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5523] [GtoPdb: 2703] [UniProtKB: Q8WTS6] | ||||||||
ChEMBL | Inhibition of recombinant Set7/9 (unknown origin) expressed in Escherichia coli BL21 (DE3) using Ac-KRSK-MCA peptide/SAM as substrate preincubated for 1 hr followed by substrate addition measured after 15 mins by Dixon plot analysis | B | 4.82 | pKi | 15000 | nM | Ki | J Med Chem (2016) 59: 3650-3660 [PMID:27088648] |
ChEMBL | Inhibition of SET7 (unknown origin) | B | 4.7 | pIC50 | 20000 | nM | IC50 | J Med Chem (2015) 58: 8166-8181 [PMID:26390175] |
ChEMBL | Inhibition of recombinant SET7/9 (unknown origin) using biotinylated histone H3-derived peptide/SAM as substrate after 60 mins by AlphaLISA assay | B | 5.47 | pIC50 | 3400 | nM | IC50 | Bioorg Med Chem (2016) 24: 4318-4323 [PMID:27448773] |
ChEMBL | Inhibition of recombinant Set7/9 (unknown origin) expressed in Escherichia coli BL21 (DE3) using biotinylated histone H3-derived peptide/SAM as substrate by alphaLISA | B | 6 | pIC50 | 1000 | nM | IC50 | J Med Chem (2016) 59: 3650-3660 [PMID:27088648] |
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 | 8.4 | pKi | 3.94 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Muscarinic M1 radioligand binding (ligand: [3H] N-Methylscopolamine) | B | 7.8 | pIC50 | 16 | 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 | 7.92 | pKi | 12 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Muscarinic M2 radioligand binding (ligand: [3H] N-Methylscopolamine) | B | 7.46 | pIC50 | 35 | 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 | 8.02 | pKi | 9.65 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine) | B | 7.34 | pIC50 | 46 | 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 | 8.66 | pKi | 2.19 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine) | B | 7.8 | pIC50 | 16 | 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 | 8.56 | pKi | 2.75 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine) | B | 8.42 | pIC50 | 3.83 | nM | IC50 | DrugMatrix in vitro pharmacology data |
NET/Norepinephrine transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL222] [GtoPdb: 926] [UniProtKB: P23975] | ||||||||
ChEMBL | DRUGMATRIX: Norepinephrine Transporter radioligand binding (ligand: [125I] RTI-55) | B | 6.25 | pKi | 559 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | Binding affinity towards Norepinephrine transporter using [3H]nisoxitine as radioligand | B | 6.54 | pKi | 290 | nM | Ki | Bioorg Med Chem Lett (2004) 14: 2279-2283 [PMID:15081025] |
ChEMBL | DRUGMATRIX: Norepinephrine Transporter radioligand binding (ligand: [125I] RTI-55) | B | 6.25 | pIC50 | 564 | nM | IC50 | DrugMatrix in vitro pharmacology data |
NET/Norepinephrine transporter in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2370] [GtoPdb: 926] [UniProtKB: O55192] | ||||||||
ChEMBL | Binding affinity to Norepinephrine transporter using [3H]-nisoxatine as radioligand in stably transfected NIH3T3 cells | B | 6.54 | pKi | 290 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 655-658 [PMID:11266163] |
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 | 7.15 | pKi | 70 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1A radioligand binding (ligand: [3H] 8-OH-DPAT) | B | 6.91 | pIC50 | 122 | nM | IC50 | DrugMatrix in vitro pharmacology data |
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 | 5.9 | pKi | 1263 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol) | B | 5.56 | pIC50 | 2778 | 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 towards 5-hydroxytryptamine 2A receptor using [3H]ketanserin | B | 8.52 | pKi | 3 | nM | Ki | Bioorg Med Chem Lett (2004) 14: 2279-2283 [PMID:15081025] |
ChEMBL | Displacement of [3H]ketanserin from 5-hydroxytryptamine 2A receptor expressed NIH3T3 cells | B | 8.8 | pKi | 1.6 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 655-658 [PMID:11266163] |
ChEMBL | Antagonist activity at 5HT2A receptor | F | 9.34 | pKi | 0.46 | nM | Ki | J Med Chem (2012) 55: 5749-5759 [PMID:22694093] |
ChEMBL | DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2A radioligand binding (ligand: [3H] Ketanserin) | B | 9.56 | pKi | 0.28 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2A radioligand binding (ligand: [3H] Ketanserin) | B | 9.01 | pIC50 | 0.97 | nM | IC50 | DrugMatrix in vitro pharmacology data |
5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL322] [GtoPdb: 6] [UniProtKB: P14842] | ||||||||
ChEMBL | Displacement of [3H]ketanserin from 5-hydroxytryptamine 2A receptor of rat brain cortex | B | 8.3 | pKi | 5 | nM | Ki | Bioorg Med Chem Lett (1997) 7: 1635-1638 |
ChEMBL | Binding affinity against 5-hydroxytryptamine 2A receptor from rat forebrain using [3H]ketanserin as radioligand | B | 8.8 | pKi | 1.6 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 563-566 [PMID:11229772] |
ChEMBL | Displacement of [3H]ketanserin from Sprague-Dawley rat cerebral cortex 5-HT2A receptor after 30 mins by liquid scintillation counting analysis | B | 8.8 | pKi | 1.6 | nM | Ki | Bioorg Med Chem (2016) 24: 4318-4323 [PMID:27448773] |
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 | 8.22 | pKi | 6.01 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide) | B | 8.02 | pIC50 | 9.44 | 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 towards 5-hydroxytryptamine 2C receptor using [3H]mesulergine as radioligand | B | 7.96 | pKi | 11 | nM | Ki | Bioorg Med Chem Lett (2004) 14: 2279-2283 [PMID:15081025] |
ChEMBL | DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2C radioligand binding (ligand: [3H] Mesulergine) | B | 8.89 | pKi | 1.28 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2C radioligand binding (ligand: [3H] Mesulergine) | B | 8.61 | pIC50 | 2.44 | nM | IC50 | DrugMatrix in vitro pharmacology data |
5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3006] [GtoPdb: 8] [UniProtKB: P34968] | ||||||||
ChEMBL | Binding affinity to 5-hydroxytryptamine 2C receptor using [3H]Mesulergine as radioligand in stably transfected NIH3T3 cells | B | 7.96 | pKi | 11 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 655-658 [PMID:11266163] |
5-HT6 receptor/Serotonin 6 (5-HT6) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3371] [GtoPdb: 11] [UniProtKB: P50406] | ||||||||
GtoPdb | - | - | 6.8 | pKi | - | - | - | J Neurochem (1996) 66: 47-56 [PMID:8522988] |
ChEMBL | DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide) | B | 6.89 | pKi | 130 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide) | B | 6.55 | pIC50 | 281 | nM | IC50 | DrugMatrix in vitro pharmacology data |
5-HT6 receptor in Rat [GtoPdb: 11] [UniProtKB: P31388] | ||||||||
GtoPdb | - | - | 6.9 | pKi | - | - | - | Mol Pharmacol (1993) 43: 320-7 [PMID:7680751] |
5-HT7 receptor/Serotonin 7 (5-HT7) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3155] [GtoPdb: 12] [UniProtKB: P34969] | ||||||||
GtoPdb | - | - | 6.9 | pKi | - | - | - | J Biol Chem (1993) 268: 23422-6 [PMID:8226867] |
ChEMBL | Displacement of [3H]5-HT from recombinant human 5-HT7 receptor expressed in African green monkey COS7 cells | B | 6.9 | pKi | 125.89 | nM | Ki | Eur J Med Chem (2019) 183: 111705-111705 [PMID:31581003] |
ChEMBL | Non-selective inhibitory activity was determined against 5-hydroxytryptamine 7 receptor | B | 7.3 | pKi | 50.12 | nM | Ki | J Med Chem (2003) 46: 5638-5650 [PMID:14667218] |
5-HT7 receptor/Serotonin 7 (5-HT7) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3223] [GtoPdb: 12] [UniProtKB: P32305] | ||||||||
ChEMBL | Binding affinity towards 5-hydroxytryptamine 7 receptor | B | 7.3 | pKi | 50.12 | nM | Ki | Bioorg Med Chem Lett (2000) 10: 1097-1100 [PMID:10843226] |
GtoPdb | - | - | 7.5 | pKi | - | - | - |
J Biol Chem (1993) 268: 18200-4 [PMID:8394362]; Proc Natl Acad Sci USA (1993) 90: 8547-51 [PMID:8397408] |
SERT/Serotonin transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL228] [GtoPdb: 928] [UniProtKB: P31645] | ||||||||
ChEMBL | Binding affinity towards Serotonin transporter using [3H]paroxetine as radioligand | B | 5.39 | pKi | 4100 | nM | Ki | Bioorg Med Chem Lett (2004) 14: 2279-2283 [PMID:15081025] |
SERT/Serotonin transporter in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4642] [GtoPdb: 928] [UniProtKB: Q60857] | ||||||||
ChEMBL | Binding affinity to Serotonin transporter using [3H]-paroxetine as radioligand in stably transfected NIH3T3 cells | B | 5.39 | pKi | 4100 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 655-658 [PMID:11266163] |
Voltage-dependent L-type calcium channel subunit alpha-1C in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2366456] [UniProtKB: O35505] | ||||||||
ChEMBL | Inhibition of Cav1.2 calcium current measured using whole cell patch clamp in guinea pig ventricular myocytes | F | 4.37 | pIC50 | 42220 | nM | IC50 | IC50 data for the L-type calcium channel extracted from a set of literature articles |
ChEMBL | Inhibition of Cav1.2 calcium current measured using whole cell patch clamp in guinea pig ventricular myocytes | F | 5.11 | pIC50 | 7750 | nM | IC50 | IC50 data for the L-type calcium channel extracted from a set of literature articles |
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]