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ChEMBL ligand: CHEMBL6437 (J16.389I, Mianserin, Mianserina, Mianserine, Tolvon) |
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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/Alpha-1a adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL229] [GtoPdb: 22] [UniProtKB: P35348] | ||||||||
ChEMBL | Inhibition of specific [3H]prazosin binding (0.2 nM) to rat brain membranes alpha-1 adrenergic receptor | F | 6.6 | pKd | 251.19 | nM | Kd | J Med Chem (1984) 27: 495-503 [PMID:6142954] |
GtoPdb | - | - | 7.6 | pKi | - | - | - | Jpn J Pharmacol (2001) 86: 189-95 [PMID:11459121] |
ChEMBL | Binding affinity for human cloned Alpha-1A adrenergic receptor | B | 6.39 | pIC50 | 407.38 | nM | IC50 | Bioorg Med Chem Lett (2002) 12: 243-248 [PMID:11755364] |
ChEMBL | Binding affinity for human cloned Alpha-1A adrenergic receptor | B | 6.39 | pIC50 | 407.38 | nM | IC50 | Bioorg Med Chem Lett (2002) 12: 249-253 [PMID:11755365] |
Alpha-1a adrenergic receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4892] [UniProtKB: P18130] | ||||||||
ChEMBL | Displacement of [3H]prazosin from calf cerebral cortex alpha-1 adrenergic receptor | B | 7.37 | pKi | 43 | nM | Ki | J Med Chem (1984) 27: 1182-1185 [PMID:6088770] |
ChEMBL | Binding activity against alpha-1 adrenergic receptor from calf cerebral cortex, using [3H]-prazosin as the radioligand | B | 7.37 | pKi | 43 | nM | Ki | J Med Chem (1983) 26: 1696-1701 [PMID:6139479] |
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 | 7.04 | pKi | 91 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin) | B | 6.65 | pIC50 | 224 | nM | IC50 | DrugMatrix in vitro pharmacology data |
ChEMBL | Compound was tested for its inhibitory activity against Alpha-1 adrenergic receptor | B | 10.15 | pIC50 | 0.07 | nM | IC50 | J Med Chem (1999) 42: 3154-3162 [PMID:10447960] |
α1B-adrenoceptor in Human [GtoPdb: 23] [UniProtKB: P35368] | ||||||||
GtoPdb | - | - | 7.4 | 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 | 7.18 | pKi | 66 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Alpha-1B adrenergic receptor radioligand binding (ligand: prazosin) | B | 6.92 | pIC50 | 119 | 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 | 7.39 | pKi | 41 | nM | Ki | DrugMatrix in vitro pharmacology data |
GtoPdb | - | - | 7.5 | pKi | - | - | - | Jpn J Pharmacol (2001) 86: 189-95 [PMID:11459121] |
ChEMBL | DRUGMATRIX: Alpha-1D adrenergic receptor radioligand binding (ligand: prazosin) | B | 7.08 | pIC50 | 83 | 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 | 7.8 | pKi | 16 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | Inhibition of [3H]rauwolscine binding to Alpha-2A adrenergic receptor | B | 8.32 | pKi | 4.8 | nM | Ki | J Med Chem (2005) 48: 1709-1712 [PMID:15771415] |
ChEMBL | DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912) | B | 7.37 | pIC50 | 43 | nM | IC50 | DrugMatrix in vitro pharmacology data |
ChEMBL | Binding affinity for human cloned Alpha-2A adrenergic receptor | B | 7.68 | pIC50 | 20.89 | nM | IC50 | Bioorg Med Chem Lett (2002) 12: 243-248 [PMID:11755364] |
Alpha-2a adrenergic receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4744] [UniProtKB: Q28838] | ||||||||
ChEMBL | Binding activity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligand | B | 7.77 | pKi | 17 | nM | Ki | J Med Chem (1983) 26: 1696-1701 [PMID:6139479] |
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 | 7.62 | pKi | 24 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Alpha-2B adrenergic receptor radioligand binding (ligand: Rauwolscine) | B | 7.28 | pIC50 | 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 | 7.59 | pKi | 26 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | Inhibition of [3H]rauwolscine binding to Alpha-2C adrenergic receptor | B | 8.42 | pKi | 3.8 | nM | Ki | J Med Chem (2005) 48: 1709-1712 [PMID:15771415] |
ChEMBL | DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912) | B | 6.75 | pIC50 | 179 | nM | IC50 | DrugMatrix in vitro pharmacology data |
ChEMBL | Binding affinity for human cloned Alpha-2C adrenergic receptor | B | 7.37 | pIC50 | 42.66 | nM | IC50 | Bioorg Med Chem Lett (2002) 12: 243-248 [PMID:11755364] |
ChEMBL | Binding affinity for human cloned Alpha-2C adrenergic receptor | B | 7.37 | pIC50 | 42.66 | nM | IC50 | Bioorg Med Chem Lett (2002) 12: 249-253 [PMID:11755365] |
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 | 6.57 | pKi | 271 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390) | B | 6.27 | pIC50 | 543 | nM | IC50 | DrugMatrix in vitro pharmacology data |
D1 receptor/Dopamine D1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL265] [GtoPdb: 214] [UniProtKB: P18901] | ||||||||
ChEMBL | Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D1 | B | 5.85 | pKi | 1420 | nM | Ki | J Med Chem (2005) 48: 1709-1712 [PMID:15771415] |
D2 receptor/Dopamine D2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416] | ||||||||
ChEMBL | Inhibition of [3H]-spiperone binding to human Dopamine receptor D2 | B | 5.66 | pKi | 2197 | nM | Ki | J Med Chem (2005) 48: 1709-1712 [PMID:15771415] |
ChEMBL | Binding affinity for human cloned Dopamine receptor D2L | B | 5.15 | pIC50 | 7079.46 | nM | IC50 | Bioorg Med Chem Lett (2002) 12: 243-248 [PMID:11755364] |
ChEMBL | Binding affinity for human cloned Dopamine receptor D2L | B | 5.15 | pIC50 | 7079.46 | nM | IC50 | Bioorg Med Chem Lett (2002) 12: 249-253 [PMID:11755365] |
D2 receptor/Dopamine D2 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL339] [GtoPdb: 215] [UniProtKB: P61169] | ||||||||
ChEMBL | The binding affinity at the Dopamine receptor D2 determined using [3H]spiperone | B | 6 | pKi | 1000 | nM | Ki | J Med Chem (2002) 45: 3280-3285 [PMID:12109911] |
ChEMBL | Binding affinity towards Dopamine receptor D2 at 1.0 uM concentration | B | 6.08 | pKi | 828 | nM | Ki | J Med Chem (1987) 30: 1433-1454 [PMID:3039136] |
ChEMBL | Binding affinity for rat Dopamine receptor D2 | B | 5.45 | pIC50 | 3548.13 | nM | IC50 | Bioorg Med Chem Lett (2002) 12: 243-248 [PMID:11755364] |
ChEMBL | Binding affinity for rat Dopamine receptor D2 | B | 5.45 | pIC50 | 3548.13 | nM | IC50 | Bioorg Med Chem Lett (2002) 12: 249-253 [PMID:11755365] |
D3 receptor/Dopamine D3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462] | ||||||||
ChEMBL | Inhibition of [125I]iodosulpiride binding to human Dopamine receptor D3 | B | 5.55 | pKi | 2841 | nM | Ki | J Med Chem (2005) 48: 1709-1712 [PMID:15771415] |
ChEMBL | Binding affinity for human cloned Dopamine receptor D3 | B | 5.41 | pIC50 | 3890.45 | nM | IC50 | Bioorg Med Chem Lett (2002) 12: 243-248 [PMID:11755364] |
ChEMBL | Binding affinity for human cloned Dopamine receptor D3 | B | 5.41 | pIC50 | 3890.45 | nM | IC50 | Bioorg Med Chem Lett (2002) 12: 249-253 [PMID:11755365] |
D3 receptor/Dopamine D3 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3138] [GtoPdb: 216] [UniProtKB: P19020] | ||||||||
ChEMBL | Tested for binding affinity against dopamine receptor D3 expressed in Sf9 cells. | B | 5.82 | pKi | 1524 | nM | Ki | J Med Chem (1993) 36: 1499-1500 [PMID:8098771] |
D4 receptor/Dopamine D4 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL219] [GtoPdb: 217] [UniProtKB: P21917] | ||||||||
ChEMBL | Binding affinity for human cloned Dopamine receptor D4 | B | 5.48 | pIC50 | 3311.31 | nM | IC50 | Bioorg Med Chem Lett (2002) 12: 243-248 [PMID:11755364] |
ChEMBL | Binding affinity for human cloned Dopamine receptor D4 | B | 5.48 | pIC50 | 3311.31 | nM | IC50 | Bioorg Med Chem Lett (2002) 12: 249-253 [PMID:11755365] |
DAT/Dopamine transporter in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL338] [GtoPdb: 927] [UniProtKB: P23977] | ||||||||
ChEMBL | Inhibition of dopamine (DA) uptake into rat brain synaptosomes | F | 5 | pKi | >10000 | nM | Ki | J Med Chem (1984) 27: 943-946 [PMID:6747993] |
ChEMBL | Inhibition of the uptake of tritiated dopamine (DA) in rat synaptosomes | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (1987) 30: 1433-1454 [PMID:3039136] |
G-protein coupled receptor in Honeybee (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2366519] [UniProtKB: Q9NG02] | ||||||||
ChEMBL | Antagonist activity at Apis mellifera tyramine receptor TyR1 | B | 4.14 | pIC50 | 73000 | nM | IC50 | Pest Manag Sci (2013) 69: 126-134 [PMID:23129510] |
H1 receptor/Histamine H1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL231] [GtoPdb: 262] [UniProtKB: P35367] | ||||||||
ChEMBL | Inhibition of [3H]pyrilamine binding to human Histamine H1 receptor | B | 8.77 | pKi | 1.7 | nM | Ki | J Med Chem (2005) 48: 1709-1712 [PMID:15771415] |
ChEMBL | DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine) | B | 9.76 | pKi | 0.17 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | Binding affinity for human cloned Histamine H1 receptor expressed in CHO cells using [3H]pyrilamine as radioligand | B | 8.47 | pIC50 | 3.39 | nM | IC50 | Bioorg Med Chem Lett (2002) 12: 243-248 [PMID:11755364] |
ChEMBL | DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine) | B | 8.82 | pIC50 | 1.51 | nM | IC50 | DrugMatrix in vitro pharmacology data |
Histamine H1 receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3943] [UniProtKB: P31389] | ||||||||
ChEMBL | Inhibition of [3H]mepyramine binding with histamine H1 receptor in guinea pig cerebellum membranes after 30 min | B | 9.07 | pKi | 0.85 | 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 | pKi | 992 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine) | B | 6 | pIC50 | 1008 | 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 | 6.06 | pIC50 | 880 | 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 | 6.46 | pKi | 343 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Muscarinic M1 radioligand binding (ligand: [3H] N-Methylscopolamine) | B | 5.85 | pIC50 | 1423 | 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 | 6.42 | pKi | 383 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Muscarinic M2 radioligand binding (ligand: [3H] N-Methylscopolamine) | B | 5.97 | pIC50 | 1078 | 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 | 6.53 | pKi | 298 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine) | B | 5.85 | pIC50 | 1405 | 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 | 6.54 | pKi | 288 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine) | B | 5.68 | pIC50 | 2066 | 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 | 6.64 | pKi | 230 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine) | B | 6.49 | pIC50 | 320 | nM | IC50 | DrugMatrix in vitro pharmacology data |
M5 receptor/Muscarinic acetylcholine receptor M5 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL277] [GtoPdb: 17] [UniProtKB: P08911] | ||||||||
ChEMBL | Binding affinity towards muscarinic acetylcholine receptor by inhibiting specific binding of [3H]quinuclidinyl benzilate (0.8 nM) in vitro to membranes of rat brain without cerebellum | B | 5.72 | pIC50 | 1900 | nM | IC50 | J Med Chem (1984) 27: 995-1003 [PMID:6747997] |
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 | 6.79 | pKi | 161 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Norepinephrine Transporter radioligand binding (ligand: [125I] RTI-55) | B | 6.79 | pIC50 | 163 | nM | IC50 | DrugMatrix in vitro pharmacology data |
Norepinephrine transporter in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL304] [UniProtKB: Q9WTR4] | ||||||||
ChEMBL | Inhibition of [3H]nisoxetine binding to rat Norepinephrine transporter | B | 7 | pKi | 101 | nM | Ki | J Med Chem (2005) 48: 1709-1712 [PMID:15771415] |
ChEMBL | Inhibition of norepinephrine (NE) into rat brain synaptosomes | F | 7.59 | pKi | 26 | nM | Ki | J Med Chem (1984) 27: 943-946 [PMID:6747993] |
ChEMBL | Inhibition of uptake of tritiated norepinephrine (NE) in rat synaptosomes | B | 7.59 | pKi | 26 | nM | Ki | J Med Chem (1987) 30: 1433-1454 [PMID:3039136] |
ChEMBL | The binding affinity at the Norepinephrine transporter reuptake sites determined using competition binding assay | B | 7.66 | pIC50 | 22 | nM | IC50 | J Med Chem (2002) 45: 3280-3285 [PMID:12109911] |
5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908] | ||||||||
ChEMBL | Binding affinity to 5HT1A receptor | B | 6.4 | pKd | 398.11 | nM | Kd | J Med Chem (2009) 52: 6107-6125 [PMID:19754201] |
ChEMBL | The binding affinity at the 5-hydroxytryptamine 1A receptor determined using [3H]5-CT | B | 6.3 | pKi | >500 | nM | Ki | J Med Chem (2002) 45: 3280-3285 [PMID:12109911] |
ChEMBL | Binding affinity for human cloned 5-hydroxytryptamine 1A receptor | B | 6.4 | pIC50 | 398.11 | nM | IC50 | Bioorg Med Chem Lett (2002) 12: 243-248 [PMID:11755364] |
ChEMBL | Binding affinity for human cloned 5-hydroxytryptamine 1A receptor | B | 6.4 | pIC50 | 398.11 | nM | IC50 | Bioorg Med Chem Lett (2002) 12: 249-253 [PMID:11755365] |
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 | 6.3 | pKi | 498 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1A radioligand binding (ligand: [3H] 8-OH-DPAT) | B | 6.06 | pIC50 | 872 | nM | IC50 | DrugMatrix in vitro pharmacology data |
5-HT1B receptor in Mouse [GtoPdb: 2] [UniProtKB: P28334] | ||||||||
GtoPdb | - | - | 8.3 | pKi | - | - | - | Proc Natl Acad Sci USA (1992) 89: 3020-4 [PMID:1557407] |
5-HT1B receptor/Serotonin 1b (5-HT1b) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3459] [GtoPdb: 2] [UniProtKB: P28564] | ||||||||
ChEMBL | Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand. | B | 5.33 | pKi | 4700 | nM | Ki | J Med Chem (1987) 30: 1-12 [PMID:3543362] |
5-HT1D receptor/Serotonin 1d (5-HT1d) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1983] [GtoPdb: 3] [UniProtKB: P28221] | ||||||||
ChEMBL | Binding affinity for human cloned 5-hydroxytryptamine 1D receptor | B | 6.42 | pIC50 | 380.19 | nM | IC50 | Bioorg Med Chem Lett (2002) 12: 243-248 [PMID:11755364] |
ChEMBL | Binding affinity for human cloned 5-hydroxytryptamine 1D receptor | B | 6.42 | pIC50 | 380.19 | nM | IC50 | Bioorg Med Chem Lett (2002) 12: 249-253 [PMID:11755365] |
5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223] | ||||||||
ChEMBL | Displacement of [3H]ketanserin from human 5HT2A receptor expressed in tsA201 cell membranes after 1 hr by scintillation counting analysis | B | 7.57 | pKi | 27 | nM | Ki | J Med Chem (2013) 56: 1211-1227 [PMID:23301527] |
ChEMBL | Displacement of [3H]ketanserin from human 5HT2A receptor expressed in tsA201 cell membranes after 1 hr by scintillation counting analysis | B | 7.57 | pKi | 26.92 | nM | Ki | J Med Chem (2013) 56: 1211-1227 [PMID:23301527] |
ChEMBL | Antagonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced intracellular calcium release measured for 90 secs by fluorescence assay | F | 8.09 | pKi | 8.13 | nM | Ki | J Med Chem (2013) 56: 1211-1227 [PMID:23301527] |
ChEMBL | Antagonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced intracellular calcium release measured for 90 secs by fluorescence assay | F | 8.09 | pKi | 8.1 | nM | Ki | J Med Chem (2013) 56: 1211-1227 [PMID:23301527] |
ChEMBL | Inhibition of [125I]R91150 binding to human 5-hydroxytryptamine 2A receptor | B | 8.37 | pKi | 4.3 | nM | Ki | J Med Chem (2005) 48: 1709-1712 [PMID:15771415] |
ChEMBL | Displacement of [3H]ketanserin from recombinant human 5-HT2A receptor expressed in HEK293 cell membranes after 60 mins by liquid scintillation counting method | B | 8.49 | pKi | 3.2 | nM | Ki | Bioorg Med Chem Lett (2018) 28: 2039-2049 [PMID:29730027] |
ChEMBL | Displacement of [3H]-ketanserin from recombinant human 5HT2A receptor expressed in HEK293 cells measured after 1.5 hrs by microbeta scintillation counting analysis | B | 8.55 | pKi | 2.8 | nM | Ki | Eur J Med Chem (2019) 166: 144-158 [PMID:30703658] |
ChEMBL | Displacement of [3H]ketanserin from human 5HT2A receptor expressed in HEK293 cells incubated for 1.5 hrs by Cheng-Prusoff analysis based microbeta scintillation counting method | B | 8.55 | pKi | 2.8 | nM | Ki | Eur J Med Chem (2019) 180: 383-397 [PMID:31325785] |
ChEMBL | Displacement of [3H]-ketanserin from human 5-HT2A receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation counting method | B | 8.66 | pKi | 2.2 | nM | Ki | Eur J Med Chem (2017) 137: 108-116 [PMID:28575721] |
ChEMBL | Displacement of [3H]-ketanserin from human 5-HT2A receptor expressed in CHO-K1 cell membranes after 60 mins by microbeta scintillation counting analysis | B | 8.7 | pKi | 2 | nM | Ki | Bioorg Med Chem (2018) 26: 527-535 [PMID:29269256] |
ChEMBL | Displacement of [3H]-ketanserin from recombinant human 5HT2A receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting method | B | 8.72 | pKi | 1.91 | nM | Ki | Eur J Med Chem (2020) 191: 112149-112149 [PMID:32105980] |
ChEMBL | Displacement of [3H]-ketanserin from human 5-HT2A receptor expressed in CHOK1 cell membranes after 60 mins by microbeta scintillation counting method | B | 8.92 | pKi | 1.2 | nM | Ki | Medchemcomm (2017) 8: 1690-1696 [PMID:30108880] |
ChEMBL | DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2A radioligand binding (ligand: [3H] Ketanserin) | B | 9.3 | pKi | 0.5 | nM | Ki | DrugMatrix in vitro pharmacology data |
GtoPdb | - | - | 9.6 | pKi | - | - | - |
Synapse (2000) 35: 79-95 [PMID:10611634]; Naunyn Schmiedebergs Arch Pharmacol (2004) 370: 114-23 [PMID:15322733]; Cardiovasc Drugs Ther (2003) 17: 427-34 [PMID:15107597] |
ChEMBL | Binding affinity for human cloned Alpha-2A adrenergic receptor | B | 7.68 | pIC50 | 20.89 | nM | IC50 | Bioorg Med Chem Lett (2002) 12: 249-253 [PMID:11755365] |
ChEMBL | Binding affinity for human cloned 5-hydroxytryptamine 2A receptor expressed in L929 cells using [125I]R91150 as radioligand | B | 7.98 | pIC50 | 10.47 | nM | IC50 | Bioorg Med Chem Lett (2002) 12: 243-248 [PMID:11755364] |
ChEMBL | DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2A radioligand binding (ligand: [3H] Ketanserin) | B | 8.75 | pIC50 | 1.76 | 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 rat cerebral cortex 5HT2A receptor measured after 20 mins by liquid scintillation counter method | B | 7.74 | pKi | 18.4 | nM | Ki | Bioorg Med Chem (2016) 24: 3994-4007 [PMID:27377863] |
ChEMBL | Displacement of [3H]ketanserin from 5HT2A in rat brain cerebral cortex after 20 mins by scintillation counting | B | 8.3 | pKi | 5 | nM | Ki | Eur J Med Chem (2011) 46: 4474-4488 [PMID:21816515] |
ChEMBL | Displacement of [3H]Ketanserin from 5HT2A receptor in Rattus norvegicus (rat) cerebral cortex by filter binding assay | B | 8.46 | pKi | 3.5 | nM | Ki | Med Chem Res (2008) 17: 507-514 |
ChEMBL | Displacement of [3H]ketanserin (0.5 nM) from rat cerebral cortex 5-hydroxytryptamine 2A receptors | B | 8.6 | pKi | 2.5 | nM | Ki | J Med Chem (2003) 46: 265-283 [PMID:12519065] |
ChEMBL | The binding affinity at 5-hydroxytryptamine 2A receptor was determined using [3H]ketanserin | B | 8.82 | pKi | 1.5 | nM | Ki | J Med Chem (2002) 45: 3280-3285 [PMID:12109911] |
GtoPdb | - | - | 9 | pKi | - | - | - |
J Pharmacol Exp Ther (1998) 286: 85-90 [PMID:9655845]; Psychopharmacology (Berl) (1996) 126: 234-40 [PMID:8876023] |
5-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595] | ||||||||
ChEMBL | Displacement of [3H]-5HT from human 5-HT2B receptor expressed in african green monkey COS7 cells assessed as inhibition constant | B | 8.05 | pKi | 9 | 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 | 8.33 | pKi | 4.64 | nM | Ki | DrugMatrix in vitro pharmacology data |
GtoPdb | - | - | 8.8 | pKi | - | - | - |
Naunyn Schmiedebergs Arch Pharmacol (2004) 370: 114-23 [PMID:15322733]; Naunyn Schmiedebergs Arch Pharmacol (1998) 357: 17-24 [PMID:9459568]; Br J Pharmacol (1999) 127: 1075-82 [PMID:10455251] |
ChEMBL | DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide) | B | 8.14 | pIC50 | 7.29 | nM | IC50 | DrugMatrix in vitro pharmacology data |
5-HT2B receptor in Rat [GtoPdb: 7] [UniProtKB: P30994] | ||||||||
GtoPdb | - | - | 7.3 | pKi | - | - | - | Mol Pharmacol (1993) 43: 419-26 [PMID:8450835] |
5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335] | ||||||||
ChEMBL | Evaluated for the binding affinity to porcine choroid plexus at 5-hydroxytryptamine 2C receptor binding site by using [3H]-MES as a radioligand. | B | 8 | pKi | 10 | nM | Ki | J Med Chem (1987) 30: 1-12 [PMID:3543362] |
ChEMBL | Antagonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced intracellular calcium release measured for 90 secs by fluorescence assay | F | 8.09 | pKi | 8.13 | nM | Ki | J Med Chem (2013) 56: 1211-1227 [PMID:23301527] |
ChEMBL | Antagonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced intracellular calcium release measured for 90 secs by fluorescence assay | F | 8.1 | pKi | 8 | nM | Ki | J Med Chem (2013) 56: 1211-1227 [PMID:23301527] |
ChEMBL | Inhibition of [3H]mesulergine binding to human 5-hydroxytryptamine 2C receptor | B | 8.36 | pKi | 4.4 | nM | Ki | J Med Chem (2005) 48: 1709-1712 [PMID:15771415] |
ChEMBL | Binding affinity of compound towards 5-hydroxytryptamine 1C receptor using [3H]mesulergine (1.2 nM) ligand in choroid Plexus pig was determined | B | 8.42 | pKi | 3.8 | nM | Ki | J Med Chem (1997) 40: 952-960 [PMID:9083484] |
ChEMBL | Displacement of [3H]mesulergine from human 5HT2C receptor expressed in tsA201 cell membranes after 1 hr by scintillation counting analysis | B | 8.76 | pKi | 1.74 | nM | Ki | J Med Chem (2013) 56: 1211-1227 [PMID:23301527] |
ChEMBL | Displacement of [3H]mesulergine from human 5HT2C receptor expressed in tsA201 cell membranes after 1 hr by scintillation counting analysis | B | 8.77 | pKi | 1.7 | nM | Ki | J Med Chem (2013) 56: 1211-1227 [PMID:23301527] |
GtoPdb | - | - | 9.2 | pKi | - | - | - |
Synapse (2000) 35: 79-95 [PMID:10611634]; Naunyn Schmiedebergs Arch Pharmacol (2004) 370: 114-23 [PMID:15322733]; J Neurochem (1999) 72: 2127-34 [PMID:10217294] |
ChEMBL | DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2C radioligand binding (ligand: [3H] Mesulergine) | B | 9.22 | pKi | 0.61 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | Binding affinity for human cloned 5-hydroxytryptamine 2C receptor expressed in CHO cells using [3H]mesulergine as radioligand | B | 8.13 | pIC50 | 7.41 | nM | IC50 | Bioorg Med Chem Lett (2002) 12: 243-248 [PMID:11755364] |
ChEMBL | DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2C radioligand binding (ligand: [3H] Mesulergine) | B | 8.94 | pIC50 | 1.16 | nM | IC50 | DrugMatrix in vitro pharmacology data |
5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL324] [GtoPdb: 8] [UniProtKB: P08909] | ||||||||
ChEMBL | The binding affinity at 5-hydroxytryptamine 2C receptor was determined using [3H]mesulergine | B | 8.85 | pKi | 1.4 | nM | Ki | J Med Chem (2002) 45: 3280-3285 [PMID:12109911] |
GtoPdb | - | - | 9.4 | pKi | - | - | - |
Psychopharmacology (Berl) (1996) 126: 234-40 [PMID:8876023]; J Neurochem (1997) 69: 1138-44 [PMID:9282936] |
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 | Binding affinity for human cloned 5-hydroxytryptamine 3 receptor | B | 5.85 | pIC50 | 1412.54 | nM | IC50 | Bioorg Med Chem Lett (2002) 12: 243-248 [PMID:11755364] |
ChEMBL | Binding affinity for human cloned 5-hydroxytryptamine 3 receptor | B | 5.85 | pIC50 | 1412.54 | nM | IC50 | Bioorg Med Chem Lett (2002) 12: 249-253 [PMID:11755365] |
5-HT3A/5-HT3B/Serotonin 3 (5-HT3) receptor in Rat (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2094116] [GtoPdb: 373, 374] [UniProtKB: P35563, Q9JJ16] | ||||||||
ChEMBL | The binding affinity at 5-hydroxytryptamine 3 receptor was determined using [3H]LY-278584 | B | 7.15 | pKi | 70 | nM | Ki | J Med Chem (2002) 45: 3280-3285 [PMID:12109911] |
5-HT6 receptor/Serotonin 6 (5-HT6) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3371] [GtoPdb: 11] [UniProtKB: P50406] | ||||||||
ChEMBL | Binding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligand | B | 7.26 | pKi | 55 | nM | Ki | J Med Chem (2003) 46: 2795-2812 [PMID:12825922] |
GtoPdb | - | - | 7.3 | pKi | - | - | - |
J Neurochem (1996) 66: 47-56 [PMID:8522988]; 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 | 7.4 | pKi | 40 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide) | B | 7.07 | pIC50 | 85 | nM | IC50 | DrugMatrix in vitro pharmacology data |
5-HT6 receptor in Rat [GtoPdb: 11] [UniProtKB: P31388] | ||||||||
GtoPdb | - | - | 7.4 | pKi | - | - | - |
Mol Pharmacol (1993) 43: 320-7 [PMID:7680751]; Neuropharmacology (1997) 36: 713-20 [PMID:9225298]; Mol Pharmacol (1998) 54: 577-83 [PMID:9730917] |
5-HT7 receptor/Serotonin 7 (5-HT7) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3155] [GtoPdb: 12] [UniProtKB: P34969] | ||||||||
ChEMBL | Binding affinity towards rodent 5-hydroxytryptamine 7 receptor | B | 5.1 | pKi | 8010 | nM | Ki | J Med Chem (2003) 46: 2795-2812 [PMID:12825922] |
ChEMBL | Non-selective inhibitory activity was determined against 5-hydroxytryptamine 7 receptor | B | 7.2 | pKi | 63.1 | nM | Ki | J Med Chem (2003) 46: 5638-5650 [PMID:14667218] |
ChEMBL | Inhibition of [3H]5-HT binding to human 5-hydroxytryptamine 7 receptor | B | 7.25 | pKi | 56 | nM | Ki | J Med Chem (2005) 48: 1709-1712 [PMID:15771415] |
GtoPdb | - | - | 7.6 | pKi | - | - | - | Br J Pharmacol (1997) 122: 126-32 [PMID:9298538] |
ChEMBL | Binding affinity for human cloned 5-hydroxytryptamine 7 receptor | B | 6.94 | pIC50 | 114.82 | nM | IC50 | Bioorg Med Chem Lett (2002) 12: 243-248 [PMID:11755364] |
5-HT7 receptor in Mouse [GtoPdb: 12] [UniProtKB: P32304] | ||||||||
GtoPdb | - | - | 7 | pKi | - | - | - | Mol Pharmacol (1993) 44: 229-36 [PMID:8394987] |
5-HT7 receptor/Serotonin 7 (5-HT7) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3223] [GtoPdb: 12] [UniProtKB: P32305] | ||||||||
ChEMBL | Binding affinity towards rat 5-hydroxytryptamine 7 receptor | B | 7 | pKi | 100 | nM | Ki | J Med Chem (2003) 46: 2795-2812 [PMID:12825922] |
ChEMBL | Binding affinity towards 5-hydroxytryptamine 7 receptor | B | 7.2 | pKi | 63.1 | nM | Ki | Bioorg Med Chem Lett (2000) 10: 1097-1100 [PMID:10843226] |
GtoPdb | - | - | 7.4 | 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 | DRUGMATRIX: Transporter, Serotonin (5-Hydroxytryptamine) (SERT) radioligand binding (ligand: [3H] Paroxetine) | B | 5.96 | pKi | 1098 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Transporter, Serotonin (5-Hydroxytryptamine) (SERT) radioligand binding (ligand: [3H] Paroxetine) | B | 5.68 | pIC50 | 2068 | nM | IC50 | DrugMatrix in vitro pharmacology data |
SERT/Serotonin transporter in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL313] [GtoPdb: 928] [UniProtKB: P31652] | ||||||||
ChEMBL | Inhibition of serotonin (5-HT) uptake into rat brain synaptosomes | B | 6 | pKi | >1000 | nM | Ki | J Med Chem (1984) 27: 943-946 [PMID:6747993] |
ChEMBL | Inhibition the uptake of tritiated serotonin (5-HT) by the serotonin transporter SERT in rat synaptosomes | B | 6 | pKi | >1000 | nM | Ki | J Med Chem (1987) 30: 1433-1454 [PMID:3039136] |
ChEMBL | The binding affinity at the 5-HT reuptake sites determined using competition binding assay | B | 5.54 | pIC50 | 2900 | nM | IC50 | J Med Chem (2002) 45: 3280-3285 [PMID:12109911] |
LPA1 receptor in Human [GtoPdb: 272] [UniProtKB: Q92633] | ||||||||
GtoPdb | - | - | 7 | pIC50 | ~100 | nM | IC50 | Eur J Pharmacol (2020) 873: 172963 [PMID:32007501] |
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]