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ChEMBL ligand: CHEMBL6437 (J16.389I, Mianserin, 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 | 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: 577-583 [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: 577-583 [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 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]