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ChEMBL ligand: CHEMBL71 (Aminazine, Chlorpromazine, Chlorpromazine hibenzate, Chlorpromazine phenolphthalinate, Chlorpromazine tannate, Chlorpromazinum, Elmarin, Esmind, Fenactil, J2.794D, Largactil, Largactilothiazine, Megaphen, Novomazina, NSC-167745, NSC-226514, Propaphenin, Sanopron, SKF-2601A, Sonazine, Thorazine, Wintermin) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
---|---|---|---|---|---|---|---|---|
Acetylcholine receptor protein alpha chain in Torpedo californica (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3097] [UniProtKB: P02710] | ||||||||
ChEMBL | Displacement of [3H]PCP from nAChR in Torpedo nobiliana electric organs membranes by scintillation counting method | B | 4.79 | pIC50 | 16400 | nM | IC50 | J Pestic Sci (1995) 20: 49-56 |
ChEMBL | Displacement of [3H]PCP from nAChR in Torpedo nobiliana electric organs membranes in presence of 100 uM carbachol by scintillation counting method | B | 5.89 | pIC50 | 1280 | nM | IC50 | J Pestic Sci (1995) 20: 49-56 |
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 | 8.46 | pKi | 3.46 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin) | B | 8.07 | pIC50 | 8.54 | nM | IC50 | DrugMatrix in vitro pharmacology data |
α1B-adrenoceptor/Alpha-1b adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL315] [GtoPdb: 23] [UniProtKB: P15823] | ||||||||
ChEMBL | DRUGMATRIX: Alpha-1B adrenergic receptor radioligand binding (ligand: prazosin) | B | 8.3 | pKi | 4.96 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Alpha-1B adrenergic receptor radioligand binding (ligand: prazosin) | B | 8.05 | pIC50 | 8.97 | 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 | 8.71 | pKi | 1.96 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Alpha-1D adrenergic receptor radioligand binding (ligand: prazosin) | B | 8.4 | pIC50 | 3.99 | 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] | ||||||||
GtoPdb | - | - | 6.6 | pKi | - | - | - |
Mol Pharmacol (1992) 42: 1-5 [PMID:1353247]; Eur J Pharmacol (1994) 252: 43-9 [PMID:7908642]; Pharmacol Res Perspect (2022) 10: e00936 [PMID:35224877] |
ChEMBL | DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912) | B | 6.88 | pKi | 132 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912) | B | 6.45 | pIC50 | 352 | 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 | 7.92 | pKi | 12 | nM | Ki | DrugMatrix in vitro pharmacology data |
GtoPdb | - | - | 8.3 | pKi | - | - | - |
Mol Pharmacol (1992) 42: 1-5 [PMID:1353247]; Eur J Pharmacol (1994) 252: 43-9 [PMID:7908642]; Pharmacol Res Perspect (2022) 10: e00936 [PMID:35224877] |
ChEMBL | DRUGMATRIX: Alpha-2B adrenergic receptor radioligand binding (ligand: Rauwolscine) | B | 7.59 | pIC50 | 26 | 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 | 7.27 | pKi | 54 | nM | Ki | DrugMatrix in vitro pharmacology data |
GtoPdb | - | - | 7.4 | pKi | - | - | - |
Mol Pharmacol (1992) 42: 1-5 [PMID:1353247]; Eur J Pharmacol (1994) 252: 43-9 [PMID:7908642]; Pharmacol Res Perspect (2022) 10: e00936 [PMID:35224877] |
ChEMBL | DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912) | B | 6.43 | pIC50 | 374 | nM | IC50 | DrugMatrix in vitro pharmacology data |
Arachidonate 15-lipoxygenase in Rabbit (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4358] [UniProtKB: P12530] | ||||||||
ChEMBL | DRUGMATRIX: Lipoxygenase 15-LO enzyme inhibition (substrate: Linoleic acid) | B | 4.8 | pIC50 | 15951 | nM | IC50 | DrugMatrix in vitro pharmacology data |
ABCB11/Bile salt export pump in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6020] [GtoPdb: 778] [UniProtKB: O95342] | ||||||||
ChEMBL | TP_TRANSPORTER: increase in dihydrofluorescein intracellular accumulation (dihydrofluorescein: 1 uM) in SK-E2 cells (expressing BSEP) | F | 4.47 | pIC50 | 33500 | nM | IC50 | Pharm Res (2003) 20: 537-544 [PMID:12739759] |
ChEMBL | TP_TRANSPORTER: increase in bodipy intracellular accumulation (Bodipy: 0.2 uM) in SK-E2 cells (expressing BSEP) | F | 4.51 | pIC50 | 30900 | nM | IC50 | Pharm Res (2003) 20: 537-544 [PMID:12739759] |
Calmodulin in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6093] [UniProtKB: P0DP23] | ||||||||
ChEMBL | Binding affinity to human calmodulin expressed in Escherichia coli using M124C-mBBr fluorescent biosensor by spectrofluorometer analysis | B | 5.91 | pKd | 1240 | nM | Kd | J Nat Prod (2013) 76: 1454-1460 [PMID:23876004] |
ChEMBL | Inhibition of recombinant calmodulin mediated bovine brain PDE1 activation assessed as effect on inorganic phosphate release using variable calmodulin level by spectrophotometry | B | 4.71 | pKi | 19280 | nM | Ki | Bioorg Med Chem (2009) 17: 2167-2174 [PMID:19013822] |
ChEMBL | Inhibition of Calmodulin-dependent PDE1 activity assessed as inorganic phosphate release after 30 min | B | 4.99 | pIC50 | 10300 | nM | IC50 | Eur J Med Chem (2011) 46: 2699-2708 [PMID:21514702] |
ChEMBL | Binding affinity to CaM (unknown origin) by equilibrium dialysis method | B | 5.1 | pIC50 | 8000 | nM | IC50 | Eur J Med Chem (2016) 116: 36-45 [PMID:27043269] |
ChEMBL | Inhibition of recombinant calmodulin mediated bovine brain PDE1 activation assessed as effect on inorganic phosphate release by spectrophotometry | B | 5.14 | pIC50 | 7260 | nM | IC50 | Bioorg Med Chem (2009) 17: 2167-2174 [PMID:19013822] |
Calmodulin in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6092] [UniProtKB: P62157] | ||||||||
ChEMBL | Binding affinity to bovine brain CaM by FTPFACE analysis | B | 5.51 | pKd | 3100 | nM | Kd | Eur J Med Chem (2016) 116: 36-45 [PMID:27043269] |
ChEMBL | Displacement of [3H]W-7 from bovine brain CaM | B | 5.6 | pIC50 | 2500 | nM | IC50 | Eur J Med Chem (2016) 116: 36-45 [PMID:27043269] |
δ receptor/Delta opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL236] [GtoPdb: 317] [UniProtKB: P41143] | ||||||||
ChEMBL | DRUGMATRIX: Opiate delta1 (OP1, DOP) radioligand binding (ligand: [3H] Naltrindole) | B | 5.13 | pKi | 7365 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Opiate delta1 (OP1, DOP) radioligand binding (ligand: [3H] Naltrindole) | B | 4.68 | pIC50 | 20894 | 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 | 6.95 | pKi | 112 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cells | B | 7.02 | pKi | 96 | nM | Ki | Bioorg Med Chem Lett (2009) 19: 538-542 [PMID:19091563] |
GtoPdb | - | - | 7.1 | pKi | - | - | - | Nature (1991) 350: 614-9 [PMID:1826762] |
ChEMBL | DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390) | B | 6.65 | pIC50 | 225 | 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-23,390 binding to Dopamine receptor D1 at 0.25 nM | B | 7.3 | pKi | 50 | nM | Ki | J Med Chem (1988) 31: 1941-1946 [PMID:3050089] |
ChEMBL | Binding affinity against dopamine receptor D1 | B | 7.45 | pKi | 35.48 | nM | Ki | J Med Chem (1994) 37: 519-525 [PMID:7907148] |
ChEMBL | In vitro binding affinity against Dopamine receptor D1 in rat striatal tissue | B | 7.46 | pKi | 35 | nM | Ki | J Med Chem (1993) 36: 2107-2114 [PMID:8101877] |
ChEMBL | Binding affinity against Dopamine receptor D1 by using [3H]SCH-23390 as radioligand | B | 8.67 | pIC50 | 2.15 | nM | IC50 | J Med Chem (1995) 38: 318-327 [PMID:7830274] |
D2 receptor/Dopamine D2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416] | ||||||||
GtoPdb | - | - | 7.6 | pKi | - | - | - |
J Pharmacol Exp Ther (1994) 268: 417-26 [PMID:8301582]; Eur J Pharmacol (1992) 225: 331-7 [PMID:1354163] |
ChEMBL | DRUGMATRIX: Dopamine D2L radioligand binding (ligand: [3H] Spiperone) | B | 7.74 | pKi | 18 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | Displacement of [3H]spiperone from human dopamine D2 receptor short form expressed in CHO cells | B | 8 | pKi | 10 | nM | Ki | J Med Chem (2007) 50: 5103-5108 [PMID:17880057] |
ChEMBL | Displacement of [3H]spiperone from dopamine D2-like receptor in porcine striata homogenate | B | 8.1 | pKi | 8 | nM | Ki | J Med Chem (2006) 49: 6848-6857 [PMID:17154515] |
ChEMBL | Displacement of [3H]spiperone from human D2 receptor transfected in HEK cells | B | 8.21 | pKi | 6.1 | nM | Ki | J Med Chem (2014) 57: 4368-4381 [PMID:24779610] |
ChEMBL | Displacement of [3H]spiperone from human dopamine D2 receptor expressed in CHO cells | B | 8.39 | pKi | 4.06 | nM | Ki | Bioorg Med Chem Lett (2009) 19: 538-542 [PMID:19091563] |
ChEMBL | Displacement of [3H]-methylspiperone from human D2 receptor transfected in CHO-K1 cells measured after 60 mins by scintillation counting method | B | 8.63 | pKi | 2.34 | nM | Ki | J Med Chem (2021) 64: 12603-12629 [PMID:34436892] |
ChEMBL | Displacement of [3H]-raclopride from human D2 receptor expressed in HEK cells incubated for 1 hr by Cheng-Prusoff analysis based microbeta scintillation counting method | B | 8.74 | pKi | 1.8 | nM | Ki | Eur J Med Chem (2019) 180: 383-397 [PMID:31325785] |
ChEMBL | Displacement of [3H]-raclopride from recombinant human D2 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting analysis | B | 8.74 | pKi | 1.8 | nM | Ki | Eur J Med Chem (2019) 166: 144-158 [PMID:30703658] |
ChEMBL | Displacement of [3H]-N-methylspiperone from human dopamine D2long receptor expressed in HEK293 cells after 30 mins by scintillation counting | B | 8.92 | pKi | 1.2 | nM | Ki | Bioorg Med Chem (2012) 20: 6366-6374 [PMID:23018094] |
ChEMBL | DRUGMATRIX: Dopamine D2L radioligand binding (ligand: [3H] Spiperone) | B | 7.27 | pIC50 | 54 | nM | IC50 | DrugMatrix in vitro pharmacology data |
ChEMBL | Binding affinity to dopamine D2 receptor (unknown origin) by radioligand binding assay | B | 7.92 | pIC50 | 12 | nM | IC50 | J Med Chem (2013) 56: 8955-8971 [PMID:23919353] |
ChEMBL | Antagonist activity at human D2 receptor expressed in CHO-K1 cells co-expressing Galphaqi5 assessed as decrease in apomorphine-induced calcium mobilization preincubated for 30 mins followed by apomorphine challenge measured for 30 secs by aequorin-derived luminescence assay | F | 8.52 | pIC50 | 3 | nM | IC50 | Bioorg Med Chem Lett (2018) 28: 2039-2049 [PMID:29730027] |
ChEMBL | Antagonist activity against human recombinant dopmaine D2L receptor expressed in CHOK1 cells assessed as reduction in apomorphine-induced increase in intracellular Ca2+ levels by aequorin based radiometric and luminescence plate counting method | F | 9 | pIC50 | 1 | nM | IC50 | Eur J Med Chem (2015) 92: 221-235 [PMID:25557493] |
ChEMBL | Antagonist activity at human dopamine D2 receptor expressed in CHOK1 cells assessed as inhibition of apomorphine-induced calcium mobilization by radiometric and luminescence plate counting method | F | 9 | pIC50 | 1 | nM | IC50 | Eur J Med Chem (2015) 92: 221-235 [PMID:25557493] |
Dopamine D2 receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3998] [UniProtKB: P20288] | ||||||||
ChEMBL | Competition in vitro with the dopamine receptor D2 antagonist [3H]spiperone, for binding sites on calf caudate membranes. | B | 7.1 | pIC50 | 80 | nM | IC50 | J Med Chem (1993) 36: 912-918 [PMID:8096548] |
D2 receptor/Dopamine D2 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL339] [GtoPdb: 215] [UniProtKB: P61169] | ||||||||
ChEMBL | Tested for Competitive binding inhibition of [3H]spiperone to Dopamine receptor D2 in rat striatal membrane. | B | 7.3 | pKi | 50 | nM | Ki | Bioorg Med Chem Lett (1993) 3: 1241-1244 |
GtoPdb | - | - | 7.5 | pKi | - | - | - | Nature (1990) 347: 146-51 [PMID:1975644] |
ChEMBL | In vitro binding affinity for dopamine receptor D2 of rat nucleus accumbens labeled with [3H]spiperone | B | 8 | pKi | 10 | nM | Ki | J Med Chem (1987) 30: 1100-1105 [PMID:2884314] |
ChEMBL | Binding affinity towards dopamine receptor D2 by displacing [3H]spiperone radioligand in rat striatum | B | 8.11 | pKi | 7.8 | nM | Ki | J Med Chem (1992) 35: 552-558 [PMID:1346653] |
ChEMBL | Inhibition of [3H]spiperone binding to Dopamine receptor D2 at 0.02 nM | B | 8.3 | pKi | 4.97 | nM | Ki | J Med Chem (1988) 31: 1941-1946 [PMID:3050089] |
ChEMBL | Compound was evaluated for the binding affinity against [3H]U-86,170-labeled dopamine receptor D2 in cloned CHO cells | B | 8.52 | pKi | 3 | nM | Ki | J Med Chem (1993) 36: 1053-1068 [PMID:8097537] |
ChEMBL | Compound was evaluated for binding affinity towards Dopamine receptor D2 in striatal membranes, using [3H]- spiperone as radioligand in the presence of sodium chloride | B | 8.66 | pKi | 2.19 | nM | Ki | J Med Chem (1991) 34: 1612-1624 [PMID:1827843] |
ChEMBL | In vitro binding affinity against Dopamine D2 receptor in rat striatal tissue. | B | 8.7 | pKi | 2.01 | nM | Ki | J Med Chem (1993) 36: 2107-2114 [PMID:8101877] |
ChEMBL | Binding affinity against dopamine D2 receptor | B | 8.7 | pKi | 2 | nM | Ki | J Med Chem (1994) 37: 519-525 [PMID:7907148] |
ChEMBL | Compound was evaluated for binding affinity towards Dopamine receptor D2 in striatal membranes, using [3H]- spiperone as radioligand in the absence of sodium chloride | B | 8.75 | pKi | 1.77 | nM | Ki | J Med Chem (1991) 34: 1612-1624 [PMID:1827843] |
ChEMBL | Compound was tested for inhibitory activity against the binding of [3H]spiperone to Dopamine receptor D2 in rat striatal membranes | B | 8.92 | pKi | 1.2 | nM | Ki | J Med Chem (1987) 30: 1631-1635 [PMID:2887659] |
ChEMBL | Compound was tested in vitro for its affinity towards rat striatal Dopamine receptor D2 labeled with [3H]- spiperone | B | 7.4 | pIC50 | 40 | nM | IC50 | J Med Chem (1986) 29: 359-369 [PMID:2869146] |
ChEMBL | Ability to bind at dopamine receptor D2 of rat corpus striatum by displacing [3H]spiperone | B | 7.4 | pIC50 | 40 | nM | IC50 | J Med Chem (1989) 32: 1147-1156 [PMID:2542551] |
D3 receptor/Dopamine D3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462] | ||||||||
GtoPdb | - | - | 7.5 | pKi | - | - | - |
J Pharmacol Exp Ther (1994) 268: 417-26 [PMID:8301582]; Eur J Pharmacol (1992) 225: 331-7 [PMID:1354163] |
ChEMBL | Displacement of [3H]N-methylspiperone from human dopamine D3 receptor expressed in HEK293T cell membranes by radioligand binding assay | B | 7.83 | pKi | 14.79 | nM | Ki | Bioorg Med Chem Lett (2018) 28: 1897-1902 [PMID:29631959] |
ChEMBL | Displacement of [3H]N-methylspiperone from human dopamine D3 receptor by PDSP assay | B | 7.96 | pKi | 11 | nM | Ki | Bioorg Med Chem (2016) 24: 2060-2071 [PMID:27032890] |
ChEMBL | Displacement of [3H]N-methylspiperone from human dopamine D3 receptor expressed in HEK293T cell membranes by radioligand binding assay | B | 8.12 | pKi | 7.6 | nM | Ki | Bioorg Med Chem Lett (2018) 28: 1897-1902 [PMID:29631959] |
ChEMBL | Displacement of [3H]spiperone from human dopamine D3 receptor expressed in CHO cells | B | 8.16 | pKi | 6.9 | nM | Ki | Bioorg Med Chem Lett (2009) 19: 538-542 [PMID:19091563] |
ChEMBL | DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone) | B | 8.38 | pKi | 4.21 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | Displacement of [3H]-N-methylspiperone from human dopamine D3 receptor expressed in HEK293 cells after 30 mins by scintillation counting | B | 8.42 | pKi | 3.8 | nM | Ki | Bioorg Med Chem (2012) 20: 6366-6374 [PMID:23018094] |
ChEMBL | Displacement of [3H]N-Methylspiperone from dopamine D3 receptor (unknown origin) | B | 8.48 | pKi | 3.31 | nM | Ki | Bioorg Med Chem Lett (2014) 24: 576-579 [PMID:24365159] |
ChEMBL | Displacement of [3H]N-Methylspiperone from dopamine D3 receptor (unknown origin) | B | 8.48 | pKi | 3.3 | nM | Ki | Bioorg Med Chem Lett (2014) 24: 576-579 [PMID:24365159] |
ChEMBL | Displacement of [125I]iodosulpiride from human Dopamine receptor D3 expressed in CHO cells | B | 8.52 | pKi | 3 | nM | Ki | J Med Chem (2003) 46: 4377-4392 [PMID:14521403] |
ChEMBL | Displacement of [3H]spiperone from human dopamine D3 receptor expressed in CHO cells | B | 8.8 | pKi | 1.58 | nM | Ki | J Med Chem (2007) 50: 5103-5108 [PMID:17880057] |
ChEMBL | DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone) | B | 7.92 | pIC50 | 12 | nM | IC50 | DrugMatrix in vitro pharmacology data |
D3 receptor in Rat [GtoPdb: 216] [UniProtKB: P19020] | ||||||||
GtoPdb | - | - | 7.2 | pKi | - | - | - | Nature (1990) 347: 146-51 [PMID:1975644] |
D4 receptor/Dopamine D4 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL219] [GtoPdb: 217] [UniProtKB: P21917] | ||||||||
ChEMBL | DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone) | B | 6.32 | pKi | 479 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | Displacement of [3H]N-Methylspiperone from dopamine D4 receptor (unknown origin) | B | 7.5 | pKi | 31.62 | nM | Ki | Bioorg Med Chem Lett (2014) 24: 576-579 [PMID:24365159] |
ChEMBL | Displacement of [3H]N-Methylspiperone from dopamine D4 receptor (unknown origin) | B | 7.52 | pKi | 30 | nM | Ki | Bioorg Med Chem Lett (2014) 24: 576-579 [PMID:24365159] |
ChEMBL | Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells | B | 7.6 | pKi | 25.12 | nM | Ki | J Med Chem (2007) 50: 5103-5108 [PMID:17880057] |
GtoPdb | - | - | 7.8 | pKi | - | - | - | Eur J Pharmacol (1993) 236: 483-6 [PMID:8102973] |
ChEMBL | DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone) | B | 5.86 | pIC50 | 1365 | nM | IC50 | DrugMatrix in vitro pharmacology data |
D5 receptor/Dopamine D5 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1850] [GtoPdb: 218] [UniProtKB: P21918] | ||||||||
ChEMBL | Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK cells | B | 6.76 | pKi | 172 | nM | Ki | Bioorg Med Chem Lett (2009) 19: 538-542 [PMID:19091563] |
GtoPdb | - | - | 6.9 | pKi | - | - | - | Nature (1991) 350: 614-9 [PMID:1826762] |
DAT/Dopamine transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL238] [GtoPdb: 927] [UniProtKB: Q01959] | ||||||||
ChEMBL | DRUGMATRIX: Dopamine Transporter radioligand binding (ligand: [125I] RTI-55) | B | 5.68 | pKi | 2100 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Dopamine Transporter radioligand binding (ligand: [125I] RTI-55) | B | 5.58 | pIC50 | 2643 | nM | IC50 | DrugMatrix in vitro pharmacology data |
epidermal growth factor receptor/Epidermal growth factor receptor erbB1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL203] [GtoPdb: 1797] [UniProtKB: P00533] | ||||||||
ChEMBL | DRUGMATRIX: Protein Tyrosine Kinase, EGF Receptor enzyme inhibition (substrate: Poly(Glu:Tyr)) | B | 4.54 | pIC50 | 28868 | nM | IC50 | DrugMatrix in vitro pharmacology data |
GluN2D/GluN3B/GluN1/GluN2A/GluN2B/GluN2C/GluN3A/Glutamate [NMDA] receptor in Human (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL2094124] [GtoPdb: 459, 461, 455, 456, 457, 458, 460] [UniProtKB: O15399, O60391, Q05586, Q12879, Q13224, Q14957, Q8TCU5] | ||||||||
ChEMBL | Binding affinity against dextromethorpin binding site associated with N-methyl-D-aspartate glutamate receptor from guinea pig mitochondrial pellet P2 determined using [3H]1 as radioligand. | B | 5.96 | pIC50 | 1100 | nM | IC50 | J Med Chem (1992) 35: 4135-4142 [PMID:1433216] |
ChEMBL | Inhibition of [3H]1 binding to dextromethorpin binding site of guinea pig microsomal pellet P3 N-methyl-D-aspartate glutamate receptor | B | 6.22 | pIC50 | 600 | nM | IC50 | J Med Chem (1992) 35: 4135-4142 [PMID:1433216] |
GluN1/GluN2A/GluN2B/GluN2C/GluN2D/GluN3B/GluN3A/Glutamate NMDA receptor in Rat (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL1907608] [GtoPdb: 455, 456, 457, 458, 459, 461, 460] [UniProtKB: P35439, Q00959, Q00960, Q00961, Q62645, Q8VHN2, Q9R1M7] | ||||||||
ChEMBL | Displacement of [3H]MK-801 from NMDA receptor in Wistar rat brain membranes by scintillation counting analysis | B | 4.68 | pIC50 | 21000 | nM | IC50 | Bioorg Med Chem Lett (2015) 25: 4131-4135 [PMID:26296478] |
ChEMBL | Binding affinity against dextromethorpin binding site of N-methyl-D-aspartate glutamate receptor from rat brain using [3H]1 | B | 5.89 | pIC50 | 1300 | nM | IC50 | J Med Chem (1992) 35: 4135-4142 [PMID:1433216] |
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 | 5.32 | pKi | 4774.3 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Potassium Channel HERG radioligand binding (ligand: [3H] Astemizole) | B | 5.23 | pIC50 | 5827.5 | nM | IC50 | DrugMatrix in vitro pharmacology data |
ChEMBL | Inhibition of human Potassium channel HERG expressed in mammalian cells | B | 5.83 | pIC50 | 1479.11 | nM | IC50 | Bioorg Med Chem Lett (2003) 13: 2773-2775 [PMID:12873512] |
ChEMBL | Inhibition of partially open human voltage-gated potassium channel subunit Kv11.1 (ERG K+ channel) | F | 5.83 | pIC50 | 1479.11 | nM | IC50 | Bioorg Med Chem Lett (2005) 15: 1737-1741 [PMID:15745831] |
ChEMBL | Inhibitory concentration against potassium channel HERG | B | 5.83 | pIC50 | 1479.11 | nM | IC50 | Bioorg Med Chem Lett (2005) 15: 2886-2890 [PMID:15911273] |
ChEMBL | Inhibition of human ERG expressed in CHO cells by whole cell patch clamp technique | B | 5.83 | pIC50 | 1479.11 | nM | IC50 | Bioorg Med Chem (2008) 16: 6252-6260 [PMID:18448342] |
ChEMBL | Inhibition of human ERG in MCF7 cells | B | 5.83 | pIC50 | 1479.11 | nM | IC50 | Eur J Med Chem (2009) 44: 1926-1932 [PMID:19110341] |
ChEMBL | Inhibition of human ERG | B | 5.83 | pIC50 | 1479.11 | nM | IC50 | Eur J Med Chem (2011) 46: 618-630 [PMID:21185626] |
ChEMBL | Inhibition of hERG K channel | F | 5.83 | pIC50 | 1470 | nM | IC50 | Cardiovasc Res (2011) 91: 53-61 [PMID:21300721] |
ChEMBL | K+ channel blocking activity in Chinese hamster ovary cells expressing HERG Kv11.1 | F | 5.83 | pIC50 | 1470 | nM | IC50 | J Med Chem (2002) 45: 3844-3853 [PMID:12190308] |
H1 receptor/Histamine H1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL231] [GtoPdb: 262] [UniProtKB: P35367] | ||||||||
GtoPdb | - | - | 8.2 | pKi | - | - | - | Neuropsychopharmacology (2003) 28: 519-26 [PMID:12629531] |
ChEMBL | Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO cells | B | 8.37 | pKi | 4.25 | nM | Ki | Bioorg Med Chem Lett (2009) 19: 538-542 [PMID:19091563] |
ChEMBL | DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine) | B | 8.71 | pKi | 1.96 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine) | B | 7.77 | pIC50 | 17 | nM | IC50 | DrugMatrix in vitro pharmacology data |
ChEMBL | Binding affinity to histamine H1 receptor (unknown origin) by radioligand binding assay | B | 7.92 | pIC50 | 12 | nM | IC50 | J Med Chem (2013) 56: 8955-8971 [PMID:23919353] |
Histamine H1 receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3943] [UniProtKB: P31389] | ||||||||
ChEMBL | Displacement of [3H]pyrilamine from histaminergic H1 receptor guinea pig cerebellum | B | 7.3 | pKi | 50.12 | nM | Ki | J Med Chem (2007) 50: 5103-5108 [PMID:17880057] |
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 | 5.59 | pKi | 2582 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine) | B | 5.58 | pIC50 | 2626 | nM | IC50 | DrugMatrix in vitro pharmacology data |
H3 receptor/Histamine H3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL264] [GtoPdb: 264] [UniProtKB: Q9Y5N1] | ||||||||
ChEMBL | Displacement of [125I]iodoproxyfan from human histamine H3 receptor expressed in CHO/HEK293 cells | B | 6 | pKi | >1000 | nM | Ki | Bioorg Med Chem Lett (2009) 19: 538-542 [PMID:19091563] |
κ receptor/Kappa opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL237] [GtoPdb: 318] [UniProtKB: P41145] | ||||||||
ChEMBL | DRUGMATRIX: Opiate kappa (OP2, KOP) radioligand binding (ligand: [3H] Diprenorphine) | B | 5.35 | pKi | 4433 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Opiate kappa (OP2, KOP) radioligand binding (ligand: [3H] Diprenorphine) | B | 4.96 | pIC50 | 11082 | nM | IC50 | DrugMatrix in vitro pharmacology data |
MC3 receptor/Melanocortin receptor 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4644] [GtoPdb: 284] [UniProtKB: P41968] | ||||||||
ChEMBL | DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH) | B | 4.67 | pKi | 21244 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH) | B | 4.61 | pIC50 | 24343 | nM | IC50 | DrugMatrix in vitro pharmacology data |
MC4 receptor/Melanocortin receptor 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL259] [GtoPdb: 285] [UniProtKB: P32245] | ||||||||
ChEMBL | DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH) | B | 4.84 | pKi | 14619 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH) | B | 4.82 | pIC50 | 15204 | nM | IC50 | DrugMatrix in vitro pharmacology data |
MC5 receptor/Melanocortin receptor 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4608] [GtoPdb: 286] [UniProtKB: P33032] | ||||||||
ChEMBL | DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH) | B | 5.15 | pKi | 7145 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH) | B | 5.12 | pIC50 | 7617 | nM | IC50 | DrugMatrix in vitro pharmacology data |
μ receptor/Mu opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372] | ||||||||
ChEMBL | DRUGMATRIX: Opiate mu (OP3, MOP) radioligand binding (ligand: [3H] Diprenorphine) | B | 5.23 | pKi | 5844 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Opiate mu (OP3, MOP) radioligand binding (ligand: [3H] Diprenorphine) | B | 4.84 | pIC50 | 14397 | nM | IC50 | DrugMatrix in vitro pharmacology data |
M1 receptor/Muscarinic acetylcholine receptor M1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL216] [GtoPdb: 13] [UniProtKB: P11229] | ||||||||
ChEMBL | Displacement of [3H]pirenzepine from human M1 receptor expressed in CHO cells | B | 6.9 | pKi | 125.89 | nM | Ki | J Med Chem (2007) 50: 5103-5108 [PMID:17880057] |
ChEMBL | DRUGMATRIX: Muscarinic M1 radioligand binding (ligand: [3H] N-Methylscopolamine) | B | 7.7 | pKi | 20 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Muscarinic M1 radioligand binding (ligand: [3H] N-Methylscopolamine) | B | 7.08 | pIC50 | 83 | 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 | 6.63 | pKi | 232 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Muscarinic M2 radioligand binding (ligand: [3H] N-Methylscopolamine) | B | 6.19 | pIC50 | 652 | 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 | 7.36 | pKi | 44 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine) | B | 6.69 | pIC50 | 206 | 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 | Displacement of [3H]4-DAMP from human M4 receptor expressed in CHO cells | B | 6.8 | pKi | 158.49 | nM | Ki | J Med Chem (2007) 50: 5103-5108 [PMID:17880057] |
ChEMBL | DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine) | B | 7.68 | pKi | 21 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine) | B | 6.83 | pIC50 | 149 | 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 | 7.74 | pKi | 18 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine) | B | 7.6 | pIC50 | 25 | nM | IC50 | DrugMatrix in vitro pharmacology data |
NK2 receptor/Neurokinin 2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2327] [GtoPdb: 361] [UniProtKB: P21452] | ||||||||
ChEMBL | DRUGMATRIX: Tachykinin NK2 radioligand binding (ligand: [3H] SR-48968) | B | 5.04 | pKi | 9065 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Tachykinin NK2 radioligand binding (ligand: [3H] SR-48968) | B | 4.57 | pIC50 | 27195 | 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 | 7.72 | pKi | 19 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Norepinephrine Transporter radioligand binding (ligand: [125I] RTI-55) | B | 7.72 | pIC50 | 19 | nM | IC50 | DrugMatrix in vitro pharmacology data |
ABCB1/P-glycoprotein 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4302] [GtoPdb: 768] [UniProtKB: P08183] | ||||||||
ChEMBL | Concentration giving half of the maximal ATPase activity calculated for the high-affinity binding site of the CHO P-Glycoprotein (P-gp) in two-affinity model | B | 4.91 | pKi | 12200 | nM | Ki | J Med Chem (2002) 45: 5671-5686 [PMID:12477351] |
ChEMBL | High affinity constant at binding site of human P-Glycoprotein (P-gp) in two-affinity model | B | 6.22 | pKi | 600 | nM | Ki | J Med Chem (2002) 45: 5671-5686 [PMID:12477351] |
Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364] | ||||||||
ChEMBL | Antimicrobial activity against Plasmodium falciparum | F | 4.55 | pIC50 | 28000 | nM | IC50 | Bioorg Med Chem (2010) 18: 2225-2231 [PMID:20185316] |
ChEMBL | DNDI: Malaria in Vitro, 72 hour | F | 5.52 | pIC50 | 3030 | nM | IC50 | Antiprotozoal Activity Profiling of Approved Drugs: A Starting Point toward Drug Repositioning |
Pleiotropic ABC efflux transporter of multiple drugs in Saccharomyces cerevisiae S288c (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1697658] [UniProtKB: P33302] | ||||||||
ChEMBL | Inhibition of Pdr5p-mediated rhodamine 6G transport in Saccharomyces cerevisiae MKPDR5h plasma membrane by spectrofluorometric assay | B | 5.35 | pIC50 | 4500 | nM | IC50 | Antimicrob Agents Chemother (2009) 53: 1516-1527 [PMID:19188399] |
K2P2.1/Potassium channel subfamily K member 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2321615] [GtoPdb: 514] [UniProtKB: O95069] | ||||||||
ChEMBL | Inhibition of of human TREK1 expressed in whole COS cells assessed as reduction in channel currents | B | 5.57 | pIC50 | 2700 | nM | IC50 | J Med Chem (2016) 59: 5149-5157 [PMID:26588045] |
Prion protein in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4869] [UniProtKB: P04156] | ||||||||
ChEMBL | Half maximal inhibition of Prion protein PrPsc formation was assayed in ScN2a cells | B | 5.7 | pEC50 | 2000 | nM | EC50 | J Med Chem (2003) 46: 3563-3564 [PMID:12904059] |
Prion protein in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3698] [UniProtKB: P04925] | ||||||||
ChEMBL | Activity at mouse prion protein expressed in Escherichia coli | B | 5.7 | pEC50 | 2000 | nM | EC50 | J Med Chem (2018) 61: 1276-1284 [PMID:29328660] |
erb-b2 receptor tyrosine kinase 2/Receptor protein-tyrosine kinase erbB-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1824] [GtoPdb: 2019] [UniProtKB: P04626] | ||||||||
ChEMBL | DRUGMATRIX: Protein Tyrosine Kinase, ERBB2 (HER2) enzyme inhibition (substrate: Poly(Glu:Tyr)) | B | 4.71 | pIC50 | 19366 | nM | IC50 | DrugMatrix in vitro pharmacology data |
Sarcoplasmic/endoplasmic reticulum calcium ATP-ase in Rabbit (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4693] [UniProtKB: P04191] | ||||||||
ChEMBL | Inhibition of rabbit skeletal muscle microsomes SERCA1a incubated for 10 mins by enzyme-coupled method | B | 4.64 | pIC50 | 23000 | nM | IC50 | J Med Chem (2020) 63: 1937-1963 [PMID:32030976] |
5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908] | ||||||||
ChEMBL | Compound was evaluated for the binding affinity against [3H]8-OH-DPAT-labeled 5-hydroxytryptamine 1A receptor sites in cloned CHO cells | B | 6.17 | pKi | 673 | nM | Ki | J Med Chem (1993) 36: 1053-1068 [PMID:8097537] |
GtoPdb | - | - | 6.2 | pKi | - | - | - | Eur J Pharmacol (1998) 355: 245-56 [PMID:9760039] |
5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327] | ||||||||
ChEMBL | DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1A radioligand binding (ligand: [3H] 8-OH-DPAT) | B | 5.57 | pKi | 2677 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | The compound was tested for its binding affinity towards 5-hydroxytryptamine 1A receptor by displacing [3H]WB-4101 radioligand in rat hippocampus | B | 6.75 | pKi | 179 | nM | Ki | J Med Chem (1992) 35: 552-558 [PMID:1346653] |
ChEMBL | DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1A radioligand binding (ligand: [3H] 8-OH-DPAT) | B | 5.33 | pIC50 | 4685 | nM | IC50 | DrugMatrix in vitro pharmacology data |
ChEMBL | Ability to bind at 5-hydroxytryptamine 1A receptor of rat hippocampus by displacing [3H]8-OH-DPAT | B | 6.43 | pIC50 | 372 | nM | IC50 | J Med Chem (1989) 32: 1147-1156 [PMID:2542551] |
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 | 5.74 | pKi | 1837 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol) | B | 5.39 | pIC50 | 4041 | 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 | Displacement of [3H]-ketanserin from human human 5-HT2A receptor transfected in CHO-K1 cells measured after 60 mins by scintillation counting method | B | 7.92 | pKi | 12.02 | nM | Ki | J Med Chem (2021) 64: 12603-12629 [PMID:34436892] |
GtoPdb | - | - | 8.1 | pKi | - | - | - | Neuropsychopharmacology (2003) 28: 519-26 [PMID:12629531] |
ChEMBL | Displacement of [3H]ketanserin from human 5HT2A receptor expressed in CHO cells | B | 8.2 | pKi | 6.31 | nM | Ki | J Med Chem (2007) 50: 5103-5108 [PMID:17880057] |
ChEMBL | Displacement of [3H]Ketanserin from 5-HT2A receptor (unknown origin) | B | 8.23 | pKi | 5.9 | nM | Ki | Bioorg Med Chem Lett (2014) 24: 576-579 [PMID:24365159] |
ChEMBL | Displacement of [3H]Ketanserin from 5-HT2A receptor (unknown origin) | B | 8.23 | pKi | 5.89 | nM | Ki | Bioorg Med Chem Lett (2014) 24: 576-579 [PMID:24365159] |
ChEMBL | DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2A radioligand binding (ligand: [3H] Ketanserin) | B | 8.96 | pKi | 1.1 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2A radioligand binding (ligand: [3H] Ketanserin) | B | 8.41 | pIC50 | 3.85 | nM | IC50 | DrugMatrix in vitro pharmacology data |
ChEMBL | Binding affinity to 5HT2A receptor (unknown origin) by radioligand binding assay | B | 8.47 | pIC50 | 3.4 | nM | IC50 | J Med Chem (2013) 56: 8955-8971 [PMID:23919353] |
5-HT2A receptor in Rat [GtoPdb: 6] [UniProtKB: P14842] | ||||||||
GtoPdb | - | - | 8.7 | pKi | - | - | - | J Pharmacol Exp Ther (1998) 286: 85-90 [PMID:9655845] |
5-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595] | ||||||||
ChEMBL | DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide) | B | 7.1 | pKi | 80 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | Displacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation counting | B | 7.28 | pKi | 52 | nM | Ki | J Med Chem (2010) 53: 7573-7586 [PMID:20958049] |
ChEMBL | Displacement of [3H]DOI from 5HT2B receptor expressed in CHO cells | B | 7.4 | pKi | 39.81 | nM | Ki | J Med Chem (2007) 50: 5103-5108 [PMID:17880057] |
ChEMBL | DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide) | B | 6.9 | pIC50 | 126 | 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 | Displacement of [3H]mesulergine from 5HT2C receptor expressed in CHO cells | B | 7.4 | pKi | 39.81 | nM | Ki | J Med Chem (2007) 50: 5103-5108 [PMID:17880057] |
ChEMBL | Displacement of [3H]Mesulergine from 5-HT2C receptor (unknown origin) | B | 7.52 | pKi | 30.2 | nM | Ki | Bioorg Med Chem Lett (2014) 24: 576-579 [PMID:24365159] |
ChEMBL | Displacement of [3H]Mesulergine from 5-HT2C receptor (unknown origin) | B | 7.52 | pKi | 30 | nM | Ki | Bioorg Med Chem Lett (2014) 24: 576-579 [PMID:24365159] |
ChEMBL | Displacement of [3H]mesulergine from 5-HT2C receptor after 1.5 hrs by scintillation counting | B | 7.57 | pKi | 27 | nM | Ki | Bioorg Med Chem (2011) 19: 5756-5762 [PMID:21907583] |
GtoPdb | - | - | 8.2 | pKi | - | - | - |
Neuropsychopharmacology (2003) 28: 519-26 [PMID:12629531]; J Pharmacol Exp Ther (2000) 295: 226-32 [PMID:10991983] |
ChEMBL | DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2C radioligand binding (ligand: [3H] Mesulergine) | B | 8.56 | pKi | 2.74 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2C radioligand binding (ligand: [3H] Mesulergine) | B | 8.28 | pIC50 | 5.24 | nM | IC50 | DrugMatrix in vitro pharmacology data |
5-HT6 receptor/Serotonin 6 (5-HT6) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3371] [GtoPdb: 11] [UniProtKB: P50406] | ||||||||
ChEMBL | Displacement of [3H]LSD from 5-HT6 receptor (unknown origin) | B | 7.22 | pKi | 60.26 | nM | Ki | Bioorg Med Chem Lett (2014) 24: 576-579 [PMID:24365159] |
ChEMBL | Displacement of [3H]LSD from 5-HT6 receptor (unknown origin) | B | 7.22 | pKi | 60 | nM | Ki | Bioorg Med Chem Lett (2014) 24: 576-579 [PMID:24365159] |
ChEMBL | Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells | B | 7.3 | pKi | 50.12 | nM | Ki | J Med Chem (2007) 50: 5103-5108 [PMID:17880057] |
ChEMBL | Binding affinity for human 5-hydroxytryptamine 6 receptor | B | 7.3 | pKi | <50 | nM | Ki | J Med Chem (2005) 48: 1781-1795 [PMID:15771424] |
ChEMBL | DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide) | B | 7.59 | pKi | 26 | nM | Ki | DrugMatrix in vitro pharmacology data |
GtoPdb | - | - | 7.8 | pKi | - | - | - |
J Neurochem (1996) 66: 47-56 [PMID:8522988]; Psychopharmacology (Berl.) (2005) 179: 461-9 [PMID:15821958] |
ChEMBL | Binding affinity towards human 5-hydroxytryptamine 6 receptor | B | 8.4 | pKi | 4 | nM | Ki | J Med Chem (2003) 46: 2795-2812 [PMID:12825922] |
ChEMBL | DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide) | B | 7.24 | pIC50 | 57 | nM | IC50 | DrugMatrix in vitro pharmacology data |
5-HT6 receptor in Rat [GtoPdb: 11] [UniProtKB: P31388] | ||||||||
GtoPdb | - | - | 8.4 | pKi | - | - | - | J Pharmacol Exp Ther (1994) 268: 1403-10 [PMID:7908055] |
5-HT7 receptor/Serotonin 7 (5-HT7) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3155] [GtoPdb: 12] [UniProtKB: P34969] | ||||||||
ChEMBL | Displacement of [3H]LSD from 5-HT7 receptor (unknown origin) | B | 6.92 | pKi | 120.23 | nM | Ki | Bioorg Med Chem Lett (2014) 24: 576-579 [PMID:24365159] |
ChEMBL | Displacement of [3H]LSD from 5-HT7 receptor (unknown origin) | B | 6.92 | pKi | 119 | nM | Ki | Bioorg Med Chem Lett (2014) 24: 576-579 [PMID:24365159] |
ChEMBL | Displacement of [3H]LSD from human 5HT7 receptor expressed in CHO cells | B | 7.5 | pKi | 31.62 | nM | Ki | J Med Chem (2007) 50: 5103-5108 [PMID:17880057] |
ChEMBL | Displacement of [3H]LSD from 5-HT7 receptor after 1.5 hrs by scintillation counting | B | 7.57 | pKi | 27 | nM | Ki | Bioorg Med Chem (2011) 19: 5756-5762 [PMID:21907583] |
GtoPdb | - | - | 7.6 | pKi | - | - | - | Psychopharmacology (Berl.) (2005) 179: 461-9 [PMID:15821958] |
ChEMBL | Displacement of [3H]-LSD from 5HT7 receptor (unknown origin) expressed in CHOK1 cells | B | 7.96 | pKi | 11 | nM | Ki | Bioorg Med Chem (2013) 21: 2568-2576 [PMID:23541835] |
ChEMBL | Displacement of [3H]-LSD from 5HT7 receptor (unknown origin) expressed in CHOK1 cells | B | 7.97 | pKi | 10.72 | nM | Ki | Bioorg Med Chem (2013) 21: 2568-2576 [PMID:23541835] |
5-HT7 receptor in Mouse [GtoPdb: 12] [UniProtKB: P32304] | ||||||||
GtoPdb | - | - | 5.3 | 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] | ||||||||
GtoPdb | - | - | 7.6 | pKi | - | - | - | J Pharmacol Exp Ther (1994) 268: 1403-10 [PMID:7908055] |
ChEMBL | Binding affinity towards rat 5-hydroxytryptamine 7 receptor | B | 7.68 | pKi | 21 | nM | Ki | J Med Chem (2003) 46: 2795-2812 [PMID:12825922] |
SERT/Serotonin transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL228] [GtoPdb: 928] [UniProtKB: P31645] | ||||||||
ChEMBL | Displacement of [3H]paraxetine from human 5HT transporter expressed in HEK293 cells | B | 7.2 | pKi | 63.1 | nM | Ki | J Med Chem (2007) 50: 5103-5108 [PMID:17880057] |
ChEMBL | DRUGMATRIX: Transporter, Serotonin (5-Hydroxytryptamine) (SERT) radioligand binding (ligand: [3H] Paroxetine) | B | 7.68 | pKi | 21 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | Binding affinity to SERT (unknown origin) by radioligand binding assay | B | 6.92 | pIC50 | 120 | nM | IC50 | J Med Chem (2013) 56: 8955-8971 [PMID:23919353] |
ChEMBL | DRUGMATRIX: Transporter, Serotonin (5-Hydroxytryptamine) (SERT) radioligand binding (ligand: [3H] Paroxetine) | B | 7.41 | pIC50 | 39 | nM | IC50 | DrugMatrix in vitro pharmacology data |
sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL287] [GtoPdb: 2552] [UniProtKB: Q99720] | ||||||||
ChEMBL | DRUGMATRIX: Sigma1 radioligand binding (ligand: [3H] Haloperidol) | B | 6.72 | pKi | 189 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Sigma1 radioligand binding (ligand: [3H] Haloperidol) | B | 6.35 | pIC50 | 451 | nM | IC50 | DrugMatrix in vitro pharmacology data |
Organic cation transporter 1/Solute carrier family 22 member 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5685] [GtoPdb: 1019] [UniProtKB: O15245] | ||||||||
ChEMBL | Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells by confocal microscopy | B | 4.57 | pIC50 | 27000 | nM | IC50 | J Med Chem (2008) 51: 5932-5942 [PMID:18788725] |
ChEMBL | TP_TRANSPORTER: inhibition of TEA uptake in OCT1-expressing HeLa cells | F | 5.37 | pIC50 | 4300 | nM | IC50 | Mol Pharmacol (2003) 63: 489-498 [PMID:12606755] |
sphingomyelin phosphodiesterase 1/Sphingomyelin phosphodiesterase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2760] [GtoPdb: 2514] [UniProtKB: P17405] | ||||||||
ChEMBL | Inhibition of mmLDL-stimulated acid sphingomyelinase in human PBMC lysates using 3H-sphingomyelin as substrate preincubated for 30 mins followed by mmLDL stimulation measured after 2 hrs by HPLC method | B | 4.96 | pIC50 | 11000 | nM | IC50 | Eur J Med Chem (2018) 153: 73-104 [PMID:29031494] |
Trypanothione reductase in Trypanosoma cruzi (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5131] [UniProtKB: P28593] | ||||||||
ChEMBL | Inhibitory activity against Trypanosoma cruzi trypanothione reductase | B | 4.97 | pKi | 10800 | nM | Ki | J Med Chem (2000) 43: 3148-3156 [PMID:10956223] |
ChEMBL | Inhibitory activity against recombinant Trypanosoma cruzi (Trypanosoma cruzi) Trypanothione reductase (linear competitive type) | B | 4.97 | pKi | 10800 | nM | Ki | J Med Chem (1998) 41: 148-156 [PMID:9457238] |
ChEMBL | Inhibition of Trypanosoma cruzi recombinant trypanothione reductase | B | 5.49 | pKi | 3200 | nM | Ki | Bioorg Med Chem (2008) 16: 6689-6695 [PMID:18558492] |
ChEMBL | Inhibitory activity against recombinant Trypanosoma cruzi (Trypanosoma cruzi) Trypanothione reductase | B | 4.45 | pIC50 | 35400 | nM | IC50 | J Med Chem (1998) 41: 148-156 [PMID:9457238] |
ChEMBL | Inhibition of Trypanosoma cruzi recombinant trypanothione reductase | B | 5.24 | pIC50 | 5800 | nM | IC50 | Bioorg Med Chem (2008) 16: 6689-6695 [PMID:18558492] |
FYN proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase FYN in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1841] [GtoPdb: 2026] [UniProtKB: P06241] | ||||||||
ChEMBL | DRUGMATRIX: Protein Tyrosine Kinase, Fyn enzyme inhibition (substrate: Poly(Glu:Tyr)) | B | 5.06 | pIC50 | 8680 | nM | IC50 | DrugMatrix in vitro pharmacology data |
TRPV1/Vanilloid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5102] [GtoPdb: 507] [UniProtKB: O35433] | ||||||||
ChEMBL | Displacement of [3H]RTX from rat TRPV1 receptor expressed in CHO cells | B | 5.89 | pKi | 1300 | nM | Ki | Bioorg Med Chem (2007) 15: 6043-6053 [PMID:17629487] |
ChEMBL | Antagonist activity at rat TRPV1 receptor expressed in CHO cells by Ca2+ uptake assay | F | 6.28 | pKi | 520 | nM | Ki | Bioorg Med Chem (2007) 15: 6043-6053 [PMID:17629487] |
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]