sertindole [Ligand Id: 98] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL12713 (LU 23-174, LU-23-174, Serdolect, Serlect, Sertindole, Zerdol) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| Alpha-1a adrenergic receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4892] [UniProtKB: P18130] | ||||||||
| ChEMBL | Displacement of [3H]prazosin (0.3 nM) from bovine Alpha-1A adrenergic receptor expressed in BHK cells | B | 9.43 | pKi | 0.37 | nM | Ki | J Med Chem (2003) 46: 265-283 [PMID:12519065] |
| ChEMBL | Displacement of [3H]prozosin from bovine cloned Alpha-1A receptor expressed in BHK cells | B | 9.43 | pKi | 0.37 | nM | Ki | J Med Chem (2010) 53: 7021-7034 [PMID:20857909] |
| ChEMBL | Displacement of [3H]prazosine from bovine alpha1A adrenoceptor expressed in BHK cells after 20 mins by scintillation counting analysis | B | 9.43 | pKi | 0.37 | nM | Ki | Bioorg Med Chem (2013) 21: 196-204 [PMID:23218776] |
| α1A-adrenoceptor/Alpha-1a adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL319] [GtoPdb: 22] [UniProtKB: P43140] | ||||||||
| ChEMBL | Displacement of [3H]prazosin from Alpha-1 adrenergic receptor in whole rat brain membranes | B | 8.47 | pIC50 | 3.4 | nM | IC50 | J Med Chem (1992) 35: 4823-4831 [PMID:1336054] |
| ChEMBL | Binding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranes | B | 8.47 | pIC50 | 3.4 | nM | IC50 | J Med Chem (1996) 39: 3723-3738 [PMID:8809161] |
| Alpha-1b adrenergic receptor in Hamster (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3122] [UniProtKB: P18841] | ||||||||
| ChEMBL | Displacement of [3H]prazosin (0.5 nM) from hamster Alpha-1B adrenergic receptor expressed in rat-1 cells | B | 9.48 | pKi | 0.33 | nM | Ki | J Med Chem (2003) 46: 265-283 [PMID:12519065] |
| ChEMBL | Displacement of [3H]prozosin from hamster cloned alpha-1b receptor | B | 9.48 | pKi | 0.33 | nM | Ki | J Med Chem (2010) 53: 7021-7034 [PMID:20857909] |
| ChEMBL | Displacement of [3H]prazosine from hamster alpha1B adrenoceptor expressed in Rat1 cells after 20 mins by scintillation counting analysis | B | 9.48 | pKi | 0.33 | nM | Ki | Bioorg Med Chem (2013) 21: 196-204 [PMID:23218776] |
| α1D-adrenoceptor/Alpha-1d adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL326] [GtoPdb: 24] [UniProtKB: P23944] | ||||||||
| ChEMBL | Displacement of [3H]prazosin (0.3 nM) from rat Alpha-1D adrenergic receptor expressed in CHO cells | B | 9.18 | pKi | 0.66 | nM | Ki | J Med Chem (2003) 46: 265-283 [PMID:12519065] |
| ChEMBL | Displacement of [3H]prozosin from rat cloned alpha1d receptor | B | 9.18 | pKi | 0.66 | nM | Ki | J Med Chem (2010) 53: 7021-7034 [PMID:20857909] |
| ChEMBL | Displacement of [3H]prazosine from rat alpha1D adrenoceptor expressed in CHO cells after 20 mins by scintillation counting analysis | B | 9.18 | pKi | 0.66 | nM | Ki | Bioorg Med Chem (2013) 21: 196-204 [PMID:23218776] |
| D1 receptor/Dopamine D1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2056] [GtoPdb: 214] [UniProtKB: P21728] | ||||||||
| ChEMBL | Binding affinity towards human Dopamine receptor D1 | B | 6.68 | pKi | 210 | nM | Ki | J Med Chem (2004) 47: 1303-1314 [PMID:14998318] |
| D1 receptor/Dopamine D1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL265] [GtoPdb: 214] [UniProtKB: P18901] | ||||||||
| ChEMBL | Ability to displace [3H]-SCH- 23390 (0.2 nM) from corpus striatum of rat Dopamine receptor D1 | B | 7.92 | pKi | 12 | nM | Ki | J Med Chem (2003) 46: 265-283 [PMID:12519065] |
| D2 receptor/Dopamine D2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416] | ||||||||
| ChEMBL | Binding affinity towards human Dopamine receptor D2 | B | 8.13 | pKi | 7.4 | nM | Ki | J Med Chem (2004) 47: 1303-1314 [PMID:14998318] |
| GtoPdb | - | - | 8.92 | pKi | 1.2 | nM | Ki |
Neuropsychopharmacology (2003) 28: 519-26 [PMID:12629531]; Eur J Pharmacol (2002) 450: 37-41 [PMID:12176106]; Clinical Neuroscience Research (2001) 1: 53-60 |
| ChEMBL | Displacement of [3H]prozosin from human cloned dopamine D2 receptor expressed in CHO cells | B | 9.35 | pKi | 0.45 | nM | Ki | J Med Chem (2010) 53: 7021-7034 [PMID:20857909] |
| ChEMBL | Displacement of [3H]spiperone from human dopamine D2 receptor expressed in CHO cells after 30 mins by scintillation counting analysis | B | 9.35 | pKi | 0.45 | nM | Ki | Bioorg Med Chem (2013) 21: 196-204 [PMID:23218776] |
| D2 receptor/Dopamine D2 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL339] [GtoPdb: 215] [UniProtKB: P61169] | ||||||||
| ChEMBL | Displacement of [3H]spiperone (0.5 nM) from rat corpus striatum dopamine D2 receptor | B | 9.35 | pKi | 0.45 | nM | Ki | J Med Chem (2003) 46: 265-283 [PMID:12519065] |
| ChEMBL | Displacement of [3H]-spiperone from Dopamine receptor D2 from rat striatal membranes | B | 8.39 | pIC50 | 4.1 | nM | IC50 | J Med Chem (1992) 35: 4813-4822 [PMID:1336053] |
| ChEMBL | Displacement of [3H]spiperone from Dopamine receptor D2 rat striatal membranes | B | 8.39 | pIC50 | 4.1 | nM | IC50 | J Med Chem (1992) 35: 4823-4831 [PMID:1336054] |
| ChEMBL | Binding affinity at dopamine D2 receptor by [3H]spiperone displacement. | B | 8.39 | pIC50 | 4.1 | nM | IC50 | J Med Chem (1994) 37: 950-962 [PMID:8151622] |
| ChEMBL | Tested for the inhibition of [3H]spiperone binding to dopamine D2 receptor | B | 8.39 | pIC50 | 4.1 | nM | IC50 | J Med Chem (1992) 35: 1092-1101 [PMID:1348090] |
| ChEMBL | Binding affinity to dopamine receptor D2 using a [3H]-spiperone binding assay in rat cortical membranes | B | 8.39 | pIC50 | 4.1 | nM | IC50 | J Med Chem (1996) 39: 3723-3738 [PMID:8809161] |
| D3 receptor/Dopamine D3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462] | ||||||||
| ChEMBL | Binding affinity towards human Dopamine receptor D3 | B | 8.09 | pKi | 8.2 | nM | Ki | J Med Chem (2004) 47: 1303-1314 [PMID:14998318] |
| ChEMBL | Ability to displace [3H]spiperone (0.3 nM) from CHO cells of human Dopamine receptor D3 | B | 8.59 | pKi | 2.6 | nM | Ki | J Med Chem (2003) 46: 265-283 [PMID:12519065] |
| GtoPdb | - | - | 8.8 | pKi | 1.6 | nM | Ki |
Psychopharmacology (Berl.) (1996) 124: 57-73 [PMID:8935801]; Neuropsychopharmacology (1998) 18: 63-101 [PMID:9430133]; Clinical Neuroscience Research (2001) 1: 53-60 |
| D4 receptor/Dopamine D4 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL219] [GtoPdb: 217] [UniProtKB: P21917] | ||||||||
| ChEMBL | Binding affinity towards human dopamine-4.2 receptor | B | 7.68 | pKi | 21 | nM | Ki | J Med Chem (2004) 47: 1303-1314 [PMID:14998318] |
| ChEMBL | Displacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cells | B | 7.96 | pKi | 11 | nM | Ki | J Med Chem (2003) 46: 265-283 [PMID:12519065] |
| GtoPdb | - | - | 9.07 | pKi | 0.85 | nM | Ki |
J Pharmacol Exp Ther (2005) 315: 1278-87 [PMID:16135699]; Mol Psychiatry (1998) 3: 123-34 [PMID:9577836]; Neuropsychopharmacology (1997) 16: 93-110; discussion 111-35 [PMID:9015795]; Clinical Neuroscience Research (2001) 1: 53-60 |
| Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809] | ||||||||
| ChEMBL | Inhibition of human ERG | B | 7.83 | pIC50 | 14.79 | nM | IC50 | Eur J Med Chem (2011) 46: 618-630 [PMID:21185626] |
| ChEMBL | Inhibition of human ERG channel | B | 7.83 | pIC50 | 14.7 | nM | IC50 | J Med Chem (2009) 52: 4266-4276 [PMID:19534531] |
| ChEMBL | Inhibition of human ERG channel | B | 7.83 | pIC50 | 14.7 | nM | IC50 | J Med Chem (2009) 52: 4266-4276 [PMID:19534531] |
| ChEMBL | Inhibition of human voltage-gated potassium channel subunit Kv11.1 (ERG K+ channel) in open state | F | 7.85 | pIC50 | 14.13 | nM | IC50 | Bioorg Med Chem Lett (2005) 15: 1737-1741 [PMID:15745831] |
| ChEMBL | Inhibition of human ERG in MCF7 cells | B | 7.85 | pIC50 | 14.13 | nM | IC50 | Eur J Med Chem (2009) 44: 1926-1932 [PMID:19110341] |
| ChEMBL | Inhibition of hERG K channel | F | 7.85 | pIC50 | 14 | nM | IC50 | Cardiovasc Res (2011) 91: 53-61 [PMID:21300721] |
| ChEMBL | K+ channel blocking activity in human embryonic kidney cells expressing HERG Kv11.1 | F | 7.85 | pIC50 | 14 | nM | IC50 | J Med Chem (2002) 45: 3844-3853 [PMID:12190308] |
| ChEMBL | Inhibitory concentration against potassium channel HERG | B | 8 | pIC50 | 10 | nM | IC50 | Bioorg Med Chem Lett (2005) 15: 2886-2890 [PMID:15911273] |
| ChEMBL | Inhibition of human Potassium channel HERG expressed in mammalian cells | B | 8 | pIC50 | 10 | nM | IC50 | Bioorg Med Chem Lett (2003) 13: 2773-2775 [PMID:12873512] |
| ChEMBL | Inhibition of human ERG expressed in CHO cells by whole cell patch clamp technique | B | 8 | pIC50 | 10 | nM | IC50 | Bioorg Med Chem (2008) 16: 6252-6260 [PMID:18448342] |
| ChEMBL | Inhibitory activity against Potassium channel HERG | B | 8.52 | pIC50 | 3 | nM | IC50 | J Med Chem (2003) 46: 2017-2022 [PMID:12747773] |
| ChEMBL | Inhibition of K+ channel activity in CHO cells expressing HERG Kv11.1 | B | 8.52 | pIC50 | 3 | nM | IC50 | Bioorg Med Chem Lett (2003) 13: 1829-1835 [PMID:12729675] |
| ChEMBL | Inhibitory concentration against hERG currents after prolonged depolarizing pulses | F | 8.52 | pIC50 | ~3 | nM | IC50 | J Med Chem (2001) 44: 1627-1653 [PMID:11356099] |
| ChEMBL | Inhibition of human cloned ERG expressed in CHO cells assessed as inhibition of potassium channel current by automated patch clamp assay | B | 8.57 | pIC50 | 2.7 | nM | IC50 | J Med Chem (2014) 57: 4543-4557 [PMID:24805037] |
| H1 receptor/Histamine H1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL231] [GtoPdb: 262] [UniProtKB: P35367] | ||||||||
| ChEMBL | Binding affinity towards human histamine H1 receptor | B | 6.24 | pKi | 570 | nM | Ki | J Med Chem (2004) 47: 1303-1314 [PMID:14998318] |
| GtoPdb | - | - | 6.9 | pKi | - | - | - |
Psychopharmacology (Berl.) (1996) 124: 57-73 [PMID:8935801]; Neuropsychopharmacology (2003) 28: 519-26 [PMID:12629531] |
| ChEMBL | Displacement of [3H]prozosin from human cloned histamine H1 receptor expressed in CHO cells | B | 9.29 | pKi | 0.51 | nM | Ki | J Med Chem (2010) 53: 7021-7034 [PMID:20857909] |
| ABCB1/P-glycoprotein 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4302] [GtoPdb: 768] [UniProtKB: P08183] | ||||||||
| ChEMBL | Inhibition of human ABCB1-mediated rhodamine 123 efflux in mouse L5178 cells expressing human MDR1 after 20 mins by FACS analysis | B | 5.19 | pIC50 | 6500 | nM | IC50 | J Med Chem (2011) 54: 1740-1751 [PMID:21341745] |
| 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908] | ||||||||
| GtoPdb | - | - | 6.6 | pKi | - | - | - |
Eur J Pharmacol (1998) 355: 245-56 [PMID:9760039]; Psychopharmacology (Berl.) (1996) 124: 57-73 [PMID:8935801] |
| ChEMBL | Ability to displace [3H]5-CT (2.0 nM) from HeLa cells of human 5-hydroxytryptamine 1A receptor | B | 7.48 | pKi | 33 | nM | Ki | J Med Chem (2003) 46: 265-283 [PMID:12519065] |
| 5-HT1B receptor/Serotonin 1b (5-HT1b) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1898] [GtoPdb: 2] [UniProtKB: P28222] | ||||||||
| GtoPdb | - | - | 7 | pKi | - | - | - | Psychopharmacology (Berl.) (1996) 124: 57-73 [PMID:8935801] |
| ChEMBL | Ability to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptor | B | 7.25 | pKi | 56 | nM | Ki | J Med Chem (2003) 46: 265-283 [PMID:12519065] |
| 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223] | ||||||||
| ChEMBL | Binding affinity towards human serotonin 5-hydroxytryptamine 2A receptor | B | 9.07 | pKi | 0.85 | nM | Ki | J Med Chem (2004) 47: 1303-1314 [PMID:14998318] |
| ChEMBL | Binding affinity towards Serotonin 5-hydroxytryptamine 2A receptor | B | 9.22 | pKi | 0.6 | nM | Ki | J Med Chem (2003) 46: 2017-2022 [PMID:12747773] |
| GtoPdb | - | - | 9.4 | pKi | - | - | - |
Psychopharmacology (Berl.) (1996) 124: 57-73 [PMID:8935801]; Neuropsychopharmacology (2003) 28: 519-26 [PMID:12629531]; Eur J Pharmacol (2002) 450: 37-41 [PMID:12176106] |
| 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 (0.5 nM) from rat cerebral cortex 5-hydroxytryptamine 2A receptors | B | 9.7 | pKi | 0.2 | nM | Ki | J Med Chem (2003) 46: 265-283 [PMID:12519065] |
| ChEMBL | Binding affinity to serotonin 5-hydroxytryptamine 2A receptors using a radioligand [3H]ketanserin binding assay in rat cortical membranes | B | 9.41 | pIC50 | 0.39 | nM | IC50 | J Med Chem (1996) 39: 3723-3738 [PMID:8809161] |
| 5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335] | ||||||||
| ChEMBL | Binding affinity towards human serotonin 5-hydroxytryptamine 2C receptor | B | 8.89 | pKi | 1.3 | nM | Ki | J Med Chem (2004) 47: 1303-1314 [PMID:14998318] |
| ChEMBL | Displacement of [3H]mesulergine from human 5HT2C receptor in human tsA201 cells | B | 9 | pKi | 1 | nM | Ki | Bioorg Med Chem Lett (2010) 20: 5431-5433 [PMID:20719507] |
| GtoPdb | - | - | 9.2 | pKi | - | - | - |
Neuropsychopharmacology (2003) 28: 519-26 [PMID:12629531]; J Pharmacol Exp Ther (2000) 295: 226-32 [PMID:10991983] |
| ChEMBL | Displacement of [3H]prozosin from human cloned 5HT2C receptor expressed in CHO cells | B | 9.7 | pKi | 0.2 | nM | Ki | J Med Chem (2010) 53: 7021-7034 [PMID:20857909] |
| 5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL324] [GtoPdb: 8] [UniProtKB: P08909] | ||||||||
| ChEMBL | Displacement of [3H]mesulergine (0.5 nM) from rat 5-hydroxytryptamine 2C receptor expressed in SR-3T3 cells | B | 9.29 | pKi | 0.51 | nM | Ki | J Med Chem (2003) 46: 265-283 [PMID:12519065] |
| 5-HT6 receptor/Serotonin 6 (5-HT6) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3371] [GtoPdb: 11] [UniProtKB: P50406] | ||||||||
| ChEMBL | Displacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cells | B | 8.3 | pKi | 5 | nM | Ki | Bioorg Med Chem Lett (2010) 20: 5431-5433 [PMID:20719507] |
| Kv1.5/Voltage-gated potassium channel subunit Kv1.5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4306] [GtoPdb: 542] [UniProtKB: P22460] | ||||||||
| ChEMBL | Inhibition of voltage-gated potassium channel subunit Kv1.5 | F | 5.7 | pIC50 | 2000 | nM | IC50 | J Med Chem (2001) 44: 1627-1653 [PMID:11356099] |
| 5-HT1D receptor in Human [GtoPdb: 3] [UniProtKB: P28221] | ||||||||
| GtoPdb | - | - | 7.2 | pKi | - | - | - | Psychopharmacology (Berl.) (1996) 124: 57-73 [PMID:8935801] |
| 5-ht1e receptor in Human [GtoPdb: 4] [UniProtKB: P28566] | ||||||||
| GtoPdb | - | - | 6.4 | pKi | - | - | - | Psychopharmacology (Berl.) (1996) 124: 57-73 [PMID:8935801] |
| 5-HT1F receptor in Human [GtoPdb: 5] [UniProtKB: P30939] | ||||||||
| GtoPdb | - | - | 6.4 | pKi | - | - | - | Psychopharmacology (Berl.) (1996) 124: 57-73 [PMID:8935801] |
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]
