sertindole [Ligand Id: 98] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL12713 (LU 23-174, LU-23-174, Serdolect, Sertindole, Zerdol)
  • Alpha-1a adrenergic receptor in Bovine [ChEMBL: CHEMBL4892] [UniProtKB: P18130]
  • α1A-adrenoceptor/Alpha-1a adrenergic receptor in Rat [ChEMBL: CHEMBL319] [GtoPdb: 22] [UniProtKB: P43140]
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  • Alpha-1b adrenergic receptor in Hamster [ChEMBL: CHEMBL3122] [UniProtKB: P18841]
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  • α1D-adrenoceptor/Alpha-1d adrenergic receptor in Rat [ChEMBL: CHEMBL326] [GtoPdb: 24] [UniProtKB: P23944]
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  • D1 receptor/Dopamine D1 receptor in Human [ChEMBL: CHEMBL2056] [GtoPdb: 214] [UniProtKB: P21728]
  • D1 receptor/Dopamine D1 receptor in Rat [ChEMBL: CHEMBL265] [GtoPdb: 214] [UniProtKB: P18901]
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  • D2 receptor/Dopamine D2 receptor in Human [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
  • D2 receptor/Dopamine D2 receptor in Rat [ChEMBL: CHEMBL339] [GtoPdb: 215] [UniProtKB: P61169]
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  • D3 receptor/Dopamine D3 receptor in Human [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462]
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  • D4 receptor/Dopamine D4 receptor in Human [ChEMBL: CHEMBL219] [GtoPdb: 217] [UniProtKB: P21917]
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  • H1 receptor/Histamine H1 receptor in Human [ChEMBL: CHEMBL231] [GtoPdb: 262] [UniProtKB: P35367]
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  • 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908]
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  • 5-HT1B receptor/Serotonin 1b (5-HT1b) receptor in Human [ChEMBL: CHEMBL1898] [GtoPdb: 2] [UniProtKB: P28222]
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  • 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223]
  • 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Rat [ChEMBL: CHEMBL322] [GtoPdb: 6] [UniProtKB: P14842]
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  • 5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335]
  • 5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Rat [ChEMBL: CHEMBL324] [GtoPdb: 8] [UniProtKB: P08909]
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  • 5-HT6 receptor/Serotonin 6 (5-HT6) receptor in Human [ChEMBL: CHEMBL3371] [GtoPdb: 11] [UniProtKB: P50406]
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  • Kv1.5/Voltage-gated potassium channel subunit Kv1.5 in Human [ChEMBL: CHEMBL4306] [GtoPdb: 542] [UniProtKB: P22460]
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  • 5-HT1D receptor in Human [GtoPdb: 3] [UniProtKB: P28221]
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  • 5-ht1e receptor in Human [GtoPdb: 4] [UniProtKB: P28566]
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  • 5-HT1F receptor in Human [GtoPdb: 5] [UniProtKB: P30939]
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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 34:

Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]