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

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ChEMBL ligand: CHEMBL12713 (Serlect, Sertindole, LU 23-174, LU-23-174)
  • 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 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]