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, Sertindol, Sertindole, Zerdol) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| 5-HT1A receptor/5-hydroxytryptamine receptor 1A 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/5-hydroxytryptamine receptor 1B 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/5-hydroxytryptamine receptor 2A 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/5-hydroxytryptamine receptor 2A 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/5-hydroxytryptamine receptor 2C 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/5-hydroxytryptamine receptor 2C 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/5-hydroxytryptamine receptor 6 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] |
| 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] |
| ABCB1/ATP-dependent translocase ABCB1 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] |
| D1 receptor/D(1A) dopamine 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/D(1A) dopamine 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/D(2) dopamine 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] |
| ChEMBL | Binding affinity to dopamine D2 receptor (unknown origin) assessed as inhibition constant | B | 9.42 | pKi | 0.38 | nM | Ki | RSC Med Chem (2024) 15: 788-808 [PMID:38516587] |
| D2 receptor/D(2) dopamine 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/D(3) dopamine 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/D(4) dopamine 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 |
| 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] |
| Kv1.5/Potassium voltage-gated channel subfamily A member 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] |
| Kv11.1/Voltage-gated inwardly rectifying potassium channel KCNH2 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] |
| 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 36:
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]
