ziprasidone [Ligand Id: 59] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL708 (CP-88059, Geodon, Zipradon, Ziprasidone)
  • α1A-adrenoceptor/Alpha-1a adrenergic receptor in Human [ChEMBL: CHEMBL229] [GtoPdb: 22] [UniProtKB: P35348]
  • α1A-adrenoceptor/Alpha-1a adrenergic receptor in Rat [ChEMBL: CHEMBL319] [GtoPdb: 22] [UniProtKB: P43140]
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  • D1 receptor/Dopamine D1 receptor in Human [ChEMBL: CHEMBL2056] [GtoPdb: 214] [UniProtKB: P21728]
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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]
  • H1 receptor/Histamine H1 receptor in Rat [ChEMBL: CHEMBL4701] [GtoPdb: 262] [UniProtKB: P31390]
  • Histamine H1 receptor in Guinea pig [ChEMBL: CHEMBL3943] [UniProtKB: P31389]
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  • M1 receptor/Muscarinic acetylcholine receptor M1 in Human [ChEMBL: CHEMBL216] [GtoPdb: 13] [UniProtKB: P11229]
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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-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-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Human [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595]
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  • 5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335]
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  • 5-HT6 receptor/Serotonin 6 (5-HT6) receptor in Human [ChEMBL: CHEMBL3371] [GtoPdb: 11] [UniProtKB: P50406]
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  • 5-HT7 receptor/Serotonin 7 (5-HT7) receptor in Human [ChEMBL: CHEMBL3155] [GtoPdb: 12] [UniProtKB: P34969]
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  • SERT/Serotonin transporter in Human [ChEMBL: CHEMBL228] [GtoPdb: 928] [UniProtKB: P31645]
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  • 5-HT1B receptor in Human [GtoPdb: 2] [UniProtKB: P28222]
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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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  • NET in Rat [GtoPdb: 926]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
α1A-adrenoceptor/Alpha-1a adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL229] [GtoPdb: 22] [UniProtKB: P35348]
ChEMBL Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors. B 8.22 pKi 6 nM Ki US-8598119-B2. Methods and compositions for sleep disorders and other disorders (2013)
α1A-adrenoceptor/Alpha-1a adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL319] [GtoPdb: 22] [UniProtKB: P43140]
ChEMBL Displacement of [3H]prazosin from rat adrenergic alpha1A receptor expressed in fibroblast cells B 9.3 pKi 0.5 nM Ki Bioorg Med Chem Lett (2008) 18: 489-493 [PMID:18160289]
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 6.48 pKi 330 nM Ki J Med Chem (2004) 47: 1303-1314 [PMID:14998318]
ChEMBL Binding affinity to human cloned dopamine D1 receptor B 6.89 pKi 130 nM Ki Bioorg Med Chem (2008) 16: 7291-7301 [PMID:18595716]
ChEMBL Binding affinity against dopamine receptor D1 B 8.02 pKi 9.5 nM Ki J Med Chem (2001) 44: 477-501 [PMID:11170639]
D2 receptor/Dopamine D2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
ChEMBL Displacement of [3H]spiperone from human dopamine D2 receptor short form expressed in CHO cells B 7.9 pKi 12.59 nM Ki J Med Chem (2007) 50: 5103-5108 [PMID:17880057]
ChEMBL Binding affinity towards human Dopamine receptor D2 B 8.01 pKi 9.7 nM Ki J Med Chem (2004) 47: 1303-1314 [PMID:14998318]
ChEMBL Displacement of [3H]methylspiperone from human low affinity Dopamine D2S receptor by competition binding assay B 8.07 pKi 8.5 nM Ki J Med Chem (2012) 55: 9735-9750 [PMID:23043306]
ChEMBL Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors. B 8.3 pKi 5 nM Ki US-8598119-B2. Methods and compositions for sleep disorders and other disorders (2013)
ChEMBL Displacement of [3H]spiperone from human D2L receptor expressed in CHO cells B 8.3 pKi 5 nM Ki Bioorg Med Chem Lett (2008) 18: 489-493 [PMID:18160289]
ChEMBL Binding affinity to dopamine D2 receptor (unknown origin) by radioligand binding assay B 8.32 pKi 4.8 nM Ki J Med Chem (2013) 56: 8955-8971 [PMID:23919353]
ChEMBL Binding affinity to human cloned dopamine D2 receptor B 8.51 pKi 3.1 nM Ki Bioorg Med Chem (2008) 16: 7291-7301 [PMID:18595716]
GtoPdb - - 8.55 pKi 2.8 nM Ki Neuropsychopharmacology (1998) 18: 63-101 [PMID:9430133]
ChEMBL Binding affinity towards human D2 dopamine receptor. B 8.55 pKi 2.8 nM Ki J Med Chem (2001) 44: 477-501 [PMID:11170639]
ChEMBL Displacement of [3H]-raclopride from human D2R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis B 8.68 pKi 2.1 nM Ki Eur J Med Chem (2020) 185: 111857-111857 [PMID:31734022]
ChEMBL Displacement of [3H]-Raclopride from D2L receptor (unknown origin) B 8.68 pKi 2.1 nM Ki ACS Med Chem Lett (2017) 8: 390-394 [PMID:28435524]
ChEMBL Displacement of [3H] raclopride from human recombinant D2L receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting method B 9.05 pKi 0.9 nM Ki Eur J Med Chem (2019) 170: 261-275 [PMID:30904783]
ChEMBL Displacement of [3H]-methylspiperone from human D2 long receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method B 9.05 pKi 0.9 nM Ki Eur J Med Chem (2019) 179: 1-15 [PMID:31229883]
ChEMBL Displacement of [3H]-methylspiperone from human D2 long receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method B 9.07 pKi 0.85 nM Ki Eur J Med Chem (2019) 179: 1-15 [PMID:31229883]
ChEMBL Displacement of [3H]-raclopride from human D2LR expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method B 9.1 pKi 0.8 nM Ki Eur J Med Chem (2018) 145: 790-804 [PMID:29407591]
ChEMBL Inhibitory concentration against dopamine receptor D2 B 8.3 pIC50 5 nM IC50 J Med Chem (2005) 48: 6523-6543 [PMID:16220969]
D2 receptor/Dopamine D2 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL339] [GtoPdb: 215] [UniProtKB: P61169]
ChEMBL Displacement of [3H]NPA from rat brain Dopamine receptor D2 B 8.32 pKi 4.8 nM Ki J Med Chem (1996) 39: 143-148 [PMID:8568801]
ChEMBL Displacement of [3H]NPA from rat brain Dopamine receptor D2 B 8.32 pKi 4.79 nM Ki J Med Chem (1996) 39: 143-148 [PMID:8568801]
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 pKi 10 nM Ki J Med Chem (2001) 44: 477-501 [PMID:11170639]
ChEMBL Binding affinity towards human Dopamine receptor D3 B 8.12 pKi 7.5 nM Ki J Med Chem (2004) 47: 1303-1314 [PMID:14998318]
ChEMBL Binding affinity to human cloned dopamine D3 receptor B 8.14 pKi 7.2 nM Ki Bioorg Med Chem (2008) 16: 7291-7301 [PMID:18595716]
ChEMBL Binding affinity to dopamine D3 receptor (unknown origin) by radioligand binding assay B 8.14 pKi 7.2 nM Ki J Med Chem (2013) 56: 8955-8971 [PMID:23919353]
ChEMBL Displacement of [3H]spiperone from human dopamine D3 receptor expressed in CHO cells B 8.2 pKi 6.31 nM Ki J Med Chem (2007) 50: 5103-5108 [PMID:17880057]
D4 receptor/Dopamine D4 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL219] [GtoPdb: 217] [UniProtKB: P21917]
ChEMBL Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells B 7.3 pKi 50.12 nM Ki J Med Chem (2007) 50: 5103-5108 [PMID:17880057]
ChEMBL Binding affinity towards human dopamine-4.2 receptor B 7.41 pKi 39 nM Ki J Med Chem (2004) 47: 1303-1314 [PMID:14998318]
ChEMBL Binding affinity towards human dopamine receptor D4 B 7.41 pKi 39 nM Ki J Med Chem (2001) 44: 477-501 [PMID:11170639]
ChEMBL Binding affinity to human cloned dopamine D4 receptor B 7.49 pKi 32 nM Ki Bioorg Med Chem (2008) 16: 7291-7301 [PMID:18595716]
Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809]
ChEMBL Inhibition of human ERG B 6 pIC50 <1000 nM IC50 Bioorg Med Chem Lett (2010) 20: 7312-7316 [PMID:21055935]
ChEMBL K+ channel blocking activity in human embryonic kidney cells expressing HERG Kv11.1 F 6.82 pIC50 152 nM IC50 J Med Chem (2002) 45: 3844-3853 [PMID:12190308]
ChEMBL Inhibition of human ERG in MCF7 cells B 6.82 pIC50 151.36 nM IC50 Eur J Med Chem (2009) 44: 1926-1932 [PMID:19110341]
ChEMBL Inhibition of partially open human voltage-gated potassium channel subunit Kv11.1 (ERG K+ channel) F 6.82 pIC50 151.36 nM IC50 Bioorg Med Chem Lett (2005) 15: 1737-1741 [PMID:15745831]
ChEMBL Inhibition of human ERG B 6.9 pIC50 125.89 nM IC50 Eur J Med Chem (2011) 46: 618-630 [PMID:21185626]
ChEMBL Inhibition of human ERG channel B 6.9 pIC50 125 nM IC50 J Med Chem (2009) 52: 4266-4276 [PMID:19534531]
ChEMBL Inhibition of human ERG channel B 6.9 pIC50 125 nM IC50 J Med Chem (2009) 52: 4266-4276 [PMID:19534531]
ChEMBL Inhibition of human ERG expressed in CHO cells by whole cell patch clamp technique B 6.92 pIC50 120.23 nM IC50 Bioorg Med Chem (2008) 16: 6252-6260 [PMID:18448342]
ChEMBL Inhibitory concentration against potassium channel HERG B 6.92 pIC50 120.23 nM IC50 Bioorg Med Chem Lett (2005) 15: 2886-2890 [PMID:15911273]
H1 receptor/Histamine H1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL231] [GtoPdb: 262] [UniProtKB: P35367]
ChEMBL Binding affinity towards human H1 receptor B 6.29 pKi 510 nM Ki J Med Chem (2001) 44: 477-501 [PMID:11170639]
ChEMBL Binding affinity to H1 histamine receptor (unknown origin) B 7.3 pKi 50 nM Ki Bioorg Med Chem Lett (2021) 31: 127681-127681 [PMID:33189775]
ChEMBL Binding affinity to human cloned histamine H1 receptor B 7.33 pKi 47 nM Ki Bioorg Med Chem (2008) 16: 7291-7301 [PMID:18595716]
GtoPdb - - 7.8 pKi - - - Psychopharmacology (Berl.) (1996) 124: 57-73 [PMID:8935801];
Neuropsychopharmacology (2003) 28: 519-26 [PMID:12629531]
ChEMBL Binding affinity towards human histamine H1 receptor B 8.28 pKi 5.3 nM Ki J Med Chem (2004) 47: 1303-1314 [PMID:14998318]
H1 receptor/Histamine H1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4701] [GtoPdb: 262] [UniProtKB: P31390]
ChEMBL Displacement of [3H]mepyramine from H1R in rat brain B 6.82 pIC50 150 nM IC50 Proc Natl Acad Sci U S A (2007) 104: 3456-3459 [PMID:17360666]
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 7.8 pKi 15.85 nM Ki J Med Chem (2007) 50: 5103-5108 [PMID:17880057]
Histone H1.0 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3707465] [UniProtKB: P07305]
ChEMBL Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors. B 7.82 pKi 15 nM Ki US-8598119-B2. Methods and compositions for sleep disorders and other disorders (2013)
M1 receptor/Muscarinic acetylcholine receptor M1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL216] [GtoPdb: 13] [UniProtKB: P11229]
ChEMBL Binding affinity towards human M1 receptor. B 5 pKi >10000 nM Ki J Med Chem (2001) 44: 477-501 [PMID:11170639]
ChEMBL Binding affinity to human cloned muscarinic M1 receptor B 5.29 pKi 5100 nM Ki Bioorg Med Chem (2008) 16: 7291-7301 [PMID:18595716]
5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908]
ChEMBL Binding affinity towards human 5-hydroxytryptamine 1 receptor B 7.43 pKi 37 nM Ki J Med Chem (2001) 44: 477-501 [PMID:11170639]
ChEMBL Displacement of [3H]8OHDPAT from human 5HT1A receptor B 8.4 pKi 4 nM Ki Bioorg Med Chem Lett (2008) 18: 489-493 [PMID:18160289]
ChEMBL Binding affinity to human cloned 5HT1A receptor B 8.6 pKi 2.5 nM Ki Bioorg Med Chem (2008) 16: 7291-7301 [PMID:18595716]
ChEMBL Displacement of [3H]-8-OH-DPAT from human 5-HT1AR expressed in HEK293 cell membranes after 1 hr by microbeta counting method B 8.7 pKi 2 nM Ki Eur J Med Chem (2018) 145: 790-804 [PMID:29407591]
ChEMBL Displacement of [3H]8-OH-DPAT from human 5HT1A receptor expressed in CHO cells B 8.8 pKi 1.58 nM Ki J Med Chem (2007) 50: 5103-5108 [PMID:17880057]
GtoPdb - - 8.9 pKi - - - Eur J Pharmacol (1998) 355: 245-56 [PMID:9760039];
Psychopharmacology (Berl.) (1996) 124: 57-73 [PMID:8935801]
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 5-HT2AR expressed in CHO-K1 cell membranes after 1.5 hrs by microbeta counting method B 8.77 pKi 1.7 nM Ki Eur J Med Chem (2018) 145: 790-804 [PMID:29407591]
ChEMBL Displacement of [3H]ketanserin from human 5HT2A receptor expressed in CHO cells B 9.2 pKi 0.63 nM Ki J Med Chem (2007) 50: 5103-5108 [PMID:17880057]
ChEMBL Binding affinity to 5HT2A receptor (unknown origin) by radioligand binding assay B 9.4 pKi 0.4 nM Ki J Med Chem (2013) 56: 8955-8971 [PMID:23919353]
ChEMBL Binding affinity to human cloned 5HT2A receptor B 9.41 pKi 0.39 nM Ki Bioorg Med Chem (2008) 16: 7291-7301 [PMID:18595716]
GtoPdb - - 9.51 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];
J Psychopharmacol (Oxford) (2009) 23: 65-73 [PMID:18308814]
ChEMBL Binding affinity towards human serotonin 5-hydroxytryptamine 2A receptor B 9.52 pKi 0.3 nM Ki J Med Chem (2004) 47: 1303-1314 [PMID:14998318]
ChEMBL Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors. B 9.55 pKi 0.28 nM Ki US-8598119-B2. Methods and compositions for sleep disorders and other disorders (2013)
ChEMBL Binding affinity for human 5-hydroxytryptamine 2A receptor B 9.6 pKi 0.25 nM Ki J Med Chem (2001) 44: 477-501 [PMID:11170639]
ChEMBL Displacement of [3H]ketanserin from human 5HT2A receptor expressed in Swiss 3T3 cells B 10.1 pKi 0.08 nM Ki Bioorg Med Chem Lett (2008) 18: 489-493 [PMID:18160289]
ChEMBL Inhibitory concentration against 5-hydroxytryptamine 2 receptor B 9.38 pIC50 0.42 nM IC50 J Med Chem (2005) 48: 6523-6543 [PMID:16220969]
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 from rat brain 5-hydroxytryptamine 2A receptor B 9.38 pKi 0.42 nM Ki J Med Chem (1996) 39: 143-148 [PMID:8568801]
5-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595]
ChEMBL Displacement of [3H]LSD from 5HT2B receptor expressed in CHO cells B 8.8 pKi 1.58 nM Ki J Med Chem (2007) 50: 5103-5108 [PMID:17880057]
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 7.89 pKi 13 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 7.89 pKi 13 nM Ki Bioorg Med Chem Lett (2010) 20: 5431-5433 [PMID:20719507]
ChEMBL Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors. B 8 pKi 10 nM Ki US-8598119-B2. Methods and compositions for sleep disorders and other disorders (2013)
ChEMBL Binding affinity to 5HT2C receptor (unknown origin) by radioligand binding assay B 8.89 pKi 1.3 nM Ki J Med Chem (2013) 56: 8955-8971 [PMID:23919353]
ChEMBL Displacement of [3H]mesulergine from 5HT2C receptor expressed in CHO cells B 8.9 pKi 1.26 nM Ki J Med Chem (2007) 50: 5103-5108 [PMID:17880057]
GtoPdb - - 9.01 pKi - - - Neuropsychopharmacology (2003) 28: 519-26 [PMID:12629531];
J Pharmacol Exp Ther (2000) 295: 226-32 [PMID:10991983];
J Psychopharmacol (Oxford) (2009) 23: 65-73 [PMID:18308814]
ChEMBL Binding affinity to human cloned 5HT2C receptor B 9.14 pKi 0.72 nM Ki Bioorg Med Chem (2008) 16: 7291-7301 [PMID:18595716]
ChEMBL Binding affinity towards human 5-hydroxytryptamine 2C receptor B 9.26 pKi 0.55 nM Ki J Med Chem (2001) 44: 477-501 [PMID:11170639]
5-HT3E/5-HT3B/5-HT3A/5-HT3D/5-HT3C/Serotonin 3 (5-HT3) receptor in Human (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL2094132] [GtoPdb: 377, 374, 373, 376, 375] [UniProtKB: A5X5Y0, O95264, P46098, Q70Z44, Q8WXA8]
ChEMBL Displacement of [3H]BLR-43694 from human 5HT3 receptor expressed in HEK293 cells B 6.4 pKi 398.11 nM Ki J Med Chem (2007) 50: 5103-5108 [PMID:17880057]
5-HT6 receptor/Serotonin 6 (5-HT6) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3371] [GtoPdb: 11] [UniProtKB: P50406]
ChEMBL Binding affinity to human cloned 5HT6 receptor B 7.12 pKi 76 nM Ki Bioorg Med Chem (2008) 16: 7291-7301 [PMID:18595716]
ChEMBL Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells B 7.2 pKi 63.1 nM Ki J Med Chem (2007) 50: 5103-5108 [PMID:17880057]
ChEMBL Displacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cells B 7.21 pKi 61 nM Ki Bioorg Med Chem Lett (2010) 20: 5431-5433 [PMID:20719507]
ChEMBL Binding affinity to 5HT6 receptor (unknown origin) by radioligand binding assay B 7.21 pKi 61 nM Ki J Med Chem (2013) 56: 8955-8971 [PMID:23919353]
ChEMBL Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method B 7.7 pKi 20 nM Ki Eur J Med Chem (2018) 145: 790-804 [PMID:29407591]
5-HT7 receptor/Serotonin 7 (5-HT7) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3155] [GtoPdb: 12] [UniProtKB: P34969]
ChEMBL Binding affinity to 5HT7 receptor (unknown origin) by radioligand binding assay B 8.22 pKi 6 nM Ki J Med Chem (2013) 56: 8955-8971 [PMID:23919353]
ChEMBL Displacement of [3H]LSD from human 5HT7 receptor expressed in CHO cells B 8.3 pKi 5.01 nM Ki J Med Chem (2007) 50: 5103-5108 [PMID:17880057]
ChEMBL Displacement of [3H]-5-CT from human 5-HT7R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method B 8.3 pKi 5 nM Ki Eur J Med Chem (2018) 145: 790-804 [PMID:29407591]
GtoPdb - - 8.4 pKi - - - Psychopharmacology (Berl.) (2005) 179: 461-9 [PMID:15821958]
SERT/Serotonin transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL228] [GtoPdb: 928] [UniProtKB: P31645]
ChEMBL Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors. B 6 pKi >1000 nM Ki US-8598119-B2. Methods and compositions for sleep disorders and other disorders (2013)
ChEMBL Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors. B 6.95 pKi 112 nM Ki US-8598119-B2. Methods and compositions for sleep disorders and other disorders (2013)
ChEMBL Displacement of [3H]paraxetine from human 5HT transporter expressed in HEK293 cells B 7.1 pKi 79.43 nM Ki J Med Chem (2007) 50: 5103-5108 [PMID:17880057]
ChEMBL Binding affinity to human SERT B 7.28 pKi 53 nM Ki Bioorg Med Chem (2008) 16: 7291-7301 [PMID:18595716]
GtoPdb - - 7.28 pKi 53 nM Ki
Transporter in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6184] [UniProtKB: Q63380]
ChEMBL Binding affinity to rat NET B 7.32 pKi 48 nM Ki Bioorg Med Chem (2008) 16: 7291-7301 [PMID:18595716]
5-HT1B receptor in Human [GtoPdb: 2] [UniProtKB: P28222]
GtoPdb - - 8.3 pKi - - - Psychopharmacology (Berl.) (1996) 124: 57-73 [PMID:8935801]
5-HT1D receptor in Human [GtoPdb: 3] [UniProtKB: P28221]
GtoPdb - - 9 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]
NET in Rat [GtoPdb: 926]
GtoPdb - - 7.32 pKi 48 nM Ki Bioorg Med Chem (2008) 16: 7291-301 [PMID:18595716]

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]