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

Click here for a description of the charts and data table

Please tell us if you are using this feature and what you think!

ChEMBL ligand: CHEMBL708 (CP-88059, Geodon, Zipradon, Ziprasidona, 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]
There should be some charts here, you may need to enable JavaScript!
There should be some charts here, you may need to enable JavaScript!
  • D1 receptor/Dopamine D1 receptor in Human [ChEMBL: CHEMBL2056] [GtoPdb: 214] [UniProtKB: P21728]
There should be some charts here, you may need to enable JavaScript!
  • 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]
There should be some charts here, you may need to enable JavaScript!
  • D3 receptor/Dopamine D3 receptor in Human [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462]
There should be some charts here, you may need to enable JavaScript!
  • D4 receptor/Dopamine D4 receptor in Human [ChEMBL: CHEMBL219] [GtoPdb: 217] [UniProtKB: P21917]
There should be some charts here, you may need to enable JavaScript!
There should be some charts here, you may need to enable JavaScript!
  • 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]
There should be some charts here, you may need to enable JavaScript!
  • M1 receptor/Muscarinic acetylcholine receptor M1 in Human [ChEMBL: CHEMBL216] [GtoPdb: 13] [UniProtKB: P11229]
There should be some charts here, you may need to enable JavaScript!
  • 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908]
There should be some charts here, you may need to enable JavaScript!
  • 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]
There should be some charts here, you may need to enable JavaScript!
  • 5-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Human [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595]
There should be some charts here, you may need to enable JavaScript!
  • 5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335]
There should be some charts here, you may need to enable JavaScript!
There should be some charts here, you may need to enable JavaScript!
  • 5-HT6 receptor/Serotonin 6 (5-HT6) receptor in Human [ChEMBL: CHEMBL3371] [GtoPdb: 11] [UniProtKB: P50406]
There should be some charts here, you may need to enable JavaScript!
  • 5-HT7 receptor/Serotonin 7 (5-HT7) receptor in Human [ChEMBL: CHEMBL3155] [GtoPdb: 12] [UniProtKB: P34969]
There should be some charts here, you may need to enable JavaScript!
  • SERT/Serotonin transporter in Human [ChEMBL: CHEMBL228] [GtoPdb: 928] [UniProtKB: P31645]
There should be some charts here, you may need to enable JavaScript!
There should be some charts here, you may need to enable JavaScript!
  • 5-HT1B receptor in Human [GtoPdb: 2] [UniProtKB: P28222]
There should be some charts here, you may need to enable JavaScript!
  • 5-HT1D receptor in Human [GtoPdb: 3] [UniProtKB: P28221]
There should be some charts here, you may need to enable JavaScript!
  • 5-ht1e receptor in Human [GtoPdb: 4] [UniProtKB: P28566]
There should be some charts here, you may need to enable JavaScript!
  • NET in Rat [GtoPdb: 926]
There should be some charts here, you may need to enable JavaScript!
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]
Aspartate aminotransferase, cytoplasmic in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2189139] [UniProtKB: P17174]
ChEMBL Inhibition of GOT1 (unknown origin) B 5.27 pIC50 5390 nM IC50 Bioorg Med Chem Lett (2022) 73: 128883-128883 [PMID:35820623]
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 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)
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]
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 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]