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ChEMBL ligand: CHEMBL708 (CP-88059, Geodon, Zipradon, Ziprasidone) |
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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] |
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]