sonepiprazole [Ligand Id: 980] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL69759 (Sonepiprazol, Sonepiprazole, U-101387)
  • α2A-adrenoceptor/Alpha-2a adrenergic receptor in Human [ChEMBL: CHEMBL1867] [GtoPdb: 25] [UniProtKB: P08913]
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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]
  • D3 receptor/Dopamine D3 receptor in Rat [ChEMBL: CHEMBL3138] [GtoPdb: 216] [UniProtKB: P19020]
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  • D4 receptor/Dopamine D4 receptor in Human [ChEMBL: CHEMBL219] [GtoPdb: 217] [UniProtKB: P21917]
  • D4 receptor/Dopamine D4 receptor in Rat [ChEMBL: CHEMBL3361] [GtoPdb: 217] [UniProtKB: P30729]
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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]
  • 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Rat [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327]
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  • 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
α2A-adrenoceptor/Alpha-2a adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1867] [GtoPdb: 25] [UniProtKB: P08913]
ChEMBL Inhibition of alpha2A adrenergic receptor (unknown origin) B 5.8 pKi >1600 nM Ki J Med Chem (2017) 60: 7233-7243 [PMID:28489950]
D1 receptor/Dopamine D1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2056] [GtoPdb: 214] [UniProtKB: P21728]
ChEMBL Inhibition of human dopamine D1 receptor B 5.08 pKi >8378 nM Ki J Med Chem (2017) 60: 7233-7243 [PMID:28489950]
D2 receptor/Dopamine D2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
ChEMBL Inhibition of human dopamine D2 receptor B 5.29 pKi 5147 nM Ki J Med Chem (2017) 60: 7233-7243 [PMID:28489950]
D2 receptor/Dopamine D2 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL339] [GtoPdb: 215] [UniProtKB: P61169]
ChEMBL Binding affinity of [3H]U-86170 towards Dopamine receptor D2 in cloned mammalian receptor expressed in cultured cells or from rat whole brain B 5.37 pKi >4300 nM Ki J Med Chem (1996) 39: 2435-2437 [PMID:8691438]
D3 receptor/Dopamine D3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462]
ChEMBL Inhibition of human dopamine D3 receptor B 5.56 pKi >2778 nM Ki J Med Chem (2017) 60: 7233-7243 [PMID:28489950]
D3 receptor/Dopamine D3 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3138] [GtoPdb: 216] [UniProtKB: P19020]
ChEMBL Binding affinity of [3H]spiperone towards Dopamine receptor D3 in cloned mammalian receptor expressed in cultured cells or from rat whole brain. B 5.24 pKi 5800 nM Ki J Med Chem (1996) 39: 2435-2437 [PMID:8691438]
D4 receptor/Dopamine D4 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL219] [GtoPdb: 217] [UniProtKB: P21917]
ChEMBL Binding affinity towards human dopamine receptor D4 B 8.17 pKi 6.8 nM Ki J Med Chem (2001) 44: 477-501 [PMID:11170639]
ChEMBL Inhibition of human dopamine D4 receptor B 8.44 pKi 3.6 nM Ki J Med Chem (2017) 60: 7233-7243 [PMID:28489950]
GtoPdb - - 8.9 pKi 1.4 nM Ki Eur J Pharmacol (1997) 322: 283-6 [PMID:9098699]
D4 receptor/Dopamine D4 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3361] [GtoPdb: 217] [UniProtKB: P30729]
ChEMBL Binding affinity of [3H]spiperone towards Dopamine receptor D4 expressed in cultured cells or from rat whole brain. B 8.14 pKi 7.2 nM Ki J Med Chem (1996) 39: 2435-2437 [PMID:8691438]
GtoPdb - - 8.7 pKi - - - Mol Pharmacol (2004) 66: 1491-9 [PMID:15448188]
H1 receptor/Histamine H1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL231] [GtoPdb: 262] [UniProtKB: P35367]
ChEMBL Inhibition of histamine H1 receptor (unknown origin) B 5.8 pKi >1600 nM Ki J Med Chem (2017) 60: 7233-7243 [PMID:28489950]
5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908]
ChEMBL Inhibition of serotonin 5-HT1A receptor (unknown origin) B 5.8 pKi >1600 nM Ki J Med Chem (2017) 60: 7233-7243 [PMID:28489950]
5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327]
ChEMBL Binding affinity of [3H]-8-OH-DPAT towards 5-hydroxytryptamine 1A receptor in cloned mammalian receptor expressed in cultured cells or from rat whole brain. B 5.43 pKi >3700 nM Ki J Med Chem (1996) 39: 2435-2437 [PMID:8691438]
5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223]
ChEMBL Inhibition of serotonin 5-HT2 receptor (unknown origin) B 5.8 pKi >1600 nM Ki J Med Chem (2017) 60: 7233-7243 [PMID:28489950]

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]