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

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ChEMBL ligand: CHEMBL69759 (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 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]