AS-19 [Ligand Id: 8433] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL2164327
  • 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908]
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  • 5-HT5A receptor/Serotonin 5a (5-HT5a) receptor in Human [ChEMBL: CHEMBL3426] [GtoPdb: 10] [UniProtKB: P47898]
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  • 5-HT7 receptor/Serotonin 7 (5-HT7) receptor in Human [ChEMBL: CHEMBL3155] [GtoPdb: 12] [UniProtKB: P34969]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908]
ChEMBL Displacement of [3H]-5-carboxamidotryptamine from human 5-HT1A receptor expressed in HEK293T cell membranes incubated for 90 mins by scintillation counting method B 6.62 pKi 240 nM Ki Bioorg Med Chem (2020) 28: 115262-115262 [PMID:31882369]
ChEMBL Antagonist activity at 5-HT1A receptor (unknown origin) B 7.05 pKi 89.7 nM Ki Eur J Med Chem (2019) 183: 111705-111705 [PMID:31581003]
ChEMBL Displacement of [3H]8-OH-DPAT from recombinant human 5-HT1A receptor after 60 mins by scintillation counting analysis B 7.05 pKi 89.7 nM Ki Medchemcomm (2018) 9: 1882-1890 [PMID:30568756]
5-HT5A receptor/Serotonin 5a (5-HT5a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3426] [GtoPdb: 10] [UniProtKB: P47898]
ChEMBL Displacement of [3H]LSD from recombinant human 5-HT5a receptor after 120 mins by scintillation counting analysis B 7.01 pKi 98.5 nM Ki Medchemcomm (2018) 9: 1882-1890 [PMID:30568756]
5-HT7 receptor/Serotonin 7 (5-HT7) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3155] [GtoPdb: 12] [UniProtKB: P34969]
ChEMBL Displacement of [3H]-5-carboxamidotryptamine from human 5-HT7A receptor expressed in HEK293 cell membranes incubated for 90 mins by scintillation counting method B 7.92 pKi 12 nM Ki Bioorg Med Chem (2020) 28: 115262-115262 [PMID:31882369]
GtoPdb - - 9.22 pKi 0.6 nM Ki Bioorg Med Chem (2013) 21: 2568-76 [PMID:23541835]
ChEMBL Binding affinity to human 5HT7 receptor expressed in HEK-293F cells B 9.22 pKi 0.6 nM Ki Bioorg Med Chem (2013) 21: 2568-2576 [PMID:23541835]
ChEMBL Binding affinity to 5-HT7 receptor (unknown origin) B 9.22 pKi 0.6 nM Ki J Med Chem (2018) 61: 8475-8503 [PMID:29767995]
ChEMBL Antagonist activity at 5-HT7 receptor (unknown origin) B 9.22 pKi 0.6 nM Ki Eur J Med Chem (2019) 183: 111705-111705 [PMID:31581003]
ChEMBL Displacement of [3H]LSD from human recombinant 5-HT7 receptor after 120 mins by scintillation counting analysis B 9.22 pKi 0.6 nM Ki Medchemcomm (2018) 9: 1882-1890 [PMID:30568756]

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]