flesinoxan [Ligand Id: 1] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1742477 (Flesinoxan)
  • D2 receptor/Dopamine D2 receptor in Rat [ChEMBL: CHEMBL339] [GtoPdb: 215] [UniProtKB: P61169]
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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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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
D2 receptor/Dopamine D2 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL339] [GtoPdb: 215] [UniProtKB: P61169]
ChEMBL In vitro displacement of [3H]spiperone from Dopamine receptor D2 binding site in rat striatum. B 6.85 pKi 140 nM Ki J. Med. Chem. (1997) 40: 300-312 [PMID:9022796]
5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908]
GtoPdb - - 9.3 pKi - - - Eur J Pharmacol (1998) 355: 245-56 [PMID:9760039]
ChEMBL Compound was tested for its potency against human 5-hydroxytryptamine 1A receptor expressed in CHO cells F 8.18 pEC50 6.61 nM EC50 Bioorg. Med. Chem. Lett. (1998) 8: 2457-2462 [PMID:9873561]
5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327]
ChEMBL Binding affinity was evaluated by determining in vitro displacement of [3H]8-OH-DPAT from the central 5-hydroxytryptamine 1A receptor recognition site in rat frontal cortex homogenate. B 8.77 pKi 1.7 nM Ki J. Med. Chem. (1997) 40: 300-312 [PMID:9022796]
ChEMBL Inhibition of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor of rat frontal cortex membranes B 8.77 pKi 1.7 nM Ki Bioorg. Med. Chem. Lett. (1998) 8: 2457-2462 [PMID:9873561]

ChEMBL data shown on this page come from version 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]