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Synonyms: compound 3 [PMID: 31532644] | LY-3154207
Compound class: Synthetic organic
Comment: LY3154207 is a potent, selective and orally active dopamine D1 receptor positive allosteric modulator (PAM) . The allosteric binding site of LY3154207 has been determined to reside at the intracellular loop 2 (ICL2) region of the receptor.
D1 PAMs are being developed to address the poor drug-like properties of selective orthosteric D1 agonists. In particular, LY3154207 does not induce tachyphylaxis in preclinical models, whereas orthosteric agonists do. LY3154207 exhibits pro-cognitive and motor-enhancing effects in vivo, and is being considered for potential utility in the treatment of neuropsychiatric disorders .
Ligand Activity Visualisation Charts
These are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts.✖
|LY3154207 produces minimal agonist activity . In vivo experiments using LY3154207 were carried out in mice engineered to express the human D1 receptor because of the difference in potency that was determined between the human and mouse D1 receptors for LY3154207. The in vitro EC50 potentiator potency of LY3154207 for the human D5 receptor was determined to be >10 μM .|
|Selectivity at GPCRs|
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