Synonyms: gamma-Secretase Inhibitor IX | GSI-IX | LY-374973
Compound class:
Synthetic organic
Comment: DAPT is a γ-secretase inhibitor [1] that is used experimentally to inhibit NOTCH pathway signalling. Chemically it is a modified di-peptide (IUPAC Condensed name Unk-Ala-Phg-OtBu).
Ligand Activity Visualisation ChartsThese 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. ✖ |
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References |
1. Czerwinski A, Valenzuela F, Afonine P, Dauter M, Dauter Z. (2010)
N-{N-[2-(3,5-Difluorophenyl)acetyl]-(S)-alanyl}-(S)-phenylglycine tert-butyl ester (DAPT): an inhibitor of γ-secretase, revealing fine electronic and hydrogen-bonding features. Acta Crystallogr C, 66 (Pt 12): o585-8. [PMID:21123889] |
2. Dovey HF, John V, Anderson JP, Chen LZ, de Saint Andrieu P, Fang LY, Freedman SB, Folmer B, Goldbach E, Holsztynska EJ et al.. (2001)
Functional gamma-secretase inhibitors reduce beta-amyloid peptide levels in brain. J Neurochem, 76 (1): 173-81. [PMID:11145990] |
3. Iben LG, Olson RE, Balanda LA, Jayachandra S, Robertson BJ, Hay V, Corradi J, Prasad CV, Zaczek R, Albright CF et al.. (2007)
Signal peptide peptidase and gamma-secretase share equivalent inhibitor binding pharmacology. J Biol Chem, 282 (51): 36829-36. [PMID:17932033] |