Synonyms: G-868 | GDC 0623 | GDC0623 | RG-7421 | RG7421
Compound class:
Synthetic organic
Comment: GDC-0623 (RG-7420) is an ATP-uncompetitive MEK1 inhibitor that was developed by Genentech for anti-cancer potential [3]. The structure of GDC-0623 was disclosed for the first time in 'Supplementary Figure 1a' provided with Hatzivassiliou et al. (2013) [2].
![]() 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. Akinleye A, Furqan M, Mukhi N, Ravella P, Liu D. (2013)
MEK and the inhibitors: from bench to bedside. J Hematol Oncol, 6: 27. [PMID:23587417] |
2. Hatzivassiliou G, Haling JR, Chen H, Song K, Price S, Heald R, Hewitt JF, Zak M, Peck A, Orr C et al.. (2013)
Mechanism of MEK inhibition determines efficacy in mutant KRAS- versus BRAF-driven cancers. Nature, 501 (7466): 232-6. [PMID:23934108] |
3. Robarge KD, Lee W, Eigenbrot C, Ultsch M, Wiesmann C, Heald R, Price S, Hewitt J, Jackson P, Savy P et al.. (2014)
Structure based design of novel 6,5 heterobicyclic mitogen-activated protein kinase kinase (MEK) inhibitors leading to the discovery of imidazo[1,5-a] pyrazine G-479. Bioorg Med Chem Lett, 24 (19): 4714-4723. [PMID:25193232] |