Synonyms: CI 1040 | CI1040 | PD-184352 | PD184352
Compound class:
Synthetic organic
Comment: CI-1040 is an investigational MEK1/2 inhibitor [1], which acts as a negative allosteric modulator of kinase activity.
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. Davies SP, Reddy H, Caivano M, Cohen P. (2000)
Specificity and mechanism of action of some commonly used protein kinase inhibitors. Biochem J, 351 (Pt 1): 95-105. [PMID:10998351] |
2. Davis MI, Hunt JP, Herrgard S, Ciceri P, Wodicka LM, Pallares G, Hocker M, Treiber DK, Zarrinkar PP. (2011)
Comprehensive analysis of kinase inhibitor selectivity. Nat Biotechnol, 29 (11): 1046-51. [PMID:22037378] |
3. Sebolt-Leopold JS, Dudley DT, Herrera R, Van Becelaere K, Wiland A, Gowan RC, Tecle H, Barrett SD, Bridges A, Przybranowski S et al.. (1999)
Blockade of the MAP kinase pathway suppresses growth of colon tumors in vivo. Nat Med, 5 (7): 810-6. [PMID:10395327] |
4. Wodicka LM, Ciceri P, Davis MI, Hunt JP, Floyd M, Salerno S, Hua XH, Ford JM, Armstrong RC, Zarrinkar PP et al.. (2010)
Activation state-dependent binding of small molecule kinase inhibitors: structural insights from biochemistry. Chem Biol, 17 (11): 1241-9. [PMID:21095574] |