- Advanced search
- Immuno Portal
- Malaria Portal
Synonyms: cobimetinib butyrate | cobimetinib fumarate | cometinib | Cotellic® | GDC-0973 | XL-518 | XL518
cobimetinib is an approved drug (FDA & EMA (2015))
Compound class: Synthetic organic
Comment: Cobimetinib is an allosteric inhibitor of MEK serine/threonine protein kinases, with selectivity for MEK1 and MEK2 .
Note that cobimetinib has been erroneously referred to as cometinib and this has propagated in online resources- cometinib is not an official synonym.
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.✖
View more information in the IUPHAR Pharmacology Education Project: cobimetinib
1. Ascierto PA, Kirkwood JM, Grob JJ, Simeone E, Grimaldi AM, Maio M, Palmieri G, Testori A, Marincola FM, Mozzillo N. (2012)
The role of BRAF V600 mutation in melanoma.
J Transl Med, 10: 85. [PMID:22554099]
2. Davies H, Bignell GR, Cox C, Stephens P, Edkins S, Clegg S, Teague J, Woffendin H, Garnett MJ, Bottomley W et al.. (2002)
Mutations of the BRAF gene in human cancer.
Nature, 417 (6892): 949-54. [PMID:12068308]
3. Rice KD, Aay N, Anand NK, Blazey CM, Bowles OJ, Bussenius J, Costanzo S, Curtis JK, Defina SC, Dubenko L et al.. (2012)
Novel Carboxamide-Based Allosteric MEK Inhibitors: Discovery and Optimization Efforts toward XL518 (GDC-0973).
ACS Med Chem Lett, 3 (5): 416-21. [PMID:24900486]
4. Wan PT, Garnett MJ, Roe SM, Lee S, Niculescu-Duvaz D, Good VM, Jones CM, Marshall CJ, Springer CJ, Barford D et al.. (2004)
Mechanism of activation of the RAF-ERK signaling pathway by oncogenic mutations of B-RAF.
Cell, 116 (6): 855-67. [PMID:15035987]