Synonyms: compound 2b [PMID: 21375264] | Ro 4402257 | Ro-4402257 | Ro4402257
Compound class:
Synthetic organic
Comment: Pamapimod is an ATP-competitive (Type I), orally bioavailable and highly selective inhibitor of p38α mitogen-activated protein kinase (MAPK14), that was developed for immunomodulatory potential [4].
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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Bioactivity Comments |
Pamapimod exhibits submicromolar binding affinity for only seven out of >300 kinases tested [4]. It binds p38α (MAPK14) and p38β (MAPK11), but not p38γ (MAPK12) or p38δ (MAPK13). Pamapimod potently inhibited cytokine production in a selection of in vitro and in vivo models, including inhibition of TNFα production by human monocytic THP-1 cells, and inhibition of LPS-induced IL-1β production in human whole blood. |
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