Doramapimod

Description	Doramapimod, also known as BIRB-796, is a member of the N-pyrazole-N'-naphthly urea class of p38MAPK inhibitors, which binds to the kinase with both slow association and dissociation rates. BIRB 796 shows no significant inhibition to ERK-1, SYK, IKK2β, ZAP-70, EGF receptor kinase, HER2, protein kinase A (PKA), PKC, PKC-α, PKC-β (I and II) and PKC-γ. BIRB 796 greatly improves binding affinity by forming a hydrogen bond between the morpholine oxygen and the ATP-binding domain of p38α. BIRB 796 represents one of the most potent and slowest dissociating inhibitors against human p38 MAP kinase now known.BIRB 796 potently inhibits c-Raf-1 and Jnk2α2 with IC50 of 1.4 and 0.1 nM, respectively.BIRB796 also inhibits the activity and the activation of SAPK3/p38γ at a higher concentration than it does in p38α.
Pathways	MAPK Pathway
Targets	p38 MAPK Raf

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