Target family: p38 subfamily (type: enzyme)
Target: mitogen-activated protein kinase 14

Ligand: PF-670462 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.71999979019165 pIC50
Reference (Journal): An inhibitor of casein kinase I epsilon induces phase delays in circadian rhythms under free-running and entrained conditions.
Published in: J Pharmacol Exp Ther

Ligand: PF-03715455 (Synthetic organic)
Interaction type: Inhibitor
Action: Binding
Ligand approved: no
Primary target: yes
Median affinity: 12 pKd
Reference (Journal): Design and synthesis of inhaled p38 inhibitors for the treatment of chronic obstructive pulmonary disease.
Published in: J Med Chem

Ligand: PF-03715455 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 9.0600004196167 pIC50
Reference (Journal): Design and synthesis of inhaled p38 inhibitors for the treatment of chronic obstructive pulmonary disease.
Published in: J Med Chem

Ligand: pexmetinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.460000038146973 pIC50
Reference (Journal): Pexmetinib: A Novel Dual Inhibitor of Tie2 and p38 MAPK with Efficacy in Preclinical Models of Myelodysplastic Syndromes and Acute Myeloid Leukemia.
Published in: Cancer Res

Ligand: pamapimod (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 8.890000343322754 pKd
Reference (Journal): Discovery of 6-(2,4-difluorophenoxy)-2-[3-hydroxy-1-(2-hydroxyethyl)propylamino]-8-methyl-8H-pyrido[2,3-d]pyrimidin-7-one (pamapimod) and 6-(2,4-difluorophenoxy)-8-methyl-2-(tetrahydro-2H-pyran-4-ylamino)pyrido[2,3-d]pyrimidin-7(8H)-one (R1487) as orally bioavailable and highly selective inhibitors of p38α mitogen-activated protein kinase.
Published in: J Med Chem

Ligand: neflamapimod (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 8 pIC50
Reference (Journal): A quantitative analysis of kinase inhibitor selectivity.
Published in: Nat Biotechnol

Ligand: NDPPC (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7 pIC50

Ligand: MW150 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 7 pKi
Reference (Patent): Map kinase modulators and uses thereof.

Ligand: MW150 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 7 pKi
Reference (Journal): Targeting human central nervous system protein kinases: An isoform selective p38αMAPK inhibitor that attenuates disease progression in Alzheimer's disease mouse models.
Published in: ACS Chem Neurosci

Ligand: MAPK13-IN-1 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 5.440000057220459 pIC50
Reference (Journal): IL-13-induced airway mucus production is attenuated by MAPK13 inhibition.
Published in: J Clin Invest

Ligand: losmapimod (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 8.100000381469727 pKi
Reference (Journal): p38alpha mitogen-activated protein kinase inhibitors: optimization of a series of biphenylamides to give a molecule suitable for clinical progression.
Published in: J Med Chem

Ligand: doramapimod (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 9.350000381469727 pKd
Reference (Journal): Comprehensive analysis of kinase inhibitor selectivity.
Published in: Nat Biotechnol

Ligand: doramapimod (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 7.699999809265137 pIC50
Reference (Journal): Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD).
Published in: Bioorg Med Chem Lett

Ligand: dilmapimod (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 5 pIC50
Reference (Patent): Novel trisubstituted-8H-pyrido[2,3-d]pyrimidin-7-one compound for the treatment of CSBP/p38 kinase mediated diseases.

Ligand: compound 4e [PMID: 35546685] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 10 pIC50
Reference (Journal): Design, Synthesis, and Biological Characterization of Inhaled p38α/β MAPK Inhibitors for the Treatment of Lung Inflammatory Diseases.
Published in: J Med Chem

Ligand: compound 12 [PMID: 22521646] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 9.1899995803833 pIC50
Reference (Journal): Novel triazolopyridylbenzamides as potent and selective p38α inhibitors.
Published in: Bioorg Med Chem Lett

Ligand: CBS-3595 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.300000190734863 pIC50
Reference (Journal): Discovery of N-{4-[5-(4-Fluorophenyl)-3-methyl-2-methylsulfanyl-3H-imidazol-4-yl]-pyridin-2-yl}-acetamide (CBS-3595), a Dual p38α MAPK/PDE-4 Inhibitor with Activity against TNFα-Related Diseases.
Published in: J Med Chem

Ligand: BMS-582949 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 7.889999866485596 pIC50
Reference (Journal): Discovery of 4-(5-(cyclopropylcarbamoyl)-2-methylphenylamino)-5-methyl-N-propylpyrrolo[1,2-f][1,2,4]triazine-6-carboxamide (BMS-582949), a clinical p38α MAP kinase inhibitor for the treatment of inflammatory diseases.
Published in: J Med Chem

Ligand: AZD7624 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 10 pIC50
Reference (Patent): Pyrazinone derivatives and their use in the treatment of lung diseases

Ligand: AZD6703 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 7.809999942779541 pIC50
Reference (Journal): The discovery of N-cyclopropyl-4-methyl-3-[6-(4-methylpiperazin-1-yl)-4-oxoquinazolin-3(4H)-yl]benzamide (AZD6703), a clinical p38α MAP kinase inhibitor for the treatment of inflammatory diseases.
Published in: Bioorg Med Chem Lett

Ligand: ARRY-371797 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.350000381469727 pIC50
Reference (Journal): Selective p38alpha inhibitors clinically evaluated for the treatment of chronic inflammatory disorders.
Published in: J Med Chem

Ligand: acumapimod (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6 pIC50
Reference (Patent): 5-membered heterocycle-based p38 kinase inhibitors

Ligand: 7-hydroxystaurosporine (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 7.019999980926514 pIC50
Reference (Journal): p53-deficient cells rely on ATM- and ATR-mediated checkpoint signaling through the p38MAPK/MK2 pathway for survival after DNA damage.
Published in: Cancer Cell