Target family: ERK subfamily (type: enzyme)
Target: mitogen-activated protein kinase 1

Ligand: ASTX029 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.569999694824219 pIC50
Reference (Journal): Discovery of ASTX029, A Clinical Candidate Which Modulates the Phosphorylation and Catalytic Activity of ERK1/2.
Published in: J Med Chem

Ligand: compound 27 [PMID: 29775310] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.520000457763672 pIC50
Reference (Journal): Fragment-Based Discovery of a Potent, Orally Bioavailable Inhibitor That Modulates the Phosphorylation and Catalytic Activity of ERK1/2.
Published in: J Med Chem

Ligand: edaxeterkib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.300000190734863 pIC50
Reference (Patent): Inhibitors of erk and methods of use

Ligand: ERK inhibitor II (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 6.849999904632568 pKi
Reference (Journal): Identification of a selective ERK inhibitor and structural determination of the inhibitor-ERK2 complex.
Published in: Biochem Biophys Res Commun

Ligand: ERK inhibitor III (Synthetic organic)
Interaction type: Inhibitor
Action: Binding
Ligand approved: no
Primary target: yes
Median affinity: 4.889999866485596 pKd
Reference (Journal): Characterization of ATP-independent ERK inhibitors identified through in silico analysis of the active ERK2 structure.
Published in: Bioorg Med Chem Lett

Ligand: laduviglusib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 5 pIC50
Reference (Journal): Selective glycogen synthase kinase 3 inhibitors potentiate insulin activation of glucose transport and utilization in vitro and in vivo.
Published in: Diabetes

Ligand: MK-8353 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 8.0600004196167 pIC50
Reference (Journal): Development of MK-8353, an orally administered ERK1/2 inhibitor, in patients with advanced solid tumors.
Published in: JCI Insight

Ligand: ravoxertinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity:  pIC50
Reference (Patent): Serine/threonine kinase inhibitors

Ligand: ravoxertinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity:  pIC50
Reference (Journal): Discovery of (S)-1-(1-(4-Chloro-3-fluorophenyl)-2-hydroxyethyl)-4-(2-((1-methyl-1H-pyrazol-5-yl)amino)pyrimidin-4-yl)pyridin-2(1H)-one (GDC-0994), an Extracellular Signal-Regulated Kinase 1/2 (ERK1/2) Inhibitor in Early Clinical Development.
Published in: J Med Chem

Ligand: rineterkib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 10.579999923706055 pIC50
Reference (Patent): Aminoheteroaryl benzamides as kinase inhibitors

Ligand: SCH772984 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 9 pIC50
Reference (Journal): Discovery of a novel ERK inhibitor with activity in models of acquired resistance to BRAF and MEK inhibitors.
Published in: Cancer Discov

Ligand: SCH772984 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 8.399999618530273 pIC50
Reference (Journal): Discovery of a novel ERK inhibitor with activity in models of acquired resistance to BRAF and MEK inhibitors.
Published in: Cancer Discov

Ligand: tizaterkib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 9.180000305175781 pIC50
Reference (Journal): AZD0364 Is a Potent and Selective ERK1/2 Inhibitor That Enhances Antitumor Activity in <i>KRAS</i>-Mutant Tumor Models when Combined with the MEK Inhibitor, Selumetinib.
Published in: Mol Cancer Ther

Ligand: ulixertinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 9.520000457763672 pIC50
Reference (Journal): Structure-Guided Design of Highly Selective and Potent Covalent Inhibitors of ERK1/2.
Published in: J Med Chem

Ligand: VTX-11e (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 8.699999809265137 pKi
Reference (Journal): Structure-guided design of potent and selective pyrimidylpyrrole inhibitors of extracellular signal-regulated kinase (ERK) using conformational control.
Published in: J Med Chem