Target family: Kelch-like proteins (type: other_protein)
Target: kelch like ECH-associated protein 1

Ligand: compound 10 [PMID: 31411465] (Synthetic organic)
Interaction type: None
Action: Binding
Ligand approved: no
Primary target: no
Median affinity: 7.71999979019165 pKd
Reference (Journal): A Comparative Assessment Study of Known Small-Molecule Keap1-Nrf2 Protein-Protein Interaction Inhibitors: Chemical Synthesis, Binding Properties, and Cellular Activity.
Published in: J Med Chem

Ligand: CPUY192018 (Synthetic organic)
Interaction type: None
Action: Binding
Ligand approved: no
Primary target: no
Median affinity: 7.400000095367432 pKd
Reference (Journal): An inhibitor of the Keap1-Nrf2 protein-protein interaction protects NCM460 colonic cells and alleviates experimental colitis.
Published in: Sci Rep

Ligand: CPUY192018 (Synthetic organic)
Interaction type: None
Action: Binding
Ligand approved: no
Primary target: no
Median affinity: 7.539999961853027 pEC50
Reference (Journal): Discovery of potent Keap1-Nrf2 protein-protein interaction inhibitor based on molecular binding determinants analysis.
Published in: J Med Chem

Ligand: CPUY192018 (Synthetic organic)
Interaction type: None
Action: Binding
Ligand approved: no
Primary target: no
Median affinity: 8.4399995803833 pKd
Reference (Journal): Discovery of potent Keap1-Nrf2 protein-protein interaction inhibitor based on molecular binding determinants analysis.
Published in: J Med Chem

Ligand: CPUY192018 (Synthetic organic)
Interaction type: None
Action: Binding
Ligand approved: no
Primary target: no
Median affinity: 7.840000152587891 pIC50
Reference (Journal): Structure-Activity and Structure-Property Relationship and Exploratory in Vivo Evaluation of the Nanomolar Keap1-Nrf2 Protein-Protein Interaction Inhibitor.
Published in: J Med Chem

Ligand: isoquinoline 17 [PMID: 30122040] (Synthetic organic)
Interaction type: None
Action: Binding
Ligand approved: no
Primary target: no
Median affinity: 7.21999979019165 pIC50
Reference (Journal): Replacement of a Naphthalene Scaffold in Kelch-like ECH-Associated Protein 1 (KEAP1)/Nuclear Factor (Erythroid-derived 2)-like 2 (NRF2) Inhibitors.
Published in: J Med Chem

Ligand: isoquinoline 17 [PMID: 30122040] (Synthetic organic)
Interaction type: None
Action: Binding
Ligand approved: no
Primary target: no
Median affinity: 6.989999771118164 pKd
Reference (Journal): Replacement of a Naphthalene Scaffold in Kelch-like ECH-Associated Protein 1 (KEAP1)/Nuclear Factor (Erythroid-derived 2)-like 2 (NRF2) Inhibitors.
Published in: J Med Chem

Ligand: Nrf2 peptide [PMID: 23647822] (Peptide)
Interaction type: Inhibitor
Action: Binding
Ligand approved: no
Primary target: yes
Median affinity: 7.480000019073486 pIC50
Reference (Journal): Small molecules inhibit the interaction of Nrf2 and the Keap1 Kelch domain through a non-covalent mechanism.
Published in: Bioorg Med Chem

Ligand: RA839 (Synthetic organic)
Interaction type: None
Action: Binding
Ligand approved: no
Primary target: no
Median affinity: 5.21999979019165 pKd
Reference (Journal): Characterization of RA839, a Noncovalent Small Molecule Binder to Keap1 and Selective Activator of Nrf2 Signaling.
Published in: J Biol Chem

Ligand: RA839 (Synthetic organic)
Interaction type: None
Action: Binding
Ligand approved: no
Primary target: no
Median affinity: 6.849999904632568 pIC50
Reference (Journal): Characterization of RA839, a Noncovalent Small Molecule Binder to Keap1 and Selective Activator of Nrf2 Signaling.
Published in: J Biol Chem

Ligand: bardoxolone (Synthetic organic)
Interaction type: None
Action: Binding
Ligand approved: no
Primary target: no
Median affinity: 7 pIC50
Reference (Journal): Structure of the BTB domain of Keap1 and its interaction with the triterpenoid antagonist CDDO.
Published in: PLoS ONE

Ligand: biKEAP1 (Synthetic organic)
Interaction type: Inhibitor
Action: Binding
Ligand approved: no
Primary target: no
Median affinity: 8.069999694824219 pIC50
Reference (Journal): Bivalent inhibitors of the BTB E3 ligase KEAP1 enable instant NRF2 activation to suppress acute inflammatory response.
Published in: Cell Chem Biol