Target Poor or Non Binder(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T72491 | Target Info | |||
| Target Name | Keap1-Nrf2[dual DLG and ETGE] PPI (KEAP1-Nrf2 DLG and ETGE) | ||||
| Synonyms |
Kelch-like protein 19-Nrf2[dual DLG and ETGE]; Kelch-like ECH-associated protein 1-Nrf2[dual DLG and ETGE]; KLHL19-Nrf2[dual DLG and ETGE]; KIAA0132-Nrf2[dual DLG and ETGE]; INrf2-Nrf2[dual DLG and ETGE]; Cytosolic inhibitor of Nrf2-Nrf2[dual DLG and ETGE]
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| Target Type | Patented-recorded Target | ||||
| Gene Name | KEAP1-NFE2L2 | ||||
| UniProt ID | |||||
| Poor Binders of This Target (in total, 6 binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
Chembl4165400
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Investigative | Compound Info | ||
| Synonyms |
BDBM50321304
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| Activity |
IC50 = 69700 nM
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[1] | |||
| Compound Name |
(1R,2S)-2-[(1R)-1-[(1,3-Dioxoisoindol-2-yl)methyl]-3,4-dihydro-1H-isoquinoline-2-carbonyl]cyclohexane-1-carboxylic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL2381969; BDBM50491279; BRD-K74320884-001-01-7; BRD-K74320884-001-02-5
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| Activity |
EC50 ~ 100000 nM
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[2] | |||
| Compound Name |
Chembl4176009
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Investigative | Compound Info | ||
| Synonyms |
BDBM50321303
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| Activity |
IC50 ~ 100000 nM
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[1] | |||
| Compound Name |
2-[[(1S)-2-(Cyclohexanecarbonyl)-3,4-dihydro-1H-isoquinolin-1-yl]methyl]isoindole-1,3-dione
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3186228; SCHEMBL14921399; BDBM50321305; BRD-K90435233-001-01-1
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| Activity |
IC50 ~ 100000 nM
|
[1] | |||
| Compound Name |
(1S,2R)-2-[(1S)-1-[(1,3-Dioxoisoindol-2-yl)methyl]-3,4-dihydro-1H-isoquinoline-2-carbonyl]cyclohexane-1-carboxylic acid
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL2381970; ML 334; SCHEMBL14933965; BDBM50491278
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| Activity |
EC50 ~ 100000 nM
|
[2] | |||
| Compound Name |
2-({5-[(2,4-Dimethylphenyl)sulfonyl]-6-Oxo-1,6-Dihydropyrimidin-2-Yl}sulfanyl)-N-[2-(Trifluoromethyl)phenyl]acetamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL2402206; BDBM50120421; MCULE-8022045809; Q27454740; 4ID
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| Activity |
EC50 = 118000 nM
|
[3] | |||
| Click to Show/Hide the Information of All Poor Binders | |||||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Non-covalent Small-Molecule Kelch-like ECH-Associated Protein 1-Nuclear Factor Erythroid 2-Related Factor 2 (Keap1-Nrf2) Inhibitors and Their Potential for Targeting Central Nervous System Diseases. J Med Chem. 2018 Sep 27;61(18):8088-8103. | ||||
| REF 2 | Discovery of a small-molecule inhibitor and cellular probe of Keap1-Nrf2 protein-protein interaction. Bioorg Med Chem Lett. 2013 May 15;23(10):3039-43. | ||||
| REF 3 | Design, Synthesis, and Evaluation of Triazole Derivatives That Induce Nrf2 Dependent Gene Products and Inhibit the Keap1-Nrf2 Protein-Protein Interaction. J Med Chem. 2015 Sep 24;58(18):7186-94. | ||||
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