Target
Kelch-like ECH-associated protein 1 [321-609]
Ligand
BDBM304755
Substrate
n/a
Meas. Tech.
Nrf2-Keap1 FP Assay #1
IC50
55±n/a nM
Citation
 Davies, TGWoolford, AJWillems, HMNorton, DHeightman, TDKerns, JK Nrf2 regulators US Patent  US10144731 Publication Date 12/4/2018 
Target
Name:
Kelch-like ECH-associated protein 1 [321-609]
Synonyms:
INRF2 | KEAP1 | KEAP1_HUMAN | KIAA0132 | KLHL19 | Keap1 (aa 321-609)
Type:
Enzyme Catalytic Domain
Mol. Mass.:
31620.58
Organism:
Homo sapiens (Human)
Description:
Q14145[321-609]
Residue:
289
Sequence:
APKVGRLIYTAGGYFRQSLSYLEAYNPSDGTWLRLADLQVPRSGLAGCVVGGLLYAVGGRNNSPDGNTDSSALDCYNPMTNQWSPCAPMSVPRNRIGVGVIDGHIYAVGGSHGCIHHNSVERYEPERDEWHLVAPMLTRRIGVGVAVLNRLLYAVGGFDGTNRLNSAECYYPERNEWRMITAMNTIRSGAGVCVLHNCIYAAGGYDGQDQLNSVERYDVETETWTFVAPMKHRRSALGITVHQGRIYVLGGYDGHTFLDSVECYDPDTDTWSEVTRMTSGRSGVGVAVT
  
Inhibitor
Name:
BDBM304755
Synonyms:
3-(3-(((R)-4-ethyl-1,1-dioxido-3,4-dihydro-2H-pyrido[2,3-b][1,4,5]oxathiazepin-2-yl)methyl)-4-methylphenyl)-3-(1-ethyl-4-methyl-1H-benzo[d][1,2,3]triazol-5-yl)propanoic acid | BDBM304838 | BDBM304885 | BDBM304886 | US10144731, Example 40
Type:
Small organic molecule
Emp. Form.:
C29H33N5O5S
Mol. Mass.:
563.668
SMILES:
CC[C@@H]1CN(Cc2cc(ccc2C)C(CC(O)=O)c2ccc3n(CC)nnc3c2C)S(=O)(=O)c2cccnc2O1 |r|
Structure:
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