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Compound Detail

CHEMBL5273301

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CCOc1ccc(S(=O)(=O)Nc2cc3c(C(=O)NO)cn(S(=O)(=O)c4ccc(OCC)cc4)c3c3ccccc23)cc1

Basic Information

ChEMBL ID CHEMBL5273301
Phase Preclinical
Structure Type MOL
InChI Key RHJCLYVCHFGTKZ-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

609.7
MW (Da)
4.75
ALogP
9
HBA
3
HBD
153.0
PSA (Ų)
0.15
QED
1
Ro5 Violations
10
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C29H27N3O8S2
MW 609.68
Aromatic Rings 5
Heavy Atoms 42
NP-Likeness -1.02

Activity Summary

IC50 1 meas. best 6.7

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Keap1/Nrf2
CHEMBL3038498
IC50 6.7 6.7 200.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Keap1/Nrf2 IC50 = 200.0 nM 6.7 Inhibition of human Keap1-Nrf2 protein-protein interaction by fluorescence polar... 32668381

Literature References

PubMed DOI Target Context # Activities
32668381 10.1016/j.ejmech.2020.112532 Keap1/Nrf2 1

Data from ChEMBL 36 via Core Engine