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Compound Detail

CHEMBL5220988

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COc1ccc(S(=O)(=O)NCc2cc(C(NC(=O)c3cccc4c3-c3ccccc3C4=O)C(=O)O)ccc2OC)cc1

Basic Information

ChEMBL ID CHEMBL5220988
Phase Preclinical
Structure Type MOL
InChI Key USJUOKGRSMIVHQ-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

586.6
MW (Da)
3.95
ALogP
7
HBA
3
HBD
148.1
PSA (Ų)
0.22
QED
1
Ro5 Violations
10
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C31H26N2O8S
MW 586.62
Aromatic Rings 4
Heavy Atoms 42
NP-Likeness -0.65

Activity Summary

Ki 1 meas. best 4.98

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Keap1/Nrf2
CHEMBL3038498
Ki 4.98 4.98 10500.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Keap1/Nrf2 Ki = 10500.0 nM 4.98 Inhibition of recombinant human His-tagged Keap1 kelch domain (321 to 609 residu... 36263945

Literature References

PubMed DOI Target Context # Activities
36263945 10.1021/acs.jmedchem.2c00830 Keap1/Nrf2 1

Data from ChEMBL 36 via Core Engine