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Compound Detail

CHEMBL4173296

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COc1ccc(S(=O)(=O)N(CC(=O)O)c2nnc(N(CC(=O)O)S(=O)(=O)c3ccc(OC)cc3)c3ccccc23)cc1

Basic Information

ChEMBL ID CHEMBL4173296
Phase Preclinical
Structure Type MOL
InChI Key XSXFVSYWZDKSFF-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

616.6
MW (Da)
2.21
ALogP
10
HBA
2
HBD
193.6
PSA (Ų)
0.24
QED
1
Ro5 Violations
12
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C26H24N4O10S2
MW 616.63
Aromatic Rings 4
Heavy Atoms 42
NP-Likeness -0.60

Activity Summary

IC50 1 meas. best 5.96

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Keap1/Nrf2
CHEMBL3038498
IC50 5.96 5.96 1100.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Keap1/Nrf2 IC50 = 1100.0 nM 5.96 Inhibition of Keap1 Kelch domain (unknown origin) /Nrf2 (unknown origin) interac... 30122040

Literature References

PubMed DOI Target Context # Activities
30122040 10.1021/acs.jmedchem.8b01133 Keap1/Nrf2 3
30122040 10.1021/acs.jmedchem.8b01133 ADMET 2
30122040 10.1021/acs.jmedchem.8b01133 Kelch-like ECH-associated protein 1 1
30122040 10.1021/acs.jmedchem.8b01133 No relevant target 1

Data from ChEMBL 36 via Core Engine