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Compound Detail

CHEMBL3235898

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O=C1NN(c2cccc(Cl)c2)C(=O)/C1=C\c1ccc(-c2ccc(C(=O)O)c(Cl)c2)o1

Basic Information

ChEMBL ID CHEMBL3235898
Phase Preclinical
Structure Type MOL
InChI Key XVLQZWSQEMKEIL-YBEGLDIGSA-N
1
Targets
2
Activities
2
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

443.2
MW (Da)
4.41
ALogP
4
HBA
2
HBD
99.8
PSA (Ų)
0.46
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H12Cl2N2O5
MW 443.24
Aromatic Rings 3
Heavy Atoms 30
NP-Likeness -1.45

Activity Summary

Kd 1 meas. best 4.82
Ki 1 meas.

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Keap1/Nrf2
CHEMBL3038498
Kd 4.82 4.82 15200.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Keap1/Nrf2 Kd = 15200.0 nM 4.82 Inhibition of Keap1-Nrf2 (unknown origin) interaction assessed as compound's equ... 24417449

Literature References

PubMed DOI Target Context # Activities
31411465 10.1021/acs.jmedchem.9b00723 Kelch-like ECH-associated protein 1 8
31411465 10.1021/acs.jmedchem.9b00723 No relevant target 2
24417449 10.1021/jm4017174 Keap1/Nrf2 1
24417449 10.1021/jm4017174 Kelch-like ECH-associated protein 1 1

Data from ChEMBL 36 via Core Engine