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Compound Detail

CHEMBL5220253

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O=C(O)c1cc(F)c(Cl)nc1Cl

Basic Information

ChEMBL ID CHEMBL5220253
Phase Preclinical
Structure Type MOL
InChI Key LTDGKGCHRNNCAC-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

210.0
MW (Da)
2.23
ALogP
2
HBA
1
HBD
50.2
PSA (Ų)
0.72
QED
0
Ro5 Violations
1
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C6H2Cl2FNO2
MW 209.99
Aromatic Rings 1
Heavy Atoms 12
NP-Likeness -1.21

Activity Summary

Ki 1 meas. best 2.6

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Keap1/Nrf2
CHEMBL3038498
Ki 2.6 2.6 2500000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Keap1/Nrf2 Ki = 2500000.0 nM 2.6 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 Kelch-like ECH-associated protein 1 4
36263945 10.1021/acs.jmedchem.2c00830 Keap1/Nrf2 1

Data from ChEMBL 36 via Core Engine