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Compound Detail

CHEMBL477933

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CN1CCc2[nH]c3ccc(CC(=O)[O-])cc3c2C1.[K+]

Basic Information

ChEMBL ID CHEMBL477933
Phase Preclinical
Structure Type MOL
InChI Key YJCMGAJNWZVVIG-UHFFFAOYSA-M
Parent Compound CHEMBL1208025
Active Moiety CHEMBL1208025
1
Targets
3
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

244.3
MW (Da)
1.78
ALogP
2
HBA
2
HBD
56.3
PSA (Ų)
0.85
QED
0
Ro5 Violations
2
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C14H15KN2O2
MW 282.38
Aromatic Rings 2
Heavy Atoms 18
NP-Likeness -0.46

Activity Summary

IC50 3 meas. best 4.27

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Aldo-keto reductase family 1 member B1
CHEMBL2622
IC50 4.27 4.27 54000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Aldo-keto reductase family 1 member B1 IC50 = 54000.0 nM 4.27 Inhibition of Wistar rat lens aldose reductase 2 18395454

Literature References

PubMed DOI Target Context # Activities
18395454 10.1016/j.bmc.2008.03.039 Aldo-keto reductase family 1 member B1 1
18395454 10.1016/j.bmc.2008.03.039 Unchecked 1
18395454 10.1016/j.bmc.2008.03.039 NON-PROTEIN TARGET 1
18395454 10.1016/j.bmc.2008.03.039 No relevant target 1

Data from ChEMBL 36 via Core Engine