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Compound Detail

CHEMBL4876602

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C[C@@H](Sc1nc2c(cnn2C)c(=O)n1-c1ccccc1)c1ccccc1

Basic Information

ChEMBL ID CHEMBL4876602
Phase Preclinical
Structure Type MOL
InChI Key JNPNRKXZLIGUCT-CQSZACIVSA-N
3
Targets
3
Activities
1
Assay Types
4
PK Parameters
5
Publications
0
Known Names

Molecular Properties

362.5
MW (Da)
3.97
ALogP
6
HBA
0
HBD
52.7
PSA (Ų)
0.41
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C20H18N4OS
MW 362.46
Aromatic Rings 4
Heavy Atoms 26
NP-Likeness -1.96

Activity Summary

IC50 3 meas. best 7.47

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Retinaldehyde dehydrogenase 3
CHEMBL3579
IC50 7.47 7.47 34.0 1
Retinal dehydrogenase 2
CHEMBL3112384
IC50 7.4 7.4 40.0 1
Aldehyde dehydrogenase 1A1
CHEMBL3577
IC50 7.16 7.16 70.0 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 253.72 ng.hr.mL-1 Mus musculus
Cmax 300.0 nM Mus musculus
T1/2 0.1333 hr Mus musculus
T1/2 0.5 hr Mus musculus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
33341649 10.1016/j.ejmech.2020.113060 Aldehyde dehydrogenase 1A1 4
33341649 10.1016/j.ejmech.2020.113060 ADMET 4
33341649 10.1016/j.ejmech.2020.113060 Retinaldehyde dehydrogenase 3 3
33341649 10.1016/j.ejmech.2020.113060 Retinal dehydrogenase 2 1
33341649 10.1016/j.ejmech.2020.113060 SK-OV-3 1

Data from ChEMBL 36 via Core Engine