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Compound Detail

CHEMBL4861872

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CC(Sc1nc2nn(C3(C)COC3)cc2c(=O)n1-c1ccccc1)c1ccccc1

Basic Information

ChEMBL ID CHEMBL4861872
Phase Preclinical
Structure Type MOL
InChI Key ZNWMCWVIVQIVDB-UHFFFAOYSA-N
3
Targets
3
Activities
1
Assay Types
6
PK Parameters
5
Publications
0
Known Names

Molecular Properties

418.5
MW (Da)
4.18
ALogP
7
HBA
0
HBD
61.9
PSA (Ų)
0.36
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C23H22N4O2S
MW 418.52
Aromatic Rings 4
Heavy Atoms 30
NP-Likeness -1.15

Activity Summary

IC50 3 meas. best 7.3

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Retinaldehyde dehydrogenase 3
CHEMBL3579
IC50 7.3 7.3 50.0 1
Aldehyde dehydrogenase 1A1
CHEMBL3577
IC50 7.03 7.03 93.0 1
Retinal dehydrogenase 2
CHEMBL3112384
IC50 6.95 6.95 112.0 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 9625.96 ng.hr.mL-1 Mus musculus
AUC 9751.52 ng.hr.mL-1 Mus musculus
Cmax 7000.0 nM Mus musculus
Cmax 7000.0 nM Mus musculus
T1/2 1.0 hr Mus musculus
T1/2 1.6 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 ADMET 6
33341649 10.1016/j.ejmech.2020.113060 Retinaldehyde dehydrogenase 3 2
33341649 10.1016/j.ejmech.2020.113060 No relevant target 1
33341649 10.1016/j.ejmech.2020.113060 Aldehyde dehydrogenase 1A1 1
33341649 10.1016/j.ejmech.2020.113060 Retinal dehydrogenase 2 1

Data from ChEMBL 36 via Core Engine