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Compound Detail

CHEMBL4213258

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COc1ccc(-n2c(SCc3cccc(F)c3)nc3c(cnn3C)c2=O)cc1

Basic Information

ChEMBL ID CHEMBL4213258
Phase Preclinical
Structure Type MOL
InChI Key CYFVHDRSKPOKLU-UHFFFAOYSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

396.4
MW (Da)
3.56
ALogP
7
HBA
0
HBD
61.9
PSA (Ų)
0.38
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C20H17FN4O2S
MW 396.45
Aromatic Rings 4
Heavy Atoms 28
NP-Likeness -2.42

Activity Summary

IC50 3 meas. best 6.11

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Retinaldehyde dehydrogenase 3
CHEMBL3579
IC50 6.11 6.11 780.0 1
Retinal dehydrogenase 2
CHEMBL3112384
IC50 5.75 5.75 1770.0 1
Aldehyde dehydrogenase 1A1
CHEMBL3577
IC50 5.09 5.09 8200.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
30221940 10.1021/acs.jmedchem.8b00930 Aldehyde dehydrogenase 1A1 1
30221940 10.1021/acs.jmedchem.8b00930 Retinal dehydrogenase 2 1
30221940 10.1021/acs.jmedchem.8b00930 Retinaldehyde dehydrogenase 3 1
30221940 10.1021/acs.jmedchem.8b00930 Aldehyde dehydrogenase, mitochondrial 1

Data from ChEMBL 36 via Core Engine