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Compound Detail

CHEMBL255168

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CN(C)c1ccc(/C=C/C(=O)/C=C/c2ccc(N(C)C)cc2)cc1

Basic Information

ChEMBL ID CHEMBL255168
Phase Preclinical
Structure Type MOL
InChI Key JWTSVUUPJIIXTO-KAVGSWPWSA-N
2
Targets
3
Activities
2
Assay Types
0
PK Parameters
16
Publications
0
Known Names

Molecular Properties

320.4
MW (Da)
4.11
ALogP
3
HBA
0
HBD
23.6
PSA (Ų)
0.75
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H24N2O
MW 320.44
Aromatic Rings 2
Heavy Atoms 24
NP-Likeness -0.13

Activity Summary

IC50 2 meas. best 5.62
Ki 1 meas. best 8.57

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Unchecked
CHEMBL612545
Ki 8.57 8.57 2.7 1
17-beta-hydroxysteroid dehydrogenase type 3
CHEMBL4234
IC50 5.62 5.62 2400.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
25442312 10.1016/j.bmcl.2014.09.074 ADMET 7
25442312 10.1016/j.bmcl.2014.09.074 MDCK 6
23800686 10.1016/j.bmcl.2013.05.080 11-beta-hydroxysteroid dehydrogenase 1 4
20346654 10.1016/j.bmcl.2010.02.089 17-beta-hydroxysteroid dehydrogenase type 3 3
30108820 10.1039/C6MD00649C Candida albicans 3
30108820 10.1039/C6MD00649C Candida tropicalis 3
30108820 10.1039/C6MD00649C Pichia kudriavzevii 3
18234497 10.1016/j.bmcl.2007.12.068 J774.A1 2
21493068 10.1016/j.bmcl.2011.03.037 Plasmodium falciparum 2
23800686 10.1016/j.bmcl.2013.05.080 11-beta-hydroxysteroid dehydrogenase type 2 2
21417461 10.1021/jm101404k Unchecked 1
21493068 10.1016/j.bmcl.2011.03.037 HeLa 1
23800686 10.1016/j.bmcl.2013.05.080 NON-PROTEIN TARGET 1
25442312 10.1016/j.bmcl.2014.09.074 Caco-2 1
29223100 10.1016/j.ejmech.2017.11.048 Nuclear factor erythroid 2-related factor 2 1
29223100 10.1016/j.ejmech.2017.11.048 Luciferin 4-monooxygenase 1

Data from ChEMBL 36 via Core Engine