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Compound Detail

CHEMBL384692

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CC(C)(C(=O)NC1CC2CC(C1)CC(C(N)=O)C2)N1CCN(c2ccc(C(F)(F)F)cn2)CC1

Basic Information

ChEMBL ID CHEMBL384692
Phase Preclinical
Structure Type MOL
InChI Key IEKKYUOJPWUXAI-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

481.6
MW (Da)
2.80
ALogP
5
HBA
2
HBD
91.6
PSA (Ų)
0.68
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 C24H34F3N5O2
MW 481.56
Aromatic Rings 1
Heavy Atoms 34
NP-Likeness -1.47

Activity Summary

IC50 1 meas. best 6.57

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
11-beta-hydroxysteroid dehydrogenase 1
CHEMBL4235
IC50 6.57 6.57 269.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
11-beta-hydroxysteroid dehydrogenase 1 IC50 = 269.0 nM 6.57 Inhibition of human 11beta-HSD1 16890427

Literature References

PubMed DOI Target Context # Activities
16890427 10.1016/j.bmcl.2006.07.062 11-beta-hydroxysteroid dehydrogenase 1 3
16890427 10.1016/j.bmcl.2006.07.062 11-beta-hydroxysteroid dehydrogenase type 2 2
16890427 10.1016/j.bmcl.2006.07.062 ADMET 1

Data from ChEMBL 36 via Core Engine