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Compound Detail

CHEMBL403283

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Cn1c(-c2ccccc2C(F)(F)F)cnc1C12CCC(c3nnc(-c4ccc(F)cc4)[nH]3)(CC1)CC2

Basic Information

ChEMBL ID CHEMBL403283
Phase Preclinical
Structure Type MOL
InChI Key UAXCWJFNZPJHSI-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

495.5
MW (Da)
6.57
ALogP
4
HBA
1
HBD
59.4
PSA (Ų)
0.33
QED
1
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C27H25F4N5
MW 495.52
Aromatic Rings 4
Heavy Atoms 36
NP-Likeness -0.70

Activity Summary

IC50 1 meas. best 8.33

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
11-beta-hydroxysteroid dehydrogenase 1
CHEMBL4235
IC50 8.33 8.33 4.7 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
11-beta-hydroxysteroid dehydrogenase 1 IC50 = 4.677 nM 8.33 Inhibition of 11beta-HSD1 18314331

Literature References

PubMed DOI Target Context # Activities
18314331 10.1016/j.bmcl.2008.02.042 11-beta-hydroxysteroid dehydrogenase 1 1

Data from ChEMBL 36 via Core Engine