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Compound Detail

CHEMBL2391969

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Cn1c(-c2ccccc2C(F)(F)F)nnc1C12CCC(c3noc(C(C)(F)F)n3)(CC1)CC2

Basic Information

ChEMBL ID CHEMBL2391969
Phase Preclinical
Structure Type MOL
InChI Key AHAIJYTWSYJSSZ-UHFFFAOYSA-N
3
Targets
4
Activities
2
Assay Types
0
PK Parameters
10
Publications
0
Known Names

Molecular Properties

467.4
MW (Da)
5.54
ALogP
6
HBA
0
HBD
69.6
PSA (Ų)
0.47
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 C22H22F5N5O
MW 467.44
Aromatic Rings 3
Heavy Atoms 33
NP-Likeness -0.80

Activity Summary

IC50 3 meas. best 8.35
Ki 1 meas. best 8.15

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
11-beta-hydroxysteroid dehydrogenase 1
CHEMBL2391
IC50 8.35 8.35 4.5 1
11-beta-hydroxysteroid dehydrogenase 1
CHEMBL2391
Ki 8.15 8.15 7.0 1
11-beta-hydroxysteroid dehydrogenase type 2
CHEMBL3746
IC50 7.52 7.52 30.4 1
11-beta-hydroxysteroid dehydrogenase 1
CHEMBL4235
IC50 5.51 5.51 3100.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
23659858 10.1016/j.bmcl.2013.03.011 Brain 4
23659858 10.1016/j.bmcl.2013.03.011 Plasma 4
23659858 10.1016/j.bmcl.2013.03.011 Rattus norvegicus 3
23659858 10.1016/j.bmcl.2013.03.011 11-beta-hydroxysteroid dehydrogenase 1 3
23659858 10.1016/j.bmcl.2013.03.011 ADMET 2
23659858 10.1016/j.bmcl.2013.03.011 Mus musculus 2
23659858 10.1016/j.bmcl.2013.03.011 Cerebrospinal fluid 2
23659858 10.1016/j.bmcl.2013.03.011 Nucleic Acid 1
23659858 10.1016/j.bmcl.2013.03.011 Unchecked 1
23659858 10.1016/j.bmcl.2013.03.011 11-beta-hydroxysteroid dehydrogenase type 2 1

Data from ChEMBL 36 via Core Engine