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Compound Detail

CHEMBL2377211

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Cc1cc(N)nc(NS(=O)(=O)c2ccc(-c3ccc(C#N)cc3)cc2)c1

Basic Information

ChEMBL ID CHEMBL2377211
Phase Preclinical
Structure Type MOL
InChI Key XRGIKGDSURWPTL-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
3
PK Parameters
3
Publications
0
Known Names

Molecular Properties

364.4
MW (Da)
3.31
ALogP
5
HBA
2
HBD
108.9
PSA (Ų)
0.74
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C19H16N4O2S
MW 364.43
Aromatic Rings 3
Heavy Atoms 26
NP-Likeness -1.34

Activity Summary

EC50 1 meas. best 7.31

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
11-beta-hydroxysteroid dehydrogenase 1
CHEMBL4235
EC50 7.31 7.31 49.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 0.25 mL.min-1.kg-1 Rattus norvegicus
F 81.0 % Rattus norvegicus
T1/2 17.0 hr Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
11-beta-hydroxysteroid dehydrogenase 1 EC50 = 49.0 nM 7.31 Inhibition of 11beta-HSD1 in human HEK293 cells 23489629

Literature References

PubMed DOI Target Context # Activities
23489629 10.1016/j.bmcl.2013.02.066 Rattus norvegicus 4
23489629 10.1016/j.bmcl.2013.02.066 Liver microsomes 1
23489629 10.1016/j.bmcl.2013.02.066 11-beta-hydroxysteroid dehydrogenase 1 1

Data from ChEMBL 36 via Core Engine