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Compound Detail

CHEMBL2407668

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COc1cc(CNC(=O)[C@@]2(Cc3ccccc3)OC(=O)N([C@H](C)c3ccccc3)C2=O)cc(OC)c1

Basic Information

ChEMBL ID CHEMBL2407668
Phase Preclinical
Structure Type MOL
InChI Key UOOMYPHRFLZIRW-WHLCRQNOSA-N
1
Targets
1
Activities
1
Assay Types
4
PK Parameters
2
Publications
0
Known Names

Molecular Properties

488.5
MW (Da)
4.04
ALogP
6
HBA
1
HBD
94.2
PSA (Ų)
0.46
QED
0
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C28H28N2O6
MW 488.54
Aromatic Rings 3
Heavy Atoms 36
NP-Likeness -0.33

Activity Summary

IC50 1 meas. best 7.27

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Mineralocorticoid receptor
CHEMBL1994
IC50 7.27 7.27 54.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 46.0 mL.min-1.kg-1 Rattus norvegicus
Cmax 60.0 nM Rattus norvegicus
F 7.0 % Rattus norvegicus
T1/2 1.2 hr Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
23777778 10.1016/j.bmcl.2013.05.077 Rattus norvegicus 7
23777778 10.1016/j.bmcl.2013.05.077 Mineralocorticoid receptor 1

Data from ChEMBL 36 via Core Engine