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Compound Detail

CHEMBL3234863

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C[C@H](c1ccccc1)N1C(=O)O[C@](Cc2ccccc2)(c2nnc(C3(c4ccccc4)CC3)o2)C1=O

Basic Information

ChEMBL ID CHEMBL3234863
Phase Preclinical
Structure Type MOL
InChI Key IYSJAKSFBLSTEX-ACSYHNTCSA-N
1
Targets
1
Activities
1
Assay Types
4
PK Parameters
13
Publications
0
Known Names

Molecular Properties

479.5
MW (Da)
5.33
ALogP
6
HBA
0
HBD
85.5
PSA (Ų)
0.36
QED
1
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C29H25N3O4
MW 479.54
Aromatic Rings 4
Heavy Atoms 36
NP-Likeness -0.16

Activity Summary

IC50 1 meas. best 7.09

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Mineralocorticoid receptor
CHEMBL1994
IC50 7.09 7.09 82.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 7.9 mL.min-1.kg-1 Rattus norvegicus
F 89.0 % Rattus norvegicus
T1/2 2.8 hr Rattus norvegicus
Vd 1.0 L.kg-1 Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
24630411 10.1016/j.bmcl.2014.02.057 Rattus norvegicus 5
24630411 10.1016/j.bmcl.2014.02.057 Liver microsome 2
24630411 10.1016/j.bmcl.2014.02.057 Unchecked 2
24630411 10.1016/j.bmcl.2014.02.057 Mineralocorticoid receptor 1
24630411 10.1016/j.bmcl.2014.02.057 Androgen receptor 1
24630411 10.1016/j.bmcl.2014.02.057 Estrogen receptor 1
24630411 10.1016/j.bmcl.2014.02.057 Glucocorticoid receptor 1
24630411 10.1016/j.bmcl.2014.02.057 Progesterone receptor 1
24630411 10.1016/j.bmcl.2014.02.057 Voltage-gated inwardly rectifying potassium channel KCNH2 1
24630411 10.1016/j.bmcl.2014.02.057 Cytochrome P450 3A4 1
24630411 10.1016/j.bmcl.2014.02.057 Cytochrome P450 2D6 1
24630411 10.1016/j.bmcl.2014.02.057 Cytochrome P450 2C9 1
24630411 10.1016/j.bmcl.2014.02.057 Molecular identity unknown 1

Data from ChEMBL 36 via Core Engine