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Compound Detail

CHEMBL4079083

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O=C1COc2ccc(N3CCOC[C@H]3c3ccccc3)nc2N1

Basic Information

ChEMBL ID CHEMBL4079083
Phase Preclinical
Structure Type MOL
InChI Key AUSLDGVMWQDFIM-ZDUSSCGKSA-N
1
Targets
3
Activities
1
Assay Types
1
PK Parameters
4
Publications
0
Known Names

Molecular Properties

311.3
MW (Da)
1.99
ALogP
5
HBA
1
HBD
63.7
PSA (Ų)
0.92
QED
0
Ro5 Violations
2
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C17H17N3O3
MW 311.34
Aromatic Rings 2
Heavy Atoms 23
NP-Likeness -0.88

Activity Summary

IC50 3 meas. best 5.93

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Mineralocorticoid receptor
CHEMBL1994
IC50 5.93 5.7833 1181.0 3

Pharmacokinetic Data

Parameter Value Units Species
CL 8.9 mL.min-1.g-1 Homo sapiens

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
29300474 10.1021/acs.jmedchem.7b01515 Mineralocorticoid receptor 2
28051871 10.1021/acs.jmedchem.6b01065 Mineralocorticoid receptor 1
29300474 10.1021/acs.jmedchem.7b01515 No relevant target 1
29300474 10.1021/acs.jmedchem.7b01515 Liver 1

Data from ChEMBL 36 via Core Engine