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Compound Detail

CHEMBL4473402

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O=C1COc2ccc(C(=O)N3CCOc4ccccc43)cc2N1

Basic Information

ChEMBL ID CHEMBL4473402
Phase Preclinical
Structure Type MOL
InChI Key ATZGRDKFIWORFR-UHFFFAOYSA-N
1
Targets
2
Activities
2
Assay Types
1
PK Parameters
5
Publications
0
Known Names

Molecular Properties

310.3
MW (Da)
2.06
ALogP
4
HBA
1
HBD
67.9
PSA (Ų)
0.88
QED
0
Ro5 Violations
1
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C17H14N2O4
MW 310.31
Aromatic Rings 2
Heavy Atoms 23
NP-Likeness -1.58

Activity Summary

IC50 1 meas. best 5.5
Ki 1 meas. best 6.0

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Mineralocorticoid receptor
CHEMBL1994
Ki 6.0 6.0 1000.0 1
Mineralocorticoid receptor
CHEMBL1994
IC50 5.5 5.5 3162.3 1

Pharmacokinetic Data

Parameter Value Units Species
CL 4.0 mL.min-1.g-1 Homo sapiens

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
30596500 10.1021/acs.jmedchem.8b01523 Mineralocorticoid receptor 3
30596500 10.1021/acs.jmedchem.8b01523 No relevant target 2
30596500 10.1021/acs.jmedchem.8b01523 Glucocorticoid receptor 1
30596500 10.1021/acs.jmedchem.8b01523 Progesterone receptor 1
30596500 10.1021/acs.jmedchem.8b01523 ADMET 1

Data from ChEMBL 36 via Core Engine