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Compound Detail

CHEMBL219140

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COc1ccc(F)cc1C(C)(C)CC(O)(Cn1ccc(=O)c2ncccc21)C(F)(F)F

Basic Information

ChEMBL ID CHEMBL219140
Phase Preclinical
Structure Type MOL
InChI Key AKVKAFLTKMIROA-UHFFFAOYSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

438.4
MW (Da)
4.21
ALogP
5
HBA
1
HBD
64.3
PSA (Ų)
0.59
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H22F4N2O3
MW 438.42
Aromatic Rings 3
Heavy Atoms 31
NP-Likeness -0.79

Activity Summary

IC50 3 meas. best 7.25

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
HFF
CHEMBL614071
IC50 7.25 7.25 56.0 1
Glucocorticoid receptor
CHEMBL2034
IC50 7.11 7.11 77.0 1
Mineralocorticoid receptor
CHEMBL1994
IC50 5.96 5.96 1100.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
17181172 10.1021/jm061273t HFF 4
17181172 10.1021/jm061273t Glucocorticoid receptor 1
17181172 10.1021/jm061273t Progesterone receptor 1
17181172 10.1021/jm061273t Mineralocorticoid receptor 1
17181172 10.1021/jm061273t HeLa 1

Data from ChEMBL 36 via Core Engine