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Compound Detail

CHEMBL4871954

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COc1cc([C@H](O)[C@H]2CCCC3=Cc4c(cnn4-c4ccc(C)cc4)C[C@@]32C)cc(F)c1F

Basic Information

ChEMBL ID CHEMBL4871954
Phase Preclinical
Structure Type MOL
InChI Key IEHMKTVARCQJKJ-AIGMYPEUSA-N
1
Targets
2
Activities
2
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

450.5
MW (Da)
5.95
ALogP
4
HBA
1
HBD
47.3
PSA (Ų)
0.53
QED
1
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C27H28F2N2O2
MW 450.53
Aromatic Rings 3
Heavy Atoms 33
NP-Likeness -0.17

Activity Summary

EC50 1 meas. best 4.0
IC50 1 meas. best 6.8

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Glucocorticoid receptor
CHEMBL3368
IC50 6.8 6.8 158.5 1
Glucocorticoid receptor
CHEMBL3368
EC50 4.0 4.0 100000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
34676039 10.1021/acsmedchemlett.1c00379 Glucocorticoid receptor 8

Data from ChEMBL 36 via Core Engine