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Compound Detail

CHEMBL309243

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C=CC[C@H](O)[C@H]1CCCC2=Cc3c(cnn3-c3ccc(F)cc3)C[C@@]21C

Basic Information

ChEMBL ID CHEMBL309243
Phase Preclinical
Structure Type MOL
InChI Key QELYUNHSBLBUDL-HJNYFJLDSA-N
3
Targets
5
Activities
2
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

352.4
MW (Da)
4.69
ALogP
3
HBA
1
HBD
38.0
PSA (Ų)
0.81
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H25FN2O
MW 352.45
Aromatic Rings 2
Heavy Atoms 26
NP-Likeness 0.13

Activity Summary

EC50 4 meas. best 8.03
IC50 1 meas. best 8.41

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Glucocorticoid receptor
CHEMBL2034
IC50 8.41 8.41 3.9 1
Glucocorticoid receptor
CHEMBL2034
EC50 8.03 7.105 9.3 2
Mus musculus
CHEMBL375
EC50 7.44 7.44 36.2 1
Glutamine synthetase
CHEMBL4612
EC50 7.18 7.18 66.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
15115388 10.1021/jm030585i Glucocorticoid receptor 3
15115388 10.1021/jm030585i Glutamine synthetase 1
15115388 10.1021/jm030585i Mus musculus 1

Data from ChEMBL 36 via Core Engine