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Compound Detail

CHEMBL313982

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COc1ccc(C2=NN(C3C4CC5CC(C4)CC3C5)C(=O)[C@@H]3CC=CC[C@H]23)cc1OC

Basic Information

ChEMBL ID CHEMBL313982
Phase Preclinical
Structure Type MOL
InChI Key CSNUCLKQPKBQNG-AGRQWJSISA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

420.6
MW (Da)
4.66
ALogP
4
HBA
0
HBD
51.1
PSA (Ų)
0.67
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 C26H32N2O3
MW 420.55
Aromatic Rings 1
Heavy Atoms 31
NP-Likeness -0.17

Activity Summary

IC50 1 meas. best 9.3

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Phosphodiesterase 4
CHEMBL2093863
IC50 9.3 9.3 0.5 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Phosphodiesterase 4 IC50 = 0.5012 nM 9.3 Inhibitory activity against phosphodiesterase 4 carried out in the cytosol of hu... 12036361

Literature References

PubMed DOI Target Context # Activities
12036361 10.1021/jm0110338 Phosphodiesterase 4 1
12036361 10.1021/jm0110338 Mus musculus 1

Data from ChEMBL 36 via Core Engine