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Compound Detail

CHEMBL274528

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COc1cc2cc(CO)c(CO)c(-c3ccnc(-n4ccc(=O)c5ccccc54)c3)c2cc1OC

Basic Information

ChEMBL ID CHEMBL274528
Phase Preclinical
Structure Type MOL
InChI Key LKQLMGVBCLAGOJ-UHFFFAOYSA-N
4
Targets
4
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

468.5
MW (Da)
4.21
ALogP
7
HBA
2
HBD
93.8
PSA (Ų)
0.39
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 C28H24N2O5
MW 468.51
Aromatic Rings 5
Heavy Atoms 35
NP-Likeness -0.02

Activity Summary

IC50 4 meas. best 7.4

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Phosphodiesterase 4
CHEMBL2093863
IC50 7.4 7.4 40.0 1
Phosphodiesterase 3
CHEMBL2094125
IC50 6.4 6.4 400.0 1
Phosphodiesterase 1
CHEMBL2095150
IC50 5.05 5.05 9000.0 1
cGMP-specific 3',5'-cyclic phosphodiesterase
CHEMBL1827
IC50 4.7 4.7 20000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
10090791 10.1021/jm980314l Phosphodiesterase 4 2
10090791 10.1021/jm980314l Phosphodiesterase 1 1
10090791 10.1021/jm980314l Phosphodiesterase 3 1
10090791 10.1021/jm980314l cGMP-specific 3',5'-cyclic phosphodiesterase 1

Data from ChEMBL 36 via Core Engine