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Compound Detail

CHEMBL543491

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COc1cc2c(-c3ccnc(-n4nc(-c5cccnc5)c5ccccc5c4=O)c3)c(CO)c(CO)cc2cc1OCc1ccccc1.Cl.Cl

Basic Information

ChEMBL ID CHEMBL543491
Phase Preclinical
Structure Type MOL
InChI Key RVKKSTDMZDAERR-UHFFFAOYSA-N
Parent Compound CHEMBL1192277
Active Moiety CHEMBL1192277
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

622.7
MW (Da)
6.24
ALogP
9
HBA
2
HBD
119.6
PSA (Ų)
0.19
QED
2
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C38H32Cl2N4O5
MW 695.60
Aromatic Rings 7
Heavy Atoms 47
NP-Likeness -0.48

Activity Summary

IC50 1 meas. best 6.16

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Phosphodiesterase 4
CHEMBL2093863
IC50 6.16 6.16 700.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Phosphodiesterase 4 IC50 = 700.0 nM 6.16 In vitro inhibition of Phosphodiesterase 4 from guinea pig lung 10090791

Literature References

PubMed DOI Target Context # Activities
10090791 10.1021/jm980314l Phosphodiesterase 4 2
10090791 10.1021/jm980314l Phosphodiesterase 3 1

Data from ChEMBL 36 via Core Engine