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Compound Detail

CHEMBL553278

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COc1cc2nc(CO)c(CO)c(-c3ccnc(-n4nc(-c5cccnc5)c5ccccc5c4=O)c3)c2cc1OC.Cl

Basic Information

ChEMBL ID CHEMBL553278
Phase Preclinical
Structure Type MOL
InChI Key QTMJGZGUVMBLOY-UHFFFAOYSA-N
Parent Compound CHEMBL1194765
Active Moiety CHEMBL1194765
1
Targets
2
Activities
2
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

547.6
MW (Da)
4.06
ALogP
10
HBA
2
HBD
132.5
PSA (Ų)
0.30
QED
1
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C31H26ClN5O5
MW 584.03
Aromatic Rings 6
Heavy Atoms 41
NP-Likeness -0.74

Activity Summary

IC50 1 meas. best 7.16
Ki 1 meas. best 6.92

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Phosphodiesterase 4
CHEMBL2093863
IC50 7.16 7.16 70.0 1
Phosphodiesterase 4
CHEMBL2093863
Ki 6.92 6.92 120.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Phosphodiesterase 4 IC50 = 70.0 nM 7.16 Inhibition of phosphodiesterase 4 12824031
Phosphodiesterase 4 Ki = 120.0 nM 6.92 Inhibition of rolipram binding to phosphodiesterase 4 12824031

Literature References

PubMed DOI Target Context # Activities
12824031 10.1016/s0960-894x(03)00438-4 Phosphodiesterase 4 3

Data from ChEMBL 36 via Core Engine