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Compound Detail

CHEMBL123266

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O=C(N[C@@H]1N=C(c2ccccc2)c2cc(O)cc3c2N(CC3)C1=O)c1cc2ccccc2cn1

Basic Information

ChEMBL ID CHEMBL123266
Phase Preclinical
Structure Type MOL
InChI Key LRSRAJPLDDBOMK-VWLOTQADSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

448.5
MW (Da)
3.44
ALogP
5
HBA
2
HBD
94.9
PSA (Ų)
0.50
QED
0
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C27H20N4O3
MW 448.48
Aromatic Rings 4
Heavy Atoms 34
NP-Likeness -0.10

Activity Summary

IC50 1 meas. best 6.39

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Phosphodiesterase 4
CHEMBL2093863
IC50 6.39 6.39 410.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Phosphodiesterase 4 IC50 = 410.0 nM 6.39 Inhibition of phosphodiesterase 4 extracted from human U937 cells by using radio... 10636238

Literature References

PubMed DOI Target Context # Activities
10636238 10.1016/s0960-894x(99)00573-9 Phosphodiesterase 4 2
10636238 10.1016/s0960-894x(99)00573-9 Phosphodiesterase 3 1
10636238 10.1016/s0960-894x(99)00573-9 Phosphodiesterase, PDE1/PDE5 1

Data from ChEMBL 36 via Core Engine