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Compound Detail

CHEMBL111925

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Cc1cc2c3c(c1)C(c1ccccc1)=N[C@@H](NC(=O)c1ccncc1)C(=O)N3CC2

Basic Information

ChEMBL ID CHEMBL111925
Phase Preclinical
Structure Type MOL
InChI Key KYFWUBJMTHVBIF-QFIPXVFZSA-N
4
Targets
8
Activities
1
Assay Types
0
PK Parameters
12
Publications
0
Known Names

Molecular Properties

396.4
MW (Da)
2.89
ALogP
4
HBA
1
HBD
74.7
PSA (Ų)
0.74
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 C24H20N4O2
MW 396.45
Aromatic Rings 3
Heavy Atoms 30
NP-Likeness -0.48

Activity Summary

IC50 8 meas. best 6.0

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Unchecked
CHEMBL612545
IC50 6.0 5.39 990.0 3
Phosphodiesterase 4
CHEMBL2093863
IC50 5.96 5.9533 1100.0 3
Phosphodiesterase 3
CHEMBL2094125
IC50 4.45 4.45 35800.0 1
Phosphodiesterase, PDE1/PDE5
CHEMBL2097161
IC50 4.13 4.13 73400.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
11123995 10.1021/jm000315p Phosphodiesterase 4 3
11123995 10.1021/jm000315p Unchecked 3
10636238 10.1016/s0960-894x(99)00573-9 Phosphodiesterase 4 2
11123995 10.1021/jm000315p Phosphodiesterase 3 1
11123995 10.1021/jm000315p Phosphodiesterase, PDE1/PDE5 1
11123995 10.1021/jm000315p Rattus norvegicus 1
15149695 10.1016/j.bmcl.2004.03.067 Phosphodiesterase 4 1
10636238 10.1016/s0960-894x(99)00573-9 Phosphodiesterase 3 1
10636238 10.1016/s0960-894x(99)00573-9 Phosphodiesterase, PDE1/PDE5 1
10636238 10.1016/s0960-894x(99)00573-9 Rattus norvegicus 1
10636238 10.1016/s0960-894x(99)00573-9 Canis familiaris 1
18686943 10.1021/jm800582j Unchecked 1

Data from ChEMBL 36 via Core Engine