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Compound Detail

CHEMBL4534373

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COc1cc2nnc3[nH]nc(C)c3c2cc1OC

Basic Information

ChEMBL ID CHEMBL4534373
Phase Preclinical
Structure Type MOL
InChI Key NOAZBIGPIKIKDQ-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

244.2
MW (Da)
1.83
ALogP
5
HBA
1
HBD
72.9
PSA (Ų)
0.74
QED
0
Ro5 Violations
2
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C12H12N4O2
MW 244.25
Aromatic Rings 3
Heavy Atoms 18
NP-Likeness -0.77

Activity Summary

IC50 2 meas. best 7.08

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A
CHEMBL4409
IC50 7.08 7.08 84.0 1
cGMP-inhibited 3',5'-cyclic phosphodiesterase 3A
CHEMBL241
IC50 5.96 5.96 1110.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
30587449 10.1016/j.bmcl.2018.12.029 ADMET 2
30587449 10.1016/j.bmcl.2018.12.029 cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A 1
30587449 10.1016/j.bmcl.2018.12.029 cGMP-dependent 3',5'-cyclic phosphodiesterase 1
30587449 10.1016/j.bmcl.2018.12.029 cGMP-inhibited 3',5'-cyclic phosphodiesterase 3A 1
30587449 10.1016/j.bmcl.2018.12.029 3',5'-cyclic-AMP phosphodiesterase 4D 1

Data from ChEMBL 36 via Core Engine