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Compound Detail

CHEMBL5276846

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COc1ccc(Cl)c(-c2nc(C)c3nnc4ccc(-c5ccnc(F)c5)cc4n23)c1

Basic Information

ChEMBL ID CHEMBL5276846
Phase Preclinical
Structure Type MOL
InChI Key LAUDMPJASNSMFC-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

419.9
MW (Da)
5.12
ALogP
6
HBA
0
HBD
65.2
PSA (Ų)
0.38
QED
1
Ro5 Violations
3
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H15ClFN5O
MW 419.85
Aromatic Rings 5
Heavy Atoms 30
NP-Likeness -1.28

Activity Summary

IC50 2 meas. best 8.48

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
cGMP-dependent 3',5'-cyclic phosphodiesterase
CHEMBL2652
IC50 8.48 8.48 3.3 1
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A
CHEMBL4409
IC50 7.28 7.28 53.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
33412421 10.1016/j.ejmech.2020.113123 cGMP-dependent 3',5'-cyclic phosphodiesterase 1
33412421 10.1016/j.ejmech.2020.113123 cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A 1
33412421 10.1016/j.ejmech.2020.113123 Unchecked 1

Data from ChEMBL 36 via Core Engine