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Compound Detail

CHEMBL4098282

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[3H]C([3H])([3H])n1nc(-c2cnn(C)c2-c2ccc(C(F)(F)F)cc2)c2c(N3CCC3)ncnc21

Basic Information

ChEMBL ID CHEMBL4098282
Phase Preclinical
Structure Type MOL
InChI Key SHAVEYUXRBIMLA-BHTRQJOGSA-N
Parent Compound CHEMBL2381192
Active Moiety CHEMBL2381192
2
Targets
3
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

413.4
MW (Da)
3.66
ALogP
7
HBA
0
HBD
64.7
PSA (Ų)
0.51
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 C20H18F3N7
MW 419.43
Aromatic Rings 4
Heavy Atoms 30
NP-Likeness -1.61

Activity Summary

Kd 3 meas. best 8.56

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
cGMP-dependent 3',5'-cyclic phosphodiesterase
CHEMBL4650
Kd 8.56 8.56 2.8 1
Unchecked
CHEMBL612545
Kd 8.49 8.485 3.2 2

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
28574706 10.1021/acs.jmedchem.7b00397 Unchecked 2
28574706 10.1021/acs.jmedchem.7b00397 cGMP-dependent 3',5'-cyclic phosphodiesterase 1

Data from ChEMBL 36 via Core Engine