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Compound Detail

CHEMBL3732768

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COc1ncc([C@@H](C)Nc2ncnc3c2CN(c2ccc(C)cc2C#N)CC3)cn1

Basic Information

ChEMBL ID CHEMBL3732768
Phase Preclinical
Structure Type MOL
InChI Key OSQOURHXWJQPNS-OAHLLOKOSA-N
2
Targets
3
Activities
1
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

401.5
MW (Da)
3.19
ALogP
8
HBA
1
HBD
99.8
PSA (Ų)
0.70
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H23N7O
MW 401.47
Aromatic Rings 3
Heavy Atoms 30
NP-Likeness -1.32

Activity Summary

IC50 3 meas. best 8.0

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
P2X purinoceptor 3
CHEMBL2998
IC50 8.0 8.0 10.0 1
P2X2/P2X3 heterotrimeric receptor
CHEMBL3831281
IC50 8.0 7.395 10.0 2

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
27426300 10.1016/j.bmcl.2016.07.013 P2X purinoceptor 3 1

Data from ChEMBL 36 via Core Engine