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Compound Detail

CHEMBL1650528

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OCCCc1cc(-c2ccccc2C(F)(F)F)cc2nc(C3=NOC4(CCCCC4)C3)[nH]c12

Basic Information

ChEMBL ID CHEMBL1650528
Phase Preclinical
Structure Type MOL
InChI Key GAPVJVYIORQQLN-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

457.5
MW (Da)
6.00
ALogP
4
HBA
2
HBD
70.5
PSA (Ų)
0.49
QED
1
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H26F3N3O2
MW 457.50
Aromatic Rings 3
Heavy Atoms 33
NP-Likeness -0.13

Activity Summary

IC50 2 meas. best 9.7

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Transient receptor potential M8 protein
CHEMBL1667665
IC50 9.7 9.7 0.2 1
Cytochrome P450 2C9
CHEMBL3397
IC50 5.17 5.17 6800.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
21128593 10.1021/jm101075v Liver microsomes 2
21128593 10.1021/jm101075v ADMET 1
21128593 10.1021/jm101075v Cytochrome P450 2C9 1
21128593 10.1021/jm101075v Transient receptor potential M8 protein 1

Data from ChEMBL 36 via Core Engine