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Compound Detail

CHEMBL401437

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Cc1ncc(-c2ccc(C(F)(F)F)cc2)c(NC23CC4CC(CC(C4)C2)C3)n1

Basic Information

ChEMBL ID CHEMBL401437
Phase Preclinical
Structure Type MOL
InChI Key UPYWSHBFDZRRIP-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

387.4
MW (Da)
5.85
ALogP
3
HBA
1
HBD
37.8
PSA (Ų)
0.72
QED
1
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H24F3N3
MW 387.45
Aromatic Rings 2
Heavy Atoms 28
NP-Likeness -0.87

Activity Summary

EC50 1 meas. best 5.46

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
GABA-B receptor
CHEMBL2111463
EC50 5.46 5.46 3467.4 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
GABA-B receptor EC50 = 3467.37 nM 5.46 Activity at GABAB 1b/2 receptor expressed in CHO-K1 cells assessed as effect on ... 17884493

Literature References

PubMed DOI Target Context # Activities
17884493 10.1016/j.bmcl.2007.09.023 GABA-B receptor 4
17884493 10.1016/j.bmcl.2007.09.023 No relevant target 2

Data from ChEMBL 36 via Core Engine