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Compound Detail

CHEMBL493794

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COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CC(C)(N)c3ccccc3)c2=O)c1F

Basic Information

ChEMBL ID CHEMBL493794
Phase Preclinical
Structure Type MOL
InChI Key LFQIPHGDVFLIHU-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

509.5
MW (Da)
4.33
ALogP
6
HBA
1
HBD
79.2
PSA (Ų)
0.40
QED
1
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C28H26F3N3O3
MW 509.53
Aromatic Rings 4
Heavy Atoms 37
NP-Likeness -0.72

Activity Summary

Ki 1 meas. best 7.64

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Gonadotropin-releasing hormone receptor
CHEMBL1855
Ki 7.64 7.64 23.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Gonadotropin-releasing hormone receptor Ki = 23.0 nM 7.64 Binding affinity at human GnRH receptor 18419112

Literature References

PubMed DOI Target Context # Activities
18419112 10.1021/jm701249f Gonadotropin-releasing hormone receptor 1

Data from ChEMBL 36 via Core Engine