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Compound Detail

CHEMBL453167

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COc1cccc(-c2cn(Cc3c(F)cccc3S(C)(=O)=O)c(=O)n(C[C@H](NCCCC(=O)O)c3ccccc3)c2=O)c1F

Basic Information

ChEMBL ID CHEMBL453167
Phase Preclinical
Structure Type MOL
InChI Key JELUMXNSIYVRCU-VWLOTQADSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

627.7
MW (Da)
3.61
ALogP
9
HBA
2
HBD
136.7
PSA (Ų)
0.21
QED
1
Ro5 Violations
13
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C31H31F2N3O7S
MW 627.67
Aromatic Rings 4
Heavy Atoms 44
NP-Likeness -0.93

Activity Summary

Ki 1 meas. best 8.47

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Gonadotropin-releasing hormone receptor
CHEMBL1855
Ki 8.47 8.47 3.4 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Gonadotropin-releasing hormone receptor Ki = 3.4 nM 8.47 Binding affinity to human GnRHR 18442910

Literature References

PubMed DOI Target Context # Activities
18442910 10.1016/j.bmcl.2008.04.036 Gonadotropin-releasing hormone receptor 1
18442910 10.1016/j.bmcl.2008.04.036 Cytochrome P450 3A4 1

Data from ChEMBL 36 via Core Engine