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Compound Detail

CHEMBL526327

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COc1cccc(-c2cn(Cc3c(F)cccc3F)c(=O)n(C[C@H](NCCCC(=O)O)c3ccccc3)c2=O)c1F

Basic Information

ChEMBL ID CHEMBL526327
Phase Preclinical
Structure Type MOL
InChI Key DEOLAXKUWDBBIS-VWLOTQADSA-N
2
Targets
2
Activities
2
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

567.6
MW (Da)
4.35
ALogP
7
HBA
2
HBD
102.6
PSA (Ų)
0.25
QED
1
Ro5 Violations
12
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C30H28F3N3O5
MW 567.56
Aromatic Rings 4
Heavy Atoms 41
NP-Likeness -0.75

Activity Summary

IC50 1 meas. best 4.48
Ki 1 meas. best 7.66

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Gonadotropin-releasing hormone receptor
CHEMBL1855
Ki 7.66 7.66 22.0 1
Cytochrome P450 3A4
CHEMBL340
IC50 4.48 4.48 33000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Gonadotropin-releasing hormone receptor Ki = 22.0 nM 7.66 Binding affinity to human GnRHR 18442910
Cytochrome P450 3A4 IC50 = 33000.0 nM 4.48 Inhibition of CYP3A4 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