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Compound Detail

CHEMBL499026

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N[C@@H](Cn1c(=O)c(-c2ccc(COC(=O)CO)cc2)cn(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1

Basic Information

ChEMBL ID CHEMBL499026
Phase Preclinical
Structure Type MOL
InChI Key KCCHSZZXJXIDAP-VWLOTQADSA-N
2
Targets
2
Activities
2
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

571.5
MW (Da)
3.62
ALogP
8
HBA
2
HBD
116.5
PSA (Ų)
0.23
QED
1
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C29H25F4N3O5
MW 571.53
Aromatic Rings 4
Heavy Atoms 41
NP-Likeness -0.70

Activity Summary

IC50 1 meas. best 6.92
Ki 1 meas. best 8.0

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Gonadotropin-releasing hormone receptor
CHEMBL1855
Ki 8.0 8.0 10.0 1
Cytochrome P450 3A4
CHEMBL340
IC50 6.92 6.92 120.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Gonadotropin-releasing hormone receptor Ki = 10.0 nM 8.0 Binding affinity to human GnRHR 18442910
Cytochrome P450 3A4 IC50 = 120.0 nM 6.92 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