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Compound Detail

CHEMBL4449332

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Cc1c(N2CCN(Cc3ccc(C(F)(F)F)o3)CC2)c(=O)n(C[C@H](NCCCC(=O)O)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F

Basic Information

ChEMBL ID CHEMBL4449332
Phase Preclinical
Structure Type MOL
InChI Key JLKXURLUTOXXPN-NDEPHWFRSA-N
3
Targets
9
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

739.7
MW (Da)
5.65
ALogP
9
HBA
2
HBD
113.0
PSA (Ų)
0.13
QED
2
Ro5 Violations
13
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C35H36F7N5O5
MW 739.69
Aromatic Rings 4
Heavy Atoms 52
NP-Likeness -1.01

Activity Summary

IC50 9 meas. best 9.36

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Gonadotropin-releasing hormone receptor
CHEMBL1855
IC50 9.36 8.622 0.4 5
Gonadotropin-releasing hormone receptor
CHEMBL5647
IC50 8.43 8.155 3.7 2
Gonadotropin-releasing hormone receptor
CHEMBL3066
IC50 6.55 6.415 279.2 2

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
27608177 10.1021/acs.jmedchem.6b01071 Gonadotropin-releasing hormone receptor 9
27608177 10.1021/acs.jmedchem.6b01071 Unchecked 2
27608177 10.1021/acs.jmedchem.6b01071 Cytochrome P450 3A4 1

Data from ChEMBL 36 via Core Engine