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Compound Detail

CHEMBL497747

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NCc1ccc(-c2cn(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)cc1

Basic Information

ChEMBL ID CHEMBL497747
Phase Preclinical
Structure Type MOL
InChI Key NKSITFUAIXVDAQ-DEOSSOPVSA-N
2
Targets
2
Activities
2
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

512.5
MW (Da)
4.04
ALogP
6
HBA
2
HBD
96.0
PSA (Ų)
0.37
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 C27H24F4N4O2
MW 512.51
Aromatic Rings 4
Heavy Atoms 37
NP-Likeness -0.90

Activity Summary

IC50 1 meas. best 5.04
Ki 1 meas. best 5.96

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Gonadotropin-releasing hormone receptor
CHEMBL1855
Ki 5.96 5.96 1100.0 1
Cytochrome P450 3A4
CHEMBL340
IC50 5.04 5.04 9100.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Gonadotropin-releasing hormone receptor Ki = 1100.0 nM 5.96 Binding affinity to human GnRHR 18442910
Cytochrome P450 3A4 IC50 = 9100.0 nM 5.04 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