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Compound Detail

CHEMBL365362

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Cn1c(=O)cc(-c2cccc(Cl)c2)c2cc(C(NC=O)c3cncn3Cc3ccc(C#N)cc3)ccc21

Basic Information

ChEMBL ID CHEMBL365362
Phase Preclinical
Structure Type MOL
InChI Key JHZVNQFWHURWJH-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

508.0
MW (Da)
4.81
ALogP
6
HBA
1
HBD
92.7
PSA (Ų)
0.32
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 C29H22ClN5O2
MW 507.98
Aromatic Rings 5
Heavy Atoms 37
NP-Likeness -1.10

Activity Summary

IC50 2 meas. best 8.68

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Protein farnesyltransferase
CHEMBL2095178
IC50 8.68 8.68 2.1 1
Unchecked
CHEMBL612545
IC50 8.68 8.68 2.1 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Protein farnesyltransferase IC50 = 2.1 nM 8.68 Inhibition of bovine farnesyltransferase 15808463
Unchecked IC50 = 2.089 nM 8.68 Inhibition of FTase 19515462

Literature References

PubMed DOI Target Context # Activities
15808463 10.1016/j.bmcl.2005.02.062 Protein farnesyltransferase 2
15808463 10.1016/j.bmcl.2005.02.062 Geranylgeranyl transferase type I 1
19515462 10.1016/j.ejmech.2009.04.045 Unchecked 1

Data from ChEMBL 36 via Core Engine