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Compound Detail

CHEMBL158333

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Cn1cncc1C(OCc1ccc(C#N)cc1NS(=O)(=O)c1cccc2ccccc12)c1ccc(C#N)cc1

Basic Information

ChEMBL ID CHEMBL158333
Phase Preclinical
Structure Type MOL
InChI Key AKKQWZHJOANNGA-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

533.6
MW (Da)
5.42
ALogP
7
HBA
1
HBD
120.8
PSA (Ų)
0.28
QED
2
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C30H23N5O3S
MW 533.61
Aromatic Rings 5
Heavy Atoms 39
NP-Likeness -1.28

Activity Summary

IC50 1 meas. best 5.58

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Protein farnesyltransferase
CHEMBL2094108
IC50 5.58 5.58 2630.3 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Protein farnesyltransferase IC50 = 2630.27 nM 5.58 Inhibition of FTase 16455255

Literature References

PubMed DOI Target Context # Activities
14736242 10.1021/jm030434f Protein farnesyltransferase 2
14736242 10.1021/jm030434f Geranylgeranyl transferase type I 1
16455255 10.1016/j.bmcl.2006.01.019 Protein farnesyltransferase 1

Data from ChEMBL 36 via Core Engine