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Compound Detail

CHEMBL346696

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COc1cccc(-c2cc(N)ccc2COC(c2ccc(C#N)cc2)c2cncn2C)c1

Basic Information

ChEMBL ID CHEMBL346696
Phase Preclinical
Structure Type MOL
InChI Key NVTDTBWAXYAWGW-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

424.5
MW (Da)
4.86
ALogP
6
HBA
1
HBD
86.1
PSA (Ų)
0.43
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C26H24N4O2
MW 424.50
Aromatic Rings 4
Heavy Atoms 32
NP-Likeness -0.76

Activity Summary

IC50 2 meas. best 7.4

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Unchecked
CHEMBL612545
IC50 7.4 7.4 40.0 1
Protein farnesyltransferase
CHEMBL2094108
IC50 4.39 4.39 40738.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Unchecked IC50 = 40.0 nM 7.4 Inhibition of FTase 17236767
Protein farnesyltransferase IC50 = 40738.03 nM 4.39 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
17236767 10.1016/j.bmcl.2006.12.087 Unchecked 1

Data from ChEMBL 36 via Core Engine