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Compound Detail

CHEMBL363751

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N#Cc1ccc(COCc2cncn2Cc2ccc(C#N)cc2-c2ccc3c(c2)OCO3)c(-c2ccc3c(c2)OCO3)c1

Basic Information

ChEMBL ID CHEMBL363751
Phase Preclinical
Structure Type MOL
InChI Key GQYPRGGNCKGHIV-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

568.6
MW (Da)
6.18
ALogP
9
HBA
0
HBD
111.5
PSA (Ų)
0.22
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 C34H24N4O5
MW 568.59
Aromatic Rings 5
Heavy Atoms 43
NP-Likeness -0.47

Activity Summary

IC50 2 meas. best 6.47

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Protein farnesyltransferase
CHEMBL2095178
IC50 6.47 6.47 340.0 1
Unchecked
CHEMBL612545
IC50 6.46 6.46 346.7 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Protein farnesyltransferase IC50 = 340.0 nM 6.47 Inhibition of bovine farnesyltransferase 15454229
Unchecked IC50 = 346.74 nM 6.46 Inhibition of FTase 19515462

Literature References

PubMed DOI Target Context # Activities
15454229 10.1016/j.bmcl.2004.08.011 Protein farnesyltransferase 2
15454229 10.1016/j.bmcl.2004.08.011 Geranylgeranyl transferase type I 1
19515462 10.1016/j.ejmech.2009.04.045 Unchecked 1

Data from ChEMBL 36 via Core Engine