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Compound Detail

CHEMBL185058

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N#Cc1ccc(COCc2cncn2Cc2ccc(C#N)nc2)c(-c2cccc(Cl)c2)c1

Basic Information

ChEMBL ID CHEMBL185058
Phase Preclinical
Structure Type MOL
InChI Key LFWOYECGWXQDAT-UHFFFAOYSA-N
2
Targets
3
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

439.9
MW (Da)
5.11
ALogP
6
HBA
0
HBD
87.5
PSA (Ų)
0.40
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 C25H18ClN5O
MW 439.91
Aromatic Rings 4
Heavy Atoms 32
NP-Likeness -1.15

Activity Summary

IC50 3 meas. best 8.52

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Protein farnesyltransferase
CHEMBL2095178
IC50 8.52 8.52 3.0 1
Unchecked
CHEMBL612545
IC50 8.52 8.52 3.0 2

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Protein farnesyltransferase IC50 = 3.0 nM 8.52 Inhibition of bovine farnesyltransferase 15454229
Unchecked IC50 = 3.02 nM 8.52 Inhibition of FTase 19515462
Unchecked IC50 = 3.02 nM 8.52 Inhibition of farnesyltransferase 17448576

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
17448576 10.1016/j.ejmech.2007.02.003 Unchecked 1

Data from ChEMBL 36 via Core Engine