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Compound Detail

CHEMBL346290

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Cc1ncc(C(OCc2ccc(C#N)cc2-c2ccc3c(c2)OCO3)c2ccc(C#N)cc2)n1C

Basic Information

ChEMBL ID CHEMBL346290
Phase Preclinical
Structure Type MOL
InChI Key KLNLNTKIKMROQI-UHFFFAOYSA-N
1
Targets
2
Activities
2
Assay Types
4
PK Parameters
4
Publications
0
Known Names

Molecular Properties

462.5
MW (Da)
5.17
ALogP
7
HBA
0
HBD
93.1
PSA (Ų)
0.39
QED
1
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C28H22N4O3
MW 462.51
Aromatic Rings 4
Heavy Atoms 35
NP-Likeness -0.57

Activity Summary

EC50 1 meas. best 8.01
IC50 1 meas. best 5.79

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Protein farnesyltransferase
CHEMBL2094108
EC50 8.01 8.01 9.8 1
Protein farnesyltransferase
CHEMBL2094108
IC50 5.79 5.79 1621.8 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 100.0 ng.hr.mL-1 Canis lupus familiaris
CL 31.17 mL.min-1.kg-1 Canis lupus familiaris
F 15.2 % Canis lupus familiaris
T1/2 0.9 hr Canis lupus familiaris

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
14736242 10.1021/jm030434f Canis familiaris 4
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