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Compound Detail

CHEMBL131000

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Cn1cncc1C(OCc1c(-c2cccc(F)c2)cc(C#N)c(=O)n1C)c1ccc(C#N)cc1

Basic Information

ChEMBL ID CHEMBL131000
Phase Preclinical
Structure Type MOL
InChI Key IFMBONPPUMOMTJ-UHFFFAOYSA-N
1
Targets
2
Activities
2
Assay Types
2
PK Parameters
4
Publications
0
Known Names

Molecular Properties

453.5
MW (Da)
3.97
ALogP
7
HBA
0
HBD
96.6
PSA (Ų)
0.44
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C26H20FN5O2
MW 453.48
Aromatic Rings 4
Heavy Atoms 34
NP-Likeness -1.09

Activity Summary

EC50 1 meas. best 7.96
IC50 1 meas. best 8.68

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Protein farnesyltransferase
CHEMBL2094108
IC50 8.68 8.68 2.1 1
Protein farnesyltransferase
CHEMBL2094108
EC50 7.96 7.96 11.0 1

Pharmacokinetic Data

Parameter Value Units Species
F 61.0 % Canis lupus familiaris
F 42.0 % Cercopithecidae

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
14592494 10.1016/j.bmcl.2003.08.058 Protein farnesyltransferase 2
14592494 10.1016/j.bmcl.2003.08.058 Geranylgeranyl transferase type I 1
14592494 10.1016/j.bmcl.2003.08.058 Canis familiaris 1
14592494 10.1016/j.bmcl.2003.08.058 ADMET 1

Data from ChEMBL 36 via Core Engine