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Compound Detail

CHEMBL131170

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Cn1cncc1C(OCc1c(-c2ccc3c(c2)OC(F)(F)O3)cc(C#N)c(=O)n1C)c1ccc(C#N)cc1

Basic Information

ChEMBL ID CHEMBL131170
Phase Preclinical
Structure Type MOL
InChI Key ONSUIKYVBGOGPD-UHFFFAOYSA-N
2
Targets
3
Activities
2
Assay Types
2
PK Parameters
4
Publications
0
Known Names

Molecular Properties

515.5
MW (Da)
4.16
ALogP
9
HBA
0
HBD
115.1
PSA (Ų)
0.38
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 C27H19F2N5O4
MW 515.48
Aromatic Rings 4
Heavy Atoms 38
NP-Likeness -0.83

Activity Summary

IC50 2 meas. best 9.16
EC50 1 meas. best 7.72

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Protein farnesyltransferase
CHEMBL2094108
IC50 9.16 9.16 0.7 1
Protein farnesyltransferase
CHEMBL2094108
EC50 7.72 7.72 19.0 1
Geranylgeranyl transferase type I
CHEMBL2095164
IC50 5.21 5.21 6200.0 1

Pharmacokinetic Data

Parameter Value Units Species
F 63.0 % Canis lupus familiaris
F 34.0 % 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