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Compound Detail

CHEMBL187175

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COc1cccc(-c2cc(C#N)ccc2COCc2cncn2Cc2ccc(C#N)cc2)c1

Basic Information

ChEMBL ID CHEMBL187175
Phase Preclinical
Structure Type MOL
InChI Key NUJXPVZUWBELDZ-UHFFFAOYSA-N
3
Targets
3
Activities
2
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

434.5
MW (Da)
5.07
ALogP
6
HBA
0
HBD
83.9
PSA (Ų)
0.39
QED
1
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C27H22N4O2
MW 434.50
Aromatic Rings 4
Heavy Atoms 33
NP-Likeness -0.88

Activity Summary

IC50 2 meas. best 9.34
EC50 1 meas. best 7.5

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Protein farnesyltransferase
CHEMBL2094108
IC50 9.34 9.34 0.5 1
Protein farnesyltransferase
CHEMBL2096912
EC50 7.5 7.5 32.0 1
Geranylgeranyl transferase type I
CHEMBL2095164
IC50 5.0 5.0 10000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
15380198 10.1016/j.bmcl.2004.07.083 Protein farnesyltransferase 2
15380198 10.1016/j.bmcl.2004.07.083 Geranylgeranyl transferase type I 1
15380198 10.1016/j.bmcl.2004.07.083 Protein farnesyl/geranylgeranyl transferase 1

Data from ChEMBL 36 via Core Engine