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Compound Detail

CHEMBL380451

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CC1(c2cccc3ccccc23)C(=O)N(CCCn2ccnc2)C(=O)N1Cc1cccc(Oc2ccccc2)c1

Basic Information

ChEMBL ID CHEMBL380451
Phase Preclinical
Structure Type MOL
InChI Key PPUPMAFZXZRFPN-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

530.6
MW (Da)
6.60
ALogP
5
HBA
0
HBD
67.7
PSA (Ų)
0.20
QED
2
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C33H30N4O3
MW 530.63
Aromatic Rings 5
Heavy Atoms 40
NP-Likeness -0.97

Activity Summary

IC50 1 meas. best 9.14

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Protein farnesyltransferase
CHEMBL2094108
IC50 9.14 9.14 0.7 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Protein farnesyltransferase IC50 = 0.72 nM 9.14 Inhibition of farnesyl transferase 16442288

Literature References

PubMed DOI Target Context # Activities
16442288 10.1016/j.bmcl.2005.12.074 Protein farnesyltransferase 1

Data from ChEMBL 36 via Core Engine