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Compound Detail

CHEMBL354588

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COCC[C@H]1CN(C2c3ccc(Cl)cc3CCc3cc(Br)cnc32)CCN1C(=O)Cc1cc[n+]([O-])cc1

Basic Information

ChEMBL ID CHEMBL354588
Phase Preclinical
Structure Type MOL
InChI Key OVQRCNZLFIDOIZ-ZZDYIDRTSA-N
1
Targets
1
Activities
1
Assay Types
2
PK Parameters
2
Publications
0
Known Names

Molecular Properties

585.9
MW (Da)
4.11
ALogP
5
HBA
0
HBD
72.6
PSA (Ų)
0.32
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 C28H30BrClN4O3
MW 585.93
Aromatic Rings 3
Heavy Atoms 37
NP-Likeness -0.83

Activity Summary

IC50 1 meas. best 7.47

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Protein farnesyltransferase
CHEMBL2094108
IC50 7.47 7.47 34.0 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 19900.0 ng.hr.mL-1 Mus musculus
Cmax 9000.0 nM Mus musculus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
9526562 10.1021/jm970462w Mus musculus 3
9526562 10.1021/jm970462w Protein farnesyltransferase 2

Data from ChEMBL 36 via Core Engine