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Compound Detail

CHEMBL308283

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CSCC[C@H](NC(=O)C1(NC(=O)[C@@H](NC(=O)[C@@H](N)CS)C(C)C)Cc2ccccc2C1)C(=O)O

Basic Information

ChEMBL ID CHEMBL308283
Phase Preclinical
Structure Type BOTH
InChI Key REZJOXXWQFILST-BZSNNMDCSA-N
1
Targets
2
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

510.7
MW (Da)
0.36
ALogP
7
HBA
6
HBD
150.6
PSA (Ų)
0.22
QED
2
Ro5 Violations
12
Rot. Bonds

Drug Information

Molecule Type Protein
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C23H34N4O5S2
MW 510.68
Aromatic Rings 1
Heavy Atoms 34
NP-Likeness -0.23

Activity Summary

IC50 2 meas. best 5.54

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Protein farnesyltransferase
CHEMBL2094108
IC50 5.54 5.54 2900.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Protein farnesyltransferase IC50 = 2900.0 nM 5.54 In vitro inhibitory activity against Farnesyltransferase 8568812

Literature References

PubMed DOI Target Context # Activities
8568812 10.1021/jm950642a Protein farnesyltransferase 1
27690430 10.1021/acs.jmedchem.6b01029 Unchecked 1

Data from ChEMBL 36 via Core Engine