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Compound Detail

CHEMBL178483

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CSCC[C@H](NC(=O)c1ccc(CN[C@H](/C=C/CC(C)C)CC2CCCCC2)cc1-c1ccccc1C)C(=O)[O-].[Li+]

Basic Information

ChEMBL ID CHEMBL178483
Phase Preclinical
Structure Type MOL
InChI Key SIPKBMXEZANOQM-BFRBHUIESA-M
Parent Compound CHEMBL1204532
Active Moiety CHEMBL1204532
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

564.8
MW (Da)
7.63
ALogP
4
HBA
3
HBD
78.4
PSA (Ų)
0.19
QED
2
Ro5 Violations
15
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C34H47LiN2O3S
MW 570.77
Aromatic Rings 2
Heavy Atoms 40
NP-Likeness -0.01

Activity Summary

IC50 1 meas. best 9.66

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Protein farnesyltransferase
CHEMBL2095197
IC50 9.66 9.66 0.2 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Protein farnesyltransferase IC50 = 0.22 nM 9.66 In vitro inhibitory activity against Farnesyltransferase (FTase) 10579847

Literature References

PubMed DOI Target Context # Activities
10579847 10.1021/jm990335v Protein farnesyltransferase 1

Data from ChEMBL 36 via Core Engine