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Compound Detail

CHEMBL138719

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COC(=O)[C@H](CCSC)NC(=O)c1ccc(CNCc2c[nH]cn2)cc1-c1ccccc1C

Basic Information

ChEMBL ID CHEMBL138719
Phase Preclinical
Structure Type MOL
InChI Key KZCMMZOLCBZLNG-QHCPKHFHSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
7
Publications
0
Known Names

Molecular Properties

466.6
MW (Da)
3.70
ALogP
6
HBA
3
HBD
96.1
PSA (Ų)
0.37
QED
0
Ro5 Violations
11
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H30N4O3S
MW 466.61
Aromatic Rings 3
Heavy Atoms 33
NP-Likeness -0.87

Activity Summary

IC50 2 meas. best 7.7

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Protein farnesyltransferase
CHEMBL2096912
IC50 7.7 7.7 20.0 1
Protein farnesyltransferase
CHEMBL2094108
IC50 4.47 4.47 34000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
11277514 10.1016/s0960-894x(01)00055-5 Plasmodium falciparum 2
11277514 10.1016/s0960-894x(01)00055-5 Protein farnesyltransferase 2
14711313 10.1021/jm030236o Protein farnesyltransferase 1
14711313 10.1021/jm030236o Trypanosoma brucei brucei 1
14711313 10.1021/jm030236o Trypanosoma brucei rhodesiense 1
14711313 10.1021/jm030236o NIH3T3 1
23953690 10.1016/j.bmc.2013.07.039 HT-1080 1

Data from ChEMBL 36 via Core Engine