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Compound Detail

CHEMBL185816

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C[S+]([O-])CC[C@H](NC(=O)[C@H]1O[C@@H](CNC(=O)[C@@H](N)CSSC(C)(C)C)CC[C@@H]1OCc1ccccc1)C(=O)O

Basic Information

ChEMBL ID CHEMBL185816
Phase Preclinical
Structure Type MOL
InChI Key ORZKKQUVLOUJDP-XOUJPBFKSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

603.8
MW (Da)
2.08
ALogP
9
HBA
4
HBD
163.0
PSA (Ų)
0.17
QED
1
Ro5 Violations
15
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C26H41N3O7S3
MW 603.83
Aromatic Rings 1
Heavy Atoms 39
NP-Likeness 0.35

Activity Summary

IC50 1 meas. best 5.66

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Protein farnesyltransferase
CHEMBL2094108
IC50 5.66 5.66 2200.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Protein farnesyltransferase IC50 = 2200.0 nM 5.66 Inhibition of [3H]FPP incorporation by Protein Farnesyltransferase 15267228

Literature References

PubMed DOI Target Context # Activities
15267228 10.1021/jm049927q Protein farnesyltransferase 1
15267228 10.1021/jm049927q Geranylgeranyl transferase type I 1

Data from ChEMBL 36 via Core Engine