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Compound Detail

CHEMBL53732

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COC(=O)c1cccc(-c2ccc(NC[C@@H](N)CS)cc2)c1

Basic Information

ChEMBL ID CHEMBL53732
Phase Preclinical
Structure Type MOL
InChI Key XJBBINSSZZHBDZ-OAHLLOKOSA-N
2
Targets
3
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

316.4
MW (Da)
2.81
ALogP
5
HBA
3
HBD
64.3
PSA (Ų)
0.57
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C17H20N2O2S
MW 316.43
Aromatic Rings 2
Heavy Atoms 22
NP-Likeness -0.54

Activity Summary

IC50 3 meas. best 6.04

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Protein farnesyltransferase
CHEMBL2094108
IC50 6.04 6.035 917.0 2
Geranylgeranyl transferase type I
CHEMBL2095164
IC50 4.0 4.0 100000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
8568811 10.1021/jm950414g Protein farnesyltransferase 1
8568811 10.1021/jm950414g Geranylgeranyl transferase type I 1
11754590 10.1021/jm0103099 Protein farnesyltransferase 1
11754590 10.1021/jm0103099 Geranylgeranyl transferase type I 1

Data from ChEMBL 36 via Core Engine