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Compound Detail

CHEMBL431632

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Cl.N[C@@H](CS)C(=O)Nc1ccc(NC(=O)C(c2ccccc2)c2ccccc2)c(C(=O)c2ccccc2)c1

Basic Information

ChEMBL ID CHEMBL431632
Phase Preclinical
Structure Type MOL
InChI Key GNSPLSWKGNLIOS-UQIIZPHYSA-N
Parent Compound CHEMBL1185755
Active Moiety CHEMBL1185755
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

509.6
MW (Da)
4.88
ALogP
5
HBA
4
HBD
101.3
PSA (Ų)
0.19
QED
1
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C30H28ClN3O3S
MW 546.09
Aromatic Rings 4
Heavy Atoms 37
NP-Likeness -0.74

Activity Summary

IC50 1 meas. best 7.44

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Farnesyltransferase
CHEMBL2111393
IC50 7.44 7.44 36.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Farnesyltransferase IC50 = 36.0 nM 7.44 Inhibitory activity against farnesyltransferase. 11520197

Literature References

PubMed DOI Target Context # Activities
11520197 10.1021/jm010872r Farnesyltransferase 1

Data from ChEMBL 36 via Core Engine