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Compound Detail

CHEMBL99867

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Cc1ccc(CC(=O)Nc2ccc(NC(=O)[C@@H](N)CS)cc2C(=O)c2ccccc2)cc1.Cl

Basic Information

ChEMBL ID CHEMBL99867
Phase Preclinical
Structure Type MOL
InChI Key RLGVELMPNXASBG-BOXHHOBZSA-N
Parent Compound CHEMBL1179787
Active Moiety CHEMBL1179787
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

447.6
MW (Da)
3.60
ALogP
5
HBA
4
HBD
101.3
PSA (Ų)
0.31
QED
0
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H26ClN3O3S
MW 484.02
Aromatic Rings 3
Heavy Atoms 32
NP-Likeness -1.07

Activity Summary

IC50 1 meas. best 7.11

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Farnesyltransferase
CHEMBL2111393
IC50 7.11 7.11 77.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Farnesyltransferase IC50 = 77.0 nM 7.11 Inhibitory activity against farnesyltransferase. 11520197

Literature References

PubMed DOI Target Context # Activities
11520197 10.1021/jm010872r Farnesyltransferase 1
11520197 10.1021/jm010872r K562 1

Data from ChEMBL 36 via Core Engine