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Compound Detail

CHEMBL41473

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O=C(Cc1cc[n+]([O-])cc1)N1CCC(C2c3ccc(Cl)cc3C=Cc3cc(Br)cnc32)CC1

Basic Information

ChEMBL ID CHEMBL41473
Phase Preclinical
Structure Type MOL
InChI Key FYTHCBFIMNBITR-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
5
PK Parameters
6
Publications
0
Known Names

Molecular Properties

524.9
MW (Da)
5.23
ALogP
3
HBA
0
HBD
60.1
PSA (Ų)
0.35
QED
2
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C26H23BrClN3O2
MW 524.85
Aromatic Rings 3
Heavy Atoms 33
NP-Likeness -0.66

Activity Summary

IC50 2 meas. best 7.52

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Protein farnesyltransferase
CHEMBL2094108
IC50 7.52 7.52 30.0 1
COS-1
CHEMBL614563
IC50 6.16 6.16 700.0 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 19000.0 ng.hr.mL-1 Mus musculus
AUC 18600.0 ng.hr.mL-1 Mus musculus
Cmax 20958.37 nM Mus musculus
F 100.0 % Mus musculus
T1/2 0.4433 hr Mus musculus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Protein farnesyltransferase IC50 = 30.0 nM 7.52 Inhibition of Farnesyltransferase 9572881
COS-1 IC50 = 700.0 nM 6.16 Inhibitory activity was measured against COS cell 9572881

Literature References

PubMed DOI Target Context # Activities
9572881 10.1021/jm980013b Mus musculus 4
9572881 10.1021/jm980013b DLD-1 2
9572881 10.1021/jm980013b Protein farnesyltransferase 1
9572881 10.1021/jm980013b Unchecked 1
9572881 10.1021/jm980013b COS-1 1
9572881 10.1021/jm980013b ADMET 1

Data from ChEMBL 36 via Core Engine