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Compound Detail

CHEMBL30270

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N#Cc1ccc(Cn2cncc2CN2CCN(c3cccc(Cl)c3)C(=O)C2)cc1Oc1cccnc1

Basic Information

ChEMBL ID CHEMBL30270
Phase Preclinical
Structure Type MOL
InChI Key YRERXVCECMZRBL-UHFFFAOYSA-N
2
Targets
3
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

499.0
MW (Da)
4.49
ALogP
7
HBA
0
HBD
87.3
PSA (Ų)
0.37
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C27H23ClN6O2
MW 498.97
Aromatic Rings 4
Heavy Atoms 36
NP-Likeness -1.82

Activity Summary

IC50 3 meas. best 7.77

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Protein farnesyltransferase
CHEMBL2094108
IC50 7.77 6.365 17.0 2
Geranylgeranyl transferase type I
CHEMBL2095164
IC50 4.28 4.28 52000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
11378366 10.1016/s0960-894x(01)00240-2 Protein farnesyltransferase 2
11378366 10.1016/s0960-894x(01)00240-2 Geranylgeranyl transferase type I 2

Data from ChEMBL 36 via Core Engine