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Compound Detail

CHEMBL207304

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CC(C)N(C)[C@H](C)[C@@H](c1ccc2cc(OCC3(C(=O)O)CCCC3)ccc2c1)n1ccnc1

Basic Information

ChEMBL ID CHEMBL207304
Phase Preclinical
Structure Type MOL
InChI Key MYLJXYCXVOMQPS-NLFFAJNJSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

449.6
MW (Da)
5.38
ALogP
5
HBA
1
HBD
67.6
PSA (Ų)
0.48
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 C27H35N3O3
MW 449.60
Aromatic Rings 3
Heavy Atoms 33
NP-Likeness -0.31

Activity Summary

IC50 2 meas. best 8.8

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cytochrome P450 26A1
CHEMBL5141
IC50 8.8 8.8 1.6 1
Cytochrome P450 3A4
CHEMBL340
IC50 6.1 6.1 800.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Cytochrome P450 26A1 IC50 = 1.6 nM 8.8 Inhibition of CYP26 expressed in human T47D cell line 16504501
Cytochrome P450 3A4 IC50 = 800.0 nM 6.1 Inhibition of CYP3A4 16504501

Literature References

PubMed DOI Target Context # Activities
16504501 10.1016/j.bmcl.2006.02.020 Cytochrome P450 26A1 1
16504501 10.1016/j.bmcl.2006.02.020 Cytochrome P450 3A4 1

Data from ChEMBL 36 via Core Engine