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Compound Detail

CHEMBL207638

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C[C@H]([C@@H](c1ccc2cc(OCC3(C(=O)O)CCCCC3)ccc2c1)n1ccnc1)N(C)C

Basic Information

ChEMBL ID CHEMBL207638
Phase Preclinical
Structure Type MOL
InChI Key VZAYORFJMPOFKB-DVECYGJZSA-N
2
Targets
2
Activities
1
Assay Types
4
PK Parameters
7
Publications
0
Known Names

Molecular Properties

435.6
MW (Da)
4.99
ALogP
5
HBA
1
HBD
67.6
PSA (Ų)
0.54
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 C26H33N3O3
MW 435.57
Aromatic Rings 3
Heavy Atoms 32
NP-Likeness -0.22

Activity Summary

IC50 2 meas. best 7.95

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cytochrome P450 26A1
CHEMBL5141
IC50 7.95 7.95 11.2 1
Cytochrome P450 3A4
CHEMBL340
IC50 5.1 5.1 8000.0 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 17492.0 ng.hr.mL-1 Mus musculus
Cmax 23000.0 nM Mus musculus
F 99.0 % Mus musculus
T1/2 2.46 hr Mus musculus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Cytochrome P450 26A1 IC50 = 11.2 nM 7.95 Inhibition of CYP26 expressed in human T47D cell line 16504501
Cytochrome P450 3A4 IC50 = 8000.0 nM 5.1 Inhibition of CYP3A4 16504501

Literature References

PubMed DOI Target Context # Activities
16504501 10.1016/j.bmcl.2006.02.020 Mus musculus 4
16504501 10.1016/j.bmcl.2006.02.020 Cytochrome P450 26A1 1
16504501 10.1016/j.bmcl.2006.02.020 Cytochrome P450 3A4 1
16504501 10.1016/j.bmcl.2006.02.020 T47D 1
16504501 10.1016/j.bmcl.2006.02.020 Cytochrome P450 1A2 1
16504501 10.1016/j.bmcl.2006.02.020 Cytochrome P450 2D6 1
16504501 10.1016/j.bmcl.2006.02.020 Cytochrome P450 2C9 1

Data from ChEMBL 36 via Core Engine