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Compound Detail

CHEMBL208063

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C=C1/C(=C\C=C2/CCC[C@]3(C)C([C@H](C)OCC(=O)NCC(F)(F)C(F)(F)F)=CCC23)C[C@@H](O)C[C@@H]1O

Basic Information

ChEMBL ID CHEMBL208063
Phase Preclinical
Structure Type MOL
InChI Key SVCSMAZYWOQCBW-UHYXHLJDSA-N
1
Targets
1
Activities
1
Assay Types
2
PK Parameters
6
Publications
0
Known Names

Molecular Properties

519.5
MW (Da)
4.77
ALogP
4
HBA
3
HBD
78.8
PSA (Ų)
0.33
QED
1
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C26H34F5NO4
MW 519.55
Aromatic Rings 0
Heavy Atoms 36
NP-Likeness 1.26

Activity Summary

IC50 1 meas. best 8.72

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Keratinocyte
CHEMBL613995
IC50 8.72 8.72 1.9 1

Pharmacokinetic Data

Parameter Value Units Species
CL 130.88 mL.min-1.kg-1 Rattus norvegicus
CL 278.0 mL.min-1.g-1 Homo sapiens

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Keratinocyte IC50 = 1.9 nM 8.72 Antiproliferative activity against human keratinocyte assessed as inhibition of ... 16630723

Literature References

PubMed DOI Target Context # Activities
16630723 10.1016/j.bmcl.2006.03.014 Mus musculus 2
16630723 10.1016/j.bmcl.2006.03.014 Keratinocyte 2
16630723 10.1016/j.bmcl.2006.03.014 Rattus norvegicus 2
16630723 10.1016/j.bmcl.2006.03.014 Vitamin D3 receptor 1
16630723 10.1016/j.bmcl.2006.03.014 Liver microsomes 1
16630723 10.1016/j.bmcl.2006.03.014 Homo sapiens 1

Data from ChEMBL 36 via Core Engine