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Compound Detail

CHEMBL257848

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COc1ccc([C@@H]2[C@@H]([C@H](O)CCc3ccccc3)OC(=O)N2c2ccc(F)cc2)c(O)c1

Basic Information

ChEMBL ID CHEMBL257848
Phase Preclinical
Structure Type MOL
InChI Key VUKKLODPZNJDBU-GMKZXUHWSA-N
1
Targets
1
Activities
1
Assay Types
1
PK Parameters
3
Publications
0
Known Names

Molecular Properties

437.5
MW (Da)
4.60
ALogP
5
HBA
2
HBD
79.2
PSA (Ų)
0.56
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 C25H24FNO5
MW 437.47
Aromatic Rings 3
Heavy Atoms 32
NP-Likeness 0.17

Activity Summary

Ki 1 meas. best 5.32

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
NPC1-like intracellular cholesterol transporter 1
CHEMBL5161
Ki 5.32 5.32 4800.0 1

Pharmacokinetic Data

Parameter Value Units Species
T1/2 4.15 hr Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
18063367 10.1016/j.bmcl.2007.11.083 NPC1-like intracellular cholesterol transporter 1 1
18063367 10.1016/j.bmcl.2007.11.083 Hamster 1
18063367 10.1016/j.bmcl.2007.11.083 Liver 1

Data from ChEMBL 36 via Core Engine