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Compound Detail

CHEMBL357613

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COc1ccccc1N1CCN(CC(O)c2oc3ccccc3c2CCc2ccccc2)CC1

Basic Information

ChEMBL ID CHEMBL357613
Phase Preclinical
Structure Type MOL
InChI Key HJWAAFLBIVYLHY-UHFFFAOYSA-N
2
Targets
2
Activities
2
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

456.6
MW (Da)
5.08
ALogP
5
HBA
1
HBD
49.1
PSA (Ų)
0.40
QED
1
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C29H32N2O3
MW 456.59
Aromatic Rings 4
Heavy Atoms 34
NP-Likeness -0.49

Activity Summary

EC50 1 meas. best 6.75
IC50 1 meas. best 6.06

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
ATP-dependent translocase ABCB1
CHEMBL4302
EC50 6.75 6.75 177.0 1
CCRF-CEM/VCR-1000
CHEMBL614540
IC50 6.06 6.06 880.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
14584949 10.1021/jm030876r No relevant target 2
8941391 10.1021/jm960384x CCRF-CEM 2
14584949 10.1021/jm030876r CCRF-CEM/VCR-1000 1
8941391 10.1021/jm960384x No relevant target 1
17352460 10.1021/jm060604z ATP-dependent translocase ABCB1 1

Data from ChEMBL 36 via Core Engine