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Compound Detail

CHEMBL2449384

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O=C(CCc1ccccc1)c1cc(OCc2ccccc2)ccc1OC[C@H](O)CN1CCN(Cc2ccccc2)CC1

Basic Information

ChEMBL ID CHEMBL2449384
Phase Preclinical
Structure Type MOL
InChI Key GUKJTWYUEMCIOS-JGCGQSQUSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

564.7
MW (Da)
5.64
ALogP
6
HBA
1
HBD
62.2
PSA (Ų)
0.20
QED
2
Ro5 Violations
14
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C36H40N2O4
MW 564.73
Aromatic Rings 4
Heavy Atoms 42
NP-Likeness -0.68

Activity Summary

EC50 1 meas. best 6.94

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
ATP-dependent translocase ABCB1
CHEMBL4302
EC50 6.94 6.94 114.8 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
ATP-dependent translocase ABCB1 EC50 = 114.82 nM 6.94 SUPPLEMENTARY: Inhibition of P-glycoprotein expressed in MDR CCRF vcr1000 cells ... -

Literature References

PubMed DOI Target Context # Activities
- 10.6019/CHEMBL2449286 ATP-dependent translocase ABCB1 1

Data from ChEMBL 36 via Core Engine