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Compound Detail

CHEMBL2449435

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Cc1cccc(N2CCN(C[C@@H](O)COc3ccccc3C(=O)CCc3ccccc3)CC2)c1C

Basic Information

ChEMBL ID CHEMBL2449435
Phase Preclinical
Structure Type MOL
InChI Key DXOBZGMBGHYACS-AREMUKBSSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

472.6
MW (Da)
4.68
ALogP
5
HBA
1
HBD
53.0
PSA (Ų)
0.43
QED
0
Ro5 Violations
10
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C30H36N2O3
MW 472.63
Aromatic Rings 3
Heavy Atoms 35
NP-Likeness -0.95

Activity Summary

EC50 1 meas. best 8.25

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
ATP-dependent translocase ABCB1
CHEMBL4302
EC50 8.25 8.25 5.6 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
ATP-dependent translocase ABCB1 EC50 = 5.623 nM 8.25 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