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Compound Detail

CHEMBL4852415

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COc1ccc(-c2ccnc(Nc3cc(C(=O)Nc4ccc(CCN5CCc6cc(OC)c(OC)cc6C5)cc4)ccc3C)n2)cc1

Basic Information

ChEMBL ID CHEMBL4852415
Phase Preclinical
Structure Type MOL
InChI Key DVKDXMRTPUTJOG-UHFFFAOYSA-N
1
Targets
2
Activities
1
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

629.8
MW (Da)
7.07
ALogP
8
HBA
2
HBD
97.8
PSA (Ų)
0.16
QED
2
Ro5 Violations
11
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C38H39N5O4
MW 629.76
Aromatic Rings 5
Heavy Atoms 47
NP-Likeness -1.21

Activity Summary

IC50 2 meas. best 7.79

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Unchecked
CHEMBL612545
IC50 7.79 7.79 16.2 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Unchecked IC50 = 16.24 nM 7.79 Reversal of BCRP-mediated multidrug resistance in MDCK-II cells assessed as pote... 33938746

Literature References

PubMed DOI Target Context # Activities
33938746 10.1021/acs.jmedchem.1c00246 MDCK-II 2
33938746 10.1021/acs.jmedchem.1c00246 ATP-dependent translocase ABCB1 2
33938746 10.1021/acs.jmedchem.1c00246 Unchecked 2
33938746 10.1021/acs.jmedchem.1c00246 K562 1
33938746 10.1021/acs.jmedchem.1c00246 K562/A02 1
33938746 10.1021/acs.jmedchem.1c00246 No relevant target 1

Data from ChEMBL 36 via Core Engine