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Compound Detail

CHEMBL595816

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COc1ccc(/C=C/C(=O)c2ccc(OC)c(OC)c2)cc1OC

Basic Information

ChEMBL ID CHEMBL595816
Phase Preclinical
Structure Type MOL
InChI Key NLVWDGQCMVBWDD-VMPITWQZSA-N
2
Targets
5
Activities
1
Assay Types
0
PK Parameters
13
Publications
0
Known Names

Molecular Properties

328.4
MW (Da)
3.62
ALogP
5
HBA
0
HBD
54.0
PSA (Ų)
0.57
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 C19H20O5
MW 328.36
Aromatic Rings 2
Heavy Atoms 24
NP-Likeness 0.01

Activity Summary

IC50 5 meas. best 5.66

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
K562
CHEMBL385
IC50 5.66 5.66 2200.0 1
Broad substrate specificity ATP-binding cassette transporter ABCG2
CHEMBL5393
IC50 5.48 5.3967 3280.0 3

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
28256373 10.1016/j.bmcl.2017.02.038 RAW264.7 9
24275249 10.1016/j.ejmech.2013.10.073 Molecular identity unknown 4
22112540 10.1016/j.bmc.2011.10.074 Broad substrate specificity ATP-binding cassette transporter ABCG2 2
31610374 10.1016/j.ejmech.2019.111752 No relevant target 2
19837593 10.1016/j.bmc.2009.09.039 K562 1
20060305 10.1016/j.bmc.2009.12.045 HCT-116 1
22112540 10.1016/j.bmc.2011.10.074 ATP-dependent translocase ABCB1 1
22112540 10.1016/j.bmc.2011.10.074 Multidrug resistance-associated protein 1 1
27100033 10.1016/j.ejmech.2016.03.067 Broad substrate specificity ATP-binding cassette transporter ABCG2 1
28242551 10.1016/j.ejmech.2017.02.007 Unchecked 1
31610374 10.1016/j.ejmech.2019.111752 Unchecked 1
31610374 10.1016/j.ejmech.2019.111752 MCF7 1
31610374 10.1016/j.ejmech.2019.111752 NCI-H460 1

Data from ChEMBL 36 via Core Engine