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Compound Detail

CHEMBL155285

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COc1cc2c(cc1OC)CN(CCc1ccc(NC(=O)c3ccccc3NC(=O)c3ccco3)cc1)CC2

Basic Information

ChEMBL ID CHEMBL155285
Phase Preclinical
Structure Type MOL
InChI Key BSJNRONUCRMMKI-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
13
Publications
0
Known Names

Molecular Properties

525.6
MW (Da)
5.40
ALogP
6
HBA
2
HBD
93.0
PSA (Ų)
0.30
QED
2
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C31H31N3O5
MW 525.61
Aromatic Rings 4
Heavy Atoms 39
NP-Likeness -1.25

Activity Summary

IC50 1 meas. best 5.48

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
EMT6
CHEMBL614294
IC50 5.48 5.48 3300.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
EMT6 IC50 = 3300.0 nM 5.48 Reversal effect on the accumulation of [3H]- daunorubicin in mouse mammary carci... 10098671

Literature References

PubMed DOI Target Context # Activities
26197160 10.1016/j.ejmech.2015.06.049 ADMET 7
26197160 10.1016/j.ejmech.2015.06.049 ATP-dependent translocase ABCB1 5
26197160 10.1016/j.ejmech.2015.06.049 Broad substrate specificity ATP-binding cassette transporter ABCG2 4
26197160 10.1016/j.ejmech.2015.06.049 SW-620 3
26197160 10.1016/j.ejmech.2015.06.049 HepG2 3
26197160 10.1016/j.ejmech.2015.06.049 MCF7 2
26197160 10.1016/j.ejmech.2015.06.049 Unchecked 2
10098671 10.1016/s0960-894x(99)00030-x EMT6 1
26197160 10.1016/j.ejmech.2015.06.049 HCT-116 1
26197160 10.1016/j.ejmech.2015.06.049 Hepatocyte 1
26197160 10.1016/j.ejmech.2015.06.049 K562 1
26197160 10.1016/j.ejmech.2015.06.049 Multidrug resistance-associated protein 1 1
26197160 10.1016/j.ejmech.2015.06.049 NON-PROTEIN TARGET 1

Data from ChEMBL 36 via Core Engine