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Compound Detail

CHEMBL5407291

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COc1cc(CC(=O)OCc2c(OC(C)C)ccc3c(C)c(Cc4ccccc4)c(=O)oc23)cc(OC)c1OC

Basic Information

ChEMBL ID CHEMBL5407291
Phase Preclinical
Structure Type MOL
InChI Key SPOSWQWTHALSRX-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
7
Publications
0
Known Names

Molecular Properties

546.6
MW (Da)
5.79
ALogP
8
HBA
0
HBD
93.4
PSA (Ų)
0.17
QED
2
Ro5 Violations
11
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C32H34O8
MW 546.62
Aromatic Rings 4
Heavy Atoms 40
NP-Likeness -0.12

Activity Summary

IC50 1 meas. best 8.0

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
A2780/Taxol
CHEMBL4483224
IC50 8.0 8.0 10.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
A2780/Taxol IC50 = 10.0 nM 8.0 Reversal of multi-drug resistance in human A2780/Taxol cells incubated for 48 hr... 36871374

Literature References

PubMed DOI Target Context # Activities
36871374 10.1016/j.ejmech.2023.115218 ATP-dependent translocase ABCB1 6
36871374 10.1016/j.ejmech.2023.115218 A2780/Taxol 5
36871374 10.1016/j.ejmech.2023.115218 ADMET 4
36871374 10.1016/j.ejmech.2023.115218 Unchecked 2
36871374 10.1016/j.ejmech.2023.115218 Voltage-gated inwardly rectifying potassium channel KCNH2 2
36871374 10.1016/j.ejmech.2023.115218 No relevant target 2
36871374 10.1016/j.ejmech.2023.115218 A2780 1

Data from ChEMBL 36 via Core Engine