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Compound Detail

CHEMBL5429019

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COc1ccc(OC)c2c1c(OC)cc1c(=O)cc(-c3cc(F)cc(NC(=O)COCCOCCN)c3)oc12

Basic Information

ChEMBL ID CHEMBL5429019
Phase Preclinical
Structure Type MOL
InChI Key XEFZSLVMWYLTMA-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

540.5
MW (Da)
3.71
ALogP
9
HBA
2
HBD
131.5
PSA (Ų)
0.20
QED
1
Ro5 Violations
12
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C28H29FN2O8
MW 540.54
Aromatic Rings 4
Heavy Atoms 39
NP-Likeness -0.38

Activity Summary

IC50 2 meas. best 8.35

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cytochrome P450 1B1
CHEMBL4878
IC50 8.35 8.35 4.4 1
Cytochrome P450 1A1
CHEMBL2231
IC50 5.97 5.97 1060.9 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
38031326 10.1021/acs.jmedchem.3c01474 Unchecked 2
38031326 10.1021/acs.jmedchem.3c01474 Cytochrome P450 1B1 1
38031326 10.1021/acs.jmedchem.3c01474 Cytochrome P450 1A1 1
38031326 10.1021/acs.jmedchem.3c01474 Cytochrome P450 1A2 1

Data from ChEMBL 36 via Core Engine