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Compound Detail

CHEMBL5405256

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

Basic Information

ChEMBL ID CHEMBL5405256
Phase Preclinical
Structure Type MOL
InChI Key ABJNKMICWCLJMM-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

584.6
MW (Da)
3.73
ALogP
10
HBA
2
HBD
140.7
PSA (Ų)
0.16
QED
1
Ro5 Violations
15
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C30H33FN2O9
MW 584.60
Aromatic Rings 4
Heavy Atoms 42
NP-Likeness -0.35

Activity Summary

IC50 1 meas. best 8.84

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cytochrome P450 1B1
CHEMBL4878
IC50 8.84 8.84 1.4 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Cytochrome P450 1B1 IC50 = 1.44 nM 8.84 Inhibition of recombinant CYP1B1 (unknown origin) using 7-ethoxyresorufin as sub... 38031326

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