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Compound Detail

CHEMBL4778382

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COc1ccc(OC)c2c1c(OC)cc1c(=O)cc(-c3cc(Cl)cc(N4CCN(C)CC4)c3)oc12

Basic Information

ChEMBL ID CHEMBL4778382
Phase Preclinical
Structure Type MOL
InChI Key SEYBJARSCAYWJT-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

495.0
MW (Da)
5.04
ALogP
7
HBA
0
HBD
64.4
PSA (Ų)
0.36
QED
1
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C27H27ClN2O5
MW 494.98
Aromatic Rings 4
Heavy Atoms 35
NP-Likeness -0.16

Activity Summary

IC50 1 meas. best 6.28

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cytochrome P450 1B1
CHEMBL4878
IC50 6.28 6.28 519.4 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Cytochrome P450 1B1 IC50 = 519.4 nM 6.28 Inhibition of recombinant human CYP1B1 using 7-ethoxyresorufin as substrate afte... 33069055

Literature References

PubMed DOI Target Context # Activities
33069055 10.1016/j.ejmech.2020.112895 Unchecked 2
33069055 10.1016/j.ejmech.2020.112895 Cytochrome P450 1B1 1
33069055 10.1016/j.ejmech.2020.112895 Cytochrome P450 1A1 1
33069055 10.1016/j.ejmech.2020.112895 Cytochrome P450 1A2 1

Data from ChEMBL 36 via Core Engine