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Compound Detail

CHEMBL4740121

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COc1c(-c2cc(-c3ccccc3)n(-c3ccc(C#N)cc3)n2)ccc2occc12

Basic Information

ChEMBL ID CHEMBL4740121
Phase Preclinical
Structure Type MOL
InChI Key MEXURXCEUNSVJA-UHFFFAOYSA-N
2
Targets
3
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

391.4
MW (Da)
5.83
ALogP
5
HBA
0
HBD
64.0
PSA (Ų)
0.39
QED
1
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H17N3O2
MW 391.43
Aromatic Rings 5
Heavy Atoms 30
NP-Likeness -0.73

Activity Summary

IC50 3 meas. best 6.55

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cytochrome P450 1A1
CHEMBL2231
IC50 6.55 6.43 280.0 2
Cytochrome P450 1B1
CHEMBL4878
IC50 5.24 5.24 5700.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
30448188 10.1016/j.bmc.2018.11.013 Cytochrome P450 1A1 5
30448188 10.1016/j.bmc.2018.11.013 Cytochrome P450 1B1 2

Data from ChEMBL 36 via Core Engine