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Compound Detail

CHEMBL4074105

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C#CCOc1ccc(-c2nc3ccccc3c(=O)[nH]2)cc1

Basic Information

ChEMBL ID CHEMBL4074105
Phase Preclinical
Structure Type MOL
InChI Key OGSJBMHENPCLPK-UHFFFAOYSA-N
3
Targets
7
Activities
1
Assay Types
0
PK Parameters
7
Publications
0
Known Names

Molecular Properties

276.3
MW (Da)
2.60
ALogP
3
HBA
1
HBD
55.0
PSA (Ų)
0.75
QED
0
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C17H12N2O2
MW 276.30
Aromatic Rings 3
Heavy Atoms 21
NP-Likeness -1.24

Activity Summary

IC50 7 meas. best 8.7

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cytochrome P450 1B1
CHEMBL4878
IC50 8.7 7.7867 2.0 3
Cytochrome P450 1A1
CHEMBL2231
IC50 6.1 5.975 790.0 2
Cytochrome P450 1A2
CHEMBL3356
IC50 5.0 5.0 10000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
28259840 10.1016/j.ejmech.2017.02.032 Cytochrome P450 1A1 6
28259840 10.1016/j.ejmech.2017.02.032 Cytochrome P450 1B1 6
28259840 10.1016/j.ejmech.2017.02.032 Cytochrome P450 1A2 2
28259840 10.1016/j.ejmech.2017.02.032 Cytochrome P450 2D6 2
28259840 10.1016/j.ejmech.2017.02.032 Cytochrome P450 3A4 2
28259840 10.1016/j.ejmech.2017.02.032 Cytochrome P450 2C9 2
28259840 10.1016/j.ejmech.2017.02.032 Cytochrome P450 2C19 2

Data from ChEMBL 36 via Core Engine