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Compound Detail

CHEMBL379019

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COc1ccc(C(c2cc3ccc(OC)cc3o2)n2cncn2)cc1

Basic Information

ChEMBL ID CHEMBL379019
Phase Preclinical
Structure Type MOL
InChI Key VUWROJIVKURNQN-UHFFFAOYSA-N
1
Targets
2
Activities
1
Assay Types
0
PK Parameters
7
Publications
0
Known Names

Molecular Properties

335.4
MW (Da)
3.68
ALogP
6
HBA
0
HBD
62.3
PSA (Ų)
0.56
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C19H17N3O3
MW 335.36
Aromatic Rings 4
Heavy Atoms 25
NP-Likeness -0.61

Activity Summary

IC50 2 meas. best 6.89

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Aromatase
CHEMBL1978
IC50 6.89 6.89 130.0 2

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
16451067 10.1021/jm0508282 Aromatase 2
16451067 10.1021/jm0508282 Hepatocyte 2
16451067 10.1021/jm0508282 1,25-dihydroxyvitamin D(3) 24-hydroxylase, mitochondrial 1
16451067 10.1021/jm0508282 Cytochrome P450 26A1 1
16451067 10.1021/jm0508282 17-beta-hydroxysteroid dehydrogenase type 1 1
16451067 10.1021/jm0508282 17-beta-hydroxysteroid dehydrogenase type 3 1
28622580 10.1016/j.ejmech.2017.05.041 Aromatase 1

Data from ChEMBL 36 via Core Engine