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Compound Detail

CHEMBL2282050

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C[C@]12CCC(=O)C=C1CC[C@@H]1[C@@H]2CC[C@]2(C)C(=O)/C(=C/c3cccc(OCCCn4ccnc4)c3)C[C@@H]12

Basic Information

ChEMBL ID CHEMBL2282050
Phase Preclinical
Structure Type MOL
InChI Key ROHZDDWWOUFWCK-WMEBYZSTSA-N
1
Targets
2
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

498.7
MW (Da)
6.45
ALogP
5
HBA
0
HBD
61.2
PSA (Ų)
0.34
QED
1
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C32H38N2O3
MW 498.67
Aromatic Rings 2
Heavy Atoms 37
NP-Likeness 0.33

Activity Summary

IC50 2 meas. best 5.36

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Aromatase
CHEMBL1978
IC50 5.36 5.36 4400.0 2

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Aromatase IC50 = 4400.0 nM 5.36 Inhibition of aromatase in Homo sapiens (human) placental microsome assessed as ... -
Aromatase IC50 = 4400.0 nM 5.36 Inhibition of aromatase (unknown origin) 26301554

Literature References

PubMed DOI Target Context # Activities
- 10.1007/s00044-012-0059-1 Aromatase 2
26301554 10.1016/j.ejmech.2015.08.010 Aromatase 1

Data from ChEMBL 36 via Core Engine