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Compound Detail

CHEMBL3623213

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C[C@]12CCC(=O)C=C1CC[C@@H]1[C@@H]2CC[C@]2(C)C(=O)[C@@H](n3ccnc3)C[C@@H]12

Basic Information

ChEMBL ID CHEMBL3623213
Phase Preclinical
Structure Type MOL
InChI Key FJTZEZQHMRVBGI-RMLDPDKQSA-N
1
Targets
3
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

352.5
MW (Da)
4.14
ALogP
4
HBA
0
HBD
52.0
PSA (Ų)
0.76
QED
0
Ro5 Violations
1
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H28N2O2
MW 352.48
Aromatic Rings 1
Heavy Atoms 26
NP-Likeness 1.31

Activity Summary

IC50 3 meas. best 6.75

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Aromatase
CHEMBL1978
IC50 6.75 6.75 179.9 3

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Aromatase IC50 = 180.0 nM 6.75 Inhibition of aromatase (unknown origin) 26301554
Aromatase IC50 = 180.0 nM 6.75 Inhibition of aromatase (unknown origin) 26469743
Aromatase IC50 = 179.89 nM 6.75 Inhibition of aromatase (unknown origin) 33017749

Literature References

PubMed DOI Target Context # Activities
26301554 10.1016/j.ejmech.2015.08.010 Aromatase 1
26469743 10.1016/j.ejmech.2015.09.038 Aromatase 1
33017749 10.1016/j.ejmech.2020.112845 Aromatase 1

Data from ChEMBL 36 via Core Engine