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Compound Detail

CHEMBL425194

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COc1cc2c(cc1O)CC[C@@H]1[C@@H]2CC[C@]2(C)C(=O)CC[C@@H]12

Basic Information

ChEMBL ID CHEMBL425194
Phase Preclinical
Structure Type MOL
InChI Key WHEUWNKSCXYKBU-QPWUGHHJSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
7
Publications
0
Known Names

Molecular Properties

300.4
MW (Da)
3.83
ALogP
3
HBA
1
HBD
46.5
PSA (Ų)
0.86
QED
0
Ro5 Violations
1
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

Natural Product First in Class Prodrug

Extended Properties

Molecular Formula C19H24O3
MW 300.40
Aromatic Rings 1
Heavy Atoms 22
NP-Likeness 2.03

Activity Summary

IC50 3 meas. best 6.68

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
17-beta-hydroxysteroid dehydrogenase type 1
CHEMBL3181
IC50 6.68 6.68 207.0 1
Estrogen receptor
CHEMBL206
IC50 4.96 4.96 11000.0 1
Aromatase
CHEMBL1978
IC50 4.77 4.77 16982.4 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
18052315 10.1021/jm070639e Plasma 5
19836949 10.1016/j.bmcl.2009.09.113 17-beta-hydroxysteroid dehydrogenase type 1 2
19772289 10.1021/jm900921c 3-keto-steroid reductase/17-beta-hydroxysteroid dehydrogenase 7 2
16078843 10.1021/jm050066a MCF7 1
19836949 10.1016/j.bmcl.2009.09.113 Estrogen receptor 1
27687674 10.1016/j.bmcl.2016.09.046 Cytochrome P450 1B1 1
33017749 10.1016/j.ejmech.2020.112845 Aromatase 1

Data from ChEMBL 36 via Core Engine