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Compound Detail

CHEMBL5177342

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C[C@]12CC[C@@H]3c4ccc(O)cc4CC[C@H]3[C@@H]1C[C@H]1OC(=O)C[C@]12O

Basic Information

ChEMBL ID CHEMBL5177342
Phase Preclinical
Structure Type MOL
InChI Key NLUGVTJBNRSIKH-UQZPWQSVSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
15
Publications
0
Known Names

Molecular Properties

328.4
MW (Da)
2.90
ALogP
4
HBA
2
HBD
66.8
PSA (Ų)
0.72
QED
0
Ro5 Violations
0
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C20H24O4
MW 328.41
Aromatic Rings 1
Heavy Atoms 24
NP-Likeness 2.44

Activity Summary

EC50 2 meas. best 10.85

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Estrogen receptor
CHEMBL206
EC50 10.85 10.85 0.0 1
Estrogen receptor beta
CHEMBL242
EC50 7.64 7.64 23.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Estrogen receptor EC50 = 0.014 nM 10.85 Modulation of ER-alpha (unknown origin) 35964426
Estrogen receptor beta EC50 = 23.0 nM 7.64 Modulation of ER-beta (unknown origin) 35964426

Literature References

PubMed DOI Target Context # Activities
- 10.6019/CHEMBL5303304 Fibroblast 15
- 10.6019/CHEMBL5303304 U2OS 10
- 10.6019/CHEMBL5303304 HEK-293T 7
35964426 10.1016/j.ejmech.2022.114658 Estrogen receptor 1
35964426 10.1016/j.ejmech.2022.114658 Estrogen receptor beta 1
- 10.6019/CHEMBL5308504 Casein kinase I isoform delta 1
- 10.6019/CHEMBL5308504 Cyclin-dependent kinase 2 1
- 10.6019/CHEMBL5308504 Glycogen synthase kinase-3 beta 1
- 10.6019/CHEMBL5308504 Mitogen-activated protein kinase 1 1
- 10.6019/CHEMBL5308504 Aurora kinase A 1
- 10.6019/CHEMBL5308504 Tyrosine-protein kinase ABL1 1
- 10.6019/CHEMBL5308504 Fibroblast growth factor receptor 3 1
- 10.6019/CHEMBL5308504 Peregrin 1
- 10.6019/CHEMBL5308504 Transcription intermediary factor 1-alpha 1
- 10.6019/CHEMBL5308504 Bromodomain-containing protein 4 1

Data from ChEMBL 36 via Core Engine