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Compound Detail

CHEMBL4100590

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COC(=O)C(C)C/C(=C(\c1ccc(O)cc1)c1ccc(OCCN(C)C)cc1)c1ccccc1

Basic Information

ChEMBL ID CHEMBL4100590
Phase Preclinical
Structure Type MOL
InChI Key DYYQOUVXQYDGMR-DQSJHHFOSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

459.6
MW (Da)
5.49
ALogP
5
HBA
1
HBD
59.0
PSA (Ų)
0.32
QED
1
Ro5 Violations
10
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C29H33NO4
MW 459.59
Aromatic Rings 3
Heavy Atoms 34
NP-Likeness -0.07

Activity Summary

IC50 2 meas. best 7.3

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Steroid hormone receptor ERR2
CHEMBL3751
IC50 7.3 7.3 50.0 1
Estrogen-related receptor gamma
CHEMBL3585238
IC50 5.56 5.56 2780.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
28189393 10.1016/j.bmc.2017.01.019 Steroid hormone receptor ERR1 1
28189393 10.1016/j.bmc.2017.01.019 Steroid hormone receptor ERR2 1
28189393 10.1016/j.bmc.2017.01.019 Estrogen-related receptor gamma 1
28189393 10.1016/j.bmc.2017.01.019 Estrogen receptor 1
28189393 10.1016/j.bmc.2017.01.019 Estrogen receptor beta 1

Data from ChEMBL 36 via Core Engine