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Compound Detail

CHEMBL378593

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CC(C)c1cc(Oc2c(Br)cc3nc(C(=O)O)cc(O)c3c2Br)ccc1O

Basic Information

ChEMBL ID CHEMBL378593
Phase Preclinical
Structure Type MOL
InChI Key DXDHCVCAJKZAHT-UHFFFAOYSA-N
2
Targets
4
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

497.1
MW (Da)
5.78
ALogP
5
HBA
3
HBD
99.9
PSA (Ų)
0.42
QED
1
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C19H15Br2NO5
MW 497.14
Aromatic Rings 3
Heavy Atoms 27
NP-Likeness 0.07

Activity Summary

IC50 4 meas. best 7.29

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Thyroid hormone receptor beta
CHEMBL1947
IC50 7.29 7.29 51.0 2
Thyroid hormone receptor alpha
CHEMBL1860
IC50 6.6 6.6 250.0 2

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
16338239 10.1016/j.bmcl.2005.11.077 Thyroid hormone receptor alpha 2
16338239 10.1016/j.bmcl.2005.11.077 Thyroid hormone receptor beta 2
16338239 10.1016/j.bmcl.2005.11.077 Thyroid hormone receptor 1
17467994 10.1016/j.bmc.2007.04.015 Thyroid hormone receptor alpha 1
17467994 10.1016/j.bmc.2007.04.015 Thyroid hormone receptor beta 1

Data from ChEMBL 36 via Core Engine