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Compound Detail

CHEMBL2203702

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O=C(O)Cc1cc(Cl)c(Oc2ccc(O)c(C(=O)NCC(c3ccccc3)c3ccccc3)c2)c(Cl)c1

Basic Information

ChEMBL ID CHEMBL2203702
Phase Preclinical
Structure Type MOL
InChI Key LXIBPBIVTHEEQG-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

536.4
MW (Da)
6.68
ALogP
4
HBA
3
HBD
95.9
PSA (Ų)
0.22
QED
2
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C29H23Cl2NO5
MW 536.41
Aromatic Rings 4
Heavy Atoms 37
NP-Likeness -0.45

Activity Summary

EC50 2 meas. best 9.33

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Thyroid hormone receptor beta
CHEMBL1947
EC50 9.33 9.33 0.5 1
Thyroid hormone receptor alpha
CHEMBL1860
EC50 7.75 7.75 18.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Thyroid hormone receptor beta EC50 = 0.47 nM 9.33 Binding affinity to TRbeta1 22512468
Thyroid hormone receptor alpha EC50 = 18.0 nM 7.75 Binding affinity to TRalpha1 22512468

Literature References

PubMed DOI Target Context # Activities
22512468 10.1021/jm2004706 Thyroid hormone receptor beta 1
22512468 10.1021/jm2004706 Thyroid hormone receptor alpha 1

Data from ChEMBL 36 via Core Engine