General
Preferred name
SOBETIROME
Synonyms
GC 1 ()
GC-1 ()
IACS-010759 ()
GC1 ()
QRX-431 ()
B7-2/GM-CSF ()
SOBETIROMA ()
P&D ID
PD005196
CAS
211110-63-3
Tags
available
drug candidate
Drug indication
Schizophrenia
X-linked adrenoleukodystrophy
Solid tumour/cancer
Dyslipidemia
Dementia
Drug Status
investigational
Max Phase
2.0
Structure
Probe scores
P&D probe-likeness score
[[ v.score ]]%
Structure formats
[[ format ]]
[[ compound[format === 'MOL' ? 'molblock' : format.toLowerCase()] ]]
Description
(extracted from source data)
DESCRIPTION Sobetirome (GC-1) is a thyroid hormone receptor ¦Â (TR¦Â)-specific agonist which bind selectively to TR¦Â-1 with an EC50 of 0.16 ¦ÌM[1].
PRICE 112
DESCRIPTION Sobetirome (IACS-010759) is a selective agonist of thyroid hormone receptor ?? (TR??) and binds selectively to TR??-1 (EC50: 0.16 ??M).
DESCRIPTION PPARalpha antagonist (Tocris Bioactive Compound Library)
DESCRIPTION High affinity thyroid receptor alpha (TRalpha) and TRbeta agonist; thyromimetic (Tocriscreen Plus)
DESCRIPTION Sobetirome selectively binds to and activates TRbeta over TRalpha and this receptor selectivity led to the hypothesis that sobetirome would lower cholesterol through activation of liver TRbeta without stimulating cardiac function through TRalpha activation in the heart. The tissue selective thyromimetic properties of sobetirome have been demonstrated in numerous animal models, which led to its clinical development as a novel cholesterol-lowering agent. Treatment of hypercholestemia obesity, and thyroid proliferative disorders. (BOC Sciences Bioactive Compounds)
DESCRIPTION Sobetirome (IACS-010759) is a selective agonist of thyroid hormone receptor β (TRβ) and binds selectively to TRβ-1 (EC50: 0.16 μM). (TargetMol Bioactive Compound Library)
Compound Sets
22
AdooQ Bioactive Compound Library
BOC Sciences Bioactive Compounds
Cayman Chemical Bioactives
ChEMBL Drugs
Concise Guide to Pharmacology 2017/18
Concise Guide to Pharmacology 2019/20
Concise Guide to Pharmacology 2021/22
Concise Guide to Pharmacology 2023/24
CZ-OPENSCREEN Bioactive Library
Drug Repurposing Hub
DrugBank
DrugMAP
EU-OPENSCREEN Bioactive Compound Library
EUbOPEN Chemogenomics Library
Guide to Pharmacology
LSP-MoA library (Laboratory of Systems Pharmacology)
MedChem Express Bioactive Compound Library
ReFrame library
TargetMol Bioactive Compound Library
Tocris Bioactive Compound Library
Tocriscreen Plus
External IDs
30
Properties
(calculated by RDKit )
Molecular Weight
328.17
Hydrogen Bond Acceptors
3
Hydrogen Bond Donors
2
Rotatable Bonds
6
Ring Count
2
Aromatic Ring Count
2
cLogP
4.19
TPSA
66.76
Fraction CSP3
0.35
Chiral centers
0.0
Largest ring
6.0
QED
0.83
Structural alerts
0
No structural alerts detected
Custom attributes
(extracted from source data)
Target Type
Nuclear Receptors
Target
THR
TRβ
TR¦Â
THRA, THRB
Thyroid hormone receptor
Primary Target
Other Nuclear Receptors
MOA
Agonist
Thyroid hormone receptor(THR)
Thyroid hormone receptor agonist
Pathway
Endocrinology/Hormones
Vitamin D Related/Nuclear Receptor
Recommended Cell Concentration
1 uM
Source data