Activities
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| # | Molecule ChEMBL ID | Compound Key | Standard Type | Standard Relation | Standard Value | Standard Text Value | Standard Units | pChEMBL Value | Comment | Assay ChEMBL ID | Assay Description | BAO Label | Assay Organism | Target ChEMBL ID | Target Name | Target Organism | Target Type | Document ChEMBL ID | Source Description | Cell ChEMBL ID | |
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| 1. |
tolrestat
|
Activity
|
---
|
---
|
---
|
---
|
---
|
Active
|
Prevention of cataract development in severely galactosemic Sprague-Dawley Albino rat assessed as lens opacification administered four timely daily as 3% eye-drop solution in precorneal region for 13 days by slit-lamp microscopy
|
organism-based format
|
Rattus norvegicus
|
Rattus norvegicus
|
Rattus norvegicus
|
ORGANISM
|
Scientific Literature
| ||||||
| 2. |
tolrestat
|
AC50
|
>
|
30000.0
|
---
|
nM
|
---
|
Summarised AC50 (mean value for measurements with a relation sign "="; largest value for measurements with relation sign ">")
|
Binding affinity towards human ADORA1 (agonistic activity) in an in vitro assay with cellular components measured by scintillation counting
|
single protein format
|
---
|
Adenosine A1 receptor
|
Homo sapiens
|
SINGLE PROTEIN
|
Scientific Literature
| ||||||
| 3. |
tolrestat
|
AC50
|
>
|
30000.0
|
---
|
nM
|
---
|
Summarised AC50 (mean value for measurements with a relation sign "="; largest value for measurements with relation sign ">")
|
Compound was evaluated for inhibition of human MAOA in an in vitro cell free assay measured by fluorescence spectroscopy
|
assay format
|
---
|
Monoamine oxidase A
|
Homo sapiens
|
SINGLE PROTEIN
|
Scientific Literature
| ||||||
| 4. |
110
|
log10(%HIA +10)
|
=
|
1.881
|
---
|
---
|
---
|
---
|
Drug absorption in human assessed as human intestinal absorption rate
|
tissue-based format
|
Homo sapiens
|
ADMET
|
---
|
ADMET
|
Scientific Literature
| ||||||
| 5. |
Tolrestat
|
Activity
|
=
|
0.0
|
---
|
%
|
---
|
---
|
Prevention of nuclear cataract development in severe galactosemic Albino rat assessed as nuclear cataract appearance at 3% ophthalmic solution administered topically QID after 12 days by slit-lamp microscopy
|
organism-based format
|
Rattus norvegicus
|
Rattus norvegicus
|
Rattus norvegicus
|
ORGANISM
|
Scientific Literature
| ||||||
| 6. |
Tolrestat
|
Activity
|
=
|
0.0
|
---
|
%
|
---
|
---
|
Prevention of nuclear cataract development in severe galactosemic Albino rat assessed as nuclear cataract appearance at 3% ophthalmic solution administered topically QID after 13 days by slit-lamp microscopy
|
organism-based format
|
Rattus norvegicus
|
Rattus norvegicus
|
Rattus norvegicus
|
ORGANISM
|
Scientific Literature
| ||||||
| 7. |
Tolrestat
|
Activity
|
=
|
0.0
|
---
|
%
|
---
|
---
|
Prevention of nuclear cataract development in severe galactosemic Albino rat assessed as nuclear cataract appearance at 1% ophthalmic solution administered topically QID after 13 days by slit-lamp microscopy
|
organism-based format
|
Rattus norvegicus
|
Rattus norvegicus
|
Rattus norvegicus
|
ORGANISM
|
Scientific Literature
| ||||||
| 8. |
tolrestat
|
AC50
|
>
|
30000.0
|
---
|
nM
|
---
|
Summarised AC50 (mean value for measurements with a relation sign "="; largest value for measurements with relation sign ">")
|
Compound was evaluated for inhibition of human PDE3A in an in vitro cell free assay measured by time-resolved fluorescence resonance energy transfer method
|
assay format
|
---
|
Phosphodiesterase 3A
|
Homo sapiens
|
SINGLE PROTEIN
|
Scientific Literature
| ||||||
| 9. |
TOLRESTAT
|
Hepatotoxicity (acute)
|
=
|
2.0
|
---
|
---
|
---
|
references out of a total of 9
|
Acute liver toxicity defined via clinical observations and clear clinical-chemistry results: serum ALT or AST activity > 6 N or serum alkaline phosphatases activity > 1.7 N. This category includes cytolytic, choleostatic and mixed liver toxicity. Value is number of references indexed. [column 'AIGUE' in source]
|
tissue-based format
|
Homo sapiens
|
Unchecked
|
---
|
UNCHECKED
|
Scientific Literature
| ||||||
| 10. |
TOLRESTAT
|
Hepatotoxicity (chronic liver disease)
|
=
|
0.0
|
---
|
---
|
---
|
references out of a total of 9
|
Chronic liver disease either proven histopathologically, or through a chonic elevation of serum amino-transferase activity after 6 months. Value is number of references indexed. [column 'CHRON' in source]
|
tissue-based format
|
Homo sapiens
|
Unchecked
|
---
|
UNCHECKED
|
Scientific Literature
| ||||||
| 11. |
tolrestat
|
AC50
|
>
|
30000.0
|
---
|
nM
|
---
|
Summarised AC50 (mean value for measurements with a relation sign "="; largest value for measurements with relation sign ">")
|
Binding affinity towards rat Gabra1 in an in vitro assay with cellular components measured by scintillation counting
|
single protein format
|
---
|
GABA receptor alpha-1 subunit
|
Rattus norvegicus
|
SINGLE PROTEIN
|
Scientific Literature
| ||||||
| 12. |
Tolrestat
|
IC50
|
=
|
96.0
|
---
|
nM
|
7.02
|
---
|
Evaluated for inhibition of Aldose reductase 2
|
single protein format
|
---
|
Aldose reductase
|
Bos taurus
|
SINGLE PROTEIN
|
Scientific Literature
| ||||||
| 13. |
Tolrestat
|
IC50
|
---
|
---
|
---
|
nM
|
---
|
Not Active
|
In vitro inhibitory activity against aldehyde reductase 1 (ALR1) from rat kidney.
|
single protein format
|
---
|
Aldehyde reductase
|
Rattus norvegicus
|
SINGLE PROTEIN
|
Scientific Literature
| ||||||
| 14. |
Tolrestat
|
Nuclear cataract
|
=
|
32.0
|
---
|
%
|
---
|
---
|
Ability to prevent cataract development in severly galactosemic rat treated with 1 percent ophthalmic solution on day 17
|
organism-based format
|
Rattus norvegicus
|
Rattus norvegicus
|
Rattus norvegicus
|
ORGANISM
|
Scientific Literature
| ||||||
| 15. |
Tolrestat
|
IC50
|
=
|
54.0
|
---
|
nM
|
7.27
|
---
|
Inhibition of reductase activity of N-terminal 6His-tagged AKR1B10 expressed in Escherichia coli BL21(DE3) assessed as inhibition of NADPH linked pyridine-3-aldehyde reduction
|
assay format
|
---
|
Aldo-keto reductase family 1 member B10
|
Homo sapiens
|
SINGLE PROTEIN
|
Scientific Literature
| ||||||
| 16. |
Tolrestat
|
IC50
|
=
|
46.0
|
---
|
nM
|
7.34
|
---
|
In vitro inhibitory activity against aldose reductase (ALR2) from rat lens extraction.
|
single protein format
|
---
|
Aldose reductase
|
Rattus norvegicus
|
SINGLE PROTEIN
|
Scientific Literature
| ||||||
| 17. |
tolrestat
|
Nuclear cataract
|
=
|
0.0
|
---
|
%
|
---
|
---
|
Effect of the treatment on day 13 with ophthalmic solution (3%)on development of nuclear cataract in severely galactosemic rats
|
organism-based format
|
Rattus norvegicus
|
Rattus norvegicus
|
Rattus norvegicus
|
ORGANISM
|
Scientific Literature
| ||||||
| 18. |
2 (tolrestat)
|
Reduction
|
=
|
90.0
|
---
|
%
|
---
|
---
|
In vivo inhibition of polyol accumulation in galactosemic rat diaphragm at dose 6 mg/kg administered perorally
|
organism-based format
|
Rattus norvegicus
|
Rattus norvegicus
|
Rattus norvegicus
|
ORGANISM
|
Scientific Literature
| ||||||
| 19. |
2 (tolrestat)
|
IC50
|
=
|
50.0
|
---
|
nM
|
7.30
|
---
|
Inhibitory concentration to aldose reductase (ALR-2) obtained from rat lens
|
single protein format
|
---
|
Aldose reductase
|
Rattus norvegicus
|
SINGLE PROTEIN
|
Scientific Literature
| ||||||
| 20. |
tolrestat
|
Nuclear cataract
|
=
|
0.0
|
---
|
%
|
---
|
---
|
Effect of the treatment on day 17 with ophthalmic solution (3%)on development of nuclear cataract in severely galactosemic rats
|
organism-based format
|
Rattus norvegicus
|
Rattus norvegicus
|
Rattus norvegicus
|
ORGANISM
|
Scientific Literature
|
Showing 1-20
out of 258 records
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