Approval Year
Substance Class |
Protein
Created
by
admin
on
Edited
Tue Apr 01 17:44:15 GMT 2025
by
admin
on
Tue Apr 01 17:44:15 GMT 2025
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Protein Type | RECEPTOR |
Protein Sub Type | |
Sequence Origin | HUMAN |
Sequence Type | COMPLETE |
Record UNII |
0C5V0MRU6P
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Record Status |
Validated (UNII)
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Record Version |
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-
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Preferred Name | English | ||
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Code System | Code | Type | Description | ||
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0C5V0MRU6P
Created by
admin on Tue Apr 01 17:44:15 GMT 2025 , Edited by admin on Tue Apr 01 17:44:15 GMT 2025
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PRIMARY |
Related Record | Type | Details | ||
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AGONIST -> TARGET | |||
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AGONIST -> TARGET |
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AGONIST -> TARGET |
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AGONIST -> TARGET | |||
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AGONIST -> TARGET |
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AGONIST -> TARGET |
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AGONIST -> TARGET | |||
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AGONIST -> TARGET |
When bound to bile acids, FXR repressed transcription of the gene encoding cholesterol 7α-hydroxylase, which is the rate-limiting enzyme in bile acid synthesis, and activated the gene encoding intestinal bile acid?binding protein, which is a candidate bile acid transporter.
AGONIST
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AGONIST -> TARGET |
Alpha screen
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AGONIST -> TARGET | |||
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AGONIST -> TARGET |
Time-resolved fluorescence resonance energy (TR-FRET)
BINDING
EC50
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AGONIST -> TARGET |
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AGONIST -> TARGET |
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INHIBITOR->OFF-TARGET |
Inhibition of the FXR by danicopan has the potential to promote cholestasis.
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AGONIST -> TARGET |
GAL-4 ASSAY
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AGONIST -> TARGET |
CDCA, had a
half-maximal effective concentration (EC50) of
50 mMand 10 micromolar murine and human FXR,
respectively (Fig. 1B). These concentrations are
well within the physiologic intracellular range
reported in vivo (11).
AGONIST
IC50
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AGONIST -> TARGET | |||
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AGONIST -> TARGET | |||
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INHIBITOR -> TARGET |
IC50
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AGONIST -> TARGET |
Structural Modifications
Modification Type | Location Site | Location Type | Residue Modified | Extent | Fragment Name | Fragment Approval |
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AMINO ACID REPLACEMENT | [1_145] [1_164] | SERINE | DEXFOSFOSERINE | VI4F0K069V | ||
AMINO ACID REPLACEMENT | [1_456] | THREONINE | THREONINE PHOSPHATE | 3L4WX7B1EI | ||
AMINO ACID REPLACEMENT | [1_167] [1_227] | LYSINE | N6-ACETYLLYSINE | 470AD5VY1X | ||
AMINO ACID REPLACEMENT | [1_220] | LYSINE | N6-METHYLLYSINE | FCR6T2IYVU |
Name | Property Type | Amount | Referenced Substance | Defining | Parameters | References |
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MOL_WEIGHT:NUMBER AVERAGE(CALCULATED) | CHEMICAL |
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