Approval Year
| Substance Class |
Protein
Created
by
admin
on
Edited
Tue Apr 01 16:45:34 GMT 2025
by
admin
on
Tue Apr 01 16:45:34 GMT 2025
|
| Protein Type | RECEPTOR |
| Protein Sub Type | ACETYLCHOLINE RECEPTOR |
| Sequence Origin | HUMAN |
| Sequence Type | COMPLETE |
| Record UNII |
W3JX5KZ4V2
|
| Record Status |
Validated (UNII)
|
| Record Version |
|
-
Download
| Name | Type | Language | ||
|---|---|---|---|---|
|
Common Name | English | ||
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Preferred Name | English | ||
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Common Name | English | ||
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Common Name | English | ||
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Common Name | English |
| Code System | Code | Type | Description | ||
|---|---|---|---|---|---|
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W3JX5KZ4V2
Created by
admin on Tue Apr 01 16:45:34 GMT 2025 , Edited by admin on Tue Apr 01 16:45:34 GMT 2025
|
PRIMARY | |||
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P20309
Created by
admin on Tue Apr 01 16:45:34 GMT 2025 , Edited by admin on Tue Apr 01 16:45:34 GMT 2025
|
PRIMARY | |||
|
P20309
Created by
admin on Tue Apr 01 16:45:34 GMT 2025 , Edited by admin on Tue Apr 01 16:45:34 GMT 2025
|
PRIMARY |
| From | To |
|---|---|
| 1_141 | 1_221 |
| 1_517 | 1_520 |
| Glycosylation Type | HUMAN |
| Glycosylation Link Type | Site |
|---|---|
| N | 1_5 |
| N | 1_6 |
| N | 1_15 |
| N | 1_41 |
| N | 1_48 |
| Related Record | Type | Details | ||
|---|---|---|---|---|
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INHIBITOR -> TARGET |
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INHIBITOR -> TARGET |
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INHIBITOR -> TARGET |
Ki
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INHIBITOR -> TARGET |
In the airways, it exhibits pharmacological effects through inhibition of M3 receptor at the smooth muscle leading to bronchodilation.
BINDING
Kd
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INHIBITOR -> TARGET |
Ki
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INHIBITOR -> TARGET |
Binding assay
IC50
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NON-INHIBITOR->OFF-TARGET |
NON-INHIBITOR
Ki
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NON-BINDER->OFF TARGET |
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INHIBITOR -> TARGET |
S-ISOMER BINDS WITH LESS AVIDITY
IC50
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PARTIAL AGONIST->TARGET |
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INHIBITOR -> TARGET |
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INHIBITOR -> TARGET |
Ki
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INHIBITOR -> TARGET |
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AGONIST -> TARGET |
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INHIBITOR -> TARGET |
BINDING
IC50
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INHIBITOR -> TARGET |
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INHIBITOR -> TARGET |
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INHIBITOR -> TARGET |
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INHIBITOR -> TARGET |
Kd
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INHIBITOR -> TARGET |
BINDING
IC50
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RADIOLIGAND->TARGET |
Kd
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INHIBITOR -> TARGET |
Ki
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INHIBITOR -> TARGET |
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AGONIST -> TARGET |
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WEAK INHIBITOR->TARGET |
Membranes from transfected CHO cells
BINDING
IC50
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INHIBITOR -> TARGET |
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INHIBITOR -> TARGET |
BINDING
IC50
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INHIBITOR -> TARGET |
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INHIBITOR -> TARGET |
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INHIBITOR -> TARGET |
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POSITIVE ALLOSTERIC MODULATOR (PAM)->TARGET |
Increases the binding affinity of acetylcholine to receptor.
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AGONIST -> TARGET |
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INHIBITOR -> TARGET |
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INHIBITOR -> TARGET |
THRX-195518 possesses activity at target muscarinic receptors that was slightly lower (approximately one-third to one-tenth) than revefenacin.
BINDING
Ki
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INHIBITOR->OFF-TARGET |
Radioligand binding assay
BINDING
IC50
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AGONIST -> TARGET |
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NON-INHIBITOR->OFF-TARGET |
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INHIBITOR -> TARGET |
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INHIBITOR -> TARGET |
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INHIBITOR -> TARGET |
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INHIBITOR -> TARGET |
Appears to be more bladder-selective for the M3 receptor relative to salivary glands.eptor
Ki
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INHIBITOR -> TARGET |
IC50
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INHIBITOR -> TARGET |
Kd
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AGONIST -> TARGET |
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Structural Modifications
| Modification Type | Location Site | Location Type | Residue Modified | Extent | Fragment Name | Fragment Approval |
|---|---|---|---|---|---|---|
| AMINO ACID SUBSTITUTION | [1_385] | DEXFOSFOSERINE | VI4F0K069V |
| Name | Property Type | Amount | Referenced Substance | Defining | Parameters | References |
|---|---|---|---|---|---|---|
| MOL_WEIGHT | CHEMICAL |
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| Molecular Formula | CHEMICAL |
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