Approval Year
| Substance Class |
Protein
Created
by
admin
on
Edited
Tue Apr 01 16:42:55 GMT 2025
by
admin
on
Tue Apr 01 16:42:55 GMT 2025
|
| Protein Sub Type | |
| Sequence Origin | HUMAN |
| Sequence Type | COMPLETE |
| Record UNII |
8HOL4T03PN
|
| Record Status |
Validated (UNII)
|
| Record Version |
|
-
Download
| Name | Type | Language | ||
|---|---|---|---|---|
|
Preferred Name | English | ||
|
Common Name | English | ||
|
Common Name | English |
| Code System | Code | Type | Description | ||
|---|---|---|---|---|---|
|
P08173
Created by
admin on Tue Apr 01 16:42:55 GMT 2025 , Edited by admin on Tue Apr 01 16:42:55 GMT 2025
|
PRIMARY | |||
|
8HOL4T03PN
Created by
admin on Tue Apr 01 16:42:55 GMT 2025 , Edited by admin on Tue Apr 01 16:42:55 GMT 2025
|
PRIMARY |
| From | To |
|---|---|
| 1_105 | 1_185 |
| Glycosylation Type | HUMAN |
| Glycosylation Link Type | Site |
|---|---|
| N | 1_8 |
| N | 1_13 |
| Related Record | Type | Details | ||
|---|---|---|---|---|
|
INHIBITOR -> TARGET |
Binding Assay
IC50
|
||
|
INHIBITOR -> TARGET |
Kd
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||
|
POSITIVE ALLOSTERIC MODULATOR (PAM)->TARGET |
BINDING
Ki
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||
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|
INHIBITOR -> TARGET | |||
|
|
RADIOLIGAND->TARGET |
Ki
|
||
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INHIBITOR -> 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
|
||
|
INHIBITOR -> TARGET |
Binding Assay
IC50
|
||
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INHIBITOR -> TARGET |
IC50
|
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|
AGONIST -> TARGET |
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AGONIST -> TARGET |
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INHIBITOR -> TARGET |
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NON-AGONIST->OFF-TARGET |
Ki
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|
INHIBITOR -> TARGET |
Membranes from transfected CHO cells
BINDING
IC50
|
||
|
LIGAND->TARGET |
Binding Assay
Kd
|
||
|
INHIBITOR -> TARGET |
Ki
|
||
|
AGONIST -> TARGET |
|
||
|
INHIBITOR -> TARGET |
BINDING
Kd
|
||
|
POSITIVE ALLOSTERIC MODULATOR (PAM)->TARGET |
Shown to be a PAM of ACh function in a cell-based Ca2+mobilization assay. In this assay, increasing concentrations of MK-6884 potentiated the ability of a fixed concentration of ACh (EC20) to mobilize intracellular Ca2+
ALLOSTERIC ACTIVATOR
EC50
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||
|
AGONIST -> TARGET |
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|
NON-INHIBITOR->OFF TARGET |
NON-INHIBITOR
Ki
|
||
|
INHIBITOR -> TARGET |
ANTAGONIST
|
Structural Modifications
| Modification Type | Location Site | Location Type | Residue Modified | Extent | Fragment Name | Fragment Approval |
|---|---|---|---|---|---|---|
| AMINO ACID SUBSTITUTION | [1_459] [1_463] [1_477] | THREONINE PHOSPHATE | 3L4WX7B1EI |
| Name | Property Type | Amount | Referenced Substance | Defining | Parameters | References |
|---|---|---|---|---|---|---|
| Molecular Formula | CHEMICAL |
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| MOL_WEIGHT | CHEMICAL |
|