Approval Year
| Substance Class |
Protein
Created
by
admin
on
Edited
Tue Apr 01 18:31:41 GMT 2025
by
admin
on
Tue Apr 01 18:31:41 GMT 2025
|
| Protein Type | RECEPTOR |
| Protein Sub Type | |
| Sequence Origin | HUMAN |
| Sequence Type | COMPLETE |
| Record UNII |
OY9O3N5W0A
|
| Record Status |
Validated (UNII)
|
| Record Version |
|
-
Download
| Name | Type | Language | ||
|---|---|---|---|---|
|
Preferred Name | English | ||
|
Common Name | English | ||
|
Common Name | English |
| Code System | Code | Type | Description | ||
|---|---|---|---|---|---|
|
OY9O3N5W0A
Created by
admin on Tue Apr 01 18:31:41 GMT 2025 , Edited by admin on Tue Apr 01 18:31:41 GMT 2025
|
PRIMARY | |||
|
P41180
Created by
admin on Tue Apr 01 18:31:41 GMT 2025 , Edited by admin on Tue Apr 01 18:31:41 GMT 2025
|
PRIMARY |
| From | To |
|---|---|
| 1_112 | 2_112 |
| 1_110 | 2_110 |
| 2_566 | 2_579 |
| 2_549 | 2_563 |
| 2_527 | 2_546 |
| 2_523 | 2_543 |
| 2_418 | 2_430 |
| 2_339 | 2_376 |
| 2_217 | 2_542 |
| 2_41 | 2_82 |
| 1_566 | 1_579 |
| 1_549 | 1_563 |
| 1_527 | 1_546 |
| 1_523 | 1_543 |
| 1_418 | 1_430 |
| 1_339 | 1_376 |
| 1_217 | 1_542 |
| 1_41 | 1_82 |
| Glycosylation Type | HUMAN |
| Glycosylation Link Type | Site |
|---|---|
| N | 1_71 |
| N | 1_111 |
| N | 1_242 |
| N | 1_268 |
| N | 1_367 |
| N | 1_381 |
| N | 1_427 |
| N | 1_449 |
| N | 1_469 |
| N | 1_522 |
| N | 1_575 |
| N | 2_71 |
| N | 2_111 |
| N | 2_242 |
| N | 2_268 |
| N | 2_367 |
| N | 2_381 |
| N | 2_427 |
| N | 2_449 |
| N | 2_469 |
| N | 2_522 |
| N | 2_575 |
| Related Record | Type | Details | ||
|---|---|---|---|---|
|
INHIBITOR -> TARGET |
|
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|
AGONIST -> TARGET |
|
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|
AGONIST -> TARGET |
ALLOSTERIC
EC50
|
||
|
AGONIST -> TARGET |
In HEK293T cells transiently transfected with human CaSR. CaSR activity was quantified by measuring accumulation of IP-1.
AGONIST
EC50
|
||
|
AGONIST -> TARGET | |||
|
POSITIVE ALLOSTERIC MODULATOR (PAM)->TARGET |
|
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|
INHIBITOR -> TARGET |
|
||
|
AGONIST -> TARGET |
|
||
|
AGONIST -> TARGET |
A stable clone of HEK-293T overexpressing the human calcium-sensing receptor (hCaSR) was used. Activation of the hCaSR by KP-2067 GLUTATHIONE DISULFIDE were characterized in the presence of 1.2 mM calcium by quantifying inositol monophosphate (IP-1), a stable intracellular metabolite of IP-3 synthesis and surrogate of Gq (G protein, q polypeptide) activation in vitro.
AGONIST
EC50
|
||
|
AGONIST -> TARGET |
In HEK293T/CaSR cells (HEK293T cells stable transfected with human CaSR). CaSR activity was quantified by measuring accumulation of inositol-1-phosphate (IP-1 ) in the presence of calcium (1.2 mM).
AGONIST
EC50
|
||
|
INHIBITOR -> TARGET |
|
Structural Modifications
| Modification Type | Location Site | Location Type | Residue Modified | Extent | Fragment Name | Fragment Approval |
|---|---|---|---|---|---|---|
| AMINO_ACID_SUBSTITUTION | [1_901] [1_1042] [2_901] [2_1042] | SITE_SPECIFIC | DEXFOSFOSERINE | VI4F0K069V |
| Name | Property Type | Amount | Referenced Substance | Defining | Parameters | References |
|---|---|---|---|---|---|---|
| MOL_WEIGHT | CHEMICAL |
|
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| Molecular Formula | CHEMICAL |
|