Approval Year
| Substance Class |
Protein
Created
by
admin
on
Edited
Sat Dec 16 11:49:36 UTC 2023
by
admin
on
Sat Dec 16 11:49:36 UTC 2023
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| Protein Sub Type | |
| Sequence Type | COMPLETE |
| Record UNII |
T3CA3UN9ZA
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| Record Status |
Validated (UNII)
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| Record Version |
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-
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| Code System | Code | Type | Description | ||
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PROTEIN ARGININE METHYLTRANSFERASE 5
Created by
admin on Sat Dec 16 11:49:36 UTC 2023 , Edited by admin on Sat Dec 16 11:49:36 UTC 2023
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PRIMARY | |||
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T3CA3UN9ZA
Created by
admin on Sat Dec 16 11:49:36 UTC 2023 , Edited by admin on Sat Dec 16 11:49:36 UTC 2023
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PRIMARY | |||
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O14744
Created by
admin on Sat Dec 16 11:49:36 UTC 2023 , Edited by admin on Sat Dec 16 11:49:36 UTC 2023
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PRIMARY |
| Related Record | Type | Details | ||
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INHIBITOR -> TARGET |
Collectively, pre-clinical pharmacology studies indicate that JBI-778 is a potent and selective, substrate competitive-SAM cooperative, brain penetrant protein arginine methyl transferase 5 (PRMT5) inhibitor. JBI-778 shows higher selectivity against other PRMTs. The compound shows an IC50 of ~3 nM against PRMT5:MEP50 in the biochemical assay
COMPETITIVE INHIBITOR
IC50
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INHIBITOR -> TARGET |
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INHIBITOR -> TARGET |
COMPETITIVE INHIBITOR
Kd
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INHIBITOR -> TARGET |
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INHIBITOR -> TARGET |
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INHIBITOR -> TARGET |
MTA competes with the activating cofactor S-adenosyl-l-methionine (SAM), causing a decrease in PRMT5 activity and sensitizes the MTAP-del cells to further loss of PRMT5 activity.
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INHIBITOR -> TARGET |
inhibitor of the PRMT5/MEP50 complex; Cellular assay MTAP-deleted cell line
IN-VITRO
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| Name | Property Type | Amount | Referenced Substance | Defining | Parameters | References |
|---|---|---|---|---|---|---|
| Molecular Formula | CHEMICAL |
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| MOL_WEIGHT | CHEMICAL |
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