Approval Year
| Substance Class |
Protein
Created
by
admin
on
Edited
Tue Apr 01 17:40:35 GMT 2025
by
admin
on
Tue Apr 01 17:40:35 GMT 2025
|
| Protein Sub Type | |
| Sequence Origin | HUMAN |
| Sequence Type | COMPLETE |
| Record UNII |
1EKV1NFY3Y
|
| Record Status |
Validated (UNII)
|
| Record Version |
|
-
Download
| Name | Type | Language | ||
|---|---|---|---|---|
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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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1EKV1NFY3Y
Created by
admin on Tue Apr 01 17:40:35 GMT 2025 , Edited by admin on Tue Apr 01 17:40:35 GMT 2025
|
PRIMARY |
| From | To |
|---|---|
| 1_32 | 1_74 |
| 1_216 | 1_500 |
| 1_337 | 1_344 |
| 1_382 | 1_389 |
| 1_482 | 1_501 |
| 1_486 | 1_504 |
| 1_507 | 1_519 |
| 1_522 | 1_535 |
| Glycosylation Type | HUMAN |
| Glycosylation Link Type | Site |
|---|---|
| N | 1_185 |
| N | 1_268 |
| N | 1_320 |
| N | 1_384 |
| N | 1_529 |
| Related Record | Type | Details | ||
|---|---|---|---|---|
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NEGATIVE ALLOSTERIC MODULATOR (NAM)->TARGET |
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AGONIST -> TARGET |
Ki
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LIGAND->TARGET | |||
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POSITIVE ALLOSTERIC MODULATOR (PAM)->TARGET |
EC50
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RADIOLIGAND->TARGET |
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INHIBITOR -> TARGET |
ANTAGONIST
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INHIBITOR -> TARGET |
In Rodents
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RADIOLIGAND->TARGET |
ALLOSTERIC
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MODULATOR->TARGET |
The pharmacokinetics and effects of JNJ-40411813 on cognition and subjective awareness were evaluated. Plasma JNJ-40411813 exposure was dose-dependent, t max ranged from 3-4 h and t 1/2 19.4-34.2 h across the dose levels. JNJ-40411813 significantly (p=0.02) reduced continuity of attention score (150 mg dose) and ameliorated smoking withdrawal-induced changes in power of attention and quality of episodic memory versus placebo. A modest reduction in alertness was observed at 150-225 mg doses, JNJ-40411813 (500 mg) reduced S(+) ketamine-induced negative symptoms by approximately 43% and 30% in cohorts 1 and 3, respectively. JNJ-40411813 was generally well-tolerated.
ALLOSTERIC ACTIVATOR
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NEGATIVE ALLOSTERIC MODULATOR (NAM)->TARGET |
Complete selectivity against mGluR1,3,4,5,6,8 (IC50 > 10000 nM). Flipr Assay
IC50
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ACTIVATOR -> TARGET |
EC50
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INHIBITOR -> TARGET |
MAY BE RESPONSIBLE FOR ANTIDEPRESSANT ACTIVITY OF KETAMINE
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INHIBITOR -> TARGET |
Functional assay for cAMP formation.
IC50
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NEGATIVE ALLOSTERIC MODULATOR->TARGET |
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INHIBITOR -> TARGET |
MAY BE RESPONSIBLE FOR ANTIDEPRESSANT ACTIVITY OF KETAMINE
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AGONIST -> TARGET |
cAMP decrease.
EC50
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INHIBITOR -> TARGET |
Ki
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LIGAND->TARGET |
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AGONIST -> TARGET |
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![Structure of 2-[[3-[(4-Acetyl-3-hydroxy-2-propylphenoxy)methyl]phenyl]thio]-4-pyridinecarboxylic acid](/img/e6f03671-23d6-4b18-b903-e96b353fc50f.svg "Structure of 2-[[3-[(4-Acetyl-3-hydroxy-2-propylphenoxy)methyl]phenyl]thio]-4-pyridinecarboxylic acid")
| Name | Property Type | Amount | Referenced Substance | Defining | Parameters | References |
|---|---|---|---|---|---|---|
| MOL_WEIGHT | CHEMICAL |
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| Molecular Formula | CHEMICAL |
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