Approval Year
| Substance Class |
Protein
Created
by
admin
on
Edited
Tue Apr 01 16:34:09 GMT 2025
by
admin
on
Tue Apr 01 16:34:09 GMT 2025
|
| Protein Type | RECEPTOR |
| Protein Sub Type | |
| Sequence Origin | HUMAN |
| Sequence Type | COMPLETE |
| Record UNII |
NJ1Q2Q7LO5
|
| Record Status |
Validated (UNII)
|
| Record Version |
|
-
Download
| Name | Type | Language | ||
|---|---|---|---|---|
|
Preferred Name | English | ||
|
Common Name | English | ||
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Common Name | English | ||
|
Common Name | English | ||
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Common Name | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Common Name | English |
| Code System | Code | Type | Description | ||
|---|---|---|---|---|---|
|
P21554
Created by
admin on Tue Apr 01 16:34:09 GMT 2025 , Edited by admin on Tue Apr 01 16:34:09 GMT 2025
|
PRIMARY | |||
|
P21554
Created by
admin on Tue Apr 01 16:34:09 GMT 2025 , Edited by admin on Tue Apr 01 16:34:09 GMT 2025
|
PRIMARY | |||
|
NJ1Q2Q7LO5
Created by
admin on Tue Apr 01 16:34:09 GMT 2025 , Edited by admin on Tue Apr 01 16:34:09 GMT 2025
|
PRIMARY |
| Glycosylation Type | HUMAN |
| Glycosylation Link Type | Site |
|---|---|
| N | 1_77 |
| N | 1_83 |
| N | 1_112 |
| Related Record | Type | Details | ||
|---|---|---|---|---|
|
AGONIST -> TARGET |
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INHIBITOR -> TARGET |
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|
AGONIST -> TARGET |
Ki
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|
AGONIST -> TARGET |
Mouse AtT-20 neuroblastoma cells stably transfected with human CB1
EC50
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|
AGONIST -> TARGET |
Ki
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|
AGONIST -> TARGET |
EC50
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INHIBITOR -> TARGET |
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INHIBITOR -> TARGET |
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|
AGONIST -> TARGET |
EC50
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|
AGONIST -> TARGET | |||
|
AGONIST -> TARGET |
Ki
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|
AGONIST -> TARGET |
EC50
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|
AGONIST -> TARGET |
Ki
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|
AGONIST -> TARGET |
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LIGAND->TARGET |
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INHIBITOR -> TARGET |
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|
AGONIST -> TARGET |
Mouse AtT-20 neuroblastoma cells stably transfected with human CB1
EC50
|
||
|
AGONIST -> TARGET |
Ki
|
||
|
INHIBITOR -> TARGET |
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|
AGONIST -> TARGET |
EC50
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|
AGONIST -> TARGET |
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INHIBITOR -> TARGET |
cannabinoid CB1 receptor signalling inhibitor
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|
AGONIST -> TARGET |
Ki
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AGONIST -> TARGET |
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|
AGONIST -> TARGET |
Ki
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|
AGONIST -> TARGET |
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|
AGONIST -> TARGET |
IC50
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||
|
AGONIST -> TARGET |
Mouse AtT-20 neuroblastoma cells stably transfected with human CB1
EC50
|
||
|
AGONIST -> TARGET |
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|
AGONIST -> TARGET |
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|
AGONIST -> TARGET |
EC50
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|
AGONIST -> TARGET |
Ki
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|
AGONIST -> TARGET |
Ki
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|
AGONIST -> TARGET |
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|
AGONIST -> TARGET |
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|
AGONIST -> TARGET |
Ki
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|
AGONIST -> TARGET |
Ki
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||
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|
AGONIST -> TARGET |
Ki
|
||
|
AGONIST -> TARGET |
Mouse AtT-20 neuroblastoma cells stably transfected with human CB1
EC50
|
||
|
AGONIST -> TARGET |
|
||
|
AGONIST -> TARGET |
Mouse AtT-20 neuroblastoma cells stably transfected with human CB1
EC50
|
||
|
WEAK AGONIST->TARGET |
EC50
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|
|
AGONIST -> TARGET |
Ki
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|
AGONIST -> TARGET |
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NEGATIVE ALLOSTERIC MODULATOR->TARGET |
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|
AGONIST -> TARGET |
Ki
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|
AGONIST -> TARGET |
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NEGATIVE ALLOSTERIC MODULATOR (NAM)->TARGET |
?9-tetrahydrocannabinol (THC), substantially increases the synthesis of pregnenolone in the brain via activation of the type-1 cannabinoid (CB1) receptor. Pregnenolone then, acting as a signaling-specific inhibitor of the CB1 receptor, reduces several effects of THC. This negative feedback mediated by pregnenolone reveals a previously unknown paracrine/autocrine loop protecting the brain from CB1 receptor overactivation.
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|
AGONIST -> TARGET |
Ki
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|
AGONIST -> TARGET | |||
|
AGONIST -> TARGET |
Ki
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|
ACTIVATOR -> TARGET |
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|
AGONIST -> TARGET |
Ki
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|
AGONIST -> TARGET |
Strong agonist
EC50
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|
AGONIST -> TARGET |
Ki
|
||
|
AGONIST -> TARGET |
Mouse AtT-20 neuroblastoma cells stably transfected with human CB1
EC50
|
||
|
AGONIST -> TARGET |
|
||
|
AGONIST -> TARGET |
EC50
|
||
|
|
AGONIST -> TARGET |
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|
AGONIST -> TARGET |
EC50
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|
AGONIST -> TARGET |
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|
AGONIST -> TARGET |
Ki
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|
AGONIST -> TARGET |
Ki
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|
AGONIST -> TARGET |
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|
AGONIST -> TARGET |
EC50
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ACTIVATOR -> TARGET |
Inhibits a anandamide selective transport mechanism (reuptake)
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|
AGONIST -> TARGET |
Ki
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|
AGONIST -> TARGET |
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RADIOLIGAND->TARGET |
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|
AGONIST -> TARGET | |||
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INVERSE AGONIST->TARGET |
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AGONIST -> TARGET | |||
|
AGONIST -> TARGET |
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|
AGONIST -> TARGET |
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|
AGONIST -> TARGET |
Ki
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|
AGONIST -> TARGET |
Ki
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||
|
AGONIST -> TARGET |
EC50
|
||
|
|
AGONIST -> TARGET |
Ki
|
||
|
AGONIST -> TARGET |
Ki
|
||
|
AGONIST -> TARGET |
EC50
|
||
|
AGONIST -> TARGET |
Mouse AtT-20 neuroblastoma cells stably transfected with human CB1
EC50
|
||
|
|
AGONIST -> TARGET |
Ki
|
||
|
AGONIST -> TARGET |
EC50
|
||
|
AGONIST -> TARGET |
Mouse AtT-20 neuroblastoma cells stably transfected with human CB1
EC50
|
||
|
AGONIST -> TARGET |
|
||
|
|
AGONIST -> TARGET |
Ki
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|
AGONIST -> TARGET |
Ki
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RADIOLIGAND->TARGET |
Kd
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AGONIST -> TARGET |
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AGONIST -> TARGET |
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|
AGONIST -> TARGET |
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|
AGONIST -> TARGET |
EC50
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|
LIGAND->TARGET | |||
|
AGONIST -> TARGET |
Mouse AtT-20 neuroblastoma cells stably transfected with human CB1
EC50
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||
|
AGONIST -> TARGET |
Mouse AtT-20 neuroblastoma cells stably transfected with human CB1
EC50
|
||
|
INHIBITOR -> TARGET |
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|
AGONIST -> TARGET |
Mouse AtT-20 neuroblastoma cells stably transfected with human CB1
EC50
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|
INHIBITOR -> TARGET |
AM281 is a selective CB1 receptor antagonis
BINDING
IC50
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AGONIST -> TARGET |
EC50
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|
AGONIST -> TARGET |
EC50
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|
AGONIST -> TARGET |
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AGONIST -> TARGET |
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INHIBITOR -> TARGET |
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|
AGONIST -> TARGET |
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INHIBITOR -> TARGET | |||
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POSITIVE ALLOSTERIC MODULATOR->TARGET |
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|
AGONIST -> TARGET |
Mouse AtT-20 neuroblastoma cells stably transfected with human CB1
EC50
|
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|
AGONIST -> TARGET |
Ki
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|
INVERSE AGONIST->TARGET |
Rimonabant was the first CB1r antagonist to be approved for the treatment of obesity in Europe (Van Gaal et al., 2005; Henness et al., 2006). It was withdrawn from the market in 2008 because it was found to cause a significant drug-related risk of serious psychiatric disorders including anxiety and depression (Christensen et al., 2007).
Ki
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|
AGONIST -> TARGET |
Mouse AtT-20 neuroblastoma cells stably transfected with human CB1
EC50
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NON-BINDER->OFF TARGET |
Ki
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|
AGONIST -> TARGET |
|
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|
AGONIST -> TARGET |
Emax 99% of CP55940
EC50
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|
AGONIST -> TARGET |
Ki
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INVERSE AGONIST->TARGET |
|
||
|
AGONIST -> TARGET |
Mouse AtT-20 neuroblastoma cells stably transfected with human CB1
EC50
|
||
|
|
AGONIST -> TARGET |
EC50
|
||
|
AGONIST -> TARGET |
|
||
|
AGONIST -> TARGET |
Ki
|
||
|
AGONIST -> TARGET |
EC50
|
||
|
AGONIST -> TARGET |
Mouse AtT-20 neuroblastoma cells stably transfected with human CB1
EC50
|
||
|
|
INVERSE AGONIST->TARGET | |||
|
AGONIST -> TARGET |
Ki
|
||
|
AGONIST -> TARGET |
EC50
|
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|
AGONIST -> TARGET |
Very potent cannabinoid effects in animal studies.
Ki
|
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|
AGONIST -> TARGET |
EC50
|
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|
AGONIST -> TARGET |
A potent agonist
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INHIBITOR -> TARGET |
BINDING
IC50
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|
AGONIST -> TARGET |
EC50
|
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RADIOLIGAND->TARGET |
IC50
|
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|
AGONIST -> TARGET |
EC50
|
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|
AGONIST -> TARGET |
EC50
|
||
|
|
WEAK AGONIST->TARGET |
Ki
|
||
|
INHIBITOR -> TARGET |
IC50
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INHIBITOR -> TARGET |
Ki
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|
AGONIST -> TARGET |
|
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|
AGONIST -> TARGET |
Natural agonist
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|
AGONIST -> TARGET |
EC50
|
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|
AGONIST -> TARGET |
EC50
|
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INHIBITOR -> TARGET |
|
||
|
INVERSE AGONIST->TARGET |
IC50
|
||
|
AGONIST -> TARGET |
Ki
|
||
|
AGONIST -> TARGET |
EC50
|
||
|
AGONIST -> TARGET |
Ki
|
||
|
AGONIST -> TARGET |
EC50
|
||
|
AGONIST -> TARGET |
|
||
|
AGONIST -> TARGET |
|
||
|
AGONIST -> TARGET |
|
||
|
AGONIST -> TARGET |
Mouse AtT-20 neuroblastoma cells stably transfected with human CB1
EC50
|
||
|
AGONIST -> TARGET |
|
||
|
NEGATIVE ALLOSTERIC MODULATOR (NAM)->TARGET |
Assumed from CBD and CBDA
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INHIBITOR -> TARGET | |||
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INHIBITOR -> TARGET |
Ki
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|
AGONIST -> TARGET |
Assumed target and agonist
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|
AGONIST -> TARGET | |||
|
AGONIST -> TARGET |
|
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|
AGONIST -> TARGET |
5F-CUMYL-PEGACLONE acts as a potent full agonist of the CB1 receptor.
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AGONIST -> TARGET |
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AGONIST -> TARGET |
Exhibit cannabinoid (CB) receptor activity but overall potency is expected to be low.
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|
AGONIST -> TARGET |
Ki
|
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RADIOLIGAND->TARGET |
|
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RADIOLIGAND->TARGET |
Ki
|
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|
INHIBITOR -> TARGET |
|
||
|
AGONIST -> TARGET |
Mouse AtT-20 neuroblastoma cells stably transfected with human CB1
EC50
|
||
|
AGONIST -> TARGET |
|
||
|
AGONIST -> TARGET | |||
|
|
AGONIST -> TARGET |
Ki
|
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|
AGONIST -> TARGET |
Ki
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INHIBITOR -> TARGET |
|
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|
AGONIST -> TARGET |
Mouse AtT-20 neuroblastoma cells stably transfected with human CB1
EC50
|
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|
AGONIST -> TARGET |
ASSUMED ACTIVITY FROM ANALOGS
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AGONIST -> TARGET |
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AGONIST -> TARGET |
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|
AGONIST -> TARGET |
|
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AGONIST -> TARGET |
Emax=142% relative to JWH-018
EC50
|
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|
AGONIST -> TARGET |
Potent agonist of both the CB1 receptor and the CB2 receptor.
EC50
|
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AGONIST -> TARGET |
An endogenous agonist
|
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|
AGONIST -> TARGET |
Mouse AtT-20 neuroblastoma cells stably transfected with human CB1
EC50
|
||
|
INHIBITOR -> TARGET |
Rimonabant (SR141716) is a highly potent, brain penetrated and selective central cannabinoid receptor (CB1) antagonist
BINDING
IC50
|
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|
AGONIST -> TARGET |
|
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|
AGONIST -> TARGET |
EC50
|
||
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|
AGONIST -> TARGET |
Ki
|
||
|
AGONIST -> TARGET | |||
|
AGONIST -> TARGET |
|
||
|
AGONIST -> TARGET | |||
|
AGONIST -> TARGET |
Mouse AtT-20 neuroblastoma cells stably transfected with human CB1
EC50
|
||
|
AGONIST -> TARGET |
|
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|
AGONIST -> TARGET |
Ki
|
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INHIBITOR -> TARGET |
INVERSE AGONIST/ANTAGONIST
|
| Name | Property Type | Amount | Referenced Substance | Defining | Parameters | References |
|---|---|---|---|---|---|---|
| MOL_WEIGHT | CHEMICAL |
|
||||
| Molecular Formula | CHEMICAL |
|