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Approval Year

Substance Class Protein
Created
by admin
on Sun Dec 18 08:11:55 UTC 2022
Edited
by admin
on Sun Dec 18 08:11:55 UTC 2022
Protein Sub Type
Sequence Origin HUMAN
Sequence Type COMPLETE
Record UNII
W3JX5KZ4V2
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
MUSCARINIC ACETYLCHOLINE RECEPTOR M3
Common Name English
CHRM3
Common Name English
Code System Code Type Description
FDA UNII
W3JX5KZ4V2
Created by admin on Sun Dec 18 08:11:58 UTC 2022 , Edited by admin on Sun Dec 18 08:11:58 UTC 2022
PRIMARY
UNIPROT
P20309
Created by admin on Sun Dec 18 08:11:58 UTC 2022 , Edited by admin on Sun Dec 18 08:11:58 UTC 2022
PRIMARY
PHAROS
P20309
Created by admin on Sun Dec 18 08:11:58 UTC 2022 , Edited by admin on Sun Dec 18 08:11:58 UTC 2022
PRIMARY
From To
1_141 1_221
1_517 1_520
Glycosylation Type HUMAN
Glycosylation Link Type Site
N 1_5
N 1_6
N 1_15
N 1_41
N 1_48
Related Record Type Details
INHIBITOR -> TARGET
NON-INHIBITOR->OFF TARGET
Corresponding M3 fragment acid 19 elicited no significant M3 effect when dosed at 1 nmol/kg, strongly supporting our rationale of combining the two pharmacologies into a single agent through a labile moiety.
Ki
INHIBITOR -> TARGET
In the airways, it exhibits pharmacological effects through inhibition of M3 receptor at the smooth muscle leading to bronchodilation.
BINDING
Kd
ANTAGONIST->TARGET
Ki
INHIBITOR -> TARGET
Binding assay
IC50
NON-INHIBITOR->OFF TARGET
NON-INHIBITOR
Ki
INHIBITOR -> TARGET
S-ISOMER BINDS WITH LESS AVIDITY
IC50
INHIBITOR -> TARGET
Ki
INHIBITOR -> TARGET
INHIBITOR -> TARGET
INHIBITOR -> TARGET
INHIBITOR -> TARGET
INHIBITOR -> TARGET
Ki
INHIBITOR -> TARGET
INHIBITOR -> TARGET
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->OFF-TARGET
Radioligand binding assay
BINDING
IC50
NON-INHIBITOR->OFF TARGET
INHIBITOR -> TARGET
INHIBITOR -> TARGET
INHIBITOR -> TARGET
INHIBITOR -> TARGET
Appears to be more bladder-selective for the M3 receptor relative to salivary glands.eptor
Ki
AGONIST -> TARGET
Name Property Type Amount Referenced Substance Defining Parameters References
MOL_WEIGHT CHEMICAL