Compile Data Set for Download or QSAR
Report error Found 13 Enz. Inhib. hit(s) for PDB: 8FX5
TargetMuscarinic acetylcholine receptor M4(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM50003359(CHEMBL73149 | LY 246708 | CHEMBL21536 | 5-(4-Hexyl...)
Affinity DataEC50:  6nMAssay Description:Positive allosteric modulatory activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assess...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/17/2021
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetMuscarinic acetylcholine receptor M4(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM50003359(CHEMBL73149 | LY 246708 | CHEMBL21536 | 5-(4-Hexyl...)
Affinity DataEC50:  18nMAssay Description:Agonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isopr...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/17/2021
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetMuscarinic acetylcholine receptor M4(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM50003359(CHEMBL73149 | LY 246708 | CHEMBL21536 | 5-(4-Hexyl...)
Affinity DataEC50:  6.20nMAssay Description:Agonist activity at human muscarinic M4 receptor expressed in BHK-21 cells coexpressing Galpha16 subunit assessed as increase of acetylcholine-induce...More data for this Ligand-Target Pair
In Depth
Date in BDB:
1/2/2013
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetMuscarinic acetylcholine receptor M4(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM50003359(CHEMBL73149 | LY 246708 | CHEMBL21536 | 5-(4-Hexyl...)
Affinity DataEC50:  6.31E+3nMAssay Description:Agonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein engagement assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/10/2016
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetMuscarinic acetylcholine receptor M4(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM50003359(CHEMBL73149 | LY 246708 | CHEMBL21536 | 5-(4-Hexyl...)
Affinity DataEC50:  16nMAssay Description:Agonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein activation assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/10/2016
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetMuscarinic acetylcholine receptor M4(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM50003359(CHEMBL73149 | LY 246708 | CHEMBL21536 | 5-(4-Hexyl...)
Affinity DataEC50:  186nMAssay Description:Agonist activity at human M4 receptor expressed in HEK293T cells by BRET based beta-arrestin engagement assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/10/2016
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetMuscarinic acetylcholine receptor M4(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM50003359(CHEMBL73149 | LY 246708 | CHEMBL21536 | 5-(4-Hexyl...)
Affinity DataEC50:  229nMAssay Description:Agonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/2/2016
Entry Details Article
PubMedPDB3D3D Structure (crystal)
LigandPNGBDBM50003359(CHEMBL73149 | LY 246708 | CHEMBL21536 | 5-(4-Hexyl...)
Affinity DataIC50: 9.70nMAssay Description:Displacement of [3H]-OXO-M (oxotremorine-M) from the central muscarinic receptor sites of the rat brain membranesMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/17/2010
Entry Details Article
PDB3D3D Structure (crystal)
LigandPNGBDBM50003359(CHEMBL73149 | LY 246708 | CHEMBL21536 | 5-(4-Hexyl...)
Affinity DataIC50: 9.70nMAssay Description:Binding affinity against muscarinic receptor in rat brain membranes using oxotremorine-M as ligandMore data for this Ligand-Target Pair
In Depth
Date in BDB:
9/29/2012
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetMuscarinic acetylcholine receptor M4(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM50003359(CHEMBL73149 | LY 246708 | CHEMBL21536 | 5-(4-Hexyl...)
Affinity DataIC50: 25nMAssay Description:Inhibitory activity was evaluated against Muscarinic acetylcholine receptor M4 expressed in A9 L cellsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
9/22/2013
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetMuscarinic acetylcholine receptor M4(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM50003359(CHEMBL73149 | LY 246708 | CHEMBL21536 | 5-(4-Hexyl...)
Affinity DataKi:  11nMAssay Description:Displacement of [3H]NMS from human M4 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/10/2016
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetMuscarinic acetylcholine receptor M4(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM50003359(CHEMBL73149 | LY 246708 | CHEMBL21536 | 5-(4-Hexyl...)
Affinity DataKi:  19.9nMMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/28/2012
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetMuscarinic acetylcholine receptor M4(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM50003359(CHEMBL73149 | LY 246708 | CHEMBL21536 | 5-(4-Hexyl...)
Affinity DataKi:  72nMAssay Description:Displacement of [3H]-4-DAMP from human muscarinic M4 receptor expressed in BHK-21 cellsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
1/2/2013
Entry Details Article
PubMedPDB3D3D Structure (crystal)