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Found 22 hits Enz. Inhib. hit(s) with Target = 'Muscarinic acetylcholine receptor M1/M2/M3/M4/M5' and Ligand = 'BDBM50004665'   
Target/Host
(Institution)
LigandTarget/Host
Links
Ligand
Links
Trg + Lig
Links
Ki
nM
ΔG°
kJ/mole
IC50
nM
Kd
nM
EC50/IC50
nM
koff
s-1
kon
M-1s-1
pHTemp
°C
Muscarinic acetylcholine receptor M1/M2/M3/M4/M5


(RAT)
BDBM50004665
PNG
((oxotremorine)1-(4-Pyrrolidin-1-yl-but-2-ynyl)-pyr...)
Show SMILES O=C1CCCN1CC#CCN1CCCC1
Show InChI InChI=1S/C12H18N2O/c15-12-6-5-11-14(12)10-4-3-9-13-7-1-2-8-13/h1-2,5-11H2
PDB
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0.5n/an/an/an/an/an/an/an/a


TBA

Assay Description
In vitro ability to displace 3H-cis-methyltrimethylammoniummethyl-1,3-dioxolane [3H]CD) from rat cortical Muscarinic acetylcholine receptor in compet...


Citation and Details

BindingDB Entry DOI: 10.7270/Q2RF5X57
More data for this
Ligand-Target Pair
Muscarinic acetylcholine receptor M1/M2/M3/M4/M5


(RAT)
BDBM50004665
PNG
((oxotremorine)1-(4-Pyrrolidin-1-yl-but-2-ynyl)-pyr...)
Show SMILES O=C1CCCN1CC#CCN1CCCC1
Show InChI InChI=1S/C12H18N2O/c15-12-6-5-11-14(12)10-4-3-9-13-7-1-2-8-13/h1-2,5-11H2
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0.5n/an/an/an/an/an/an/an/a



Upjohn Company

Curated by ChEMBL


Assay Description
Binding affinity to muscarinic acetylcholine receptor was determined in presence of [3H]OXO-M radioligand (in vitro)


J Med Chem 34: 2314-27 (1991)


BindingDB Entry DOI: 10.7270/Q2057J5V
More data for this
Ligand-Target Pair
Muscarinic acetylcholine receptor M1/M2/M3/M4/M5


(RAT)
BDBM50004665
PNG
((oxotremorine)1-(4-Pyrrolidin-1-yl-but-2-ynyl)-pyr...)
Show SMILES O=C1CCCN1CC#CCN1CCCC1
Show InChI InChI=1S/C12H18N2O/c15-12-6-5-11-14(12)10-4-3-9-13-7-1-2-8-13/h1-2,5-11H2
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0.5n/an/an/an/an/an/an/an/a



American Cyanamid Company

Curated by ChEMBL


Assay Description
Competitive inhibition of recombinant TAK1-TAB1 assessed as [33P]gamma-ATP incorporation into substrate histone H1 peptide by filter plate assay


J Med Chem 33: 3190-8 (1990)


BindingDB Entry DOI: 10.7270/Q2M32Z0K
More data for this
Ligand-Target Pair
Muscarinic acetylcholine receptor M1/M2/M3/M4/M5


(RAT)
BDBM50004665
PNG
((oxotremorine)1-(4-Pyrrolidin-1-yl-but-2-ynyl)-pyr...)
Show SMILES O=C1CCCN1CC#CCN1CCCC1
Show InChI InChI=1S/C12H18N2O/c15-12-6-5-11-14(12)10-4-3-9-13-7-1-2-8-13/h1-2,5-11H2
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4n/an/an/an/an/an/an/an/a



American Cyanamid Company

Curated by ChEMBL


Assay Description
Binding activity to muscarinic acetylcholine receptor in rat heart, assayed using [3H]-QNB as a radioligand.


J Med Chem 33: 3190-8 (1990)


BindingDB Entry DOI: 10.7270/Q2M32Z0K
More data for this
Ligand-Target Pair
Muscarinic acetylcholine receptor M1/M2/M3/M4/M5


(RAT)
BDBM50004665
PNG
((oxotremorine)1-(4-Pyrrolidin-1-yl-but-2-ynyl)-pyr...)
Show SMILES O=C1CCCN1CC#CCN1CCCC1
Show InChI InChI=1S/C12H18N2O/c15-12-6-5-11-14(12)10-4-3-9-13-7-1-2-8-13/h1-2,5-11H2
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60n/an/an/an/an/an/an/an/a


TBA

Assay Description
In vitro ability to displace [3H]quinuclidinyl benzilate [3H]QNB) from rat cortical Muscarinic acetylcholine receptor in competition assay


Citation and Details

BindingDB Entry DOI: 10.7270/Q2RF5X57
More data for this
Ligand-Target Pair
Muscarinic acetylcholine receptor M1/M2/M3/M4/M5


(RAT)
BDBM50004665
PNG
((oxotremorine)1-(4-Pyrrolidin-1-yl-but-2-ynyl)-pyr...)
Show SMILES O=C1CCCN1CC#CCN1CCCC1
Show InChI InChI=1S/C12H18N2O/c15-12-6-5-11-14(12)10-4-3-9-13-7-1-2-8-13/h1-2,5-11H2
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60n/an/an/an/an/an/an/an/a



American Cyanamid Company

Curated by ChEMBL


Assay Description
Competitive inhibition of recombinant TAK1-TAB1 assessed as [33P]gamma-ATP incorporation into substrate histone H1 peptide by filter plate assay


J Med Chem 33: 3190-8 (1990)


BindingDB Entry DOI: 10.7270/Q2M32Z0K
More data for this
Ligand-Target Pair
Muscarinic acetylcholine receptor M1/M2/M3/M4/M5


(RAT)
BDBM50004665
PNG
((oxotremorine)1-(4-Pyrrolidin-1-yl-but-2-ynyl)-pyr...)
Show SMILES O=C1CCCN1CC#CCN1CCCC1
Show InChI InChI=1S/C12H18N2O/c15-12-6-5-11-14(12)10-4-3-9-13-7-1-2-8-13/h1-2,5-11H2
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140n/an/an/an/an/an/an/an/a



American Cyanamid Company

Curated by ChEMBL


Assay Description
Binding activity to the muscarinic acetylcholine receptor in rat cortex, assayed using [3H]PZ as a radioligand.


J Med Chem 33: 3190-8 (1990)


BindingDB Entry DOI: 10.7270/Q2M32Z0K
More data for this
Ligand-Target Pair
Muscarinic acetylcholine receptor M1/M2/M3/M4/M5


(RAT)
BDBM50004665
PNG
((oxotremorine)1-(4-Pyrrolidin-1-yl-but-2-ynyl)-pyr...)
Show SMILES O=C1CCCN1CC#CCN1CCCC1
Show InChI InChI=1S/C12H18N2O/c15-12-6-5-11-14(12)10-4-3-9-13-7-1-2-8-13/h1-2,5-11H2
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140n/an/an/an/an/an/an/an/a



American Cyanamid Company

Curated by ChEMBL


Assay Description
Binding activity to muscarinic acetylcholine receptor in rat heart, assayed using [3H]QNB as a radioligand in the presence of Gpp(NH)p.


J Med Chem 33: 3190-8 (1990)


BindingDB Entry DOI: 10.7270/Q2M32Z0K
More data for this
Ligand-Target Pair
Muscarinic acetylcholine receptor M1/M2/M3/M4/M5


(RAT)
BDBM50004665
PNG
((oxotremorine)1-(4-Pyrrolidin-1-yl-but-2-ynyl)-pyr...)
Show SMILES O=C1CCCN1CC#CCN1CCCC1
Show InChI InChI=1S/C12H18N2O/c15-12-6-5-11-14(12)10-4-3-9-13-7-1-2-8-13/h1-2,5-11H2
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193n/an/an/an/an/an/an/an/a



Upjohn Company

Curated by ChEMBL


Assay Description
Binding affinity to muscarinic acetylcholine receptor was determined in presence of [3H]QNB radioligand (in vitro)


J Med Chem 34: 2314-27 (1991)


BindingDB Entry DOI: 10.7270/Q2057J5V
More data for this
Ligand-Target Pair
Muscarinic acetylcholine receptor M1/M2/M3/M4/M5


(RAT)
BDBM50004665
PNG
((oxotremorine)1-(4-Pyrrolidin-1-yl-but-2-ynyl)-pyr...)
Show SMILES O=C1CCCN1CC#CCN1CCCC1
Show InChI InChI=1S/C12H18N2O/c15-12-6-5-11-14(12)10-4-3-9-13-7-1-2-8-13/h1-2,5-11H2
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230n/an/an/an/an/an/an/an/a



University of Uppsala

Curated by ChEMBL


Assay Description
Inhibition of Shh signaling in mouse Shh-light2 cells by Gli-dependent firefly luciferase reporter gene assay


J Med Chem 35: 3270-9 (1992)


BindingDB Entry DOI: 10.7270/Q2KP813K
More data for this
Ligand-Target Pair
Muscarinic acetylcholine receptor M1/M2/M3/M4/M5


(RAT)
BDBM50004665
PNG
((oxotremorine)1-(4-Pyrrolidin-1-yl-but-2-ynyl)-pyr...)
Show SMILES O=C1CCCN1CC#CCN1CCCC1
Show InChI InChI=1S/C12H18N2O/c15-12-6-5-11-14(12)10-4-3-9-13-7-1-2-8-13/h1-2,5-11H2
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830n/an/an/an/an/an/an/an/a



University of Uppsala

Curated by ChEMBL


Assay Description
In vitro inhibition of binding of (-)-[3H]-NMS to Muscarinic acetylcholine receptor of rat cerebral cortex was determined


J Med Chem 33: 580-4 (1990)


BindingDB Entry DOI: 10.7270/Q2GB2687
More data for this
Ligand-Target Pair
Muscarinic acetylcholine receptor M1/M2/M3/M4/M5


(RAT)
BDBM50004665
PNG
((oxotremorine)1-(4-Pyrrolidin-1-yl-but-2-ynyl)-pyr...)
Show SMILES O=C1CCCN1CC#CCN1CCCC1
Show InChI InChI=1S/C12H18N2O/c15-12-6-5-11-14(12)10-4-3-9-13-7-1-2-8-13/h1-2,5-11H2
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Article
n/an/a 1.5n/an/an/an/an/an/a



TBA

Curated by ChEMBL


Assay Description
Inhibition of 0.1 nM [3H]cis-methyldioxolane binding to rat neocortex muscarinic receptor


Bioorg Med Chem Lett 2: 803-808 (1992)


Article DOI: 10.1016/S0960-894X(00)80535-1
BindingDB Entry DOI: 10.7270/Q2Z0382N
More data for this
Ligand-Target Pair
Muscarinic acetylcholine receptor M1/M2/M3/M4/M5


(RAT)
BDBM50004665
PNG
((oxotremorine)1-(4-Pyrrolidin-1-yl-but-2-ynyl)-pyr...)
Show SMILES O=C1CCCN1CC#CCN1CCCC1
Show InChI InChI=1S/C12H18N2O/c15-12-6-5-11-14(12)10-4-3-9-13-7-1-2-8-13/h1-2,5-11H2
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Article
n/an/a 2n/an/an/an/an/an/a



TBA

Curated by ChEMBL


Assay Description
Binding affinity against Muscarinic receptor M2 in rat brain using [3H]-QNB (quinuclidinyl benzylate) radioligand at a concentration of 0.12 nM


Bioorg Med Chem Lett 7: 1033-1036 (1997)


Article DOI: 10.1016/S0960-894X(97)00150-9
BindingDB Entry DOI: 10.7270/Q2S46RZ2
More data for this
Ligand-Target Pair
Muscarinic acetylcholine receptor M1/M2/M3/M4/M5


(RAT)
BDBM50004665
PNG
((oxotremorine)1-(4-Pyrrolidin-1-yl-but-2-ynyl)-pyr...)
Show SMILES O=C1CCCN1CC#CCN1CCCC1
Show InChI InChI=1S/C12H18N2O/c15-12-6-5-11-14(12)10-4-3-9-13-7-1-2-8-13/h1-2,5-11H2
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n/an/a 2.80n/an/an/an/an/an/a



Sandoz Pharma Ltd.

Curated by ChEMBL


Assay Description
Ability to displace [3H]cis--2-methyl-5-((dimethylamino)methyl)-1,3-di oxolane from muscarinic acetylcholine receptor in rat cortical tissue.


J Med Chem 35: 15-27 (1992)


BindingDB Entry DOI: 10.7270/Q29022RV
More data for this
Ligand-Target Pair
Muscarinic acetylcholine receptor M1/M2/M3/M4/M5


(RAT)
BDBM50004665
PNG
((oxotremorine)1-(4-Pyrrolidin-1-yl-but-2-ynyl)-pyr...)
Show SMILES O=C1CCCN1CC#CCN1CCCC1
Show InChI InChI=1S/C12H18N2O/c15-12-6-5-11-14(12)10-4-3-9-13-7-1-2-8-13/h1-2,5-11H2
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n/an/a 17n/an/an/an/an/an/a



SmithKline Beecham Pharmaceuticals

Curated by ChEMBL


Assay Description
In vitro ability to displace [3H]oxotremorine-M (OXO-M) from rat cerebral cortex muscarinic acetylcholine receptor


J Med Chem 35: 2392-406 (1992)


BindingDB Entry DOI: 10.7270/Q2TF00K5
More data for this
Ligand-Target Pair
Muscarinic acetylcholine receptor M1/M2/M3/M4/M5


(RAT)
BDBM50004665
PNG
((oxotremorine)1-(4-Pyrrolidin-1-yl-but-2-ynyl)-pyr...)
Show SMILES O=C1CCCN1CC#CCN1CCCC1
Show InChI InChI=1S/C12H18N2O/c15-12-6-5-11-14(12)10-4-3-9-13-7-1-2-8-13/h1-2,5-11H2
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n/an/a 17n/an/an/an/an/an/a



SmithKline Beecham Pharmaceuticals

Curated by ChEMBL


Assay Description
In vitro inhibition of [3H]OXO-M binding to Muscarinic receptor from rat cortical homogenates


J Med Chem 35: 1280-90 (1992)


BindingDB Entry DOI: 10.7270/Q2G1632Q
More data for this
Ligand-Target Pair
Muscarinic acetylcholine receptor M1/M2/M3/M4/M5


(RAT)
BDBM50004665
PNG
((oxotremorine)1-(4-Pyrrolidin-1-yl-but-2-ynyl)-pyr...)
Show SMILES O=C1CCCN1CC#CCN1CCCC1
Show InChI InChI=1S/C12H18N2O/c15-12-6-5-11-14(12)10-4-3-9-13-7-1-2-8-13/h1-2,5-11H2
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Article
n/an/a 407n/an/an/an/an/an/a



TBA

Curated by ChEMBL


Assay Description
Inhibition of 0.03 nM [3H]quinuclidinyl benzylate binding to rat neocortex muscarinic receptor


Bioorg Med Chem Lett 2: 803-808 (1992)


Article DOI: 10.1016/S0960-894X(00)80535-1
BindingDB Entry DOI: 10.7270/Q2Z0382N
More data for this
Ligand-Target Pair
Muscarinic acetylcholine receptor M1/M2/M3/M4/M5


(RAT)
BDBM50004665
PNG
((oxotremorine)1-(4-Pyrrolidin-1-yl-but-2-ynyl)-pyr...)
Show SMILES O=C1CCCN1CC#CCN1CCCC1
Show InChI InChI=1S/C12H18N2O/c15-12-6-5-11-14(12)10-4-3-9-13-7-1-2-8-13/h1-2,5-11H2
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n/an/a 660n/an/an/an/an/an/a



Hoechst-Roussel Pharmaceuticals Inc.

Curated by ChEMBL


Assay Description
Inhibition of [3H]quinuclidinyl benzilate (QNB) binding from rat forebrain membranes in the presence of Zn


J Med Chem 39: 570-81 (1996)


Article DOI: 10.1021/jm9506433
BindingDB Entry DOI: 10.7270/Q2BR8R7K
More data for this
Ligand-Target Pair
Muscarinic acetylcholine receptor M1/M2/M3/M4/M5


(RAT)
BDBM50004665
PNG
((oxotremorine)1-(4-Pyrrolidin-1-yl-but-2-ynyl)-pyr...)
Show SMILES O=C1CCCN1CC#CCN1CCCC1
Show InChI InChI=1S/C12H18N2O/c15-12-6-5-11-14(12)10-4-3-9-13-7-1-2-8-13/h1-2,5-11H2
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n/an/a 2.70E+3n/an/an/an/an/an/a



Hoechst-Roussel Pharmaceuticals Inc.

Curated by ChEMBL


Assay Description
Inhibition of [3H]quinuclidinyl benzilate (QNB) binding from rat forebrain membranes in the absence of Zn


J Med Chem 39: 570-81 (1996)


Article DOI: 10.1021/jm9506433
BindingDB Entry DOI: 10.7270/Q2BR8R7K
More data for this
Ligand-Target Pair
Muscarinic acetylcholine receptor M1/M2/M3/M4/M5


(RAT)
BDBM50004665
PNG
((oxotremorine)1-(4-Pyrrolidin-1-yl-but-2-ynyl)-pyr...)
Show SMILES O=C1CCCN1CC#CCN1CCCC1
Show InChI InChI=1S/C12H18N2O/c15-12-6-5-11-14(12)10-4-3-9-13-7-1-2-8-13/h1-2,5-11H2
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n/an/a 3.30E+3n/an/an/an/an/an/a



SmithKline Beecham Pharmaceuticals

Curated by ChEMBL


Assay Description
In vitro inhibition of [3H]QNB binding to Muscarinic receptor from rat cortical homogenates


J Med Chem 35: 1280-90 (1992)


BindingDB Entry DOI: 10.7270/Q2G1632Q
More data for this
Ligand-Target Pair
Muscarinic acetylcholine receptor M1/M2/M3/M4/M5


(RAT)
BDBM50004665
PNG
((oxotremorine)1-(4-Pyrrolidin-1-yl-but-2-ynyl)-pyr...)
Show SMILES O=C1CCCN1CC#CCN1CCCC1
Show InChI InChI=1S/C12H18N2O/c15-12-6-5-11-14(12)10-4-3-9-13-7-1-2-8-13/h1-2,5-11H2
PDB
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n/an/a 3.30E+3n/an/an/an/an/an/a



SmithKline Beecham Pharmaceuticals

Curated by ChEMBL


Assay Description
In vitro ability to displace [3H]quinuclidinyl benzilate (QNB) from rat cerebral cortex muscarinic acetylcholine receptor


J Med Chem 35: 2392-406 (1992)


BindingDB Entry DOI: 10.7270/Q2TF00K5
More data for this
Ligand-Target Pair
Muscarinic acetylcholine receptor M1/M2/M3/M4/M5


(Homo sapiens (Human))
BDBM50004665
PNG
((oxotremorine)1-(4-Pyrrolidin-1-yl-but-2-ynyl)-pyr...)
Show SMILES O=C1CCCN1CC#CCN1CCCC1
Show InChI InChI=1S/C12H18N2O/c15-12-6-5-11-14(12)10-4-3-9-13-7-1-2-8-13/h1-2,5-11H2
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MMDB

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n/an/an/a 930n/an/an/an/an/a



University of Uppsala

Curated by ChEMBL


Assay Description
Dissociation constant of the drug-Muscarinic acetylcholine receptor complex.


J Med Chem 33: 580-4 (1990)


BindingDB Entry DOI: 10.7270/Q2GB2687
More data for this
Ligand-Target Pair