前往化源商城

92-35-3 靶点实验数据

HepG2 Cytotoxicity Assay Measured in Cell-Based System Using Plate Reader - 7071-02_Inhibitor_Dose_DryPowder_Activity_Set16
来源:ChEMBL 靶标:Muscarinic acetylcholine receptor M4
External ID: CHEMBL5576405
Protocol: N/A
Comment: Journal: Bioorg Med Chem
Year: 2024
Volume: 105
First Page: 117728
Last Page: 117728
DOI: 10.1016/j.bmc.2024.117728

Target ChEMBL ID: CHEMBL1821
ChEMBL Target Name: Muscarinic acetylcholine receptor M4
ChEMBL Target Type: SINGLE PROTEIN - Target is a single protein chain
Relationship Type: D - Direct protein target assigned
Confidence: Direct single protein target assigned
Standard TypeStandard RelationStandard Value
FC=3
HepG2 Cytotoxicity Assay Measured in Cell-Based System Using Plate Reader - 7071-02_Inhibitor_Dose_DryPowder_Activity_Set16
来源:IUPHAR-DB 靶标:M1 receptor (Acetylcholine receptors (muscarinic)) [Homo sapiens]
External ID: 13_Human
Protocol: The International Union of Basic and Clinical Pharmacology/British Pharmacological Society (IUPHAR/BPS) Guide to PHARMACOLOGY Database (GtoPdb) uses expert subcommittees to collate peer-reviewed information from the published literature regarding individual protein targets, and describes the pharmacology, genetics, function and anatomy of each target. Its pages provide a richly curated overview of the pharmacology of receptors, ion channels, enzymes and other target types, which can be found by following the external link to the GtoPdb website.

Comment: The data collected focuses on ligands at human receptors. Data are provided at rat or mouse orthologues where there are significant species differences, or where data are not yet available at the human target.

Information on individual experimental protocols can be found in the primary references listed for each ligand.

Affinity data are expressed as pKi [-log(Ki)], pKd [-log(Kd)], pIC50 [-log(IC50)], pEC50 [-log(EC50)], pKB [-log(KB)], pA2 or as a micromolar concentration range. In most cases the original concentration can be found in the primary reference.
pKi_minpKi_maxpKd_minpKd_maxpIC50_minpIC50_maxpEC50_minpEC50_maxpKB_minpKB_maxTypeActionReference (PubMed ID)
10.510.5AntagonistAntagonist20133736
4.14.7AgonistPartial agonist1310135
6.46.4Allosteric modulatorPositive10860942
7.37.6AntagonistAntagonist12512959,16439611
6.46.4AgonistFull agonist9224827
7.67.67.27.2AntagonistAntagonist12122494,20590605,21524581
5.15.1AgonistPartial agonist9224827
44AgonistFull agonist9224827
10.610.8AntagonistAntagonist3443095,11578621
1111.1Allosteric modulatorNegative10799315
6.26.2AgonistPartial agonist21558436
9.39.3AntagonistAntagonist20133736
9.99.9AntagonistAntagonist16439611
7.47.4AgonistFull agonist11504829
5.15.1Allosteric modulatorPositive10860942
7.27.5AntagonistAntagonist9671109,1994002
55Allosteric modulatorNegative9224827
5.25.2Allosteric modulatorPositive19438238
9.39.3AntagonistAntagonist11303071
7.17.1AntagonistAntagonist7925952
HepG2 Cytotoxicity Assay Measured in Cell-Based System Using Plate Reader - 7071-02_Inhibitor_Dose_DryPowder_Activity_Set16
来源:IUPHAR-DB 靶标:M2 receptor (Acetylcholine receptors (muscarinic)) [Homo sapiens]
External ID: 14_Human
Protocol: The International Union of Basic and Clinical Pharmacology/British Pharmacological Society (IUPHAR/BPS) Guide to PHARMACOLOGY Database (GtoPdb) uses expert subcommittees to collate peer-reviewed information from the published literature regarding individual protein targets, and describes the pharmacology, genetics, function and anatomy of each target. Its pages provide a richly curated overview of the pharmacology of receptors, ion channels, enzymes and other target types, which can be found by following the external link to the GtoPdb website.

Comment: The data collected focuses on ligands at human receptors. Data are provided at rat or mouse orthologues where there are significant species differences, or where data are not yet available at the human target.

Information on individual experimental protocols can be found in the primary references listed for each ligand.

Affinity data are expressed as pKi [-log(Ki)], pKd [-log(Kd)], pIC50 [-log(IC50)], pEC50 [-log(EC50)], pKB [-log(KB)], pA2 or as a micromolar concentration range. In most cases the original concentration can be found in the primary reference.
pKi_minpKi_maxpKd_minpKd_maxpIC50_minpIC50_maxpEC50_minpEC50_maxpA2_minpA2_maxTypeActionReference (PubMed ID)
10.410.4AntagonistAntagonist23357106
10.310.3AntagonistAntagonist23435542
9.69.6AntagonistAntagonist9454790
4.95Allosteric modulatorPositive7651370,12815174,9224827
5.75.7AgonistFull agonist9224827
6.97.16.26.2AntagonistAntagonist12122494,20590605,21524581
4.94.9AgonistPartial agonist9224827
44AgonistFull agonist9224827
10.110.6AntagonistAntagonist3443095
4.25.7AgonistFull agonist9454790,12235229,9224827
55AntagonistAntagonist10799315
7.27.2AgonistFull agonist11504829
7.89.2AntagonistAntagonist3443095,16188951,2704370,12235229,11303071,12049493,9454790
9.89.8AgonistFull agonist23062057
7.67.6AntagonistAntagonist2704370
6.77.2AntagonistAntagonist2704370,9454790
6.76.7AntagonistAntagonist2704370
6.16.1AgonistAgonist9399977
8.48.6AntagonistInverse agonist16188951,20590605,9671109
5.15.1Allosteric modulatorNeutral9224827
HepG2 Cytotoxicity Assay Measured in Cell-Based System Using Plate Reader - 7071-02_Inhibitor_Dose_DryPowder_Activity_Set16
来源:IUPHAR-DB 靶标:M3 receptor (Acetylcholine receptors (muscarinic)) [Homo sapiens]
External ID: 15_Human
Protocol: The International Union of Basic and Clinical Pharmacology/British Pharmacological Society (IUPHAR/BPS) Guide to PHARMACOLOGY Database (GtoPdb) uses expert subcommittees to collate peer-reviewed information from the published literature regarding individual protein targets, and describes the pharmacology, genetics, function and anatomy of each target. Its pages provide a richly curated overview of the pharmacology of receptors, ion channels, enzymes and other target types, which can be found by following the external link to the GtoPdb website.

Comment: The data collected focuses on ligands at human receptors. Data are provided at rat or mouse orthologues where there are significant species differences, or where data are not yet available at the human target.

Information on individual experimental protocols can be found in the primary references listed for each ligand.

Affinity data are expressed as pKi [-log(Ki)], pKd [-log(Kd)], pIC50 [-log(IC50)], pEC50 [-log(EC50)], pKB [-log(KB)], pA2 or as a micromolar concentration range. In most cases the original concentration can be found in the primary reference.
pKi_minpKi_maxpKd_minpKd_maxpIC50_minpIC50_maxpEC50_minpEC50_maxTypeActionReference (PubMed ID)
10.710.7AntagonistAntagonist23435542
9.511.1AntagonistAntagonist16847442,8441333
4.25.7Allosteric modulatorNegative9224827,7651370
5.75.7AgonistFull agonist9224827
7.786.96.9AntagonistAntagonist12122494,20590605,21524581
5.15.1AgonistPartial agonist9224827
4.24.2AgonistFull agonist9224827
77AgonistPartial agonist10323594
10.410.4AntagonistAntagonist3443095
55AntagonistAntagonist10799315
5.25.2Allosteric modulatorNeutral9224827
3.64Allosteric modulatorNegative9224827,9495826
10.410.4AntagonistAntagonist16847442
7.17.7AgonistFull agonist11504829
8.38.3AgonistFull agonist11504829
8.48.4AntagonistAntagonist1346637
8.98.9AntagonistAntagonist2704370
8.98.9AntagonistAntagonist2704370
6.16.1AntagonistAntagonist2704370
7.87.8AntagonistAntagonist2704370
HepG2 Cytotoxicity Assay Measured in Cell-Based System Using Plate Reader - 7071-02_Inhibitor_Dose_DryPowder_Activity_Set16
来源:IUPHAR-DB 靶标:M4 receptor (Acetylcholine receptors (muscarinic)) [Homo sapiens]
External ID: 16_Human
Protocol: The International Union of Basic and Clinical Pharmacology/British Pharmacological Society (IUPHAR/BPS) Guide to PHARMACOLOGY Database (GtoPdb) uses expert subcommittees to collate peer-reviewed information from the published literature regarding individual protein targets, and describes the pharmacology, genetics, function and anatomy of each target. Its pages provide a richly curated overview of the pharmacology of receptors, ion channels, enzymes and other target types, which can be found by following the external link to the GtoPdb website.

Comment: The data collected focuses on ligands at human receptors. Data are provided at rat or mouse orthologues where there are significant species differences, or where data are not yet available at the human target.

Information on individual experimental protocols can be found in the primary references listed for each ligand.

Affinity data are expressed as pKi [-log(Ki)], pKd [-log(Kd)], pIC50 [-log(IC50)], pEC50 [-log(EC50)], pKB [-log(KB)], pA2 or as a micromolar concentration range. In most cases the original concentration can be found in the primary reference.
pKi_minpKi_maxpKd_minpKd_maxpIC50_minpIC50_maxpEC50_minpEC50_maxTypeActionReference (PubMed ID)
5.35.3Allosteric modulatorNeutral10860942
6.46.4Allosteric modulatorNeutral10860942
5.95.9AgonistFull agonist9224827
6.86.8AntagonistAntagonist20590605
5.25.2AgonistPartial agonist9224827
44AgonistFull agonist9224827
7.27.2AgonistPartial agonist10323594
9.710.5AntagonistAntagonist3443095,11578621
5.95.9AntagonistAntagonist12512959
55AntagonistAntagonist10799315
4.76Allosteric modulatorNegative9224827,9495826
7.37.3AgonistFull agonist11504829
8.68.6AgonistFull agonist11504829
8.68.6AntagonistAntagonist1346637
8.58.5AntagonistAntagonist2704370
8.38.3AntagonistAntagonist2704370
77AntagonistAntagonist8759038
7.17.1AntagonistAntagonist2704370
66AgonistAgonist9399977
4.24.2Allosteric modulatorPositive9224827