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763-10-0 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:IUPHAR-DB 靶标:mevalonate kinase (Lanosterol biosynthesis pathway) [Homo sapiens]
External ID: 640_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_maxTypeActionReference (PubMed ID)
4.14.1InhibitorCompetitive9392419
4.74.7InhibitorCompetitive9392419
7.57.5InhibitorInhibition14679225
77.5InhibitorFeedback inhibition9392419,18302342
HepG2 Cytotoxicity Assay Measured in Cell-Based System Using Plate Reader - 7071-02_Inhibitor_Dose_DryPowder_Activity_Set16
来源:IUPHAR-DB 靶标:mevalonate kinase (Lanosterol biosynthesis pathway) [Rattus norvegicus]
External ID: 640_Rat
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_maxpIC50_minpIC50_maxTypeActionReference (PubMed ID)
5.35.3InhibitorFeedback inhibition16524256
6.36.3InhibitorInhibition14679225
HepG2 Cytotoxicity Assay Measured in Cell-Based System Using Plate Reader - 7071-02_Inhibitor_Dose_DryPowder_Activity_Set16
来源:ChEMBL 靶标:Squalene synthase ERG9
External ID: CHEMBL3281967
Protocol: N/A
Comment: Compounds with activity <= 10uM or explicitly reported as active by ChEMBL are flagged as active in this PubChem assay presentation.

Journal: J. Med. Chem.
Year: 1977
Volume: 20
Issue: 2
First Page: 243
Last Page: 249
DOI: 10.1021/jm00212a011

Target ChEMBL ID: CHEMBL3271930
ChEMBL Target Name: Squalene synthase
ChEMBL Target Type: SINGLE PROTEIN - Target is a single protein chain
Relationship Type: H - Homologous protein target assigned
Confidence: Homologous single protein target assigned
PubChem Standard ValueStandard TypeStandard RelationStandard ValueStandard UnitsActivity Comment
InhibitionActive
HepG2 Cytotoxicity Assay Measured in Cell-Based System Using Plate Reader - 7071-02_Inhibitor_Dose_DryPowder_Activity_Set16
来源:ChEMBL 靶标:Squalene synthase ERG9
External ID: CHEMBL3281969
Protocol: N/A
Comment: Journal: J. Med. Chem.
Year: 1977
Volume: 20
Issue: 2
First Page: 243
Last Page: 249
DOI: 10.1021/jm00212a011

Target ChEMBL ID: CHEMBL3271930
ChEMBL Target Name: Squalene synthase
ChEMBL Target Type: SINGLE PROTEIN - Target is a single protein chain
Relationship Type: H - Homologous protein target assigned
Confidence: Homologous single protein target assigned
Standard TypeStandard UnitsActivity Comment
Inhibition%Not Active
HepG2 Cytotoxicity Assay Measured in Cell-Based System Using Plate Reader - 7071-02_Inhibitor_Dose_DryPowder_Activity_Set16
来源:ChEMBL 靶标:Squalene synthase ERG9
External ID: CHEMBL3281968
Protocol: N/A
Comment: Journal: J. Med. Chem.
Year: 1977
Volume: 20
Issue: 2
First Page: 243
Last Page: 249
DOI: 10.1021/jm00212a011

Target ChEMBL ID: CHEMBL3271930
ChEMBL Target Name: Squalene synthase
ChEMBL Target Type: SINGLE PROTEIN - Target is a single protein chain
Relationship Type: H - Homologous protein target assigned
Confidence: Homologous single protein target assigned
Standard TypeStandard UnitsActivity Comment
Inhibition%Active
Inhibition%Active
HepG2 Cytotoxicity Assay Measured in Cell-Based System Using Plate Reader - 7071-02_Inhibitor_Dose_DryPowder_Activity_Set16
来源:ChEMBL 靶标:2-C-methyl-D-erythritol 2,4-cyclodiphosphate synthase
External ID: CHEMBL4810482
Protocol: N/A
Comment: Journal: Bioorg Med Chem Lett
Year: 2021
Volume: 48
First Page: 128273
Last Page: 128273
DOI: 10.1016/j.bmcl.2021.128273

Target ChEMBL ID: CHEMBL3091270
ChEMBL Target Name: 2-C-methyl-D-erythritol 2,4-cyclodiphosphate synthase
ChEMBL Target Type: SINGLE PROTEIN - Target is a single protein chain
Relationship Type: H - Homologous protein target assigned
Confidence: Homologous single protein target assigned
Standard TypeActivity Comment
ActivityNot Active
HepG2 Cytotoxicity Assay Measured in Cell-Based System Using Plate Reader - 7071-02_Inhibitor_Dose_DryPowder_Activity_Set16
来源:IUPHAR-DB 靶标:diphosphomevalonate decarboxylase (Lanosterol biosynthesis pathway) [Rattus norvegicus]
External ID: 642_Rat
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_maxpIC50_minpIC50_maxTypeActionReference (PubMed ID)
3.93.9InhibitorCompetitive17888661
HepG2 Cytotoxicity Assay Measured in Cell-Based System Using Plate Reader - 7071-02_Inhibitor_Dose_DryPowder_Activity_Set16
来源:ChEMBL 靶标:Phosphatidylinositol 3,4,5-trisphosphate 5-phosphatase 2
External ID: CHEMBL5053564
Protocol: N/A
Comment: Journal: J Med Chem
Year: 2021
Volume: 64
Issue: 7.0
First Page: 3813
Last Page: 3826
DOI: 10.1021/acs.jmedchem.0c01944

Target ChEMBL ID: CHEMBL2331064
ChEMBL Target Name: Phosphatidylinositol 3,4,5-trisphosphate 5-phosphatase 2
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 TypeActivity Comment
ActivityActive
ActivityActive