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175139-41-0 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:ChEMBL 靶标:Rattus norvegicus
External ID: CHEMBL935141
Protocol: N/A
Comment: Journal: J. Med. Chem.
Year: 2008
Volume: 51
Issue: 5
First Page: 1385
Last Page: 1392
DOI: 10.1021/jm070579c

Target ChEMBL ID: CHEMBL376
ChEMBL Target Name: Rattus norvegicus
ChEMBL Target Type: ORGANISM - Target is a complete organism
Relationship Type: N - Non-molecular target assigned
Confidence: Target assigned is non-molecular
Standard TypeStandard RelationStandard ValueStandard UnitsActivity Comment
InhibitionNot Determined
Inhibition=79%
Inhibition=75%
Inhibition=81%
HepG2 Cytotoxicity Assay Measured in Cell-Based System Using Plate Reader - 7071-02_Inhibitor_Dose_DryPowder_Activity_Set16
来源:ChEMBL 靶标:Rattus norvegicus
External ID: CHEMBL935142
Protocol: N/A
Comment: Journal: J. Med. Chem.
Year: 2008
Volume: 51
Issue: 5
First Page: 1385
Last Page: 1392
DOI: 10.1021/jm070579c

Target ChEMBL ID: CHEMBL376
ChEMBL Target Name: Rattus norvegicus
ChEMBL Target Type: ORGANISM - Target is a complete organism
Relationship Type: N - Non-molecular target assigned
Confidence: Target assigned is non-molecular
Standard TypeStandard RelationStandard ValueStandard UnitsActivity Comment
InhibitionNot Determined
Inhibition=72%
Inhibition=72%
Inhibition=49%
HepG2 Cytotoxicity Assay Measured in Cell-Based System Using Plate Reader - 7071-02_Inhibitor_Dose_DryPowder_Activity_Set16
来源:ChEMBL 靶标:Corticotropin-releasing factor receptor 1
External ID: CHEMBL935136
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: 2008
Volume: 51
Issue: 5
First Page: 1385
Last Page: 1392
DOI: 10.1021/jm070579c

Target ChEMBL ID: CHEMBL4649
ChEMBL Target Name: Corticotropin releasing factor receptor 1
ChEMBL Target Type: SINGLE PROTEIN - Target is a single protein chain
Relationship Type: D - Direct protein target assigned
Confidence: Direct single protein target assigned
PubChem Standard ValueStandard TypeStandard RelationStandard ValueStandard UnitsActivity Comment
0.75IC50=750nM
0.0309IC50=30.9nM
0.0068IC50=6.8nM
0.005129IC50=5.129nM
0.0051IC50=5.1nM
HepG2 Cytotoxicity Assay Measured in Cell-Based System Using Plate Reader - 7071-02_Inhibitor_Dose_DryPowder_Activity_Set16
来源:ChEMBL 靶标:Corticotropin-releasing factor receptor 1
External ID: CHEMBL1764891
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: Bioorg. Med. Chem. Lett.
Year: 2011
Volume: 21
Issue: 8
First Page: 2365
Last Page: 2371
DOI: 10.1016/j.bmcl.2011.02.086

Target ChEMBL ID: CHEMBL1800
ChEMBL Target Name: Corticotropin releasing factor receptor 1
ChEMBL Target Type: SINGLE PROTEIN - Target is a single protein chain
Relationship Type: D - Direct protein target assigned
Confidence: Direct single protein target assigned
PubChem Standard ValueStandard TypeStandard RelationStandard ValueStandard Units
0.97IC50=970nM
1.6IC50=1600nM
HepG2 Cytotoxicity Assay Measured in Cell-Based System Using Plate Reader - 7071-02_Inhibitor_Dose_DryPowder_Activity_Set16
来源:ChEMBL 靶标:N/A
External ID: CHEMBL935084
Protocol: N/A
Comment: Journal: J. Med. Chem.
Year: 2008
Volume: 51
Issue: 5
First Page: 1377
Last Page: 1384
DOI: 10.1021/jm070578k
Standard TypeStandard RelationStandard Value
pKa=3.5
HepG2 Cytotoxicity Assay Measured in Cell-Based System Using Plate Reader - 7071-02_Inhibitor_Dose_DryPowder_Activity_Set16
来源:ChEMBL 靶标:N/A
External ID: CHEMBL935085
Protocol: N/A
Comment: Journal: J. Med. Chem.
Year: 2008
Volume: 51
Issue: 5
First Page: 1377
Last Page: 1384
DOI: 10.1021/jm070578k
Standard TypeStandard RelationStandard ValueStandard Units
Solubility<1ug.mL-1
HepG2 Cytotoxicity Assay Measured in Cell-Based System Using Plate Reader - 7071-02_Inhibitor_Dose_DryPowder_Activity_Set16
来源:ChEMBL 靶标:Corticotropin-releasing factor receptor 1
External ID: CHEMBL935083
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: 2008
Volume: 51
Issue: 5
First Page: 1377
Last Page: 1384
DOI: 10.1021/jm070578k

Target ChEMBL ID: CHEMBL4649
ChEMBL Target Name: Corticotropin releasing factor receptor 1
ChEMBL Target Type: SINGLE PROTEIN - Target is a single protein chain
Relationship Type: D - Direct protein target assigned
Confidence: Direct single protein target assigned
PubChem Standard ValueStandard TypeStandard RelationStandard ValueStandard Units
0.0098IC50=9.8nM
0.03162IC50=31.62nM
0.086IC50=86nM
0.0123IC50=12.3nM
HepG2 Cytotoxicity Assay Measured in Cell-Based System Using Plate Reader - 7071-02_Inhibitor_Dose_DryPowder_Activity_Set16
来源:ChEMBL 靶标:Canis lupus familiaris
External ID: CHEMBL934316
Protocol: N/A
Comment: Journal: J. Med. Chem.
Year: 2008
Volume: 51
Issue: 5
First Page: 1385
Last Page: 1392
DOI: 10.1021/jm070579c

Target ChEMBL ID: CHEMBL373
ChEMBL Target Name: Canis familiaris
ChEMBL Target Type: ORGANISM - Target is a complete organism
Relationship Type: N - Non-molecular target assigned
Confidence: Target assigned is non-molecular
Standard TypeStandard RelationStandard ValueStandard Units
T1/2=8.3hr
T1/2=8.8hr
HepG2 Cytotoxicity Assay Measured in Cell-Based System Using Plate Reader - 7071-02_Inhibitor_Dose_DryPowder_Activity_Set16
来源:ChEMBL 靶标:Rattus norvegicus
External ID: CHEMBL935092
Protocol: N/A
Comment: Journal: J. Med. Chem.
Year: 2008
Volume: 51
Issue: 5
First Page: 1377
Last Page: 1384
DOI: 10.1021/jm070578k

Target ChEMBL ID: CHEMBL376
ChEMBL Target Name: Rattus norvegicus
ChEMBL Target Type: ORGANISM - Target is a complete organism
Relationship Type: N - Non-molecular target assigned
Confidence: Target assigned is non-molecular
Standard TypeStandard RelationStandard ValueStandard Units
MED=10mg kg-1
ID50=35mg.kg-1
HepG2 Cytotoxicity Assay Measured in Cell-Based System Using Plate Reader - 7071-02_Inhibitor_Dose_DryPowder_Activity_Set16
来源:ChEMBL 靶标:N/A
External ID: CHEMBL935093
Protocol: N/A
Comment: Journal: J. Med. Chem.
Year: 2008
Volume: 51
Issue: 5
First Page: 1377
Last Page: 1384
DOI: 10.1021/jm070578k
Standard TypeStandard RelationStandard ValueStandard Units
Solubility=0.2ug.mL-1
HepG2 Cytotoxicity Assay Measured in Cell-Based System Using Plate Reader - 7071-02_Inhibitor_Dose_DryPowder_Activity_Set16
来源:ChEMBL 靶标:N/A
External ID: CHEMBL935094
Protocol: N/A
Comment: Journal: J. Med. Chem.
Year: 2008
Volume: 51
Issue: 5
First Page: 1377
Last Page: 1384
DOI: 10.1021/jm070578k
Standard TypeStandard RelationStandard ValueStandard Units
Solubility=3ug.mL-1
HepG2 Cytotoxicity Assay Measured in Cell-Based System Using Plate Reader - 7071-02_Inhibitor_Dose_DryPowder_Activity_Set16
来源:ChEMBL 靶标:Canis lupus familiaris
External ID: CHEMBL934319
Protocol: N/A
Comment: Journal: J. Med. Chem.
Year: 2008
Volume: 51
Issue: 5
First Page: 1385
Last Page: 1392
DOI: 10.1021/jm070579c

Target ChEMBL ID: CHEMBL373
ChEMBL Target Name: Canis familiaris
ChEMBL Target Type: ORGANISM - Target is a complete organism
Relationship Type: N - Non-molecular target assigned
Confidence: Target assigned is non-molecular
Standard TypeStandard RelationStandard ValueStandard Units
Tmax=1.5hr
HepG2 Cytotoxicity Assay Measured in Cell-Based System Using Plate Reader - 7071-02_Inhibitor_Dose_DryPowder_Activity_Set16
来源:ChEMBL 靶标:Rattus norvegicus
External ID: CHEMBL935088
Protocol: N/A
Comment: Journal: J. Med. Chem.
Year: 2008
Volume: 51
Issue: 5
First Page: 1377
Last Page: 1384
DOI: 10.1021/jm070578k

Target ChEMBL ID: CHEMBL376
ChEMBL Target Name: Rattus norvegicus
ChEMBL Target Type: ORGANISM - Target is a complete organism
Relationship Type: N - Non-molecular target assigned
Confidence: Target assigned is non-molecular
Standard TypeStandard RelationStandard ValueStandard Units
Inhibition=75%
HepG2 Cytotoxicity Assay Measured in Cell-Based System Using Plate Reader - 7071-02_Inhibitor_Dose_DryPowder_Activity_Set16
来源:ChEMBL 靶标:Canis lupus familiaris
External ID: CHEMBL934313
Protocol: N/A
Comment: Journal: J. Med. Chem.
Year: 2008
Volume: 51
Issue: 5
First Page: 1385
Last Page: 1392
DOI: 10.1021/jm070579c

Target ChEMBL ID: CHEMBL373
ChEMBL Target Name: Canis familiaris
ChEMBL Target Type: ORGANISM - Target is a complete organism
Relationship Type: N - Non-molecular target assigned
Confidence: Target assigned is non-molecular
Standard TypeStandard RelationStandard ValueStandard Units
CL=4.1mL.min-1.kg-1
CL=17mL.min-1.kg-1
HepG2 Cytotoxicity Assay Measured in Cell-Based System Using Plate Reader - 7071-02_Inhibitor_Dose_DryPowder_Activity_Set16
来源:ChEMBL 靶标:Canis lupus familiaris
External ID: CHEMBL934314
Protocol: N/A
Comment: Journal: J. Med. Chem.
Year: 2008
Volume: 51
Issue: 5
First Page: 1385
Last Page: 1392
DOI: 10.1021/jm070579c

Target ChEMBL ID: CHEMBL373
ChEMBL Target Name: Canis familiaris
ChEMBL Target Type: ORGANISM - Target is a complete organism
Relationship Type: N - Non-molecular target assigned
Confidence: Target assigned is non-molecular
Standard TypeStandard RelationStandard ValueStandard Units
Vdss=1.1L.kg-1
Vdss=5.3L.kg-1
HepG2 Cytotoxicity Assay Measured in Cell-Based System Using Plate Reader - 7071-02_Inhibitor_Dose_DryPowder_Activity_Set16
来源:ChEMBL 靶标:Rattus norvegicus
External ID: CHEMBL935090
Protocol: N/A
Comment: Journal: J. Med. Chem.
Year: 2008
Volume: 51
Issue: 5
First Page: 1377
Last Page: 1384
DOI: 10.1021/jm070578k

Target ChEMBL ID: CHEMBL376
ChEMBL Target Name: Rattus norvegicus
ChEMBL Target Type: ORGANISM - Target is a complete organism
Relationship Type: N - Non-molecular target assigned
Confidence: Target assigned is non-molecular
Standard TypeStandard RelationStandard ValueStandard UnitsData Validity Comment
Inhibition=72%
HepG2 Cytotoxicity Assay Measured in Cell-Based System Using Plate Reader - 7071-02_Inhibitor_Dose_DryPowder_Activity_Set16
来源:ChEMBL 靶标:Corticotropin-releasing factor receptor 1
External ID: CHEMBL1811340
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: 2011
Volume: 54
Issue: 12
First Page: 4187
Last Page: 4206
DOI: 10.1021/jm200365y

Target ChEMBL ID: CHEMBL4649
ChEMBL Target Name: Corticotropin releasing factor receptor 1
ChEMBL Target Type: SINGLE PROTEIN - Target is a single protein chain
Relationship Type: D - Direct protein target assigned
Confidence: Direct single protein target assigned
PubChem Standard ValueStandard TypeStandard RelationStandard ValueStandard Units
0.0061IC50=6.1nM
HepG2 Cytotoxicity Assay Measured in Cell-Based System Using Plate Reader - 7071-02_Inhibitor_Dose_DryPowder_Activity_Set16
来源:ChEMBL 靶标:Canis lupus familiaris
External ID: CHEMBL934315
Protocol: N/A
Comment: Journal: J. Med. Chem.
Year: 2008
Volume: 51
Issue: 5
First Page: 1385
Last Page: 1392
DOI: 10.1021/jm070579c

Target ChEMBL ID: CHEMBL373
ChEMBL Target Name: Canis familiaris
ChEMBL Target Type: ORGANISM - Target is a complete organism
Relationship Type: N - Non-molecular target assigned
Confidence: Target assigned is non-molecular
Standard TypeStandard RelationStandard ValueStandard Units
Vd=3.1L.kg-1
Vd=12L.kg-1
HepG2 Cytotoxicity Assay Measured in Cell-Based System Using Plate Reader - 7071-02_Inhibitor_Dose_DryPowder_Activity_Set16
来源:ChEMBL 靶标:Canis lupus familiaris
External ID: CHEMBL935235
Protocol: N/A
Comment: Journal: J. Med. Chem.
Year: 2008
Volume: 51
Issue: 5
First Page: 1385
Last Page: 1392
DOI: 10.1021/jm070579c

Target ChEMBL ID: CHEMBL373
ChEMBL Target Name: Canis familiaris
ChEMBL Target Type: ORGANISM - Target is a complete organism
Relationship Type: N - Non-molecular target assigned
Confidence: Target assigned is non-molecular
Standard TypeStandard RelationStandard ValueStandard Units
Tmax=1.9hr
HepG2 Cytotoxicity Assay Measured in Cell-Based System Using Plate Reader - 7071-02_Inhibitor_Dose_DryPowder_Activity_Set16
来源:ChEMBL 靶标:Canis lupus familiaris
External ID: CHEMBL935237
Protocol: N/A
Comment: Journal: J. Med. Chem.
Year: 2008
Volume: 51
Issue: 5
First Page: 1385
Last Page: 1392
DOI: 10.1021/jm070579c

Target ChEMBL ID: CHEMBL373
ChEMBL Target Name: Canis familiaris
ChEMBL Target Type: ORGANISM - Target is a complete organism
Relationship Type: N - Non-molecular target assigned
Confidence: Target assigned is non-molecular
Standard TypeStandard RelationStandard ValueStandard Units
F=37%
HepG2 Cytotoxicity Assay Measured in Cell-Based System Using Plate Reader - 7071-02_Inhibitor_Dose_DryPowder_Activity_Set16
来源:BindingDB 靶标:N/A
External ID: BindingDB_2468_1
Protocol: N/A
Comment: Compounds with any of Ki, IC50, Kd, or EC50 activity value <= 10uM are labeled as "Active".
If multiple measurements are available for a given compound, it is labeled as "Active" if any of the measurements meet the criterion. Activity values are checked in the order of Ki, IC50, Kd, and EC50. The first entry that meets the above activity threshold is used to determine "Standard Type", "Standard Relation", and "PubChem Standard Value". Otherwise, the first non-empty entry will be used to set those values.
Standard TypePubChem Standard ValueIC50Target Accession(s)LigandTarget
IC500.00727.2P35353BDBM20967Corticotropin-releasing factor receptor 1
IC500.00565.6P35353BDBM20968Corticotropin-releasing factor receptor 1
IC500.00646.4P35353BDBM20969Corticotropin-releasing factor receptor 1
HepG2 Cytotoxicity Assay Measured in Cell-Based System Using Plate Reader - 7071-02_Inhibitor_Dose_DryPowder_Activity_Set16
来源:ChEMBL 靶标:Canis lupus familiaris
External ID: CHEMBL934321
Protocol: N/A
Comment: Journal: J. Med. Chem.
Year: 2008
Volume: 51
Issue: 5
First Page: 1385
Last Page: 1392
DOI: 10.1021/jm070579c

Target ChEMBL ID: CHEMBL373
ChEMBL Target Name: Canis familiaris
ChEMBL Target Type: ORGANISM - Target is a complete organism
Relationship Type: N - Non-molecular target assigned
Confidence: Target assigned is non-molecular
Standard TypeStandard RelationStandard ValueStandard Units
F=3.6%
HepG2 Cytotoxicity Assay Measured in Cell-Based System Using Plate Reader - 7071-02_Inhibitor_Dose_DryPowder_Activity_Set16
来源:BindingDB 靶标:N/A
External ID: BindingDB_2466_1
Protocol: N/A
Comment: Compounds with any of Ki, IC50, Kd, or EC50 activity value <= 10uM are labeled as "Active".
If multiple measurements are available for a given compound, it is labeled as "Active" if any of the measurements meet the criterion. Activity values are checked in the order of Ki, IC50, Kd, and EC50. The first entry that meets the above activity threshold is used to determine "Standard Type", "Standard Relation", and "PubChem Standard Value". Otherwise, the first non-empty entry will be used to set those values.
Standard TypeStandard RelationPubChem Standard ValueIC50 QualifierIC50Target Accession(s)LigandTarget
IC500.15150P35353BDBM20936Corticotropin-releasing factor receptor 1
IC500.01515P35353BDBM20938Corticotropin-releasing factor receptor 1