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Assay Detail

CHEMBL3096919

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Displacement of TAMRA-labeled dexamethasone from glucocorticoid receptor (unknown origin) by fluorescence polarization competitive binding assay
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Glucocorticoid receptor (CHEMBL2034)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Function-regulating pharmacophores in a sulfonamide class of glucocorticoid receptor agonists.
Kuzmich D, Bentzien J, Betageri R, DiSalvo D, Fadra-Khan T, Harcken C, Kukulka A, Nabozny G, Nelson R, Pack E, Souza D, Thomson D.
Bioorg Med Chem Lett (2013) 23 : 6640 -6644
PubMed 24215891 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 27 7.68 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3093463 1 9.00
CHEMBL3093461 1 8.70
CHEMBL3093462 1 8.70
CHEMBL384467 DEXAMETHASONE 4.0 1 8.46
CHEMBL3093440 1 8.30
CHEMBL3093453 1 8.30
CHEMBL3093441 1 8.00
CHEMBL3093446 1 8.00
CHEMBL3093452 1 8.00
CHEMBL3093443 1 7.82
CHEMBL3093444 1 7.82
CHEMBL3093456 1 7.82
CHEMBL3093445 1 7.75
CHEMBL3093448 1 7.70
CHEMBL3093460 1 7.70
CHEMBL3093454 1 7.60
CHEMBL3093442 1 7.46
CHEMBL3093447 1 7.43
CHEMBL395795 1 7.40
CHEMBL3093457 1 7.22
CHEMBL396029 1 7.19
CHEMBL3093458 1 7.02
CHEMBL3093459 1 6.68
CHEMBL3093451 1 6.55
CHEMBL3093450 1 6.50
CHEMBL3093455 1 6.47
CHEMBL3093449 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3093463 IC50 = 1.0 nM 9.00
CHEMBL3093461 IC50 = 2.0 nM 8.70
CHEMBL3093462 IC50 = 2.0 nM 8.70
CHEMBL384467 DEXAMETHASONE IC50 = 3.5 nM 8.46
CHEMBL3093440 IC50 = 5.0 nM 8.30
CHEMBL3093453 IC50 = 5.0 nM 8.30
CHEMBL3093441 IC50 = 10.0 nM 8.00
CHEMBL3093446 IC50 = 10.0 nM 8.00
CHEMBL3093452 IC50 = 10.0 nM 8.00
CHEMBL3093443 IC50 = 15.0 nM 7.82
CHEMBL3093444 IC50 = 15.0 nM 7.82
CHEMBL3093456 IC50 = 15.0 nM 7.82
CHEMBL3093445 IC50 = 18.0 nM 7.75
CHEMBL3093448 IC50 = 20.0 nM 7.70
CHEMBL3093460 IC50 = 20.0 nM 7.70
CHEMBL3093454 IC50 = 25.0 nM 7.60
CHEMBL3093442 IC50 = 35.0 nM 7.46
CHEMBL3093447 IC50 = 37.0 nM 7.43
CHEMBL395795 IC50 = 40.0 nM 7.40
CHEMBL3093457 IC50 = 60.0 nM 7.22
CHEMBL396029 IC50 = 64.0 nM 7.19
CHEMBL3093458 IC50 = 95.0 nM 7.02
CHEMBL3093459 IC50 = 210.0 nM 6.68
CHEMBL3093451 IC50 = 280.0 nM 6.55
CHEMBL3093450 IC50 = 320.0 nM 6.50
CHEMBL3093455 IC50 = 340.0 nM 6.47
CHEMBL3093449 IC50 > 10000.0 nM -