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Assay Detail

CHEMBL899207

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

Binding
Displacement of TAMRA labeled mifepristone at human mineralocorticoid receptor in insect cell
36
Total Activities
36
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Mineralocorticoid receptor (CHEMBL1994)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Identification of dissociated non-steroidal glucocorticoid receptor agonists.
Kuzmich D, Kirrane T, Proudfoot J, Bekkali Y, Zindell R, Beck L, Nelson R, Shih CK, Kukulka AJ, Paw Z, Reilly P, Deleon R, Cardozo M, Nabozny G, Thomson D.
Bioorg Med Chem Lett (2007) 17 : 5025 -5031
PubMed 17692519 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 36 6.27 7.48

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL384467 DEXAMETHASONE 4.0 1 7.48
CHEMBL263091 1 6.89
CHEMBL393392 1 6.66
CHEMBL392501 1 6.60
CHEMBL236755 1 6.52
CHEMBL235063 1 6.50
CHEMBL392289 1 6.46
CHEMBL401219 1 6.40
CHEMBL392500 1 6.37
CHEMBL236754 1 6.35
CHEMBL400609 1 6.30
CHEMBL429987 1 6.29
CHEMBL237377 1 6.27
CHEMBL391917 1 6.19
CHEMBL237595 1 6.15
CHEMBL235689 1 6.14
CHEMBL235480 1 6.12
CHEMBL392568 1 6.06
CHEMBL237807 1 6.05
CHEMBL392499 1 6.03
CHEMBL235280 1 5.98
CHEMBL235688 1 5.96
CHEMBL237385 1 5.87
CHEMBL237843 1 5.85
CHEMBL236403 1 5.80
CHEMBL429627 1 5.75
CHEMBL400628 1 -
CHEMBL396669 1 -
CHEMBL235060 1 -
CHEMBL236406 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL384467 DEXAMETHASONE IC50 = 33.0 nM 7.48
CHEMBL263091 IC50 = 130.0 nM 6.89
CHEMBL393392 IC50 = 220.0 nM 6.66
CHEMBL392501 IC50 = 250.0 nM 6.60
CHEMBL236755 IC50 = 300.0 nM 6.52
CHEMBL235063 IC50 = 320.0 nM 6.50
CHEMBL392289 IC50 = 345.0 nM 6.46
CHEMBL401219 IC50 = 400.0 nM 6.40
CHEMBL392500 IC50 = 430.0 nM 6.37
CHEMBL236754 IC50 = 450.0 nM 6.35
CHEMBL400609 IC50 = 500.0 nM 6.30
CHEMBL429987 IC50 = 510.0 nM 6.29
CHEMBL237377 IC50 = 535.0 nM 6.27
CHEMBL391917 IC50 = 650.0 nM 6.19
CHEMBL237595 IC50 = 715.0 nM 6.15
CHEMBL235689 IC50 = 730.0 nM 6.14
CHEMBL235480 IC50 = 760.0 nM 6.12
CHEMBL392568 IC50 = 875.0 nM 6.06
CHEMBL237807 IC50 = 900.0 nM 6.05
CHEMBL392499 IC50 = 940.0 nM 6.03
CHEMBL235280 IC50 = 1050.0 nM 5.98
CHEMBL235688 IC50 = 1100.0 nM 5.96
CHEMBL237385 IC50 = 1350.0 nM 5.87
CHEMBL237843 IC50 = 1400.0 nM 5.85
CHEMBL236403 IC50 = 1600.0 nM 5.80
CHEMBL429627 IC50 = 1800.0 nM 5.75
CHEMBL235536 IC50 > 1420.0 nM -
CHEMBL238044 IC50 > 2000.0 nM -
CHEMBL392309 IC50 > 512.0 nM -
CHEMBL391076 IC50 > 2000.0 nM -
CHEMBL236747 IC50 > 1130.0 nM -
CHEMBL236748 IC50 > 1050.0 nM -
CHEMBL236406 IC50 > 740.0 nM -
CHEMBL235060 IC50 > 2000.0 nM -
CHEMBL396669 IC50 > 1300.0 nM -
CHEMBL400628 IC50 > 1300.0 nM -