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Assay Detail

CHEMBL4008040

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

Binding
Displacement of [3H]-Aldosterone from MR overexpressed in human 293 cells measured after 2 hrs by Microbeta scintillation counting method
14
Total Activities
14
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

Mineralocorticoid receptor (CHEMBL1994)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Modulating Mineralocorticoid Receptor with Non-steroidal Antagonists. New Opportunities for the Development of Potent and Selective Ligands without Off-Target Side Effects.
Martín-Martínez M, Pérez-Gordillo FL, Álvarez de la Rosa D, Rodríguez Y, Gerona-Navarro G, González-Muñiz R, Zhou MM.
J Med Chem (2017) 60 : 2629 -2650
PubMed 28051871 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 14 9.54 10.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4095917 1 10.10
CHEMBL4086416 1 9.64
CHEMBL4088896 LY2623091 2.0 1 9.48
CHEMBL4099276 1 9.40
CHEMBL4063735 1 9.10
CHEMBL4091539 1 -
CHEMBL4101755 1 -
CHEMBL4083760 1 -
CHEMBL4068598 1 -
CHEMBL4104314 1 -
CHEMBL4094179 1 -
CHEMBL4066645 1 -
CHEMBL4067668 1 -
CHEMBL4078561 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4095917 Ki = 0.08 nM 10.10
CHEMBL4086416 Ki = 0.23 nM 9.64
CHEMBL4088896 LY2623091 Ki = 0.33 nM 9.48
CHEMBL4099276 Ki = 0.4 nM 9.40
CHEMBL4063735 Ki = 0.79 nM 9.10
CHEMBL4091539 Ki <= 10.0 nM -
CHEMBL4101755 Ki <= 10.0 nM -
CHEMBL4083760 Ki <= 10.0 nM -
CHEMBL4068598 Ki <= 10.0 nM -
CHEMBL4104314 Ki <= 10.0 nM -
CHEMBL4094179 Ki <= 10.0 nM -
CHEMBL4066645 Ki <= 10.0 nM -
CHEMBL4067668 Ki <= 10.0 nM -
CHEMBL4078561 Ki <= 10.0 nM -