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Assay Detail

CHEMBL4028141

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

Binding
Displacement of [3H]-aldosterone from human GST-tagged MR ligand binding domain after 4 hrs by liquid scintillation counting
16
Total Activities
15
Compounds Tested
2
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

Identification of Morpholino-2H-pyrido[3,2-b][1,4]oxazin-3(4H)-ones as Nonsteroidal Mineralocorticoid Antagonists.
Piotrowski DW, Futatsugi K, Casimiro-Garcia A, Wei L, Sammons MF, Herr M, Jiao W, Lavergne SY, Coffey SB, Wright SW, Song K, Loria PM, Banker ME, Petersen DN, Bauman J.
J Med Chem (2018) 61 : 1086 -1097
PubMed 29300474 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 15 6.96 7.89
Ki 1 8.20 8.20

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2181928 2 8.20
CHEMBL4086109 1 7.89
CHEMBL4097160 1 7.89
CHEMBL4064593 1 7.72
CHEMBL4078214 1 7.41
CHEMBL4100538 1 7.25
CHEMBL4082524 1 7.07
CHEMBL4098088 1 6.96
CHEMBL4079143 1 6.95
CHEMBL4059632 1 6.56
CHEMBL4062345 1 6.40
CHEMBL4062371 1 6.14
CHEMBL4079083 1 5.93
CHEMBL4071008 1 5.65
CHEMBL4081584 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2181928 Ki = 6.3 nM 8.20
CHEMBL4086109 IC50 = 13.0 nM 7.89
CHEMBL4097160 IC50 = 13.0 nM 7.89
CHEMBL4064593 IC50 = 19.0 nM 7.72
CHEMBL2181928 IC50 = 25.0 nM 7.60
CHEMBL4078214 IC50 = 39.0 nM 7.41
CHEMBL4100538 IC50 = 56.0 nM 7.25
CHEMBL4082524 IC50 = 86.0 nM 7.07
CHEMBL4098088 IC50 = 109.0 nM 6.96
CHEMBL4079143 IC50 = 113.0 nM 6.95
CHEMBL4059632 IC50 = 276.0 nM 6.56
CHEMBL4062345 IC50 = 401.0 nM 6.40
CHEMBL4062371 IC50 = 727.0 nM 6.14
CHEMBL4079083 IC50 = 1181.0 nM 5.93
CHEMBL4071008 IC50 = 2225.0 nM 5.65
CHEMBL4081584 IC50 > 10000.0 nM -