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Assay Detail

CHEMBL1680624

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

Functional
Antagonist activity at human mineralocorticoid receptor expressed in HEK293 cells assessed as inhibition of R5050-induced transcriptional activity by GRE-driven luciferase reporter gene assay
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Mineralocorticoid receptor (CHEMBL1994)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Novel 3-aryl indoles as progesterone receptor antagonists for uterine fibroids.
Richardson TI, Clarke CA, Yu KL, Yee YK, Bleisch TJ, Lopez JE, Jones SA, Hughes NE, Muehl BS, Lugar CW, Moore TL, Shetler PK, Zink RW, Osborne JJ, Montrose-Rafizadeh C, Patel N, Geiser AG, Galvin RJ, Dodge JA.
ACS Med Chem Lett (2011) 2 : 148 -153
PubMed 24900294 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 6.17 7.57

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL235206 1 7.57
CHEMBL1672542 1 7.19
CHEMBL391231 1 6.51
CHEMBL1672546 1 5.62
CHEMBL1672547 1 5.09
CHEMBL1672548 1 5.01
CHEMBL1672549 1 -
CHEMBL1672541 1 -
CHEMBL1672545 1 -
CHEMBL1672544 1 -
CHEMBL1672543 1 -
CHEMBL1672540 3-[(4-METHOXYPHENYL)PHENYLMETHYL]INDOLE 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL235206 IC50 = 27.2 nM 7.57
CHEMBL1672542 IC50 = 64.1 nM 7.19
CHEMBL391231 IC50 = 306.0 nM 6.51
CHEMBL1672546 IC50 = 2420.0 nM 5.62
CHEMBL1672547 IC50 = 8150.0 nM 5.09
CHEMBL1672548 IC50 = 9800.0 nM 5.01
CHEMBL1672549 IC50 > 10000.0 nM -
CHEMBL1672541 IC50 > 10000.0 nM -
CHEMBL1672545 IC50 > 10000.0 nM -
CHEMBL1672544 IC50 > 10000.0 nM -
CHEMBL1672543 IC50 > 10000.0 nM -
CHEMBL1672540 3-[(4-METHOXYPHENYL)PHENYLMETHYL]INDOLE IC50 > 10000.0 nM -