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Assay Detail

CHEMBL1680621

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

Binding
Displacement of [3H]methyltrienolone from human glucocorticoid receptor expressed in HEK293 cells
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Glucocorticoid receptor (CHEMBL2034)
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
Ki 12 6.71 8.23

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL235206 1 8.23
CHEMBL1672542 1 8.19
CHEMBL1672540 3-[(4-METHOXYPHENYL)PHENYLMETHYL]INDOLE 1 7.30
CHEMBL391231 1 7.26
CHEMBL1672541 1 6.80
CHEMBL1672547 1 6.28
CHEMBL1672549 1 6.11
CHEMBL1672544 1 6.03
CHEMBL1672546 1 6.01
CHEMBL1672545 1 5.82
CHEMBL1672548 1 5.73
CHEMBL1672543 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL235206 Ki = 5.93 nM 8.23
CHEMBL1672542 Ki = 6.39 nM 8.19
CHEMBL1672540 3-[(4-METHOXYPHENYL)PHENYLMETHYL]INDOLE Ki = 50.2 nM 7.30
CHEMBL391231 Ki = 54.4 nM 7.26
CHEMBL1672541 Ki = 157.0 nM 6.80
CHEMBL1672547 Ki = 523.0 nM 6.28
CHEMBL1672549 Ki = 780.0 nM 6.11
CHEMBL1672544 Ki = 927.0 nM 6.03
CHEMBL1672546 Ki = 977.0 nM 6.01
CHEMBL1672545 Ki = 1530.0 nM 5.82
CHEMBL1672548 Ki = 1860.0 nM 5.73
CHEMBL1672543 Ki > 4290.0 nM -