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Assay Detail

CHEMBL839524

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

Binding
Inhibition of human Estrogen receptor beta
23
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Estrogen receptor beta (CHEMBL242)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Liver-selective glucocorticoid antagonists: a novel treatment for type 2 diabetes.
von Geldern TW, Tu N, Kym PR, Link JT, Jae HS, Lai C, Apelqvist T, Rhonnstad P, Hagberg L, Koehler K, Grynfarb M, Goos-Nilsson A, Sandberg J, Osterlund M, Barkhem T, Höglund M, Wang J, Fung S, Wilcox D, Nguyen P, Jakob C, Hutchins C, Färnegårdh M, Kauppi B, Ohman L, Jacobson PB.
J Med Chem (2004) 47 : 4213 -4230
PubMed 15293993 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 23 7.14 7.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL415621 1 7.89
CHEMBL408376 1 7.89
CHEMBL407672 1 7.52
CHEMBL406027 1 7.41
CHEMBL440251 1 7.32
CHEMBL2096708 1 7.29
CHEMBL427568 2 7.05
CHEMBL411185 1 6.80
CHEMBL384975 1 6.72
CHEMBL436859 1 6.62
CHEMBL364368 1 6.24
CHEMBL414318 1 -
CHEMBL1276308 MIFEPRISTONE 4.0 1 -
CHEMBL266935 1 -
CHEMBL2096804 1 -
CHEMBL406064 1 -
CHEMBL266673 1 -
CHEMBL265125 1 -
CHEMBL409123 1 -
CHEMBL263942 1 -
CHEMBL266656 1 -
CHEMBL414041 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL415621 Ki = 13.0 nM 7.89
CHEMBL408376 Ki = 13.0 nM 7.89
CHEMBL407672 Ki = 30.0 nM 7.52
CHEMBL406027 Ki = 39.0 nM 7.41
CHEMBL440251 Ki = 48.0 nM 7.32
CHEMBL2096708 Ki = 51.0 nM 7.29
CHEMBL427568 Ki = 89.0 nM 7.05
CHEMBL427568 Ki = 110.0 nM 6.96
CHEMBL411185 Ki = 160.0 nM 6.80
CHEMBL384975 Ki = 190.0 nM 6.72
CHEMBL436859 Ki = 240.0 nM 6.62
CHEMBL364368 Ki = 570.0 nM 6.24
CHEMBL265125 Ki - nM -
CHEMBL414041 Ki - nM -
CHEMBL409123 Ki - nM -
CHEMBL263942 Ki > 750.0 nM -
CHEMBL266656 Ki - nM -
CHEMBL266673 Ki - nM -
CHEMBL406064 Ki - nM -
CHEMBL2096804 Ki - nM -
CHEMBL266935 Ki > 750.0 nM -
CHEMBL1276308 MIFEPRISTONE Ki > 750.0 nM -
CHEMBL414318 Ki - nM -