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BioAssay: AID 348700

Estrogenic activity in human MCF7 cells assessed as cell proliferation after 6 days by WST8 assay

Novel diphenylamine-type estrogen receptor ligands were designed and synthesized, and their biological activities were evaluated by means of binding assays for estrogen receptor-alpha and -beta and cell proliferation assay using MCF-7 cells. Compounds 4f, 11b, 12c, and 8 showed moderate estrogenic activities. We propose that the diphenylamine skeleton may be a privileged structure for various nuclear receptor ligands, including RAR, RXR, and AR ligands. ..more
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 Tested Compounds
 Tested Compounds
All(19)
 
 
Active(16)
 
 
Inactive(3)
 
 
 Tested Substances
 Tested Substances
All(19)
 
 
Active(16)
 
 
Inactive(3)
 
 
 Related BioAssays
 Related BioAssays
AID: 348700
Data Source: ChEMBL (496729)
BioAssay Type: Confirmatory, Concentration-Response Relationship Observed
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2010-05-26
Modify Date: 2014-05-27

Data Table ( Complete ):           View Active Data    View All Data
BioActive Compounds: 16
Description:
Title: Promising core structure for nuclear receptor ligands: design and synthesis of novel estrogen receptor ligands based on diphenylamine skeleton.

Abstract: Novel diphenylamine-type estrogen receptor ligands were designed and synthesized, and their biological activities were evaluated by means of binding assays for estrogen receptor-alpha and -beta and cell proliferation assay using MCF-7 cells. Compounds 4f, 11b, 12c, and 8 showed moderate estrogenic activities. We propose that the diphenylamine skeleton may be a privileged structure for various nuclear receptor ligands, including RAR, RXR, and AR ligands.
(PMID: 18760603)
Comment
Compounds with activity <= 50uM or explicitly reported as active by ChEMBL are flagged as active in this PubChem assay presentation.
Putative Target:
ChEMBL Target ID: 80224
Target Type: CELL-LINE
Cell Line: MCF7
Tissue: Breast carcinoma cells
Pref Name: MCF7
Organism: Homo sapiens
Tax ID: 9606
Confidence: Target assigned is non-molecular
Relationship Type: Non-molecular target assigned
Categorized Comment - additional comments and annotations
From ChEMBL:
Assay Type: Functional
Assay Data Source: Scientific Literature
BAO: Assay Format: cell-based format
Assay Cell Type: MCF7
Result Definitions
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TIDNameDescriptionHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
1EC50*EC50 PubChem standard valueFloatμM
2Activity activity commentActivity activity commentString
3Activity standard flagActivity standard flagInteger
4Activity qualifierActivity qualifierString
5Activity published valueActivity published valueFloat
6Activity standard valueActivity standard valueFloat
7Activity data validityActivity data validityString
8EC50 activity commentEC50 activity commentString
9EC50 standard flagEC50 standard flagInteger
10EC50 qualifierEC50 qualifierString
11EC50 published valueEC50 published valueFloat10'-12M
12EC50 standard valueEC50 standard valueFloatnM
13EC50 data validityEC50 data validityString
14EC50 activity commentEC50 activity commentString
15EC50 standard flagEC50 standard flagInteger
16EC50 qualifierEC50 qualifierString
17EC50 published valueEC50 published valueFloat10'-5M
18EC50 standard valueEC50 standard valueFloatnM
19EC50 data validityEC50 data validityString
20EC50 activity commentEC50 activity commentString
21EC50 standard flagEC50 standard flagInteger
22EC50 qualifierEC50 qualifierString
23EC50 published valueEC50 published valueFloat10'-6M
24EC50 standard valueEC50 standard valueFloatnM
25EC50 data validityEC50 data validityString
26EC50 activity commentEC50 activity commentString
27EC50 standard flagEC50 standard flagInteger
28EC50 qualifierEC50 qualifierString
29EC50 published valueEC50 published valueFloat10'-7M
30EC50 standard valueEC50 standard valueFloatnM
31EC50 data validityEC50 data validityString
32EC50 activity commentEC50 activity commentString
33EC50 standard flagEC50 standard flagInteger
34EC50 qualifierEC50 qualifierString
35EC50 published valueEC50 published valueFloat10'-8M
36EC50 standard valueEC50 standard valueFloatnM
37EC50 data validityEC50 data validityString
38EC50 activity commentEC50 activity commentString
39EC50 standard flagEC50 standard flagInteger
40EC50 qualifierEC50 qualifierString
41EC50 published valueEC50 published valueFloat10'-9M
42EC50 standard valueEC50 standard valueFloatnM
43EC50 data validityEC50 data validityString

* Activity Concentration.

Data Table (Concise)
Data Table ( Complete ):     View Active Data    View All Data
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