BDBM50125052 CHEMBL3623004::US10130617, Example 1::US20240043442, Example AZD9496::US20240131013, Compound AZD-9496::WO-2014/191726, Example 1

SMILES C[C@@H]1Cc2c3ccccc3[nH]c2[C@H](N1CC(C)(C)F)c4c(cc(cc4F)/C=C/C(=O)O)F

InChI Key InChIKey=DFBDRVGWBHBJNR-UHFFFAOYSA-N

Data  25 IC50

PDB links: 1 PDB ID matches this monomer.

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Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 25 hits for monomerid = 50125052   

TargetEstrogen receptor(Human)
Astrazeneca

Curated by ChEMBL
LigandPNGBDBM50125052(CHEMBL3623004 | US10130617, Example 1 | WO-2014/19...)
Affinity DataIC50: 0.316nMAssay Description:Induction of ERalpha degradation in human MCF7 cells assessed as downregulation of ER alpha receptor expression measured after 18 to 22 hrs by immuno...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/17/2021
Entry Details Article
PubMed
TargetEstrogen receptor(Human)
Astrazeneca

Curated by ChEMBL
LigandPNGBDBM50125052(CHEMBL3623004 | US10130617, Example 1 | WO-2014/19...)
Affinity DataIC50: 0.400nMAssay Description:Compound activity was analyzed using celltiter-glo luminescent viability assay (Promega #G7572) in breast cancer cell line MCF-7. Cells grown in log ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/12/2024
Entry Details
Go to US Patent

TargetSteroid hormone receptor ERR1(Human)
Olema Pharmaceuticals

US Patent
LigandPNGBDBM50125052(CHEMBL3623004 | US10130617, Example 1 | WO-2014/19...)
Affinity DataIC50: 0.372nMAssay Description:Compounds were screened for their ability to displace a fluorescent labelled tracer ERα ligand via time resolved fluorescent energy transfer usi...More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/16/2024
Entry Details
Go to US Patent

TargetEstrogen receptor(Human)
Astrazeneca

Curated by ChEMBL
LigandPNGBDBM50125052(CHEMBL3623004 | US10130617, Example 1 | WO-2014/19...)
Affinity DataIC50: 0.600nMAssay Description:Binding affinity to human ERalpha Y537S mutant ligand binding domainMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/17/2024
Entry Details
PubMed
TargetEstrogen receptor(Human)
Astrazeneca

Curated by ChEMBL
LigandPNGBDBM50125052(CHEMBL3623004 | US10130617, Example 1 | WO-2014/19...)
Affinity DataIC50: 0.5nMAssay Description:Binding affinity to human ERalpha D538G mutant ligand binding domainMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/17/2024
Entry Details
PubMed
TargetEstrogen receptor(Human)
Astrazeneca

Curated by ChEMBL
LigandPNGBDBM50125052(CHEMBL3623004 | US10130617, Example 1 | WO-2014/19...)
Affinity DataIC50: 0.200nMAssay Description:Binding affinity to human wild type ERalpha ligand binding domainMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/17/2024
Entry Details
PubMed
TargetEstrogen receptor(Human)
Astrazeneca

Curated by ChEMBL
LigandPNGBDBM50125052(CHEMBL3623004 | US10130617, Example 1 | WO-2014/19...)
Affinity DataIC50: 0.372nMAssay Description:Compounds were screened for their ability to displace a fluorescent labelled tracer ERβ ligand via time resolved fluorescent energy transfer usi...More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/16/2023
Entry Details
Go to US Patent

TargetEstrogen receptor(Human)
Astrazeneca

Curated by ChEMBL
LigandPNGBDBM50125052(CHEMBL3623004 | US10130617, Example 1 | WO-2014/19...)
Affinity DataIC50: 0.372nMAssay Description:Compounds were screened for their ability to displace a fluorescent labelled tracer ERβ ligand via time resolved fluorescent energy transfer usi...More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/16/2023
Entry Details
Go to US Patent

TargetEstrogen receptor(Human)
Astrazeneca

Curated by ChEMBL
LigandPNGBDBM50125052(CHEMBL3623004 | US10130617, Example 1 | WO-2014/19...)
Affinity DataIC50: 1nMAssay Description:Compounds were screened for their ability to displace a fluorescent labelled tracer ERβ ligand via time resolved fluorescent energy transfer usi...More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/16/2023
Entry Details
Go to US Patent

TargetEstrogen receptor(Human)
Astrazeneca

Curated by ChEMBL
LigandPNGBDBM50125052(CHEMBL3623004 | US10130617, Example 1 | WO-2014/19...)
Affinity DataIC50: 0.640nMAssay Description:Compounds were screened for their ability to displace a fluorescent labelled tracer ERβ ligand via time resolved fluorescent energy transfer usi...More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/16/2023
Entry Details
Go to US Patent

TargetEstrogen receptor(Human)
Astrazeneca

Curated by ChEMBL
LigandPNGBDBM50125052(CHEMBL3623004 | US10130617, Example 1 | WO-2014/19...)
Affinity DataIC50: 0.180nMAssay Description:Induction of estrogen receptor degradation in human MCF7 cellsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/25/2022
Entry Details Article
PubMed
TargetEstrogen receptor(Human)
Astrazeneca

Curated by ChEMBL
LigandPNGBDBM50125052(CHEMBL3623004 | US10130617, Example 1 | WO-2014/19...)
Affinity DataIC50: 0.210nMAssay Description:Binding affinity to estrogen receptor (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/25/2022
Entry Details Article
PubMed
TargetEstrogen receptor(Human)
Astrazeneca

Curated by ChEMBL
LigandPNGBDBM50125052(CHEMBL3623004 | US10130617, Example 1 | WO-2014/19...)
Affinity DataIC50: 0.794nMAssay Description:Displacement of fluorescent labelled fluormone ES2 from human recombinant GST tagged ER alpha LBD ( 282 to 595 residues) expressed in baculovirus inf...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/17/2021
Entry Details Article
PubMed
TargetProgesterone receptor(Human)
Astrazeneca

Curated by ChEMBL
LigandPNGBDBM50125052(CHEMBL3623004 | US10130617, Example 1 | WO-2014/19...)
Affinity DataIC50: 0.282nMAssay Description:Antagonist activity at progesterone receptor in human MCF cells assessed as estradiol-induced receptor responseMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/11/2016
Entry Details Article
PubMed
TargetEstrogen receptor(Human)
Astrazeneca

Curated by ChEMBL
LigandPNGBDBM50125052(CHEMBL3623004 | US10130617, Example 1 | WO-2014/19...)
Affinity DataIC50: 640nMAssay Description:The ability of compounds to bind to isolated Estrogen Receptor Alpha Ligand binding domain (ER alpha LBD (GST)) was assessed in competition assays us...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/28/2019
Entry Details
Go to US Patent

TargetEstrogen receptor(Human)
Astrazeneca

Curated by ChEMBL
LigandPNGBDBM50125052(CHEMBL3623004 | US10130617, Example 1 | WO-2014/19...)
Affinity DataIC50: 140nMAssay Description:The ability of compounds to down-regulate Estrogen Receptor (ER) numbers was assessed in a cell based immuno-fluorescence assay using the MCF-7 human...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/28/2019
Entry Details
Go to US Patent

TargetProgesterone receptor(Human)
Astrazeneca

Curated by ChEMBL
LigandPNGBDBM50125052(CHEMBL3623004 | US10130617, Example 1 | WO-2014/19...)
Affinity DataIC50: 11nMAssay Description:Agonist activity at progesterone receptor in human MCF7 cells in presence of 0.25 uM tamoxifenMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/11/2016
Entry Details Article
PubMed
TargetEstrogen receptor(Human)
Astrazeneca

Curated by ChEMBL
LigandPNGBDBM50125052(CHEMBL3623004 | US10130617, Example 1 | WO-2014/19...)
Affinity DataIC50: 0.209nMAssay Description:Antagonist activity at ERalpha receptor in human MCF7 cells in presence of 0.25 uM tamoxifenMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/11/2016
Entry Details Article
PubMed
TargetGlucocorticoid receptor(Human)
Astrazeneca

Curated by ChEMBL
LigandPNGBDBM50125052(CHEMBL3623004 | US10130617, Example 1 | WO-2014/19...)
Affinity DataIC50: 9.20E+3nMAssay Description:Binding affinity to glucocorticoid receptor (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/11/2016
Entry Details Article
PubMed
TargetProgesterone receptor(Human)
Astrazeneca

Curated by ChEMBL
LigandPNGBDBM50125052(CHEMBL3623004 | US10130617, Example 1 | WO-2014/19...)
Affinity DataIC50: 540nMAssay Description:Binding affinity to progesterone receptor (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/11/2016
Entry Details Article
PubMed
TargetAndrogen receptor(Human)
Astrazeneca

Curated by ChEMBL
LigandPNGBDBM50125052(CHEMBL3623004 | US10130617, Example 1 | WO-2014/19...)
Affinity DataIC50: 3.00E+4nMAssay Description:Binding affinity to androgen receptor (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/11/2016
Entry Details Article
PubMed
TargetEstrogen receptor(Human)
Astrazeneca

Curated by ChEMBL
LigandPNGBDBM50125052(CHEMBL3623004 | US10130617, Example 1 | WO-2014/19...)
Affinity DataIC50: 0.800nMAssay Description:Binding affinity to ERalpha receptor (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/11/2016
Entry Details Article
PubMed
TargetEstrogen receptor(Human)
Astrazeneca

Curated by ChEMBL
LigandPNGBDBM50125052(CHEMBL3623004 | US10130617, Example 1 | WO-2014/19...)
Affinity DataIC50: 0.800nMAssay Description:Binding affinity to ERalpha receptor (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/11/2016
Entry Details Article
PubMed
TargetEstrogen receptor(Human)
Astrazeneca

Curated by ChEMBL
LigandPNGBDBM50125052(CHEMBL3623004 | US10130617, Example 1 | WO-2014/19...)
Affinity DataIC50: 0.138nMAssay Description:Antagonist activity at ERalpha receptor in human MCF7 cellsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/11/2016
Entry Details Article
PubMed
TargetProgesterone receptor(Human)
Astrazeneca

Curated by ChEMBL
LigandPNGBDBM50125052(CHEMBL3623004 | US10130617, Example 1 | WO-2014/19...)
Affinity DataIC50: 3.16E+3nMAssay Description:Agonist activity at progesterone receptor in human MCF7 cellsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/11/2016
Entry Details Article
PubMed