BDBM50125052 CHEMBL3623004::US10130617, Example 1::WO-2014/191726, Example 1

SMILES C[C@@H]1Cc2c([nH]c3ccccc23)[C@H](N1CC(C)(C)F)c1c(F)cc(\C=C\C(O)=O)cc1F

InChI Key InChIKey=DFBDRVGWBHBJNR-BBNFHIFMSA-N

Data  20 IC50

PDB links: 1 PDB ID matches this monomer.

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Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 20 hits for monomerid = 50125052   

TargetProgesterone receptor(Homo sapiens (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 DepthDetails ArticlePubMed
TargetEstrogen receptor(Homo sapiens (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 ERβ ligand via time resolved fluorescent energy transfer usi...More data for this Ligand-Target Pair
TargetEstrogen receptor(Homo sapiens (Human))
Olema Pharmaceuticals

US Patent
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
TargetEstrogen receptor(Homo sapiens (Human))
Olema Pharmaceuticals

US Patent
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
TargetEstrogen receptor(Homo sapiens (Human))
Olema Pharmaceuticals

US Patent
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
TargetAndrogen receptor(Homo sapiens (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 DepthDetails ArticlePubMed
TargetProgesterone receptor(Homo sapiens (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 DepthDetails ArticlePubMed
TargetGlucocorticoid receptor(Homo sapiens (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 DepthDetails ArticlePubMed
TargetEstrogen receptor(Homo sapiens (Human))
Olema Pharmaceuticals

US Patent
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
TargetProgesterone receptor(Homo sapiens (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 DepthDetails ArticlePubMed
TargetEstrogen receptor(Homo sapiens (Human))
Olema Pharmaceuticals

US Patent
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
TargetEstrogen receptor(Homo sapiens (Human))
Olema Pharmaceuticals

US Patent
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
TargetEstrogen receptor(Homo sapiens (Human))
Olema Pharmaceuticals

US Patent
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
TargetEstrogen receptor(Homo sapiens (Human))
Olema Pharmaceuticals

US Patent
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
TargetEstrogen receptor(Homo sapiens (Human))
Olema Pharmaceuticals

US Patent
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
TargetEstrogen receptor(Homo sapiens (Human))
Olema Pharmaceuticals

US Patent
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
TargetEstrogen receptor(Homo sapiens (Human))
Olema Pharmaceuticals

US Patent
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
TargetEstrogen receptor(Homo sapiens (Human))
Olema Pharmaceuticals

US Patent
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
TargetEstrogen receptor(Homo sapiens (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 ERβ ligand via time resolved fluorescent energy transfer usi...More data for this Ligand-Target Pair
TargetProgesterone receptor(Homo sapiens (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 DepthDetails ArticlePubMed