BDBM300969 BDBM300970::N-(1-(3- fluoropropyl) azetidin-3-yl)-6- ((6S,8R)-6- deuterio-8- methyl-7- (2,2,2- trifluoroethyl)- 6,7,8,9- tetrahydro-3H- pyrazolo[4,3- f]isoquinolin- 6-yl)pyridin-3- amine::US10131663, Example 35::US10590130, Example 32::US10961241, Example 17::US10961241, Example 36
SMILES C[C@@H]1Cc2c(ccc3[nH]ncc23)[C@H](N1CC(F)(F)F)c1ccc(NC2CN(CCCF)C2)cn1
InChI Key
Data 28 IC50
Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB
Found 28 hits for monomerid = 300969
Affinity DataIC50: 1.5nMAssay Description:The assay principle is that ER alpha-LBD (GST) is added to a fluorescent ligand to form a receptor/fluorophore complex. A terbium-labelled anti-GST a...More data for this Ligand-Target Pair
Affinity DataIC50: 0.158nMAssay Description:Induction of ERalpha degradation in human MCF7 cells incubated for 18 to 22 hrs by immuno-fluorescence assayMore data for this Ligand-Target Pair
Affinity DataIC50: 1.80nMAssay Description:The assay principle is that ER alpha-LBD (GST) is added to a fluorescent ligand to form a receptor/fluorophore complex. A terbium-labelled anti-GST a...More data for this Ligand-Target Pair
Affinity DataIC50: 0.120nMAssay 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
TargetPotassium voltage-gated channel subfamily H member 2(Homo sapiens (Human))
Astrazeneca
US Patent
Astrazeneca
US Patent
Affinity DataIC50: 2.40nMAssay Description:hERG (human ether go go-related gene) potassium channels are essential for normal electrical activity in the heart. Arrhythmia can be induced by a bl...More data for this Ligand-Target Pair
TargetPotassium voltage-gated channel subfamily H member 2(Homo sapiens (Human))
Astrazeneca
US Patent
Astrazeneca
US Patent
Affinity DataIC50: 2.10nMAssay Description:hERG (human ether go go-related gene) potassium channels are essential for normal electrical activity in the heart. Arrhythmia can be induced by a bl...More data for this Ligand-Target Pair
TargetPotassium voltage-gated channel subfamily H member 2(Homo sapiens (Human))
Astrazeneca
US Patent
Astrazeneca
US Patent
Affinity DataIC50: 1.5nMAssay Description:hERG (human ether go go-related gene) potassium channels are essential for normal electrical activity in the heart. Arrhythmia can be induced by a bl...More data for this Ligand-Target Pair
TargetPotassium voltage-gated channel subfamily H member 2(Homo sapiens (Human))
Astrazeneca
US Patent
Astrazeneca
US Patent
Affinity DataIC50: 1.80nMAssay Description:hERG (human ether go go-related gene) potassium channels are essential for normal electrical activity in the heart. Arrhythmia can be induced by a bl...More data for this Ligand-Target Pair
Affinity DataIC50: 2.20E+4nMAssay Description:ER: The ability of compounds to bind to isolated Estrogen Receptor Alpha Ligand binding domain (ER alpha-LBD (GST)) was assessed in competition assay...More data for this Ligand-Target Pair
Affinity DataIC50: 1.40E+4nMAssay Description:ER: The ability of compounds to bind to isolated Estrogen Receptor Alpha Ligand binding domain (ER alpha-LBD (GST)) was assessed in competition assay...More data for this Ligand-Target Pair
Affinity DataIC50: 2.40nMAssay Description:The assay was performed as follows with all reagent additions carried out using the Beckman Coulter BioRAPTR FRD microfluidic workstation:1. Acoustic...More data for this Ligand-Target Pair
Affinity DataIC50: 1.5nMAssay Description:The assay was performed as follows with all reagent additions carried out using the Beckman Coulter BioRAPTR FRD microfluidic workstation:1. Acoustic...More data for this Ligand-Target Pair
Affinity DataIC50: 1.80nMAssay Description:The assay was performed as follows with all reagent additions carried out using the Beckman Coulter BioRAPTR FRD microfluidic workstation:1. Acoustic...More data for this Ligand-Target Pair
Affinity DataIC50: >3.00E+4nMAssay Description:Inhibition of CYP2C9 in human liver microsomesMore data for this Ligand-Target Pair
Affinity DataIC50: >3.00E+4nMAssay Description:Inhibition of CYP2C19 in human liver microsomesMore data for this Ligand-Target Pair
Affinity DataIC50: >3.00E+4nMAssay Description:Inhibition of CYP1A2 in human liver microsomesMore data for this Ligand-Target Pair
Affinity DataIC50: 6.30nMAssay Description:Induction of ERalpha degradation in human MCF7 cells assessed as decrease in ERalpha expression in presence of tamoxifen by Western blot analysisMore data for this Ligand-Target Pair
Affinity DataIC50: 0.126nMAssay Description:Induction of ERalpha degradation in human MCF7 cells assessed as decrease in ERalpha expression in presence of cycloheximide by Western blot analysisMore data for this Ligand-Target Pair
Affinity DataIC50: <316nMAssay Description:Agonist activity at ERalpha in human MCF7 cells assessed as increase in progesterone receptor expression level by western blot analysisMore data for this Ligand-Target Pair
Affinity DataIC50: 0.158nMAssay Description:Induction of ERalpha degradation in human MCF7 cells assessed as decrease in ERalpha expression by Western blot analysisMore data for this Ligand-Target Pair
Affinity DataIC50: 330nMAssay Description:Antagonist activity at human histamine H3 receptor expressed in CHO-K1 cells after 10 mins by HTRF assayMore data for this Ligand-Target Pair
TargetPotassium voltage-gated channel subfamily H member 2(Homo sapiens (Human))
Astrazeneca
US Patent
Astrazeneca
US Patent
Affinity DataIC50: 2.20E+4nMAssay Description:Inhibition of human ERG by plate-based planar patch clamp techniqueMore data for this Ligand-Target Pair
Affinity DataIC50: 2.20E+3nMAssay Description:Inhibition of CYP3A4 in human liver microsomesMore data for this Ligand-Target Pair
Affinity DataIC50: 4.30E+3nMAssay Description:Inhibition of CYP2D6 in human liver microsomesMore data for this Ligand-Target Pair
Affinity DataIC50: 0.158nMAssay Description:Induction of ERalpha degradation in human MCF7 cells assessed as decrease in ER-alpha level incubated for 18 to 24 hrs by Alexa fluor 488/Hoechst sta...More data for this Ligand-Target Pair
Affinity DataIC50: 2.5nMAssay Description:Displacement of fluormone ES2 green reagent from human GST-tagged ERalpha LBD (282 to 595 residues) expressed in baculovirus infected insect cells in...More data for this Ligand-Target Pair
Affinity DataIC50: 2.5nMAssay 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
Affinity DataIC50: 0.170nMAssay 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