BDBM50249196 (15R)-8-cyano-15-methyl-N-(1,3-thiazol-2-yl)tetracyclo[6.6.2.0^{2,7}.0^{9,14}]hexadeca-2,4,6,9(14),10,12-hexaene-15-carboxamide::CHEMBL473801

SMILES C[C@]1(CC2(C#N)c3ccccc3C1c1ccccc21)C(=O)Nc1nccs1

InChI Key

Data  4 KI  3 EC50

  Tab Delimited (TSV)   2D SDfile   Computed 3D by Vconf -m prep SDfile
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Exact match

Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 7 hits for monomerid = 50249196   

TargetGlucocorticoid receptor(Human)
Bristol-Myers Squibb

Curated by ChEMBL
LigandPNGBDBM50249196((15R)-8-cyano-15-methyl-N-(1,3-thiazol-2-yl)tetrac...)
Affinity DataKi:  0.900nMAssay Description:Displacement of FITC-dexamethasone from human recombinant glucocorticoid receptor alpha by fluorescence polarization assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/23/2012
Entry Details Article
PubMed
TargetGlucocorticoid receptor(Human)
Bristol-Myers Squibb

Curated by ChEMBL
LigandPNGBDBM50249196((15R)-8-cyano-15-methyl-N-(1,3-thiazol-2-yl)tetrac...)
Affinity DataEC50:  19.4nMAssay Description:Transrepression activity at GR in IL-1-beta-stimulated human A549 cells assessed as inhibition of NF-kappaB-dependent E-selectin transcription by luc...More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/23/2012
Entry Details Article
PubMed
TargetProgesterone receptor(Human)
Bristol-Myers Squibb

Curated by ChEMBL
LigandPNGBDBM50249196((15R)-8-cyano-15-methyl-N-(1,3-thiazol-2-yl)tetrac...)
Affinity DataKi:  34nMAssay Description:Displacement of radioligand from progesterone receptor by fluorescence polarization assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/23/2012
Entry Details Article
PubMed
TargetGlucocorticoid receptor(Human)
Bristol-Myers Squibb

Curated by ChEMBL
LigandPNGBDBM50249196((15R)-8-cyano-15-methyl-N-(1,3-thiazol-2-yl)tetrac...)
Affinity DataEC50:  243nMAssay Description:Transrepression activity at GR in PMA-stimulated human A549 cells assessed as inhibition of AP1 response element-induced luciferase reporter gene act...More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/23/2012
Entry Details Article
PubMed
TargetGlucocorticoid receptor(Human)
Bristol-Myers Squibb

Curated by ChEMBL
LigandPNGBDBM50249196((15R)-8-cyano-15-methyl-N-(1,3-thiazol-2-yl)tetrac...)
Affinity DataEC50: >1.00E+4nMAssay Description:Agonist activity at GR ligand binding domain expressed in human NP1 cells assessed as glucocorticoid response element transactivation by GAL4 lucifer...More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/23/2012
Entry Details Article
PubMed
TargetAndrogen receptor(Human)
Bristol-Myers Squibb

Curated by ChEMBL
LigandPNGBDBM50249196((15R)-8-cyano-15-methyl-N-(1,3-thiazol-2-yl)tetrac...)
Affinity DataKi: >1.00E+4nMAssay Description:Displacement of radioligand from androgen receptor by fluorescence polarization assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/23/2012
Entry Details Article
PubMed
TargetEstrogen receptor(Human)
Bristol-Myers Squibb

Curated by ChEMBL
LigandPNGBDBM50249196((15R)-8-cyano-15-methyl-N-(1,3-thiazol-2-yl)tetrac...)
Affinity DataKi:  2.63E+4nMAssay Description:Displacement of radioligand from estrogen receptor alpha by fluorescence polarization assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/23/2012
Entry Details Article
PubMed