BDBM50249150 8,15-dimethyl-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::CHEMBL474189

SMILES CC1(CC2(C)c3ccccc3C1c1ccccc21)C(=O)Nc1nccs1

InChI Key

Data  6 KI  12 EC50

  Tab Delimited (TSV)   2D SDfile   Computed 3D by Vconf -m prep SDfile
Find this compound or compounds like it in BindingDB:
   Substructure
Similarity at least:  must be >=0.5
Exact match

Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 18 hits for monomerid = 50249150   

TargetGlucocorticoid receptor(Human)
Bristol-Myers Squibb

Curated by ChEMBL
LigandPNGBDBM50249150(8,15-dimethyl-N-(1,3-thiazol-2-yl)tetracyclo[6.6.2...)
Affinity DataKi:  1nMAssay Description:Displacement of GS-red from glucocorticoid receptor by fluorescence polarization assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/20/2012
Entry Details Article
PubMed
TargetGlucocorticoid receptor(Human)
Bristol-Myers Squibb

Curated by ChEMBL
LigandPNGBDBM50249150(8,15-dimethyl-N-(1,3-thiazol-2-yl)tetracyclo[6.6.2...)
Affinity DataKi:  1nMAssay 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
LigandPNGBDBM50249150(8,15-dimethyl-N-(1,3-thiazol-2-yl)tetracyclo[6.6.2...)
Affinity DataKi:  1nMAssay 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
LigandPNGBDBM50249150(8,15-dimethyl-N-(1,3-thiazol-2-yl)tetracyclo[6.6.2...)
Affinity DataEC50:  1.40nMAssay Description:Transrepression activity at glucocorticoid receptor alpha in IL-1beta-stimulated human A549 cells assessed as inhibition of NFkappaB-dependent E-sele...More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/20/2012
Entry Details Article
PubMed
TargetGlucocorticoid receptor(Human)
Bristol-Myers Squibb

Curated by ChEMBL
LigandPNGBDBM50249150(8,15-dimethyl-N-(1,3-thiazol-2-yl)tetracyclo[6.6.2...)
Affinity DataEC50:  5.30nMAssay Description:Transrepression activity at glucocorticoid receptor alpha in phorbol myristate acetate-stimulated human A549 cells assessed as inhibition of AP1 resp...More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/20/2012
Entry Details Article
PubMed
TargetGlucocorticoid receptor(Human)
Bristol-Myers Squibb

Curated by ChEMBL
LigandPNGBDBM50249150(8,15-dimethyl-N-(1,3-thiazol-2-yl)tetracyclo[6.6.2...)
Affinity DataEC50:  5.30nMAssay 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
LigandPNGBDBM50249150(8,15-dimethyl-N-(1,3-thiazol-2-yl)tetracyclo[6.6.2...)
Affinity DataEC50:  8.30nMAssay 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
TargetGlucocorticoid receptor(Human)
Bristol-Myers Squibb

Curated by ChEMBL
LigandPNGBDBM50249150(8,15-dimethyl-N-(1,3-thiazol-2-yl)tetracyclo[6.6.2...)
Affinity DataEC50:  8.30nMAssay 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
TargetGlucocorticoid receptor(Human)
Bristol-Myers Squibb

Curated by ChEMBL
LigandPNGBDBM50249150(8,15-dimethyl-N-(1,3-thiazol-2-yl)tetracyclo[6.6.2...)
Affinity DataEC50:  14.7nMAssay 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
LigandPNGBDBM50249150(8,15-dimethyl-N-(1,3-thiazol-2-yl)tetracyclo[6.6.2...)
Affinity DataEC50:  14.7nMAssay 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
TargetProgesterone receptor(Human)
Bristol-Myers Squibb

Curated by ChEMBL
LigandPNGBDBM50249150(8,15-dimethyl-N-(1,3-thiazol-2-yl)tetracyclo[6.6.2...)
Affinity DataKi:  31nMAssay 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
LigandPNGBDBM50249150(8,15-dimethyl-N-(1,3-thiazol-2-yl)tetracyclo[6.6.2...)
Affinity DataEC50:  117nMAssay Description:Transactivation activity at GR-alpha in human NP1 Hela cells assessed as induction of GAL4-DBD after 20 hrs by luciferase reporter gene assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/20/2012
Entry Details Article
PubMed
TargetGlucocorticoid receptor(Human)
Bristol-Myers Squibb

Curated by ChEMBL
LigandPNGBDBM50249150(8,15-dimethyl-N-(1,3-thiazol-2-yl)tetracyclo[6.6.2...)
Affinity DataEC50:  117nMAssay 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
TargetGlucocorticoid receptor(Human)
Bristol-Myers Squibb

Curated by ChEMBL
LigandPNGBDBM50249150(8,15-dimethyl-N-(1,3-thiazol-2-yl)tetracyclo[6.6.2...)
Affinity DataEC50:  121nMAssay 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
LigandPNGBDBM50249150(8,15-dimethyl-N-(1,3-thiazol-2-yl)tetracyclo[6.6.2...)
Affinity DataKi:  2.90E+3nMAssay 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
LigandPNGBDBM50249150(8,15-dimethyl-N-(1,3-thiazol-2-yl)tetracyclo[6.6.2...)
Affinity DataKi: >5.00E+3nMAssay 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
TargetGlucocorticoid receptor(Human)
Bristol-Myers Squibb

Curated by ChEMBL
LigandPNGBDBM50249150(8,15-dimethyl-N-(1,3-thiazol-2-yl)tetracyclo[6.6.2...)
Affinity DataEC50: >5.00E+3nMAssay 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
TargetGlucocorticoid receptor(Human)
Bristol-Myers Squibb

Curated by ChEMBL
LigandPNGBDBM50249150(8,15-dimethyl-N-(1,3-thiazol-2-yl)tetracyclo[6.6.2...)
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