BDBM50548385 Glpg-1205::Glpg1205

SMILES O=c1nc(OC[C@@H]2COCCO2)cc2-c3ccc(cc3CCn12)C#CC1CC1

InChI Key InChIKey=IRBAWVGZNJIROV-SFHVURJKSA-N

Data  1 KI  11 IC50  6 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 18 hits for monomerid = 50548385   

TargetG-protein coupled receptor 84(Homo sapiens (Human))
Galapagos

Curated by ChEMBL
LigandPNGBDBM50548385(Glpg-1205 | Glpg1205)
Affinity DataKi:  30nMAssay Description:Displacement of [3H]-9-(2-phenylethyl)-2-(2-pyrazin-2-yloxyethoxy)-6,7-dihydropyrimido[6,1-a]isoquinolin-4-one from recombinant FLAG-tagged GPR84 (un...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetG-protein coupled receptor 84(Homo sapiens (Human))
Galapagos

Curated by ChEMBL
LigandPNGBDBM50548385(Glpg-1205 | Glpg1205)
Affinity DataEC50:  2.92E+3nMAssay Description:Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as right shift in 6-OAU-induced calcium response curve b...More data for this Ligand-Target Pair
In DepthDetails PubMed
TargetCytochrome P450 3A4(Homo sapiens (Human))
Galapagos

Curated by ChEMBL
LigandPNGBDBM50548385(Glpg-1205 | Glpg1205)
Affinity DataIC50: >5.00E+4nMAssay Description:Inhibition of human CYP3A4 in human liver microsomes using testosterone as substrate and in presence of co-factor preincubated for 20 mins followed b...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCytochrome P450 3A4(Homo sapiens (Human))
Galapagos

Curated by ChEMBL
LigandPNGBDBM50548385(Glpg-1205 | Glpg1205)
Affinity DataIC50: >5.00E+4nMAssay Description:Inhibition of CYP3A4 in human liver microsomes using midazolam as substrate and in presence of co-factor preincubated for 20 mins followed by substra...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCytochrome P450 2D6(Homo sapiens (Human))
Galapagos

Curated by ChEMBL
LigandPNGBDBM50548385(Glpg-1205 | Glpg1205)
Affinity DataIC50:  3.46E+4nMAssay Description:Inhibition of CYP2D6 in human liver microsomes using probe substrate and in presence of co-factor preincubated for 20 mins followed by substrate addi...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCytochrome P450 2C9(Homo sapiens (Human))
Galapagos

Curated by ChEMBL
LigandPNGBDBM50548385(Glpg-1205 | Glpg1205)
Affinity DataIC50: >1.00E+5nMAssay Description:Inhibition of CYP2C9 in human liver microsomes using probe substrate and in presence of co-factor preincubated for 20 mins followed by substrate addi...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCytochrome P450 2C19(Homo sapiens (Human))
Galapagos

Curated by ChEMBL
LigandPNGBDBM50548385(Glpg-1205 | Glpg1205)
Affinity DataIC50: >1.00E+5nMAssay Description:Inhibition of CYP2C19 in human liver microsomes using probe substrate and in presence of co-factor preincubated for 20 mins followed by substrate add...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCytochrome P450 1A2(Homo sapiens (Human))
Galapagos

Curated by ChEMBL
LigandPNGBDBM50548385(Glpg-1205 | Glpg1205)
Affinity DataIC50: >1.00E+5nMAssay Description:Inhibition of CYP1A2 in human liver microsomes using probe substrate and in presence of co-factor preincubated for 20 mins followed by substrate addi...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetG-protein coupled receptor 84(Homo sapiens (Human))
Galapagos

Curated by ChEMBL
LigandPNGBDBM50548385(Glpg-1205 | Glpg1205)
Affinity DataIC50:  54nMAssay Description:Antagonist activity at recombinant human GPR84 stably overexpressed in HEK293T cell membranes co-expressing G-alpha assessed as inhibition of DIM-sti...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetG-protein coupled receptor 84(Homo sapiens (Human))
Galapagos

Curated by ChEMBL
LigandPNGBDBM50548385(Glpg-1205 | Glpg1205)
Affinity DataIC50:  112nMAssay Description:Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in 6-OAU induced intracellular calcium resp...More data for this Ligand-Target Pair
In DepthDetails PubMed
TargetG-protein coupled receptor 84(Homo sapiens (Human))
Galapagos

Curated by ChEMBL
LigandPNGBDBM50548385(Glpg-1205 | Glpg1205)
Affinity DataIC50:  58nMAssay Description:Antagonist activity at human GPR84 expressed in HEK293 cells assessed as reversal of 6-OAU induced inhibition of forskolin induced intracellular cAMP...More data for this Ligand-Target Pair
In DepthDetails PubMed
TargetG-protein coupled receptor 84(Homo sapiens (Human))
Galapagos

Curated by ChEMBL
LigandPNGBDBM50548385(Glpg-1205 | Glpg1205)
Affinity DataEC50:  2.21E+4nMAssay Description:Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as right shift in 3-OH-C12-induced calcium response curv...More data for this Ligand-Target Pair
In DepthDetails PubMed
TargetG-protein coupled receptor 84(Homo sapiens (Human))
Galapagos

Curated by ChEMBL
LigandPNGBDBM50548385(Glpg-1205 | Glpg1205)
Affinity DataEC50:  4.86E+4nMAssay Description:Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as right shift in 3-OH-C12-induced calcium response curv...More data for this Ligand-Target Pair
In DepthDetails PubMed
TargetG-protein coupled receptor 84(Homo sapiens (Human))
Galapagos

Curated by ChEMBL
LigandPNGBDBM50548385(Glpg-1205 | Glpg1205)
Affinity DataEC50:  9.24E+4nMAssay Description:Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as right shift in 3-OH-C12-induced calcium response curv...More data for this Ligand-Target Pair
In DepthDetails PubMed
TargetG-protein coupled receptor 84(Homo sapiens (Human))
Galapagos

Curated by ChEMBL
LigandPNGBDBM50548385(Glpg-1205 | Glpg1205)
Affinity DataEC50:  611nMAssay Description:Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as right shift in 6-OAU-induced calcium response curve b...More data for this Ligand-Target Pair
In DepthDetails PubMed
TargetG-protein coupled receptor 84(Homo sapiens (Human))
Galapagos

Curated by ChEMBL
LigandPNGBDBM50548385(Glpg-1205 | Glpg1205)
Affinity DataEC50:  655nMAssay Description:Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as right shift in 6-OAU-induced calcium response curve b...More data for this Ligand-Target Pair
In DepthDetails PubMed
TargetCytochrome P450 3A4(Homo sapiens (Human))
Galapagos

Curated by ChEMBL
LigandPNGBDBM50548385(Glpg-1205 | Glpg1205)
Affinity DataIC50: >5.00E+4nMAssay Description:Time-dependent inhibition of CYP3A4 in human liver microsomes using testosterone as substrate and in presence of co-factor by LC-MS/MS analysisMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCytochrome P450 3A4(Homo sapiens (Human))
Galapagos

Curated by ChEMBL
LigandPNGBDBM50548385(Glpg-1205 | Glpg1205)
Affinity DataIC50: >5.00E+4nMAssay Description:Time-dependent inhibition of CYP3A4 in human liver microsomes using midazolam as substrate and in presence of co-factor by LC-MS/MS analysisMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed