BDBM21358 2-[1-({6-chloroimidazo[2,1-b][1,3]thiazole-5-}sulfonyl)-1H-indol-3-yl]ethan-1-amine::N1-(6-chloroimidazo[2,1-b][1,3]thiazole-5-sulfonyl)tryptamine::SAX-187::WAY-181187

SMILES NCCc1cn(c2ccccc12)S(=O)(=O)c1c(Cl)nc2sccn12

InChI Key InChIKey=RYBOXBBYCVOYNO-UHFFFAOYSA-N

Data  10 KI  6 IC50  3 EC50

  Tab Delimited (TSV)   2D SDfile   Computed 3D by Vconf -m prep SDfile
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Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 17 hits for monomerid = 21358   

TargetCytochrome P450 1A2(Human)
Wyeth Research

LigandPNGBDBM21358(2-[1-({6-chloroimidazo[2,1-b][1,3]thiazole-5-}sulf...)
Affinity DataIC50: 1.49E+5nMpH: 7.4 T: 2°CAssay Description:The effect of compound on cytochrome P450 (CYP) enzyme catalytic activity was determined in human liver microsomes, using a cocktail of probe substra...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/7/2008
Entry Details Article
PubMed
TargetCytochrome P450 2A6(Human)
Wyeth Research

LigandPNGBDBM21358(2-[1-({6-chloroimidazo[2,1-b][1,3]thiazole-5-}sulf...)
Affinity DataIC50: 4.10E+4nMpH: 7.4 T: 2°CAssay Description:The effect of compound on cytochrome P450 (CYP) enzyme catalytic activity was determined in human liver microsomes, using a cocktail of probe substra...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/7/2008
Entry Details Article
PubMed
TargetCytochrome P450 2C19(Human)
Wyeth Research

LigandPNGBDBM21358(2-[1-({6-chloroimidazo[2,1-b][1,3]thiazole-5-}sulf...)
Affinity DataIC50: 1.12E+5nMpH: 7.4 T: 2°CAssay Description:The effect of compound on cytochrome P450 (CYP) enzyme catalytic activity was determined in human liver microsomes, using a cocktail of probe substra...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/7/2008
Entry Details Article
PubMed
TargetCytochrome P450 2C9(Human)
Wyeth Research

LigandPNGBDBM21358(2-[1-({6-chloroimidazo[2,1-b][1,3]thiazole-5-}sulf...)
Affinity DataIC50: 5.00E+5nMpH: 7.4 T: 2°CAssay Description:The effect of compound on cytochrome P450 (CYP) enzyme catalytic activity was determined in human liver microsomes, using a cocktail of probe substra...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/7/2008
Entry Details Article
PubMed
TargetCytochrome P450 2D6(Human)
Wyeth Research

LigandPNGBDBM21358(2-[1-({6-chloroimidazo[2,1-b][1,3]thiazole-5-}sulf...)
Affinity DataIC50: 1.96E+5nMpH: 7.4 T: 2°CAssay Description:The effect of compound on cytochrome P450 (CYP) enzyme catalytic activity was determined in human liver microsomes, using a cocktail of probe substra...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/7/2008
Entry Details Article
PubMed
TargetCytochrome P450 3A4(Human)
Wyeth Research

LigandPNGBDBM21358(2-[1-({6-chloroimidazo[2,1-b][1,3]thiazole-5-}sulf...)
Affinity DataIC50: 3.30E+4nMpH: 7.4 T: 2°CAssay Description:The effect of compound on cytochrome P450 (CYP) enzyme catalytic activity was determined in human liver microsomes, using a cocktail of probe substra...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/7/2008
Entry Details Article
PubMed
Target5-hydroxytryptamine receptor 6(Human)
Universitat De Barcelona

Curated by ChEMBL
LigandPNGBDBM21358(2-[1-({6-chloroimidazo[2,1-b][1,3]thiazole-5-}sulf...)
Affinity DataEC50:  6.5nMAssay Description:Agonist activity at human 5HT6 receptor expressed in HeLa cells assessed as induction of cAMP production after 10 mins by radioimmunoassayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/30/2010
Entry Details Article
PubMed
Target5-hydroxytryptamine receptor 6(Human)
Universitat De Barcelona

Curated by ChEMBL
LigandPNGBDBM21358(2-[1-({6-chloroimidazo[2,1-b][1,3]thiazole-5-}sulf...)
Affinity DataKi:  2nM ΔG°:  -11.7kcal/mole EC50:  6.5nMpH: 7.4 T: 2°CAssay Description:IC50 values for each test compound were determined from nonlinear regression analysis of data collected from ligand binding experiments. The inhibiti...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/7/2008
Entry Details Article
PubMed
Target5-hydroxytryptamine receptor 6(Human)
Universitat De Barcelona

Curated by ChEMBL
LigandPNGBDBM21358(2-[1-({6-chloroimidazo[2,1-b][1,3]thiazole-5-}sulf...)
Affinity DataKi:  2nMAssay Description:Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation countingMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/20/2012
Entry Details Article
PubMed
Target5-hydroxytryptamine receptor 6(Human)
Universitat De Barcelona

Curated by ChEMBL
LigandPNGBDBM21358(2-[1-({6-chloroimidazo[2,1-b][1,3]thiazole-5-}sulf...)
Affinity DataKi:  2nM ΔG°:  -12.3kcal/mole EC50:  6.5nMpH: 7.4 T: 2°CAssay Description:Radioligand binding assays were performed using membranes from HEK-293 transfected with human 5-HT6 receptor. In these membranes the receptor concent...More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
Target5-hydroxytryptamine receptor 6(Human)
Universitat De Barcelona

Curated by ChEMBL
LigandPNGBDBM21358(2-[1-({6-chloroimidazo[2,1-b][1,3]thiazole-5-}sulf...)
Affinity DataKi:  2nMAssay Description:Displacement of [3H]lysergic acid diethylamide from human 5-HT6 receptor expressed in HeLa cells after 120 mins by scintillation counterMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/4/2016
Entry Details Article
PubMed
Target5-hydroxytryptamine receptor 6(Human)
Universitat De Barcelona

Curated by ChEMBL
LigandPNGBDBM21358(2-[1-({6-chloroimidazo[2,1-b][1,3]thiazole-5-}sulf...)
Affinity DataKi:  2nMAssay Description:Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/30/2010
Entry Details Article
PubMed
Target5-hydroxytryptamine receptor 6(Human)
Universitat De Barcelona

Curated by ChEMBL
LigandPNGBDBM21358(2-[1-({6-chloroimidazo[2,1-b][1,3]thiazole-5-}sulf...)
Affinity DataKi:  2.20nMAssay Description:Displacement of [3H]-LSD from human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition constant incubated for 120 mins by Topcount s...More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/15/2024
Entry Details
PubMed
Target5-hydroxytryptamine receptor 6(Human)
Universitat De Barcelona

Curated by ChEMBL
LigandPNGBDBM21358(2-[1-({6-chloroimidazo[2,1-b][1,3]thiazole-5-}sulf...)
Affinity DataKi:  2.20nMAssay Description:Binding affinity to 5-HT6R (unknown origin) assessed as inhibition constantMore data for this Ligand-Target Pair
In Depth
Date in BDB:
6/26/2023
Entry Details
PubMed
Target5-hydroxytryptamine receptor 2C(Human)
Wyeth Research

LigandPNGBDBM21358(2-[1-({6-chloroimidazo[2,1-b][1,3]thiazole-5-}sulf...)
Affinity DataKi:  124nM ΔG°:  -9.32kcal/molepH: 7.4 T: 2°CAssay Description:IC50 values for each test compound were determined from nonlinear regression analysis of data collected from ligand binding experiments. The inhibiti...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/7/2008
Entry Details Article
PubMed
Target5-hydroxytryptamine receptor 2B(Human)
Wyeth Research

LigandPNGBDBM21358(2-[1-({6-chloroimidazo[2,1-b][1,3]thiazole-5-}sulf...)
Affinity DataKi:  458nM ΔG°:  -8.55kcal/molepH: 7.4 T: 2°CAssay Description:IC50 values for each test compound were determined from nonlinear regression analysis of data collected from ligand binding experiments. The inhibiti...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/7/2008
Entry Details Article
PubMed
Target5-hydroxytryptamine receptor 7(Human)
Wyeth Research

LigandPNGBDBM21358(2-[1-({6-chloroimidazo[2,1-b][1,3]thiazole-5-}sulf...)
Affinity DataKi:  679nM ΔG°:  -8.32kcal/molepH: 7.4 T: 2°CAssay Description:IC50 values for each test compound were determined from nonlinear regression analysis of data collected from ligand binding experiments. The inhibiti...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/7/2008
Entry Details Article
PubMed