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TargetApoptosis regulator Bcl-2(Human)
University of Caen Normandy

Curated by ChEMBL
LigandPNGBDBM50162774(ABT-199 | US11420968, Example ABT-199 | Venetoclax)
Affinity DataKi:  0.0180nMAssay Description:Inhibition of wild-type BCL-2 (unknown origin) expressed in Escherichia coli BL21 cells using biotinylated BIMBH3 or BAXBH3 peptide by surface plasmo...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

TargetInduced myeloid leukemia cell differentiation protein Mcl-1(Human)
University of Caen Normandy

Curated by ChEMBL
LigandPNGBDBM50519624(CHEMBL4468645)
Affinity DataKi:  0.0400nMAssay Description:Inhibition of TAMRA-labeled BIM BH3 peptide binding to human Mcl1 (171 to 327 residues) incubated for 120 mins by fluorescence polarizationMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sidPDB
In DepthDetails ArticlePubMedPDB3D3D Structure (crystal)

TargetApoptosis regulator Bcl-2(Human)
University of Caen Normandy

Curated by ChEMBL
LigandPNGBDBM50519612(CHEMBL591907)
Affinity DataKi:  0.0440nMAssay Description:Inhibition of His-tagged Bcl-2 (unknown origin) incubated for 30 mins by TR-FRET assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

TargetInduced myeloid leukemia cell differentiation protein Mcl-1(Human)
University of Caen Normandy

Curated by ChEMBL
LigandPNGBDBM50519617(CHEMBL4560418)
Affinity DataKi:  0.0500nMAssay Description:Inhibition of TAMRA-labeled BIM BH3 peptide binding to human Mcl1 (171 to 327 residues) incubated for 120 mins by fluorescence polarizationMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sidPDB
In DepthDetails ArticlePubMedPDB3D3D Structure (crystal)

TargetApoptosis regulator Bcl-2(Human)
University of Caen Normandy

Curated by ChEMBL
LigandPNGBDBM178570(US9125913, 129)
Affinity DataKi: <0.100nMAssay Description:Inhibition of His-tagged Bcl-2 (unknown origin) incubated for 30 mins by TR-FRET assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

TargetInduced myeloid leukemia cell differentiation protein Mcl-1(Human)
University of Caen Normandy

Curated by ChEMBL
LigandPNGBDBM50519618(CHEMBL4465718)
Affinity DataKi:  0.140nMAssay Description:Inhibition of TAMRA-labeled BIM BH3 peptide binding to human Mcl1 (171 to 327 residues) incubated for 120 mins by fluorescence polarizationMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sidPDB
In DepthDetails ArticlePubMedPDB3D3D Structure (crystal)

TargetInduced myeloid leukemia cell differentiation protein Mcl-1(Human)
University of Caen Normandy

Curated by ChEMBL
LigandPNGBDBM333146(Compound I | US10196404, Example 1 | US10196404, E...)
Affinity DataKi:  0.200nMAssay Description:Inhibition of N-terminal GST-tagged-Mcl1 (E171 to G327) (unknown origin) expressed in Escherichia coli using HyLite Fluor 647-labeled Bim peptide C a...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMedPDB3D3D Structure (crystal)

TargetApoptosis regulator Bcl-2(Human)
University of Caen Normandy

Curated by ChEMBL
LigandPNGBDBM50519609(CHEMBL4561305)
Affinity DataKi:  0.360nMAssay Description:Inhibition of wild-type BCL-2 (unknown origin) expressed in Escherichia coli BL21 cells using biotinylated BIMBH3 or BAXBH3 peptide by surface plasmo...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed

TargetAromatase(Human)
Centre D'Etudes Et De Recherche Sur Le MéDicament De Normandie

Curated by ChEMBL
LigandPNGBDBM8611(4-{5H,6H,7H,8H-imidazo[1,5-a]pyridin-5-yl}benzonit...)
Affinity DataKi:  0.600nMAssay Description:Inhibition constant for human aromatase cytochrome P450 19A1 activityMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

TargetInduced myeloid leukemia cell differentiation protein Mcl-1(Human)
University of Caen Normandy

Curated by ChEMBL
LigandPNGBDBM50244142(CHEMBL4086356 | US10533010, Example I-240 | US1120...)
Affinity DataKi: <1nMAssay Description:Inhibition of FITC-labelled BAK peptide binding to human MBP-fused Mcl-1 (172 to 327 residues) expressed in Escherichia coli BL21 CodonPlus (DE3) RIL...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMedPDB3D3D Structure (crystal)

TargetInduced myeloid leukemia cell differentiation protein Mcl-1(Human)
University of Caen Normandy

Curated by ChEMBL
LigandPNGBDBM50519614(CHEMBL4439276)
Affinity DataKi: <1.20nMAssay Description:Displacement of fluorescein labelled Puma-BH3 peptide from C-terminal MBP-fused human Mcl-1 (173 to 321 residues) expressed in Escherichia coli BL21(...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMedPDB3D3D Structure (crystal)

Target5-hydroxytryptamine receptor 4(Guinea pig)
Université

Curated by ChEMBL
LigandPNGBDBM50293279(1-Methyl-5-[(1-propylpiperidin-4-yl)methyloxy]-pyr...)
Affinity DataKi:  1.74nMAssay Description:Displacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum membraneMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

Target5-hydroxytryptamine receptor 3A(Human)
Université

Curated by ChEMBL
LigandPNGBDBM50108392((3-ENDO)-8-METHYL-8-AZABICYCLO[3.2.1]OCT-3-YL 1H-I...)
Affinity DataKi:  2.80nMAssay Description:Binding affinity at 5HT3 receptorMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMedPDB3D3D Structure (crystal)

Target5-hydroxytryptamine receptor 4(Guinea pig)
Université

Curated by ChEMBL
LigandPNGBDBM50122716(5-(Piperidin-4-ylmethoxy)-9-propyl-1,2,3,4-tetrahy...)
Affinity DataKi:  2.90nMAssay Description:Ability to displace [3H]GR-113808 from 5-hydroxytryptamine 4 receptorMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

Target5-hydroxytryptamine receptor 7(Human)
Université

Curated by ChEMBL
LigandPNGBDBM50170158(1-(2-Methoxy-phenyl)-4-(1-o-tolyl-1H-pyrrol-3-ylme...)
Affinity DataKi:  4.70nMAssay Description:Binding affinity against Human 5-HT7R expressed in sf9 cellsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

Target5-hydroxytryptamine receptor 7(Human)
Université

Curated by ChEMBL
LigandPNGBDBM50170158(1-(2-Methoxy-phenyl)-4-(1-o-tolyl-1H-pyrrol-3-ylme...)
Affinity DataKi:  4.70nMAssay Description:Displacement of [3H]LSD from human 5HT7 in sf9 cellsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

Target5-hydroxytryptamine receptor 4(Guinea pig)
Université

Curated by ChEMBL
LigandPNGBDBM50413548(CHEMBL512679)
Affinity DataKi:  5.37nMAssay Description:Displacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum membraneMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

Target5-hydroxytryptamine receptor 7(Human)
Université

Curated by ChEMBL
LigandPNGBDBM50170156(2-(3-((4-(2-methoxyphenyl)piperazin-1-yl)methyl)-1...)
Affinity DataKi:  5.40nMAssay Description:Binding affinity against Human 5-HT7R expressed in sf9 cellsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

Target5-hydroxytryptamine receptor 7(Human)
Université

Curated by ChEMBL
LigandPNGBDBM50170156(2-(3-((4-(2-methoxyphenyl)piperazin-1-yl)methyl)-1...)
Affinity DataKi:  5.40nMAssay Description:Displacement of [3H]LSD from human 5HT7 in sf9 cellsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

Target5-hydroxytryptamine receptor 7(Human)
Université

Curated by ChEMBL
LigandPNGBDBM50210122(CHEMBL234881 | [2-(2',6'-dimethyl-biphenyl-3-yl)-e...)
Affinity DataKi:  6.20nMAssay Description:Displacement of [3H]LSD from human 5HT7 in sf9 cellsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

Target5-hydroxytryptamine receptor 4(Guinea pig)
Université

Curated by ChEMBL
LigandPNGBDBM50413547(CHEMBL448702)
Affinity DataKi:  6.46nMAssay Description:Displacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum membraneMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

Target5-hydroxytryptamine receptor 7(Human)
Université

Curated by ChEMBL
LigandPNGBDBM50210124(2-(2'-methyl-biphenyl-3-yl)-ethylamine | CHEMBL234...)
Affinity DataKi:  7.5nMAssay Description:Displacement of [3H]LSD from human 5HT7 in sf9 cellsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

Target5-hydroxytryptamine receptor 7(Human)
Université

Curated by ChEMBL
LigandPNGBDBM50210123(CHEMBL395870 | N,N-dimethyl-2-(2'-methylbiphenyl-3...)
Affinity DataKi:  7.60nMAssay Description:Displacement of [3H]LSD from human 5HT7 in sf9 cellsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

Target5-hydroxytryptamine receptor 7(Human)
Université

Curated by ChEMBL
LigandPNGBDBM50210126(CHEMBL232792 | [2-(2'-methoxy-biphenyl-3-yl)-ethyl...)
Affinity DataKi:  8.40nMAssay Description:Displacement of [3H]LSD from human 5HT7 in sf9 cellsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

Target5-hydroxytryptamine receptor 4(Guinea pig)
Université

Curated by ChEMBL
LigandPNGBDBM50413546(CHEMBL513254)
Affinity DataKi:  8.51nMAssay Description:Displacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum membraneMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

Target5-hydroxytryptamine receptor 7(Human)
Université

Curated by ChEMBL
LigandPNGBDBM50210125(CHEMBL232791 | [2-(2',6'-dimethoxy-biphenyl-3-yl)-...)
Affinity DataKi:  8.60nMAssay Description:Displacement of [3H]LSD from human 5HT7 in sf9 cellsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

Target5-hydroxytryptamine receptor 4(Guinea pig)
Université

Curated by ChEMBL
LigandPNGBDBM50413545(CHEMBL469575)
Affinity DataKi:  8.71nMAssay Description:Displacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum membraneMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

Target5-hydroxytryptamine receptor 4(Guinea pig)
Université

Curated by ChEMBL
LigandPNGBDBM50413544(CHEMBL511794)
Affinity DataKi:  9.55nMAssay Description:Displacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum membraneMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

Target5-hydroxytryptamine receptor 1A(Rat)
Université

Curated by ChEMBL
LigandPNGBDBM50170158(1-(2-Methoxy-phenyl)-4-(1-o-tolyl-1H-pyrrol-3-ylme...)
Affinity DataKi:  9.90nMAssay Description:Binding affinity against rat 5-HT1A receptorMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

Target5-hydroxytryptamine receptor 1A(Rat)
Université

Curated by ChEMBL
LigandPNGBDBM50170158(1-(2-Methoxy-phenyl)-4-(1-o-tolyl-1H-pyrrol-3-ylme...)
Affinity DataKi:  9.90nMAssay Description:Binding affinity to rat 5HT1AMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

Target5-hydroxytryptamine receptor 4(Guinea pig)
Université

Curated by ChEMBL
LigandPNGBDBM50122722(9-Butyl-5-(piperidin-4-ylmethoxy)-1,2,3,4-tetrahyd...)
Affinity DataKi:  10nMAssay Description:Ability to displace [3H]GR-113808 from 5-hydroxytryptamine 4 receptorMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

TargetAromatase(Human)
Centre D'Etudes Et De Recherche Sur Le MéDicament De Normandie

Curated by ChEMBL
LigandPNGBDBM50070095(3-Phenyl-2-[1-pyridin-4-yl-meth-(Z)-ylidene]-indan...)
Affinity DataKi:  10nMAssay Description:Inhibition constant for human aromatase cytochrome P450 19A1 activityMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

TargetAromatase(Human)
Centre D'Etudes Et De Recherche Sur Le MéDicament De Normandie

Curated by ChEMBL
LigandPNGBDBM50070097((Z)-6-(4-chlorophenyl)-7-(pyridin-4-ylmethylene)-6...)
Affinity DataKi:  10nMAssay Description:Inhibition constant for human aromatase cytochrome P450 19A1 activityMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

Target5-hydroxytryptamine receptor 4(Guinea pig)
Université

Curated by ChEMBL
LigandPNGBDBM50122721(6-(1-Ethyl-piperidin-4-ylmethoxy)-8,9,10,11-tetrah...)
Affinity DataKi:  11nMAssay Description:Ability to displace [3H]GR-113808 from 5-hydroxytryptamine 4 receptorMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

Target5-hydroxytryptamine receptor 4(Guinea pig)
Université

Curated by ChEMBL
LigandPNGBDBM50413543(CHEMBL472481)
Affinity DataKi:  11.2nMAssay Description:Displacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum membraneMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

Target5-hydroxytryptamine receptor 4(Guinea pig)
Université

Curated by ChEMBL
LigandPNGBDBM50413542(CHEMBL469582)
Affinity DataKi:  11.8nMAssay Description:Displacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum membraneMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

Target5-hydroxytryptamine receptor 4(Guinea pig)
Université

Curated by ChEMBL
LigandPNGBDBM50413541(CHEMBL469593)
Affinity DataKi:  12.9nMAssay Description:Displacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum membraneMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

Target5-hydroxytryptamine receptor 4(Guinea pig)
Université

Curated by ChEMBL
LigandPNGBDBM50122723(9-Ethyl-5-(piperidin-4-ylmethoxy)-1,2,3,4-tetrahyd...)
Affinity DataKi:  13nMAssay Description:Ability to displace [3H]GR-113808 from 5-hydroxytryptamine 4 receptorMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

Target5-hydroxytryptamine receptor 4(Guinea pig)
Université

Curated by ChEMBL
LigandPNGBDBM50122719(9-Pentyl-5-(piperidin-4-ylmethoxy)-1,2,3,4-tetrahy...)
Affinity DataKi:  13nMAssay Description:Ability to displace [3H]GR-113808 from 5-hydroxytryptamine 4 receptorMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

Target5-hydroxytryptamine receptor 4(Guinea pig)
Université

Curated by ChEMBL
LigandPNGBDBM50122718(6-(1-Propyl-piperidin-4-ylmethoxy)-8,9,10,11-tetra...)
Affinity DataKi:  13nMAssay Description:Ability to displace [3H]GR-113808 from 5-hydroxytryptamine 4 receptorMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

Target5-hydroxytryptamine receptor 4(Guinea pig)
Université

Curated by ChEMBL
LigandPNGBDBM50122720(6-(1-Butyl-piperidin-4-ylmethoxy)-8,9,10,11-tetrah...)
Affinity DataKi:  16nMAssay Description:Ability to displace [3H]GR-113808 from 5-hydroxytryptamine 4 receptorMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

Target5-hydroxytryptamine receptor 4(Guinea pig)
Université

Curated by ChEMBL
LigandPNGBDBM50413539(CHEMBL450595)
Affinity DataKi:  16.2nMAssay Description:Displacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum membraneMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

Target5-hydroxytryptamine receptor 4(Guinea pig)
Université

Curated by ChEMBL
LigandPNGBDBM50413540(CHEMBL471662)
Affinity DataKi:  16.2nMAssay Description:Displacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum membraneMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

Target5-hydroxytryptamine receptor 7(Human)
Université

Curated by ChEMBL
LigandPNGBDBM50170159(2-{3-[4-(2-Methoxy-phenyl)-piperazin-1-ylmethyl]-p...)
Affinity DataKi:  18nMAssay Description:Displacement of [3H]LSD from human 5HT7 in sf9 cellsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

Target5-hydroxytryptamine receptor 7(Human)
Université

Curated by ChEMBL
LigandPNGBDBM50170159(2-{3-[4-(2-Methoxy-phenyl)-piperazin-1-ylmethyl]-p...)
Affinity DataKi:  18nMAssay Description:Binding affinity against Human 5-HT7R expressed in sf9 cellsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

Target5-hydroxytryptamine receptor 4(Guinea pig)
Université

Curated by ChEMBL
LigandPNGBDBM50413538(CHEMBL516340)
Affinity DataKi:  18.2nMAssay Description:Displacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum membraneMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

Target5-hydroxytryptamine receptor 1A(Rat)
Université

Curated by ChEMBL
LigandPNGBDBM50170159(2-{3-[4-(2-Methoxy-phenyl)-piperazin-1-ylmethyl]-p...)
Affinity DataKi:  18.5nMAssay Description:Binding affinity against rat 5-HT1A receptorMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

Target5-hydroxytryptamine receptor 1A(Rat)
Université

Curated by ChEMBL
LigandPNGBDBM50170159(2-{3-[4-(2-Methoxy-phenyl)-piperazin-1-ylmethyl]-p...)
Affinity DataKi:  18.5nMAssay Description:Binding affinity to rat 5HT1AMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

Target5-hydroxytryptamine receptor 7(Rat)
Université

Curated by ChEMBL
LigandPNGBDBM50170156(2-(3-((4-(2-methoxyphenyl)piperazin-1-yl)methyl)-1...)
Affinity DataKi:  19nMAssay Description:Binding affinity against rat 5-HT7R expressed in HEK-293 cellsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

Target5-hydroxytryptamine receptor 4(Guinea pig)
Université

Curated by ChEMBL
LigandPNGBDBM50413522(CHEMBL511312)
Affinity DataKi:  19.1nMAssay Description:Displacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum membraneMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

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