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Report error Found 31 Enz. Inhib. hit(s) for PDB: 8DPF
Target5-hydroxytryptamine receptor 2C(Human)
Arena Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50161646((1R)-8-chloro-2,3,4,5-tetrahydro-1-methyl-1H-3-ben...)
Affinity DataKi:  15nMAssay Description:Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from recombinant human 5HT2C receptor expressed in HEK293 cells measured after 2...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMedPDB3D3D Structure (crystal)

Target5-hydroxytryptamine receptor 2C(Human)
Arena Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50161646((1R)-8-chloro-2,3,4,5-tetrahydro-1-methyl-1H-3-ben...)
Affinity DataKi:  15nMAssay Description:Displacement of [125I]DOI from human recombinant 5HT2C receptor expressed in HEK293 cells by scintillation countingMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMedPDB3D3D Structure (crystal)

Target5-hydroxytryptamine receptor 2C(Human)
Arena Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50161646((1R)-8-chloro-2,3,4,5-tetrahydro-1-methyl-1H-3-ben...)
Affinity DataKi:  15nMAssay Description:Displacement of [3H]DOI from recombinant human 5HT2C receptor expressed in HEK293T cell membranes after 1 hr by beta scintillation counting methodMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMedPDB3D3D Structure (crystal)

Target5-hydroxytryptamine receptor 2C(Human)
Arena Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50161646((1R)-8-chloro-2,3,4,5-tetrahydro-1-methyl-1H-3-ben...)
Affinity DataKi:  15nMAssay Description:Agonist activity at 5-HT2CR (unknown origin)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMedPDB3D3D Structure (crystal)

Target5-hydroxytryptamine receptor 2C(Human)
Arena Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50161646((1R)-8-chloro-2,3,4,5-tetrahydro-1-methyl-1H-3-ben...)
Affinity DataKi:  167nMAssay Description:Displacement of [3H]meselurgine from human 5HT2C receptor expressed in Swiss mouse 3T3 cells by scintillation proximity assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMedPDB3D3D Structure (crystal)

Target5-hydroxytryptamine receptor 2C(Human)
Arena Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50161646((1R)-8-chloro-2,3,4,5-tetrahydro-1-methyl-1H-3-ben...)
Affinity DataKi:  257nMAssay Description:Displacement of [3H]mesulergine from 5HT2C receptor (unknown origin)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMedPDB3D3D Structure (crystal)

Target5-hydroxytryptamine receptor 2C(Human)
Arena Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50161646((1R)-8-chloro-2,3,4,5-tetrahydro-1-methyl-1H-3-ben...)
Affinity DataEC50:  9nMAssay Description:Agonist activity at human 5HT2C receptor expressed in HEK293 cells by inositol phosphate accumulation assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMedPDB3D3D Structure (crystal)

Target5-hydroxytryptamine receptor 2C(Dog)
Pfizer

Curated by ChEMBL
LigandPNGBDBM50161646((1R)-8-chloro-2,3,4,5-tetrahydro-1-methyl-1H-3-ben...)
Affinity DataEC50:  16.2nMAssay Description:Agonist activity at dog 5HT2C receptorMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMedPDB3D3D Structure (crystal)

Target5-hydroxytryptamine receptor 2C(Human)
Arena Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50161646((1R)-8-chloro-2,3,4,5-tetrahydro-1-methyl-1H-3-ben...)
Affinity DataEC50:  210nMAssay Description:Agonist activity at human 5HT2C receptor expressed in CHO-K1 cells assessed as increase of fluorescence based calcium mobilization by FLIPR assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMedPDB3D3D Structure (crystal)

Target5-hydroxytryptamine receptor 2C(Human)
Arena Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50161646((1R)-8-chloro-2,3,4,5-tetrahydro-1-methyl-1H-3-ben...)
Affinity DataEC50:  9nMAssay Description:Agonist activity at 5-HT2C receptor (unknown origin)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMedPDB3D3D Structure (crystal)

Target5-hydroxytryptamine receptor 2C(Human)
Arena Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50161646((1R)-8-chloro-2,3,4,5-tetrahydro-1-methyl-1H-3-ben...)
Affinity DataEC50:  40nMAssay Description:Agonist activity at tTA containing TEV cleavage site-fused 5-HT2C-INI receptor isoform (unknown origin) expressed in TEV-fused beta-arrestin2 express...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMedPDB3D3D Structure (crystal)

Target5-hydroxytryptamine receptor 2C(Human)
Arena Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50161646((1R)-8-chloro-2,3,4,5-tetrahydro-1-methyl-1H-3-ben...)
Affinity DataEC50:  40nMAssay Description:Agonist activity at tTA containing TEV cleavage site-fused 5-HT2C-INI receptor isoform (unknown origin) expressed in TEV-fused beta-arrestin2 express...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMedPDB3D3D Structure (crystal)

Target5-hydroxytryptamine receptor 2C(Human)
Arena Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50161646((1R)-8-chloro-2,3,4,5-tetrahydro-1-methyl-1H-3-ben...)
Affinity DataEC50:  2.10nMAssay Description:Agonist activity at human 5-HT2C-INI receptor isoform expressed in Flp-IN HEK293 cells assessed as induction of Gq-mediated calcium flux measured eve...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMedPDB3D3D Structure (crystal)

Target5-hydroxytryptamine receptor 2C(Human)
Arena Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50161646((1R)-8-chloro-2,3,4,5-tetrahydro-1-methyl-1H-3-ben...)
Affinity DataEC50:  2.10nMAssay Description:Agonist activity at human 5-HT2C-INI receptor isoform expressed in Flp-IN HEK293 cells assessed as induction of Gq-mediated calcium flux measured eve...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMedPDB3D3D Structure (crystal)

Target5-hydroxytryptamine receptor 2C(Human)
Arena Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50161646((1R)-8-chloro-2,3,4,5-tetrahydro-1-methyl-1H-3-ben...)
Affinity DataEC50:  7.90nMAssay Description:Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMedPDB3D3D Structure (crystal)

Target5-hydroxytryptamine receptor 2C(Human)
Arena Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50161628((1R,S)-8-chloro-2,3,4,5-tetrahydro-1-methyl-1H-3-b...)
Affinity DataEC50:  13nMAssay Description:Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMedPDB3D3D Structure (crystal)

Target5-hydroxytryptamine receptor 2C(Human)
Arena Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50161646((1R)-8-chloro-2,3,4,5-tetrahydro-1-methyl-1H-3-ben...)
Affinity DataEC50:  4.80nMAssay Description:Agonist activity at recombinant human unedited 5HT2C receptor isoform INI expressed in Flp-In-293 cells assessed as increase in calcium influx measur...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMedPDB3D3D Structure (crystal)

Target5-hydroxytryptamine receptor 2C(Human)
Arena Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50161646((1R)-8-chloro-2,3,4,5-tetrahydro-1-methyl-1H-3-ben...)
Affinity DataEC50:  4.80nMAssay Description:Agonist activity at recombinant human unedited 5HT2C receptor isoform INI expressed in Flp-In-293 cells assessed as increase in calcium influx measur...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMedPDB3D3D Structure (crystal)

Target5-hydroxytryptamine receptor 2C(Human)
Arena Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50161646((1R)-8-chloro-2,3,4,5-tetrahydro-1-methyl-1H-3-ben...)
Affinity DataEC50:  7.60nMAssay Description:Agonist activity at recombinant human 5HT2C receptor expressed in HEK293 cells assessed as accumulation of inositol phosphate measured after 2 hrs in...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMedPDB3D3D Structure (crystal)

Target5-hydroxytryptamine receptor 2C(Human)
Arena Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50161646((1R)-8-chloro-2,3,4,5-tetrahydro-1-methyl-1H-3-ben...)
Affinity DataEC50:  2.60nMAssay Description:Agonist activity at human 5-HT2C receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 dire...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMedPDB3D3D Structure (crystal)

Target5-hydroxytryptamine receptor 2C(Human)
Arena Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50161646((1R)-8-chloro-2,3,4,5-tetrahydro-1-methyl-1H-3-ben...)
Affinity DataEC50:  2.60nMAssay Description:Agonist activity at human 5-HT2C receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 dire...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMedPDB3D3D Structure (crystal)

Target5-hydroxytryptamine receptor 2C(Human)
Arena Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50161646((1R)-8-chloro-2,3,4,5-tetrahydro-1-methyl-1H-3-ben...)
Affinity DataEC50:  3.5nMAssay Description:Agonist activity at human 5-HT2C INI receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMedPDB3D3D Structure (crystal)

Target5-hydroxytryptamine receptor 2C(Human)
Arena Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50161646((1R)-8-chloro-2,3,4,5-tetrahydro-1-methyl-1H-3-ben...)
Affinity DataEC50:  3.40nMAssay Description:Agonist activity at human 5-HT2C INI receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMedPDB3D3D Structure (crystal)

Target5-hydroxytryptamine receptor 2C(Human)
Arena Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50161646((1R)-8-chloro-2,3,4,5-tetrahydro-1-methyl-1H-3-ben...)
Affinity DataEC50:  59nMAssay Description:Agonist activity at human 5-HT2C INI receptor expressed in human HEK293 cells assessed as induction of beta-arrestin-2 recruitment incubated for 20 h...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMedPDB3D3D Structure (crystal)

Target5-hydroxytryptamine receptor 2C(Human)
Arena Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50161646((1R)-8-chloro-2,3,4,5-tetrahydro-1-methyl-1H-3-ben...)
Affinity DataEC50:  2.70nMAssay Description:Agonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMedPDB3D3D Structure (crystal)

Target5-hydroxytryptamine receptor 2C(Human)
Arena Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50161646((1R)-8-chloro-2,3,4,5-tetrahydro-1-methyl-1H-3-ben...)
Affinity DataEC50:  2.70nMAssay Description:Agonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMedPDB3D3D Structure (crystal)

Target5-hydroxytryptamine receptor 2C(Human)
Arena Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50161646((1R)-8-chloro-2,3,4,5-tetrahydro-1-methyl-1H-3-ben...)
Affinity DataEC50:  2.70nMAssay Description:Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMedPDB3D3D Structure (crystal)

Target5-hydroxytryptamine receptor 2C(Human)
Arena Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50161646((1R)-8-chloro-2,3,4,5-tetrahydro-1-methyl-1H-3-ben...)
Affinity DataEC50:  3.60nMAssay Description:Agonist activity at human 5-HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMedPDB3D3D Structure (crystal)

Target5-hydroxytryptamine receptor 2C(Human)
Arena Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50161646((1R)-8-chloro-2,3,4,5-tetrahydro-1-methyl-1H-3-ben...)
Affinity DataEC50:  59nMAssay Description:Agonist activity at human 5-HT2C INI receptor expressed in human HEK293 cells assessed as induction of beta-arrestin-2 recruitment incubated for 20 h...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMedPDB3D3D Structure (crystal)

Target5-hydroxytryptamine receptor 2C(Human)
Arena Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50161628((1R,S)-8-chloro-2,3,4,5-tetrahydro-1-methyl-1H-3-b...)
Affinity DataEC50:  11nMAssay Description:Effective concentration towards 5-hydroxytryptamine 2A receptors transfected in HEK-293 cells was determined by measuring [3H]-phosphoinositol releas...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMedPDB3D3D Structure (crystal)

Target5-hydroxytryptamine receptor 2C(Human)
Arena Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50161646((1R)-8-chloro-2,3,4,5-tetrahydro-1-methyl-1H-3-ben...)
Affinity DataEC50:  11nMAssay Description:Effective concentration towards 5-hydroxytryptamine 2A receptors transfected in HEK-293 cells was determined by measuring [3H]-phosphoinositol releas...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMedPDB3D3D Structure (crystal)