Compile Data Set for Download or QSAR
Report error Found 24 Enz. Inhib. hit(s) for PDB: 7F58
TargetMelanocortin receptor 4(Rat)
Merck

Curated by ChEMBL
LigandPNGBDBM50119368((R)-1,2,3,4-Tetrahydro-isoquinoline-3-carboxylic a...)
Affinity DataIC50: 0.600nMAssay Description:Evaluated for binding affinity against rat Melanocortin-4 receptor (rMC4R) by displacing [125I]NDP-alpha-MSH radioligand expressed in CHO cellsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetMelanocortin receptor 4(Human)
Nanyang Technological University

Curated by ChEMBL
LigandPNGBDBM50119368((R)-1,2,3,4-Tetrahydro-isoquinoline-3-carboxylic a...)
Affinity DataEC50:  1nMAssay Description:Agonist activity at human MC4 receptor expressed in HEK293 cellsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/15/2012
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetMelanocortin receptor 4(Human)
Nanyang Technological University

Curated by ChEMBL
LigandPNGBDBM50119368((R)-1,2,3,4-Tetrahydro-isoquinoline-3-carboxylic a...)
Affinity DataIC50: 1.20nMAssay Description:Evaluated for binding affinity against human Melanocortin-4 receptor (hMC4R) by displacing [125I]NDP-alpha-MSH radioligand expressed in CHO cellsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetMelanocortin receptor 4(Human)
Nanyang Technological University

Curated by ChEMBL
LigandPNGBDBM50119368((R)-1,2,3,4-Tetrahydro-isoquinoline-3-carboxylic a...)
Affinity DataIC50: 1.20nMAssay Description:Activity against human MC4R by cAMP accumulationMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetMelanocortin receptor 4(Human)
Nanyang Technological University

Curated by ChEMBL
LigandPNGBDBM50119368((R)-1,2,3,4-Tetrahydro-isoquinoline-3-carboxylic a...)
Affinity DataIC50: 1.20nMAssay Description:Concentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC4R expressed in CHO cellsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetMelanocortin receptor 4(Human)
Nanyang Technological University

Curated by ChEMBL
LigandPNGBDBM50119368((R)-1,2,3,4-Tetrahydro-isoquinoline-3-carboxylic a...)
Affinity DataIC50: 1.20nMAssay Description:Evaluated for Functional Activity at Melanocortin-4 receptor as effective concentration at 50% maximum CMP accumulationMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetMelanocortin receptor 4(Human)
Nanyang Technological University

Curated by ChEMBL
LigandPNGBDBM50119368((R)-1,2,3,4-Tetrahydro-isoquinoline-3-carboxylic a...)
Affinity DataIC50: 1.20nMAssay Description:Displacement of [125]NDP-MSH from human MC4 receptor expressed in HEK293 cellsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetMelanocortin receptor 4(Human)
Nanyang Technological University

Curated by ChEMBL
LigandPNGBDBM50119368((R)-1,2,3,4-Tetrahydro-isoquinoline-3-carboxylic a...)
Affinity DataEC50:  1.5nMAssay Description:Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as stimulation of cAMP productionMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetMelanocortin receptor 4(Human)
Nanyang Technological University

Curated by ChEMBL
LigandPNGBDBM50119368((R)-1,2,3,4-Tetrahydro-isoquinoline-3-carboxylic a...)
Affinity DataEC50:  2.10nMAssay Description:Activity against human MC4R by cAMP accumulationMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetMelanocortin receptor 4(Human)
Nanyang Technological University

Curated by ChEMBL
LigandPNGBDBM50119368((R)-1,2,3,4-Tetrahydro-isoquinoline-3-carboxylic a...)
Affinity DataEC50:  2.10nMAssay Description:Evaluated for Functional Activity at Melanocortin-4 receptor as effective concentration at 50% maximum CMP accumulationMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetMelanocortin receptor 4(Human)
Nanyang Technological University

Curated by ChEMBL
LigandPNGBDBM50119368((R)-1,2,3,4-Tetrahydro-isoquinoline-3-carboxylic a...)
Affinity DataEC50:  2.10nMAssay Description:Agonist activity at human MC4 receptorMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/15/2012
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetMelanocortin receptor 4(Human)
Nanyang Technological University

Curated by ChEMBL
LigandPNGBDBM50119368((R)-1,2,3,4-Tetrahydro-isoquinoline-3-carboxylic a...)
Affinity DataEC50:  2.10nMAssay Description:Functional activity as concentration at 50% maximum cAMP accumulation in human Melanocortin-4 receptorMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetMelanocortin receptor 4(Rat)
Merck

Curated by ChEMBL
LigandPNGBDBM50119368((R)-1,2,3,4-Tetrahydro-isoquinoline-3-carboxylic a...)
Affinity DataEC50:  2.90nMAssay Description:Functional activity as concentration of the compound at 50% maximum cAMP accumulation in rat Melanocortin-4 receptor (rMC4R)More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetMelanocortin receptor 4(Human)
Nanyang Technological University

Curated by ChEMBL
LigandPNGBDBM50119368((R)-1,2,3,4-Tetrahydro-isoquinoline-3-carboxylic a...)
Affinity DataKi:  3nMAssay Description:Displacement of europium labeled NDP-alpha-MSH from human MC4 receptor expressed in HEK293 cellsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/15/2012
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetMelanocortin receptor 4(Human)
Nanyang Technological University

Curated by ChEMBL
LigandPNGBDBM50119368((R)-1,2,3,4-Tetrahydro-isoquinoline-3-carboxylic a...)
Affinity DataEC50:  3.60nMAssay Description:Stimulation of adenylate cyclase in HEK293 cells expressing the human MC4R receptor was determined by measuring cAMP accumulation using the RPA559 SP...More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetMelanocortin receptor 4(Human)
Nanyang Technological University

Curated by ChEMBL
LigandPNGBDBM50119368((R)-1,2,3,4-Tetrahydro-isoquinoline-3-carboxylic a...)
Affinity DataEC50:  4nMAssay Description:In vitro cAMP accumulation in HEK cells transfected with human melanocortin receptor-4 (hMC4R)More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/8/2012
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetMelanocortin receptor 4(Human)
Nanyang Technological University

Curated by ChEMBL
LigandPNGBDBM50119368((R)-1,2,3,4-Tetrahydro-isoquinoline-3-carboxylic a...)
Affinity DataEC50:  5.70nMAssay Description:Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetMelanocortin receptor 4(Mouse)
Neurocrine Biosciences

Curated by ChEMBL
LigandPNGBDBM50119368((R)-1,2,3,4-Tetrahydro-isoquinoline-3-carboxylic a...)
Affinity DataEC50:  7.60nMAssay Description:In vitro cAMP accumulation in Y1 cells transfected with mouse Melanocortin 4 receptor (mMC4R)More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/8/2012
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetMelanocortin receptor 4(Human)
Nanyang Technological University

Curated by ChEMBL
LigandPNGBDBM50119368((R)-1,2,3,4-Tetrahydro-isoquinoline-3-carboxylic a...)
Affinity DataIC50: 9nMAssay Description:Binding activity was measured using membranes of Hi5 cells expressing the human MC4R receptorsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetMelanocortin receptor 4(Human)
Nanyang Technological University

Curated by ChEMBL
LigandPNGBDBM50119368((R)-1,2,3,4-Tetrahydro-isoquinoline-3-carboxylic a...)
Affinity DataKi:  9nMAssay Description:Inhibitory activity towards human Melanocortin 4 ReceptorMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/2/2012
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetMelanocortin receptor 4(Human)
Nanyang Technological University

Curated by ChEMBL
LigandPNGBDBM50119368((R)-1,2,3,4-Tetrahydro-isoquinoline-3-carboxylic a...)
Affinity DataKi:  10.7nMMore data for this Ligand-Target Pair
In Depth
Date in BDB:
6/8/2012
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetMelanocortin receptor 4(Human)
Nanyang Technological University

Curated by ChEMBL
LigandPNGBDBM50119368((R)-1,2,3,4-Tetrahydro-isoquinoline-3-carboxylic a...)
Affinity DataKi:  33nMAssay Description:Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptorMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetMelanocortin receptor 4(Human)
Nanyang Technological University

Curated by ChEMBL
LigandPNGBDBM50119368((R)-1,2,3,4-Tetrahydro-isoquinoline-3-carboxylic a...)
Affinity DataEC50:  49nMAssay Description:Agonist activity at human MC4 D122A mutant expressed in HEK293 cells assessed as stimulation of cAMP productionMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetMelanocortin receptor 4(Human)
Nanyang Technological University

Curated by ChEMBL
LigandPNGBDBM50119368((R)-1,2,3,4-Tetrahydro-isoquinoline-3-carboxylic a...)
Affinity DataKi:  646nMAssay Description:Displacement of [125I]NDP-alpha-MSH from MC4R D122A mutant expressed in HEK293 cellsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMedPDB3D3D Structure (crystal)