Compile Data Set for Download or QSAR
Report error Found 22 Enz. Inhib. hit(s) for PDB: 7NA8
TargetGrowth hormone secretagogue receptor type 1(Human)
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50049478(1-{[(2R)-3-(benzyloxy)-1-{1-methanesulfonyl-1,2-di...)
Affinity DataKd:  0.140nMAssay Description:Compound was evaluated for binding affinity using [35S]MK-0677 (800-1100 Ci/mmol), as radioligand having specific high activityMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetGrowth hormone secretagogue receptor type 1(Human)
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50049478(1-{[(2R)-3-(benzyloxy)-1-{1-methanesulfonyl-1,2-di...)
Affinity DataKi:  0.240nMAssay Description:Binding Affinity against Growth hormone secretagogue receptor of swine using [35S]MK-0677 as radioligandMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetGrowth hormone secretagogue receptor type 1(Human)
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50049478(1-{[(2R)-3-(benzyloxy)-1-{1-methanesulfonyl-1,2-di...)
Affinity DataEC50:  0.398nMAssay Description:Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
6/25/2020
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetGrowth hormone secretagogue receptor type 1(Human)
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50049478(1-{[(2R)-3-(benzyloxy)-1-{1-methanesulfonyl-1,2-di...)
Affinity DataEC50:  0.400nMAssay Description:Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
6/25/2020
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetGrowth hormone secretagogue receptor type 1(Human)
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50049478(1-{[(2R)-3-(benzyloxy)-1-{1-methanesulfonyl-1,2-di...)
Affinity DataIC50: 0.400nMAssay Description:Inhibition against human growth hormone secretagogue (GHS) receptorMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetGrowth hormone secretagogue receptor type 1(Human)
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50049478(1-{[(2R)-3-(benzyloxy)-1-{1-methanesulfonyl-1,2-di...)
Affinity DataIC50: 0.510nMAssay Description:Ability to displace [125I]ghrelin from cloned human Growth hormone secretagogue receptor type I (GSH1a) receptor expressed in COS-7 cellsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/27/2012
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetGrowth hormone secretagogue receptor type 1(Human)
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50049478(1-{[(2R)-3-(benzyloxy)-1-{1-methanesulfonyl-1,2-di...)
Affinity DataIC50: 0.630nMAssay Description:Functional potency measured as intracellular calcium elevation in Hek-293 cells expressing hGHSR1aMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/3/2012
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetGrowth hormone secretagogue receptor type 1(Human)
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50049478(1-{[(2R)-3-(benzyloxy)-1-{1-methanesulfonyl-1,2-di...)
Affinity DataIC50: 0.760nMAssay Description:Binding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligandMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/30/2012
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetGrowth hormone secretagogue receptor type 1(Human)
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50049478(1-{[(2R)-3-(benzyloxy)-1-{1-methanesulfonyl-1,2-di...)
Affinity DataEC50:  1.30nMAssay Description:Agonist activity at human GHS-R1More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/13/2012
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetGrowth hormone secretagogue receptor type 1(Rat)
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50049478(1-{[(2R)-3-(benzyloxy)-1-{1-methanesulfonyl-1,2-di...)
Affinity DataEC50:  1.30nMAssay Description:In vitro growth hormone release was determined in rat pituitary cell assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetGrowth hormone secretagogue receptor type 1(Human)
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50049478(1-{[(2R)-3-(benzyloxy)-1-{1-methanesulfonyl-1,2-di...)
Affinity DataEC50:  1.40nMAssay Description:Functional potency measured as intracellular calcium elevation in Hek-293 cells expressing hGHSR1aMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/3/2012
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetGrowth hormone secretagogue receptor type 1(Human)
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50049478(1-{[(2R)-3-(benzyloxy)-1-{1-methanesulfonyl-1,2-di...)
Affinity DataIC50: 2nMAssay Description:Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
6/25/2020
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetGrowth hormone secretagogue receptor type 1(Human)
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50049478(1-{[(2R)-3-(benzyloxy)-1-{1-methanesulfonyl-1,2-di...)
Affinity DataIC50: 2nMAssay Description:Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
6/25/2020
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetGrowth hormone secretagogue receptor type 1 [E24Q](Human)
Université Montpellier 1

LigandPNGBDBM50049478(1-{[(2R)-3-(benzyloxy)-1-{1-methanesulfonyl-1,2-di...)
Affinity DataKi:  8.90nMAssay Description:Briefly, direct ligand binding experiments were performed using fluorescence energy transfer with the purified receptor labeled with Alexa Fluor 350 ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/9/2017
Entry Details Article
PubMedPDB3D3D Structure (crystal)
LigandPNGBDBM50049478(1-{[(2R)-3-(benzyloxy)-1-{1-methanesulfonyl-1,2-di...)
Affinity DataKi:  9.90nMAssay Description:Briefly, direct ligand binding experiments were performed using fluorescence energy transfer with the purified receptor labeled with Alexa Fluor 350 ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/9/2017
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetDimer of Growth hormone secretagogue receptor type 1(Human)
Université Montpellier 1

LigandPNGBDBM50049478(1-{[(2R)-3-(benzyloxy)-1-{1-methanesulfonyl-1,2-di...)
Affinity DataKi:  10.2nMAssay Description:Briefly, direct ligand binding experiments were performed using fluorescence energy transfer with the purified receptor labeled with Alexa Fluor 350 ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/9/2017
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetGrowth hormone secretagogue receptor type 1(Human)
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50049478(1-{[(2R)-3-(benzyloxy)-1-{1-methanesulfonyl-1,2-di...)
Affinity DataIC50: 32nMAssay Description:Binding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligandMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/30/2012
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetGrowth hormone secretagogue receptor type 1(Human)
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50049478(1-{[(2R)-3-(benzyloxy)-1-{1-methanesulfonyl-1,2-di...)
Affinity DataKi:  65.8nMAssay Description:Briefly, direct ligand binding experiments were performed using fluorescence energy transfer with the purified receptor labeled with Alexa Fluor 350 ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/9/2017
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetDimer of Growth hormone secretagogue receptor type 1(Human)
Université Montpellier 1

LigandPNGBDBM50049478(1-{[(2R)-3-(benzyloxy)-1-{1-methanesulfonyl-1,2-di...)
Affinity DataKi:  68.4nMAssay Description:Briefly, direct ligand binding experiments were performed using fluorescence energy transfer with the purified receptor labeled with Alexa Fluor 350 ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/9/2017
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetGrowth hormone secretagogue receptor type 1 [E24Q](Human)
Université Montpellier 1

LigandPNGBDBM50049478(1-{[(2R)-3-(benzyloxy)-1-{1-methanesulfonyl-1,2-di...)
Affinity DataKi:  68.9nMAssay Description:Briefly, direct ligand binding experiments were performed using fluorescence energy transfer with the purified receptor labeled with Alexa Fluor 350 ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/9/2017
Entry Details Article
PubMedPDB3D3D Structure (crystal)
LigandPNGBDBM50049478(1-{[(2R)-3-(benzyloxy)-1-{1-methanesulfonyl-1,2-di...)
Affinity DataKi:  90.6nMAssay Description:Briefly, direct ligand binding experiments were performed using fluorescence energy transfer with the purified receptor labeled with Alexa Fluor 350 ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/9/2017
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetGrowth hormone secretagogue receptor type 1(Human)
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50049478(1-{[(2R)-3-(benzyloxy)-1-{1-methanesulfonyl-1,2-di...)
Affinity DataIC50: 300nMAssay Description:Binding affinity for human growth hormone GH secretagogue (hGHsr) receptorMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/1/2012
Entry Details Article
PubMedPDB3D3D Structure (crystal)