BindingDB PrimarySearch

Found 16 Enz. Inhib. hit(s) with Target = 'Growth hormone secretagogue receptor type 1' and Ligand = 'BDBM50049478'

Growth hormone secretagogue receptor type 1(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL

BDBM50049478(1-{[(2R)-3-(benzyloxy)-1-{1-methanesulfonyl-1,2-di...)

Ki: 0.240nMAssay Description:Binding Affinity of the compound against Growth hormone secretagogue receptor of swine using [35S]-MK-0677 as radioligandMore data for this Ligand-Target Pair

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3D Structure (crystal)

Growth hormone secretagogue receptor type 1(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL

BDBM50049478(1-{[(2R)-3-(benzyloxy)-1-{1-methanesulfonyl-1,2-di...)

Ki: 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

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3D Structure (crystal)

Growth hormone secretagogue receptor type 1(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL

BDBM50049478(1-{[(2R)-3-(benzyloxy)-1-{1-methanesulfonyl-1,2-di...)

IC50: 0.400nMAssay Description:Inhibition of the compound against human growth hormone secretagogue (GHS) receptorMore data for this Ligand-Target Pair

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3D Structure (crystal)

Growth hormone secretagogue receptor type 1(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL

BDBM50049478(1-{[(2R)-3-(benzyloxy)-1-{1-methanesulfonyl-1,2-di...)

IC50: 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

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3D Structure (crystal)

Growth hormone secretagogue receptor type 1(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL

BDBM50049478(1-{[(2R)-3-(benzyloxy)-1-{1-methanesulfonyl-1,2-di...)

IC50: 0.630nMAssay Description:Binding affinity towards human Growth hormone secretagogue receptor type 1 using competitive binding assay with radiolabeled [35S]-MK-0677 expressed ...More data for this Ligand-Target Pair

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3D Structure (crystal)

Growth hormone secretagogue receptor type 1(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL

BDBM50049478(1-{[(2R)-3-(benzyloxy)-1-{1-methanesulfonyl-1,2-di...)

IC50: 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

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3D Structure (crystal)

Growth hormone secretagogue receptor type 1(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL

BDBM50049478(1-{[(2R)-3-(benzyloxy)-1-{1-methanesulfonyl-1,2-di...)

IC50: 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

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3D Structure (crystal)

Growth hormone secretagogue receptor type 1(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL

BDBM50049478(1-{[(2R)-3-(benzyloxy)-1-{1-methanesulfonyl-1,2-di...)

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3D Structure (crystal)

Growth hormone secretagogue receptor type 1(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL

BDBM50049478(1-{[(2R)-3-(benzyloxy)-1-{1-methanesulfonyl-1,2-di...)

IC50: 32nMAssay Description:Binding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligandMore data for this Ligand-Target Pair

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3D Structure (crystal)

Growth hormone secretagogue receptor type 1(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL

BDBM50049478(1-{[(2R)-3-(benzyloxy)-1-{1-methanesulfonyl-1,2-di...)

IC50: 300nMAssay Description:Binding affinity for human growth hormone GH secretagogue (hGHsr) receptorMore data for this Ligand-Target Pair

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3D Structure (crystal)

Growth hormone secretagogue receptor type 1(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL

BDBM50049478(1-{[(2R)-3-(benzyloxy)-1-{1-methanesulfonyl-1,2-di...)

EC50: 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

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3D Structure (crystal)

Growth hormone secretagogue receptor type 1(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL

BDBM50049478(1-{[(2R)-3-(benzyloxy)-1-{1-methanesulfonyl-1,2-di...)

EC50: 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

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3D Structure (crystal)

Growth hormone secretagogue receptor type 1(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL

BDBM50049478(1-{[(2R)-3-(benzyloxy)-1-{1-methanesulfonyl-1,2-di...)

EC50: 1.30nMAssay Description:Agonist activity at human GHS-R1More data for this Ligand-Target Pair

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3D Structure (crystal)

Growth hormone secretagogue receptor type 1(Rattus norvegicus)
Merck Research Laboratories

Curated by ChEMBL

BDBM50049478(1-{[(2R)-3-(benzyloxy)-1-{1-methanesulfonyl-1,2-di...)

EC50: 1.30nMAssay Description:In vitro growth hormone release was determined in rat pituitary cell assayMore data for this Ligand-Target Pair

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3D Structure (crystal)

Growth hormone secretagogue receptor type 1(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL

BDBM50049478(1-{[(2R)-3-(benzyloxy)-1-{1-methanesulfonyl-1,2-di...)

Kd: 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

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3D Structure (crystal)

Growth hormone secretagogue receptor type 1(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL

BDBM50049478(1-{[(2R)-3-(benzyloxy)-1-{1-methanesulfonyl-1,2-di...)

EC50: 1.40nMAssay Description:Binding affinity towards human Growth hormone secretagogue receptor type 1 using competitive binding assay with radiolabeled [35S]-MK-0677 expressed ...More data for this Ligand-Target Pair

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3D Structure (crystal)

Filter my 16 hits

Targets 1▿
- Growth hormone secretagogue receptor type 1 16
Publications 11▿
- J Med Chem 61: 5974-5987 (2018) 4
- J Med Chem 46: 1191-203 (2003) 2
- Bioorg Med Chem Lett 11: 1955-7 (2001) 2
- Bioorg Med Chem Lett 8: 107-12 (1999) 1
- J Med Chem 47: 888-99 (2004) 1
- J Med Chem 39: 1767-70 (1996) 1
- Bioorg Med Chem Lett 10: 5-8 (2000) 1
- Bioorg Med Chem 15: 3054-64 (2007) 1
- J Med Chem 45: 5609-16 (2002) 1
- J Med Chem 41: 3103-27 (1998) 1
- J Biol Chem 288: 24656-65 (2013) 1
Institutions 6▿
- Merck Research Laboratories 7
- Astrazeneca 4
- University Of Montpellier 2
- Universit� Montpellier 1 1
- Novo Nordisk 1
- Universit£ 1
Affinity: 0.14 to 3.0E+2 nM▿
- Ki 2
- IC50 8
- Kd 1
- EC50 5
- Affinity ≤ nM
Xtal structures: 1
Docked structures: 0
Catalog Cmpds: 1