ibutamoren [Ligand Id: 5867] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL13817 (Ibutamoren, L-163,191, MK-677)
  • ghrelin receptor/Ghrelin receptor in Human [ChEMBL: CHEMBL4616] [GtoPdb: 246] [UniProtKB: Q92847]
  • ghrelin receptor/Ghrelin receptor in Rat [ChEMBL: CHEMBL3278] [GtoPdb: 246] [UniProtKB: O08725]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
ghrelin receptor/Ghrelin receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4616] [GtoPdb: 246] [UniProtKB: Q92847]
ChEMBL Compound was evaluated for binding affinity using [35S]MK-0677 (800-1100 Ci/mmol), as radioligand having specific high activity B 9.85 pKd 0.14 nM Kd J Med Chem (1998) 41: 3103-3127 [PMID:9703459]
GtoPdb - - 9.34 pKi 0.46 nM Ki Eur J Endocrinol (1999) 141: 180-9 [PMID:10427162]
ChEMBL Binding Affinity against Growth hormone secretagogue receptor of swine using [35S]MK-0677 as radioligand B 9.62 pKi 0.24 nM Ki J Med Chem (1996) 39: 1767-1770 [PMID:8627599]
ChEMBL Binding affinity for human growth hormone GH secretagogue (hGHsr) receptor B 6.52 pIC50 300 nM IC50 Bioorg Med Chem Lett (2000) 10: 5-8 [PMID:10636230]
ChEMBL Binding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligand B 7.49 pIC50 32 nM IC50 J Med Chem (2003) 46: 1191-1203 [PMID:12646029]
ChEMBL Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay B 8.7 pIC50 2 nM IC50 J Med Chem (2018) 61: 5974-5987 [PMID:29909635]
ChEMBL Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay B 8.7 pIC50 2 nM IC50 J Med Chem (2018) 61: 5974-5987 [PMID:29909635]
ChEMBL Binding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligand B 9.12 pIC50 0.76 nM IC50 J Med Chem (2003) 46: 1191-1203 [PMID:12646029]
ChEMBL Binding affinity towards human Growth hormone secretagogue receptor type 1 using competitive binding assay with radiolabeled [35S]-MK-0677 expressed as IC50 B 9.2 pIC50 0.63 nM IC50 Bioorg Med Chem Lett (2001) 11: 1955-1957 [PMID:11459669]
ChEMBL Ability to displace [125I]ghrelin from cloned human Growth hormone secretagogue receptor type I (GSH1a) receptor expressed in COS-7 cells B 9.29 pIC50 0.51 nM IC50 J Med Chem (2002) 45: 5609-5616 [PMID:12477342]
ChEMBL Inhibition against human growth hormone secretagogue (GHS) receptor B 9.4 pIC50 0.4 nM IC50 J Med Chem (2004) 47: 888-899 [PMID:14761190]
ChEMBL Functional potency measured as intracellular calcium elevation in Hek-293 cells expressing hGHSR1a F 8.84 pEC50 1.43 nM EC50 Bioorg Med Chem Lett (2001) 11: 1955-1957 [PMID:11459669]
ChEMBL Agonist activity at human GHS-R1 F 8.87 pEC50 1.35 nM EC50 Bioorg Med Chem (2007) 15: 3054-3064 [PMID:17329109]
ChEMBL Agonist activity at human GHS-R1 F 8.89 pEC50 1.3 nM EC50 Bioorg Med Chem (2007) 15: 3054-3064 [PMID:17329109]
ChEMBL Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis F 9.4 pEC50 0.4 nM EC50 J Med Chem (2018) 61: 5974-5987 [PMID:29909635]
ChEMBL Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis F 9.4 pEC50 0.4 nM EC50 J Med Chem (2018) 61: 5974-5987 [PMID:29909635]
ChEMBL Agonist activity at GHSR (unknown origin) B 9.7 pEC50 0.2 nM EC50 J Med Chem (2013) 56: 1197-1210 [PMID:23281966]
GtoPdb - - 9.72 pEC50 0.19 nM EC50 Mol Endocrinol (2005) 19: 2400-11 [PMID:15905359];
Eur J Endocrinol (1999) 141: 180-9 [PMID:10427162]
ghrelin receptor/Ghrelin receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3278] [GtoPdb: 246] [UniProtKB: O08725]
ChEMBL In vitro growth hormone release was determined in rat pituitary cell assay F 8.89 pEC50 1.3 nM EC50 Bioorg Med Chem Lett (1998) 8: 107-112 [PMID:9925440]

ChEMBL data shown on this page come from version 32:

Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]