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 34:

Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
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]