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ChEMBL ligand: CHEMBL13817 (Ibutamoren, L-163,191, MK-677) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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 33:
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]