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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 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]