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ChEMBL ligand: CHEMBL108335 (EP-23905, Examorelin, Hexarelin, MF-6003) |
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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] | ||||||||
GtoPdb | - | - | 7.89 | pKd | 13 | nM | Kd | J Clin Endocrinol Metab (2000) 85: 3803-7 [PMID:11061542] |
ChEMBL | Binding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligand | B | 7.74 | pIC50 | 18 | nM | IC50 | J Med Chem (2003) 46: 1191-1203 [PMID:12646029] |
ChEMBL | Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method | B | 7.8 | pIC50 | 15.9 | nM | IC50 | J Med Chem (2012) 55: 6502-6511 [PMID:22712585] |
Platelet glycoprotein 4 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2163174] [UniProtKB: Q07969] | ||||||||
ChEMBL | Displacement of photoactivatable [125I]-Tyr-Bpa-Ala-hexarelin from CD36 in Sprague-Dawley rat cardiac membranes incubated for 60 mins and followed by UV irradiation and measured after 15 mins by radioligand binding assay | B | 5.53 | pIC50 | 2970 | nM | IC50 | US-20130203686-A1. Azapeptides as cd36 binding compounds (null) |
ChEMBL | Displacement of photoactivatable [125I]-Tyr-Bpa-Ala-Hexarelin from CD36 in Sprague-Dawley rat cardiac membranes incubated for 60 mins by densitometry | B | 5.68 | pIC50 | 2080 | nM | IC50 | J Med Chem (2012) 55: 6502-6511 [PMID:22712585] |
ChEMBL | Inhibition of photoactivatable [125I]-Tyr-Bpa-Ala-hexarelin binding to CD36 in Sprague-Dawley rat heart membranes after 60 mins by SDS-PAGE analysis | B | 5.81 | pIC50 | 1560 | nM | IC50 | J Med Chem (2017) 60: 9263-9274 [PMID:29028172] |
ChEMBL | Displacement of [125]-Tyr-Bpa-Ala-Hexarelin from CD36 in Sprague-Dawley rat heart membranes incubated for 60 mins | B | 6.3 | pIC50 | 500 | nM | IC50 | WO-2018000079-A1. Novel cyclic peptides and uses thereof (null) |
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]