Click here for a description of the charts and data table
Please tell us if you are using this feature and what you think!
ChEMBL ligand: CHEMBL376756 (Human metastin 45-54, Kisspeptin-10, Kisspeptin-10 (human)) |
---|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
---|---|---|---|---|---|---|---|---|
kisspeptin receptor/Metastin receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5413] [GtoPdb: 266] [UniProtKB: Q969F8] | ||||||||
ChEMBL | Displacement of [125]metastin from metastin receptor | B | 8.89 | pKi | 1.3 | nM | Ki | J Med Chem (2007) 50: 462-471 [PMID:17266198] |
ChEMBL | Displacement of [125I]-Kp-10 from human Kiss1 receptor by TopCount scintillation counting method | B | 10.21 | pKi | 0.06 | nM | Ki | J Med Chem (2021) 64: 7555-7564 [PMID:34008968] |
GtoPdb | - | - | 10.4 | pKi | - | - | - |
Nature (2001) 411: 613-7 [PMID:11385580]; J Biol Chem (2001) 276: 34631-6 [PMID:11457843] |
ChEMBL | Binding affinity to human KISS1R expressed in CHO cell membranes | B | 10.41 | pKi | 0.04 | nM | Ki | J Med Chem (2013) 56: 8298-8307 [PMID:24047141] |
ChEMBL | Displacement of radioligand from human KISS1R transfected in CHO cells | B | 10.46 | pKi | 0.04 | nM | Ki | J Med Chem (2014) 57: 6105-6115 [PMID:24918545] |
ChEMBL | Inhibition of human KISS1R expressed in CHO cells assessed as inhibition of KISS1R-mediated cell growth after 4 days by cell counting kit-8 assay | B | 5.07 | pIC50 | 8510 | nM | IC50 | J Med Chem (2013) 56: 8298-8307 [PMID:24047141] |
ChEMBL | Displacement of [125I]kisspeptin-15 from GPR54 | B | 9.92 | pIC50 | 0.12 | nM | IC50 | ACS Med Chem Lett (2011) 2: 53-57 [PMID:24900254] |
ChEMBL | Binding affinity to human KISS1R | B | 10.09 | pIC50 | 0.08 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 6391-6396 [PMID:22975302] |
ChEMBL | Displacement of [125I]kisspeptin-15 from human GPR54 expressed in CHO cell membrane | B | 10.15 | pIC50 | 0.07 | nM | IC50 | J Med Chem (2008) 51: 7645-7649 [PMID:19007202] |
ChEMBL | Activity at metastin receptor expressed in HEK293 cells by measuring calcium release | F | 7.76 | pEC50 | 17.3 | nM | EC50 | J Med Chem (2007) 50: 462-471 [PMID:17266198] |
ChEMBL | Agonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay | F | 9.02 | pEC50 | 0.96 | nM | EC50 | J Med Chem (2016) 59: 8804-8811 [PMID:27589480] |
ChEMBL | Agonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay | F | 9.02 | pEC50 | 0.96 | nM | EC50 | J Med Chem (2014) 57: 6105-6115 [PMID:24918545] |
ChEMBL | Agonist activity at human GPR54 expressed in CHO cells assessed as effect on kisspeptin-10-induced response by FLIPR assay | F | 9.62 | pEC50 | 0.24 | nM | EC50 | J Med Chem (2008) 51: 7645-7649 [PMID:19007202] |
ChEMBL | Agonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assay | F | 10.06 | pEC50 | 0.09 | nM | EC50 | Bioorg Med Chem Lett (2019) 29: 654-658 [PMID:30598349] |
ChEMBL | Agonist activity at human OT7T175 assessed as increase in intracellular calcium level by FLIPR assay | F | 10.19 | pEC50 | 0.07 | nM | EC50 | Bioorg Med Chem Lett (2012) 22: 6328-6332 [PMID:22995619] |
ChEMBL | Agonist activity at human KISS1R assessed as induction of intracellular calcium mobilization by fluorometric analysis | F | 10.31 | pEC50 | 0.05 | nM | EC50 | Bioorg Med Chem Lett (2012) 22: 6391-6396 [PMID:22975302] |
kisspeptin receptor/Metastin receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1169599] [GtoPdb: 266] [UniProtKB: Q924U1] | ||||||||
GtoPdb | - | - | 8.8 | pKi | - | - | - | J Biol Chem (2001) 276: 34631-6 [PMID:11457843] |
ChEMBL | Displacement of radioligand from rat KISS1R transfected in CHO cells | B | 10.06 | pKi | 0.09 | nM | Ki | J Med Chem (2014) 57: 6105-6115 [PMID:24918545] |
ChEMBL | Binding affinity to rat KISS1R | B | 10.24 | pKi | 0.06 | nM | Ki | J Med Chem (2013) 56: 8298-8307 [PMID:24047141] |
ChEMBL | Binding affinity to rat KISS1R | B | 9.96 | pIC50 | 0.11 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 6391-6396 [PMID:22975302] |
ChEMBL | Agonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay | F | 8.38 | pEC50 | 4.2 | nM | EC50 | J Med Chem (2014) 57: 6105-6115 [PMID:24918545] |
ChEMBL | Agonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay | F | 8.38 | pEC50 | 4.2 | nM | EC50 | J Med Chem (2016) 59: 8804-8811 [PMID:27589480] |
NPFF1 receptor/Neuropeptide FF receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5951] [GtoPdb: 300] [UniProtKB: Q9GZQ6] | ||||||||
ChEMBL | Displacement of (D-[125I]Tyr1, MePhe3)-NPFF from NPFFR1 after 2 hrs | B | 8.33 | pIC50 | 4.7 | nM | IC50 | ACS Med Chem Lett (2011) 2: 53-57 [PMID:24900254] |
NPFF2 receptor/Neuropeptide FF receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5952] [GtoPdb: 301] [UniProtKB: Q9Y5X5] | ||||||||
ChEMBL | Displacement of (D-[125I]Tyr1, MePhe3)-NPFF from NPFFR2 after 2 hrs | B | 7.12 | pIC50 | 76 | nM | IC50 | ACS Med Chem Lett (2011) 2: 53-57 [PMID:24900254] |
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]