GW803430 [Ligand Id: 4033] activity data from GtoPdb and ChEMBL
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: CHEMBL214957 (GW3430, GW803430) |
|---|
|
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 |
|---|---|---|---|---|---|---|---|---|
| Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809] | ||||||||
| ChEMBL | Displacement of [3H]astemizole from human ERG expressed in HEK293 cells | B | 5.93 | pIC50 | 1170 | nM | IC50 | J Med Chem (2009) 52: 2076-2089 [PMID:19290642] |
| H3 receptor/Histamine H3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL264] [GtoPdb: 264] [UniProtKB: Q9Y5N1] | ||||||||
| ChEMBL | Displacement of [3H]-N-alpha-methylhistamine from human H3R expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting analysis | B | 6.68 | pKi | 208 | nM | Ki | ACS Med Chem Lett (2017) 8: 648-653 [PMID:28626527] |
| MCH1 receptor/Melanin-concentrating hormone receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL344] [GtoPdb: 280] [UniProtKB: Q99705] | ||||||||
| ChEMBL | Displacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cells | B | 8.55 | pKi | 2.8 | nM | Ki | Bioorg Med Chem Lett (2010) 20: 7020-7023 [PMID:20951036] |
| ChEMBL | Antagonist activity at MCH1R expressed in CHO cells assessed as intracellular Ca2+ mobilization after 20 mins by FLIPR assay | F | 7.05 | pIC50 | 89.13 | nM | IC50 | J Med Chem (2009) 52: 2076-2089 [PMID:19290642] |
| ChEMBL | Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as inhibition of MCH-stimulated Ca2+ influx preincubated for 120 mins followed by MCH challenge by FLIPR assay | F | 7.8 | pIC50 | 16 | nM | IC50 | Bioorg Med Chem Lett (2015) 25: 2793-2799 [PMID:26022839] |
| ChEMBL | Antagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assay | F | 9.3 | pIC50 | 0.5 | nM | IC50 | Bioorg Med Chem Lett (2006) 16: 4723-4727 [PMID:16870432] |
| ChEMBL | Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay | F | 9.3 | pIC50 | 0.5 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 6166-6171 [PMID:19773162] |
| GtoPdb | - | - | 9.3 | pIC50 | - | - | - | Bioorg Med Chem Lett (2006) 16: 4723-7 [PMID:16870432] |
| MCH1 receptor/Melanin-concentrating hormone receptor 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075228] [GtoPdb: 280] [UniProtKB: P97639] | ||||||||
| ChEMBL | Antagonist activity at rat MCHR1 | B | 9.47 | pKi | 0.34 | nM | Ki | Bioorg Med Chem Lett (2015) 25: 2793-2799 [PMID:26022839] |
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]
