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ChEMBL ligand: CHEMBL185271 (SNAP-7941) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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α1A-adrenoceptor/Alpha-1a adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL229] [GtoPdb: 22] [UniProtKB: P35348] | ||||||||
ChEMBL | Displacement of [125I]HEAT from human recombinant adrenergic alpha-1A receptor | B | 7.4 | pKi | 40 | nM | Ki | J Med Chem (2007) 50: 3883-3890 [PMID:17668922] |
D2 receptor/Dopamine D2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416] | ||||||||
ChEMBL | Displacement of [3H]spiperone from human recombinant dopamine D2 receptor | B | 5.55 | pKi | 2800 | nM | Ki | J Med Chem (2007) 50: 3883-3890 [PMID:17668922] |
MCH1 receptor/Melanin-concentrating hormone receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL344] [GtoPdb: 280] [UniProtKB: Q99705] | ||||||||
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 | 9.24 | pKd | 0.58 | nM | Kd | Bioorg Med Chem Lett (2009) 19: 6166-6171 [PMID:19773162] |
GtoPdb | - | - | 9.7 | pKd | - | - | - | Nat Med (2002) 8: 825-830 [PMID:12118247] |
ChEMBL | Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader | F | 7.82 | pIC50 | 15 | nM | IC50 | Bioorg Med Chem Lett (2004) 14: 4879-4882 [PMID:15341943] |
ChEMBL | Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes | B | 8.52 | pIC50 | 3 | nM | IC50 | Bioorg Med Chem Lett (2004) 14: 4879-4882 [PMID:15341943] |
GtoPdb | - | - | 9.2 | pA2 | - | - | - | Nat Med (2002) 8: 825-830 [PMID:12118247] |
MCH1 receptor/Melanin-concentrating hormone receptor 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075228] [GtoPdb: 280] [UniProtKB: P97639] | ||||||||
ChEMBL | Binding affinity to rat MCH1 receptor | B | 8.7 | pKi | 2 | nM | Ki | J Med Chem (2004) 47: 6864-6874 [PMID:15615535] |
ChEMBL | Displacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cells | B | 9.6 | pKi | 0.25 | nM | Ki | J Med Chem (2007) 50: 3870-3882 [PMID:17668921] |
ChEMBL | Displacement of [3H]T-226296 from rat recombinant MCH1 receptor | B | 9.6 | pKi | 0.25 | nM | Ki | J Med Chem (2007) 50: 3883-3890 [PMID:17668922] |
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]