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ChEMBL ligand: CHEMBL331382 (Metrifudil, TH 322, TH-322) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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A1 receptor/Adenosine A1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL226] [GtoPdb: 18] [UniProtKB: P30542] | ||||||||
ChEMBL | Inhibition of [3H]R-PIA binding to human Adenosine A1 receptor expressed in CHO cells | B | 7.41 | pKi | 39 | nM | Ki | J Med Chem (2005) 48: 1745-1758 [PMID:15771421] |
A1 receptor/Adenosine A1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL318] [GtoPdb: 18] [UniProtKB: P25099] | ||||||||
ChEMBL | Displacement of [3H]R-PIA from adenosine A1 receptor of Wistar rat forebrain | B | 7.01 | pKi | 98 | nM | Ki | J Med Chem (1999) 42: 3463-3477 [PMID:10479279] |
ChEMBL | Binding affinity to adenosine A1 receptor in rat brain membranes by measuring displacement of specific [3H]PIA as radioligand. | B | 7.22 | pKi | 59.6 | nM | Ki | J Med Chem (1995) 38: 1174-1188 [PMID:7707320] |
A2A receptor/Adenosine A2a receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL251] [GtoPdb: 19] [UniProtKB: P29274] | ||||||||
GtoPdb | - | - | 5.5 | pKi | - | - | - | Biochem Pharmacol (1999) 57: 65-75 [PMID:9920286] |
ChEMBL | Inhibition of [3H]-CGS- 21680 binding to human Adenosine A2A receptor expressed in CHO cells | B | 6.12 | pKi | 760 | nM | Ki | J Med Chem (2005) 48: 1745-1758 [PMID:15771421] |
A2A receptor/Adenosine A2a receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL302] [GtoPdb: 19] [UniProtKB: P30543] | ||||||||
ChEMBL | Displacement of [3H]-CGS- 21680 from adenosine A2A receptor of rat striatal tissue | B | 7.6 | pKi | 25 | nM | Ki | J Med Chem (1999) 42: 3463-3477 [PMID:10479279] |
ChEMBL | Binding affinity to adenosine A2A receptor in rat striatal membranes by measuring displacement of specific [3H]-CGS- 21680 as radioligand | B | 7.62 | pKi | 24.1 | nM | Ki | J Med Chem (1995) 38: 1174-1188 [PMID:7707320] |
A3 receptor/Adenosine A3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL256] [GtoPdb: 21] [UniProtKB: P0DMS8] | ||||||||
ChEMBL | Inhibition of [125I]-AB-MECA binding to human Adenosine A3 receptor expressed in CHO cells | B | 7.33 | pKi | 47 | nM | Ki | J Med Chem (2005) 48: 1745-1758 [PMID:15771421] |
A3 receptor/Adenosine A3 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3360] [GtoPdb: 21] [UniProtKB: P28647] | ||||||||
ChEMBL | Binding affinity determined by displacement of specific binding of [125I]N-(4-amino-3-iodophenethyl)-adenosine in membranes of CHO cells stably transfected with the rat adenosine A3 receptor | B | 6.44 | pKi | 360 | nM | Ki | J Med Chem (1995) 38: 1174-1188 [PMID:7707320] |
ChEMBL | Inhibition of [125I]AB-MECA binding to rat Adenosine A3 receptor expressed in CHO cells | B | 7.42 | pKi | 38 | nM | Ki | J Med Chem (2005) 48: 1745-1758 [PMID:15771421] |
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]