GR79236 [Ligand Id: 3288] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL2163568 (GR-79236) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| A1 receptor/Adenosine A1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL226] [GtoPdb: 18] [UniProtKB: P30542] | ||||||||
| ChEMBL | Agonist activity at Homo sapiens (human) adenosine A1 receptor expressed in CHO cells | B | 7.8 | pKi | 15.85 | nM | Ki | Med Chem Res (2004) 13: 88-98 |
| ChEMBL | Displacement of [3H]DPCPX from recombinant human A1 receptor expressed in CHO cell membranes | B | 8.41 | pKi | 3.89 | nM | Ki | Medchemcomm (2018) 9: 1920-1932 [PMID:30568760] |
| ChEMBL | Agonist activity at human A1AR expressed in HEK293T/17 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 10 mins by luciferase reporter assay | F | 8.23 | pEC50 | 5.9 | nM | EC50 | J Med Chem (2012) 55: 6467-6477 [PMID:22738238] |
| A1 receptor/Adenosine A1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL318] [GtoPdb: 18] [UniProtKB: P25099] | ||||||||
| ChEMBL | Displacement of [3H]DPCPX from rat A1 receptor | B | 8.51 | pKi | 3.1 | nM | Ki | Medchemcomm (2018) 9: 1920-1932 [PMID:30568760] |
| GtoPdb | - | - | 8.51 | pKi | 3.1 | nM | Ki | Nat Rev Drug Discov (2006) 5: 247-64 [PMID:16518376] |
| A2A receptor/Adenosine A2a receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL251] [GtoPdb: 19] [UniProtKB: P29274] | ||||||||
| ChEMBL | Agonist activity at Homo sapiens (human) adenosine A2a receptor expressed in CHO cells | F | 4.6 | pKi | 25118.86 | nM | Ki | Med Chem Res (2004) 13: 88-98 |
| GtoPdb | - | - | 5.89 | pKi | 1300 | nM | Ki | Nat Rev Drug Discov (2006) 5: 247-64 [PMID:16518376] |
| A2B receptor/Adenosine A2b receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL255] [GtoPdb: 20] [UniProtKB: P29275] | ||||||||
| ChEMBL | Agonist activity at Homo sapiens (human) adenosine A2b receptor expressed in CHO cells | B | 4.5 | pKi | 31622.78 | nM | Ki | Med Chem Res (2004) 13: 88-98 |
| A3 receptor/Adenosine A3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL256] [GtoPdb: 21] [UniProtKB: P0DMS8] | ||||||||
| ChEMBL | Agonist activity at Homo sapiens (human) adenosine A3 receptor expressed in CHO cells | B | 5.6 | pKi | 2511.89 | nM | Ki | Med Chem Res (2004) 13: 88-98 |
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]
