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 34:
Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
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]
