DEPX [Ligand Id: 445] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL11348 |
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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 | Antagonist activity at human A1 adenosine receptor | B | 6 | pIC50 | 1000 | nM | IC50 | J Med Chem (2021) 64: 7156-7178 [PMID:34019396] |
| Adenosine A1 receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4975] [UniProtKB: P28190] | ||||||||
| ChEMBL | Binding affinity against bovine brain adenosine A1 receptor by using N6-[3H]- cyclohexyladenosine | B | 8.52 | pIC50 | 3 | nM | IC50 | J Med Chem (1985) 28: 1071-1079 [PMID:2991519] |
| A1 receptor/Adenosine A1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL318] [GtoPdb: 18] [UniProtKB: P25099] | ||||||||
| ChEMBL | Inhibition of [3H]- PIA binding at adenosine A1 receptor on rat cerebral cortex membranes. | B | 7.19 | pKi | 65 | nM | Ki | J Med Chem (1987) 30: 211-214 [PMID:3806597] |
| ChEMBL | Inhibition of binding of 1 nM [3H]N-6-(phenylisopropyl)adenosine to adenosine A1 receptor in rat cortical membranes | B | 7.35 | pKi | 44.5 | nM | Ki | J Med Chem (1989) 32: 1873-1879 [PMID:2754711] |
| ChEMBL | Binding affinity against Adenosine A1 receptor in rat brain membrane, using [3H]N6-cyclohexyladenosine as the radioligand | B | 7.36 | pKi | 44 | nM | Ki | J Med Chem (1989) 32: 2247-2254 [PMID:2795597] |
| ChEMBL | Binding affinity to adenosine A1 receptor of rat brain membranes without NaCl by inhibition of [125-I]-labeled aminobenzyl adenosine binding | B | 7.32 | pIC50 | 48 | nM | IC50 | J Med Chem (1988) 31: 745-751 [PMID:3351850] |
| ChEMBL | Binding affinity towards adenosine A1 receptor of rat brain membranes with 1 M NaCl by inhibition of [125-I]-labeled aminobenzyl adenosine binding | B | 7.49 | pIC50 | 32 | nM | IC50 | J Med Chem (1988) 31: 745-751 [PMID:3351850] |
| A2B receptor/Adenosine A2b receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL255] [GtoPdb: 20] [UniProtKB: P29275] | ||||||||
| ChEMBL | Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand | B | 7.21 | pKi | 62 | nM | Ki | J Med Chem (2002) 45: 2131-2138 [PMID:12014951] |
| GtoPdb | - | - | 7.9 | pKi | - | - | - | Mol Pharmacol (1999) 56: 705-13 [PMID:10496952] |
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]
