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ChEMBL ligand: CHEMBL483688 |
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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 | Displacement of [3H]CCPA from human adenosine A1 receptor expressed in CHO cells | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2009) 52: 3994-4006 [PMID:19569717] |
A1 receptor/Adenosine A1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL318] [GtoPdb: 18] [UniProtKB: P25099] | ||||||||
ChEMBL | Displacement of [3H]CCPA from rat brain cortex adenosine A1 receptor | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2009) 52: 3994-4006 [PMID:19569717] |
A2A receptor/Adenosine A2a receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL251] [GtoPdb: 19] [UniProtKB: P29274] | ||||||||
ChEMBL | Displacement of [3H]MSX-2 from human recombinant adenosine A2A receptor expressed in CHO cells | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2009) 52: 3994-4006 [PMID:19569717] |
ChEMBL | Antagonist activity at adenosine A2A receptor (unknown origin) | F | 9.26 | pKi | 0.55 | nM | Ki | Eur J Med Chem (2022) 227: 113907-113907 [PMID:34695776] |
A2A receptor/Adenosine A2a receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL302] [GtoPdb: 19] [UniProtKB: P30543] | ||||||||
ChEMBL | Displacement of [3H]MSX-2 from rat brain striatum adenosine A2A receptor | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2009) 52: 3994-4006 [PMID:19569717] |
A2B receptor/Adenosine A2b receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL255] [GtoPdb: 20] [UniProtKB: P29275] | ||||||||
ChEMBL | Binding affinity to human recombinant adenosine A2B receptor expressed in CHO cells by kinetic experiment | B | 9.19 | pKd | 0.65 | nM | Kd | J Med Chem (2009) 52: 3994-4006 [PMID:19569717] |
ChEMBL | Binding affinity to human recombinant adenosine A2B receptor expressed in CHO cells by saturation experiment | B | 9.39 | pKd | 0.4 | nM | Kd | J Med Chem (2009) 52: 3994-4006 [PMID:19569717] |
GtoPdb | - | - | 9.4 | pKd | - | - | - | J Med Chem (2009) 52: 3994-4006 [PMID:19569717] |
ChEMBL | Antagonist activity at human adenosine A2B receptor expressed in Flp-In-CHO cell membrane assessed as inhibition of NECA-induced cAMP accumulation in presence of forskolin measured after 40 mins by alpha screen LANCE assay | F | 8.89 | pKi | 1.3 | nM | Ki | J Med Chem (2021) 64: 8161-8178 [PMID:34120444] |
ChEMBL | Displacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells | B | 9.26 | pKi | 0.55 | nM | Ki | J Med Chem (2009) 52: 3994-4006 [PMID:19569717] |
ChEMBL | Antagonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-induced cAMP accumulation preincubated for 1 hr followed by NECA induction measured after 5 mins in presence of [3H]cAMP and bovine cAMP-binding protein by liquid scintillation counting method | F | 7.74 | pIC50 | 18.3 | nM | IC50 | J Med Chem (2018) 61: 4301-4316 [PMID:29681156] |
ChEMBL | Antagonist activity at adenosine A2B receptor in human Jurkat T cells assessed as inhibition of NECA-induced increase in intracellular calcium concentration by fluorimetric measurement in presence of MSX-2 | F | 8.95 | pIC50 | 1.13 | nM | IC50 | J Med Chem (2009) 52: 3994-4006 [PMID:19569717] |
ChEMBL | Displacement of PSB-12105 from recombinant human adenosine A2B receptor expressed in CHO cell membranes preincubated for 30 mins followed by PSB-12105 addition measured after 20 mins by flow cytometric method | B | 9.13 | pIC50 | 0.74 | nM | IC50 | J Med Chem (2018) 61: 4301-4316 [PMID:29681156] |
ChEMBL | Displacement of PSB-12105 from recombinant human adenosine A2B receptor expressed in CHO cell membranes after 60 mins by flow cytometric method | B | 9.27 | pIC50 | 0.53 | nM | IC50 | J Med Chem (2018) 61: 4301-4316 [PMID:29681156] |
A2B receptor/Adenosine A2b receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2237] [GtoPdb: 20] [UniProtKB: Q60614] | ||||||||
ChEMBL | Displacement of [3H]PSB-603 from mouse recombinant adenosine A2B receptor expressed in CHO cells | B | 9.45 | pKd | 0.35 | nM | Kd | J Med Chem (2009) 52: 3994-4006 [PMID:19569717] |
GtoPdb | - | - | 9.5 | pKd | - | - | - | J Med Chem (2009) 52: 3994-4006 [PMID:19569717] |
A3 receptor/Adenosine A3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL256] [GtoPdb: 21] [UniProtKB: P0DMS8] | ||||||||
ChEMBL | Displacement of [3H]PSB-11 from human recombinant adenosine A3 receptor expressed in CHO cells | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2009) 52: 3994-4006 [PMID:19569717] |
ChEMBL | Displacement of [3H]PSB-11 from recombinant human adenosine A3 receptor expressed in CHO cell membranes after 180 mins by liquid scintillation counting method | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2018) 61: 4301-4316 [PMID:29681156] |
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]