Click here for a description of the charts and data table
Please tell us if you are using this feature and what you think!
ChEMBL ligand: CHEMBL483688 |
---|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
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] | ||||||||
GtoPdb | - | - | 5 | pKi | >10000 | nM | Ki | J Med Chem (2009) 52: 3994-4006 [PMID:19569717] |
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] | ||||||||
GtoPdb | - | - | 5 | pKi | >10000 | nM | Ki | J Med Chem (2009) 52: 3994-4006 [PMID:19569717] |
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] | ||||||||
GtoPdb | - | - | 5 | pKi | >10000 | nM | Ki | J Med Chem (2009) 52: 3994-4006 [PMID:19569717] |
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] |
A2A receptor/Adenosine A2a receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL302] [GtoPdb: 19] [UniProtKB: P30543] | ||||||||
GtoPdb | - | - | 5 | pKi | >10000 | nM | Ki | J Med Chem (2009) 52: 3994-4006 [PMID:19569717] |
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] |
GtoPdb | - | - | 9.39 | pKd | 0.4 | 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] |
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] |
GtoPdb | - | - | 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] | ||||||||
GtoPdb | - | - | 9.45 | pKd | 0.35 | nM | Kd | J Med Chem (2009) 52: 3994-4006 [PMID:19569717] |
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] |
A3 receptor/Adenosine A3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL256] [GtoPdb: 21] [UniProtKB: P0DMS8] | ||||||||
GtoPdb | - | - | 5 | pKi | >10000 | nM | Ki | J Med Chem (2009) 52: 3994-4006 [PMID:19569717] |
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 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]