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ChEMBL ligand: CHEMBL16997 |
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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 | Antagonist activity against recombinant human adenosine A1 receptor expressed in HEK293 cells in presence of [125I]IABA radioligand. | F | 6.85 | pKi | 140 | nM | Ki | J Med Chem (2000) 43: 1165-1172 [PMID:10737749] |
A1 receptor/Adenosine A1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL318] [GtoPdb: 18] [UniProtKB: P25099] | ||||||||
ChEMBL | Antagonist activity against adenosine A1 receptor in rat brain membrane in presence of [3H]R-PIA radioligand. | F | 7.82 | pKi | 15 | nM | Ki | J Med Chem (2000) 43: 1165-1172 [PMID:10737749] |
ChEMBL | Displacement of [3H]PIA from adenosine A1 receptors of rat brain membrane | B | 7.82 | pKi | 15 | nM | Ki | J Med Chem (1994) 37: 3373-3382 [PMID:7932565] |
ChEMBL | Inhibition of [3H]CCPA binding to rat adenosine A1 receptor | B | 7.82 | pKi | 15 | nM | Ki | J Med Chem (2002) 45: 1500-1510 [PMID:11906291] |
A2A receptor/Adenosine A2a receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL251] [GtoPdb: 19] [UniProtKB: P29274] | ||||||||
ChEMBL | Antagonist activity against recombinant human adenosine A2A receptor expressed in HEK293 cells in presence of [125I]iodo-ZM-241385 radioligand. | F | 6.72 | pKi | 190 | nM | Ki | J Med Chem (2000) 43: 1165-1172 [PMID:10737749] |
A2A receptor/Adenosine A2a receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL302] [GtoPdb: 19] [UniProtKB: P30543] | ||||||||
ChEMBL | Antagonist activity against adenosine A2A receptor in rat striatal membrane in presence of [3H]CGS-21680 radioligand. | F | 6.1 | pKi | 800 | nM | Ki | J Med Chem (2000) 43: 1165-1172 [PMID:10737749] |
ChEMBL | Displacement of [3H]-CGS- 21680 from adenosine A2a receptors of rat striatal membrane | B | 6.1 | pKi | 800 | nM | Ki | J Med Chem (1994) 37: 3373-3382 [PMID:7932565] |
ChEMBL | Inhibition of [3H]MSX-2 binding to rat adenosine A2A receptor | B | 6.1 | pKi | 800 | nM | Ki | J Med Chem (2002) 45: 1500-1510 [PMID:11906291] |
A2B receptor/Adenosine A2b receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL255] [GtoPdb: 20] [UniProtKB: P29275] | ||||||||
ChEMBL | Antagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPX | F | 7.22 | pKi | 60 | nM | Ki | J Med Chem (2000) 43: 1165-1172 [PMID:10737749] |
ChEMBL | Inhibition of [3H]ZM-241385 binding to human adenosine A2B receptor | B | 7.22 | pKi | 60 | nM | Ki | J Med Chem (2002) 45: 1500-1510 [PMID:11906291] |
GtoPdb | - | - | 7.3 | pKi | - | - | - | Mol Pharmacol (1999) 56: 705-13 [PMID:10496952] |
A3 receptor/Adenosine A3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL256] [GtoPdb: 21] [UniProtKB: P0DMS8] | ||||||||
GtoPdb | - | - | 7.3 | pKi | - | - | - | Proc Natl Acad Sci USA (1993) 90: 10365-9 [PMID:8234299] |
ChEMBL | Antagonist activity against human adenosine A3 receptor expressed in HEK cells in presence of [125]IAB-MECA or [125I]IABA radioligand. | F | 7.52 | pKi | 30 | nM | Ki | J Med Chem (2000) 43: 1165-1172 [PMID:10737749] |
ChEMBL | Inhibition of [3H]PSB-11 binding to human Adenosine A3 receptor | B | 7.52 | pKi | 30 | nM | Ki | J Med Chem (2002) 45: 1500-1510 [PMID:11906291] |
A3 receptor/Adenosine A3 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3360] [GtoPdb: 21] [UniProtKB: P28647] | ||||||||
ChEMBL | Antagonist activity against rat adenosine A3 receptor using [125I]I-AB-MECA or [125 I]IABA | F | 4.82 | pKi | 15000 | nM | Ki | J Med Chem (2000) 43: 1165-1172 [PMID:10737749] |
ChEMBL | Displacement of [125I]AB-MECA from membranes of CHO cells stably transfected with the rat adenosine A3 receptor cDNA | B | 4.82 | pKi | 15000 | nM | Ki | J Med Chem (1994) 37: 3373-3382 [PMID:7932565] |
GtoPdb | - | - | 7.4 | pKi | - | - | - | J Biol Chem (1994) 269: 24692-8 [PMID:7929142] |
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]