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ChEMBL ligand: CHEMBL1625681 |
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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 recombinant adenosine A1 receptor expressed in CHO cells after 60 mins by gamma counter | B | 5.79 | pKi | 1640 | nM | Ki | J Med Chem (2012) 55: 5676-5703 [PMID:22468757] |
ChEMBL | Displacement of [3H]CCPA from human adenosine receptor A1 expressed in CHO cell membranes incubated for 90 mins by radioligand competition assay | B | 5.79 | pKi | 1640 | nM | Ki | Eur J Med Chem (2020) 186: 111879-111879 [PMID:31780082] |
GtoPdb | - | - | 5.79 | pKi | 1640 | nM | Ki | Bioorg Med Chem (2003) 11: 347-56 [PMID:12517430] |
A1 receptor/Adenosine A1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL318] [GtoPdb: 18] [UniProtKB: P25099] | ||||||||
ChEMBL | Binding affinity against Adenosine A1 receptor by displacing [3H]CHA radioligand in rat brain cortical membrane | B | 6.36 | pKi | 440 | nM | Ki | J Med Chem (2002) 45: 3440-3450 [PMID:12139454] |
ChEMBL | Displacement of [3H]CCPA from rat adenosine A1 receptor expressed in CHO cells after 60 mins by gamma counter | B | 6.36 | pKi | 440 | nM | Ki | J Med Chem (2012) 55: 5676-5703 [PMID:22468757] |
ChEMBL | Displacement of [3H]CCPA from adenosine receptor A1 in rat brain cortex membranes incubated for 90 mins by radioligand competition assay | B | 6.36 | pKi | 440 | nM | Ki | Eur J Med Chem (2020) 186: 111879-111879 [PMID:31780082] |
GtoPdb | - | - | 6.36 | pKi | 440 | nM | Ki | Bioorg Med Chem (2003) 11: 347-56 [PMID:12517430] |
A2A receptor/Adenosine A2a receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL251] [GtoPdb: 19] [UniProtKB: P29274] | ||||||||
GtoPdb | - | - | 5.89 | pKi | 1280 | nM | Ki | Bioorg Med Chem (2003) 11: 347-56 [PMID:12517430] |
ChEMBL | Displacement of [3H]CGS21680 from human recombinant adenosine A2A receptor expressed in CHO cells after 60 mins by gamma counter | B | 5.89 | pKi | >1280 | nM | Ki | J Med Chem (2012) 55: 5676-5703 [PMID:22468757] |
ChEMBL | Displacement of [3H]MSX2 from human adenosine receptor A2A expressed in HEK293 cell membranes incubated for 30 mins by radioligand competition assay | B | 6.97 | pKi | 108 | nM | Ki | Eur J Med Chem (2020) 186: 111879-111879 [PMID:31780082] |
A2A receptor/Adenosine A2a receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL302] [GtoPdb: 19] [UniProtKB: P30543] | ||||||||
ChEMBL | Binding affinity to the adenosine A2A receptor by displacement of [3H]CGS-21680 in rat brain striatal membrane | B | 5.68 | pKi | 2100 | nM | Ki | J Med Chem (2002) 45: 3440-3450 [PMID:12139454] |
ChEMBL | Displacement of [3H]CGS21680 from rat adenosine A2A receptor expressed in CHO cells after 60 mins by gamma counter | B | 5.68 | pKi | 2100 | nM | Ki | J Med Chem (2012) 55: 5676-5703 [PMID:22468757] |
ChEMBL | Displacement of [3H]MSX2 from adenosine receptor A2A in rat brain striatum membranes incubated for 30 mins by radioligand competition assay | B | 5.68 | pKi | 2100 | nM | Ki | Eur J Med Chem (2020) 186: 111879-111879 [PMID:31780082] |
GtoPdb | - | - | 5.68 | pKi | 2100 | nM | Ki | Bioorg Med Chem (2003) 11: 347-56 [PMID:12517430] |
A2B receptor/Adenosine A2b receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL255] [GtoPdb: 20] [UniProtKB: P29275] | ||||||||
ChEMBL | Displacement of [3H]PSB-603 from human adenosine receptor A2B expressed in CHO cell membranes incubated for 75 mins by radioligand competition assay | B | 5.43 | pKi | 3700 | nM | Ki | Eur J Med Chem (2020) 186: 111879-111879 [PMID:31780082] |
A2B receptor in Mouse [GtoPdb: 20] [UniProtKB: Q60614] | ||||||||
GtoPdb | - | - | 5.68 | pKi | 2100 | nM | Ki | J Med Chem (2002) 45: 3440-50 [PMID:12139454] |
A3 receptor/Adenosine A3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL256] [GtoPdb: 21] [UniProtKB: P0DMS8] | ||||||||
GtoPdb | - | - | 8.31 | pKd | 4.9 | nM | Kd | Bioorg Med Chem Lett (2002) 12: 501-3 [PMID:11814828] |
ChEMBL | Binding affinity to human adenosine A3 receptor measured by radioligand binding assay | B | 5.45 | pKi | 3510 | nM | Ki | ACS Med Chem Lett (2022) 13: 623-631 [PMID:35450351] |
GtoPdb | - | - | 8.63 | pKi | 2.34 | nM | Ki | Bioorg Med Chem (2003) 11: 347-56 [PMID:12517430] |
ChEMBL | Displacement of [3H]PSB-11 from human adenosine receptor A3 expressed in CHO cell membranes incubated for 60 mins by radioligand competition assay | B | 8.63 | pKi | 2.34 | nM | Ki | Eur J Med Chem (2020) 186: 111879-111879 [PMID:31780082] |
ChEMBL | Antagonist activity at adenosine A3 receptor (unknown origin) | F | 8.63 | pKi | 2.34 | nM | Ki | Eur J Med Chem (2022) 227: 113907-113907 [PMID:34695776] |
ChEMBL | Binding affinity against human recombinant Adenosine A3 receptor stably expressed in HEK293 cells by displacing [125I]AB-MECA radioligand | B | 8.64 | pKi | 2.3 | nM | Ki | J Med Chem (2002) 45: 3440-3450 [PMID:12139454] |
ChEMBL | Binding affinity to human recombinant A3 adenosine receptor by radioligand binding assay | B | 8.64 | pKi | 2.3 | nM | Ki | J Med Chem (2011) 54: 5205-5220 [PMID:21675777] |
ChEMBL | Displacement of [125I]I-AB-MECA from human recombinant adenosine A3 receptor expressed in CHO cells after 60 mins by gamma counter | B | 8.64 | pKi | 2.3 | nM | Ki | J Med Chem (2012) 55: 5676-5703 [PMID:22468757] |
A3 receptor/Adenosine A3 receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075269] [GtoPdb: 21] [UniProtKB: Q61618] | ||||||||
ChEMBL | Binding affinity to mouse adenosine A3 receptor measured by radioligand binding assay | B | 5.2 | pKi | 6360 | nM | Ki | ACS Med Chem Lett (2022) 13: 623-631 [PMID:35450351] |
A3 receptor/Adenosine A3 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3360] [GtoPdb: 21] [UniProtKB: P28647] | ||||||||
ChEMBL | Displacement of [3H]NECA from rat adenosine receptor A3 expressed in CHO cell membranes incubated for 60 mins by radioligand competition assay | B | 5 | pKi | >10000 | nM | Ki | Eur J Med Chem (2020) 186: 111879-111879 [PMID:31780082] |
ChEMBL | Binding affinity to rat adenosine A3 receptor measured by radioligand binding assay | B | 5 | pKi | >10000 | nM | Ki | ACS Med Chem Lett (2022) 13: 623-631 [PMID:35450351] |
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]