FK-453 [Ligand Id: 5606] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL440115 (Fk453, FK-453)
  • A1 receptor/Adenosine A1 receptor in Human [ChEMBL: CHEMBL226] [GtoPdb: 18] [UniProtKB: P30542]
  • A1 receptor/Adenosine A1 receptor in Mouse [ChEMBL: CHEMBL3688] [GtoPdb: 18] [UniProtKB: Q60612]
  • A1 receptor/Adenosine A1 receptor in Rat [ChEMBL: CHEMBL318] [GtoPdb: 18] [UniProtKB: P25099]
  • Adenosine A1 receptor in Guinea pig [ChEMBL: CHEMBL2304404] [UniProtKB: P47745]
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  • A2A receptor/Adenosine A2a receptor in Human [ChEMBL: CHEMBL251] [GtoPdb: 19] [UniProtKB: P29274]
  • A2A receptor/Adenosine A2a receptor in Rat [ChEMBL: CHEMBL302] [GtoPdb: 19] [UniProtKB: P30543]
  • Adenosine A2a receptor in Guinea pig [ChEMBL: CHEMBL2605] [UniProtKB: P46616]
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  • A2B receptor/Adenosine A2b receptor in Human [ChEMBL: CHEMBL255] [GtoPdb: 20] [UniProtKB: P29275]
  • A2B receptor/Adenosine A2b receptor in Rat [ChEMBL: CHEMBL2592] [GtoPdb: 20] [UniProtKB: P29276]
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  • A3 receptor/Adenosine A3 receptor in Human [ChEMBL: CHEMBL256] [GtoPdb: 21] [UniProtKB: P0DMS8]
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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]
GtoPdb - - 7.74 pKi 18 nM Ki Nat Rev Drug Discov (2006) 5: 247-64 [PMID:16518376]
ChEMBL Binding Affinity towards Adenosine A1 receptor expressed in CHO-K1 cells versus [3H]CCPA B 7.74 pKi 18 nM Ki J. Med. Chem. (2001) 44: 170-179 [PMID:11170626]
ChEMBL Binding affinity to human adenosine A1 receptor B 9.31 pKi 0.49 nM Ki Bioorg. Med. Chem. (2010) 18: 2195-2203 [PMID:20188574]
ChEMBL Adenosine A1 receptor binding using [3H]DPCPX in human cortical membranes B 9.31 pKi 0.49 nM Ki J. Med. Chem. (1999) 42: 779-783 [PMID:10072675]
A1 receptor/Adenosine A1 receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3688] [GtoPdb: 18] [UniProtKB: Q60612]
ChEMBL Binding affinity to mouse adenosine A1 receptor B 9.26 pKi 0.55 nM Ki Bioorg. Med. Chem. (2010) 18: 2195-2203 [PMID:20188574]
A1 receptor/Adenosine A1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL318] [GtoPdb: 18] [UniProtKB: P25099]
ChEMBL Adenosine A1 receptor binding using [3H]DPCOX in rat cortical membranes B 9.31 pKi 0.49 nM Ki J. Med. Chem. (1999) 42: 779-783 [PMID:10072675]
ChEMBL Inhibition of [3H]CHA binding against Adenosine A1 receptors of rat cortical membranes B 5 pIC50 10100 nM IC50 Bioorg. Med. Chem. Lett. (1996) 6: 2059-2062
ChEMBL Inhibitory activity against cyclic AMP production in rat Adenosine A1 receptor assay B 7.76 pIC50 17.2 nM IC50 J. Med. Chem. (2001) 44: 170-179 [PMID:11170626]
ChEMBL Binding affinity to rat adenosine A1 receptor B 7.76 pIC50 17.2 nM IC50 Bioorg. Med. Chem. (2010) 18: 2195-2203 [PMID:20188574]
ChEMBL Inhibitory activity against Adenosine A1 Receptor using [3H]CHA in rat cortical membranes B 7.77 pIC50 17 nM IC50 Bioorg. Med. Chem. Lett. (1999) 9: 1979-1984 [PMID:10450966]
Adenosine A1 receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2304404] [UniProtKB: P47745]
ChEMBL Inhibition of adenosine induced negative inotropic activity against guinea-pig atria (Adenosine A1 receptor) F 5.93 pIC50 1180 nM IC50 Bioorg. Med. Chem. Lett. (1996) 6: 2059-2062
ChEMBL Binding affinity to guinea pig adenosine A1 receptor B 9.25 pIC50 0.56 nM IC50 Bioorg. Med. Chem. (2010) 18: 2195-2203 [PMID:20188574]
A2A receptor/Adenosine A2a receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL251] [GtoPdb: 19] [UniProtKB: P29274]
ChEMBL Binding Affinity for adenosine A2A receptor expressed in HEK293 cells compared to [3H]CGS-21680 B 5.89 pKi 1300 nM Ki J. Med. Chem. (2001) 44: 170-179 [PMID:11170626]
GtoPdb - - 5.89 pKi 1300 nM Ki Nat Rev Drug Discov (2006) 5: 247-64 [PMID:16518376]
ChEMBL Inhibitory activity against cyclic AMP production in rat Adenosine A2A receptor assay B 4.95 pIC50 11300 nM IC50 J. Med. Chem. (2001) 44: 170-179 [PMID:11170626]
A2A receptor/Adenosine A2a receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL302] [GtoPdb: 19] [UniProtKB: P30543]
ChEMBL Binding affinity to rat adenosine A2A receptor B 4.95 pIC50 11300 nM IC50 Bioorg. Med. Chem. (2010) 18: 2195-2203 [PMID:20188574]
ChEMBL Inhibitory activity against Adenosine A2a receptor using [3H]NECA in rat striatal membranes B 4.96 pIC50 11000 nM IC50 Bioorg. Med. Chem. Lett. (1999) 9: 1979-1984 [PMID:10450966]
Adenosine A2a receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2605] [UniProtKB: P46616]
ChEMBL Binding affinity to guinea pig adenosine A2A receptor B 5.93 pIC50 1180 nM IC50 Bioorg. Med. Chem. (2010) 18: 2195-2203 [PMID:20188574]
A2B receptor/Adenosine A2b receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL255] [GtoPdb: 20] [UniProtKB: P29275]
GtoPdb - - 6.01 pKi 980 nM Ki Nat Rev Drug Discov (2006) 5: 247-64 [PMID:16518376]
ChEMBL Inhibitory activity on NECA-induced cyclic-AMP accumulation in CHO-K1 cells expressing human Adenosine A2B receptor F 6.01 pIC50 980 nM IC50 J. Med. Chem. (2001) 44: 170-179 [PMID:11170626]
A2B receptor/Adenosine A2b receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2592] [GtoPdb: 20] [UniProtKB: P29276]
ChEMBL Inhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytes F 5.09 pIC50 8100 nM IC50 J. Med. Chem. (2001) 44: 170-179 [PMID:11170626]
A3 receptor/Adenosine A3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL256] [GtoPdb: 21] [UniProtKB: P0DMS8]
GtoPdb - - 5 pKi 10000 nM Ki Nat Rev Drug Discov (2006) 5: 247-64 [PMID:16518376]
ChEMBL Binding affinity towards adenosine A3 receptor expressed in HEK293 cells versus [125I]AB-MECA B 5.55 pKi 2800 nM Ki J. Med. Chem. (2001) 44: 170-179 [PMID:11170626]

ChEMBL data shown on this page come from version 31:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]