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 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]