MRS1067 [Ligand Id: 466] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL89093 (MRS-1067)
  • A1 receptor/Adenosine A1 receptor in Human [ChEMBL: CHEMBL226] [GtoPdb: 18] [UniProtKB: P30542]
  • A1 receptor/Adenosine A1 receptor in Rat [ChEMBL: CHEMBL318] [GtoPdb: 18] [UniProtKB: P25099]
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  • A2A receptor/Adenosine A2a receptor in Rat [ChEMBL: CHEMBL302] [GtoPdb: 19] [UniProtKB: P30543]
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  • A3 receptor/Adenosine A3 receptor in Human [ChEMBL: CHEMBL256] [GtoPdb: 21] [UniProtKB: P0DMS8]
  • A3 receptor/Adenosine A3 receptor in Rat [ChEMBL: CHEMBL3360] [GtoPdb: 21] [UniProtKB: P28647]
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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]
ChEMBL Displacement of [3H]CCPA from human recombinant adenosine A1 receptor expressed in CHO cells after 60 mins by gamma counter B 5 pKi >10000 nM Ki J Med Chem (2012) 55: 5676-5703 [PMID:22468757]
A1 receptor/Adenosine A1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL318] [GtoPdb: 18] [UniProtKB: P25099]
ChEMBL Binding affinity for Adenosine A1 receptor from rat cerebral cortex membranes using [3H](R)-PIA B 4 pKi >100000 nM Ki J Med Chem (1996) 39: 4142-4148 [PMID:8863790]
ChEMBL Displacement of specific [3H](R)-PIA binding at adenosine A1 receptor from rat brain membranes. B 4 pKi 100000 nM Ki J Med Chem (1997) 40: 2596-2608 [PMID:9258367]
ChEMBL Displacement of [3H]CCPA from rat adenosine A1 receptor expressed in CHO cells after 60 mins by gamma counter B 5 pKi >10000 nM Ki J Med Chem (2012) 55: 5676-5703 [PMID:22468757]
A2A receptor/Adenosine A2a receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL302] [GtoPdb: 19] [UniProtKB: P30543]
ChEMBL Displacement of specific [3H]-CGS- 21680 binding at Adenosine A2A receptor in rat striatal membranes. B 4 pKi >100000 nM Ki J Med Chem (1997) 40: 2596-2608 [PMID:9258367]
ChEMBL Displacement of [3H]CGS21680 from rat adenosine A2A receptor expressed in CHO cells after 60 mins by gamma counter B 5 pKi >10000 nM Ki J Med Chem (2012) 55: 5676-5703 [PMID:22468757]
ChEMBL Binding affinity for Adenosine A2A receptor from rat striatal membranes using [3H]-CGH 21680 B 7 pIC50 >100 nM IC50 J Med Chem (1996) 39: 4142-4148 [PMID:8863790]
A3 receptor/Adenosine A3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL256] [GtoPdb: 21] [UniProtKB: P0DMS8]
GtoPdb - - 6.2 pKi - - - J Med Chem (1996) 39: 2293-301 [PMID:8691424];
Neuropharmacology (1997) 36: 1157-65 [PMID:9364471]
ChEMBL Displacement of [125I]I-AB-MECA from human recombinant adenosine A3 receptor expressed in CHO cells after 60 mins by gamma counter B 6.25 pKi 561 nM Ki J Med Chem (2012) 55: 5676-5703 [PMID:22468757]
ChEMBL Displacement of specific [125I]AB-MECA binding at human adenosine A3 receptor. B 6.25 pKi 560 nM Ki J Med Chem (1997) 40: 2596-2608 [PMID:9258367]
ChEMBL In vitro binding affinity against human Adenosine A3 receptor B 6.25 pKi 560 nM Ki Bioorg Med Chem Lett (2000) 10: 31-34 [PMID:10636237]
ChEMBL In vitro binding affinity at human Adenosine A3 receptor from HEK293 cells by [125I]AB-MECA displacement. B 9.25 pKi 0.56 nM Ki J Med Chem (1996) 39: 4142-4148 [PMID:8863790]
A3 receptor/Adenosine A3 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3360] [GtoPdb: 21] [UniProtKB: P28647]
ChEMBL Displacement of [125I]I-AB-MECA from human rat adenosine A3 receptor expressed in CHO cells after 60 mins by gamma counter B 5.26 pKi 5500 nM Ki J Med Chem (2012) 55: 5676-5703 [PMID:22468757]

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]