CVT-6883 [Ligand Id: 5615] activity data from GtoPdb and ChEMBL

Click here for a description of the charts and data table

Please tell us if you are using this feature and what you think!

ChEMBL ligand: CHEMBL260933 (CVT-6883, Gs 6201, GS-6201)
  • A1 receptor/Adenosine A1 receptor in Human [ChEMBL: CHEMBL226] [GtoPdb: 18] [UniProtKB: P30542]
There should be some charts here, you may need to enable JavaScript!
  • A2A receptor/Adenosine A2a receptor in Human [ChEMBL: CHEMBL251] [GtoPdb: 19] [UniProtKB: P29274]
There should be some charts here, you may need to enable JavaScript!
  • A2B receptor/Adenosine A2b receptor in Human [ChEMBL: CHEMBL255] [GtoPdb: 20] [UniProtKB: P29275]
There should be some charts here, you may need to enable JavaScript!
  • A3 receptor/Adenosine A3 receptor in Human [ChEMBL: CHEMBL256] [GtoPdb: 21] [UniProtKB: P0DMS8]
There should be some charts here, you may need to enable JavaScript!
  • α1D-adrenoceptor/Alpha-1d adrenergic receptor in Human [ChEMBL: CHEMBL223] [GtoPdb: 24] [UniProtKB: P25100]
There should be some charts here, you may need to enable JavaScript!
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 Binding affinity to human adenosine A1 receptor B 5 pKi >10000 nM Ki J Med Chem (2012) 55: 797-811 [PMID:22148859]
GtoPdb - - 5.71 pKi 1940 nM Ki J Med Chem (2008) 51: 2267-78 [PMID:18321039]
ChEMBL Displacement of [3H]CPX from human recombinant adenosine A1 receptor expressed in CHO cells B 5.71 pKi 1940 nM Ki J Med Chem (2008) 51: 2267-2278 [PMID:18321039]
ChEMBL Binding affinity to human adenosine A1 receptor B 5.71 pKi 1940 nM Ki J Med Chem (2009) 52: 3994-4006 [PMID:19569717]
A2A receptor/Adenosine A2a receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL251] [GtoPdb: 19] [UniProtKB: P29274]
ChEMBL Binding affinity to human adenosine A2A receptor B 5 pKi >10000 nM Ki J Med Chem (2012) 55: 797-811 [PMID:22148859]
GtoPdb - - 5.48 pKi 3280 nM Ki J Med Chem (2008) 51: 2267-78 [PMID:18321039]
ChEMBL Displacement of [3H]ZM-241385 from human recombinant adenosine A2A receptor expressed in HEK293 cells B 5.48 pKi 3280 nM Ki J Med Chem (2008) 51: 2267-2278 [PMID:18321039]
ChEMBL Binding affinity to human adenosine A2A receptor B 5.48 pKi 3280 nM Ki J Med Chem (2009) 52: 3994-4006 [PMID:19569717]
A2B receptor/Adenosine A2b receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL255] [GtoPdb: 20] [UniProtKB: P29275]
ChEMBL Displacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cells B 7.66 pKi 22 nM Ki J Med Chem (2008) 51: 2267-2278 [PMID:18321039]
ChEMBL Binding affinity to human adenosine A2B receptor B 7.66 pKi 22 nM Ki J Med Chem (2009) 52: 3994-4006 [PMID:19569717]
GtoPdb - - 7.66 pKi 22 nM Ki J Med Chem (2008) 51: 2267-78 [PMID:18321039]
ChEMBL Displacement of [125I]-ABOPX from human recombinant adenosine A2B receptor expressed in HEK293 cells B 8.08 pKi 8.3 nM Ki J Med Chem (2012) 55: 797-811 [PMID:22148859]
A3 receptor/Adenosine A3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL256] [GtoPdb: 21] [UniProtKB: P0DMS8]
ChEMBL Binding affinity to human adenosine A3 receptor B 5 pKi >10000 nM Ki J Med Chem (2012) 55: 797-811 [PMID:22148859]
GtoPdb - - 5.97 pKi 1070 nM Ki J Med Chem (2008) 51: 2267-78 [PMID:18321039]
ChEMBL Displacement of [125I]ABMECA from human recombinant adenosine A3 receptor expressed in CHO cells B 5.97 pKi 1070 nM Ki J Med Chem (2008) 51: 2267-2278 [PMID:18321039]
ChEMBL Binding affinity to human adenosine A3 receptor B 5.97 pKi 1070 nM Ki J Med Chem (2009) 52: 3994-4006 [PMID:19569717]
α1D-adrenoceptor/Alpha-1d adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL223] [GtoPdb: 24] [UniProtKB: P25100]
ChEMBL PDSP Secondary Binding target: ADRA1D - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity. B 5 pKi >10000 nM Ki EUbOPEN Chemogenomics Library - PDSP Secondary Binding

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]