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ChEMBL ligand: CHEMBL1256672 (CV-1808) |
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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 Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL318] [GtoPdb: 18] [UniProtKB: P25099] | ||||||||
ChEMBL | Binding affinity against adenosine A1 receptor in rat brain membranes using [3H]CHA as radioligand | B | 6.11 | pKi | 780 | nM | Ki | J Med Chem (1992) 35: 241-252 [PMID:1732541] |
ChEMBL | Adenosine A1 receptor binding was measured in adenosine deaminase (ADA) pretreated rat cortical membranes using [3H]cyclohexyladenosine in the presence of 2-chloroadenosine | B | 6.16 | pKi | 689 | nM | Ki | J Med Chem (1990) 33: 1919-1924 [PMID:2362269] |
ChEMBL | Binding affinity at adenosine A1 receptor from rat brain membranes by [3H]N6-cyclohexyladenosine displacement. | B | 6.22 | pKi | 600 | nM | Ki | J Med Chem (1988) 31: 1282-1285 [PMID:3385722] |
ChEMBL | Inhibition of binding of [3H]N6-cyclohexyladenosine to adenosine A1 receptor of rat whole brain membranes. | B | 6.22 | pKi | 600 | nM | Ki | J Med Chem (1989) 32: 1667-1673 [PMID:2754691] |
ChEMBL | Binding affinity towards adenosine A1 receptor on rat whole brain membrane using [3H]N6-cyclohexyladenosine | B | 6.23 | pKi | 590 | nM | Ki | J Med Chem (1988) 31: 271-273 [PMID:3336027] |
ChEMBL | Binding affinity against adenosine A1 receptor using [3H]-CHA or [3H]PIA as radioligand | B | 6.25 | pKi | 560 | nM | Ki | J Med Chem (1992) 35: 407-422 [PMID:1738138] |
ChEMBL | Binding affinity against adenosine A1 receptor from rat brain membranes using [3H]cyclohexyladenosine as radioligand. | B | 6.28 | pKi | 529 | nM | Ki | J Med Chem (1992) 35: 2881-2890 [PMID:1495019] |
ChEMBL | Binding affinity to rat recombinant adenosine A1 receptor | B | 6.4 | pKi | 400 | nM | Ki | J Med Chem (2014) 57: 3623-3650 [PMID:24164628] |
ChEMBL | Concentration required for 50% inhibition of [3H]-CHA binding on rat brain adenosine A1 receptor | B | 5.86 | pIC50 | 1380 | nM | IC50 | J Med Chem (1991) 34: 2570-2579 [PMID:1875349] |
Adenosine A1 receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2304404] [UniProtKB: P47745] | ||||||||
ChEMBL | Prolongation of the stimulus-QRS interval by 50% of the maximum response at the adenosine A1 receptor in langendorff guinea pig heart preparation | F | 4.9 | pEC50 | 12589.25 | nM | EC50 | J Med Chem (1991) 34: 1334-1339 [PMID:2016707] |
A2A receptor/Adenosine A2a receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL251] [GtoPdb: 19] [UniProtKB: P29274] | ||||||||
ChEMBL | Binding affinity to human wild type adenosine A2A receptor expressed in Expi293F cells assessed as dissociation constant by surface plasmon resonance assay | B | 8.04 | pKd | 9.1 | nM | Kd | ACS Med Chem Lett (2022) 13: 1172-1181 [PMID:35859869] |
GtoPdb | - | - | 7.1 | pKi | - | - | - |
Biochem Pharmacol (1999) 57: 65-75 [PMID:9920286]; Br J Pharmacol (1997) 121: 353-60 [PMID:9179373] |
ChEMBL | Binding affinity to human wild type adenosine A2A receptor expressed in Expi293F cells assessed as inhibition constant by surface plasmon resonance assay | B | 7.12 | pKi | 76 | nM | Ki | ACS Med Chem Lett (2022) 13: 1172-1181 [PMID:35859869] |
A2A receptor/Adenosine A2a receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL302] [GtoPdb: 19] [UniProtKB: P30543] | ||||||||
ChEMBL | Binding affinity to rat recombinant adenosine receptor A2a | B | 7 | pKi | 100 | nM | Ki | J Med Chem (2014) 57: 3623-3650 [PMID:24164628] |
Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364] | ||||||||
ChEMBL | Antiplasmodial activity against Plasmodium falciparum 3D7 after 72 hrs by SYBR green assay | F | 5 | pIC50 | 10000 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
ChEMBL | Antiplasmodial activity against Plasmodium falciparum D10 after 72 hrs by SYBR green assay | F | 5 | pIC50 | 10000 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
ChEMBL | Antiplasmodial activity against Plasmodium falciparum HB3 after 72 hrs by SYBR green assay | F | 5 | pIC50 | 10000 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
ChEMBL | Antiplasmodial activity against Plasmodium falciparum W2 after 72 hrs by SYBR green assay | F | 5.2 | pIC50 | 6309.57 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
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]