MRS1523 [Ligand Id: 474] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL111545 (MRS-1523) |
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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 | - | - | 5 | pKi | >10000 | nM | Ki | . A3 Adenosine Receptors from Cell Biology to Pharmacology and Therapeutics (2010) |
| ChEMBL | Displacement of [3H]CCPA from human adenosine receptor A1 expressed in CHO cell membranes incubated for 90 mins by radioligand competition assay | B | 5 | pKi | >10000 | nM | Ki | Eur J Med Chem (2020) 186: 111879-111879 [PMID:31780082] |
| A1 receptor/Adenosine A1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL318] [GtoPdb: 18] [UniProtKB: P25099] | ||||||||
| ChEMBL | Displacement of specific [3H]-CGS- 21680R-PIA binding to Adenosine A1 receptor in rat brain membranes. | B | 4.81 | pKi | 15600 | nM | Ki | J Med Chem (1999) 42: 706-721 [PMID:10052977] |
| ChEMBL | Displacement of [3H]CCPA from adenosine receptor A1 in rat brain cortex membranes incubated for 90 mins by radioligand competition assay | B | 4.81 | pKi | 15600 | nM | Ki | Eur J Med Chem (2020) 186: 111879-111879 [PMID:31780082] |
| GtoPdb | - | - | 4.81 | pKi | 15600 | nM | Ki | . A3 Adenosine Receptors from Cell Biology to Pharmacology and Therapeutics (2010) |
| A2A receptor/Adenosine A2a receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL251] [GtoPdb: 19] [UniProtKB: P29274] | ||||||||
| ChEMBL | Displacement of [3H]MSX2 from human adenosine receptor A2A expressed in HEK293 cell membranes incubated for 30 mins by radioligand competition assay | B | 5.44 | pKi | 3660 | nM | Ki | Eur J Med Chem (2020) 186: 111879-111879 [PMID:31780082] |
| GtoPdb | - | - | 5.44 | pKi | 3660 | nM | Ki | . A3 Adenosine Receptors from Cell Biology to Pharmacology and Therapeutics (2010) |
| A2A receptor/Adenosine A2a receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL302] [GtoPdb: 19] [UniProtKB: P30543] | ||||||||
| ChEMBL | Displacement of [3H]MSX2 from adenosine receptor A2A in rat brain striatum membranes incubated for 30 mins by radioligand competition assay | B | 5.68 | pKi | 2100 | nM | Ki | Eur J Med Chem (2020) 186: 111879-111879 [PMID:31780082] |
| ChEMBL | Inhibition of [3H]-CGS- 21680 binding to Adenosine A2A receptor in rat striatal membranes. | B | 5.69 | pKi | 2050 | nM | Ki | J Med Chem (1999) 42: 706-721 [PMID:10052977] |
| GtoPdb | - | - | 5.69 | pKi | 2050 | nM | Ki | . A3 Adenosine Receptors from Cell Biology to Pharmacology and Therapeutics (2010) |
| A2B receptor/Adenosine A2b receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL255] [GtoPdb: 20] [UniProtKB: P29275] | ||||||||
| GtoPdb | - | - | 5 | pKi | >10000 | nM | Ki | . A3 Adenosine Receptors from Cell Biology to Pharmacology and Therapeutics (2010) |
| ChEMBL | Displacement of [3H]PSB-603 from human adenosine receptor A2B expressed in CHO cell membranes incubated for 75 mins by radioligand competition assay | B | 5 | pKi | >10000 | nM | Ki | Eur J Med Chem (2020) 186: 111879-111879 [PMID:31780082] |
| A2B receptor in Mouse [GtoPdb: 20] [UniProtKB: Q60614] | ||||||||
| GtoPdb | - | - | 5 | pKi | >10000 | nM | Ki | . A3 Adenosine Receptors from Cell Biology to Pharmacology and Therapeutics (2010) |
| A3 receptor/Adenosine A3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL256] [GtoPdb: 21] [UniProtKB: P0DMS8] | ||||||||
| ChEMBL | Binding affinity towards Adenosine A3 receptor (W243 mutant receptor) | B | 5.67 | pKi | 2150 | nM | Ki | J Med Chem (2002) 45: 4471-4484 [PMID:12238926] |
| ChEMBL | Binding affinity towards human Adenosine A3 receptor wild type | B | 6.62 | pKi | 238 | nM | Ki | J Med Chem (2002) 45: 4471-4484 [PMID:12238926] |
| ChEMBL | Displacement of [125I]I-AB-MECA from human adenosine A3 receptor expressed in HEK293 cells incubated for 60 mins by radioligand binding assay | B | 7.36 | pKi | 43.9 | nM | Ki | ACS Med Chem Lett (2022) 13: 623-631 [PMID:35450351] |
| GtoPdb | - | - | 7.7 | pKi | 19.9 | nM | Ki | J Med Chem (1998) 41: 3186-201 [PMID:9703464] |
| ChEMBL | Displacement of specific [125 I]AB-MECA binding at human Adenosine A3 receptor expressed in HEK cells | B | 7.72 | pKi | 7.72 | uM | Log Ki | J Med Chem (1999) 42: 706-721 [PMID:10052977] |
| ChEMBL | Displacement of specific [125 I]AB-MECA binding at human Adenosine A3 receptor expressed in HEK cells | B | 7.72 | pKi | 18.9 | nM | Ki | J Med Chem (1999) 42: 706-721 [PMID:10052977] |
| ChEMBL | Displacement of [3H]PSB-11 from human adenosine receptor A3 expressed in CHO cell membranes incubated for 60 mins by radioligand competition assay | B | 7.72 | pKi | 18.9 | nM | Ki | Eur J Med Chem (2020) 186: 111879-111879 [PMID:31780082] |
| A3 receptor/Adenosine A3 receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075269] [GtoPdb: 21] [UniProtKB: Q61618] | ||||||||
| GtoPdb | - | - | 6.14 | pKi | 731 | nM | Ki | . A3 Adenosine Receptors from Cell Biology to Pharmacology and Therapeutics (2010) |
| ChEMBL | Displacement of [125I]I-AB-MECA from mouse adenosine A3 receptor expressed in HEK293 cells incubated for 60 mins by radioligand binding assay | B | 6.46 | pKi | 349 | nM | Ki | ACS Med Chem Lett (2022) 13: 623-631 [PMID:35450351] |
| A3 receptor/Adenosine A3 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3360] [GtoPdb: 21] [UniProtKB: P28647] | ||||||||
| ChEMBL | Binding affinity of adenosine derivative for endogenous rat Adenosine A3 receptor of RBL-2H3 | B | 6.45 | pKi | 357 | nM | Ki | J Med Chem (2002) 45: 4471-4484 [PMID:12238926] |
| ChEMBL | Binding affinity of adenosine derivative for endogenous rat Adenosine A3 receptor expressed on CHO cell | B | 6.63 | pKi | 234 | nM | Ki | J Med Chem (2002) 45: 4471-4484 [PMID:12238926] |
| ChEMBL | Displacement of [125I]I-AB-MECA from rat adenosine A3 receptor expressed in HEK293 cells incubated for 60 mins by radioligand binding assay | B | 6.67 | pKi | 216 | nM | Ki | ACS Med Chem Lett (2022) 13: 623-631 [PMID:35450351] |
| ChEMBL | Displacement of specific [125I]AB-MECA binding at rat Adenosine A3 receptor stably expressed in CHO cells | B | 6.95 | pKi | 113 | nM | Ki | J Med Chem (1999) 42: 706-721 [PMID:10052977] |
| ChEMBL | Displacement of [3H]NECA from rat adenosine receptor A3 expressed in CHO cell membranes incubated for 60 mins by radioligand competition assay | B | 6.95 | pKi | 113 | nM | Ki | Eur J Med Chem (2020) 186: 111879-111879 [PMID:31780082] |
| GtoPdb | - | - | 6.95 | pKi | 113 | nM | Ki | . A3 Adenosine Receptors from Cell Biology to Pharmacology and Therapeutics (2010) |
| Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364] | ||||||||
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum HB3 after 72 hrs by SYBR green assay | F | 4.8 | pIC50 | 15848.93 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum 3D7 after 72 hrs by SYBR green assay | F | 4.9 | pIC50 | 12589.25 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum 7G8 after 72 hrs by SYBR green assay | F | 4.9 | pIC50 | 12589.25 | 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 | 4.9 | pIC50 | 12589.25 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum GB4 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 | pIC50 | 10000 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| Transmembrane domain-containing protein TMIGD3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3712907] [UniProtKB: P0DMS9] | ||||||||
| ChEMBL | Antagonist activity at adenosine A3 receptor in human NPE cells assessed as inhibition of adenosine-triggered cell shrinkage | B | 7.72 | pKi | 19 | nM | Ki | J Med Chem (2016) 59: 788-809 [PMID:26356532] |
ChEMBL data shown on this page come from version 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]
