Cl-IB-MECA [Ligand Id: 457] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL431733 (Cf102, CF-102, CF102, Chloro-ib-meca, CI-IB-MECA, CL-IB-MECA, Namodenoson) |
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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]R-PLA from human adenosine A1 receptor expressed in CHO cells after 60 mins by liquid scintillation analyzer | B | 5.91 | pKi | 1240 | nM | Ki | J Med Chem (2017) 60: 3422-3437 [PMID:28380296] |
| ChEMBL | Binding affinity for human Adenosine A1 receptor in CHO cells using [3H]N6-(R)-phenylisopropyladenosine | B | 5.91 | pKi | 1240 | nM | Ki | J Med Chem (2003) 46: 3775-3777 [PMID:12930138] |
| ChEMBL | Displacement of [3H]CCPA from recombinant human adenosine A1 receptor expressed in CHO cells | B | 5.91 | pKi | 1240 | nM | Ki | J Med Chem (2004) 47: 4766-4773 [PMID:15341491] |
| ChEMBL | Displacement of [3H]DPCPX from human adenosine A1 receptor expressed in CHO cell membrane after 180 mins | B | 6.05 | pKi | 890 | nM | Ki | Eur J Med Chem (2013) 69: 331-337 [PMID:24077183] |
| ChEMBL | Displacement of [3H]DPDPX from human adenosine A1 receptor expressed in CHO cells | B | 6.05 | pKi | 890 | nM | Ki | J Med Chem (2008) 51: 1764-1770 [PMID:18269230] |
| ChEMBL | Displacement of [3H]DPCPX from human A1 adenosine receptor expressed in CHO cell membrane | B | 6.05 | pKi | 890 | nM | Ki | J Med Chem (2012) 55: 1490-1499 [PMID:22257095] |
| ChEMBL | Displacement of [3H]DPCPX from human adenosine A1 receptor expressed in CHO cells | B | 6.05 | pKi | 890 | nM | Ki | J Med Chem (2007) 50: 5676-5684 [PMID:17927167] |
| ChEMBL | Displacement of [3H]CHA binding to Adenosine A1 receptor expressed in CHO cells | B | 6.08 | pKi | 823 | nM | Ki | J Med Chem (2004) 47: 5535-5540 [PMID:15481989] |
| ChEMBL | Displacement of [3H]CCPA from human adenosine A1 receptor in CHO cells | B | 6.65 | pKi | 222 | nM | Ki | J Med Chem (2007) 50: 3159-3162 [PMID:17555308] |
| ChEMBL | Displacement of [3H]CCPA from human A1 receptor expressed in CHO cell membranes after 60 mins by gamma counting method | B | 6.65 | pKi | 222 | nM | Ki | J Med Chem (2017) 60: 7459-7475 [PMID:28799755] |
| ChEMBL | Displacement of [3H]R-PIA from human adenosine A1 receptor expressed in CHO cells | B | 6.65 | pKi | 222 | nM | Ki | Bioorg Med Chem (2009) 17: 8003-8011 [PMID:19879151] |
| ChEMBL | Displacement of [3H]CCPA from human adenosine A1 receptor expressed in CHO cells | B | 6.65 | pKi | 222 | nM | Ki | Bioorg Med Chem Lett (2008) 18: 1612-1616 [PMID:18255292] |
| ChEMBL | Binding affinity towards recombinant human Adenosine A1 receptor was determined using [3H]R-PIA (2.0 nM) as radioligand | B | 6.65 | pKi | 222 | nM | Ki | Bioorg Med Chem Lett (2004) 14: 4851-4854 [PMID:15341938] |
| ChEMBL | Displacement of [3H]CCPA from human adenosine A1 receptor expressed in CHO cells | B | 6.65 | pKi | 222 | nM | Ki | J Med Chem (2008) 51: 6609-6613 [PMID:18811138] |
| ChEMBL | Displacement of [3H]CCPA form human adenosine A1 receptor expressed in CHO cells | B | 6.65 | pKi | 222 | nM | Ki | Bioorg Med Chem (2008) 16: 8546-8556 [PMID:18752961] |
| ChEMBL | Displacement of [3H]CCPA from human adenosine A1 receptor expressed in CHO cell membranes after 3 hrs by micro beta scintillation counting method | B | 6.66 | pKi | 220 | nM | Ki | Eur J Med Chem (2018) 157: 837-851 [PMID:30144700] |
| ChEMBL | Inhibition of [3H]R-PIA binding to human Adenosine A1 receptor expressed in CHO cells | B | 6.66 | pKi | 220 | nM | Ki | J Med Chem (2005) 48: 1745-1758 [PMID:15771421] |
| ChEMBL | Displacement of radioligand from human adenosine A1 receptor expressed in CHO cells | B | 6.66 | pKi | 220 | nM | Ki | Bioorg Med Chem Lett (2008) 18: 2813-2819 [PMID:18424135] |
| ChEMBL | Displacement of [3H]NECA from human recombinant adenosine A1 receptor expressed in CHO cells by liquid scintillation counting | B | 6.66 | pKi | 220 | nM | Ki | Bioorg Med Chem (2009) 17: 3733-3738 [PMID:19375920] |
| ChEMBL | Displacement of [3H]N6-phenylisopropyladenosine from recombinant human A1AR expressed in CHO cell membranes after 60 mins by liquid scintillation counting method | B | 6.66 | pKi | 220 | nM | Ki | J Med Chem (2016) 59: 11006-11026 [PMID:27933810] |
| GtoPdb | - | - | 6.66 | pKi | 220 | nM | Ki | Nat Rev Drug Discov (2006) 5: 247-64 [PMID:16518376] |
| ChEMBL | Binding affinity using [125I]ABA against human Adenosine A1 receptor | B | 7 | pKi | 99 | nM | Ki | J Med Chem (2003) 46: 353-355 [PMID:12540233] |
| ChEMBL | Displacement of [125I]ABA from human adenosine A1 receptor expressed in HEK cells | B | 8.28 | pKi | 5.26 | nM | Ki | Bioorg Med Chem Lett (2006) 16: 2416-2418 [PMID:16487705] |
| Adenosine A1 receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4975] [UniProtKB: P28190] | ||||||||
| ChEMBL | Displacement of [3H]DPCPX binding to adenosine A1 receptors of bovine cortical membranes | B | 6.05 | pKi | 890 | nM | Ki | J Med Chem (2005) 48: 1550-1562 [PMID:15743197] |
| A1 receptor/Adenosine A1 receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3688] [GtoPdb: 18] [UniProtKB: Q60612] | ||||||||
| ChEMBL | Displacement of [125I]N6-(4-amino-3-iodobenzyl)adenosine-5'-N-methyl-uronamide from mouse recombinant adenosine A1 receptor expressed in HEK293 cells | B | 7.46 | pKi | 35 | nM | Ki | Bioorg Med Chem Lett (2008) 18: 2813-2819 [PMID:18424135] |
| GtoPdb | - | - | 7.46 | pKi | 35 | nM | Ki | . A3 Adenosine Receptors from Cell Biology to Pharmacology and Therapeutics (2010) |
| A1 receptor/Adenosine A1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL318] [GtoPdb: 18] [UniProtKB: P25099] | ||||||||
| ChEMBL | Binding affinity for adenosine A1 receptor as displacement of [3H]R-PIA from rat brain membranes at 10e-4 M | B | 6.09 | pKi | 820 | nM | Ki | J Med Chem (1998) 41: 3186-3201 [PMID:9703464] |
| ChEMBL | Binding affinity for rat Adenosine A1 receptor in CHO cells using [3H]N6-(R)-phenylisopropyladenosine | B | 6.09 | pKi | 820 | nM | Ki | J Med Chem (2003) 46: 3775-3777 [PMID:12930138] |
| ChEMBL | Tested for the binding affinity of A1 receptor by displacing the [3H]-PIA in rat brain membranes | B | 6.09 | pKi | 820 | nM | Ki | J Med Chem (1994) 37: 3614-3621 [PMID:7932588] |
| ChEMBL | Displacement of radioligand from rat adenosine A1 receptor | B | 6.09 | pKi | 820 | nM | Ki | Bioorg Med Chem Lett (2008) 18: 2813-2819 [PMID:18424135] |
| ChEMBL | Displacement of [3H]CCPA from rat adenosine A1 receptor expressed in CHO cells after 60 mins by gamma counter | B | 6.09 | pKi | 820 | nM | Ki | J Med Chem (2012) 55: 5676-5703 [PMID:22468757] |
| GtoPdb | - | - | 6.55 | pKi | 280 | nM | Ki | . A3 Adenosine Receptors from Cell Biology to Pharmacology and Therapeutics (2010) |
| ChEMBL | Binding affinity for adenosine A1 receptor as inhibition of 3[H]-R-PIA binding in rat brain | B | 7.27 | pKi | 54 | nM | Ki | Bioorg Med Chem Lett (1998) 8: 1767-1770 [PMID:9873431] |
| A2A receptor/Adenosine A2a receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL251] [GtoPdb: 19] [UniProtKB: P29274] | ||||||||
| ChEMBL | Inhibition of [3H]-CGS- 21680 binding to human Adenosine A2A receptor expressed in CHO cells | B | 5.27 | pKi | 5400 | nM | Ki | J Med Chem (2005) 48: 1745-1758 [PMID:15771421] |
| ChEMBL | Displacement of [3H]CGS21680 from human recombinant adenosine A2a receptor expressed in HEK293 cells by liquid scintillation counting | B | 5.27 | pKi | 5400 | nM | Ki | Bioorg Med Chem (2009) 17: 3733-3738 [PMID:19375920] |
| ChEMBL | Displacement of [3 H]2-[p-(2-carboxyethyl)phenyl-ethylamino]-5'-N-ethylcarboxamidoadenosine from recombinant human adenosine receptor A2A expressed in HEK293 cell membranes after 60 mins by liquid scintillation counting method | B | 5.27 | pKi | 5400 | nM | Ki | J Med Chem (2016) 59: 11006-11026 [PMID:27933810] |
| ChEMBL | Displacement of radioligand from human adenosine A2A receptor expressed in HEK293 cells | B | 5.27 | pKi | 5400 | nM | Ki | Bioorg Med Chem Lett (2008) 18: 2813-2819 [PMID:18424135] |
| GtoPdb | - | - | 5.27 | pKi | 5360 | nM | Ki | Nat Rev Drug Discov (2006) 5: 247-64 [PMID:16518376] |
| ChEMBL | Displacement of [3H]CGS21680 from human adenosine A2A receptor expressed in HEK293 cells after 60 mins by liquid scintillation analyzer | B | 5.27 | pKi | 5370 | nM | Ki | J Med Chem (2017) 60: 3422-3437 [PMID:28380296] |
| ChEMBL | Displacement of [3H]NECA from human adenosine A2A receptor expressed in CHO cell membranes after 3 hrs by micro beta scintillation counting method | B | 5.27 | pKi | 5360 | nM | Ki | Eur J Med Chem (2018) 157: 837-851 [PMID:30144700] |
| ChEMBL | Binding affinity towards recombinant human Adenosine A2a receptor was determined using [3H]CGS-21680 (10 nM) as radioligand | B | 5.27 | pKi | 5360 | nM | Ki | Bioorg Med Chem Lett (2004) 14: 4851-4854 [PMID:15341938] |
| ChEMBL | Displacement of [3H]CGS-21680 from recombinant human adenosine A2a receptor expressed in HEK cells | B | 5.27 | pKi | 5360 | nM | Ki | J Med Chem (2004) 47: 4766-4773 [PMID:15341491] |
| ChEMBL | Displacement of [3H]CGS21680 from human adenosine A2A receptor expressed in HEK293 cells | B | 5.27 | pKi | 5360 | nM | Ki | J Med Chem (2007) 50: 3159-3162 [PMID:17555308] |
| ChEMBL | Displacement of [3H]CGS-21680 from human adenosine A2A receptor expressed in CHO cells | B | 5.27 | pKi | 5360 | nM | Ki | Bioorg Med Chem Lett (2008) 18: 1612-1616 [PMID:18255292] |
| ChEMBL | Displacement of [3H]CGS-21680 from human adenosine A2A receptor expressed in HEK293 cells | B | 5.27 | pKi | 5360 | nM | Ki | J Med Chem (2008) 51: 6609-6613 [PMID:18811138] |
| ChEMBL | Displacement of [3H]R-PIA form human adenosine A2A receptor expressed in HEK cells | B | 5.27 | pKi | 5360 | nM | Ki | Bioorg Med Chem (2008) 16: 8546-8556 [PMID:18752961] |
| ChEMBL | Displacement of [3H]CGS21680 from human adenosine A2A receptor expressed in CHO cells | B | 5.27 | pKi | 5360 | nM | Ki | Bioorg Med Chem (2009) 17: 8003-8011 [PMID:19879151] |
| ChEMBL | Displacement of [3H]CGS21680 from human adenosine A2A receptor expressed in HEK293 cells after 60 mins by liquid scintillation counting analysis | B | 5.27 | pKi | 5360 | nM | Ki | Bioorg Med Chem Lett (2013) 23: 26-36 [PMID:23200243] |
| ChEMBL | Displacement of [3H]CGS21680 from human A2A adenosine receptor expressed in HEK293 cell membranes after 60 mins by gamma counting method | B | 5.27 | pKi | 5360 | nM | Ki | J Med Chem (2017) 60: 7459-7475 [PMID:28799755] |
| ChEMBL | Binding affinity for human adenosine A2A receptor in CHO cells using [3H]CGS-21680 | B | 5.27 | pKi | 5360 | nM | Ki | J Med Chem (2003) 46: 3775-3777 [PMID:12930138] |
| ChEMBL | Competitive binding affinity to human adenosine A2A receptor expressed in HEK293 cells after 60 mins by fluorescence polarization assay in presence of MRS5346 | B | 5.43 | pKi | 3720 | nM | Ki | Bioorg Med Chem Lett (2013) 23: 26-36 [PMID:23200243] |
| ChEMBL | Displacement of [3H]CGS-21680 binding to Adenosine A2 receptor expressed in CHO cells | B | 6.35 | pKi | 448 | nM | Ki | J Med Chem (2004) 47: 5535-5540 [PMID:15481989] |
| ChEMBL | Displacement of [3H]NECA from human adenosine A2A receptor expressed in CHO cells | B | 6.4 | pKi | 401 | nM | Ki | J Med Chem (2007) 50: 5676-5684 [PMID:17927167] |
| ChEMBL | Displacement of [3H]CGS-21680 binding to adenosine A2A receptors of bovine striatal membranes | B | 6.4 | pKi | 401 | nM | Ki | J Med Chem (2005) 48: 1550-1562 [PMID:15743197] |
| ChEMBL | Displacement of [3H]NECA from human A2A adenosine receptor expressed in CHO cell membrane | B | 6.4 | pKi | 401 | nM | Ki | J Med Chem (2012) 55: 1490-1499 [PMID:22257095] |
| ChEMBL | Displacement of [3H]NECA from human adenosine A2A receptor expressed in CHO cell membrane after 90 mins | B | 6.4 | pKi | 401 | nM | Ki | Eur J Med Chem (2013) 69: 331-337 [PMID:24077183] |
| ChEMBL | Displacement of [3H]NECA from human adenosine A2A receptor expressed in CHO cells | B | 6.4 | pKi | 401 | nM | Ki | J Med Chem (2008) 51: 1764-1770 [PMID:18269230] |
| A2A receptor/Adenosine A2a receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2115] [GtoPdb: 19] [UniProtKB: Q60613] | ||||||||
| GtoPdb | - | - | 5 | pKi | ~10000 | nM | Ki | . A3 Adenosine Receptors from Cell Biology to Pharmacology and Therapeutics (2010) |
| ChEMBL | Displacement of [3H]2-[p-(2-carboxyethyl)phenyl-ethylamino]-5'-N-ethylcarboxamidoadenosine from mouse recombinant adenosine A2A receptor expressed in HEK293 cells | B | 5 | pKi | 10000 | nM | Ki | Bioorg Med Chem Lett (2008) 18: 2813-2819 [PMID:18424135] |
| A2A receptor/Adenosine A2a receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL302] [GtoPdb: 19] [UniProtKB: P30543] | ||||||||
| ChEMBL | Binding affinity for adenosine A2A receptor as displacement of [3H]-CGS- 21680 from rat striatal membranes at 10e-4 M | B | 6.33 | pKi | 470 | nM | Ki | J Med Chem (1998) 41: 3186-3201 [PMID:9703464] |
| ChEMBL | Binding affinity for rat adenosine A2A receptor of CHO cells using [3H]CGS-21680 | B | 6.33 | pKi | 470 | nM | Ki | J Med Chem (2003) 46: 3775-3777 [PMID:12930138] |
| ChEMBL | Tested for the binding affinity of A2a receptor by displacing the [3H]-CGS- 21680 in rat striatal membranes | B | 6.33 | pKi | 470 | nM | Ki | J Med Chem (1994) 37: 3614-3621 [PMID:7932588] |
| ChEMBL | Displacement of radioligand from rat adenosine A2A receptor | B | 6.33 | pKi | 470 | nM | Ki | Bioorg Med Chem Lett (2008) 18: 2813-2819 [PMID:18424135] |
| ChEMBL | Displacement of [3H]CGS21680 from rat adenosine A2A receptor expressed in CHO cells after 60 mins by gamma counter | B | 6.33 | pKi | 470 | nM | Ki | J Med Chem (2012) 55: 5676-5703 [PMID:22468757] |
| GtoPdb | - | - | 6.33 | pKi | 470 | nM | Ki | . A3 Adenosine Receptors from Cell Biology to Pharmacology and Therapeutics (2010) |
| ChEMBL | Binding affinity for adenosine A2a receptor as inhibition of 3[H]-CGS 21680 binding in rat striatum | B | 7.25 | pKi | 56 | nM | Ki | Bioorg Med Chem Lett (1998) 8: 1767-1770 [PMID:9873431] |
| 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 | Antagonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated adenylyl cyclase activity by [alpha-32P]ATP based assay | F | 5 | pKi | >10000 | nM | Ki | Eur J Med Chem (2018) 157: 837-851 [PMID:30144700] |
| A2B receptor/Adenosine A2b receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2237] [GtoPdb: 20] [UniProtKB: Q60614] | ||||||||
| GtoPdb | - | - | 5 | pKi | >10000 | nM | Ki | . A3 Adenosine Receptors from Cell Biology to Pharmacology and Therapeutics (2010) |
| ChEMBL | Activation of mouse adenosine A2B receptor | B | 5 | pEC50 | >=10000 | nM | EC50 | Bioorg Med Chem Lett (2008) 18: 2813-2819 [PMID:18424135] |
| 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 measured by radioligand binding assay | B | 5.85 | pKi | 1400 | nM | Ki | ACS Med Chem Lett (2022) 13: 623-631 [PMID:35450351] |
| ChEMBL | Binding affinity towards human adenosine A3 receptor | B | 7 | pKi | >=99 | nM | Ki | Eur J Med Chem (2022) 231: 114103-114103 [PMID:35152062] |
| ChEMBL | Binding affinity towards Adenosine A3 receptor (H95A mutant receptor) | B | 7.22 | pKi | 60 | nM | Ki | J Med Chem (2002) 45: 4471-4484 [PMID:12238926] |
| ChEMBL | Competitive binding affinity to human adenosine A3 receptor expressed in CHO cells after 90 mins by flow cytometric analysis in presence of MRS5449 | B | 7.56 | pKi | 27.7 | nM | Ki | Bioorg Med Chem Lett (2013) 23: 26-36 [PMID:23200243] |
| ChEMBL | Binding affinity at Mutant (H272E) human adenosine A3 receptor expressed in COS-7 cells | B | 7.7 | pKi | 20.1 | nM | Ki | J Med Chem (2001) 44: 4125-4136 [PMID:11708915] |
| ChEMBL | Binding affinity using [125I]ABA against human Adenosine A3 receptor | B | 7.85 | pKi | 14 | nM | Ki | J Med Chem (2003) 46: 353-355 [PMID:12540233] |
| ChEMBL | Binding affinity for CHO cell membrane expressing human A3AR with GTPgammaS using [3H]8-ethyl-4-methyl-2-phenyl-(8R)-4,5,7,8-tetrahydro-1H-imidazo[2,1-i]-purin-5-one | B | 8.2 | pKi | 6.3 | nM | Ki | J Med Chem (2002) 45: 4471-4484 [PMID:12238926] |
| ChEMBL | Binding affinity at wild-type Adenosine A3 receptor expressed in COS-7 cells | B | 8.37 | pKi | 4.3 | nM | Ki | J Med Chem (2001) 44: 4125-4136 [PMID:11708915] |
| ChEMBL | Binding affinity towards Adenosine A3 receptor (W243 mutant) receptor | B | 8.54 | pKi | 2.9 | nM | Ki | J Med Chem (2002) 45: 4471-4484 [PMID:12238926] |
| ChEMBL | Binding affinity towards human Adenosine A3 receptor wild type | B | 8.64 | pKi | 2.3 | nM | Ki | J Med Chem (2002) 45: 4471-4484 [PMID:12238926] |
| ChEMBL | Displacement of [125I]I-AB-MECA from human recombinant adenosine A3 receptor expressed in CHO cells after 60 mins by gamma counter | B | 8.66 | pKi | 2.2 | nM | Ki | J Med Chem (2012) 55: 5676-5703 [PMID:22468757] |
| ChEMBL | Binding affinity for CHO cell membrane expressing human Adenosine A3 receptor using [3H]8-ethyl-4-methyl-2-phenyl-(8R)-4,5,7,8-tetrahydro-1H-imidazo[2,1-i]-purin-5-one | B | 8.82 | pKi | 1.5 | nM | Ki | J Med Chem (2002) 45: 4471-4484 [PMID:12238926] |
| ChEMBL | Displacement of [3H]CGS21680 form human adenosine A3 receptor expressed in CHO cells | B | 8.85 | pKi | 1.4 | nM | Ki | Bioorg Med Chem (2008) 16: 8546-8556 [PMID:18752961] |
| ChEMBL | Binding affinity towards human Adenosine A3 receptor stably transfected in CHO cells was determined using [125I]I-AB-MECA (1.0 nM) as radioligand | B | 8.85 | pKi | 1.4 | nM | Ki | Bioorg Med Chem Lett (2004) 14: 4851-4854 [PMID:15341938] |
| ChEMBL | Displacement of [125I]-AB MECA from recombinant human adenosine A3 receptor expressed in HEK cells | B | 8.85 | pKi | 1.4 | nM | Ki | J Med Chem (2004) 47: 4766-4773 [PMID:15341491] |
| ChEMBL | Inhibition of [125I]-AB-MECA binding to human Adenosine A3 receptor expressed in CHO cells | B | 8.85 | pKi | 1.4 | nM | Ki | J Med Chem (2005) 48: 1745-1758 [PMID:15771421] |
| ChEMBL | Displacement of [125I]AB-MECA from human adenosine A3 receptor expressed in CHO cells | B | 8.85 | pKi | 1.4 | nM | Ki | J Med Chem (2007) 50: 3159-3162 [PMID:17555308] |
| ChEMBL | Displacement of [3H]ABMECA from human adenosine A3 receptor expressed in CHO cells | B | 8.85 | pKi | 1.4 | nM | Ki | Bioorg Med Chem Lett (2008) 18: 1612-1616 [PMID:18255292] |
| ChEMBL | Displacement of radioligand from human adenosine A3 receptor expressed in CHO cells | B | 8.85 | pKi | 1.4 | nM | Ki | Bioorg Med Chem Lett (2008) 18: 2813-2819 [PMID:18424135] |
| ChEMBL | Displacement of [125I]I-AB-MECA from human adenosine A3 receptor expressed in CHO cells | B | 8.85 | pKi | 1.4 | nM | Ki | J Med Chem (2008) 51: 6609-6613 [PMID:18811138] |
| ChEMBL | Displacement of [3H]I-AB-MECA from human recombinant adenosine A3 receptor expressed in CHO cells by liquid scintillation counting | B | 8.85 | pKi | 1.4 | nM | Ki | Bioorg Med Chem (2009) 17: 3733-3738 [PMID:19375920] |
| ChEMBL | Displacement of [125I]AB-MECA from human adenosine A3 receptor expressed in CHO cells | B | 8.85 | pKi | 1.4 | nM | Ki | Bioorg Med Chem (2009) 17: 8003-8011 [PMID:19879151] |
| ChEMBL | Displacement of [125I]I-AB-MECA from human adenosine A3 receptor expressed in CHO cells after 90 mins by gamma counting analysis | B | 8.85 | pKi | 1.4 | nM | Ki | Bioorg Med Chem Lett (2013) 23: 26-36 [PMID:23200243] |
| ChEMBL | Binding affinity to Adenosine receptor A3 (unknown origin) | B | 8.85 | pKi | 1.4 | nM | Ki | J Med Chem (2016) 59: 810-840 [PMID:26390077] |
| ChEMBL | Displacement of [125I]I-AB-MECA from human adenosine A3 receptor expressed in CHO cells after 60 mins by gamma counting analysis | B | 8.85 | pKi | 1.4 | nM | Ki | J Med Chem (2017) 60: 3422-3437 [PMID:28380296] |
| ChEMBL | Displacement of [125I]I-AB-MECA from human A3 adenosine receptor expressed in CHO cell membranes after 60 mins by gamma counting method | B | 8.85 | pKi | 1.4 | nM | Ki | J Med Chem (2017) 60: 7459-7475 [PMID:28799755] |
| ChEMBL | Displacement of [3H]HEMADO from human adenosine A3 receptor expressed in CHO cell membranes after 3 hrs by micro beta scintillation counting method | B | 8.85 | pKi | 1.4 | nM | Ki | Eur J Med Chem (2018) 157: 837-851 [PMID:30144700] |
| ChEMBL | Binding affinity to human A3AR assessed as inhibitor constant | B | 8.85 | pKi | 1.4 | nM | Ki | ACS Med Chem Lett (2020) 11: 1935-1941 [PMID:33062176] |
| ChEMBL | Affinity for human Adenosine A3 receptor expressed in CHO cell | B | 8.85 | pKi | 1.4 | nM | Ki | J Med Chem (2002) 45: 4471-4484 [PMID:12238926] |
| GtoPdb | - | - | 8.9 | pKi | - | - | - |
Naunyn Schmiedebergs Arch Pharmacol (2000) 361: 225-34 [PMID:10731034]; Neuropharmacology (1997) 36: 1157-65 [PMID:9364471]; J Med Chem (1994) 37: 3614-21 [PMID:7932588] |
| ChEMBL | Binding affinity for adenosine A3 receptor as inhibition of [125I]AB-MECA binding to human receptor expressed in HEK 293 cells | B | 8.96 | pKi | 1.1 | nM | Ki | Bioorg Med Chem Lett (1998) 8: 1767-1770 [PMID:9873431] |
| ChEMBL | Binding affinity to human adenosine A3 receptor | B | 9 | pKi | 1 | nM | Ki | Bioorg Med Chem (2009) 17: 8003-8011 [PMID:19879151] |
| ChEMBL | Binding affinity for human Adenosine A3 receptor in CHO cells using [125I]-iodo-AB-MECA | B | 9 | pKi | 1 | nM | Ki | J Med Chem (2003) 46: 3775-3777 [PMID:12930138] |
| ChEMBL | Binding affinity to A3AR (unknown origin) | B | 9 | pKi | 1 | nM | Ki | Bioorg Med Chem (2014) 22: 4257-4268 [PMID:24931275] |
| ChEMBL | Displacement of [125I]ABA from human adenosine A3 receptor expressed in HEK cells | B | 9.2 | pKi | 0.64 | nM | Ki | Bioorg Med Chem Lett (2006) 16: 2416-2418 [PMID:16487705] |
| ChEMBL | Displacement of [125I]I-AB-MEAC from human adenosine A3 receptor expressed in CHO cells | B | 9.42 | pKi | 0.38 | nM | Ki | Eur J Med Chem (2009) 44: 1377-1382 [PMID:18973967] |
| ChEMBL | Displacement of [125I]AB-MECA from adenosine A3 receptor from HEK293 cell membranes | B | 9.48 | pKi | 0.33 | nM | Ki | J Med Chem (1998) 41: 3186-3201 [PMID:9703464] |
| ChEMBL | Displacement of [125I]AB-MECA binding to Adenosine A3 receptor expressed in CHO cells | B | 9.48 | pKi | 0.33 | nM | Ki | J Med Chem (2004) 47: 5535-5540 [PMID:15481989] |
| ChEMBL | Displacement of [125I]AB-MECA from human adenosine A3 receptor expressed in CHO cells | B | 9.66 | pKi | 0.22 | nM | Ki | J Med Chem (2008) 51: 1764-1770 [PMID:18269230] |
| ChEMBL | Displacement of [125I]AB-MECA from human adenosine A3 receptor expressed in CHO cell membrane after 90 mins | B | 9.66 | pKi | 0.22 | nM | Ki | Eur J Med Chem (2013) 69: 331-337 [PMID:24077183] |
| ChEMBL | Displacement of [125I]AB-MECA from human A3 adenosine receptor expressed in CHO cell membrane | B | 9.66 | pKi | 0.22 | nM | Ki | J Med Chem (2012) 55: 1490-1499 [PMID:22257095] |
| ChEMBL | Displacement of [3H]AB-MECA from human adenosine A3 receptor expressed in CHO cells | B | 9.66 | pKi | 0.22 | nM | Ki | J Med Chem (2007) 50: 5676-5684 [PMID:17927167] |
| ChEMBL | Displacement of [125I]AB-MECA from adenosine A3 receptors in bovine cortical membranes | B | 9.66 | pKi | 0.22 | nM | Ki | J Med Chem (2005) 48: 1550-1562 [PMID:15743197] |
| ChEMBL | Displacement of [3H]NECA from recombinant human adenosine A3 receptor expressed in CHO cell membranes measured after 180 mins | B | 9.7 | pKi | 0.2 | nM | Ki | Medchemcomm (2018) 9: 81-86 [PMID:30108902] |
| ChEMBL | Inhibition of (10 uM) forskolin-mediated cAMP production in CHO cells expressing human Adenosine A3 receptor | F | 8.66 | pIC50 | 2.2 | nM | IC50 | J Med Chem (2004) 47: 5535-5540 [PMID:15481989] |
| ChEMBL | Agonist activity at human recombinant A3AR expressed in CHO cells assessed as inhibition of forskolin-induced stimulation of cAMP production | F | 8.92 | pIC50 | 1.21 | nM | IC50 | Bioorg Med Chem (2014) 22: 4257-4268 [PMID:24931275] |
| ChEMBL | Partial agonist activity at recombinant human A3AR expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins in presence of A2BAR blocker PSB-603 by Glo-sensor assay | F | 8.39 | pEC50 | 4.1 | nM | EC50 | J Med Chem (2020) 63: 4334-4348 [PMID:32271569] |
| ChEMBL | Effect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptor | F | 8.55 | pEC50 | 2.8 | nM | EC50 | J Med Chem (2002) 45: 4471-4484 [PMID:12238926] |
| ChEMBL | Agonist activity at human A3 adenosine receptor expressed in CHO cells assessed as inhibition of forskolin stimulated cAMP formation incubated for 45 mins followed by forskolin stimulation and measured after 15 mins by liquid scintillation spectrometry analysis | F | 8.92 | pEC50 | 1.21 | nM | EC50 | J Med Chem (2021) 64: 12525-12536 [PMID:34435786] |
| ChEMBL | Agonist activity at human adenosine A3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP | F | 8.92 | pEC50 | 1.2 | nM | EC50 | Bioorg Med Chem Lett (2008) 18: 1612-1616 [PMID:18255292] |
| A3 receptor/Adenosine A3 receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075269] [GtoPdb: 21] [UniProtKB: Q61618] | ||||||||
| GtoPdb | - | - | 9.74 | pKi | 0.18 | nM | Ki | . A3 Adenosine Receptors from Cell Biology to Pharmacology and Therapeutics (2010) |
| ChEMBL | Displacement of [125I]N6-(-amino-3-iodobenzyl)adenosine-5'-N-methyl-uronamide from mouse recombinant adenosine A3 receptor expressed in HEK293 cells | B | 9.74 | pKi | 0.18 | nM | Ki | Bioorg Med Chem Lett (2008) 18: 2813-2819 [PMID:18424135] |
| ChEMBL | Agonist activity at mouse adenosine A3 receptor expressed in HEK293 cell membranes assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 30 mins followed by forsolkin addition measured after 15 mins by immunoassay | F | 9.34 | pEC50 | 0.46 | nM | EC50 | J Med Chem (2016) 59: 3249-3263 [PMID:26890707] |
| ChEMBL | Agonist activity at mouse adenosine A3 receptor expressed in HEK293 cell membranes assessed as inhibition of forskolin-stimulated cAMP production preincubated for 30 mins prior to forskolin-treatment measured after 15 mins by ELISA | F | 9.82 | pEC50 | 0.15 | nM | EC50 | J Med Chem (2013) 56: 5949-5963 [PMID:23789857] |
| A3 receptor/Adenosine A3 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3360] [GtoPdb: 21] [UniProtKB: P28647] | ||||||||
| ChEMBL | Displacement of [125I]AB-MECA from rat A3AR transfected in CHO cell membrane assessed as inhibition constant incubated for 1 hr by gamma counter method | B | 8.85 | pKi | 1.4 | nM | Ki | J Med Chem (2023) 66: 12249-12265 [PMID:37603705] |
| ChEMBL | Binding affinity of adenosine derivative for endogenous rat Adenosine A3 receptor expressed on CHO cell | B | 9.05 | pKi | 0.9 | nM | Ki | J Med Chem (2002) 45: 4471-4484 [PMID:12238926] |
| GtoPdb | - | - | 9.48 | pKi | 0.33 | nM | Ki | . A3 Adenosine Receptors from Cell Biology to Pharmacology and Therapeutics (2010) |
| ChEMBL | Binding affinity for rat Adenosine A3 receptor | B | 9.48 | pKi | 0.33 | nM | Ki | Bioorg Med Chem Lett (2003) 13: 817-820 [PMID:12617898] |
| ChEMBL | Binding affinity for rat Adenosine A3 receptor in CHO cells [125I]-iodo-AB-MECA | B | 9.48 | pKi | 0.33 | nM | Ki | J Med Chem (2003) 46: 3775-3777 [PMID:12930138] |
| ChEMBL | Displacement of radioligand from rat A3 adenosine receptor | B | 9.48 | pKi | 0.33 | nM | Ki | Bioorg Med Chem Lett (2008) 18: 2813-2819 [PMID:18424135] |
| ChEMBL | Displacement of [125I]I-AB-MECA from rat adenosine A3 receptor expressed in CHO cells | B | 9.48 | pKi | 0.33 | nM | Ki | J Med Chem (2008) 51: 6609-6613 [PMID:18811138] |
| ChEMBL | Displacement of [125I]I-AB-MECA from human rat adenosine A3 receptor expressed in CHO cells after 60 mins by gamma counter | B | 9.48 | pKi | 0.33 | nM | Ki | J Med Chem (2012) 55: 5676-5703 [PMID:22468757] |
| ChEMBL | Inhibition of [125I]AB-MECA binding to rat Adenosine A3 receptor expressed in CHO cells | B | 9.48 | pKi | 0.33 | nM | Ki | J Med Chem (2005) 48: 1745-1758 [PMID:15771421] |
| ChEMBL | Tested for the binding affinity of A3 receptor by displacing N6-[[125I]-4-amino-3-iodobenzyl]-adenosine-5''-N-methyluronamide from membranes of CHO cells transfected with rat A3-cDNA | B | 9.48 | pKi | 0.33 | nM | Ki | J Med Chem (1994) 37: 3614-3621 [PMID:7932588] |
| ABCG2/ATP-binding cassette sub-family G member 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5393] [GtoPdb: 792] [UniProtKB: Q9UNQ0] | ||||||||
| ChEMBL | Activation of human ABCG2-mediated ATPase activity preincubated for 2 mins followed by ATP addition and measured after 20 mins by colorimetric assay | B | 5.85 | pEC50 | 1420 | nM | EC50 | Eur J Med Chem (2022) 231: 114103-114103 [PMID:35152062] |
| Equilibrative nucleoside transporter 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4604] [GtoPdb: 1117] [UniProtKB: O54698] | ||||||||
| ChEMBL | Inhibition of [3H]S-(4-Nitrobenzyl)-6-thioinosine binding to adenosine uptake sites in rat brain membranes | F | 4.82 | pKi | 15200 | nM | Ki | J Med Chem (1994) 37: 3614-3621 [PMID:7932588] |
| Peroxisome proliferator-activated receptor-β/δ/Peroxisome proliferator-activated receptor delta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3979] [GtoPdb: 594] [UniProtKB: Q03181] | ||||||||
| ChEMBL | Displacement of Fluormone-Pan-PPAR Green from human GST-tagged PPARdelta LBD by TR-FRET assay | B | 9.37 | pKi | 0.43 | nM | Ki | J Med Chem (2017) 60: 7459-7475 [PMID:28799755] |
| ChEMBL | Antagonist at PPARdelta LBD (unknown origin) assessed as increase in recruitment of coactivator peptide C33 cotreated with PPARdelta agonist GW501516 by TR-FRET assay | B | 4.53 | pEC50 | 29800 | nM | EC50 | Bioorg Med Chem (2020) 28: 115226-115226 [PMID:31806266] |
| ChEMBL | Competitive binding affinity to GST-tagged human PPARdelta LBD incubated for 1 to 6 hrs by TR-FRET assay | B | 6.72 | pEC50 | 191 | nM | EC50 | Bioorg Med Chem (2020) 28: 115226-115226 [PMID:31806266] |
| Peroxisome proliferator-activated receptor-γ/Peroxisome proliferator-activated receptor gamma in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL235] [GtoPdb: 595] [UniProtKB: P37231] | ||||||||
| ChEMBL | Displacement of Fluormone-Pan-PPAR Green from human GST-tagged PPARgamma LBD by TR-FRET assay | B | 8.66 | pKi | 2.18 | nM | Ki | J Med Chem (2017) 60: 7459-7475 [PMID:28799755] |
| ChEMBL | Competitive binding affinity to GST-tagged human PPARgamma LBD incubated for 1 to 6 hrs by TR-FRET assay | B | 5.53 | pEC50 | 2940 | nM | EC50 | Bioorg Med Chem (2020) 28: 115226-115226 [PMID:31806266] |
| Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364] | ||||||||
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum HB3 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 | 4.9 | pIC50 | 12589.25 | 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 | 5 | pIC50 | 10000 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum Dd2 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 7G8 after 72 hrs by SYBR green assay | F | 5.1 | pIC50 | 7943.28 | 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] |
| 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223] | ||||||||
| ChEMBL | Displacement of [3H]ketanserin from human 5-HT2A receptor expressed in HEK-T cell membranes incubated for 90 mins under dark condition by microbeta scintillation counting method | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2016) 59: 11006-11026 [PMID:27933810] |
| ChEMBL | Binding affinity to 5HT2A receptor (unknown origin) assessed as inhibition constant | B | 5 | pKi | >10000 | nM | Ki | RSC Med Chem (2021) 12: 1808-1825 [PMID:34825182] |
| 5-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595] | ||||||||
| ChEMBL | Displacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting method | B | 5.56 | pKi | 2770 | nM | Ki | J Med Chem (2016) 59: 11006-11026 [PMID:27933810] |
| ChEMBL | Binding affinity to 5HT2B receptor (unknown origin) assessed as inhibition constant | B | 5.56 | pKi | 2770 | nM | Ki | RSC Med Chem (2021) 12: 1808-1825 [PMID:34825182] |
| 5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335] | ||||||||
| ChEMBL | Displacement of [3H]mesulergine from human 5-HT2CR expressed in Flp-In HEK cell membranes incubated for 90 mins under dark condition by microbeta scintillation counting method | B | 5 | pKi | 10000 | nM | Ki | J Med Chem (2016) 59: 11006-11026 [PMID:27933810] |
| ChEMBL | Binding affinity to 5HT2C receptor (unknown origin) assessed as inhibition constant | B | 5 | pKi | 10000 | nM | Ki | RSC Med Chem (2021) 12: 1808-1825 [PMID:34825182] |
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]
