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ChEMBL ligand: CHEMBL190 (Theophyl, Elixicon, Slo-Bid, Bronkodyl, Accurbron, Theochron, Theophylline melting point standard, Theoclear-100, Theoclear-80, Aerolate Iii, Theograd, T-Phyl, Aerolate, NSC-2066, Theocin, Somophyllin-T, Somophyllin-Crt, Theoclear L.A.-130, Nuelin, Theoclear-200, Aerolate Jr, Theovent, Theo-24, Aquaphyllin, Theo-Dur, Theophyl-Sr, Lasma, Pro-Vent, Theophylline monohydrate, Theophylline, Uniphyl, Theolair, Respbid, Quibron, Nuelin SA-250, Nuelin SA, Theolair-Sr, Labid, Theobid, Duraphyl, Slo-Phyllin, Dimethylxanthine, Aerolate Sr, Theolixir, Elixophyllin, Elixophyllin Sr, Quibron-T/Sr, Sustaire, Uniphyllin Continus, Uni-Dur, Quibron-T, Elixomin, Theophyl-225, Theobid Jr., Lanophyllin, Theophylline-Sr, Theoclear L.A.-260) |
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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 | Dissociation constant against Adenosine A1 receptor | B | 4.92 | pKd | 12000 | nM | Kd | J. Med. Chem. (2005) 48: 2026-2035 [PMID:15771445] |
ChEMBL | Displacement of [3H]DPCPX from human recombinant adenosine A1 receptor expressed in CHO-A1 cell membrane | B | 5 | pKi | 10100 | nM | Ki | Bioorg. Med. Chem. (2010) 18: 2081-2088 [PMID:20202853] |
ChEMBL | DRUGMATRIX: Adenosine A1 radioligand binding (ligand: DPCPX) | B | 5 | pKi | 9977 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | Binding affinity to adenosine A1 receptor | B | 5.07 | pKi | 8500 | nM | Ki | J. Nat. Prod. (2000) 63: 315-317 [PMID:10757709] |
ChEMBL | Displacement of [3H]CPX from human adenosine A3 receptor expressed in CHO cells | B | 5.16 | pKi | 6920 | nM | Ki | J. Med. Chem. (2006) 49: 3682-3692 [PMID:16759111] |
ChEMBL | Binding affinity to human adenosine A1 receptor | B | 5.17 | pKi | 6770 | nM | Ki | Bioorg. Med. Chem. (2010) 18: 2195-2203 [PMID:20188574] |
ChEMBL | Binding affinity to human adenosine A1 receptor | B | 5.17 | pKi | 6770 | nM | Ki | Bioorg. Med. Chem. (2013) 21: 7435-7452 [PMID:24139167] |
ChEMBL | Displacement of [3H]CCPA from human A1 adenosine receptor expressed in CHO cells | B | 5.17 | pKi | 6770 | nM | Ki | MedChemComm (2016) 7: 845-852 |
ChEMBL | Binding affinity to human adenosine A1 receptor by radioligand displacement assay | B | 5.17 | pKi | 6770 | nM | Ki | MedChemComm (2018) 9: 951-962 |
GtoPdb | - | - | 5.2 | pKi | - | - | - |
J. Biol. Chem. (1994) 269: 32077-84 [PMID:7798201]; Naunyn Schmiedebergs Arch. Pharmacol. (1998) 357: 1-9 [PMID:9459566]; Biochem. Pharmacol. (2005) 70: 1601-12 [PMID:16219300]; Biochem. Pharmacol. (2001) 62: 1163-73 [PMID:11705449] |
ChEMBL | Displacement of [125I]DPCPX from human cloned adenosine A1 receptor expressed in CHO cells | B | 5.21 | pKi | 6200 | nM | Ki | Bioorg. Med. Chem. (2008) 16: 6086-6102 [PMID:18468446] |
ChEMBL | Displacement of [3H]CHA from cloned human adenosine A1 receptor expressed in CHO cells | B | 5.21 | pKi | 6200 | nM | Ki | J. Med. Chem. (2005) 48: 7932-7945 [PMID:16335918] |
ChEMBL | Displacement of [3H]DPCPX from human adenosine A1 receptor expressed in CHO cells | B | 5.21 | pKi | 6200 | nM | Ki | J. Med. Chem. (2006) 49: 3916-3925 [PMID:16789747] |
ChEMBL | Displacement of [3H]DPCPX from human adenosine A1 receptor expressed in CHO cells | B | 5.21 | pKi | 6200 | nM | Ki | J. Med. Chem. (2007) 50: 4061-4074 [PMID:17665891] |
ChEMBL | Displacement of [3H]DPCPX from human cloned adenosine A1 receptor expressed in CHO cells | B | 5.21 | pKi | 6200 | nM | Ki | J. Med. Chem. (2009) 52: 2407-2419 [PMID:19301821] |
ChEMBL | Binding affinity against human adenosine A1 receptor expressed in CHO cells using [3H]CHA | B | 5.21 | pKi | 6200 | nM | Ki | J. Med. Chem. (2004) 47: 3580-3590 [PMID:15214785] |
ChEMBL | Binding affinity to human adenosine A1 receptor | B | 5.21 | pKi | 6200 | nM | Ki | J. Med. Chem. (2009) 52: 3994-4006 [PMID:19569717] |
ChEMBL | Binding affinity for adenosine A1 receptor by using as [3H]CPX iradioligand n membranes from Chinese hamster ovary cells | B | 9.22 | pKi | 0.6 | nM | Ki | Bioorg. Med. Chem. Lett. (2005) 15: 609-612 [PMID:15664822] |
ChEMBL | DRUGMATRIX: Adenosine A1 radioligand binding (ligand: DPCPX) | B | 4.77 | pIC50 | 17104 | nM | IC50 | DrugMatrix in vitro pharmacology data |
Adenosine A1 receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4975] [UniProtKB: P28190] | ||||||||
ChEMBL | Antagonist binding of N6-cyclohexyl-[3H]-adenosine to bovine brain | B | 4.7 | pKi | 20000 | nM | Ki | J. Med. Chem. (1982) 25: 197-207 [PMID:6279840] |
ChEMBL | Affinity to A1 adenosine receptor was measured by the displacement of [3H]PIA in bovine brain cortical membrane | B | 5.07 | pKi | 8500 | nM | Ki | J. Med. Chem. (1994) 37: 2970-2975 [PMID:8071944] |
ChEMBL | Displacement of [3H]CPX from adenosine A1 receptor of calf brain cortical membrane | B | 5.22 | pKi | 6000 | nM | Ki | J. Med. Chem. (1991) 34: 1202-1206 [PMID:2002461] |
ChEMBL | Displacement of [3H]CHA from adenosine A1 receptor in bovine brain membranes | B | 5.42 | pKi | 3800 | nM | Ki | J. Med. Chem. (2000) 43: 3118-3124 [PMID:10956220] |
ChEMBL | Displacement of [3H]CHA from adenosine A1 receptor in bovine cerebral cortical membranes | B | 5.42 | pKi | 3800 | nM | Ki | J. Med. Chem. (2005) 48: 7932-7945 [PMID:16335918] |
ChEMBL | Displacement of [3H]DPCPX from adenosine A1 receptor in bovine brain membranes | B | 5.42 | pKi | 3800 | nM | Ki | J. Med. Chem. (2006) 49: 3916-3925 [PMID:16789747] |
ChEMBL | Displacement of [3H]DPCPX from bovine brain cortical membrane adenosine A1 receptor | B | 5.42 | pKi | 3800 | nM | Ki | J. Med. Chem. (2009) 52: 2407-2419 [PMID:19301821] |
ChEMBL | Displacement of [125I]DPCPX from adenosine A1 receptor in bovine brain membrane | B | 5.42 | pKi | 3800 | nM | Ki | Bioorg. Med. Chem. (2008) 16: 6086-6102 [PMID:18468446] |
ChEMBL | Binding affinity towards adenosine A1 receptor of bovine brain membrane using [3H]-CHA at 20 uM | B | 5.42 | pKi | 3800 | nM | Ki | J. Med. Chem. (2000) 43: 1158-1164 [PMID:10737748] |
ChEMBL | Binding affinity against adenosine A1 receptor in bovine brain membranes by [3H]CHA displacement. | B | 5.42 | pKi | 3800 | nM | Ki | J. Med. Chem. (2004) 47: 3580-3590 [PMID:15214785] |
ChEMBL | Binding affinity against bovine brain adenosine A1 receptor using N6-[3H]- cyclohexyladenosine | B | 4.9 | pIC50 | 12700 | nM | IC50 | J. Med. Chem. (1985) 28: 1071-1079 [PMID:2991519] |
ChEMBL | Binding affinity against bovine brain adenosine A1 receptor using N6-[3H]- cyclohexyladenosine | B | 5.61 | pIC50 | 2430 | nM | IC50 | J. Med. Chem. (1985) 28: 1071-1079 [PMID:2991519] |
A1 receptor/Adenosine A1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL318] [GtoPdb: 18] [UniProtKB: P25099] | ||||||||
ChEMBL | Displacement of [3H]CHA from adenosine A1 receptor in rat brain cortical membrane | B | 4.59 | pKi | 26000 | nM | Ki | J. Nat. Prod. (1998) 61: 301-305 [PMID:9514015] |
ChEMBL | Ability to inhibit binding of [3H]CHA to adenosine A1 receptor in rat brain cortical membranes. | B | 4.77 | pKi | 17000 | nM | Ki | J. Med. Chem. (1997) 40: 4396-4405 [PMID:9435909] |
ChEMBL | Binding affinity to rat adenosine A1 receptor | B | 4.85 | pKi | 14000 | nM | Ki | Bioorg. Med. Chem. (2013) 21: 7435-7452 [PMID:24139167] |
ChEMBL | Ability to inhibit binding of [3H]R-PIA to Adenosine A1 receptor in rat brain cortical membranes | B | 4.85 | pKi | 14000 | nM | Ki | J. Med. Chem. (1997) 40: 4396-4405 [PMID:9435909] |
ChEMBL | Binding affinity at Adenosine A1 receptor in rat brain cortical membrane using [3H]N6-R-phenylisopropyladenosine (R-PIA) as radioligand | B | 4.85 | pKi | 14000 | nM | Ki | J. Med. Chem. (1993) 36: 3341-3349 [PMID:8230124] |
ChEMBL | Ability to inhibit binding of 1 nM [3H]cyclohexyladenosine to adenosine A1 receptor in rat cerebral cortical membranes | B | 4.85 | pKi | 14000 | nM | Ki | J. Med. Chem. (1986) 29: 1305-1308 [PMID:3806581] |
ChEMBL | Binding affinity to A1 adenosine receptor from rat cortical membrane in presence of [3H]R-(phenylisopropyl)-adenosine | B | 4.85 | pKi | 14000 | nM | Ki | J. Med. Chem. (1994) 37: 1526-1534 [PMID:8182711] |
ChEMBL | Binding affinity for Adenosine A1 receptor from rat brain using [3H]-PIA as radioligand | B | 4.85 | pKi | 14000 | nM | Ki | J. Med. Chem. (1990) 33: 2818-2821 [PMID:2213834] |
ChEMBL | Antagonism of binding of 1 nM [3H]cyclohexyladenosine to adenosine A1 receptors on rat cortical membranes | B | 4.85 | pKi | 14000 | nM | Ki | J. Med. Chem. (1985) 28: 487-492 [PMID:2984420] |
ChEMBL | Binding affinity for adenosine A1 receptor from rat brain membranes using [3H]PIA as radioligand | B | 4.85 | pKi | 14000 | nM | Ki | J. Med. Chem. (1993) 36: 2639-2644 [PMID:8410976] |
ChEMBL | Binding of 1 nM [3H]CHA to Adenosine A1 receptor of rat cerebral cortical membranes | B | 4.85 | pKi | 14000 | nM | Ki | J. Med. Chem. (1988) 31: 2034-2039 [PMID:3172141] |
ChEMBL | Binding affinity to rat adenosine A1 receptor | B | 4.85 | pKi | 14000 | nM | Ki | Bioorg. Med. Chem. (2010) 18: 2195-2203 [PMID:20188574] |
ChEMBL | Inhibition of (R)-N6-([3H]-phenylisopropyl) adenosine binding to adenosine A1 receptor from rat cortical membranes | B | 4.89 | pKi | 13000 | nM | Ki | J. Med. Chem. (1992) 35: 2342-2345 [PMID:1613758] |
ChEMBL | Inhibition of 1 nM [3H]- N6-(phenylisopropyl) adenosine binding to Adenosine A1 receptor in rat cerebral cortical membranes | B | 4.89 | pKi | 13000 | nM | Ki | J. Med. Chem. (1989) 32: 1231-1237 [PMID:2724296] |
ChEMBL | Binding affinity towards adenosine A1 receptor in rat forebrain membranes using N6-[3H]cyclohexyladenosine | B | 5.01 | pKi | 9700 | nM | Ki | J. Med. Chem. (1992) 35: 3066-3075 [PMID:1501234] |
ChEMBL | Displacement of [3H]CPX from adenosine A1 receptor of rat brain cortical membrane | B | 5.04 | pKi | 9200 | nM | Ki | J. Med. Chem. (1991) 34: 1202-1206 [PMID:2002461] |
GtoPdb | - | - | 5.06 | pKi | 8740 | nM | Ki |
Drug Dev Res (1999) : 45-53; J. Med. Chem. (1993) 36: 3341-9 [PMID:8230124] |
ChEMBL | Inhibition of 1 nM [3H]- N6 -(phenylisopropyl) adenosine binding to Adenosine A1 receptor in rat fat cell membrane | B | 5.06 | pKi | 8700 | nM | Ki | J. Med. Chem. (1989) 32: 1231-1237 [PMID:2724296] |
ChEMBL | Binding affinity against adenosine A1 receptor using [3H]-CHA or [3H]PIA as radioligand | B | 5.07 | pKi | 8500 | nM | Ki | J. Med. Chem. (1992) 35: 407-422 [PMID:1738138] |
ChEMBL | Binding affinity to rat adenosine A1 receptor | B | 5.07 | pKi | 8500 | nM | Ki | J. Med. Chem. (2009) 52: 3994-4006 [PMID:19569717] |
ChEMBL | Displacement of [3H]PIA from adenosine A1 receptors of rat brain membrane | B | 5.07 | pKi | 8500 | nM | Ki | J. Med. Chem. (1994) 37: 3373-3382 [PMID:7932565] |
ChEMBL | Binding affinity against Adenosine A1 receptor in rat brain membrane, using [3H]N6-cyclohexyladenosine as the radioligand | B | 5.07 | pKi | 8500 | nM | Ki | J. Med. Chem. (1989) 32: 2247-2254 [PMID:2795597] |
ChEMBL | Inhibition of [3H]CHA binding to Adenosine A1 receptor in rat brain membranes | B | 5.07 | pKi | 8500 | nM | Ki | J. Med. Chem. (1990) 33: 1708-1713 [PMID:2342066] |
ChEMBL | Inhibition of rat recombinant adenosine A1 receptor | B | 5.07 | pKi | 8500 | nM | Ki | J. Med. Chem. (2014) 57: 3623-3650 [PMID:24164628] |
ChEMBL | Inhibition of N6-[3H]cyclohexyladenosine binding to adenosine A1 receptor from whole brain membranes | B | 5.07 | pKi | 8470 | nM | Ki | J. Med. Chem. (1992) 35: 2342-2345 [PMID:1613758] |
ChEMBL | Binding affinity against Adenosine A1 receptor using N6-[3H]-cyclohexyladenosinene in rat whole brain membranes | B | 5.07 | pKi | 8470 | nM | Ki | J. Med. Chem. (1992) 35: 924-930 [PMID:1548682] |
ChEMBL | Tested for binding affinity against Adenosine A1 receptor from rat forebrain membranes, using N6-[3H]- cyclohexyladenosine as radioligand | B | 5.07 | pKi | 8470 | nM | Ki | J. Med. Chem. (1993) 36: 2508-2518 [PMID:8355252] |
ChEMBL | Inhibition of binding of 1 nM [3H]N-6-(phenylisopropyl)adenosine to adenosine A1 receptor in rat cortical membranes | B | 5.07 | pKi | 8470 | nM | Ki | J. Med. Chem. (1989) 32: 1873-1879 [PMID:2754711] |
ChEMBL | Binding affinity towards adenosine A1 receptor in rat whole brain membranes using N6-[3H]cyclohexyladenosine | B | 5.07 | pKi | 8470 | nM | Ki | J. Med. Chem. (1992) 35: 3066-3075 [PMID:1501234] |
ChEMBL | In vitro binding affinity to Adenosine A1 receptor of rat cerebral cortical membranes using 1 nM [3H]PIA | B | 5.13 | pKi | 7400 | nM | Ki | J. Med. Chem. (1988) 31: 2034-2039 [PMID:3172141] |
ChEMBL | Binding affinity of specific [3H]R-PIA binding to rat Adenosine A1 receptor in HEK293 cells | B | 5.16 | pKi | 6920 | nM | Ki | J. Med. Chem. (2002) 45: 2131-2138 [PMID:12014951] |
ChEMBL | Inhibition of [3H]-CHA binding to rat brain membrane Adenosine A1 receptor | B | 6.15 | pKi | 700 | nM | Ki | J. Med. Chem. (1990) 33: 3127-3130 [PMID:2258897] |
ChEMBL | Antagonism of adenosine A1 receptor assessed from the ability to inhibit binding of [3H]cyclohexyladenosine to rat cerebral cortical membranes | B | 4.55 | pIC50 | 28000 | nM | IC50 | J. Med. Chem. (1984) 27: 1364-1367 [PMID:6090665] |
ChEMBL | Binding affinity against adenosine A1 receptor in rat brain membrane preparations using N6-[3H]cyclohexyladenosine as a radioligand | B | 4.7 | pIC50 | 20000 | nM | IC50 | J. Med. Chem. (1987) 30: 91-96 [PMID:3806606] |
ChEMBL | Inhibition of adenosine binding to A1 receptor of rat brain homogenates | B | 4.72 | pIC50 | 19000 | nM | IC50 | J. Med. Chem. (1994) 37: 476-485 [PMID:8120866] |
ChEMBL | Inhibition of binding towards adenosine A1 receptor using [3H]N-cyclohexyladenosine ([3H]CHA) in rat whole brain membranes. | B | 5 | pIC50 | >10000 | nM | IC50 | J. Med. Chem. (1988) 31: 1014-1020 [PMID:3361572] |
Adenosine A1 receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2304404] [UniProtKB: P47745] | ||||||||
ChEMBL | Binding affinity against adenosine A1 receptor from guinea pig forebrain membranes, using N6-[3H]cyclohexyladenosine as radioligand. | B | 4.64 | pKi | 23000 | nM | Ki | J. Med. Chem. (1992) 35: 2342-2345 [PMID:1613758] |
ChEMBL | Inhibition of N6-[3H]cyclohexyladenosine binding to guinea pig forebrain membrane Adenosine A1 receptor | B | 4.64 | pKi | 23000 | nM | Ki | J. Med. Chem. (1992) 35: 924-930 [PMID:1548682] |
ChEMBL | Binding affinity against Adenosine A1 receptor from guinea pig forebrain membranes by N6-[3H]- cyclohexyladenosine displacement. | B | 4.64 | pKi | 23000 | nM | Ki | J. Med. Chem. (1993) 36: 2508-2518 [PMID:8355252] |
ChEMBL | Binding affinity against adenosine A1 receptor in guinea pig forebrain membranes using N6-[3H]cyclohexyladenosine as radioligand | B | 4.64 | pKi | 23000 | nM | Ki | J. Med. Chem. (1992) 35: 3066-3075 [PMID:1501234] |
ChEMBL | Inhibition of [3H]cyclohexyladenosine binding to guinea pig forebrain membranes Adenosine A1 receptor | B | 4.64 | pKi | 23000 | nM | Ki | J. Med. Chem. (1991) 34: 466-469 [PMID:1992150] |
ChEMBL | Binding affinity against Adenosine A1 receptor using N6-[3H]cyclohexyladenosine in guinea pig membranes | B | 4.89 | pKi | 13000 | nM | Ki | J. Med. Chem. (1992) 35: 924-930 [PMID:1548682] |
ChEMBL | Affinity against adenosine A1 receptor in the brain membranes by the displacement of [3H]CPX. | B | 5.01 | pKi | 9800 | nM | Ki | J. Med. Chem. (1992) 35: 4039-4044 [PMID:1331453] |
ChEMBL | Binding affinity against adenosine A1 receptor of cerebral cortex using [3H]CPX as a radioligand | B | 5.01 | pKi | 9800 | nM | Ki | J. Med. Chem. (1993) 36: 1380-1386 [PMID:8496906] |
A2A receptor/Adenosine A2a receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL251] [GtoPdb: 19] [UniProtKB: P29274] | ||||||||
ChEMBL | Displacement of [3H]ZM241385 from stabilized human adenosine receptor A2a expressed in HEK293 cells followed by receptor capturing on Biocore chips by SPR method | B | 5.5 | pKd | 3162.28 | nM | Kd | J. Med. Chem. (2011) 54: 4312-4323 [PMID:21661720] |
ChEMBL | The A2A-StaR2 receptor has been purified from membranes in n-decyl-beta-D-maltoside as detergent. Then it has been reconstituted into rHDLs membrane discs.Ligands were prepared over a five-fold concentration series and injected in either a multi- or a single-cycle format depending on the kinetic parameters of the ligand. The actual concentrations as well as contact and dissociation times varied between the ligands depended on the kinetics and affinity of the interaction. The data were fitted to a 1:1 interaction model using the kinetics evaluation software from Biacore. A minimum of three measurements were recorded for each interaction. | B | 5.78 | pKd | 1642.33 | nM | Kd | K4DD drug target binding kinetics data |
ChEMBL | Affinity to A2 adenosine receptor was measured by the displacement of [3H]-CGS- 21680 in bovine brain striatal membrane | B | 4.6 | pKi | 25000 | nM | Ki | J. Med. Chem. (1994) 37: 2970-2975 [PMID:8071944] |
ChEMBL | Displacement of [3H]-CGS- 21680 from adenosine A2A receptor in bovine striatal membranes. | B | 4.68 | pKi | 21000 | nM | Ki | J. Med. Chem. (2000) 43: 3118-3124 [PMID:10956220] |
ChEMBL | Displacement of [3H]CGS 21680 from adenosine A2A receptor in bovine striatal membranes | B | 4.68 | pKi | 21000 | nM | Ki | J. Med. Chem. (2006) 49: 3916-3925 [PMID:16789747] |
ChEMBL | Displacement of [3H]CGS 21680 from adenosine A2A receptor in bovine striatal membranes | B | 4.68 | pKi | 21000 | nM | Ki | J. Med. Chem. (2005) 48: 7932-7945 [PMID:16335918] |
ChEMBL | Displacement of [3H]-CGS- 21680 from adenosine A2a receptor of bovine striatal membranes | B | 4.68 | pKi | 21000 | nM | Ki | J. Med. Chem. (2004) 47: 3580-3590 [PMID:15214785] |
ChEMBL | Displacement of [3H]ZM241385 from human recombinant adenosine A2A receptor expressed in in human HeLa cell membrane | B | 4.73 | pKi | 18500 | nM | Ki | Bioorg. Med. Chem. (2010) 18: 2081-2088 [PMID:20202853] |
ChEMBL | Displacement of [3H]ZM241385 from stabilized human adenosine receptor A2a expressed in HEK293 cells followed by receptor capturing on Biocore chips by SPR method | B | 5 | pKi | >10000 | nM | Ki | J. Med. Chem. (2011) 54: 4312-4323 [PMID:21661720] |
ChEMBL | Displacement of [125I]NECA from human cloned adenosine A2A receptor expressed in CHO cells | B | 5.1 | pKi | 7900 | nM | Ki | Bioorg. Med. Chem. (2008) 16: 6086-6102 [PMID:18468446] |
ChEMBL | Displacement of [3H]NECA from cloned human adenosine A2A receptor expressed in CHO cells | B | 5.1 | pKi | 7900 | nM | Ki | J. Med. Chem. (2005) 48: 7932-7945 [PMID:16335918] |
ChEMBL | Displacement of [3H]NECA from human adenosine A2A receptor expressed in CHO cells | B | 5.1 | pKi | 7900 | nM | Ki | J. Med. Chem. (2006) 49: 3916-3925 [PMID:16789747] |
ChEMBL | Displacement of [3H]NECA from human adenosine A2A receptor expressed in CHO cells | B | 5.1 | pKi | 7900 | nM | Ki | J. Med. Chem. (2007) 50: 4061-4074 [PMID:17665891] |
ChEMBL | Displacement of [3H]NECA from human cloned adenosine A2A receptor expressed in CHO cells | B | 5.1 | pKi | 7900 | nM | Ki | J. Med. Chem. (2009) 52: 2407-2419 [PMID:19301821] |
ChEMBL | DRUGMATRIX: Adenosine A2A radioligand binding (ligand: AB-MECA) | B | 5.17 | pKi | 6741 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | Binding affinity to human adenosine A2A receptor | B | 5.17 | pKi | 6700 | nM | Ki | Bioorg. Med. Chem. (2010) 18: 2195-2203 [PMID:20188574] |
ChEMBL | Displacement of [3H]ZM-241385 from human adenosine A2a receptor expressed in HEK cells | B | 5.17 | pKi | 6700 | nM | Ki | J. Med. Chem. (2006) 49: 3682-3692 [PMID:16759111] |
ChEMBL | Binding affinity to human adenosine A2A receptor | B | 5.17 | pKi | 6700 | nM | Ki | Bioorg. Med. Chem. (2013) 21: 7435-7452 [PMID:24139167] |
ChEMBL | Binding affinity to human adenosine A2A receptor | B | 5.38 | pKi | 4200 | nM | Ki | J. Med. Chem. (2009) 52: 3994-4006 [PMID:19569717] |
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 | 5.69 | pKi | 2030 | nM | Ki | Bioorg. Med. Chem. Lett. (2013) 23: 26-36 [PMID:23200243] |
ChEMBL | Binding affinity to human adenosine A2A receptor by radioligand displacement assay | B | 5.77 | pKi | 1710 | nM | Ki | MedChemComm (2018) 9: 951-962 |
ChEMBL | Displacement of [3H]NECA from human A2A adenosine receptor expressed in CHO cells | B | 5.77 | pKi | 1710 | nM | Ki | MedChemComm (2016) 7: 845-852 |
ChEMBL | Displacement of [3H]CGS21680 from human adenosine A2A receptor expressed in HEK293 cells after 60 mins by liquid scintillation counting analysis | B | 5.77 | pKi | 1700 | nM | Ki | Bioorg. Med. Chem. Lett. (2013) 23: 26-36 [PMID:23200243] |
GtoPdb | - | - | 5.8 | pKi | - | - | - |
Naunyn Schmiedebergs Arch. Pharmacol. (1998) 357: 1-9 [PMID:9459566]; Biochem. Pharmacol. (2005) 70: 1601-12 [PMID:16219300]; Br. J. Pharmacol. (1997) 121: 353-60 [PMID:9179373]; Drug Dev Res (1999) : 45-53 |
ChEMBL | Binding affinity for adenosine A2a receptor by using as [3H]ZM-241385 radioligand in membranes from HEK-A2A cells | B | 9.22 | pKi | 0.6 | nM | Ki | Bioorg. Med. Chem. Lett. (2005) 15: 609-612 [PMID:15664822] |
ChEMBL | DRUGMATRIX: Adenosine A2A radioligand binding (ligand: AB-MECA) | B | 4.92 | pIC50 | 12007 | nM | IC50 | DrugMatrix in vitro pharmacology data |
ChEMBL | Relaxant activity on the spontaneous tone of isolated guinea pig tracheal ring chains. | F | 4.55 | pEC50 | 28200 | nM | EC50 | J. Med. Chem. (1992) 35: 4039-4044 [PMID:1331453] |
A2A receptor/Adenosine A2a receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL302] [GtoPdb: 19] [UniProtKB: P30543] | ||||||||
ChEMBL | Binding affinity to rat adenosine A2A receptor | B | 4.6 | pKi | 25000 | nM | Ki | J. Med. Chem. (2009) 52: 3994-4006 [PMID:19569717] |
ChEMBL | Inhibition of rat recombinant adenosine receptor A2a | B | 4.6 | pKi | 25000 | nM | Ki | J. Med. Chem. (2014) 57: 3623-3650 [PMID:24164628] |
ChEMBL | Displacement of [3H]-CGS- 21680 from adenosine A2a receptors of rat striatal membrane | B | 4.6 | pKi | 25000 | nM | Ki | J. Med. Chem. (1994) 37: 3373-3382 [PMID:7932565] |
ChEMBL | Displacement of [3H]CGS21680 from adenosine A2A receptor in rat brain striatal membrane | B | 4.66 | pKi | 22000 | nM | Ki | J. Nat. Prod. (1998) 61: 301-305 [PMID:9514015] |
ChEMBL | Binding affinity to rat adenosine A2A receptor | B | 4.66 | pKi | 22000 | nM | Ki | Bioorg. Med. Chem. (2010) 18: 2195-2203 [PMID:20188574] |
ChEMBL | Binding affinity to rat adenosine A2A receptor | B | 4.66 | pKi | 22000 | nM | Ki | Bioorg. Med. Chem. (2013) 21: 7435-7452 [PMID:24139167] |
GtoPdb | - | - | 4.66 | pKi | 22000 | nM | Ki |
Drug Dev Res (1999) : 45-53; J. Med. Chem. (1993) 36: 3341-9 [PMID:8230124] |
ChEMBL | Ability to inhibit binding of [3H]NECA to Adenosine A2A receptor in rat brain striatal membranes | B | 4.72 | pKi | 19000 | nM | Ki | J. Med. Chem. (1997) 40: 4396-4405 [PMID:9435909] |
ChEMBL | Ability to inhibit binding of [3H]-CGS- 21680 to adenosine A2A receptor in rat brain striatal membranes. | B | 5.03 | pKi | 9400 | nM | Ki | J. Med. Chem. (1997) 40: 4396-4405 [PMID:9435909] |
ChEMBL | Binding affinity for adenosine A2A receptor from rat brain membranes using [3H]CGS-21680 | B | 5.1 | pKi | 8000 | nM | Ki | J. Med. Chem. (1993) 36: 2639-2644 [PMID:8410976] |
ChEMBL | Binding affinity at rat Adenosine A2A receptor by [3H]-CGS- 21680 displacement. | B | 5.17 | pKi | 6700 | nM | Ki | J. Med. Chem. (2002) 45: 2131-2138 [PMID:12014951] |
Adenosine A2a receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2605] [UniProtKB: P46616] | ||||||||
ChEMBL | Affinity against adenosine A2 receptor in the brain membranes measured by the displacement of [3H]-CPX | B | 4.78 | pKi | 16600 | nM | Ki | J. Med. Chem. (1992) 35: 4039-4044 [PMID:1331453] |
ChEMBL | Compound was evaluated for its ability to antagonise cyclic [3H]AMP accumulation in [3H]adenine-labeled guinea pig cerebral cortical slices. | F | 4.85 | pKi | 14000 | nM | Ki | J. Med. Chem. (1986) 29: 1305-1308 [PMID:3806581] |