ZM-241385 [Ligand Id: 405] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL113142 (ZM-241385)
  • A1 receptor/Adenosine A1 receptor in Human [ChEMBL: CHEMBL226] [GtoPdb: 18] [UniProtKB: P30542]
  • A1 receptor/Adenosine A1 receptor in Rat [ChEMBL: CHEMBL318] [GtoPdb: 18] [UniProtKB: P25099]
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  • A2A receptor/Adenosine A2a receptor in Human [ChEMBL: CHEMBL251] [GtoPdb: 19] [UniProtKB: P29274]
  • A2A receptor/Adenosine A2a receptor in Rat [ChEMBL: CHEMBL302] [GtoPdb: 19] [UniProtKB: P30543]
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  • A2B receptor/Adenosine A2b receptor in Human [ChEMBL: CHEMBL255] [GtoPdb: 20] [UniProtKB: P29275]
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  • A3 receptor/Adenosine A3 receptor in Human [ChEMBL: CHEMBL256] [GtoPdb: 21] [UniProtKB: P0DMS8]
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  • D2 receptor/Dopamine D2 receptor in Human [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
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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 The A1-StaR receptor has been purified from membranes in n-decyl-beta-D-maltoside as detergent. 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. B 6.61 pKd 245.4 nM Kd K4DD drug target binding kinetics data
ChEMBL Antagonist activity at A1AR (unknown origin) B 5.69 pKi 2041.74 nM Ki Eur J Med Chem (2020) 187: 111936-111936 [PMID:31855793]
ChEMBL Antagonist activity at A1AR (unknown origin) B 5.69 pKi 2041.74 nM Ki Eur J Med Chem (2020) 187: 111936-111936 [PMID:31855793]
ChEMBL Antagonist activity at human adenosine A1 receptor assessed as cAMP level by cell based assay B 6.11 pKi 774 nM Ki Bioorg. Med. Chem. Lett. (2013) 23: 3427-3433 [PMID:23602401]
ChEMBL Displacement of [3H]DPCPX from human recombinant A1 receptor expressed in CHOA1 cell membranes incubated for 60 mins by radioligand binding competition assay B 6.17 pKi 683 nM Ki J Med Chem (2019) 62: 9315-9330 [PMID:31557025]
ChEMBL Displacement of [3H]DPCPX from human Adenosine A1 receptor expressed in CHO cells after 60 mins B 6.17 pKi 683 nM Ki J. Med. Chem. (2016) 59: 1967-1983 [PMID:26824742]
ChEMBL Displacement of [3H]DPCPX from human recombinant A1 receptor expressed in CHOA1 cell membranes incubated for 60 mins by radioligand binding competition assay B 6.17 pKi 683 nM Ki J Med Chem (2019) 62: 9315-9330 [PMID:31557025]
ChEMBL Displacement of [3H]DPCPX from human adenosine A1 receptor expressed in CHO cell membranes after 60 mins B 6.17 pKi 683 nM Ki J Med Chem (2017) 60: 3372-3382 [PMID:28368607]
ChEMBL Displacement of [3H]DPCPX from human cloned adenosine A1 receptor expressed in CHOK1 cells by scintillation counting B 6.27 pKi 540 nM Ki Eur. J. Med. Chem. (2009) 44: 2122-2127 [PMID:19036477]
ChEMBL Binding affinity towards human Adenosine A1 receptor expressed in CHO cells using 1 nM [3H]DPCPX B 6.51 pKi 307.9 nM Ki J. Med. Chem. (2005) 48: 6887-6896 [PMID:16250647]
ChEMBL Binding affinity against human Adenosine A1 receptor B 6.59 pKi 255 nM Ki Bioorg. Med. Chem. Lett. (2004) 14: 3307-3312 [PMID:15149696]
ChEMBL Inhibition of human recombinant adenosine A1 receptor B 6.59 pKi 255 nM Ki J. Med. Chem. (2014) 57: 3623-3650 [PMID:24164628]
GtoPdb - - 6.6 pKi - - - Naunyn Schmiedebergs Arch Pharmacol (1999) 359: 7-10 [PMID:9933143];
Nat Rev Drug Discov (2006) 5: 247-64 [PMID:16518376]
ChEMBL Displacement of [3H]DPCPX from human adenosine A1 receptor expressed in CHO cell membranes measured after 90 mins by scintillation counting method B 6.73 pKi 185 nM Ki J Med Chem (2016) 59: 10564-10576 [PMID:27933962]
ChEMBL Displacement of [125I]DPCPX from human cloned adenosine A1 receptor expressed in CHO cells after 120 mins by scintillation counting B 6.74 pKi 180 nM Ki J. Med. Chem. (2009) 52: 7640-7652 [PMID:19743865]
ChEMBL Displacement of [3H]DPCPX from human adenosine A1 receptor expressed in CHO cell membranes measured after 90 mins by scintillation counting method B 6.75 pKi 178 nM Ki Eur J Med Chem (2018) 155: 552-561 [PMID:29909340]
A1 receptor/Adenosine A1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL318] [GtoPdb: 18] [UniProtKB: P25099]
ChEMBL Inhibition of [3H]DPCPX binding to adenosine A1 receptor of rat cerebral cortex B 6.17 pKi 680 nM Ki J. Med. Chem. (2005) 48: 2009-2018 [PMID:15771443]
ChEMBL Inhibition of [3H]DPCPX binding to rat cerebral cortex adenosine A1 receptor B 6.17 pKi 680 nM Ki J. Med. Chem. (2004) 47: 4291-4299 [PMID:15294001]
A2A receptor/Adenosine A2a receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL251] [GtoPdb: 19] [UniProtKB: P29274]
ChEMBL The A2A-StaR2 receptor has been purified from membranes in n-decyl-beta-D-maltoside as detergent. 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 7.99 pKd 10.28 nM Kd K4DD drug target binding kinetics data
ChEMBL The A2A-StaR2 receptor has been purified from membranes in n-decyl-beta-D-maltoside as detergent. 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 8.4 pKd 3.99 nM Kd K4DD drug target binding kinetics data
ChEMBL The A2A-StaR2 receptor has been purified from membranes in n-decyl-beta-D-maltoside as detergent. 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 8.58 pKd 2.63 nM Kd K4DD drug target binding kinetics data
ChEMBL Purified A2A protein was immobilized via His-tag on NTA chip. Small molecule ligands were analyzed in multiple cycle kinetoc mode. No regeneration was applied. B 8.9 pKd 1.26 nM Kd K4DD drug target binding kinetics data
ChEMBL The A2A-StaR2 receptor has been purified from membranes in n-decyl-beta-D-maltoside as detergent. 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 8.91 pKd 1.23 nM Kd K4DD drug target binding kinetics data
ChEMBL The A2A-StaR2 receptor has been purified from membranes in n-decyl-beta-D-maltoside as detergent. 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 9.22 pKd 0.6 nM Kd K4DD drug target binding kinetics data
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 9.3 pKd 0.5 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. 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 9.4 pKd 0.4 nM Kd K4DD drug target binding kinetics data
ChEMBL The A2A-StaR2 receptor has been purified from membranes in n-decyl-beta-D-maltoside as detergent. 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 9.46 pKd 0.35 nM Kd K4DD drug target binding kinetics data
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 9.49 pKd 0.32 nM Kd K4DD drug target binding kinetics data
ChEMBL The A2A-StaR2 receptor has been purified from membranes in n-decyl-beta-D-maltoside as detergent. 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 9.54 pKd 0.29 nM Kd K4DD drug target binding kinetics data
ChEMBL A2A protein embedded into nanodisc was immobilized via His-tag on NTA chip. Small molecule ligands were analyzed in multiple cycle kinetic mode. No regeneration was applied. B 9.63 pKd 0.24 nM Kd K4DD drug target binding kinetics data
ChEMBL A2A protein embedded into nanodisc was immobilized via 1D4 antibody on the CM5 sensors. Small molecule ligands were analyzed in multiple cycle kinetic mode. No regeneration was applied. B 9.69 pKd 0.21 nM Kd K4DD drug target binding kinetics data
ChEMBL Displacement of [3H]ZM-241385 from human cloned adenosine A2A receptor expressed in HEK293 cells by scintillation counting B 7.19 pKi 64 nM Ki Eur. J. Med. Chem. (2009) 44: 2122-2127 [PMID:19036477]
ChEMBL Displacement of MRS5346 from C-terminal 10xHis and 1D4-tagged C-terminal-truncated human A2A adenosine receptor (1 to 316 residues) expressed in Pichia pastoris expression system after 1 hr by fluorescence polarization assay B 8.28 pKi 5.3 nM Ki ACS Med Chem Lett (2017) 8: 660-665 [PMID:28626529]
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 8.7 pKi 2 nM Ki J. Med. Chem. (2011) 54: 4312-4323 [PMID:21661720]
ChEMBL Displacement of [3H]ZM241385 from human Adenosine A2A receptor expressed in HeLa cells after 30 mins B 8.72 pKi 1.9 nM Ki J. Med. Chem. (2016) 59: 1967-1983 [PMID:26824742]
ChEMBL Displacement of [3H]ZM241385 from human recombinant A2A receptor expressed in human HeLa cell membranes incubated for 30 mins by radioligand binding competition assay B 8.72 pKi 1.9 nM Ki J Med Chem (2019) 62: 9315-9330 [PMID:31557025]
ChEMBL Displacement of [3H]4-(2-[7-amino-2-(2-furyl)[1,2,4]triazolo[2,3-a][1,3,5]triazin-5-ylamino]ethyl)phenol from human adenosine A2A receptor expressed in human Hela cell membranes after 30 mins B 8.72 pKi 1.9 nM Ki J Med Chem (2017) 60: 3372-3382 [PMID:28368607]
ChEMBL Displacement of [3H]ZM241385 from human recombinant A2A receptor expressed in human HeLa cell membranes incubated for 30 mins by radioligand binding competition assay B 8.72 pKi 1.9 nM Ki J Med Chem (2019) 62: 9315-9330 [PMID:31557025]
ChEMBL Displacement of [3H]CGS21680 from human adenosine A2A receptor expressed in HEK293 cells after 60 mins by liquid scintillation counting analysis B 8.8 pKi 1.6 nM Ki Bioorg. Med. Chem. Lett. (2013) 23: 26-36 [PMID:23200243]
ChEMBL Antagonist activity at adenosine A2A receptor (unknown origin) F 8.8 pKi 1.6 nM Ki Eur J Med Chem (2018) 144: 151-163 [PMID:29268131]
ChEMBL Antagonist activity at human adenosine A2A receptor assessed as cAMP level by cell based assay B 8.8 pKi 1.6 nM Ki Bioorg. Med. Chem. Lett. (2013) 23: 3427-3433 [PMID:23602401]
ChEMBL Displacement of [3H]-ZM241385 from human adenosine A2A receptor by scintillation spectroscopy B 8.8 pKi 1.6 nM Ki J. Med. Chem. (2016) 59: 788-809 [PMID:26356532]
ChEMBL Displacement of [3H]-ZM241385 from human adenosine A2A receptor expressed in CHO cell membranes after 1 hr by TopCount microplate scintillation counting method B 8.89 pKi 1.3 nM Ki Eur J Med Chem (2018) 144: 151-163 [PMID:29268131]
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 8.89 pKi 1.3 nM Ki Bioorg. Med. Chem. Lett. (2013) 23: 26-36 [PMID:23200243]
ChEMBL Displacement of [125I]Z241385 from human cloned adenosine A2A receptor expressed in CHO cells after 120 mins by scintillation counting B 8.92 pKi 1.2 nM Ki J. Med. Chem. (2009) 52: 7640-7652 [PMID:19743865]
ChEMBL Displacement of [3H]-CGS21680 from human adenosine A2A receptor expressed in CHO cell membranes measured after 90 mins by scintillation counting method B 9.03 pKi 0.93 nM Ki J Med Chem (2016) 59: 10564-10576 [PMID:27933962]
ChEMBL Displacement of [3H]ZM241385 from human adenosine A2A receptor expressed in CHO cell membranes measured after 60 mins by scintillation counting method B 9.04 pKi 0.91 nM Ki J Med Chem (2016) 59: 10564-10576 [PMID:27933962]
ChEMBL Displacement of [3H]ZM241385 from human adenosine A2A receptor expressed in CHO cell membranes measured after 60 mins by scintillation counting method B 9.06 pKi 0.87 nM Ki Eur J Med Chem (2018) 155: 552-561 [PMID:29909340]
ChEMBL Binding affinity against human Adenosine A2a receptor (hA2a) B 9.1 pKi 0.8 nM Ki Bioorg. Med. Chem. Lett. (2004) 14: 3307-3312 [PMID:15149696]
ChEMBL Binding affinity to human adenosine A2A receptor B 9.1 pKi 0.8 nM Ki J. Med. Chem. (2008) 51: 4449-4455 [PMID:18637670]
ChEMBL Inhibition of human recombinant adenosine receptor A2a F 9.1 pKi 0.8 nM Ki J. Med. Chem. (2014) 57: 3623-3650 [PMID:24164628]
GtoPdb - - 9.1 pKi - - - Naunyn Schmiedebergs Arch Pharmacol (1999) 359: 7-10 [PMID:9933143]
ChEMBL Displacement of [3H]-ZM241385 from wild type human adenosine receptor A2a expressed in HEK293 cell membranes after 240 mins by scintillation counting B 9.4 pKi 0.4 nM Ki J Med Chem (2016) 59: 6470-6479 [PMID:27312113]
ChEMBL Displacement of [3H]-ZM241385 from wild type human adenosine receptor A2a expressed in HEK293 cell membranes after 240 mins by scintillation counting B 9.4 pKi 0.4 nM Ki J Med Chem (2016) 59: 6470-6479 [PMID:27312113]
ChEMBL Antagonist activity at A2AR (unknown origin) B 9.52 pKi 0.3 nM Ki Eur J Med Chem (2020) 187: 111936-111936 [PMID:31855793]
ChEMBL Antagonist activity at A2AR (unknown origin) B 9.52 pKi 0.3 nM Ki Eur J Med Chem (2020) 187: 111936-111936 [PMID:31855793]
ChEMBL Binding affinity towards adenosine A2A receptor B 9.52 pKi 0.3 nM Ki Bioorg. Med. Chem. Lett. (2005) 15: 4809-4813 [PMID:16153830]
ChEMBL Binding affinity towards human Adenosine A2a receptor expressed in HEK293 cells using 6 nM [3H]CGS-21680 B 10 pKi 0.1 nM Ki J. Med. Chem. (2005) 48: 6887-6896 [PMID:16250647]
ChEMBL Antagonist activity at human adenosine A2A receptor expressed in HEK293 cell membranes assessed as inhibition of CGS241680-induced [35S]GTPgammaS binding preincubated for 10 mins followed by CGS241680 addition by TopCount scintillation counting method F 7.09 pIC50 80.8 nM IC50 Eur J Med Chem (2018) 144: 151-163 [PMID:29268131]
ChEMBL Antagonist activity at recombinant human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production after 60 mins B 7.38 pIC50 42 nM IC50 Bioorg. Med. Chem. Lett. (2013) 23: 3427-3433 [PMID:23602401]
ChEMBL Antagonist activity at recombinant human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production after 60 mins B 7.38 pIC50 41.69 nM IC50 Bioorg. Med. Chem. Lett. (2013) 23: 3427-3433 [PMID:23602401]
ChEMBL Inhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assay F 7.48 pIC50 33.11 nM IC50 J. Med. Chem. (2015) 58: 718-738 [PMID:25490054]
ChEMBL Inhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assay F 7.48 pIC50 33 nM IC50 J. Med. Chem. (2015) 58: 718-738 [PMID:25490054]
ChEMBL Inverse agonist activity at human adenosine A2A receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method B 8.84 pIC50 1.45 nM IC50 J Med Chem (2016) 59: 10564-10576 [PMID:27933962]
ChEMBL Inverse agonist activity at human adenosine A2A receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method F 8.91 pIC50 1.24 nM IC50 Eur J Med Chem (2018) 155: 552-561 [PMID:29909340]
ChEMBL Antagonist activity against human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS21680-stimulated cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method F 9.08 pIC50 0.83 nM IC50 Eur J Med Chem (2018) 155: 552-561 [PMID:29909340]
ChEMBL Antagonist activity against human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS21680-stimulated cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method B 9.17 pIC50 0.68 nM IC50 J Med Chem (2016) 59: 10564-10576 [PMID:27933962]
A2A receptor/Adenosine A2a receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL302] [GtoPdb: 19] [UniProtKB: P30543]
ChEMBL Displacement [3H]-CGS-21,680 from Adenosine A2A receptor in rat striatal membrane. B 6.28 pKi 530 nM Ki J. Med. Chem. (1996) 39: 398-406 [PMID:8558508]
ChEMBL Displacement of [3H]NECA from adenosine A2A receptor in Sprague-Dawley rat striatal membranes after 1 hr by scintillation counting analysis B 8.54 pKi 2.88 nM Ki Eur. J. Med. Chem. (2015) 104: 177-188 [PMID:26462195]
ChEMBL Displacement of [3H]NECA from rat adenosine A2A receptor expressed in CHO cell membranes by radioligand competition assay B 8.55 pKi 2.8 nM Ki J Med Chem (2019) 62: 8511-8531 [PMID:31453698]
ChEMBL Displacement of [3H]-NECA from Adenosine A2A receptor in rat striatal membranes B 8.66 pKi 2.2 nM Ki Bioorg. Med. Chem. (2015) 23: 6641-6649 [PMID:26392370]
ChEMBL Displacement of [3H]NECA from adenosine A2A receptor in rat striatal membrane B 8.7 pKi 2 nM Ki Bioorg. Med. Chem. Lett. (2016) 26: 734-738 [PMID:26776359]
ChEMBL Displacement of [3H]-NECA from Adenosine A2A receptor in Sprague-Dawley rat striatal membranes B 8.87 pKi 1.36 nM Ki Bioorg. Med. Chem. (2015) 23: 6641-6649 [PMID:26392370]
ChEMBL Displacement of [3H]NECA from adenosine A2A receptor in Sprague-Dawley rat striatal membrane after 1 hr by scintillation counting B 8.92 pKi 1.2 nM Ki Bioorg. Med. Chem. Lett. (2016) 26: 734-738 [PMID:26776359]
ChEMBL Inhibition of [3H]ZM-241,385 binding to rat brain adenosine A2a receptor B 9.05 pKi 0.9 nM Ki J. Med. Chem. (2004) 47: 4291-4299 [PMID:15294001]
ChEMBL Inhibition of [3H]ZM-241385 binding to adenosine A2a receptor of rat brain tissue B 9.05 pKi 0.9 nM Ki J. Med. Chem. (2005) 48: 2009-2018 [PMID:15771443]
A2B receptor/Adenosine A2b receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL255] [GtoPdb: 20] [UniProtKB: P29275]
ChEMBL Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes after 30 mins B 7.18 pKi 65.7 nM Ki J Med Chem (2017) 60: 3372-3382 [PMID:28368607]
ChEMBL Displacement of [3H]DPCPX from human recombinant A2B receptor expressed in human HEK293 cell membranes incubated for 30 mins by radioligand binding competition assay B 7.18 pKi 65.7 nM Ki J Med Chem (2019) 62: 9315-9330 [PMID:31557025]
ChEMBL Displacement of [3H]DPCPX from human recombinant A2B receptor expressed in human HEK293 cell membranes incubated for 30 mins by radioligand binding competition assay B 7.18 pKi 65.7 nM Ki J Med Chem (2019) 62: 9315-9330 [PMID:31557025]
ChEMBL Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells after 30 mins B 7.18 pKi 65.7 nM Ki J. Med. Chem. (2016) 59: 1967-1983 [PMID:26824742]
ChEMBL Inhibition of human recombinant adenosine receptor A2b B 7.3 pKi 50 nM Ki J. Med. Chem. (2014) 57: 3623-3650 [PMID:24164628]
ChEMBL Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated [3H]cAMP production by scintillation counting F 7.38 pKi 42 nM Ki J. Med. Chem. (2009) 52: 7640-7652 [PMID:19743865]
ChEMBL Selectivity for recombinant human adenosine A2b receptor B 7.52 pKi 30 nM Ki J. Med. Chem. (2004) 47: 4291-4299 [PMID:15294001]
ChEMBL Displacement of [3H]ZM-241385 from human A2B receptor expressed in HEK-293 cell membranes B 7.55 pKi 28 nM Ki Eur. J. Med. Chem. (2016) 108: 529-541 [PMID:26717203]
ChEMBL Displacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cell membrane B 7.71 pKi 19.3 nM Ki Bioorg. Med. Chem. (2010) 18: 2081-2088 [PMID:20202853]
GtoPdb - - 8.2 pKi - - - Mol Pharmacol (1999) 56: 705-13 [PMID:10496952];
Biochem Pharmacol (2001) 61: 657-63 [PMID:11266650];
Mol Pharmacol (2000) 58: 1349-56 [PMID:11093773];
Biochem Pharmacol (2004) 68: 305-12 [PMID:15194002]
ChEMBL Displacement of PSB-12105 from recombinant human adenosine A2B receptor expressed in CHO cell membranes preincubated for 30 mins followed by PSB-12105 addition measured after 20 mins by flow cytometric method B 7.02 pIC50 94.9 nM IC50 J Med Chem (2018) 61: 4301-4316 [PMID:29681156]
ChEMBL Inverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method F 7.29 pIC50 51 nM IC50 Eur J Med Chem (2018) 155: 552-561 [PMID:29909340]
ChEMBL Inverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method B 7.32 pIC50 48 nM IC50 J Med Chem (2016) 59: 10564-10576 [PMID:27933962]
A3 receptor/Adenosine A3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL256] [GtoPdb: 21] [UniProtKB: P0DMS8]
ChEMBL Inhibition of human recombinant adenosine A3 receptor B 5 pKi >10000 nM Ki J. Med. Chem. (2014) 57: 3623-3650 [PMID:24164628]
ChEMBL Displacement of [3H]NECA from human adenosine A3 receptor expressed in human Hela cell membranes after 180 mins B 6.06 pKi 863 nM Ki J Med Chem (2017) 60: 3372-3382 [PMID:28368607]
ChEMBL Displacement of [3H]NECA from human A3 receptor expressed in human HeLa cell membranes incubated for 180 mins by radioligand binding competition assay B 6.06 pKi 863 nM Ki J Med Chem (2019) 62: 9315-9330 [PMID:31557025]
ChEMBL Displacement of [3H]NECA from human Adenosine A3 receptor expressed in HeLa cells after 30 mins B 6.06 pKi 863 nM Ki J. Med. Chem. (2016) 59: 1967-1983 [PMID:26824742]
ChEMBL Displacement of [3H]NECA from human A3 receptor expressed in human HeLa cell membranes incubated for 180 mins by radioligand binding competition assay B 6.06 pKi 863 nM Ki J Med Chem (2019) 62: 9315-9330 [PMID:31557025]
ChEMBL Displacement of [125I]I-AB-MECA from human adenosine A3 receptor expressed in CHO cells after 90 mins by gamma counting analysis B 6.13 pKi 743 nM Ki Bioorg. Med. Chem. Lett. (2013) 23: 26-36 [PMID:23200243]
GtoPdb - - 6.13 pKi 743 nM Ki Nat Rev Drug Discov (2006) 5: 247-64 [PMID:16518376]
ChEMBL Displacement of [125I]AB-MECA from human adenosine A3 receptor expressed in CHO cell membranes measured after 120 mins by scintillation counting method B 6.17 pKi 683 nM Ki J Med Chem (2016) 59: 10564-10576 [PMID:27933962]
ChEMBL Displacement of [125I]AB-MECA from human adenosine A3 receptor expressed in CHO cell membranes measured after 120 mins by scintillation counting method B 6.17 pKi 674 nM Ki Eur J Med Chem (2018) 155: 552-561 [PMID:29909340]
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 6.52 pKi 300 nM Ki Bioorg. Med. Chem. Lett. (2013) 23: 26-36 [PMID:23200243]
D2 receptor/Dopamine D2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
ChEMBL Agonist activity at human dopamine D2L receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assay F 4 pEC50 >100000 nM EC50 J. Med. Chem. (2015) 58: 718-738 [PMID:25490054]
ChEMBL Agonist activity at human dopamine D2L receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assay F 4 pEC50 >100000 nM EC50 J. Med. Chem. (2015) 58: 718-738 [PMID:25490054]

ChEMBL data shown on this page come from version 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]