CGS 15943 [Ligand Id: 384] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL16687 (CGS-15943)
  • 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]
  • Adenosine A1 receptor in Guinea pig [ChEMBL: CHEMBL2304404] [UniProtKB: P47745]
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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]
  • A2B receptor in Mouse [GtoPdb: 20] [UniProtKB: Q60614]
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  • A3 receptor/Adenosine A3 receptor in Human [ChEMBL: CHEMBL256] [GtoPdb: 21] [UniProtKB: P0DMS8]
  • A3 receptor/Adenosine A3 receptor in Rat [ChEMBL: CHEMBL3360] [GtoPdb: 21] [UniProtKB: P28647]
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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 7.12 pKd 75.38 nM Kd K4DD drug target binding kinetics data
ChEMBL Binding affinity for human Adenosine A1 receptor from HEK293 cells B 8.35 pKi 4.5 nM Ki J. Med. Chem. (1996) 39: 4142-4148 [PMID:8863790]
ChEMBL Displacement of [3H]DPCPX from human adenosine A1 receptor expressed in CHO cells; range 4.1-4.7 B 8.36 pKi 4.4 nM Ki J. Med. Chem. (2000) 43: 4768-4780 [PMID:11123985]
GtoPdb - - 8.46 pKi 3.5 nM Ki Naunyn Schmiedebergs Arch. Pharmacol. (1999) 359: 7-10 [PMID:9933143]
A1 receptor/Adenosine A1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL318] [GtoPdb: 18] [UniProtKB: P25099]
ChEMBL Tested for the displacement [3H]PIA from Adenosine A1 receptor in rat brain membrane B 4.68 pKi 21000 nM Ki J. Med. Chem. (1996) 39: 398-406 [PMID:8558508]
ChEMBL Binding affinity was determined in radioligand binding assay at rat brain adenosine A1 receptor vs [3H]R-PIA B 7.68 pKi 21 nM Ki J. Med. Chem. (1998) 41: 2835-2845 [PMID:9667972]
ChEMBL Displacement of [3H]DPCPX binding to adenosine A1 receptor of rat brain cortical membrane B 7.68 pKi 21 nM Ki J. Med. Chem. (2001) 44: 749-762 [PMID:11262085]
ChEMBL Inhibition of [3H]CHA binding to Adenosine A1 receptor in rat brain membranes B 7.68 pKi 21 nM Ki J. Med. Chem. (1990) 33: 1708-1713 [PMID:2342066]
ChEMBL Binding affinity against adenosine A1 receptor using [3H]-CHA or [3H]PIA as radioligand B 7.68 pKi 21 nM Ki J. Med. Chem. (1992) 35: 407-422 [PMID:1738138]
ChEMBL Binding affinity towards adenosine A1 receptor in rat whole brain membranes using N6-[3H]cyclohexyladenosine B 7.69 pKi 20.5 nM Ki J. Med. Chem. (1992) 35: 3066-3075 [PMID:1501234]
GtoPdb - - 8.19 pKi 6.4 nM Ki Drugs Future (2000) : 1043-1052
ChEMBL Binding ability of adenosine A1 receptor by using [3H]CHA as radioligand in rat whole brain homogenate B 8.19 pKi 6.4 nM Ki Bioorg. Med. Chem. Lett. (1994) 4: 2539-2544
ChEMBL Displacement of [3H]CHA from rat cortical membrane Adenosine A1 receptor. Parenthesis indicate 95% confidence limit. B 8.19 pKi 6.4 nM Ki J. Med. Chem. (1998) 41: 2126-2133 [PMID:9622554]
ChEMBL Inhibition of [3H]-CHA binding to Adenosine A1 receptor in rat whole brain homogenates. B 8.19 pKi 6.4 nM Ki J. Med. Chem. (1996) 39: 1164-1171 [PMID:8676354]
ChEMBL Inhibition of rat recombinant adenosine A1 receptor B 8.46 pKi 3.5 nM Ki J. Med. Chem. (2014) 57: 3623-3650 [PMID:24164628]
ChEMBL Binding affinity for Adenosine A1 receptor from rat cerebral cortex membranes using [3H](R)-PIA B 7.68 pIC50 21 nM IC50 J. Med. Chem. (1996) 39: 4142-4148 [PMID:8863790]
ChEMBL Binding affinity towards the adenosine A1 receptor in cerebral cortices of Sprague-Dawley male rats using [3H]CHA as radioligand. B 8.22 pIC50 6 nM IC50 J. Med. Chem. (1990) 33: 2240-2254 [PMID:2374150]
Adenosine A1 receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2304404] [UniProtKB: P47745]
ChEMBL Binding affinity against adenosine A1 receptor in guinea pig forebrain membranes using N6-[3H]cyclohexyladenosine as radioligand B 8 pKi 10 nM Ki J. Med. Chem. (1992) 35: 3066-3075 [PMID:1501234]
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 8.49 pKd 3.24 nM Kd K4DD drug target binding kinetics data
ChEMBL Displacement of [3H]ZM241385 from human recombinant adenosine A2A receptor expressed in in human HeLa cell membrane B 8.64 pKi 2.27 nM Ki Bioorg. Med. Chem. (2010) 18: 2081-2088 [PMID:20202853]
ChEMBL Binding affinity for human Adenosine A2A receptor from HEK293 cells B 8.77 pKi 1.7 nM Ki J. Med. Chem. (1996) 39: 4142-4148 [PMID:8863790]
ChEMBL Binding affinity against S277E human adenosine A2A receptor expressed in CHO cells using [3H]- ZM-241385 B 9 pKi 1 nM Ki J. Med. Chem. (2003) 46: 4847-4859 [PMID:14584936]
ChEMBL Binding affinity against T88D human adenosine A2A receptor expressed in CHO cells using [3H]- ZM-241385 B 9.04 pKi 0.91 nM Ki J. Med. Chem. (2003) 46: 4847-4859 [PMID:14584936]
ChEMBL Binding affinity for HA-tagged mutant human Adenosine A2A receptor (V84L), using [3H]CGS-21680 as radioligand expressed in COS-7 cells B 9.07 pKi 0.84 nM Ki J. Med. Chem. (1997) 40: 2588-2595 [PMID:9258366]
ChEMBL Binding affinity against WT human adenosine A2A receptor expressed in CHO cells using [3H]- ZM-241385 B 9.08 pKi 0.84 nM Ki J. Med. Chem. (2003) 46: 4847-4859 [PMID:14584936]
ChEMBL Binding affinity against T88E human adenosine A2A receptor expressed in CHO cells using [3H]- ZM-241385 B 9.17 pKi 0.67 nM Ki J. Med. Chem. (2003) 46: 4847-4859 [PMID:14584936]
ChEMBL Binding affinity against H278E human adenosine A2A receptor expressed in CHO cells using [3H]- ZM-241385 B 9.28 pKi 0.52 nM Ki J. Med. Chem. (2003) 46: 4847-4859 [PMID:14584936]
ChEMBL Binding affinity for HA-tagged mutant human Adenosine A2A receptor (H250N) using [3H]-CGS-21,680 as radioligand expressed in COS-7 cells B 9.34 pKi 0.46 nM Ki J. Med. Chem. (1997) 40: 2588-2595 [PMID:9258366]
ChEMBL Displacement of [3H]-SCH- 58261 from human adenosine A2A receptor expressed in CHO cells; range 0.37-0.49 B 9.37 pKi 0.43 nM Ki J. Med. Chem. (2000) 43: 4768-4780 [PMID:11123985]
ChEMBL Binding affinity against H278D human adenosine A2A receptor stably transfected in CHO cells using [3H]- ZM-241385 as radioligand. B 9.39 pKi 0.41 nM Ki J. Med. Chem. (2003) 46: 4847-4859 [PMID:14584936]
ChEMBL Binding affinity to human adenosine A2A receptor B 9.4 pKi 0.4 nM Ki J. Med. Chem. (2008) 51: 4449-4455 [PMID:18637670]
GtoPdb - - 9.4 pKi - - - Naunyn Schmiedebergs Arch. Pharmacol. (1998) 357: 1-9 [PMID:9459566];
Naunyn Schmiedebergs Arch. Pharmacol. (1999) 359: 7-10 [PMID:9933143];
J. Biol. Chem. (1995) 270: 13987-97 [PMID:7775460];
Br. J. Pharmacol. (1997) 121: 353-60 [PMID:9179373]
ChEMBL Binding affinity against Q89D human adenosine A2A receptor expressed in CHO cells using [3H]- ZM-241385 B 9.46 pKi 0.35 nM Ki J. Med. Chem. (2003) 46: 4847-4859 [PMID:14584936]
ChEMBL Binding affinity for HA-tagged wild type human Adenosine A2A receptor (WT) using [3H]CGS-21680 as radioligand expressed in COS-7 cells B 9.85 pKi 0.14 nM Ki J. Med. Chem. (1997) 40: 2588-2595 [PMID:9258366]
ChEMBL Inhibition of 1 uM NECA-stimulated cyclic AMP levels in human platelets F 7.92 pIC50 12 nM IC50 J. Med. Chem. (1998) 41: 2126-2133 [PMID:9622554]
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 5.48 pKi 3300 nM Ki J. Med. Chem. (1996) 39: 398-406 [PMID:8558508]
ChEMBL Displacement of [3H]ZM-241385 binding in adenosine A2A receptor of rat striatal membrane B 8.48 pKi 3.3 nM Ki J. Med. Chem. (2001) 44: 749-762 [PMID:11262085]
ChEMBL Binding affinity was determined in radioligand binding assay at rat striatal Adenosine A2A receptor vs [3H]-CGS- 21680 B 8.48 pKi 3.3 nM Ki J. Med. Chem. (1998) 41: 2835-2845 [PMID:9667972]
ChEMBL Inhibition of [3H]-CGS- 21680 binding to Adenosine A2A receptor in rat striatal homogenates. B 8.92 pKi 1.2 nM Ki J. Med. Chem. (1996) 39: 1164-1171 [PMID:8676354]
ChEMBL Displacement of [3H]-CGS- from Adenosine A2a receptor of rat striatal homogenate B 8.92 pKi 1.2 nM Ki Bioorg. Med. Chem. Lett. (1994) 4: 2539-2544
ChEMBL Displacement of [3H]-CGS- 21680 from rat striatal membranes Adenosine A2A receptor. Parenthesis indicate 95% confidence limits. B 9.02 pKi 0.95 nM Ki J. Med. Chem. (1998) 41: 2126-2133 [PMID:9622554]
ChEMBL Inhibition of rat recombinant adenosine receptor A2a B 9.4 pKi 0.4 nM Ki J. Med. Chem. (2014) 57: 3623-3650 [PMID:24164628]
ChEMBL Binding affinity for Adenosine A2A receptor from rat striatal membranes using [3H]-CGH 21680 B 8.48 pIC50 3.3 nM IC50 J. Med. Chem. (1996) 39: 4142-4148 [PMID:8863790]
A2B receptor/Adenosine A2b receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL255] [GtoPdb: 20] [UniProtKB: P29275]
ChEMBL pA2 value at human Adenosine A2B receptor from Schild plots with slopes approaching unity B 8 pKd 10 nM Kd J. Med. Chem. (1998) 41: 2835-2845 [PMID:9667972]
ChEMBL Inhibition of human recombinant adenosine receptor A2b B 7.36 pKi 44 nM Ki J. Med. Chem. (2014) 57: 3623-3650 [PMID:24164628]
ChEMBL Displacement of [3H]MRS-1754 from human recombinant adenosine A2B receptor expressed in HEK293 cells B 7.47 pKi 34.2 nM Ki J. Med. Chem. (2009) 52: 3994-4006 [PMID:19569717]
ChEMBL Displacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells B 7.52 pKi 30 nM Ki J. Med. Chem. (2009) 52: 3994-4006 [PMID:19569717]
ChEMBL Displacement of [3H]DPCPX from Adenosine A2b receptor expressed in CHO cells; range 18-29 B 7.64 pKi 23 nM Ki J. Med. Chem. (2000) 43: 4768-4780 [PMID:11123985]
ChEMBL Displacement of [125I]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cells B 7.79 pKi 16.4 nM Ki J. Med. Chem. (2009) 52: 3994-4006 [PMID:19569717]
ChEMBL Displacement of [3H]MRE-2029F20 from human recombinant adenosine A2B receptor expressed in HEK293 cells B 8.01 pKi 9.8 nM Ki J. Med. Chem. (2009) 52: 3994-4006 [PMID:19569717]
GtoPdb - - 8.1 pKi - - - Naunyn Schmiedebergs Arch. Pharmacol. (1998) 357: 1-9 [PMID:9459566];
Naunyn Schmiedebergs Arch. Pharmacol. (1999) 359: 7-10 [PMID:9933143];
Biochem. Pharmacol. (2001) 61: 657-63 [PMID:11266650];
Biochem. Pharmacol. (2004) 68: 305-12 [PMID:15194002];
Drug Des Discov (1999) 16: 217-26 [PMID:10624567];
J. Pharmacol. Exp. Ther. (2009) 329: 2-13 [PMID:19141710]
ChEMBL Inhibition of 50 uM 5`-(N-ethylcarboxamido)adenosine induced cAMP production in CHO cell line expressing human Adenosine A2B receptor B 5.92 pIC50 1200 nM IC50 J. Med. Chem. (1998) 41: 2835-2845 [PMID:9667972]
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 7.22 pIC50 60.7 nM IC50 J Med Chem (2018) 61: 4301-4316 [PMID:29681156]
GtoPdb - - 7.8 pA2 - - - Br. J. Pharmacol. (1996) 119: 1286-90 [PMID:8937736]
A2B receptor in Mouse [GtoPdb: 20] [UniProtKB: Q60614]
GtoPdb - - 8.04 pKi 9.07 nM Ki J. Pharmacol. Exp. Ther. (2009) 329: 2-13 [PMID:19141710]
A3 receptor/Adenosine A3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL256] [GtoPdb: 21] [UniProtKB: P0DMS8]
ChEMBL Displacement of [3H]MRE3008-F20 from human adenosine A3 receptor expressed in CHO cells after 120 mins B 4.07 pKi 84918.05 nM Ki Bioorg. Med. Chem. Lett. (2011) 21: 818-823 [PMID:21163647]
ChEMBL Binding affinity at Mutant (H272E) human adenosine A3 receptor expressed in COS-7 cells B 5.49 pKi 3260 nM Ki J. Med. Chem. (2001) 44: 4125-4136 [PMID:11708915]
ChEMBL Binding affinity at wild-type Adenosine A3 receptor expressed in COS-7 cells B 6.6 pKi 253 nM Ki J. Med. Chem. (2001) 44: 4125-4136 [PMID:11708915]
ChEMBL Binding affinity by its ability to displace [125I]AB-MECA from human adenosine A3 receptor expressed in HEK 293 cells B 6.84 pKi 143 nM Ki J. Med. Chem. (2000) 43: 2227-2238 [PMID:10841801]
ChEMBL Displacement of specific [125I]AB-MECA binding at human adenosine A3 receptor expressed in HEK 293 cells. B 6.84 pKi 143 nM Ki J. Med. Chem. (1998) 41: 3987-3993 [PMID:9767636]
ChEMBL Displacement of [125I]AB-MECA from human adenosine A3 receptor expressed in HEK 293 cells B 6.85 pKi 140 nM Ki J. Med. Chem. (2001) 44: 749-762 [PMID:11262085]
ChEMBL Inhibition of human recombinant adenosine A3 receptor B 7.02 pKi 95 nM Ki J. Med. Chem. (2014) 57: 3623-3650 [PMID:24164628]
ChEMBL Displacement of [3H]MRE 3008F20 from human adenosine A3 receptor expressed in CHO cells B 7.07 pKi 85 nM Ki J. Med. Chem. (2006) 49: 4085-4097 [PMID:16821770]
ChEMBL Displacement of [3H]MRE3008-F20 from human adenosine A3 receptor expressed in CHO cells; range 76-95 B 7.07 pKi 85 nM Ki J. Med. Chem. (2000) 43: 4768-4780 [PMID:11123985]
ChEMBL Binding affinity for human adenosine A3 receptor B 7.07 pKi 85 nM Ki J. Med. Chem. (2005) 48: 152-162 [PMID:15634009]
ChEMBL Displacement of [125I]I-AB-MECA from human adenosine A3 receptor expressed in CHO cells after 90 mins by gamma counting analysis B 7.46 pKi 35 nM Ki Bioorg. Med. Chem. Lett. (2013) 23: 26-36 [PMID:23200243]
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 7.79 pKi 16.1 nM Ki Bioorg. Med. Chem. Lett. (2013) 23: 26-36 [PMID:23200243]
ChEMBL Displacement of [125I]AB-MECA from human Adenosine A3 receptor expressed in HEK293 cells B 7.85 pKi 14 nM Ki J. Med. Chem. (1998) 41: 2126-2133 [PMID:9622554]
ChEMBL Binding affinity at cloned human adenosine A3 receptor expressed in HEK293 cells was determined using [125I]AB-MECA as radioligand B 7.86 pKi 13.8 nM Ki J. Med. Chem. (1998) 41: 2835-2845 [PMID:9667972]
ChEMBL Antagonist activity at human adenosine A3 receptor F 7.86 pKi 13.8 nM Ki Bioorg. Med. Chem. Lett. (2011) 21: 2898-2905 [PMID:21511471]
ChEMBL Displacement of [125I]AB-MECA from human adenosine A3 receptor expressed in HEK 293 cells B 7.86 pKi 13.8 nM Ki J. Med. Chem. (1998) 41: 3987-3993 [PMID:9767636]
ChEMBL In vitro binding affinity at human Adenosine A3 receptor from HEK293 cells by [125I]AB-MECA displacement. B 7.86 pKi 13.8 nM Ki J. Med. Chem. (1996) 39: 4142-4148 [PMID:8863790]
GtoPdb - - 7.9 pKi - - - Naunyn Schmiedebergs Arch. Pharmacol. (1998) 357: 1-9 [PMID:9459566];
Naunyn Schmiedebergs Arch. Pharmacol. (1999) 359: 7-10 [PMID:9933143];
Mol. Pharmacol. (2000) 57: 968-75 [PMID:10779381];
J. Med. Chem. (1996) 39: 4142-8 [PMID:8863790]
ChEMBL Displacement of [125I]AB-MECA from human adenosine A3 receptor expressed in CHO cells B 8.1 pKi 7.9 nM Ki J. Med. Chem. (1998) 41: 3987-3993 [PMID:9767636]
ChEMBL Inhibition of cAMP accumulation in CHO cells expressing human adenosine A3 receptor F 6.39 pIC50 406 nM IC50 J. Med. Chem. (2000) 43: 4768-4780 [PMID:11123985]
A3 receptor/Adenosine A3 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3360] [GtoPdb: 21] [UniProtKB: P28647]
ChEMBL Binding affinity for Adenosine A3 receptor from rat striatal membranes B 4 pKi 100000 nM Ki J. Med. Chem. (1996) 39: 4142-4148 [PMID:8863790]
Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364]
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 W2 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 5.1 pIC50 7943.28 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 5.3 pIC50 5011.87 nM IC50 Nat. Chem. Biol. (2009) 5: 765-771 [PMID:19734910]

ChEMBL data shown on this page come from version 26:

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]