A68930 [Ligand Id: 6077] activity data from GtoPdb and ChEMBL

Click here for a description of the charts and data table

Please tell us if you are using this feature and what you think!

ChEMBL ligand: CHEMBL86931 (A-70108)
  • β1-adrenoceptor/Beta-1 adrenergic receptor in Rat [ChEMBL: CHEMBL3252] [GtoPdb: 28] [UniProtKB: P18090]
  • This target only has 1 pki data point
  • 5
1 CHEMBL86931_lig_chart_1 Beta-1 adrenergic receptor Rat
There should be some charts here, you may need to enable JavaScript!
  • D1 receptor/Dopamine D1 receptor in Human [ChEMBL: CHEMBL2056] [GtoPdb: 214] [UniProtKB: P21728]
  • D1 receptor/Dopamine D1 receptor in Rat [ChEMBL: CHEMBL265] [GtoPdb: 214] [UniProtKB: P18901]
  • 8.66
2 CHEMBL86931_lig_chart_2 Dopamine D1 receptor HumanRat
There should be some charts here, you may need to enable JavaScript!
  • D2 receptor/Dopamine D2 receptor in Rat [ChEMBL: CHEMBL339] [GtoPdb: 215] [UniProtKB: P61169]
  • 6.1
3 CHEMBL86931_lig_chart_3 Dopamine D2 receptor Rat
There should be some charts here, you may need to enable JavaScript!
  • 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Rat [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327]
  • This target only has 1 pki data point
  • 5.59
4 CHEMBL86931_lig_chart_4 Serotonin 1a (5-HT1a) receptor Rat
There should be some charts here, you may need to enable JavaScript!
  • 5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Rat [ChEMBL: CHEMBL324] [GtoPdb: 8] [UniProtKB: P08909]
  • This target only has 1 pki data point
  • 5
5 CHEMBL86931_lig_chart_5 Serotonin 2c (5-HT2c) receptor Rat
There should be some charts here, you may need to enable JavaScript!
  • D5 receptor in Human [GtoPdb: 218] [UniProtKB: P21918]
  • This target only has 0 pki data point
  • 0
6 CHEMBL86931_lig_chart_6 D5 receptor Human
There should be some charts here, you may need to enable JavaScript!
DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
β1-adrenoceptor/Beta-1 adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3252] [GtoPdb: 28] [UniProtKB: P18090]
ChEMBL Binding affinity towards beta-1 adrenergic receptor using [3H]iodocyanopindolol as radioligand in competitive binding assay B 5 pKi >10000 nM Ki J. Med. Chem. (1991) 34: 2561-2569 [PMID:1652023]
D1 receptor/Dopamine D1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2056] [GtoPdb: 214] [UniProtKB: P21728]
GtoPdb - - 6.82 pEC50 151.1 nM EC50 Pharmacol Biochem Behav (2005) 82: 495-505 [PMID:16318870]
ChEMBL Formation of cAMP on Dopamine receptor D1 in vitro in carp retina F 8.68 pEC50 2.1 nM EC50 J. Med. Chem. (1990) 33: 2948-2950 [PMID:1977907]
ChEMBL Formation of cAMP on Dopamine receptor D1 in vitro in carp retina F 8.68 pEC50 2.1 nM EC50 J. Med. Chem. (1990) 33: 2948-2950 [PMID:1977907]
ChEMBL Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina F 8.71 pEC50 1.95 nM EC50 J. Med. Chem. (1991) 34: 2561-2569 [PMID:1652023]
ChEMBL Formation of cAMP on Dopamine receptor D1 in vitro in carp retina F 8.71 pEC50 1.95 nM EC50 J. Med. Chem. (1990) 33: 2948-2950 [PMID:1977907]
ChEMBL Formation of cAMP on Dopamine receptor D1 in vitro in carp retina F 8.71 pEC50 1.95 nM EC50 J. Med. Chem. (1990) 33: 2948-2950 [PMID:1977907]
D1 receptor/Dopamine D1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL265] [GtoPdb: 214] [UniProtKB: P18901]
ChEMBL Binding affinity for dopamine receptor D1 B 8.52 pKi 3 nM Ki J. Med. Chem. (1991) 34: 2946-2953 [PMID:1833546]
ChEMBL Binding affinity was determined by measuring the ability to displace [125I]SCH-23982 from Dopamine receptor D1 in rat caudate (in vitro) B 8.52 pKi 3 nM Ki J. Med. Chem. (1990) 33: 2948-2950 [PMID:1977907]
ChEMBL Binding affinity was determined by measuring the ability to displace [125I]SCH-23982 from Dopamine receptor D1 in rat caudate (in vitro) B 8.52 pKi 3 nM Ki J. Med. Chem. (1990) 33: 2948-2950 [PMID:1977907]
ChEMBL Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1 B 8.8 pKi 1.6 nM Ki J. Med. Chem. (1991) 34: 2561-2569 [PMID:1652023]
ChEMBL Binding affinity was determined by measuring the ability to displace [125I]SCH-23982 from Dopamine receptor D1 in rat caudate (in vitro) B 8.8 pKi 1.6 nM Ki J. Med. Chem. (1990) 33: 2948-2950 [PMID:1977907]
ChEMBL Binding affinity was determined by measuring the ability to displace [125I]SCH-23982 from Dopamine receptor D1 in rat caudate (in vitro) B 8.8 pKi 1.6 nM Ki J. Med. Chem. (1990) 33: 2948-2950 [PMID:1977907]
ChEMBL Effective concentration was determined for the adenylate cyclase activity in rat striatal tissue as a measure of Dopamine receptor D1 functional activity F 8.71 pEC50 1.95 nM EC50 J. Med. Chem. (1996) 39: 285-296 [PMID:8568818]
D2 receptor/Dopamine D2 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL339] [GtoPdb: 215] [UniProtKB: P61169]
ChEMBL Binding affinity using [3H]-spiperone radioligand competitive binding assay against dopamine receptor D2 B 6.09 pKi 807 nM Ki J. Med. Chem. (1991) 34: 2561-2569 [PMID:1652023]
ChEMBL Binding affinity was determined by measuring the ability to displace [125I]N-(p-aminophenethyl)-spiroperidol from Dopamine receptor D2 in rat caudate (in vitro) B 6.09 pKi 807 nM Ki J. Med. Chem. (1990) 33: 2948-2950 [PMID:1977907]
ChEMBL Binding affinity was determined by measuring the ability to displace [125I]N-(p-aminophenethyl)-spiroperidol from Dopamine receptor D2 in rat caudate (in vitro) B 6.09 pKi 807 nM Ki J. Med. Chem. (1990) 33: 2948-2950 [PMID:1977907]
ChEMBL Binding affinity for dopamine receptor D2 B 6.11 pKi 776 nM Ki J. Med. Chem. (1991) 34: 2946-2953 [PMID:1833546]
ChEMBL Binding affinity was determined by measuring the ability to displace [125I]N-(p-aminophenethyl)-spiroperidol from Dopamine receptor D2 in rat caudate (in vitro) B 6.11 pKi 776 nM Ki J. Med. Chem. (1990) 33: 2948-2950 [PMID:1977907]
ChEMBL Binding affinity was determined by measuring the ability to displace [125I]N-(p-aminophenethyl)-spiroperidol from Dopamine receptor D2 in rat caudate (in vitro) B 6.11 pKi 776 nM Ki J. Med. Chem. (1990) 33: 2948-2950 [PMID:1977907]
ChEMBL Concentration required to inhibit 50% dopamine receptor D2 in a cell free homogenate of intermediate lobe of pituitary gland F 4.99 pEC50 10200 nM EC50 J. Med. Chem. (1991) 34: 2561-2569 [PMID:1652023]
ChEMBL Formation of cAMP on Dopamine receptor D2 in vitro in rat intermediate lobe F 4.99 pEC50 10200 nM EC50 J. Med. Chem. (1990) 33: 2948-2950 [PMID:1977907]
ChEMBL Formation of cAMP on Dopamine receptor D2 in vitro in rat intermediate lobe F 4.99 pEC50 10200 nM EC50 J. Med. Chem. (1990) 33: 2948-2950 [PMID:1977907]
ChEMBL Formation of cAMP on Dopamine receptor D2 in vitro in rat intermediate lobe F 5.41 pEC50 3910 nM EC50 J. Med. Chem. (1990) 33: 2948-2950 [PMID:1977907]
ChEMBL Formation of cAMP on Dopamine receptor D2 in vitro in rat intermediate lobe F 5.41 pEC50 3910 nM EC50 J. Med. Chem. (1990) 33: 2948-2950 [PMID:1977907]
5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327]
ChEMBL Binding affinity towards 5-hydroxytryptamine 1A receptor using [3H]8-OH-DPAT as radioligand in competitive binding assay B 5.59 pKi 2550 nM Ki J. Med. Chem. (1991) 34: 2561-2569 [PMID:1652023]
5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL324] [GtoPdb: 8] [UniProtKB: P08909]
ChEMBL Binding affinity towards 5-hydroxytryptamine 1C receptor using [125 I]-SCH23982 as radioligand in competitive binding assay B 5 pKi >10000 nM Ki J. Med. Chem. (1991) 34: 2561-2569 [PMID:1652023]
D5 receptor in Human [GtoPdb: 218] [UniProtKB: P21918]
GtoPdb - - 6.6 pEC50 251.4 nM EC50 Pharmacol Biochem Behav (2005) 82: 495-505 [PMID:16318870]

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]