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

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ChEMBL ligand: CHEMBL86931 (A-70108)
  • β1-adrenoceptor/Beta-1 adrenergic receptor in Rat [ChEMBL: CHEMBL3252] [GtoPdb: 28] [UniProtKB: P18090]
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  • 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]
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  • D2 receptor/Dopamine D2 receptor in Rat [ChEMBL: CHEMBL339] [GtoPdb: 215] [UniProtKB: P61169]
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  • 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Rat [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327]
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  • 5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Rat [ChEMBL: CHEMBL324] [GtoPdb: 8] [UniProtKB: P08909]
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  • D5 receptor in Human [GtoPdb: 218] [UniProtKB: P21918]
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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 32:

Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]