A68930 [Ligand Id: 6077] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL86931 (A-70108) |
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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 33:
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]
