A68930 [Ligand Id: 6077] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL86931 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| 5-HT1A receptor/5-hydroxytryptamine receptor 1A 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/5-hydroxytryptamine receptor 2C 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] |
| 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/D(1A) dopamine 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/D(1A) dopamine 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/D(2) dopamine 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] |
| 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 36:
Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
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]
