SKF-83566 [Ligand Id: 944] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL324017 (SK-83566, SK&F-83566) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| adenylyl cyclase 2/Adenylate cyclase type II in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3760] [GtoPdb: 1279] [UniProtKB: Q08462] | ||||||||
| ChEMBL | Inhibition of human adenylate cyclase 2 expressed in ACdelta 3/6 knockout HEK293 cells assessed as cyclic AMP accumulation incubated for 30 min followed by FSK stimulation by HTR-FRET assay | B | 5.24 | pIC50 | 5710 | nM | IC50 | Bioorg Med Chem (2023) 95: 117508-117508 [PMID:37931521] |
| D1 receptor/Dopamine D1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2056] [GtoPdb: 214] [UniProtKB: P21728] | ||||||||
| GtoPdb | - | - | 9.5 | pKi | - | - | - | Nature (1991) 350: 614-9 [PMID:1826762] |
| ChEMBL | Binding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkey | B | 9.52 | pKi | 0.3 | nM | Ki | J Med Chem (1991) 34: 3235-3241 [PMID:1956042] |
| ChEMBL | Inhibition of human D1 receptor expressed in HEK293 cells assessed as cyclic AMP accumulation incubated for 1 hr in presence of dopamine by HTR-FRET assay | F | 5.65 | pIC50 | 2240 | nM | IC50 | Bioorg Med Chem (2023) 95: 117508-117508 [PMID:37931521] |
| D2 receptor/Dopamine D2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416] | ||||||||
| ChEMBL | Binding affinity against dopamine receptor D2 by using [3H]spiperone as radioligand in caudate-putamen of monkey | B | 5.87 | pKi | 1360 | nM | Ki | J Med Chem (1991) 34: 3235-3241 [PMID:1956042] |
| D5 receptor/Dopamine D5 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1850] [GtoPdb: 218] [UniProtKB: P21918] | ||||||||
| ChEMBL | Displacement of [3H]SCH23390 from dopamine D5 receptor (unknown origin) | B | 8.4 | pKi | 3.95 | nM | Ki | Bioorg Med Chem Lett (2020) 30: 127305-127305 [PMID:32631525] |
| ChEMBL | Binding affinity to human D5 receptor | B | 8.64 | pKi | 2.3 | nM | Ki | Bioorg Med Chem Lett (2020) 30: 127053-127053 [PMID:32107165] |
| ChEMBL | Displacement of [3H]SCH23390 from dopamine D5 receptor (unknown origin) | B | 8.76 | pKi | 1.75 | nM | Ki | Bioorg Med Chem Lett (2021) 42: 128047-128047 [PMID:33882273] |
| GtoPdb | - | - | 9.4 | pKi | - | - | - | Nature (1991) 350: 614-9 [PMID:1826762] |
ChEMBL data shown on this page come from version 34:
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]
