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ChEMBL ligand: CHEMBL27441 |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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D2 receptor/Dopamine D2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416] | ||||||||
ChEMBL | Binding affinity was measured at cloned mammalian dopamine D2 receptor expressed in CHO-K1 cells (using [3H]U-86170) | B | 6.84 | pKi | 145 | nM | Ki | Bioorg Med Chem Lett (1994) 4: 689-694 |
ChEMBL | Compound was tested for agonistic activity against D2 receptor from cloned CHO cells, used [3H]U-86170 as radioligand | F | 7.85 | pKi | 14 | nM | Ki | J Med Chem (1993) 36: 1301-1315 [PMID:8496900] |
Dopamine D2 receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3998] [UniProtKB: P20288] | ||||||||
ChEMBL | Evaluated for binding towards Dopamine receptor D2 using [3H]-spiperone as radioligand, in cloned mammalian receptors expressed in CHO-K1 cells | B | 6.8 | pKi | 158 | nM | Ki | J Med Chem (1993) 36: 3188-3196 [PMID:8230107] |
ChEMBL | Binding towards Dopamine receptor D2 expressed in CHO-K1 cells using [3H]U-86170 | B | 6.84 | pKi | 145 | nM | Ki | J Med Chem (1993) 36: 3188-3196 [PMID:8230107] |
D2 receptor/Dopamine D2 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL339] [GtoPdb: 215] [UniProtKB: P61169] | ||||||||
ChEMBL | Binding towards Dopamine receptor D2 using [3H]spiperone from rat striatal membrane | B | 6.28 | pKi | 530 | nM | Ki | J Med Chem (1993) 36: 3188-3196 [PMID:8230107] |
ChEMBL | Evaluated for binding towards Dopamine receptor D2 using [3H]N-0437 as radioligand from rat striatal membrane | B | 6.52 | pKi | 300 | nM | Ki | J Med Chem (1993) 36: 3188-3196 [PMID:8230107] |
ChEMBL | Compound was tested for antagonistic activity against D2 receptor from rat striatum, used [3H]raclopride as radioligand | F | 6.75 | pKi | 179 | nM | Ki | J Med Chem (1993) 36: 1301-1315 [PMID:8496900] |
D3 receptor/Dopamine D3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462] | ||||||||
GtoPdb | - | - | 6.2 | pKi | - | - | - |
Eur J Pharmacol (1992) 225: 331-7 [PMID:1354163]; J Pharmacol Exp Ther (1995) 275: 885-898 [PMID:7473180] |
ChEMBL | Displacement of [125I]iodosulpiride from human Dopamine receptor D3 expressed in CHO cells | B | 7.15 | pKi | 70 | nM | Ki | J Med Chem (2003) 46: 4377-4392 [PMID:14521403] |
ChEMBL | Binding towards Dopamine receptor D3 expressed in CHO-K1 cells using [3H]spiperone | B | 7.59 | pKi | 26 | nM | Ki | J Med Chem (1993) 36: 3188-3196 [PMID:8230107] |
ChEMBL | Binding affinity was measured at cloned mammalian dopamine D3 receptor expressed in CHO-K1 cells (using [3H]- spiperone) | B | 7.59 | pKi | 26 | nM | Ki | Bioorg Med Chem Lett (1994) 4: 689-694 |
D3 receptor in Rat [GtoPdb: 216] [UniProtKB: P19020] | ||||||||
GtoPdb | - | - | 6 | pKi | - | - | - | Nature (1990) 347: 146-51 [PMID:1975644] |
D4 receptor/Dopamine D4 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL219] [GtoPdb: 217] [UniProtKB: P21917] | ||||||||
ChEMBL | Binding towards dopamine receptor D4 expressed in CHO-K1 cells using [3H]spiperone | B | 6.93 | pKi | 117 | nM | Ki | J Med Chem (1993) 36: 3188-3196 [PMID:8230107] |
ChEMBL | Binding affinity was measured at cloned mammalian dopamine D4 receptor expressed in CHO-K1 cells (using [3H]- spiperone) | B | 6.93 | pKi | 117 | nM | Ki | Bioorg Med Chem Lett (1994) 4: 689-694 |
5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908] | ||||||||
ChEMBL | Binding affinity against 5-hydroxytryptamine 1A receptor from bovine hippocampus, used [3H]8-OH-DPAT as radioligand | B | 6.39 | pKi | 410 | nM | Ki | J Med Chem (1993) 36: 1301-1315 [PMID:8496900] |
5-HT5A receptor/Serotonin 5a (5-HT5a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3426] [GtoPdb: 10] [UniProtKB: P47898] | ||||||||
ChEMBL | Binding affinity was measured at cloned mammalian 5-HT1A receptor expressed in CHO-K1 cells (using [3H]8-OH-DPAT ) | B | 5.63 | pKi | 2331 | nM | Ki | Bioorg Med Chem Lett (1994) 4: 689-694 |
ChEMBL data shown on this page come from version 35:
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]