(+)-AJ76 [Ligand Id: 970] activity data from GtoPdb and ChEMBL
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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 |
|---|---|---|---|---|---|---|---|---|
| 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 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]
