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ChEMBL ligand: CHEMBL45305 (Befiradol, F-13640, F13640, NLX-112) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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Dopamine D1 receptor in Pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5067] [UniProtKB: P50130] | ||||||||
ChEMBL | Displacement of [3H]SCH23390 from dopamine D1 receptor in pig cortex membranes | B | 4.59 | pKi | 26000 | nM | Ki | J Med Chem (2010) 53: 7167-7179 [PMID:20860381] |
D2 receptor/Dopamine D2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416] | ||||||||
ChEMBL | Displacement of [3H]Spiperone from human dopamine D2 short receptor | B | 4.34 | pKi | 46000 | nM | Ki | J Med Chem (2010) 53: 7167-7179 [PMID:20860381] |
ChEMBL | Displacement of [3H]Spiperone from human dopamine D2 long receptor | B | 4.82 | pKi | 15000 | nM | Ki | J Med Chem (2010) 53: 7167-7179 [PMID:20860381] |
D3 receptor/Dopamine D3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462] | ||||||||
ChEMBL | Displacement of [3H]Spiperone from human dopamine D3 receptor | B | 5 | pKi | 10000 | nM | Ki | J Med Chem (2010) 53: 7167-7179 [PMID:20860381] |
D4 receptor/Dopamine D4 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL219] [GtoPdb: 217] [UniProtKB: P21917] | ||||||||
ChEMBL | Displacement of [3H]Spiperone from human dopamine D4.4 receptor | B | 5.7 | pKi | 2000 | nM | Ki | J Med Chem (2010) 53: 7167-7179 [PMID:20860381] |
5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908] | ||||||||
GtoPdb | - | - | 8.9 | pKd | 1.4 | nM | Kd | Naunyn Schmiedebergs Arch Pharmacol (2010) 382: 321-30 [PMID:20799027] |
ChEMBL | In vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptor | F | 7.59 | pEC50 | 25.7 | nM | EC50 | J Med Chem (1999) 42: 1648-1660 [PMID:10229633] |
ChEMBL | Agonist activity at human 5HT1A receptor expressed in C6 cells assessed as stimulation of [35S]GTPgammaS binding | F | 7.63 | pEC50 | 23.44 | nM | EC50 | J Med Chem (2007) 50: 5024-5033 [PMID:17803293] |
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 in rat cortex using [3H]8-OH-DPAT as a radioligand | B | 9.07 | pKi | 0.85 | nM | Ki | J Med Chem (1999) 42: 1648-1660 [PMID:10229633] |
ChEMBL | Binding affinity to 5HT1A receptor in rat cortex membrane | B | 9.07 | pKi | 0.85 | nM | Ki | J Med Chem (2007) 50: 5024-5033 [PMID:17803293] |
Serotonin 2a (5-HT2a) receptor in Pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2490] [UniProtKB: P50129] | ||||||||
ChEMBL | Displacement of [3H]Ketanserin from 5-HT2 receptor in pig cortex membranes | B | 4.64 | pKi | 23000 | nM | Ki | J Med Chem (2010) 53: 7167-7179 [PMID:20860381] |
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]