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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 | Binding affinity to 5-HT1A receptor (unknown origin) assessed as inhibition constant | B | 9 | pKi | 1 | nM | Ki | J Med Chem (2022) 65: 10755-10808 [PMID:35939391] |
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 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]