[3H]NLX-112 [Ligand Id: 3925] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL45305 (Befiradol, F-13640, F13640, NLX-112)
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  • D2 receptor/Dopamine D2 receptor in Human [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
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  • D3 receptor/Dopamine D3 receptor in Human [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462]
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  • D4 receptor/Dopamine D4 receptor in Human [ChEMBL: CHEMBL219] [GtoPdb: 217] [UniProtKB: P21917]
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  • 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908]
  • 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Rat [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327]
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  • Serotonin 2a (5-HT2a) receptor in Pig [ChEMBL: CHEMBL2490] [UniProtKB: P50129]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
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]