fananserin [Ligand Id: 5434] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL83894 (Fananserin, RP 62203, RP-62203)
  • D2 receptor/Dopamine D2 receptor in Human [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
  • D2 receptor/Dopamine D2 receptor in Rat [ChEMBL: CHEMBL339] [GtoPdb: 215] [UniProtKB: P61169]
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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 Rat [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327]
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  • 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223]
  • 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Rat [ChEMBL: CHEMBL322] [GtoPdb: 6] [UniProtKB: P14842]
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  • 5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335]
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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 towards D2 dopamine receptor. B 6 pKi >1000 nM Ki J Med Chem (2001) 44: 477-501 [PMID:11170639]
ChEMBL Binding affinity for displacement of [3H]spiperone to human dopamine D2 (hD2) receptors stably expressed in CHO cells B 6.74 pKi 180 nM Ki J Med Chem (2002) 45: 492-503 [PMID:11784153]
D2 receptor/Dopamine D2 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL339] [GtoPdb: 215] [UniProtKB: P61169]
ChEMBL Binding constant against dopamine receptor D2 (in vivo) B 6 pKi >1000 nM Ki J Med Chem (1991) 34: 2477-2483 [PMID:1908521]
ChEMBL Displacement of [3H]spiperone from dopamine D2 receptor in Sprague-Dawley rat striatal membranes incubated for 40 mins B 6 pKi >1000 nM Ki Bioorg Med Chem (2019) 27: 3396-3407 [PMID:31253535]
ChEMBL The concentration required to inhibit [3H]spiperone binding to dopamine receptor D2 in rat brain membranes (in vitro) B 6 pIC50 >1000 nM IC50 J Med Chem (1991) 34: 2477-2483 [PMID:1908521]
D4 receptor/Dopamine D4 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL219] [GtoPdb: 217] [UniProtKB: P21917]
ChEMBL Binding affinity towards human dopamine receptor D4 B 8.54 pKi 2.9 nM Ki J Med Chem (2001) 44: 477-501 [PMID:11170639]
ChEMBL Displacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cells B 8.54 pKi 2.9 nM Ki Bioorg Med Chem Lett (2005) 15: 5253-5256 [PMID:16168646]
Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809]
ChEMBL Displacement of [3H]-dofetilide to HEK cells stably expressing hERG voltage-gated IKr potassium channel Kv11.1 B 6.7 pKi 200 nM Ki J Med Chem (2002) 45: 492-503 [PMID:11784153]
ChEMBL Inhibition of human ERG channel B 6.7 pKi 200 nM Ki J Med Chem (2009) 52: 4266-4276 [PMID:19534531]
Histamine H1 receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3943] [UniProtKB: P31389]
ChEMBL Binding constant against histamine H1 receptor (in vivo) B 7.6 pKi 25 nM Ki J Med Chem (1991) 34: 2477-2483 [PMID:1908521]
5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327]
ChEMBL Binding constant against 5-hydroxytryptamine 1A receptor (in vivo) B 7.15 pKi 70 nM Ki J Med Chem (1991) 34: 2477-2483 [PMID:1908521]
ChEMBL Displacement of [3H]-8-OH-DPAT from 5HT1A receptor in rat hippocampal membranes preincubated for 5 mins followed by addition of [3H]-8-OHDPAT and measured after 10 mins B 7.15 pKi 70 nM Ki Bioorg Med Chem (2019) 27: 3396-3407 [PMID:31253535]
5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223]
ChEMBL Displacement of [3H]ketanserin from cloned human 5HT2A receptor in HEK298 cells B 9.43 pKi 0.37 nM Ki Bioorg Med Chem Lett (2005) 15: 5253-5256 [PMID:16168646]
ChEMBL Binding affinity for displacement of [3H]ketanserin to human 5-hydroxytryptamine 2A receptor stably expressed in CHO cells B 10.4 pKi 0.04 nM Ki J Med Chem (2002) 45: 492-503 [PMID:11784153]
ChEMBL Binding affinity for human 5-hydroxytryptamine 2A receptor B 10.4 pKi 0.04 nM Ki J Med Chem (2001) 44: 477-501 [PMID:11170639]
5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL322] [GtoPdb: 6] [UniProtKB: P14842]
ChEMBL Binding affinity for displacement of [3H]ketanserin to rat 5-hydroxytryptamine 2A receptor stably expressed in CHO cells B 10.22 pKi 0.06 nM Ki J Med Chem (2002) 45: 492-503 [PMID:11784153]
ChEMBL Displacement of [3H]ketanserin from 5HT2A receptor in rat cortical membranes incubated for 15 mins by liquid scintillation spectrometry B 10.22 pKi 0.06 nM Ki Bioorg Med Chem (2019) 27: 3396-3407 [PMID:31253535]
5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335]
ChEMBL Binding affinity for displacement of [3H]mesulergine to human 5-hydroxytryptamine 2C receptor stably expressed in CHO cells B 9 pKi 1 nM Ki J Med Chem (2002) 45: 492-503 [PMID:11784153]

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]