iloperidone [Ligand Id: 87] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL14376 (HP-873, Fanapt, Iloperidone, HP 873)
  • α2A-adrenoceptor/Alpha-2a adrenergic receptor in Rat [ChEMBL: CHEMBL327] [GtoPdb: 25] [UniProtKB: P22909]
  • This target only has 0 pki data point
  • 0
1 CHEMBL14376_lig_chart_1 Alpha-2a adrenergic receptor Rat
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  • D1 receptor/Dopamine D1 receptor in Mouse [ChEMBL: CHEMBL3071] [GtoPdb: 214] [UniProtKB: Q61616]
  • This target only has 0 pki data point
  • 0
2 CHEMBL14376_lig_chart_2 Dopamine D1 receptor Mouse
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  • 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]
  • This target only has 0 pki data point
  • 0
3 CHEMBL14376_lig_chart_3 Dopamine D2 receptor HumanRat
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  • M3 receptor/Muscarinic acetylcholine receptor M3 in Rat [ChEMBL: CHEMBL320] [GtoPdb: 15] [UniProtKB: P08483]
  • This target only has 0 pki data point
  • 0
4 CHEMBL14376_lig_chart_4 Muscarinic acetylcholine receptor M3 Rat
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  • 5-HT1A receptor in Human [GtoPdb: 1] [UniProtKB: P08908]
  • 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Mouse [ChEMBL: CHEMBL3737] [GtoPdb: 1] [UniProtKB: Q64264]
  • 5-HT1A receptor in Rat [GtoPdb: 1] [UniProtKB: P19327]
  • 6.8
5 CHEMBL14376_lig_chart_5 5-HT1A receptor HumanMouseRat
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  • Serotonin 2a (5-HT2a) receptor in Bovine [ChEMBL: CHEMBL3446] [UniProtKB: Q75Z89]
  • This target only has 0 pki data point
  • 0
6 CHEMBL14376_lig_chart_6 Serotonin 2a (5-HT2a) receptor Bovine
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  • sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Human [ChEMBL: CHEMBL287] [GtoPdb: 2552] [UniProtKB: Q99720]
  • This target only has 0 pki data point
  • 0
7 CHEMBL14376_lig_chart_7 Sigma opioid receptor Human
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  • 5-HT6 receptor in Human [GtoPdb: 11] [UniProtKB: P50406]
  • 5-HT6 receptor in Rat [GtoPdb: 11] [UniProtKB: P31388]
  • 7.4
8 CHEMBL14376_lig_chart_8 5-HT6 receptor HumanRat
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  • 5-HT7 receptor in Human [GtoPdb: 12] [UniProtKB: P34969]
  • 5-HT7 receptor in Rat [GtoPdb: 12] [UniProtKB: P32305]
  • 7.7
9 CHEMBL14376_lig_chart_9 5-HT7 receptor HumanRat
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
α2A-adrenoceptor/Alpha-2a adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL327] [GtoPdb: 25] [UniProtKB: P22909]
ChEMBL Binding affinity against Alpha-1 adrenergic receptor was determined using [3H]WB-4101 radioligand B 9.4 pIC50 0.4 nM IC50 J. Med. Chem. (1995) 38: 1119-1131 [PMID:7707315]
D1 receptor/Dopamine D1 receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3071] [GtoPdb: 214] [UniProtKB: Q61616]
ChEMBL Binding affinity against Dopamine receptor D1 was determined using [3H]SCH-23390 radioligand B 6.12 pIC50 750 nM IC50 J. Med. Chem. (1995) 38: 1119-1131 [PMID:7707315]
D2 receptor/Dopamine D2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
ChEMBL Binding affinity against Dopamine receptor D2 was determined using [ [3H]-spiperone radioligand B 6.96 pIC50 110 nM IC50 J. Med. Chem. (1995) 38: 1119-1131 [PMID:7707315]
D2 receptor/Dopamine D2 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL339] [GtoPdb: 215] [UniProtKB: P61169]
ChEMBL Affinity for dopamine receptor D2 binding sites by its ability to displace [3H]spiperone from rat striatum. B 6.96 pIC50 110 nM IC50 J. Med. Chem. (1995) 38: 1119-1131 [PMID:7707315]
GtoPdb Measuring displacement of [3H]spiperone from rat striatum. - 6.96 pIC50 110 nM IC50 J Med Chem (1995) 38: 1119-31 [PMID:7707315]
M3 receptor/Muscarinic acetylcholine receptor M3 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL320] [GtoPdb: 15] [UniProtKB: P08483]
ChEMBL Binding affinity against Muscarinic acetylcholine receptor using [3H]quinuclidinyl benzilate B 6 pIC50 >1000 nM IC50 J. Med. Chem. (1995) 38: 1119-1131 [PMID:7707315]
5-HT1A receptor in Human [GtoPdb: 1] [UniProtKB: P08908]
GtoPdb - - 7 pKi - - - Neuropsychopharmacology (2001) 25: 904-14 [PMID:11750183]
5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3737] [GtoPdb: 1] [UniProtKB: Q64264]
ChEMBL Binding affinity against 5-hydroxytryptamine 1A receptor was determined using [3H]-8-OH-DPAT radioligand B 6.68 pIC50 210 nM IC50 J. Med. Chem. (1995) 38: 1119-1131 [PMID:7707315]
5-HT1A receptor in Rat [GtoPdb: 1] [UniProtKB: P19327]
GtoPdb - - 6.8 pKi - - - Eur J Pharmacol (1996) 317: 417-23 [PMID:8997630]
Serotonin 2a (5-HT2a) receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3446] [UniProtKB: Q75Z89]
ChEMBL Binding affinity against 5-hydroxytryptamine 2 receptor was determined using [ [3H]spiperone radioligand B 8.05 pIC50 9 nM IC50 J. Med. Chem. (1995) 38: 1119-1131 [PMID:7707315]
sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL287] [GtoPdb: 2552] [UniProtKB: Q99720]
ChEMBL Binding affinity against sigma receptor using [3H]-( +)-SKF10,047 radioligand B 7.19 pIC50 64 nM IC50 J. Med. Chem. (1995) 38: 1119-1131 [PMID:7707315]
5-HT6 receptor in Human [GtoPdb: 11] [UniProtKB: P50406]
GtoPdb - - 7.2 pKi - - - Neuropsychopharmacology (2001) 25: 904-14 [PMID:11750183]
5-HT6 receptor in Rat [GtoPdb: 11] [UniProtKB: P31388]
GtoPdb - - 7.4 pKi - - - Eur J Pharmacol (1996) 317: 417-23 [PMID:8997630]
5-HT7 receptor in Human [GtoPdb: 12] [UniProtKB: P34969]
GtoPdb - - 7 pKi - - - Neuropsychopharmacology (2001) 25: 904-14 [PMID:11750183]
5-HT7 receptor in Rat [GtoPdb: 12] [UniProtKB: P32305]
GtoPdb - - 7.7 pKi - - - Eur J Pharmacol (1996) 317: 417-23 [PMID:8997630]

ChEMBL data shown on this page come from version 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]