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

Click here for a description of the charts and data table

Please tell us if you are using this feature and what you think!

ChEMBL ligand: CHEMBL14376 (Fanapt, HP 873, HP-873, Iloperidone)
  • α2A-adrenoceptor/Alpha-2a adrenergic receptor in Rat [ChEMBL: CHEMBL327] [GtoPdb: 25] [UniProtKB: P22909]
There should be some charts here, you may need to enable JavaScript!
  • D1 receptor/Dopamine D1 receptor in Mouse [ChEMBL: CHEMBL3071] [GtoPdb: 214] [UniProtKB: Q61616]
There should be some charts here, you may need to enable JavaScript!
  • 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]
There should be some charts here, you may need to enable JavaScript!
  • M3 receptor/Muscarinic acetylcholine receptor M3 in Rat [ChEMBL: CHEMBL320] [GtoPdb: 15] [UniProtKB: P08483]
There should be some charts here, you may need to enable JavaScript!
  • 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]
There should be some charts here, you may need to enable JavaScript!
  • Serotonin 2a (5-HT2a) receptor in Bovine [ChEMBL: CHEMBL3446] [UniProtKB: Q75Z89]
There should be some charts here, you may need to enable JavaScript!
  • sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Human [ChEMBL: CHEMBL287] [GtoPdb: 2552] [UniProtKB: Q99720]
There should be some charts here, you may need to enable JavaScript!
  • 5-HT6 receptor in Human [GtoPdb: 11] [UniProtKB: P50406]
  • 5-HT6 receptor in Rat [GtoPdb: 11] [UniProtKB: P31388]
There should be some charts here, you may need to enable JavaScript!
  • 5-HT7 receptor in Human [GtoPdb: 12] [UniProtKB: P34969]
  • 5-HT7 receptor in Rat [GtoPdb: 12] [UniProtKB: P32305]
There should be some charts here, you may need to enable JavaScript!
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 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]