iloperidone [Ligand Id: 87] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL14376 (Fanapt, HP 873, HP-873, Iloperidona, Iloperidone) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| 5-HT1A receptor in Human [GtoPdb: 1] [UniProtKB: P08908] | ||||||||
| GtoPdb | - | - | 7 | pKi | - | - | - | Neuropsychopharmacology (2001) 25: 904-14 [PMID:11750183] |
| 5-HT1A receptor/5-hydroxytryptamine receptor 1A 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] |
| 5-hydroxytryptamine receptor 2A 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] |
| 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/D(1A) dopamine 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/D(2) dopamine 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/D(2) dopamine 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] |
| sigma non-opioid intracellular receptor 1/Sigma non-opioid intracellular receptor 1 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 36:
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]
