loxapine [Ligand Id: 205] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL831 (Adasuve, CL 62,362, CL-62362, Loxapac, Loxapina, Loxapine, Loxitane, SUM 3170, SUM-3170) |
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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 | Affinity was evaluated by inhibition of [3H]spiperone binding to COS cells transfected with human dopamine D-2(long) receptor | B | 7.68 | pKi | 21 | nM | Ki | J Med Chem (1994) 37: 2686-2696 [PMID:8064797] |
| ChEMBL | Ability to inhibit the binding of [3H]spiperone to the Dopamine receptor D2L in COS7 cells | B | 7.68 | pKi | 21 | nM | Ki | J Med Chem (1995) 38: 708-714 [PMID:7861418] |
| GtoPdb | - | - | 8.3 | pKi | 5 | nM | Ki |
Neuropsychopharmacology (2003) 28: 519-26 [PMID:12629531]; Neuropsychopharmacology (1997) 16: 93-110; discussion 111-35 [PMID:9015795] |
| ChEMBL | Compound was tested in vitro for its binding affinity towards human Dopamine receptor D2 | B | 7.27 | pIC50 | 54 | nM | IC50 | J Med Chem (1999) 42: 2235-2244 [PMID:10377229] |
| D2 receptor/Dopamine D2 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL339] [GtoPdb: 215] [UniProtKB: P61169] | ||||||||
| ChEMBL | In vitro binding affinity towards Dopamine receptor D2 in rat tissue homogenate using [3H]-spiperone as radioligand | B | 7.68 | pKi | 21 | nM | Ki | J Med Chem (2004) 47: 143-157 [PMID:14695828] |
| D3 receptor/Dopamine D3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462] | ||||||||
| GtoPdb | - | - | 7.68 | pKi | 21 | nM | Ki | Clinical Neuroscience Research (2001) 1: 53-60 |
| ChEMBL | Binding affinity towards human Dopamine receptor D3 | B | 7.66 | pIC50 | 22 | nM | IC50 | J Med Chem (1999) 42: 2235-2244 [PMID:10377229] |
| D4 receptor/Dopamine D4 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL219] [GtoPdb: 217] [UniProtKB: P21917] | ||||||||
| ChEMBL | Displacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation counting | B | 8.05 | pKi | 9 | nM | Ki | J Med Chem (2012) 55: 1572-1582 [PMID:22268448] |
| GtoPdb | - | - | 8.11 | pKi | 7.8 | nM | Ki | Neuropsychopharmacology (1997) 16: 93-110; discussion 111-35 [PMID:9015795] |
| ChEMBL | Affinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptor | B | 8.31 | pKi | 4.9 | nM | Ki | J Med Chem (1994) 37: 2686-2696 [PMID:8064797] |
| ChEMBL | Ability to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cells | B | 8.31 | pKi | 4.9 | nM | Ki | J Med Chem (1995) 38: 708-714 [PMID:7861418] |
| ChEMBL | Compound was tested in vitro for its binding affinity towards human Dopamine receptor D4.2 | B | 7.85 | pIC50 | 14 | nM | IC50 | J Med Chem (1999) 42: 2235-2244 [PMID:10377229] |
| H1 receptor in Human [GtoPdb: 262] [UniProtKB: P35367] | ||||||||
| GtoPdb | - | - | 8.2 | pKi | - | - | - | Neuropsychopharmacology (2003) 28: 519-26 [PMID:12629531] |
| H1 receptor/Histamine H1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4701] [GtoPdb: 262] [UniProtKB: P31390] | ||||||||
| ChEMBL | Binding affinity towards histamine H1 receptor from rat brain membranes using [3H]mepyramine as radioligand | B | 6 | pIC50 | 1000 | nM | IC50 | J Med Chem (1999) 42: 2235-2244 [PMID:10377229] |
| H4 receptor/Histamine H4 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3759] [GtoPdb: 265] [UniProtKB: Q9H3N8] | ||||||||
| ChEMBL | Displacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cells | B | 5.34 | pKi | 4570.88 | nM | Ki | J Med Chem (2006) 49: 4512-4516 [PMID:16854056] |
| ChEMBL | Activity at human histamine H4 receptor transfected in SK-N-MC cells by cAMP assay | F | 6.66 | pEC50 | 218.78 | nM | EC50 | J Med Chem (2006) 49: 4512-4516 [PMID:16854056] |
| M1 receptor/Muscarinic acetylcholine receptor M1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL216] [GtoPdb: 13] [UniProtKB: P11229] | ||||||||
| ChEMBL | Inhibition of binding of 1.0 nM [3H]pirenzepine to cloned human Muscarinic acetylcholine receptor M1 expressed in membranes from CHO-K1 cells | B | 5.26 | pIC50 | 5500 | nM | IC50 | J Med Chem (1999) 42: 2235-2244 [PMID:10377229] |
| K2P2.1/Potassium channel subfamily K member 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2321615] [GtoPdb: 514] [UniProtKB: O95069] | ||||||||
| ChEMBL | Inhibition of of human TREK1 expressed in whole COS cells assessed as reduction in channel currents | B | 4.7 | pIC50 | 20000 | nM | IC50 | J Med Chem (2016) 59: 5149-5157 [PMID:26588045] |
| 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223] | ||||||||
| GtoPdb | - | - | 8.1 | pKi | - | - | - | Neuropsychopharmacology (2003) 28: 519-26 [PMID:12629531] |
| ChEMBL | Displacement of [3H]ketanserin from human recombinant 5HT2A receptor expressed in CHO cells after 60 mins by liquid scintillation counting | B | 8.62 | pKi | 2.42 | nM | Ki | J Med Chem (2012) 55: 1572-1582 [PMID:22268448] |
| 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL322] [GtoPdb: 6] [UniProtKB: P14842] | ||||||||
| ChEMBL | Binding affinity towards 5-hydroxytryptamine 2A receptor from rat frontal cortex using [3H]ketanserin as radioligand | B | 8.22 | pIC50 | 6 | nM | IC50 | J Med Chem (1999) 42: 2235-2244 [PMID:10377229] |
| 5-HT2C receptor in Human [GtoPdb: 8] [UniProtKB: P28335] | ||||||||
| GtoPdb | - | - | 8 | pKi | - | - | - |
Neuropsychopharmacology (2003) 28: 519-26 [PMID:12629531]; J Pharmacol Exp Ther (2000) 295: 226-32 [PMID:10991983] |
| 5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL324] [GtoPdb: 8] [UniProtKB: P08909] | ||||||||
| ChEMBL | Compound was tested in vitro for its binding affinity towards 5-hydroxytryptamine 2C receptor from rat using [3H]mesulergine as radioligand | B | 6 | pIC50 | 1000 | nM | IC50 | J Med Chem (1999) 42: 2235-2244 [PMID:10377229] |
| 5-HT6 receptor/Serotonin 6 (5-HT6) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3371] [GtoPdb: 11] [UniProtKB: P50406] | ||||||||
| ChEMBL | Binding affinity for human 5-hydroxytryptamine 6 receptor | B | 7.3 | pKi | <50 | nM | Ki | J Med Chem (2005) 48: 1781-1795 [PMID:15771424] |
| GtoPdb | - | - | 7.6 | pKi | - | - | - |
J Neurochem (1996) 66: 47-56 [PMID:8522988]; Psychopharmacology (Berl) (2005) 179: 461-9 [PMID:15821958] |
| ChEMBL | Binding affinity towards human 5-hydroxytryptamine 6 receptor | B | 7.82 | pKi | 15 | nM | Ki | J Med Chem (2003) 46: 2795-2812 [PMID:12825922] |
| 5-HT6 receptor in Rat [GtoPdb: 11] [UniProtKB: P31388] | ||||||||
| GtoPdb | - | - | 7.8 | pKi | - | - | - |
Mol Pharmacol (1993) 43: 320-7 [PMID:7680751]; J Pharmacol Exp Ther (1994) 268: 1403-10 [PMID:7908055] |
| 5-HT7 receptor/Serotonin 7 (5-HT7) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3223] [GtoPdb: 12] [UniProtKB: P32305] | ||||||||
| ChEMBL | Binding affinity towards rat 5-hydroxytryptamine 7 receptor | B | 7.37 | pKi | 43 | nM | Ki | J Med Chem (2003) 46: 2795-2812 [PMID:12825922] |
| GtoPdb | - | - | 7.4 | pKi | - | - | - |
J Pharmacol Exp Ther (1994) 268: 1403-10 [PMID:7908055]; J Biol Chem (1993) 268: 18200-4 [PMID:8394362] |
| KNa1.1 in Human [GtoPdb: 385] [UniProtKB: Q5JUK3] | ||||||||
| GtoPdb | - | - | 5.36 | pEC50 | 4400 | nM | EC50 | J Pharmacol Exp Ther (2012) 340: 706-15 [PMID:22171093] |
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]
