loxapine [Ligand Id: 205] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL831 (Adasuve, CL 62,362, CL-62362, Loxapac, Loxapine, Loxitane, Loxitane-c oral suspension [as hydrochloride], Loxitane intramuscular [as hydrochloride], 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 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]
