perphenazine [Ligand Id: 209] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL567 (Chlorpiprazine, Decentan, Etaperazine, Fentazin, NSC-150866, Perphenazine, Perphenazine fendizoate, Perphenazine Fendizoate, Perphenazine maleate, Trilafon, Trilafon-La) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| Aldehyde dehydrogenase 1A1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3577] [UniProtKB: P00352] | ||||||||
| ChEMBL | Inhibition of ALDH1A1 in human drug-tolerant MDA-MB-231/lapatinib cells assessed as after 24 hrs | B | 6.28 | pIC50 | 524.21 | nM | IC50 | J Med Chem (2021) 64: 12877-12892 [PMID:34435487] |
| D2 receptor/Dopamine D2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416] | ||||||||
| GtoPdb | - | - | 9.59 | pKi | 0.26 | nM | Ki |
Neuropsychopharmacology (2003) 28: 519-26 [PMID:12629531]; Clinical Neuroscience Research (2001) 1: 53-60 |
| ChEMBL | Antagonist activity at dopamine D2 receptor (unknown origin) expressed in CHOK1 cells coexpressing Galpha15 assessed as inhibition of agonist-induced response incubated for 60 mins in incubator followed by 15 mins at room temperature by FLIPR assay | B | 9.52 | pIC50 | 0.3 | nM | IC50 | J Med Chem (2013) 56: 4671-4690 [PMID:23675993] |
| Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809] | ||||||||
| ChEMBL | DRUGMATRIX: Potassium Channel HERG radioligand binding (ligand: [3H] Astemizole) | B | 5.46 | pKi | 3454.1 | nM | Ki | DrugMatrix in vitro pharmacology data |
| ChEMBL | DRUGMATRIX: Potassium Channel HERG radioligand binding (ligand: [3H] Astemizole) | B | 5.38 | pIC50 | 4216 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364] | ||||||||
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum Dd2 after 72 hrs by SYBR green assay | F | 5 | pIC50 | 10000 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum D10 after 72 hrs by SYBR green assay | F | 5.2 | pIC50 | 6309.57 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum GB4 after 72 hrs by SYBR green assay | F | 5.4 | pIC50 | 3981.07 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum HB3 after 72 hrs by SYBR green assay | F | 5.4 | pIC50 | 3981.07 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum 7G8 after 72 hrs by SYBR green assay | F | 5.5 | pIC50 | 3162.28 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum 3D7 after 72 hrs by SYBR green assay | F | 5.6 | pIC50 | 2511.89 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum W2 after 72 hrs by SYBR green assay | F | 5.6 | pIC50 | 2511.89 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| Pleiotropic ABC efflux transporter of multiple drugs in Saccharomyces cerevisiae S288c (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1697658] [UniProtKB: P33302] | ||||||||
| ChEMBL | Inhibition of Pdr5p-mediated rhodamine 6G transport in Saccharomyces cerevisiae MKPDR5h plasma membrane by spectrofluorometric assay | B | 5.85 | pIC50 | 1400 | nM | IC50 | Antimicrob Agents Chemother (2009) 53: 1516-1527 [PMID:19188399] |
| 5-HT7 receptor/Serotonin 7 (5-HT7) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3155] [GtoPdb: 12] [UniProtKB: P34969] | ||||||||
| GtoPdb | - | - | 7.2 | pKi | - | - | - | Psychopharmacology (Berl.) (2005) 179: 461-9 [PMID:15821958] |
| ChEMBL | Binding affinity towards human 5-hydroxytryptamine 7 receptor | B | 7.64 | pKi | 23 | nM | Ki | J Med Chem (2003) 46: 2795-2812 [PMID:12825922] |
| 5-HT7 receptor in Rat [GtoPdb: 12] [UniProtKB: P32305] | ||||||||
| GtoPdb | - | - | 7.6 | pKi | - | - | - | J Pharmacol Exp Ther (1994) 268: 1403-10 [PMID:7908055] |
| 5-HT2A receptor in Human [GtoPdb: 6] [UniProtKB: P28223] | ||||||||
| GtoPdb | - | - | 8.2 | pKi | - | - | - | Neuropsychopharmacology (2003) 28: 519-26 [PMID:12629531] |
| 5-HT2C receptor in Human [GtoPdb: 8] [UniProtKB: P28335] | ||||||||
| GtoPdb | - | - | 6.9 | pKi | - | - | - | Neuropsychopharmacology (2003) 28: 519-26 [PMID:12629531] |
| 5-HT6 receptor in Human [GtoPdb: 11] [UniProtKB: P50406] | ||||||||
| GtoPdb | - | - | 7.1 | pKi | - | - | - | Psychopharmacology (Berl.) (2005) 179: 461-9 [PMID:15821958] |
| 5-HT6 receptor in Rat [GtoPdb: 11] [UniProtKB: P31388] | ||||||||
| GtoPdb | - | - | 7.8 | pKi | - | - | - | J Pharmacol Exp Ther (1994) 268: 1403-10 [PMID:7908055] |
| H1 receptor in Human [GtoPdb: 262] [UniProtKB: P35367] | ||||||||
| GtoPdb | - | - | 8.1 | pKi | - | - | - | Neuropsychopharmacology (2003) 28: 519-26 [PMID:12629531] |
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]
