ciglitazone [Ligand Id: 2711] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL7002 (ADD-3878, Ciglitazone, U-63,287, U-63287) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| HPGD/15-hydroxyprostaglandin dehydrogenase [NAD+] in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1293255] [GtoPdb: 1384] [UniProtKB: P15428] | ||||||||
| ChEMBL | Inhibition of PGDH (unknown origin) | B | 5.57 | pIC50 | 2700 | nM | IC50 | Bioorg Med Chem Lett (2014) 24: 630-635 [PMID:24360556] |
| acetylcholinesterase (Yt blood group)/Acetylcholinesterase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL220] [GtoPdb: 2465] [UniProtKB: P22303] | ||||||||
| ChEMBL | DRUGMATRIX: Acetylcholinesterase enzyme inhibition (substrate: acetylthiocholine) | B | 4.82 | pIC50 | 15026 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| A3 receptor/Adenosine A3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL256] [GtoPdb: 21] [UniProtKB: P0DMS8] | ||||||||
| ChEMBL | DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA) | B | 5.76 | pKi | 1722 | nM | Ki | DrugMatrix in vitro pharmacology data |
| ChEMBL | DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA) | B | 5.52 | pIC50 | 3047 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| α2A-adrenoceptor/Alpha-2a adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1867] [GtoPdb: 25] [UniProtKB: P08913] | ||||||||
| ChEMBL | DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912) | B | 5.21 | pKi | 6207 | nM | Ki | DrugMatrix in vitro pharmacology data |
| ChEMBL | DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912) | B | 4.78 | pIC50 | 16551 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| α2B-adrenoceptor/Alpha-2b adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1942] [GtoPdb: 26] [UniProtKB: P18089] | ||||||||
| ChEMBL | DRUGMATRIX: Alpha-2B adrenergic receptor radioligand binding (ligand: Rauwolscine) | B | 5.22 | pKi | 6053 | nM | Ki | DrugMatrix in vitro pharmacology data |
| ChEMBL | DRUGMATRIX: Alpha-2B adrenergic receptor radioligand binding (ligand: Rauwolscine) | B | 4.88 | pIC50 | 13258 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| β3-adrenoceptor/Beta-3 adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL246] [GtoPdb: 30] [UniProtKB: P13945] | ||||||||
| ChEMBL | DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol) | B | 4.87 | pKi | 13403 | nM | Ki | DrugMatrix in vitro pharmacology data |
| ChEMBL | DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol) | B | 4.75 | pIC50 | 17871 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| carbonic anhydrase 2/Carbonic anhydrase II in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL205] [GtoPdb: 3092] [UniProtKB: P00918] | ||||||||
| ChEMBL | DRUGMATRIX: Carbonic Anhydrase II enzyme inhibition (substrate: 4-Nitrophenyl acetate (4-NPA)) | B | 7.07 | pIC50 | 86 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| δ receptor/Delta opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL236] [GtoPdb: 317] [UniProtKB: P41143] | ||||||||
| ChEMBL | DRUGMATRIX: Opiate delta1 (OP1, DOP) radioligand binding (ligand: [3H] Naltrindole) | B | 5.02 | pKi | 9481 | nM | Ki | DrugMatrix in vitro pharmacology data |
| ChEMBL | DRUGMATRIX: Opiate delta1 (OP1, DOP) radioligand binding (ligand: [3H] Naltrindole) | B | 4.57 | pIC50 | 26894 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| D1 receptor/Dopamine D1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2056] [GtoPdb: 214] [UniProtKB: P21728] | ||||||||
| ChEMBL | DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390) | B | 5 | pKi | 9893 | nM | Ki | DrugMatrix in vitro pharmacology data |
| ChEMBL | DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390) | B | 4.7 | pIC50 | 19785 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| D3 receptor/Dopamine D3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462] | ||||||||
| ChEMBL | DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone) | B | 5.04 | pKi | 9069 | nM | Ki | DrugMatrix in vitro pharmacology data |
| ChEMBL | DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone) | B | 4.57 | pIC50 | 26704 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| epidermal growth factor receptor/Epidermal growth factor receptor erbB1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL203] [GtoPdb: 1797] [UniProtKB: P00533] | ||||||||
| ChEMBL | DRUGMATRIX: Protein Tyrosine Kinase, EGF Receptor enzyme inhibition (substrate: Poly(Glu:Tyr)) | B | 5.33 | pIC50 | 4655 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| MC5 receptor/Melanocortin receptor 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4608] [GtoPdb: 286] [UniProtKB: P33032] | ||||||||
| ChEMBL | DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH) | B | 4.57 | pKi | 26848 | nM | Ki | DrugMatrix in vitro pharmacology data |
| ChEMBL | DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH) | B | 4.54 | pIC50 | 28621 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| Monoamine oxidase A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1951] [GtoPdb: 2489] [UniProtKB: P21397] | ||||||||
| ChEMBL | DRUGMATRIX: Monoamine Oxidase MAO-A enzyme inhibition (substrate: Kynuramine) | B | 4.53 | pIC50 | 29193 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| Monoamine oxidase B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2039] [GtoPdb: 2490] [UniProtKB: P27338] | ||||||||
| ChEMBL | Inhibition of human recombinant MAO-B after 15 mins | B | 6.65 | pIC50 | 225 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 5295-5298 [PMID:20650633] |
| M2 receptor/Muscarinic acetylcholine receptor M2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL211] [GtoPdb: 14] [UniProtKB: P08172] | ||||||||
| ChEMBL | DRUGMATRIX: Muscarinic M2 radioligand binding (ligand: [3H] N-Methylscopolamine) | B | 5.12 | pKi | 7505 | nM | Ki | DrugMatrix in vitro pharmacology data |
| ChEMBL | DRUGMATRIX: Muscarinic M2 radioligand binding (ligand: [3H] N-Methylscopolamine) | B | 4.68 | pIC50 | 21107 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| M3 receptor/Muscarinic acetylcholine receptor M3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL245] [GtoPdb: 15] [UniProtKB: P20309] | ||||||||
| ChEMBL | DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine) | B | 5.5 | pKi | 3168 | nM | Ki | DrugMatrix in vitro pharmacology data |
| ChEMBL | DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine) | B | 4.83 | pIC50 | 14947 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| M4 receptor/Muscarinic acetylcholine receptor M4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1821] [GtoPdb: 16] [UniProtKB: P08173] | ||||||||
| ChEMBL | DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine) | B | 5.65 | pKi | 2263 | nM | Ki | DrugMatrix in vitro pharmacology data |
| ChEMBL | DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine) | B | 4.79 | pIC50 | 16224 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| NK2 receptor/Neurokinin 2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2327] [GtoPdb: 361] [UniProtKB: P21452] | ||||||||
| ChEMBL | DRUGMATRIX: Tachykinin NK2 radioligand binding (ligand: [3H] SR-48968) | B | 5.38 | pKi | 4192 | nM | Ki | DrugMatrix in vitro pharmacology data |
| ChEMBL | DRUGMATRIX: Tachykinin NK2 radioligand binding (ligand: [3H] SR-48968) | B | 4.9 | pIC50 | 12576 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| NET/Norepinephrine transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL222] [GtoPdb: 926] [UniProtKB: P23975] | ||||||||
| ChEMBL | DRUGMATRIX: Norepinephrine Transporter radioligand binding (ligand: [125I] RTI-55) | B | 5.66 | pKi | 2201 | nM | Ki | DrugMatrix in vitro pharmacology data |
| ChEMBL | DRUGMATRIX: Norepinephrine Transporter radioligand binding (ligand: [125I] RTI-55) | B | 5.65 | pIC50 | 2220 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| Peroxisome proliferator-activated receptor-γ/Peroxisome proliferator-activated receptor gamma in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL235] [GtoPdb: 595] [UniProtKB: P37231] | ||||||||
| ChEMBL | In vitro binding to peroxisome proliferator activated receptor gamma (PPAR gamma) using [3H]-BRL 49653 as radioligand in scintillation proximity assay (SPA) | B | 5.51 | pKi | 3090.3 | nM | Ki | J Med Chem (1998) 41: 5020-5036 [PMID:9836620] |
| ChEMBL | Competitive displacement of fluorescently labelled PPAR tracer ligand from GST-tagged human PPARgamma ligand binding domain after 1 hr in dark by TR-FRET competitive binding assay | B | 5.3 | pIC50 | >5000 | nM | IC50 | Bioorg Med Chem (2018) 26: 5870-5884 [PMID:30429097] |
| GtoPdb | - | - | 4.6 | pEC50 | - | - | - | J Med Chem (1998) 41: 5020-36 [PMID:9836620] |
| ChEMBL | Activation of peroxisome proliferator activated receptor gamma measured by induction of 50% of maximum alkaline phosphatase activity, transfection assay in CV-1 cells | F | 4.64 | pEC50 | 22908.68 | nM | EC50 | J Med Chem (1998) 41: 5020-5036 [PMID:9836620] |
| ChEMBL | Agonist activity at human PPARgamma expressed in mouse NIH/3T3 cells assessed as receptor activation after 16 hrs by luciferase based reporter gene assay | F | 4.83 | pEC50 | 14900 | nM | EC50 | J Nat Prod (2002) 65: 616-617 [PMID:11975517] |
| ChEMBL | Transactivation activity at Homo sapiens (human) PPARgamma | B | 5.52 | pEC50 | 3000 | nM | EC50 | Med Chem Res (2011) 20: 1005-1014 |
| Peroxisome proliferator-activated receptor-γ/Peroxisome proliferator-activated receptor gamma in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2459] [GtoPdb: 595] [UniProtKB: P37238] | ||||||||
| ChEMBL | In vitro transcriptional activation of Peroxisome proliferator activated receptor gamma (PPAR) expressed in CV-1 cells | F | 5.52 | pEC50 | 3000 | nM | EC50 | J Med Chem (1996) 39: 665-668 [PMID:8576907] |
| Progesterone receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1909044] [UniProtKB: Q690N0] | ||||||||
| ChEMBL | DRUGMATRIX: Progesterone radioligand binding (ligand: [3H] R-5020) | B | 5.42 | pKi | 3798 | nM | Ki | DrugMatrix in vitro pharmacology data |
| ChEMBL | DRUGMATRIX: Progesterone radioligand binding (ligand: [3H] R-5020) | B | 4.54 | pIC50 | 29118 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| SERT/Serotonin transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL228] [GtoPdb: 928] [UniProtKB: P31645] | ||||||||
| ChEMBL | DRUGMATRIX: Transporter, Serotonin (5-Hydroxytryptamine) (SERT) radioligand binding (ligand: [3H] Paroxetine) | B | 5.1 | pKi | 7941 | nM | Ki | DrugMatrix in vitro pharmacology data |
| ChEMBL | DRUGMATRIX: Transporter, Serotonin (5-Hydroxytryptamine) (SERT) radioligand binding (ligand: [3H] Paroxetine) | B | 4.83 | pIC50 | 14948 | nM | IC50 | DrugMatrix in vitro pharmacology data |
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]
