PF-05180999 [Ligand Id: 11626] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL3092562 (Pf-05180999, PF-05180999, PF-999) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| phosphodiesterase 2A/Phosphodiesterase 2A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2652] [GtoPdb: 1297] [UniProtKB: O00408] | ||||||||
| ChEMBL | Inhibition Assay: The activity of the test substances on human full-length PDE2A3 enzyme was determined using the [3H]-cGMP scintillation proximity assay (SPA) modified from the Amersham TRKQ7100 instructions (GE Healthcare, USA). | B | 8.79 | pIC50 | 1.61 | nM | IC50 | US-8598155-B2. Imidazo[5,1-f][1,2,4]triazines for the treatment of neurological disorders (2013) |
| ChEMBL | Inhibition of full length human N-terminal FLAG-tagged PDE2A3 expressed in sf21 cells using [3H]cGMP as substrate after 30 mins by SPA | B | 8.8 | pIC50 | 1.6 | nM | IC50 | J Med Chem (2018) 61: 1001-1018 [PMID:29293004] |
| GtoPdb | - | - | 8.8 | pIC50 | 1.6 | nM | IC50 | J Med Chem (2018) 61: 1001-1018 [PMID:29293004] |
| ChEMBL | Inhibition of recombinant human full length PDE2A3 expressed in insect SF-21 cells using [3H]-cGMP as substrate by scintillation proximity assay | B | 9 | pIC50 | 1 | nM | IC50 | Bioorg Med Chem Lett (2013) 23: 6522-6527 [PMID:24189054] |
| ChEMBL | Inhibition of human full length PDE2a using cGMP as substrate by Scintillation proximity assay | B | 9 | pIC50 | 1 | nM | IC50 | J Med Chem (2017) 60: 2037-2051 [PMID:28165743] |
| ChEMBL | Inhibition of PDE2A (unknown origin) | B | 9 | pIC50 | 1 | nM | IC50 | J Med Chem (2017) 60: 7658-7676 [PMID:28759228] |
| ChEMBL | Inhibition of recombinant human FLAG-tagged PDE2A3 expressed in sf21 cells using [3H]cGMP as substrate by scintillation proximity assay | B | 9 | pIC50 | 1 | nM | IC50 | J Med Chem (2017) 60: 7677-7702 [PMID:28796496] |
| phosphodiesterase 2A/Phosphodiesterase 2A in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4650] [GtoPdb: 1297] [UniProtKB: Q01062] | ||||||||
| ChEMBL | Displacement of radiolabeled 4-(azetidin-1-yl)-3-[5-[4-(trifluoromethyl)phenyl]-1H-pyrazol-4-yl]-1-(tritritiomethyl)pyrazolo[3,4-d]pyrimidine from PDE2A in rat striatal membranes after 30 mins by liquid scintillation counting method | B | 8.38 | pKi | 4.2 | nM | Ki | J Med Chem (2018) 61: 1001-1018 [PMID:29293004] |
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]
