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 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] |
| ChEMBL | Inhibition of PDE2 (unknown origin) | B | 9 | pIC50 | 1 | nM | IC50 | Eur J Med Chem (2022) 232: 114170-114170 [PMID:35144038] |
| 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 PDE2A (unknown origin) | B | 9 | pIC50 | 1 | nM | IC50 | J Med Chem (2021) 64: 7083-7109 [PMID:34042442] |
| 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] |
| 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 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]
