PF-05180999 [Ligand Id: 11626] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL3092562 (Pf-05180999, PF-05180999, PF-999)
  • phosphodiesterase 2A/Phosphodiesterase 2A in Human [ChEMBL: CHEMBL2652] [GtoPdb: 1297] [UniProtKB: O00408]
  • phosphodiesterase 2A/Phosphodiesterase 2A in Rat [ChEMBL: CHEMBL4650] [GtoPdb: 1297] [UniProtKB: Q01062]
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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 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]