TP-10 [Ligand Id: 13575] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL562513 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| phosphodiesterase 10A/cAMP and cAMP-inhibited cGMP 3`,5`-cyclic phosphodiesterase 10A in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6140] [GtoPdb: 1310] [UniProtKB: Q9QYJ6] | ||||||||
| ChEMBL | Inhibition of rat recombinant PDE10A transfected in Sf9 cells | B | 8.85 | pIC50 | 1.41 | nM | IC50 | J Med Chem (2009) 52: 5188-5196 [PMID:19630403] |
| ChEMBL | Inhibition of rat recombinant PDE10A transfected in Sf9 cells | B | 8.85 | pIC50 | 1.41 | nM | IC50 | J Med Chem (2009) 52: 5188-5196 [PMID:19630403] |
| GtoPdb | - | - | 9.52 | pIC50 | 0.3 | nM | IC50 | J Pharmacol Exp Ther (2008) 325: 681-90 [PMID:18287214] |
| ChEMBL | Inhibition of rat PDE10A | B | 9.52 | pIC50 | 0.3 | nM | IC50 | Eur J Med Chem (2011) 46: 3986-3995 [PMID:21705115] |
| phosphodiesterase 10A/Phosphodiesterase 10A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4409] [GtoPdb: 1310] [UniProtKB: Q9Y233] | ||||||||
| ChEMBL | Inhibition of N-terminal GST-tagged human recombinant PDE10A assessed as substrate hydrolysis using [3H]cAMP as substrate after 30 mins by two-step radiometric assay | B | 8.85 | pIC50 | 1.41 | nM | IC50 | Bioorg Med Chem Lett (2014) 24: 2073-2078 [PMID:24725435] |
| ChEMBL | Inhibition of human recombinant full length PDE10A using cAMP as substrate preincubated for 20 mins measured after 4 hrs | B | 9 | pIC50 | <1 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 1944-1948 [PMID:22321214] |
| ChEMBL | Inhibition of recombinant PDE10A by scintillation proximity assay | B | 9.52 | pIC50 | 0.3 | nM | IC50 | J Med Chem (2012) 55: 7299-7331 [PMID:22834877] |
| ChEMBL | Inhibition of human PDE10A (amino acids 14 to 779) using [3H]-labelled cyclic nucleotide as substrate after 1 hr b beta counting | B | 9.52 | pIC50 | 0.3 | nM | IC50 | Eur J Med Chem (2014) 84: 181-193 [PMID:25016376] |
| ChEMBL | Inhibition of recombinant full length human PDE10A by scintillation proximity assay in presence of cAMP | B | 9.52 | pIC50 | 0.3 | nM | IC50 | Medchemcomm (2015) 6: 2063-2080 |
| phosphodiesterase 10A in Rat [GtoPdb: 1310] [UniProtKB: Q9QYJ6] | ||||||||
| GtoPdb | - | - | 9.52 | pIC50 | 0.3 | nM | IC50 | J Pharmacol Exp Ther (2008) 325: 681-90 [PMID:18287214] |
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]
