TC-E 5005 [Ligand Id: 11625] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1086110
  • phosphodiesterase 10A/Phosphodiesterase 10A in Human [ChEMBL: CHEMBL4409] [GtoPdb: 1310] [UniProtKB: Q9Y233]
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  • phosphodiesterase 11A/Phosphodiesterase 11A in Human [ChEMBL: CHEMBL2717] [GtoPdb: 1311] [UniProtKB: Q9HCR9]
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  • phosphodiesterase 1B/Phosphodiesterase 1B in Human [ChEMBL: CHEMBL4425] [GtoPdb: 1295] [UniProtKB: Q01064]
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  • phosphodiesterase 2A/Phosphodiesterase 2A in Human [ChEMBL: CHEMBL2652] [GtoPdb: 1297] [UniProtKB: O00408]
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  • phosphodiesterase 3A/Phosphodiesterase 3A in Human [ChEMBL: CHEMBL241] [GtoPdb: 1298] [UniProtKB: Q14432]
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  • phosphodiesterase 4A/Phosphodiesterase 4A in Human [ChEMBL: CHEMBL254] [GtoPdb: 1300] [UniProtKB: P27815]
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  • phosphodiesterase 5A/Phosphodiesterase 5A in Human [ChEMBL: CHEMBL1827] [GtoPdb: 1304] [UniProtKB: O76074]
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  • phosphodiesterase 7A/Phosphodiesterase 7A in Human [ChEMBL: CHEMBL3012] [GtoPdb: 1305] [UniProtKB: Q13946]
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  • phosphodiesterase 7B/Phosphodiesterase 7B in Human [ChEMBL: CHEMBL4716] [GtoPdb: 1306] [UniProtKB: Q9NP56]
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  • phosphodiesterase 8A/Phosphodiesterase 8A in Human [ChEMBL: CHEMBL4640] [GtoPdb: 1307] [UniProtKB: O60658]
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  • phosphodiesterase 9A/Phosphodiesterase 9A in Human [ChEMBL: CHEMBL3535] [GtoPdb: 1309] [UniProtKB: O76083]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
phosphodiesterase 10A/Phosphodiesterase 10A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4409] [GtoPdb: 1310] [UniProtKB: Q9Y233]
ChEMBL Inhibition of PDE10A B 7.49 pIC50 32 nM IC50 Bioorg Med Chem Lett (2011) 21: 3738-3742 [PMID:21602043]
ChEMBL Inhibition of PDE10A (unknown origin) B 7.49 pIC50 32 nM IC50 Bioorg Med Chem (2013) 21: 6053-6062 [PMID:23978358]
ChEMBL Inhibition of recombinant human N-terminal His-tagged PDE10A2 expressed in HEK293 cells using cAMP as substrate measured after 60 mins B 7.77 pIC50 17 nM IC50 Bioorg Med Chem Lett (2019) 29: 406-412 [PMID:30587449]
ChEMBL Inhibition of N-terminal His-tagged human PDE10A expressed in Escherichia coli using [3H]cAMP after 1 hr by scintillation proximity assay B 8.14 pIC50 7.3 nM IC50 J Med Chem (2011) 54: 7621-7638 [PMID:21988093]
ChEMBL Inhibition of human recombinant PDE10A expressed in baculovirus-SF21 cell system assessed as hydrolysis of [3H]cAMP after 1 hr by liquid scintillation counting B 8.14 pIC50 7.28 nM IC50 J Med Chem (2010) 53: 4399-4411 [PMID:20450197]
GtoPdb - - 8.14 pIC50 7.3 nM IC50 J Med Chem (2011) 54: 7621-38 [PMID:21988093]
ChEMBL Inhibition of recombinant PDE10A1 expressed in baculovirus infected SF21 cells using [3H]cAMP as substrate after 30 mins by liquid scintillation counting B 8.15 pIC50 7 nM IC50 J Med Chem (2012) 55: 7299-7331 [PMID:22834877]
phosphodiesterase 11A/Phosphodiesterase 11A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2717] [GtoPdb: 1311] [UniProtKB: Q9HCR9]
ChEMBL Inhibition of PDE11A B 6.11 pIC50 779 nM IC50 J Med Chem (2010) 53: 4399-4411 [PMID:20450197]
ChEMBL Inhibition of recombinant human PDE11A using [3H]cAMP after 1 hr by scintillation proximity assay B 6.16 pIC50 690 nM IC50 J Med Chem (2011) 54: 7621-7638 [PMID:21988093]
phosphodiesterase 1B/Phosphodiesterase 1B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4425] [GtoPdb: 1295] [UniProtKB: Q01064]
ChEMBL Inhibition of PDE1B B 5.3 pIC50 >5000 nM IC50 J Med Chem (2010) 53: 4399-4411 [PMID:20450197]
ChEMBL Inhibition of recombinant human PDE1B using [3H]cAMP after 1 hr by scintillation proximity assay B 5.3 pIC50 >5000 nM IC50 J Med Chem (2011) 54: 7621-7638 [PMID:21988093]
phosphodiesterase 2A/Phosphodiesterase 2A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2652] [GtoPdb: 1297] [UniProtKB: O00408]
ChEMBL Inhibition of recombinant human PDE2A using [3H]cAMP after 1 hr by scintillation proximity assay B 6.57 pIC50 270 nM IC50 J Med Chem (2011) 54: 7621-7638 [PMID:21988093]
ChEMBL Inhibition of PDE2A B 6.62 pIC50 239 nM IC50 J Med Chem (2010) 53: 4399-4411 [PMID:20450197]
ChEMBL Inhibition of recombinant PDE2A expressed in baculovirus infected SF21 cells using [3H]cAMP as substrate after 30 mins by liquid scintillation counting B 6.62 pIC50 239 nM IC50 J Med Chem (2012) 55: 7299-7331 [PMID:22834877]
phosphodiesterase 3A/Phosphodiesterase 3A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL241] [GtoPdb: 1298] [UniProtKB: Q14432]
ChEMBL Inhibition of recombinant human PDE3A using [3H]cAMP after 1 hr by scintillation proximity assay B 5.3 pIC50 >5000 nM IC50 J Med Chem (2011) 54: 7621-7638 [PMID:21988093]
ChEMBL Inhibition of PDE3A B 5.43 pIC50 3700 nM IC50 J Med Chem (2010) 53: 4399-4411 [PMID:20450197]
phosphodiesterase 4A/Phosphodiesterase 4A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL254] [GtoPdb: 1300] [UniProtKB: P27815]
ChEMBL Inhibition of PDE4A B 5.3 pIC50 5000 nM IC50 J Med Chem (2010) 53: 4399-4411 [PMID:20450197]
ChEMBL Inhibition of recombinant human PDE4A using [3H]cAMP after 1 hr by scintillation proximity assay B 5.3 pIC50 >5000 nM IC50 J Med Chem (2011) 54: 7621-7638 [PMID:21988093]
phosphodiesterase 5A/Phosphodiesterase 5A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1827] [GtoPdb: 1304] [UniProtKB: O76074]
ChEMBL Inhibition of recombinant human PDE5A using [3H]cGMP after 1 hr by scintillation proximity assay B 6.04 pIC50 920 nM IC50 J Med Chem (2011) 54: 7621-7638 [PMID:21988093]
ChEMBL Inhibition of PDE5A B 6.04 pIC50 919 nM IC50 J Med Chem (2010) 53: 4399-4411 [PMID:20450197]
Phosphodiesterase 6A in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3741] [UniProtKB: P11541]
ChEMBL Inhibition of recombinant bovine PDE6A using [3H]cGMP after 1 hr by scintillation proximity assay B 6 pIC50 >1000 nM IC50 J Med Chem (2011) 54: 7621-7638 [PMID:21988093]
phosphodiesterase 7A/Phosphodiesterase 7A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3012] [GtoPdb: 1305] [UniProtKB: Q13946]
ChEMBL Inhibition of recombinant human PDE7A using [3H]cAMP after 1 hr by scintillation proximity assay B 5.48 pIC50 3345 nM IC50 J Med Chem (2011) 54: 7621-7638 [PMID:21988093]
phosphodiesterase 7B/Phosphodiesterase 7B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4716] [GtoPdb: 1306] [UniProtKB: Q9NP56]
ChEMBL Inhibition of PDE7B B 5.51 pIC50 3100 nM IC50 J Med Chem (2010) 53: 4399-4411 [PMID:20450197]
phosphodiesterase 8A/Phosphodiesterase 8A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4640] [GtoPdb: 1307] [UniProtKB: O60658]
ChEMBL Inhibition of PDE8A B 5.3 pIC50 >5000 nM IC50 J Med Chem (2010) 53: 4399-4411 [PMID:20450197]
ChEMBL Inhibition of recombinant human PDE8A using [3H]cAMP after 1 hr by scintillation proximity assay B 5.3 pIC50 >5000 nM IC50 J Med Chem (2011) 54: 7621-7638 [PMID:21988093]
phosphodiesterase 9A/Phosphodiesterase 9A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3535] [GtoPdb: 1309] [UniProtKB: O76083]
ChEMBL Inhibition of PDE9A B 5.3 pIC50 >5000 nM IC50 J Med Chem (2010) 53: 4399-4411 [PMID:20450197]
ChEMBL Inhibition of recombinant human PDE9A using [3H]cGMP after 1 hr by scintillation proximity assay B 5.3 pIC50 >5000 nM IC50 J Med Chem (2011) 54: 7621-7638 [PMID:21988093]

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]