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 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]