TPN171 [Ligand Id: 12781] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL4462192 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| phosphodiesterase 5A/Phosphodiesterase 5A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1827] [GtoPdb: 1304] [UniProtKB: O76074] | ||||||||
| ChEMBL | Binding affinity to recombinant human PDE5A1 catalytic domain (535 to 860 residues) expressed in Escherichia coli BL21 DE3 Rosetta2 pLysS cells assessed as dissociation constant at 200 to 250 uM by by isothermal titration calorimetry | B | 7.09 | pKd | 82 | nM | Kd | J Med Chem (2019) 62: 4979-4990 [PMID:31021628] |
| ChEMBL | Inhibition of N-terminal GST-tagged human PDE5A1 expressed in baculovirus infected sf9 cells using [3H]cGMP as substrate measured after 30 mins by scintillation proximity assay | B | 9.21 | pIC50 | 0.62 | nM | IC50 | J Med Chem (2019) 62: 4979-4990 [PMID:31021628] |
| GtoPdb | - | - | 9.21 | pIC50 | 0.62 | nM | IC50 | J Med Chem (2019) 62: 4979-4990 [PMID:31021628] |
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]
