LY2109761 [Ligand Id: 8075] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL260015 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| transforming growth factor beta receptor 1/TGF-beta receptor type I in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4439] [GtoPdb: 1788] [UniProtKB: P36897] | ||||||||
| GtoPdb | - | - | 7.42 | pKi | 38 | nM | Ki | Mol Cancer Ther (2008) 7: 829-40 [PMID:18413796] |
| ChEMBL | Inhibition of TGFbetaR1 in human primary T-cells assessed as TGFbeta-stimulated PSMAD phosphorylation preincubated for 1 hr followed by TGFbeta addition measured after 90 mins by Alpha screen assay | B | 6.43 | pIC50 | 370 | nM | IC50 | Bioorg Med Chem (2018) 26: 1026-1034 [PMID:29422332] |
| ChEMBL | Inhibition of TGFbeta type receptor 1 ALK5 (T204D) expressed in Sf9 cells | B | 7.16 | pIC50 | 69 | nM | IC50 | J Med Chem (2008) 51: 2302-2306 [PMID:18314943] |
| ChEMBL | Inhibition of human His-tagged TGFbetaR1 T204D mutant expressed in Sf9 insect cells after 1 hr by HTRF assay | B | 8.43 | pIC50 | 3.7 | nM | IC50 | Bioorg Med Chem (2018) 26: 1026-1034 [PMID:29422332] |
| transforming growth factor beta receptor 2/TGF-beta receptor type II in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4267] [GtoPdb: 1795] [UniProtKB: P37173] | ||||||||
| GtoPdb | - | - | 6.52 | pKi | 300 | nM | Ki | Mol Cancer Ther (2008) 7: 829-40 [PMID:18413796] |
| ChEMBL | Inhibition of wild type His-tagged TGFbetaR2 (unknown origin) after 1 hr by HTRF assay | B | 6.72 | pIC50 | 190 | nM | IC50 | Bioorg Med Chem (2018) 26: 1026-1034 [PMID:29422332] |
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]
