razuprotafib [Ligand Id: 11336] activity data from GtoPdb and ChEMBL
Click here for a description of the charts and data table
Please tell us if you are using this feature and what you think!
| ChEMBL ligand: CHEMBL3931971 (AKB-9778, Razuprotafib) |
|---|
There should be some charts here, you may need to enable JavaScript!
|
| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| RTP Type B/Receptor-type tyrosine-protein phosphatase beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2706] [GtoPdb: 1851] [UniProtKB: P23467] | ||||||||
| ChEMBL | Inhibitory Activity Assay: Non-limiting examples of the HPTPβ IC50 (μM) activity. | B | 5.05 | pIC50 | 9000 | nM | IC50 | US-11413242-B2. Formulations of Tie-2 activators and methods of use thereof (2022) |
| GtoPdb | - | - | 6.15 | pIC50 | 700 | nM | IC50 | US10220048. Compositions and methods for treating ocular diseases (2019) |
| ChEMBL | Inhibitory Activity Assay: Non-limiting examples of the HPTP-β IC50 (μM) activity. | B | 7.3 | pIC50 | <50 | nM | IC50 | US-10952992-B2. Methods of treating intraocular pressure with activators of Tie-2 (2021) |
| ChEMBL | Inhibitory Activity to HPTP-β: Non-limiting examples of the HPTP-β IC50(μM) activity for illustrative compounds are listed in TABLE 2. | B | 7.3 | pIC50 | 50 | nM | IC50 | US-11666558-B2. Methods of treating intraocular pressure with activators of Tie-2 (2023) |
| ChEMBL | HPTP Assay: HPTP-β inhibition can be tested by any method chosen by the formulator, for example, Amarasinge K. K. et al., Design and Synthesis of Potent, Non-peptidic Inhibitors of HPTPbeta Bioorg Med Chem Lett. 2006 Aug. 15; 16(16):4252-6. Epub 2006 Jun. 12. Erratum in: Bioorg Med Chem Lett. 2008 Aug. 15; 18(16):4745. Evidokimov, Artem G [corrected to Evdokimov, Artem G]: PMID: 16759857; and Klopfenstein S. R. et al. 1,2,3,4-Tetrahydroisoquinolinyl Sulfamic Acids as Phosphatase PTP1B Inhibitors Bioorg Med Chem Lett. 2006 Mar. 15; 16(6):1574-8, both of which are included herein by reference in their entirety. | B | 8.3 | pIC50 | 5 | nM | IC50 | US-10220048-B2. Compositions and methods for treating ocular diseases (2019) |
ChEMBL data shown on this page come from version 36:
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]
