example 373 [WO2012093101] [Ligand Id: 8296] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL2180765 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| complement factor D/Complement factor D in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2176771] [GtoPdb: 2842] [UniProtKB: P00746] | ||||||||
| GtoPdb | - | - | 9 | pIC50 | 1 | nM | IC50 |
WO2012093101. Indole compounds or analogues thereof useful for the treatment of age-related macular degeneration (AMD). (2012); ACS Med Chem Lett (2012) 3: 781-2 [PMID:24900375] |
| ChEMBL | Inhibition of recombinant human complement factor D after 1 hr | B | 9 | pIC50 | 1 | nM | IC50 | ACS Med Chem Lett (2012) 3: 781-782 [PMID:24900375] |
| ChEMBL | In Vitro Assay: Recombinant human factor D (expressed in E. coli and purified using standard methods) at 10 nM concentration is incubated with test compound at various concentrations for 1 hour at room temperature in 0.1 M Hepes buffer, pH 7.5, containing 1 mM MgCl2, 1 M NaCl and 0.05% CHAPS. A synthetic substrate Z-Lys-thiobenzyl and 2,4-dinitrobenzenesulfonyl-fluoresceine are added to final concentrations of 200 μM and 25 μM, respectively. The increase in fluorescence is recorded at excitation of 485 nm and emission at 535 nm in a microplate spectrofluorimeter. IC50 values are calculated from percentage of inhibition of complement factor D-activity as a function of test compound concentration. | B | 9 | pIC50 | 1 | nM | IC50 | US-9085555-B2. Complement pathway modulators and uses thereof (2015) |
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]
