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ChEMBL ligand: CHEMBL3683753 |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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complement factor D/Complement factor D in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2176771] [GtoPdb: 2842] [UniProtKB: P00746] | ||||||||
ChEMBL | Inhibition of complement factor D in human whole blood assessed as decrease in zymosan-induced AP activation mediated soluble MAC complex formation preincubated for 15 mins followed by zymosan addition measured after 40 mins by ELISA | B | 7.96 | pIC50 | 11 | nM | IC50 | J Med Chem (2017) 60: 5717-5735 [PMID:28621538] |
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 | 8.05 | pIC50 | 9 | nM | IC50 | US-9085555-B2. Complement pathway modulators and uses thereof (2015) |
GtoPdb | Measuring inhibition of recombinant human complement FD catalytic domain, using a thioesterolysis-based assay with Z-Lys-thiobenzylester as the substrate. | - | 8.22 | pIC50 | 6 | nM | IC50 | J Med Chem (2017) 60: 5717-5735 [PMID:28621538] |
ChEMBL | Inhibition of recombinant human complement factor D catalytic domain using Z-Lys-thiobenzylester as substrate preincubated for 1 hr followed by substrate addition by 2,4-dinitrobenzenesulfonyl-2,7-desmethyl-fluorecein probe based spectrofluorimetric assay | B | 8.3 | pIC50 | 5 | nM | IC50 | J Med Chem (2017) 60: 5717-5735 [PMID:28621538] |
Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809] | ||||||||
ChEMBL | Inhibition of dofetilide binding to human ERG | B | 4.52 | pIC50 | >30000 | nM | IC50 | J Med Chem (2017) 60: 5717-5735 [PMID:28621538] |
ChEMBL data shown on this page come from version 28:
Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]