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 34:

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]