ChEMBL ligand: CHEMBL4250860 (Ach-0144471, ACH-0144471, ACH-4471, Danicopan, Voydeya)
complement factor D/Complement factor D in Human [ChEMBL: CHEMBL2176771] [GtoPdb: 2842] [UniProtKB: P00746] 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
complement factor D/Complement factor D in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2176771] [GtoPdb: 2842] [UniProtKB: P00746]
GtoPdb	Binding affinity to human factor D as determined in a SPR assay	-	9	pKd	1	nM	Kd	J Med Chem (2018) 61: 3253-3276 [PMID:28977749]
ChEMBL	Binding affinity to human factor D by SPR analysis	B	9	pKd	<1	nM	Kd	J Med Chem (2018) 61: 3253-3276 [PMID:28977749]
ChEMBL	Factor D Assay: Human factor D (purified from human serum, Complement Technology, Inc.) at 80 nM final concentration is incubated with test compound at various concentrations for 5 minutes at room temperature in 50 mM Tris, 1M NaCl, pH 7.5. A synthetic substrate Z-L-Lys-SBzl and DTNB (Ellman's reagent) are added to final concentrations of 100 μM each. The increase in color is recorded at OD405 nm in a microplate in kinetic mode over 30 minutes with 30 second time points in a spectrofluorimeter. IC50 values are calculated by non-linear regression from the percentage of inhibition of complement factor D activity as a function of test compound concentration.	B	6	pIC50	<1000	nM	IC50	US-9796741-B2. Aryl, heteroaryl, and heterocyclic compounds for treatment of complement mediated disorders (2017)
ChEMBL	Human Factor D Assay: Human Factor D (purified from human serum, Complement Technology, Inc.) at 80 nM final concentration was incubated with test compound at various concentrations for 5 minutes at room temperature in 50 mM Tris, 1M NaCl, pH 7.5. A synthetic substrate Z-L-Lys-SBzl and DTNB (Ellman's reagent) are added to final concentrations of 100 μM each. Absorbance at 405 nm (A405) was recorded at 30 second intervals for 30 minutes using a microplate spectrophotometer. IC50 values are calculated by nonlinear regression of complement Factor D reaction rates as a function of test compound concentration.	B	6	pIC50	<1000	nM	IC50	US-10287301-B2. Aryl, heteroaryl, and heterocyclic compounds for treatment of medical disorders (2019)
ChEMBL	Inhibition Assay: Human Factor D (purified from human serum, Complement Technology, Inc.) at 80 nM final concentration was incubated with test compound at various concentrations for 5 minutes at room temperature in 50 mM Tris, 1M NaCl, pH 7.5. A synthetic substrate Z-L-Lys-SBzl and DTNB (Ellman's reagent) are added to final concentrations of 100 μM each. Absorbance at 405 nm (A405) was recorded at 30 second intervals for 30 minutes using a microplate spectrophotometer. IC50 values are calculated by nonlinear regression of complement Factor D reaction rates as a function of test compound concentration.	B	6	pIC50	<1000	nM	IC50	US-10822352-B2. Aryl, heteroaryl, and heterocyclic compounds for treatment of medical disorders (2020)
ChEMBL	Inhibition of human factor D using C3b as substrate assessed as decrease in formation of factor B cleavage product Ba	B	7.82	pIC50	15	nM	IC50	J Med Chem (2018) 61: 3253-3276 [PMID:28977749]
ChEMBL	Inhibition of factor D in human serum assessed as decrease in alternative pathway of complement-mediated hemolysis of PNH erythrocytes	B	8.4	pIC50	4	nM	IC50	J Med Chem (2018) 61: 3253-3276 [PMID:28977749]
ChEMBL	Inhibition of factor D in human serum assessed as decrease in C3 deposition on PNH erythrocytes	B	8.4	pIC50	4	nM	IC50	J Med Chem (2018) 61: 3253-3276 [PMID:28977749]

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]