Assay Detail
Binding
CHEMBL3705899
Review assay metadata, readout intent, target linkage, and publication context from the same page.
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.
773
Total Activities
768
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Complement pathway modulators and uses thereof
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 773 | 6.81 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2180765 | — | — | 1 | 9.00 |
| CHEMBL2180764 | — | — | 1 | 8.70 |
| CHEMBL3678905 | — | — | 1 | 8.52 |
| CHEMBL3683717 | — | — | 2 | 8.52 |
| CHEMBL3678945 | — | — | 1 | 8.52 |
| CHEMBL3678910 | — | — | 1 | 8.52 |
| CHEMBL3673804 | — | — | 1 | 8.52 |
| CHEMBL3673802 | — | — | 1 | 8.52 |
| CHEMBL3673750 | — | — | 1 | 8.52 |
| CHEMBL3673724 | — | — | 1 | 8.52 |
| CHEMBL3668673 | — | — | 1 | 8.52 |
| CHEMBL2180766 | — | — | 1 | 8.52 |
| CHEMBL3673812 | — | — | 1 | 8.40 |
| CHEMBL3683739 | — | — | 1 | 8.40 |
| CHEMBL3683725 | — | — | 1 | 8.40 |
| CHEMBL3683724 | — | — | 1 | 8.40 |
| CHEMBL3683720 | — | — | 1 | 8.40 |
| CHEMBL3678944 | — | — | 1 | 8.40 |
| CHEMBL3673738 | — | — | 1 | 8.40 |
| CHEMBL3673732 | — | — | 1 | 8.40 |
| CHEMBL3668636 | — | — | 1 | 8.40 |
| CHEMBL3668669 | — | — | 1 | 8.30 |
| CHEMBL3673726 | — | — | 1 | 8.30 |
| CHEMBL3673793 | — | — | 1 | 8.30 |
| CHEMBL3673808 | — | — | 1 | 8.30 |
| CHEMBL3678852 | — | — | 1 | 8.30 |
| CHEMBL3678898 | — | — | 1 | 8.30 |
| CHEMBL3683719 | — | — | 1 | 8.30 |
| CHEMBL3965664 | — | — | 1 | 8.30 |
| CHEMBL3683730 | — | — | 1 | 8.30 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2180765 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL2180764 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3683717 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3678945 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL2180766 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3673724 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3668673 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3678910 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3673750 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3678905 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3673802 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3673804 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3683739 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3683720 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3678944 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3673732 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3683724 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3683725 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3673738 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3668636 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3673812 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3678898 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3683730 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3683737 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3965664 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3683719 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3683717 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3668669 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3673793 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3673808 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3678852 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3673726 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3678879 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL3678913 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL3678906 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL3668685 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL3668710 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL3668640 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL3683722 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL3673730 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL3663978 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL3683732 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL3663968 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL3683746 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL3673860 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL3673821 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL3673814 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL3673752 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL3673822 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL3668711 | — | IC50 | = | 7.0 | nM | 8.15 |