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# | Aladdin ID | Assay Type | Description | Organism | Compounds | Reference | BAO Format | Source | |
---|---|---|---|---|---|---|---|---|---|
1. | ALA3602882 | Binding | Antagonist activity at cIAP1-BIR3 domain (unknown origin) assessed as inhibition of interaction with SMAC at 5 mM by fluorescence polarization assay relative to control | Homo sapiens | 2 | ALA3600342 | single protein format | Scientific Literature | |
2. | ALA3602883 | Binding | Antagonist activity at cIAP1-BIR3 domain (unknown origin) assessed as inhibition of interaction with SMAC at 0.01 uM by fluorescence polarization assay relative to control | Homo sapiens | 1 | ALA3600342 | single protein format | Scientific Literature | |
3. | ALA3602888 | Binding | Antagonist activity at cIAP1 in human EVSA-T cells after 2 hrs | Homo sapiens | 1 | ALA3600342 | cell-based format | Scientific Literature | |
4. | ALA3602889 | Binding | Antagonist activity at cIAP1 in human EVSA-T cells assessed as increase in cleaved caspase-3 level after 6 hrs | Homo sapiens | 1 | ALA3600342 | cell-based format | Scientific Literature | |
5. | ALA3602896 | Binding | Antagonist activity at cIAP1-BIR3 domain (unknown origin) assessed as inhibition of interaction with SMAC by fluorescence polarization assay | Homo sapiens | 8 | ALA3600342 | single protein format | Scientific Literature | |
6. | ALA3603531 | Binding | Inhibition of cIAP (unknown origin) assessed as inhibition of cIAP-BIR3 interaction by TR-FRET assay | Homo sapiens | 1 | ALA3600357 | single protein format | Scientific Literature | |
7. | ALA3707980 | Binding | Fluorescence Polarization (FP) Based Competitive Assay: Binding affinities of the present compounds to XIAP linker-BIR2-BIR3 (residues 120-356), cIAP1-BIR3 (residues 253-363), and cIAP-2 BIR3 (residues 238-349) proteins were determined by fluorescence polarization (FP) based competitive assays. For cIAP-1 BIR3 and cIAP-2 BIR3 assays, a fluorescently labeled Smac mimetic (Smac-2F) was used as the fluorescent probe. The Kd values of Smac-2F to cIAP-1 BIR3 and cIAP-2 BIR3 were determined by monitoring the total fluorescence polarization of mixtures composed with the fluorescent probe at a fixed concentration and proteins with increasing concentrations up to full saturation. Fluorescence polarization values were measured using the Infinite M-1000 plate reader (Tecan U.S., Research Triangle Park, N.C.) in Microfluor 2 96-well, black, round-bottom plates (Thermo Scientific). To each well, 1 nM of SMAC-2F and increasing concentrations of protein were added to a final volume of 125 ul in the assay buffer (100 mM potassium phosphate, pH 7.5). | 50 | ALA3639096 | single protein format | BindingDB Database | ||
8. | ALA3707783 | Binding | In vitro Competitive Displacement Binding Assays : Modified SMAC peptides and compounds were tested for their ability to displace the fluorescent tracer from either XIAP, clAP-1 or clAP-2. BIR3 domains of clAP-1 , clAP-2 and XIAP were incubated with test compounds or SMAC based peptides and their respective peptide probes (Peptide Protein Research) in assay buffer (50mM Hepes pH 7.5, 0.025% Tween-20, 0.01 % BSA, and 1 mM DTT). Positive controls consisted of BIR3 proteins and tracer (no inhibition) and negative controls contained tracer only (100% inhibition). The samples were incubated at room temperature for 1 hr (XIAP and clAP-2) or 3hrs (clAP-1 ) prior to being read in the BMG Pherastar in Fluorescence Polarization mode (FP 485nm, 520nm, 520nm). | 162 | ALA3639218 | single protein format | BindingDB Database | ||
9. | ALA3707504 | Binding | Fluorescence Polarization-Based Assays: An in vitro fluorescence polarization (FP) based binding assay was used to test the binding ability of the compounds of the present invention to certain IAP proteins (Nikolovska-Coleska et al., Anal. Biochem. 332:261-73 (2004)). he FP-based assay for XIAP BIR3 protein was described in detail previously (Nikolovska-Coleska et al., Anal. Biochem. 332:261-73 (2004)). Briefly, 5-carboxyfluorescein was coupled to the lysine side chain of a mutated Smac peptide with the sequence (AbuRPFK-Fam) and this fluorescently tagged peptide (named SM5F) was used as the fluorescent tracer in FP-based binding assay to XIAP BIR3. | Homo sapiens | 5 | ALA3639255 | single protein format | BindingDB Database | |
10. | ALA3804166 | Binding | Induction of cIAP1 degradation in human MCF7 cells at 1 uM after 6 hrs by by Western blot analysis | Homo sapiens | 1 | ALA3797167 | cell-based format | Scientific Literature | |
11. | ALA3804407 | Binding | Induction of cIAP1 degradation in human MCF7 cells after 6 hrs by by Western blot analysis | Homo sapiens | 1 | ALA3797167 | cell-based format | Scientific Literature | |
12. | ALA3804412 | Binding | Induction of cIAP1 degradation in human MCF7 cells at 10 to 20 uM after 6 hrs by Western blot analysis in presence of MG132 | Homo sapiens | 1 | ALA3797167 | cell-based format | Scientific Literature | |
13. | ALA1106517 | Binding | Binding affinity to cIAP1 BIR3 domain by fluorescence polarization assay | 3 | ALA1157823 | single protein format | Scientific Literature | ||
14. | ALA1248007 | Binding | Displacement of fluorescent SM5F peptide from His-tagged human cIAP1 BIR3 domain expressed in Escherichia coli BL21(DE3) cells by fluorescence polarization-based assay | Homo sapiens | 7 | ALA1240488 | cell-based format | Scientific Literature | |
15. | ALA1777015 | Binding | Competitive inhibition of human cIAP1 BIR3 domain after 2 to 3 hrs by fluorescence polarization assay | Homo sapiens | 16 | ALA1772970 | single protein format | Scientific Literature | |
16. | ALA1777016 | Binding | Binding affinity to human cIAP1 BIR3 domain after 2 to 3 hrs by fluorescence polarization-based assay | Homo sapiens | 16 | ALA1772970 | single protein format | Scientific Literature | |
17. | ALA1777017 | Binding | Competitive inhibition of human cIAP1BIR2-BIR3 domain after 2 to 3 hrs by fluorescence polarization assay | Homo sapiens | 16 | ALA1772970 | single protein format | Scientific Literature | |
18. | ALA1777018 | Binding | Binding affinity to human cIAP1 BIR2-BIR3 domain after 2 to 3 hrs by fluorescence polarization-based assay | Homo sapiens | 16 | ALA1772970 | single protein format | Scientific Literature | |
19. | ALA4351161 | Binding | Binding affinity to cIAP1-BIR3 domain (unknown origin) | Homo sapiens | 8 | ALA4350953 | single protein format | Scientific Literature | |
20. | ALA4351164 | Binding | Induction of cIAP1 (unknown origin) degradation | Homo sapiens | 1 | ALA4350953 | single protein format | Scientific Literature |
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