| # | Aladdin ID | Assay Type | Description | Organism | Compounds | Reference | BAO Format | Source | |
|---|---|---|---|---|---|---|---|---|---|
| 1. | ALA3705877 | B | Inhibition Assay: A similar assay procedure as described in Test 2 was used for HDAC6. Human recombinant full length HDAC6 expressed in a baculovirus expression system was purchased from BPS BioSciences (San Diego, Calif., U.S.A.). The substrate used in the HDAC1 assay was 5 uM of acetyl-Gly-Ala-Lys(acetyl)-AMC. TEST 2: Human recombinant HDAC4 was expressed in full length form (aa 2-1084) in Sf9 insect cells (obtained from ATCC) using baculovirus generated with Bac-to-Bac system (Invitrogen). Test compounds were serially diluted to reach final test concentrations from 0.000128 uM to 10 uM. HDAC4 and test compounds were incubated in 25 mM Tris buffer pH 8.0 containing 137 mM NaCl, 2.7 mM KCl, 1 mM MgCl2, 0.05% (w/v) bovine serum albumine and 0.005% (v/v) Triton-X-100 for 2 hours at room temperature in presence of 5 uM of acetyl-Gly-Ala-Lys(E-trifluoroacetyl)-AMC (AMC=7-amino-4-methyl coumarin) in a final volume of 9 ul. Control wells with HDAC4 only (positive control). | Homo sapiens | 148 | cell-based format | BindingDB Database | ||
| 2. | ALA3705878 | B | Inhibition Assay: A similar assay procedure as described in Test 2 was used for HDAC1. Human recombinant full length HDAC1 expressed in a baculovirus expression system was purchased from BPS BioSciences (San Diego, Calif., U.S.A.). The substrate used in the HDAC1 assay was 5 uM of acetyl-Gly-Ala-Lys(acetyl)-AMC. TEST 2: Human recombinant HDAC4 was expressed in full length form (aa 2-1084) in Sf9 insect cells (obtained from ATCC) using baculovirus generated with Bac-to-Bac system (Invitrogen). Test compounds were serially diluted to reach final test concentrations from 0.000128 uM to 10 uM. HDAC4 and test compounds were incubated in 25 mM Tris buffer pH 8.0 containing 137 mM NaCl, 2.7 mM KCl, 1 mM MgCl2, 0.05% (w/v) bovine serum albumine and 0.005% (v/v) Triton-X-100 for 2 hours at room temperature in presence of 5 uM of acetyl-Gly-Ala-Lys(E-trifluoroacetyl)-AMC (AMC=7-amino-4-methyl coumarin) in a final volume of 9 ul. Control wells with HDAC4 only (positive control). | Homo sapiens | 148 | cell-based format | BindingDB Database | ||
| 3. | ALA3705880 | B | Inhibition Assay: Human recombinant HDAC4 was expressed in full length form (aa 2-1084) in Sf9 insect cells (obtained from ATCC) using baculovirus generated with Bac-to-Bac system (Invitrogen). Test compounds were serially diluted to reach final test concentrations from 0.000128 uM to 10 uM. HDAC4 and test compounds were incubated in 25 mM Tris buffer pH 8.0 containing 137 mM NaCl, 2.7 mM KCl, 1 mM MgCl2, 0.05% (w/v) bovine serum albumine and 0.005% (v/v) Triton-X-100 for 2 hours at room temperature in presence of 5 uM of acetyl-Gly-Ala-Lys(E-trifluoroacetyl)-AMC (AMC=7-amino-4-methyl coumarin) in a final volume of 9 ul. Control wells with HDAC4 only (positive control) and without HDAC4 (negative control) were included on the microplate. Bovine trypsin (4.5 ul of a 300 nM solution) was added and the plate incubated for additional 15 minutes at room temperature. The plate was placed in a fluorescence microplate reader, and read at an excitation wavelength of 360 nm. | Homo sapiens | 148 | cell-based format | BindingDB Database | ||
| 4. | ALA4689587 | B | Inhibition of HDAC4 (unknown origin) using Boc Lys(TFA) as substrate by fluorogenic assay | Homo sapiens | 20 | single protein format | Scientific Literature | ||
| 5. | ALA4689588 | B | Inhibition of HDAC5 (unknown origin) using Boc Lys(TFA) as substrate by fluorogenic assay | Homo sapiens | 3 | single protein format | Scientific Literature | ||
| 6. | ALA4689589 | B | Inhibition of HDAC7 (unknown origin) using Boc Lys(TFA) as substrate by fluorogenic assay | Homo sapiens | 3 | single protein format | Scientific Literature | ||
| 7. | ALA4689590 | B | Inhibition of HDAC9 (unknown origin) using Boc Lys(TFA) as substrate by fluorogenic assay | Homo sapiens | 3 | single protein format | Scientific Literature | ||
| 8. | ALA4689591 | A | Inhibition of HDAC1 (unknown origin) using Ac-Arg-Gly-Lys(Ac) as substrate by fluorogenic assay | Homo sapiens | 3 | single protein format | Scientific Literature | ||
| 9. | ALA4689592 | A | Inhibition of HDAC2 (unknown origin) using Ac-Arg-Gly-Lys(Ac) as substrate by fluorogenic assay | Homo sapiens | 3 | single protein format | Scientific Literature | ||
| 10. | ALA4689593 | A | Inhibition of HDAC3/NCOR2 (unknown origin) using Boc-Lys(Ac) as substrate by fluorogenic assay | Homo sapiens | 3 | protein complex format | Scientific Literature | ||
| 11. | ALA4689594 | A | Inhibition of HDAC8 (unknown origin) using Boc-Lys(TFA) as substrate by fluorogenic assay | Homo sapiens | 3 | single protein format | Scientific Literature | ||
| 12. | ALA4689595 | A | Inhibition of HDAC6 (unknown origin) expressed in human HEK-Freestyle cells using Boc-Lys(Ac) as substrate by fluorogenic assay | Homo sapiens | 3 | cell-based format | Scientific Literature | ||
| 13. | ALA4689596 | A | Inhibition of Class 1/2b HDAC in human Jurkat E6.1 cells using Boc-Lys-(Ac)-AMC as substrate by fluorogenic assay | Homo sapiens | 16 | cell-based format | Scientific Literature | ||
| 14. | ALA4689597 | B | Inhibition of Class 2A HDAC4 in human Jurkat E6.1 cells using Boc-Lys-(TFA)-AMC as substrate by fluorogenic assay | Homo sapiens | 20 | cell-based format | Scientific Literature | ||
| 15. | ALA4689598 | A | Intrinsic Clearance in mouse liver microsomes | Mus musculus | 10 | microsome format | Scientific Literature | ||
| 16. | ALA4689599 | A | Efflux ratio of permeability from basolateral to apical over apical to basolateral side in dog MDCK-MDR1 cells relative to wild type MDCK cells | Canis lupus familiaris | 10 | cell-based format | Scientific Literature | ||
| 17. | ALA4689600 | A | Apparent permeability of the compound in dog MDCK-MDR1 cells | Canis lupus familiaris | 2 | cell-based format | Scientific Literature | ||
| 18. | ALA4689601 | P | Kinetic solubility of the compound | 10 | small-molecule physicochemical format | Scientific Literature | |||
| 19. | ALA4689602 | B | Binding affinity to immobilized HDAC4 catalytic domain (unknown origin) by surface plasmon resonance assay | Homo sapiens | 1 | single protein format | Scientific Literature | ||
| 20. | ALA4689605 | B | Binding affinity to immobilized HDAC4 catalytic domain (unknown origin) assessed as residence time by surface plasmon resonance assay | Homo sapiens | 1 | single protein format | Scientific Literature |
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