Basic Information
ID: ALA3888868
Type: Binding
Description: HIF-PH Assay: Ketoglutaric acid α-[1-14C]-sodium salt, alpha-ketoglutaric acid sodium salt, and HPLC purified peptide may be obtained from commercial sources, e.g., Perkin-Elmer (Wellesley Mass.), Sigma-Aldrich, and SynPep Corp. (Dublin Calif.), respectively. Peptides for use in the assay may be fragments of HIFα as described above or as disclosed in International Publication WO 2005/118836, incorporated by reference herein. HIF-pH, e.g., PHD1 (EGLN2) or PHD2 (EGLN1), can be expressed in, e.g., insect Hi5 cells, and partially purified, e.g., through a SP ion exchange chromatography column. Enzyme activity is determined by capturing 14CO2 using an assay described by Kivirikko and Myllyla (1982, Methods Enzymol. 82:245-304). Assay reactions contain 50 mM HEPES (pH 7.4), 100 μM α-ketoglutaric acid sodium salt, 0.30 mCi/mL ketoglutaric acid α-[1-14C]-sodium salt, 40 μM FeSO4, 1 mM ascorbate, 1541.8 units/mL Catalase, with or without 50 μM peptide substrate and various concentrations of compound of the invention. Reactions are initiated by addition of HIF-PH enzyme.
Organism: Homo sapiens
Cell type: BTI-TN-5B1-4
Activity Charts
Bioactivity
Activity Types for Assay ALA3888868
IC50
Compound Summary
| Parent Molecular Weight | ALogP | Polar Surface Area |
|---|---|---|
| 431.45 | 3.98 | 3.98 |
| 475.48 | 4.77 | 4.77 |
| 368.36 | 3.34 | 3.34 |
| 455.47 | 4.60 | 4.60 |
| 391.38 | 3.20 | 3.20 |
| 439.86 | 4.10 | 4.10 |
| 366.37 | 3.25 | 3.25 |
| 420.43 | 2.53 | 2.53 |
| 456.50 | 5.24 | 5.24 |
| 439.86 | 4.10 | 4.10 |
| 405.41 | 3.44 | 3.44 |
| 426.40 | 3.32 | 3.32 |
| 419.44 | 3.84 | 3.84 |
| 421.41 | 2.68 | 2.68 |
| 394.39 | 2.79 | 2.79 |
| 459.52 | 2.76 | 2.76 |
| 428.44 | 4.60 | 4.60 |
| 413.34 | 3.05 | 3.05 |
| 382.39 | 3.59 | 3.59 |
| 435.41 | 3.58 | 3.58 |
| 439.86 | 4.10 | 4.10 |
| 391.38 | 3.20 | 3.20 |
| 423.40 | 3.73 | 3.73 |
| 364.40 | 3.45 | 3.45 |
| 352.35 | 2.94 | 2.94 |
| 454.44 | 3.95 | 3.95 |
| 435.44 | 3.60 | 3.60 |
| 431.45 | 3.98 | 3.98 |
| 405.41 | 3.59 | 3.59 |
| 479.51 | 2.95 | 2.95 |
| 447.45 | 3.30 | 3.30 |
| 422.44 | 2.86 | 2.86 |
| 377.36 | 2.81 | 2.81 |
| 528.49 | 4.99 | 4.99 |
| 391.38 | 3.05 | 3.05 |
| 397.36 | 2.54 | 2.54 |
| 382.37 | 2.30 | 2.30 |
| 461.48 | 2.97 | 2.97 |
| 453.45 | 4.55 | 4.55 |
| 392.37 | 1.75 | 1.75 |
| 423.40 | 3.58 | 3.58 |
| 435.41 | 3.58 | 3.58 |
| 435.44 | 3.45 | 3.45 |
| 354.34 | 2.95 | 2.95 |
| 411.39 | 2.93 | 2.93 |
| 454.44 | 3.95 | 3.95 |
| 457.85 | 4.24 | 4.24 |
| 411.46 | 3.36 | 3.36 |
| 449.42 | 1.85 | 1.85 |
| 420.34 | 3.96 | 3.96 |
| 471.44 | 4.34 | 4.34 |
| 433.46 | 4.01 | 4.01 |
| 380.40 | 3.72 | 3.72 |
| 461.52 | 5.01 | 5.01 |
| 457.85 | 4.38 | 4.38 |
| 353.33 | 2.33 | 2.33 |
| 400.44 | 2.60 | 2.60 |
| 478.46 | 4.42 | 4.42 |
| 403.44 | 3.24 | 3.24 |
| 467.48 | 4.42 | 4.42 |
| 391.38 | 3.20 | 3.20 |
| 429.79 | 3.60 | 3.60 |
| 407.38 | 2.44 | 2.44 |
| 419.44 | 3.75 | 3.75 |
| 475.48 | 4.92 | 4.92 |
| 453.40 | 3.72 | 3.72 |
| 435.44 | 3.45 | 3.45 |
| 405.41 | 3.44 | 3.44 |
| 403.39 | 3.20 | 3.20 |
| 421.48 | 3.80 | 3.80 |
| 447.45 | 3.22 | 3.22 |
| 406.40 | 2.84 | 2.84 |
| 405.41 | 3.59 | 3.59 |
| 433.46 | 4.22 | 4.22 |
| 382.39 | 3.73 | 3.73 |
| 418.41 | 2.84 | 2.84 |
| 419.44 | 3.84 | 3.84 |
| 455.47 | 4.60 | 4.60 |
| 396.47 | 4.08 | 4.08 |
| 422.44 | 3.34 | 3.34 |
| 407.38 | 2.17 | 2.17 |
| 367.36 | 1.87 | 1.87 |
| 441.39 | 3.72 | 3.72 |
| 526.51 | 3.71 | 3.71 |
| 419.44 | 3.82 | 3.82 |
| 495.51 | 2.61 | 2.61 |
| 471.44 | 4.69 | 4.69 |
| 396.47 | 3.93 | 3.93 |
| 453.45 | 4.20 | 4.20 |
| 353.33 | 2.33 | 2.33 |
| 380.40 | 3.57 | 3.57 |
| 487.90 | 5.20 | 5.20 |
| 417.42 | 3.73 | 3.73 |
| 405.41 | 3.43 | 3.43 |
| 368.35 | 1.91 | 1.91 |
| 405.37 | 2.38 | 2.38 |
| 417.42 | 3.44 | 3.44 |
| 407.38 | 2.17 | 2.17 |
| 414.46 | 2.99 | 2.99 |
| 492.49 | 3.31 | 3.31 |
| 419.44 | 3.37 | 3.37 |
| 366.37 | 3.33 | 3.33 |
| 433.46 | 4.23 | 4.23 |
| 487.90 | 5.20 | 5.20 |
| 423.40 | 3.58 | 3.58 |
| 467.48 | 4.28 | 4.28 |
| 453.45 | 4.55 | 4.55 |
| 501.93 | 5.25 | 5.25 |
| 467.48 | 4.86 | 4.86 |
| 477.48 | 2.45 | 2.45 |
| 457.85 | 4.24 | 4.24 |
| 408.41 | 2.47 | 2.47 |
| 419.44 | 3.23 | 3.23 |
| 417.47 | 3.44 | 3.44 |
| 406.40 | 2.14 | 2.14 |
| 361.36 | 2.68 | 2.68 |
| 416.38 | 4.00 | 4.00 |
| 352.35 | 2.94 | 2.94 |
| 407.38 | 2.17 | 2.17 |
| 366.37 | 3.33 | 3.33 |
| 428.44 | 4.33 | 4.33 |
| 406.46 | 2.25 | 2.25 |
| 445.48 | 4.51 | 4.51 |
| 410.43 | 3.58 | 3.58 |
| 433.46 | 4.21 | 4.21 |
| 419.44 | 3.98 | 3.98 |
| 405.41 | 3.44 | 3.44 |
| 423.47 | 3.55 | 3.55 |
| 405.41 | 3.44 | 3.44 |
| 432.84 | 4.37 | 4.37 |
| 393.36 | 1.78 | 1.78 |
| 392.41 | 3.57 | 3.57 |
| 379.42 | 3.67 | 3.67 |
| 410.43 | 3.73 | 3.73 |
| 412.38 | 2.93 | 2.93 |
| 546.58 | 4.58 | 4.58 |
| 405.41 | 3.59 | 3.59 |
| 423.47 | 3.40 | 3.40 |
| 382.44 | 3.69 | 3.69 |
| 419.44 | 3.84 | 3.84 |
| 405.41 | 3.59 | 3.59 |
| 405.41 | 3.44 | 3.44 |
| 421.41 | 2.82 | 2.82 |
| 410.39 | 1.76 | 1.76 |
| 393.36 | 1.78 | 1.78 |
| 447.49 | 4.47 | 4.47 |
| 394.43 | 3.96 | 3.96 |
| 450.43 | 3.04 | 3.04 |
| 389.41 | 3.32 | 3.32 |
| 464.43 | 2.53 | 2.53 |
| 408.41 | 3.18 | 3.18 |
| 380.40 | 3.72 | 3.72 |
| 419.44 | 3.75 | 3.75 |
| 423.40 | 3.58 | 3.58 |
| 398.37 | 1.92 | 1.92 |
| 419.44 | 3.84 | 3.84 |
| 378.43 | 3.37 | 3.37 |
| 471.44 | 4.34 | 4.34 |
| 447.49 | 4.47 | 4.47 |
| 459.50 | 4.76 | 4.76 |
| 417.42 | 3.59 | 3.59 |
| 471.54 | 2.90 | 2.90 |
| 405.41 | 3.44 | 3.44 |
| 483.48 | 3.39 | 3.39 |
| 417.42 | 3.59 | 3.59 |
| 453.40 | 3.87 | 3.87 |
| 391.38 | 3.20 | 3.20 |
| 467.48 | 4.42 | 4.42 |
| 406.40 | 2.14 | 2.14 |
| 418.41 | 2.98 | 2.98 |
| 407.38 | 2.17 | 2.17 |
| 392.41 | 3.72 | 3.72 |
| 405.41 | 3.44 | 3.44 |
| 391.38 | 3.05 | 3.05 |
| 448.44 | 2.31 | 2.31 |
| 453.45 | 4.55 | 4.55 |
| 481.51 | 4.81 | 4.81 |
| 423.47 | 3.51 | 3.51 |
| 405.41 | 3.59 | 3.59 |
| 431.45 | 3.98 | 3.98 |
| 483.48 | 3.39 | 3.39 |
| 477.48 | 2.50 | 2.50 |
| 433.49 | 3.95 | 3.95 |