Basic Information
ID: ALA3706128
Type: Binding
Description: Enzyme Assay: Ketoglutaric acid alpha -[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 HIFalpha as described above or as disclosed in International Publication WO 2005/118836, incorporated by reference herein. For example, a HIF peptide for use in the HIF-PH assay is [methoxycoumarin]-DLDLEALAPYIPADDDFQL-amide. HIF-PH, e.g., HIF-PH2 (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 uM alpha -ketoglutaric acid sodium salt, 0.30 uCi/mL ketoglutaric acid alpha -[1-14C]-sodium sodium salt.
Organism: Homo sapiens
Cell type: BTI-TN-5B1-4
Activity Charts
Bioactivity
Activity Types for Assay ALA3706128
IC50
Compound Summary
| Parent Molecular Weight | ALogP | Polar Surface Area |
|---|---|---|
| 355.35 | 1.08 | 1.08 |
| 367.36 | 1.27 | 1.27 |
| 443.46 | 2.56 | 2.56 |
| 429.43 | 2.63 | 2.63 |
| 381.39 | 1.58 | 1.58 |
| 392.37 | 1.14 | 1.14 |
| 353.33 | 0.96 | 0.96 |
| 369.38 | 1.39 | 1.39 |
| 380.36 | 0.95 | 0.95 |
| 444.45 | 2.34 | 2.34 |
| 457.49 | 2.75 | 2.75 |
| 443.46 | 2.94 | 2.94 |
| 505.53 | 4.30 | 4.30 |
| 454.44 | 2.50 | 2.50 |
| 468.47 | 2.89 | 2.89 |
| 506.52 | 3.69 | 3.69 |
| 468.47 | 2.43 | 2.43 |
| 482.50 | 2.82 | 2.82 |
| 457.49 | 2.86 | 2.86 |
| 471.51 | 3.25 | 3.25 |
| 520.55 | 3.62 | 3.62 |
| 534.57 | 4.01 | 4.01 |
| 482.50 | 3.28 | 3.28 |
| 496.52 | 3.67 | 3.67 |
| 496.52 | 3.53 | 3.53 |
| 353.33 | 0.96 | 0.96 |
| 367.36 | 1.35 | 1.35 |
| 395.42 | 1.99 | 1.99 |
| 381.39 | 1.74 | 1.74 |
| 395.42 | 2.14 | 2.14 |
| 386.41 | 2.48 | 2.48 |
| 309.33 | 1.51 | 1.51 |
| 296.28 | 1.85 | 1.85 |
| 323.35 | 1.85 | 1.85 |
| 295.30 | 1.25 | 1.25 |
| 337.38 | 2.29 | 2.29 |
| 335.36 | 2.04 | 2.04 |
| 334.34 | 1.38 | 1.38 |
| 360.37 | 1.91 | 1.91 |
| 487.52 | 4.01 | 4.01 |
| 410.43 | 3.05 | 3.05 |
| 544.57 | 4.11 | 4.11 |
| 544.57 | 4.11 | 4.11 |
| 367.36 | 1.27 | 1.27 |
| 448.41 | 2.17 | 2.17 |
| 429.43 | 2.63 | 2.63 |
| 378.34 | 0.84 | 0.84 |
| 411.42 | 2.35 | 2.35 |
| 392.37 | 1.23 | 1.23 |
| 420.43 | 1.86 | 1.86 |
| 468.47 | 2.45 | 2.45 |
| 420.43 | 2.01 | 2.01 |
| 353.33 | 0.96 | 0.96 |
| 367.36 | 1.35 | 1.35 |
| 378.34 | 0.84 | 0.84 |
| 468.47 | 2.45 | 2.45 |
| 392.37 | 1.22 | 1.22 |
| 392.37 | 1.22 | 1.22 |
| 433.47 | 1.08 | 1.08 |
| 412.41 | 1.74 | 1.74 |
| 422.40 | 0.85 | 0.85 |
| 432.44 | 2.01 | 2.01 |
| 369.38 | 1.53 | 1.53 |
| 413.39 | 0.98 | 0.98 |
| 427.41 | 1.37 | 1.37 |
| 371.39 | 1.36 | 1.36 |
| 415.40 | 0.82 | 0.82 |
| 429.43 | 1.21 | 1.21 |
| 353.33 | 0.96 | 0.96 |
| 367.36 | 1.35 | 1.35 |
| 395.42 | 1.99 | 1.99 |
| 386.41 | 2.48 | 2.48 |
| 447.50 | 2.06 | 2.06 |
| 277.24 | -0.17 | -0.17 |
| 309.33 | 1.51 | 1.51 |
| 459.50 | 3.14 | 3.14 |
| 413.43 | 1.54 | 1.54 |
| 463.47 | 3.24 | 3.24 |
| 334.34 | 1.38 | 1.38 |
| 448.41 | 2.17 | 2.17 |
| 462.44 | 2.56 | 2.56 |
| 377.36 | 0.59 | 0.59 |
| 385.42 | 3.18 | 3.18 |
| 443.46 | 3.02 | 3.02 |
| 397.39 | 0.98 | 0.98 |
| 377.36 | 0.59 | 0.59 |
| 462.44 | 2.56 | 2.56 |
| 490.49 | 3.19 | 3.19 |
| 423.47 | 1.59 | 1.59 |
| 402.43 | 0.17 | 0.17 |
| 434.37 | 1.56 | 1.56 |
| 380.40 | 1.02 | 1.02 |
| 392.37 | 1.23 | 1.23 |
| 405.41 | 0.89 | 0.89 |
| 380.40 | 1.02 | 1.02 |
| 448.40 | 1.90 | 1.90 |
| 437.50 | 1.93 | 1.93 |
| 410.43 | 1.58 | 1.58 |
| 430.49 | 0.77 | 0.77 |
| 416.46 | 0.43 | 0.43 |
| 448.40 | 1.95 | 1.95 |
| 437.50 | 1.98 | 1.98 |
| 395.42 | 0.94 | 0.94 |
| 430.49 | 0.77 | 0.77 |
| 427.44 | 0.04 | 0.04 |
| 456.50 | 2.68 | 2.68 |
| 506.58 | 2.44 | 2.44 |
| 510.47 | 3.23 | 3.23 |
| 485.54 | 2.87 | 2.87 |
| 416.46 | 0.43 | 0.43 |
| 381.39 | 1.66 | 1.66 |
| 453.46 | 2.26 | 2.26 |
| 471.51 | 3.66 | 3.66 |
| 380.40 | 0.97 | 0.97 |
| 394.43 | 1.36 | 1.36 |
| 442.48 | 2.29 | 2.29 |
| 520.55 | 4.08 | 4.08 |
| 519.56 | 4.69 | 4.69 |
| 457.49 | 3.33 | 3.33 |
| 445.48 | 2.86 | 2.86 |
| 367.36 | 1.35 | 1.35 |
| 471.51 | 3.14 | 3.14 |
| 444.45 | 2.42 | 2.42 |
| 444.45 | 2.42 | 2.42 |
| 457.49 | 3.41 | 3.41 |
| 381.39 | 1.66 | 1.66 |
| 449.49 | 3.08 | 3.08 |
| 444.45 | 2.42 | 2.42 |
| 492.56 | 2.10 | 2.10 |
| 531.59 | 2.31 | 2.31 |
| 520.61 | 2.75 | 2.75 |
| 582.68 | 4.11 | 4.11 |
| 583.67 | 3.50 | 3.50 |
| 457.49 | 3.22 | 3.22 |
| 429.43 | 2.96 | 2.96 |
| 443.46 | 2.89 | 2.89 |
| 367.36 | 1.51 | 1.51 |
| 468.47 | 2.89 | 2.89 |
| 473.49 | 3.03 | 3.03 |
| 450.48 | 2.48 | 2.48 |
| 457.49 | 3.41 | 3.41 |
| 473.49 | 3.03 | 3.03 |
| 468.47 | 2.89 | 2.89 |
| 445.44 | 1.81 | 1.81 |
| 521.55 | 2.43 | 2.43 |
| 511.46 | 4.04 | 4.04 |
| 528.57 | 2.86 | 2.86 |
| 491.48 | 3.17 | 3.17 |
| 527.46 | 3.92 | 3.92 |
| 519.56 | 4.24 | 4.24 |
| 447.45 | 1.76 | 1.76 |
| 445.44 | 1.81 | 1.81 |
| 488.50 | 1.88 | 1.88 |
| 449.51 | 3.55 | 3.55 |
| 451.48 | 2.40 | 2.40 |
| 450.48 | 2.48 | 2.48 |
| 521.53 | 3.48 | 3.48 |
| 521.53 | 3.48 | 3.48 |
| 471.51 | 3.80 | 3.80 |
| 534.57 | 4.47 | 4.47 |
| 548.60 | 4.86 | 4.86 |
| 506.52 | 4.02 | 4.02 |
| 444.45 | 2.57 | 2.57 |
| 534.57 | 4.28 | 4.28 |
| 520.55 | 4.08 | 4.08 |
| 521.53 | 3.48 | 3.48 |
| 457.49 | 3.58 | 3.58 |
| 471.51 | 3.97 | 3.97 |
| 550.57 | 4.09 | 4.09 |
| 554.99 | 4.74 | 4.74 |
| 457.49 | 3.58 | 3.58 |
| 471.51 | 3.97 | 3.97 |
| 534.57 | 4.64 | 4.64 |
| 534.57 | 4.64 | 4.64 |
| 538.54 | 4.22 | 4.22 |
| 534.57 | 4.39 | 4.39 |
| 534.57 | 4.39 | 4.39 |
| 588.54 | 5.10 | 5.10 |
| 550.57 | 4.09 | 4.09 |
| 528.57 | 3.46 | 3.46 |
| 526.59 | 4.62 | 4.62 |
| 463.53 | 3.94 | 3.94 |
| 550.57 | 4.09 | 4.09 |
| 487.51 | 3.42 | 3.42 |
| 473.49 | 3.03 | 3.03 |
| 487.51 | 3.42 | 3.42 |
| 455.47 | 3.16 | 3.16 |
| 532.56 | 4.23 | 4.23 |
| 548.60 | 4.72 | 4.72 |
| 565.59 | 3.88 | 3.88 |
| 520.55 | 4.08 | 4.08 |
| 526.57 | 4.15 | 4.15 |
| 380.40 | 1.02 | 1.02 |
| 394.43 | 1.41 | 1.41 |
| 526.59 | 4.62 | 4.62 |
| 506.52 | 4.02 | 4.02 |
| 523.55 | 3.42 | 3.42 |
| 526.57 | 4.15 | 4.15 |
| 526.57 | 4.15 | 4.15 |
| 548.60 | 4.20 | 4.20 |
| 457.49 | 2.95 | 2.95 |
| 444.45 | 2.42 | 2.42 |
| 571.63 | 4.41 | 4.41 |
| 567.63 | 4.20 | 4.20 |
| 511.46 | 4.04 | 4.04 |
| 511.46 | 4.04 | 4.04 |
| 525.48 | 4.43 | 4.43 |
| 525.48 | 4.43 | 4.43 |
| 525.48 | 4.43 | 4.43 |
| 588.54 | 5.10 | 5.10 |
| 588.54 | 5.10 | 5.10 |
| 588.54 | 5.10 | 5.10 |
| 435.48 | 3.16 | 3.16 |
| 449.51 | 3.55 | 3.55 |
| 485.46 | 2.56 | 2.56 |
| 521.53 | 3.48 | 3.48 |
| 521.53 | 3.48 | 3.48 |