Basic Information
ID: ALA3888209
Type: Binding
Description: TASK-1 Inhibiition Assay: Human TASK-1 channels were expressed in Xenopus oocytes. For this purpose, oocytes were isolated from Xenopus laevis and defoliculated. Subsequently, TASK-1-encoding RNA synthesized in vitro was injected into the oocytes. After two days of TASK-1 protein expression, TASK-1 currents were measured by two-microelectrode voltage clamp. Data were acquired and analyzed using a TEC-10cx amplifier (NPI Electronic, Tamm, Germany) connected to an ITC-16 interface (Instrutech Corp., Long Island, USA) and Pulse software (HEKA Elektronik, Lambrecht, Germany). Oocytes were clamped to -90 mV and TASK-1 mediated currents were measured during 500 ms voltage pulses to 40 mV. Oocytes were continuously superfused with ND96 buffer containing 96 mM sodium chloride, 2 mM potassium chloride, 1.8 mM calcium chloride, 1 mM magnesium chloride, 5 mM 4-(2-hydroxyethyl)-piperazine-1-ethanesulfonic acid (HEPES; pH adjusted to 7.4 with sodium hydroxide). All experiments were performed at room temperature.
Activity Charts
Bioactivity
Activity Types for Assay ALA3888209
IC50
Compound Summary
| Parent Molecular Weight | ALogP | Polar Surface Area |
|---|---|---|
| 464.49 | 3.94 | 3.94 |
| 459.54 | 4.64 | 4.64 |
| 456.49 | 3.67 | 3.67 |
| 425.53 | 3.15 | 3.15 |
| 426.52 | 2.93 | 2.93 |
| 469.53 | 4.60 | 4.60 |
| 429.95 | 4.18 | 4.18 |
| 478.52 | 4.25 | 4.25 |
| 397.49 | 3.89 | 3.89 |
| 419.88 | 3.37 | 3.37 |
| 420.51 | 3.40 | 3.40 |
| 451.50 | 3.32 | 3.32 |
| 395.50 | 3.52 | 3.52 |
| 506.57 | 4.00 | 4.00 |
| 449.53 | 4.53 | 4.53 |
| 497.95 | 5.20 | 5.20 |
| 465.38 | 4.23 | 4.23 |
| 455.95 | 3.44 | 3.44 |
| 395.50 | 3.52 | 3.52 |
| 425.53 | 3.53 | 3.53 |
| 447.54 | 3.57 | 3.57 |
| 411.57 | 4.24 | 4.24 |
| 482.48 | 4.08 | 4.08 |
| 435.53 | 3.04 | 3.04 |
| 454.96 | 4.05 | 4.05 |
| 438.50 | 3.53 | 3.53 |
| 429.95 | 4.18 | 4.18 |
| 481.49 | 4.68 | 4.68 |
| 427.52 | 3.91 | 3.91 |
| 430.94 | 3.57 | 3.57 |
| 470.52 | 4.00 | 4.00 |
| 463.50 | 4.54 | 4.54 |
| 478.52 | 4.33 | 4.33 |
| 426.54 | 3.46 | 3.46 |
| 481.49 | 4.68 | 4.68 |
| 463.50 | 4.54 | 4.54 |
| 497.95 | 5.20 | 5.20 |
| 482.48 | 4.08 | 4.08 |
| 455.56 | 3.31 | 3.31 |
| 411.57 | 4.24 | 4.24 |
| 463.94 | 3.55 | 3.55 |
| 495.57 | 5.14 | 5.14 |
| 498.93 | 4.59 | 4.59 |
| 429.52 | 3.77 | 3.77 |
| 462.47 | 3.47 | 3.47 |
| 464.49 | 3.94 | 3.94 |
| 418.54 | 4.20 | 4.20 |
| 447.94 | 4.32 | 4.32 |
| 441.53 | 2.97 | 2.97 |
| 498.93 | 4.59 | 4.59 |
| 492.54 | 4.72 | 4.72 |
| 491.56 | 4.33 | 4.33 |
| 494.51 | 3.95 | 3.95 |
| 453.58 | 3.79 | 3.79 |
| 411.50 | 2.76 | 2.76 |
| 477.58 | 5.17 | 5.17 |
| 419.53 | 3.60 | 3.60 |
| 381.48 | 3.04 | 3.04 |
| 461.51 | 4.13 | 4.13 |
| 447.55 | 5.34 | 5.34 |
| 396.49 | 2.92 | 2.92 |
| 431.48 | 3.80 | 3.80 |
| 494.51 | 3.95 | 3.95 |
| 487.60 | 3.65 | 3.65 |
| 532.49 | 4.96 | 4.96 |
| 426.52 | 2.93 | 2.93 |
| 499.48 | 4.82 | 4.82 |
| 421.50 | 3.47 | 3.47 |
| 460.96 | 3.58 | 3.58 |
| 447.48 | 3.74 | 3.74 |
| 478.52 | 4.18 | 4.18 |
| 464.49 | 3.94 | 3.94 |
| 543.38 | 4.70 | 4.70 |
| 419.88 | 3.37 | 3.37 |
| 465.38 | 4.23 | 4.23 |
| 481.49 | 4.68 | 4.68 |
| 438.50 | 3.53 | 3.53 |
| 413.49 | 3.66 | 3.66 |
| 430.94 | 3.57 | 3.57 |
| 479.50 | 4.42 | 4.42 |
| 427.52 | 3.91 | 3.91 |
| 447.54 | 3.57 | 3.57 |
| 411.48 | 3.27 | 3.27 |
| 447.94 | 4.32 | 4.32 |
| 462.47 | 3.47 | 3.47 |
| 429.95 | 4.18 | 4.18 |
| 478.52 | 4.25 | 4.25 |
| 451.57 | 3.54 | 3.54 |
| 454.57 | 2.88 | 2.88 |
| 435.98 | 4.24 | 4.24 |
| 445.51 | 4.46 | 4.46 |
| 463.50 | 4.54 | 4.54 |
| 435.45 | 3.68 | 3.68 |
| 421.50 | 2.79 | 2.79 |
| 420.51 | 3.40 | 3.40 |
| 454.96 | 4.05 | 4.05 |
| 397.54 | 4.20 | 4.20 |
| 413.95 | 4.59 | 4.59 |
| 441.53 | 2.92 | 2.92 |
| 465.48 | 3.33 | 3.33 |
| 478.52 | 4.33 | 4.33 |
| 462.52 | 4.74 | 4.74 |
| 421.50 | 2.79 | 2.79 |
| 464.39 | 4.83 | 4.83 |
| 464.49 | 3.94 | 3.94 |
| 461.51 | 4.21 | 4.21 |
| 532.49 | 4.96 | 4.96 |
| 447.94 | 4.32 | 4.32 |
| 480.43 | 4.35 | 4.35 |
| 397.54 | 4.10 | 4.10 |
| 393.53 | 4.23 | 4.23 |
| 465.53 | 3.57 | 3.57 |
| 411.50 | 2.76 | 2.76 |
| 439.41 | 3.43 | 3.43 |
| 448.57 | 4.17 | 4.17 |
| 430.94 | 3.57 | 3.57 |
| 409.53 | 3.91 | 3.91 |
| 456.49 | 3.67 | 3.67 |
| 531.50 | 5.56 | 5.56 |
| 498.93 | 4.59 | 4.59 |
| 464.49 | 3.94 | 3.94 |
| 431.48 | 3.80 | 3.80 |
| 459.97 | 4.19 | 4.19 |
| 443.98 | 4.42 | 4.42 |
| 497.95 | 5.20 | 5.20 |
| 401.53 | 3.59 | 3.59 |
| 399.47 | 3.08 | 3.08 |
| 409.53 | 4.08 | 4.08 |
| 402.52 | 2.98 | 2.98 |
| 411.50 | 3.23 | 3.23 |
| 403.43 | 2.85 | 2.85 |
| 443.55 | 4.32 | 4.32 |
| 467.57 | 3.46 | 3.46 |
| 486.62 | 4.03 | 4.03 |
| 423.56 | 4.16 | 4.16 |
| 395.50 | 3.38 | 3.38 |
| 446.55 | 4.18 | 4.18 |
| 519.50 | 4.34 | 4.34 |
| 381.48 | 3.04 | 3.04 |
| 462.55 | 4.17 | 4.17 |
| 452.58 | 4.24 | 4.24 |
| 409.53 | 3.91 | 3.91 |
| 519.50 | 4.34 | 4.34 |
| 413.49 | 3.52 | 3.52 |
| 483.66 | 6.02 | 6.02 |
| 505.92 | 5.82 | 5.82 |
| 447.54 | 3.57 | 3.57 |
| 432.52 | 3.27 | 3.27 |
| 476.58 | 4.18 | 4.18 |
| 517.52 | 5.55 | 5.55 |
| 481.53 | 3.33 | 3.33 |
| 455.60 | 5.68 | 5.68 |
| 489.57 | 4.48 | 4.48 |
| 445.56 | 4.78 | 4.78 |
| 449.47 | 4.15 | 4.15 |
| 484.50 | 3.51 | 3.51 |
| 455.47 | 2.90 | 2.90 |
| 447.55 | 4.82 | 4.82 |
| 459.59 | 5.21 | 5.21 |
| 453.44 | 3.82 | 3.82 |
| 480.54 | 3.93 | 3.93 |
| 421.54 | 3.91 | 3.91 |
| 451.50 | 3.32 | 3.32 |
| 424.53 | 3.29 | 3.29 |
| 467.96 | 3.83 | 3.83 |
| 518.51 | 4.94 | 4.94 |
| 383.49 | 3.29 | 3.29 |
| 422.49 | 3.38 | 3.38 |
| 475.59 | 3.96 | 3.96 |
| 469.58 | 3.17 | 3.17 |
| 399.49 | 2.40 | 2.40 |
| 447.55 | 5.12 | 5.12 |
| 381.48 | 3.14 | 3.14 |
| 393.49 | 2.99 | 2.99 |
| 458.52 | 3.97 | 3.97 |
| 420.51 | 4.56 | 4.56 |
| 436.51 | 3.43 | 3.43 |
| 481.59 | 3.85 | 3.85 |
| 490.53 | 4.23 | 4.23 |
| 408.46 | 2.82 | 2.82 |
| 393.53 | 4.23 | 4.23 |
| 442.52 | 3.70 | 3.70 |
| 453.49 | 4.28 | 4.28 |
| 437.48 | 2.93 | 2.93 |
| 453.54 | 3.07 | 3.07 |
| 524.64 | 3.43 | 3.43 |
| 489.57 | 3.93 | 3.93 |
| 408.46 | 1.95 | 1.95 |
| 421.54 | 3.82 | 3.82 |
| 471.92 | 3.41 | 3.41 |
| 447.54 | 3.57 | 3.57 |
| 421.59 | 5.02 | 5.02 |
| 471.53 | 3.06 | 3.06 |
| 443.55 | 4.32 | 4.32 |
| 477.57 | 3.58 | 3.58 |
| 399.49 | 2.66 | 2.66 |
| 471.56 | 4.73 | 4.73 |
| 438.55 | 4.23 | 4.23 |
| 459.55 | 3.67 | 3.67 |
| 436.49 | 3.36 | 3.36 |
| 538.67 | 3.64 | 3.64 |
| 423.56 | 3.86 | 3.86 |
| 441.53 | 2.92 | 2.92 |
| 515.54 | 4.59 | 4.59 |
| 425.53 | 3.15 | 3.15 |
| 451.57 | 5.20 | 5.20 |
| 427.50 | 2.53 | 2.53 |
| 449.47 | 4.07 | 4.07 |
| 459.55 | 3.50 | 3.50 |
| 413.52 | 2.65 | 2.65 |
| 411.55 | 4.06 | 4.06 |
| 451.50 | 3.32 | 3.32 |
| 422.55 | 4.09 | 4.09 |
| 473.58 | 3.26 | 3.26 |
| 465.59 | 5.25 | 5.25 |
| 433.51 | 3.18 | 3.18 |
| 451.50 | 3.00 | 3.00 |
| 453.49 | 4.28 | 4.28 |
| 415.92 | 3.69 | 3.69 |
| 467.96 | 3.83 | 3.83 |
| 452.56 | 2.64 | 2.64 |
| 407.56 | 4.77 | 4.77 |
| 439.51 | 2.68 | 2.68 |
| 471.53 | 3.21 | 3.21 |
| 395.50 | 3.52 | 3.52 |
| 433.91 | 3.93 | 3.93 |
| 477.57 | 3.58 | 3.58 |
| 455.60 | 5.59 | 5.59 |
| 458.56 | 4.27 | 4.27 |
| 413.52 | 2.65 | 2.65 |
| 518.51 | 4.94 | 4.94 |
| 425.53 | 2.88 | 2.88 |
| 429.51 | 4.58 | 4.58 |
| 485.95 | 3.97 | 3.97 |
| 397.48 | 2.37 | 2.37 |
| 408.46 | 2.82 | 2.82 |
| 406.49 | 3.62 | 3.62 |
| 476.58 | 4.18 | 4.18 |
| 369.47 | 3.04 | 3.04 |
| 436.58 | 5.03 | 5.03 |
| 395.50 | 3.52 | 3.52 |
| 433.51 | 3.18 | 3.18 |
| 475.55 | 3.62 | 3.62 |
| 395.50 | 3.43 | 3.43 |
| 379.50 | 3.85 | 3.85 |
| 415.92 | 3.79 | 3.79 |
| 395.50 | 3.18 | 3.18 |
| 464.49 | 3.94 | 3.94 |
| 523.66 | 4.18 | 4.18 |
| 406.49 | 3.03 | 3.03 |
| 475.56 | 4.92 | 4.92 |
| 453.49 | 4.28 | 4.28 |
| 409.53 | 3.91 | 3.91 |
| 479.50 | 4.04 | 4.04 |
| 476.58 | 4.18 | 4.18 |
| 442.52 | 4.38 | 4.38 |
| 451.57 | 3.27 | 3.27 |
| 518.51 | 4.94 | 4.94 |
| 451.53 | 2.40 | 2.40 |
| 462.55 | 3.88 | 3.88 |
| 471.92 | 3.41 | 3.41 |
| 465.53 | 3.57 | 3.57 |
| 397.48 | 2.15 | 2.15 |
| 435.50 | 3.74 | 3.74 |
| 419.49 | 2.62 | 2.62 |
| 476.58 | 4.48 | 4.48 |
| 437.58 | 4.55 | 4.55 |
| 411.50 | 2.50 | 2.50 |
| 411.48 | 3.27 | 3.27 |
| 489.57 | 3.54 | 3.54 |
| 451.50 | 3.32 | 3.32 |
| 433.51 | 3.18 | 3.18 |
| 447.54 | 3.57 | 3.57 |
| 469.49 | 3.46 | 3.46 |
| 461.57 | 3.61 | 3.61 |
| 423.56 | 4.16 | 4.16 |
| 495.60 | 3.23 | 3.23 |
| 460.58 | 4.48 | 4.48 |
| 437.50 | 1.91 | 1.91 |
| 449.53 | 4.53 | 4.53 |
| 465.53 | 3.57 | 3.57 |
| 477.57 | 3.58 | 3.58 |
| 514.55 | 5.19 | 5.19 |
| 461.56 | 4.49 | 4.49 |
| 451.57 | 5.11 | 5.11 |
| 463.55 | 5.09 | 5.09 |
| 419.49 | 2.62 | 2.62 |
| 419.49 | 2.62 | 2.62 |
| 477.56 | 3.85 | 3.85 |
| 538.67 | 4.15 | 4.15 |
| 453.54 | 3.07 | 3.07 |
| 397.52 | 3.42 | 3.42 |
| 409.53 | 3.57 | 3.57 |
| 436.51 | 3.43 | 3.43 |
| 422.46 | 3.69 | 3.69 |
| 439.56 | 3.40 | 3.40 |
| 514.55 | 5.19 | 5.19 |
| 455.60 | 5.34 | 5.34 |
| 464.49 | 3.84 | 3.84 |
| 480.61 | 2.84 | 2.84 |
| 423.56 | 4.16 | 4.16 |
| 439.56 | 3.54 | 3.54 |
| 445.56 | 4.78 | 4.78 |
| 433.51 | 3.18 | 3.18 |
| 476.58 | 4.18 | 4.18 |
| 447.54 | 3.57 | 3.57 |
| 485.95 | 3.97 | 3.97 |
| 449.53 | 4.53 | 4.53 |
| 367.45 | 2.79 | 2.79 |
| 477.58 | 5.48 | 5.48 |
| 475.55 | 3.62 | 3.62 |
| 415.54 | 4.64 | 4.64 |
| 423.48 | 1.35 | 1.35 |
| 443.59 | 5.59 | 5.59 |
| 437.50 | 1.91 | 1.91 |
| 545.56 | 4.60 | 4.60 |
| 393.53 | 4.33 | 4.33 |
| 439.56 | 3.27 | 3.27 |
| 485.95 | 3.97 | 3.97 |
| 514.55 | 5.19 | 5.19 |
| 422.49 | 3.76 | 3.76 |
| 476.58 | 4.18 | 4.18 |
| 449.53 | 4.53 | 4.53 |
| 417.46 | 3.41 | 3.41 |
| 422.49 | 3.76 | 3.76 |
| 432.52 | 3.57 | 3.57 |
| 397.52 | 3.68 | 3.68 |
| 394.43 | 3.14 | 3.14 |
| 433.51 | 2.96 | 2.96 |
| 425.53 | 3.15 | 3.15 |
| 443.59 | 5.59 | 5.59 |
| 408.46 | 2.82 | 2.82 |
| 495.60 | 3.23 | 3.23 |
| 518.46 | 4.48 | 4.48 |
| 425.53 | 2.74 | 2.74 |
| 514.55 | 5.19 | 5.19 |
| 495.53 | 3.94 | 3.94 |
| 385.46 | 2.28 | 2.28 |
| 433.51 | 3.18 | 3.18 |
| 451.50 | 3.32 | 3.32 |
| 459.55 | 3.67 | 3.67 |
| 454.50 | 3.76 | 3.76 |
| 447.60 | 5.36 | 5.36 |
| 437.48 | 2.93 | 2.93 |
| 435.50 | 4.14 | 4.14 |
| 407.56 | 4.63 | 4.63 |
| 407.56 | 4.72 | 4.72 |
| 463.54 | 3.19 | 3.19 |
| 451.53 | 2.09 | 2.09 |
| 463.54 | 3.19 | 3.19 |
| 476.58 | 4.18 | 4.18 |
| 451.57 | 5.11 | 5.11 |
| 467.57 | 3.46 | 3.46 |
| 451.57 | 5.20 | 5.20 |
| 424.53 | 3.29 | 3.29 |
| 510.62 | 3.04 | 3.04 |
| 383.49 | 3.38 | 3.38 |
| 422.49 | 3.38 | 3.38 |
| 488.59 | 4.28 | 4.28 |
| 413.47 | 2.19 | 2.19 |
| 429.52 | 4.06 | 4.06 |
| 474.54 | 4.40 | 4.40 |