Assay Report Card

Basic Information

ID: ALA3705435

Type: Binding

Description: Inhibition 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 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: NaCI 96 mM, KCI2 mM, CaCI21.8 mM, MgCI21 mM, HEPES 5 mM (pH adjusted to 7.4 with NaOH).

Activity Charts

Bioactivity

Activity Types for Assay ALA3705435

IC50

Total(44)

Compound Summary

Parent Molecular Weight	ALogP	Polar Surface Area
493.43	4.14	4.14
443.88	3.89	3.89
457.45	3.39	3.39
495.35	3.73	3.73
478.42	3.65	3.65
495.42	4.40	4.40
467.36	4.14	4.14
477.43	4.26	4.26
509.45	4.79	4.79
450.90	3.63	3.63
439.46	3.25	3.25
432.91	3.49	3.49
477.43	4.26	4.26
493.43	4.14	4.14
425.89	3.75	3.75
434.45	3.11	3.11
460.34	4.41	4.41
443.88	3.89	3.89
448.47	3.50	3.50
423.46	3.55	3.55
457.45	3.39	3.39
452.44	3.25	3.25
375.45	4.13	4.13
375.45	4.13	4.13
448.47	3.50	3.50
460.48	3.50	3.50
462.50	3.75	3.75
457.91	4.55	4.55
441.45	4.03	4.03
450.45	3.33	3.33
439.48	4.24	4.24
427.47	4.24	4.24
430.48	3.28	3.28
456.52	3.85	3.85
450.90	3.63	3.63
496.40	4.32	4.32
427.43	3.38	3.38
511.33	4.68	4.68
443.88	3.89	3.89
434.45	3.11	3.11
427.43	3.38	3.38
443.88	3.89	3.89
439.46	3.25	3.25
460.34	4.41	4.41