메뉴 건너뛰기




Volumn 21, Issue 9, 2011, Pages 2646-2649

High concentration electrophysiology-based fragment screen: Discovery of novel acid-sensing ion channel 3 (ASIC3) inhibitors

Author keywords

Acid sensing ion channel 3; Electrophysiology; Fragment screening

Indexed keywords

ACID SENSING ION CHANNEL; ACID SENSING ION CHANNEL 3; TETRAHYDROISOQUINOLINE DERIVATIVE; UNCLASSIFIED DRUG;

EID: 79955467065     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2010.12.115     Document Type: Conference Paper
Times cited : (16)

References (16)
  • 7
    • 79955463077 scopus 로고    scopus 로고
    • This proprietary fragment library complies with typical fragment criteria: average MW 211, A log P 1.4, PSA 40. See Refs. 1 and 8. Importantly, measured aqueous solubilities of the fragments in the library were generally >0.8 mM enabling high concentration screening
    • This proprietary fragment library complies with typical fragment criteria: average MW 211, A log P 1.4, PSA 40. See Refs. 1 and 8. Importantly, measured aqueous solubilities of the fragments in the library were generally >0.8 mM enabling high concentration screening.
  • 11
    • 79955472448 scopus 로고    scopus 로고
    • note
    • 50 values were determined by fitting 5-pt titration data to the Hill equation. Up to 2% DMSO could be applied as vehicle with no effect on current magnitude or kinetics. Control compounds (e.g., amiloride) demonstrated similar potency on the PX instrument as we obtained by manual patch clamp electrophysiology.
  • 13
    • 79955469975 scopus 로고    scopus 로고
    • At this point, hits containing the known ASIC3 potency-conferring amidine substructure were removed due to concerns over poor physical properties. See Refs. 3-6
    • At this point, hits containing the known ASIC3 potency-conferring amidine substructure were removed due to concerns over poor physical properties. See Refs. 3-6 .
  • 15
    • 79955468407 scopus 로고    scopus 로고
    • Substitution and modification of the 4-amino group was not planned due to SAR findings from a related series. See the comparison below for an example
    • Substitution and modification of the 4-amino group was not planned due to SAR findings from a related series. See the comparison below for an example.


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.