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Assay Detail

CHEMBL866388

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Functional
Binding affinity at human GABAA alpha-4-beta-3-delta expressed in Xenopus oocytes by voltage-clamp electrophysiology
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type Oocyte
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Potent 4-arylalkyl-substituted 3-isothiazolol GABA(A) competitive/noncompetitive antagonists: synthesis and pharmacology.
Krehan D, Storustovu SI, Liljefors T, Ebert B, Nielsen B, Krogsgaard-Larsen P, Frølund B.
J Med Chem (2006) 49 : 1388 -1396
PubMed 16480274 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 2 9.05 9.46

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL202028 1 9.46
CHEMBL377925 1 8.64

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL202028 Ki = 0.35 nM 9.46
CHEMBL377925 Ki = 2.3 nM 8.64