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Assay Detail

CHEMBL740137

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

Functional
Electrophysiology using Whole-cell patch-clamp recordings in mouse embryos
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Mus musculus
Confidence 1 — Organism
Curated By Expert

Target

Mus musculus (CHEMBL375)
Type ORGANISM
Organism Mus musculus

Publication

Novel class of potent 4-arylalkyl substituted 3-isoxazolol GABA(A) antagonists: synthesis, pharmacology, and molecular modeling.
Frølund B, Jørgensen AT, Tagmose L, Stensbøl TB, Vestergaard HT, Engblom C, Kristiansen U, Sanchez C, Krogsgaard-Larsen P, Liljefors T.
J Med Chem (2002) 45 : 2454 -2468
PubMed 12036354 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 22 6.01 7.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL544544 1 7.70
CHEMBL545008 1 7.30
CHEMBL303580 GABAZINE BROMIDE 1 6.62
CHEMBL538260 1 6.43
CHEMBL555167 1 6.36
CHEMBL544302 1 6.32
CHEMBL540042 1 6.28
CHEMBL544301 1 6.15
CHEMBL555181 1 6.11
CHEMBL553552 1 6.09
CHEMBL544776 1 6.05
CHEMBL552688 1 5.96
CHEMBL543603 1 5.96
CHEMBL543125 1 5.89
CHEMBL545238 1 5.82
CHEMBL541065 1 5.52
CHEMBL542896 1 5.40
CHEMBL541566 1 5.39
CHEMBL542665 1 5.34
CHEMBL543365 1 4.99
CHEMBL553129 1 4.58
CHEMBL311761 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL544544 IC50 = 20.0 nM 7.70
CHEMBL545008 IC50 = 50.0 nM 7.30
CHEMBL303580 GABAZINE BROMIDE IC50 = 240.0 nM 6.62
CHEMBL538260 IC50 = 370.0 nM 6.43
CHEMBL555167 IC50 = 440.0 nM 6.36
CHEMBL544302 IC50 = 480.0 nM 6.32
CHEMBL540042 IC50 = 530.0 nM 6.28
CHEMBL544301 IC50 = 710.0 nM 6.15
CHEMBL555181 IC50 = 780.0 nM 6.11
CHEMBL553552 IC50 = 810.0 nM 6.09
CHEMBL544776 IC50 = 890.0 nM 6.05
CHEMBL552688 IC50 = 1100.0 nM 5.96
CHEMBL543603 IC50 = 1100.0 nM 5.96
CHEMBL543125 IC50 = 1300.0 nM 5.89
CHEMBL545238 IC50 = 1500.0 nM 5.82
CHEMBL541065 IC50 = 3000.0 nM 5.52
CHEMBL542896 IC50 = 4000.0 nM 5.40
CHEMBL541566 IC50 = 4100.0 nM 5.39
CHEMBL542665 IC50 = 4600.0 nM 5.34
CHEMBL543365 IC50 = 10300.0 nM 4.99
CHEMBL553129 IC50 = 26000.0 nM 4.58
CHEMBL311761 IC50 = 110000.0 nM -