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Assay Detail

CHEMBL4139380

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

Binding
Positive allosteric modulation of human GABAA receptor alpha1beta2gamma2L expressed in Xenopus laevis oocytes assessed as potentiation of GABA-induced current by measuring GABA EC50 at 2.5 uM incubated for 15 to 25 secs by two-electrode voltage clamp assay (Rvb = 4.5 uM)
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 7 — Homologous single protein target
Curated By Intermediate

Target

GABA-A receptor; alpha-1/beta-2/gamma-2 (CHEMBL2095172)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

Synthesis and pharmacological evaluation of neurosteroid photoaffinity ligands.
Savechenkov PY, Chiara DC, Desai R, Stern AT, Zhou X, Ziemba AM, Szabo AL, Zhang Y, Cohen JB, Forman SA, Miller KW, Bruzik KS.
Eur J Med Chem (2017) 136 : 334 -347
PubMed 28505538 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 1 6.30 6.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL190279 ALFAXALONE 2.0 1 6.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL190279 ALFAXALONE EC50 = 500.0 nM 6.30