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Assay Detail

CHEMBL5032572

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

Binding
Negative allosteric modulation activity at human GABAA alpha2beta3gamma2 stably expressed in HEK cells by whole cell patch clamp method
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK
Confidence 7 — Homologous single protein target
Curated By Autocuration

Target

GABA-A receptor; alpha-2/beta-3/gamma-2 (CHEMBL2094130)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

Neuroactive Type-A γ-Aminobutyric Acid Receptor Allosteric Modulator Steroids from the Hypobranchial Gland of Marine Mollusk, <i>Conus geographus</i>.
Niu C, Leavitt LS, Lin Z, Paguigan ND, Sun L, Zhang J, Torres JP, Raghuraman S, Chase K, Cadeddu R, Karthikeyan M, Bortolato M, Reilly CA, Hughen RW, Light AR, Olivera BM, Schmidt EW.
J Med Chem (2021) 64 : 7033 -7043
PubMed 33949869 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 4.80 4.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5086854 1 4.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5086854 IC50 = 15700.0 nM 4.80