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Assay Detail

CHEMBL1679581

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

Functional
Antagonist activity at human recombinant GABAc rho-2 receptor expressed in Xenopus laevis oocytes assessed as inhibition of GABA-induced current by two electrode voltage clamp technique
4
Total Activities
3
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type Oocyte
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Gamma-aminobutyric acid receptor subunit rho-2 (CHEMBL2375)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Novel Cyclic Phosphinic Acids as GABAC ρ Receptor Antagonists: Design, Synthesis, and Pharmacology.
Gavande N, Yamamoto I, Salam NK, Ai TH, Burden PM, Johnston GA, Hanrahan JR, Chebib M.
ACS Med Chem Lett (2011) 2 : 11 -16
PubMed 24900248 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 4.40 4.66
Kb 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL397209 2 4.66
CHEMBL1672301 1 4.29
CHEMBL1672299 1 4.24

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL397209 IC50 = 22090.0 nM 4.66
CHEMBL1672301 IC50 = 51310.0 nM 4.29
CHEMBL1672299 IC50 = 57130.0 nM 4.24
CHEMBL397209 Kb = 14900.0 nM -