Assay Detail

CHEMBL2150179

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

Binding

Allosteric modulation of gamma-aminobutyric acid receptor A alpha1beta2gamma2S expressed in Xenopus oocytes assessed as potentiation of GABA-mediated chloride current by voltage clamp analysis

ChEMBL ↗

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Target

Unchecked (CHEMBL612545) ↗

Open DB target context

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Unchecked (CHEMBL612545) is the working anchor for this assay review. Loading the live Open DB target snapshot…

Primary target Unchecked

CHEMBL612545

Anchored from Assay target.

Protein identity Unchecked

Disease frame Disease evidence pending

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Review focus Open DB context pending

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Total Activities

Compounds Tested

Activity Types

Assay Parameters

Assay Information

Assay Type	Binding
Cell Type	Oocyte
Confidence	0 — Uncurated / Unknown
Curated By	Autocuration

Target

Unchecked (CHEMBL612545) ↗

Type

UNCHECKED

Publication

Identification and characterization of GABA(A) receptor modulatory diterpenes from Biota orientalis that decrease locomotor activity in mice.

Zaugg J, Khom S, Eigenmann D, Baburin I, Hamburger M, Hering S.
J Nat Prod (2011) 74 : 1764 -1772
PubMed 21793559 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
EC50	5	6.43	7.66
Activity	2	-	-

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL646	TRIAZOLAM	4.0	1	7.66
CHEMBL655	MIDAZOLAM	4.0	1	6.84
CHEMBL1697737	CLOTIAZEPAM	2.0	1	6.74
CHEMBL513197	SANDARACOPIMARIC ACID	—	2	4.48
CHEMBL512164	ISOPIMARIC ACID	—	2	-

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL646	TRIAZOLAM	EC50	=	22.0	nM	7.66
CHEMBL655	MIDAZOLAM	EC50	=	143.0	nM	6.84
CHEMBL1697737	CLOTIAZEPAM	EC50	=	184.0	nM	6.74
CHEMBL513197	SANDARACOPIMARIC ACID	EC50	=	33300.0	nM	4.48
CHEMBL512164	ISOPIMARIC ACID	EC50	=	141600.0	nM	-
CHEMBL512164	ISOPIMARIC ACID	Activity		-	—	-
CHEMBL513197	SANDARACOPIMARIC ACID	Activity		-	—	-