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Assay Detail

CHEMBL1816618

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

Binding
Modulation of GABA Aalpha1beta2 receptor expressed in Xenopus laevis oocytes assessed as potentiation of GABA-induced chloride current at holding potential -70 mV by two-microelectrode voltage clamp technique
32
Total Activities
32
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type Oocyte
Confidence 6 — Multiple protein complex / RNA
Curated By Autocuration

Target

GABA-A receptor; GABA-A site (alpha1/beta2 interface) (CHEMBL1907597)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

Modulation of GABAA-receptors by honokiol and derivatives: subtype selectivity and structure-activity relationship.
Taferner B, Schuehly W, Huefner A, Baburin I, Wiesner K, Ecker GF, Hering S.
J Med Chem (2011) 54 : 5349 -5361
PubMed 21699169 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 32 4.76 5.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1814294 1 5.70
CHEMBL1814312 1 5.42
CHEMBL1814310 1 5.11
CHEMBL1814290 1 5.08
CHEMBL1814307 1 5.04
CHEMBL1814308 1 5.03
CHEMBL1814306 1 4.91
CHEMBL555297 1 4.90
CHEMBL1829020 1 4.84
CHEMBL1829021 1 4.83
CHEMBL1814289 1 4.77
CHEMBL1814309 1 4.73
CHEMBL557713 1 4.71
CHEMBL1814300 1 4.66
CHEMBL231391 1 4.62
CHEMBL1814305 1 4.60
CHEMBL89700 METHYLHONOKIOL 1 4.57
CHEMBL1814291 1 4.47
CHEMBL182529 1 4.45
CHEMBL180920 MAGNOLOL 1 4.43
CHEMBL16901 HONOKIOL 1 4.41
CHEMBL89828 1 4.38
CHEMBL1814295 1 4.26
CHEMBL1829017 1 4.22
CHEMBL1829023 1 -
CHEMBL1829024 1 -
CHEMBL1814302 1 -
CHEMBL1814303 1 -
CHEMBL1814293 1 -
CHEMBL1814304 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1814294 EC50 = 2000.0 nM 5.70
CHEMBL1814312 EC50 = 3800.0 nM 5.42
CHEMBL1814310 EC50 = 7700.0 nM 5.11
CHEMBL1814290 EC50 = 8400.0 nM 5.08
CHEMBL1814307 EC50 = 9200.0 nM 5.04
CHEMBL1814308 EC50 = 9300.0 nM 5.03
CHEMBL1814306 EC50 = 12400.0 nM 4.91
CHEMBL555297 EC50 = 12700.0 nM 4.90
CHEMBL1829020 EC50 = 14300.0 nM 4.84
CHEMBL1829021 EC50 = 14800.0 nM 4.83
CHEMBL1814289 EC50 = 16900.0 nM 4.77
CHEMBL1814309 EC50 = 18500.0 nM 4.73
CHEMBL557713 EC50 = 19700.0 nM 4.71
CHEMBL1814300 EC50 = 22000.0 nM 4.66
CHEMBL231391 EC50 = 23700.0 nM 4.62
CHEMBL1814305 EC50 = 25000.0 nM 4.60
CHEMBL89700 METHYLHONOKIOL EC50 = 27200.0 nM 4.57
CHEMBL1814291 EC50 = 34200.0 nM 4.47
CHEMBL182529 EC50 = 35200.0 nM 4.45
CHEMBL180920 MAGNOLOL EC50 = 36800.0 nM 4.43
CHEMBL16901 HONOKIOL EC50 = 39300.0 nM 4.41
CHEMBL89828 EC50 = 42100.0 nM 4.38
CHEMBL1814295 EC50 = 54300.0 nM 4.26
CHEMBL1829017 EC50 = 59900.0 nM 4.22
CHEMBL1829023 EC50 - -
CHEMBL1829024 EC50 - -
CHEMBL1814302 EC50 - -
CHEMBL1814303 EC50 - -
CHEMBL1814293 EC50 = 105400.0 nM -
CHEMBL1814304 EC50 - -
CHEMBL1814311 EC50 - -
CHEMBL1814292 EC50 - -