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Assay Detail

CHEMBL992760

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

Binding
Displacement of [3H]flumazenil from human recombinant GABAA alpha-2-beta-2-gamma-2S receptor expressed in HEK293 cells
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Affinity of 3-acyl substituted 4-quinolones at the benzodiazepine site of GABA(A) receptors.
Lager E, Nilsson J, Østergaard Nielsen E, Nielsen M, Liljefors T, Sterner O.
Bioorg Med Chem (2008) 16 : 6936 -6948
PubMed 18541432 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 16 8.45 9.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL469477 1 9.40
CHEMBL488283 1 9.09
CHEMBL471551 1 8.80
CHEMBL488284 1 8.77
CHEMBL487685 1 8.57
CHEMBL488285 1 7.80
CHEMBL488286 1 7.66
CHEMBL506314 1 7.51
CHEMBL470283 1 -
CHEMBL381059 1 -
CHEMBL206540 1 -
CHEMBL487867 1 -
CHEMBL487688 1 -
CHEMBL487687 1 -
CHEMBL487686 1 -
CHEMBL520411 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL469477 Ki = 0.4 nM 9.40
CHEMBL488283 Ki = 0.81 nM 9.09
CHEMBL471551 Ki = 1.6 nM 8.80
CHEMBL488284 Ki = 1.7 nM 8.77
CHEMBL487685 Ki = 2.7 nM 8.57
CHEMBL488285 Ki = 16.0 nM 7.80
CHEMBL488286 Ki = 22.0 nM 7.66
CHEMBL506314 Ki = 31.0 nM 7.51
CHEMBL470283 Ki - -
CHEMBL381059 Ki - -
CHEMBL206540 Ki - -
CHEMBL487867 Ki - -
CHEMBL487688 Ki - -
CHEMBL487687 Ki - -
CHEMBL487686 Ki - -
CHEMBL520411 Ki - -