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Assay Detail

CHEMBL992850

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

Binding
Displacement of [3H]flumazenil from GABAA receptor in rat cortical membrane
26
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
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 26 8.66 9.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL469477 1 9.77
CHEMBL488283 1 9.66
CHEMBL487687 1 9.64
CHEMBL487686 1 9.57
CHEMBL488284 1 9.38
CHEMBL487685 1 9.28
CHEMBL470285 1 9.27
CHEMBL470284 1 9.06
CHEMBL471551 1 9.05
CHEMBL471552 1 9.01
CHEMBL520411 1 9.00
CHEMBL488286 1 8.89
CHEMBL381059 1 8.85
CHEMBL487688 1 8.82
CHEMBL527430 1 8.68
CHEMBL470283 1 8.66
CHEMBL488285 1 8.60
CHEMBL488820 1 8.60
CHEMBL506314 1 8.10
CHEMBL487867 1 7.77
CHEMBL488819 1 7.75
CHEMBL447137 1 7.72
CHEMBL206540 1 7.70
CHEMBL442825 1 7.55
CHEMBL486441 1 7.52
CHEMBL470081 1 7.16

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL469477 Ki = 0.17 nM 9.77
CHEMBL488283 Ki = 0.22 nM 9.66
CHEMBL487687 Ki = 0.23 nM 9.64
CHEMBL487686 Ki = 0.27 nM 9.57
CHEMBL488284 Ki = 0.42 nM 9.38
CHEMBL487685 Ki = 0.53 nM 9.28
CHEMBL470285 Ki = 0.54 nM 9.27
CHEMBL470284 Ki = 0.87 nM 9.06
CHEMBL471551 Ki = 0.9 nM 9.05
CHEMBL471552 Ki = 0.98 nM 9.01
CHEMBL520411 Ki = 1.0 nM 9.00
CHEMBL488286 Ki = 1.3 nM 8.89
CHEMBL381059 Ki = 1.4 nM 8.85
CHEMBL487688 Ki = 1.5 nM 8.82
CHEMBL527430 Ki = 2.1 nM 8.68
CHEMBL470283 Ki = 2.2 nM 8.66
CHEMBL488285 Ki = 2.5 nM 8.60
CHEMBL488820 Ki = 2.5 nM 8.60
CHEMBL506314 Ki = 7.9 nM 8.10
CHEMBL487867 Ki = 17.1 nM 7.77
CHEMBL488819 Ki = 18.0 nM 7.75
CHEMBL447137 Ki = 19.0 nM 7.72
CHEMBL206540 Ki = 20.0 nM 7.70
CHEMBL442825 Ki = 28.0 nM 7.55
CHEMBL486441 Ki = 30.0 nM 7.52
CHEMBL470081 Ki = 69.0 nM 7.16