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Assay Detail

CHEMBL862013

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

Binding
Binding affinity to Wistar rat benzodiazepine receptor
39
Total Activities
39
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

GABA-A receptor; anion channel (CHEMBL1907607)
Type PROTEIN COMPLEX GROUP
Organism Rattus norvegicus

Publication

Synthesis, pharmacology, and structure-activity relationships of novel imidazolones and pyrrolones as modulators of GABAA receptors.
Grunwald C, Rundfeldt C, Lankau HJ, Arnold T, Höfgen N, Dost R, Egerland U, Hofmann HJ, Unverferth K.
J Med Chem (2006) 49 : 1855 -1866
PubMed 16539371 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 39 5.94 8.62

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL20042 CGS-9896 1 8.62
CHEMBL12 DIAZEPAM 4.0 1 8.17
CHEMBL204205 1 7.17
CHEMBL203572 1 7.05
CHEMBL204755 1 6.85
CHEMBL381174 1 6.46
CHEMBL203651 1 6.36
CHEMBL380524 1 6.31
CHEMBL204027 1 6.03
CHEMBL204040 1 5.98
CHEMBL203853 1 5.95
CHEMBL383127 1 5.69
CHEMBL203217 1 5.51
CHEMBL204553 1 5.49
CHEMBL203902 1 5.48
CHEMBL205164 1 5.48
CHEMBL204091 1 5.37
CHEMBL381915 1 5.36
CHEMBL204240 IMEPITOIN -1.0 1 5.36
CHEMBL203833 1 5.35
CHEMBL206705 1 5.35
CHEMBL413575 1 5.27
CHEMBL382485 1 5.20
CHEMBL204131 1 5.05
CHEMBL204081 1 4.94
CHEMBL206037 1 4.58
CHEMBL19732 CGS-8216 1 -
CHEMBL204581 1 -
CHEMBL3144798 1 -
CHEMBL412630 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL20042 CGS-9896 Ki = 2.4 nM 8.62
CHEMBL12 DIAZEPAM Ki = 6.8 nM 8.17
CHEMBL204205 Ki = 67.0 nM 7.17
CHEMBL203572 Ki = 90.0 nM 7.05
CHEMBL204755 Ki = 141.0 nM 6.85
CHEMBL381174 Ki = 344.0 nM 6.46
CHEMBL203651 Ki = 440.0 nM 6.36
CHEMBL380524 Ki = 494.0 nM 6.31
CHEMBL204027 Ki = 938.0 nM 6.03
CHEMBL204040 Ki = 1040.0 nM 5.98
CHEMBL203853 Ki = 1120.0 nM 5.95
CHEMBL383127 Ki = 2050.0 nM 5.69
CHEMBL203217 Ki = 3060.0 nM 5.51
CHEMBL204553 Ki = 3260.0 nM 5.49
CHEMBL205164 Ki = 3320.0 nM 5.48
CHEMBL203902 Ki = 3290.0 nM 5.48
CHEMBL204091 Ki = 4290.0 nM 5.37
CHEMBL381915 Ki = 4340.0 nM 5.36
CHEMBL204240 IMEPITOIN Ki = 4350.0 nM 5.36
CHEMBL203833 Ki = 4450.0 nM 5.35
CHEMBL206705 Ki = 4480.0 nM 5.35
CHEMBL413575 Ki = 5410.0 nM 5.27
CHEMBL382485 Ki = 6280.0 nM 5.20
CHEMBL204131 Ki = 8880.0 nM 5.05
CHEMBL204081 Ki = 11600.0 nM 4.94
CHEMBL206037 Ki = 26100.0 nM 4.58
CHEMBL206448 Ki - -
CHEMBL383680 Ki - -
CHEMBL206338 Ki - -
CHEMBL383066 Ki - -
CHEMBL382483 Ki - -
CHEMBL440575 Ki - -
CHEMBL381072 Ki - -
CHEMBL203968 Ki - -
CHEMBL203708 Ki - -
CHEMBL412630 Ki - -
CHEMBL3144798 Ki - -
CHEMBL204581 Ki - -
CHEMBL19732 CGS-8216 Ki - -