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Assay Detail

CHEMBL685962

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

Binding
In vitro inhibitory against Gamma-aminobutyric acid A receptor from rat cerebral cortex using [3H]flunitrazepam as the radioligand
34
Total Activities
34
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Potential anxiolytic agents. 3. Novel A-ring modified pyrido[1,2-a]benzimidazoles.
Maryanoff BE, Nortey SO, McNally JJ, Sanfilippo PJ, McComsey DF, Dubinsky B, Shank RP, Reitz AB.
Bioorg Med Chem Lett (1999) 9 : 1547 -1552
PubMed 10386933 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 34 7.66 8.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL290683 1 8.96
CHEMBL39653 1 8.96
CHEMBL418240 1 8.85
CHEMBL289181 1 8.72
CHEMBL284301 1 8.46
CHEMBL12 DIAZEPAM 4.0 1 8.31
CHEMBL39147 1 8.29
CHEMBL290520 1 8.21
CHEMBL39831 1 8.20
CHEMBL39196 1 8.20
CHEMBL289414 1 8.15
CHEMBL287783 1 8.11
CHEMBL289107 1 8.08
CHEMBL290196 1 8.00
CHEMBL290298 1 7.98
CHEMBL38740 1 7.85
CHEMBL288962 1 7.77
CHEMBL38684 1 7.75
CHEMBL416061 1 7.70
CHEMBL284856 1 7.52
CHEMBL291258 1 7.52
CHEMBL39428 1 7.40
CHEMBL38622 1 7.39
CHEMBL38549 1 7.18
CHEMBL434597 1 7.18
CHEMBL38490 1 7.02
CHEMBL289328 1 6.81
CHEMBL40077 1 6.81
CHEMBL445834 1 6.76
CHEMBL288203 1 6.74

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL290683 IC50 = 1.1 nM 8.96
CHEMBL39653 IC50 = 1.1 nM 8.96
CHEMBL418240 IC50 = 1.4 nM 8.85
CHEMBL289181 IC50 = 1.9 nM 8.72
CHEMBL284301 IC50 = 3.5 nM 8.46
CHEMBL12 DIAZEPAM IC50 = 4.9 nM 8.31
CHEMBL39147 IC50 = 5.1 nM 8.29
CHEMBL290520 IC50 = 6.1 nM 8.21
CHEMBL39831 IC50 = 6.3 nM 8.20
CHEMBL39196 IC50 = 6.3 nM 8.20
CHEMBL289414 IC50 = 7.1 nM 8.15
CHEMBL287783 IC50 = 7.8 nM 8.11
CHEMBL289107 IC50 = 8.3 nM 8.08
CHEMBL290196 IC50 = 10.1 nM 8.00
CHEMBL290298 IC50 = 10.4 nM 7.98
CHEMBL38740 IC50 = 14.0 nM 7.85
CHEMBL288962 IC50 = 17.0 nM 7.77
CHEMBL38684 IC50 = 17.7 nM 7.75
CHEMBL416061 IC50 = 19.8 nM 7.70
CHEMBL284856 IC50 = 30.1 nM 7.52
CHEMBL291258 IC50 = 30.1 nM 7.52
CHEMBL39428 IC50 = 39.5 nM 7.40
CHEMBL38622 IC50 = 40.5 nM 7.39
CHEMBL38549 IC50 = 66.2 nM 7.18
CHEMBL434597 IC50 = 65.6 nM 7.18
CHEMBL38490 IC50 = 96.3 nM 7.02
CHEMBL289328 IC50 = 156.0 nM 6.81
CHEMBL40077 IC50 = 154.0 nM 6.81
CHEMBL445834 IC50 = 174.0 nM 6.76
CHEMBL288203 IC50 = 184.0 nM 6.74
CHEMBL288378 IC50 = 291.0 nM 6.54
CHEMBL290687 IC50 = 857.0 nM 6.07
CHEMBL289707 IC50 = 4380.0 nM 5.36
CHEMBL290259 IC50 > 1000.0 nM -