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Assay Detail

CHEMBL829158

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

Binding
Inhibitory concentration of central benzodiazepine GABA-A receptor of rat cerebral cortex
38
Total Activities
38
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

Structure-activity relationships and effects on neuroactive steroid synthesis in a series of 2-phenylimidazo[1,2-a]pyridineacetamide peripheral benzodiazepine receptors ligands.
Trapani G, Laquintana V, Denora N, Trapani A, Lopedota A, Latrofa A, Franco M, Serra M, Pisu MG, Floris I, Sanna E, Biggio G, Liso G.
J Med Chem (2005) 48 : 292 -305
PubMed 15634024 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 38 5.20 7.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL179432 1 7.05
CHEMBL340752 1 7.04
CHEMBL179711 1 6.72
CHEMBL359593 1 6.13
CHEMBL179476 1 5.48
CHEMBL180377 1 5.00
CHEMBL360798 1 5.00
CHEMBL2096767 1 5.00
CHEMBL180225 1 5.00
CHEMBL179427 1 5.00
CHEMBL427317 1 5.00
CHEMBL176047 1 5.00
CHEMBL179459 1 5.00
CHEMBL362632 1 5.00
CHEMBL361857 1 5.00
CHEMBL362200 1 5.00
CHEMBL178778 1 5.00
CHEMBL361968 1 5.00
CHEMBL179568 1 5.00
CHEMBL363217 1 5.00
CHEMBL178518 1 5.00
CHEMBL362596 1 5.00
CHEMBL178676 1 5.00
CHEMBL369327 1 5.00
CHEMBL179748 1 5.00
CHEMBL362037 1 5.00
CHEMBL369753 1 5.00
CHEMBL179675 1 5.00
CHEMBL368040 1 5.00
CHEMBL179565 1 5.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL179432 IC50 = 88.92 nM 7.05
CHEMBL340752 IC50 = 91.2 nM 7.04
CHEMBL179711 IC50 = 188.36 nM 6.72
CHEMBL359593 IC50 = 736.21 nM 6.13
CHEMBL179476 IC50 = 3303.7 nM 5.48
CHEMBL427317 IC50 = 10000.0 nM 5.00
CHEMBL179567 IC50 = 10000.0 nM 5.00
CHEMBL176047 IC50 = 10000.0 nM 5.00
CHEMBL179459 IC50 = 10000.0 nM 5.00
CHEMBL362632 IC50 = 10000.0 nM 5.00
CHEMBL361857 IC50 = 10000.0 nM 5.00
CHEMBL362200 IC50 = 10000.0 nM 5.00
CHEMBL178778 IC50 = 10000.0 nM 5.00
CHEMBL360798 IC50 = 10000.0 nM 5.00
CHEMBL435489 IC50 = 10000.0 nM 5.00
CHEMBL180210 IC50 = 10000.0 nM 5.00
CHEMBL180279 IC50 = 10000.0 nM 5.00
CHEMBL178705 IC50 = 10000.0 nM 5.00
CHEMBL180523 IC50 = 10000.0 nM 5.00
CHEMBL359841 IC50 = 10000.0 nM 5.00
CHEMBL430139 IC50 = 10000.0 nM 5.00
CHEMBL362596 IC50 = 10000.0 nM 5.00
CHEMBL179565 IC50 = 10000.0 nM 5.00
CHEMBL368040 IC50 = 10000.0 nM 5.00
CHEMBL179675 IC50 = 10000.0 nM 5.00
CHEMBL369753 IC50 = 10000.0 nM 5.00
CHEMBL362037 IC50 = 10000.0 nM 5.00
CHEMBL179748 IC50 = 10000.0 nM 5.00
CHEMBL369327 IC50 = 10000.0 nM 5.00
CHEMBL178676 IC50 = 10000.0 nM 5.00
CHEMBL179427 IC50 = 10000.0 nM 5.00
CHEMBL178518 IC50 = 10000.0 nM 5.00
CHEMBL363217 IC50 = 10000.0 nM 5.00
CHEMBL179568 IC50 = 10000.0 nM 5.00
CHEMBL361968 IC50 = 10000.0 nM 5.00
CHEMBL180377 IC50 = 10000.0 nM 5.00
CHEMBL2096767 IC50 = 10000.0 nM 5.00
CHEMBL180225 IC50 = 10000.0 nM 5.00