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Assay Detail

CHEMBL828968

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

Binding
Displacement of [3H]flunitrazepam from central benzodiazepine GABA-A receptor of rat cerebral cortex
37
Total Activities
37
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
Ki 37 5.29 7.16

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL179432 1 7.16
CHEMBL179711 1 6.89
CHEMBL359593 1 6.30
CHEMBL179476 1 5.59
CHEMBL180279 1 5.16
CHEMBL180377 1 5.16
CHEMBL361968 1 5.16
CHEMBL179459 1 5.16
CHEMBL180210 1 5.16
CHEMBL178705 1 5.16
CHEMBL359841 1 5.16
CHEMBL2096767 1 5.16
CHEMBL368040 1 5.16
CHEMBL179675 1 5.16
CHEMBL179748 1 5.16
CHEMBL179565 1 5.16
CHEMBL178518 1 5.16
CHEMBL369327 1 5.16
CHEMBL430139 1 5.16
CHEMBL180225 1 5.15
CHEMBL369753 1 5.15
CHEMBL362596 1 5.15
CHEMBL361857 1 5.15
CHEMBL362200 1 5.15
CHEMBL178778 1 5.15
CHEMBL435489 1 5.15
CHEMBL363217 1 5.12
CHEMBL179568 1 5.12
CHEMBL362037 1 5.12
CHEMBL362632 1 5.12

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL179432 Ki = 68.9 nM 7.16
CHEMBL179711 Ki = 130.0 nM 6.89
CHEMBL359593 Ki = 506.0 nM 6.30
CHEMBL179476 Ki = 2560.0 nM 5.59
CHEMBL180377 Ki = 6880.0 nM 5.16
CHEMBL361968 Ki = 6880.0 nM 5.16
CHEMBL179459 Ki = 6880.0 nM 5.16
CHEMBL180279 Ki = 6880.0 nM 5.16
CHEMBL180210 Ki = 6880.0 nM 5.16
CHEMBL178705 Ki = 6880.0 nM 5.16
CHEMBL359841 Ki = 6880.0 nM 5.16
CHEMBL2096767 Ki = 6880.0 nM 5.16
CHEMBL368040 Ki = 6880.0 nM 5.16
CHEMBL179675 Ki = 6880.0 nM 5.16
CHEMBL179748 Ki = 6880.0 nM 5.16
CHEMBL179565 Ki = 6880.0 nM 5.16
CHEMBL178518 Ki = 6880.0 nM 5.16
CHEMBL369327 Ki = 6880.0 nM 5.16
CHEMBL430139 Ki = 6880.0 nM 5.16
CHEMBL362596 Ki = 7010.0 nM 5.15
CHEMBL369753 Ki = 7010.0 nM 5.15
CHEMBL361857 Ki = 7010.0 nM 5.15
CHEMBL362200 Ki = 7010.0 nM 5.15
CHEMBL178778 Ki = 7010.0 nM 5.15
CHEMBL180225 Ki = 7010.0 nM 5.15
CHEMBL435489 Ki = 7010.0 nM 5.15
CHEMBL363217 Ki = 7590.0 nM 5.12
CHEMBL179568 Ki = 7590.0 nM 5.12
CHEMBL362037 Ki = 7590.0 nM 5.12
CHEMBL362632 Ki = 7590.0 nM 5.12
CHEMBL360798 Ki = 7590.0 nM 5.12
CHEMBL179567 Ki = 7750.0 nM 5.11
CHEMBL178676 Ki = 7750.0 nM 5.11
CHEMBL180523 Ki = 7750.0 nM 5.11
CHEMBL176047 Ki = 7750.0 nM 5.11
CHEMBL427317 Ki = 7750.0 nM 5.11
CHEMBL179427 Ki = 7750.0 nM 5.11