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Assay Detail

CHEMBL652457

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

Binding
Displacement of [3H]diazepam from rat cerebral cortex benzodiazepine receptor
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

Synthesis and structure--activity relationships of fused imidazopyridines: a new series of benzodiazepine receptor ligands.
Takada S, Sasatani T, Chomei N, Adachi M, Fujishita T, Eigyo M, Murata S, Kawasaki K, Matsushita A.
J Med Chem (1996) 39 : 2844 -2851
PubMed 8709114 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 37 8.40 9.39

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3144747 1 9.39
CHEMBL95623 1 9.30
CHEMBL99255 1 9.30
CHEMBL317342 1 9.10
CHEMBL95673 1 9.10
CHEMBL20042 CGS-9896 1 9.08
CHEMBL97442 1 9.05
CHEMBL329930 1 9.05
CHEMBL93613 1 9.05
CHEMBL95471 1 9.05
CHEMBL327886 1 9.00
CHEMBL99722 1 8.96
CHEMBL95900 1 8.96
CHEMBL316964 1 8.92
CHEMBL318722 1 8.92
CHEMBL95451 1 8.85
CHEMBL319249 1 8.77
CHEMBL319082 1 8.66
CHEMBL99516 1 8.57
CHEMBL317513 1 8.48
CHEMBL441639 1 8.47
CHEMBL321971 1 8.46
CHEMBL100148 1 8.35
CHEMBL97365 1 8.31
CHEMBL97260 1 8.28
CHEMBL99458 1 8.28
CHEMBL94698 1 8.14
CHEMBL315648 1 8.11
CHEMBL97814 1 8.02
CHEMBL98623 1 7.86

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3144747 Ki = 0.41 nM 9.39
CHEMBL95623 Ki = 0.5 nM 9.30
CHEMBL99255 Ki = 0.5 nM 9.30
CHEMBL317342 Ki = 0.8 nM 9.10
CHEMBL95673 Ki = 0.8 nM 9.10
CHEMBL20042 CGS-9896 Ki = 0.83 nM 9.08
CHEMBL97442 Ki = 0.9 nM 9.05
CHEMBL329930 Ki = 0.9 nM 9.05
CHEMBL93613 Ki = 0.9 nM 9.05
CHEMBL95471 Ki = 0.9 nM 9.05
CHEMBL327886 Ki = 1.0 nM 9.00
CHEMBL99722 Ki = 1.1 nM 8.96
CHEMBL95900 Ki = 1.1 nM 8.96
CHEMBL316964 Ki = 1.2 nM 8.92
CHEMBL318722 Ki = 1.2 nM 8.92
CHEMBL95451 Ki = 1.4 nM 8.85
CHEMBL319249 Ki = 1.7 nM 8.77
CHEMBL319082 Ki = 2.2 nM 8.66
CHEMBL99516 Ki = 2.7 nM 8.57
CHEMBL317513 Ki = 3.3 nM 8.48
CHEMBL441639 Ki = 3.4 nM 8.47
CHEMBL321971 Ki = 3.5 nM 8.46
CHEMBL100148 Ki = 4.5 nM 8.35
CHEMBL97365 Ki = 4.9 nM 8.31
CHEMBL97260 Ki = 5.2 nM 8.28
CHEMBL99458 Ki = 5.3 nM 8.28
CHEMBL94698 Ki = 7.2 nM 8.14
CHEMBL315648 Ki = 7.8 nM 8.11
CHEMBL97814 Ki = 9.5 nM 8.02
CHEMBL98623 Ki = 13.7 nM 7.86
CHEMBL440886 Ki = 14.6 nM 7.84
CHEMBL98508 Ki = 15.56 nM 7.81
CHEMBL94523 Ki = 18.8 nM 7.73
CHEMBL320603 Ki = 40.0 nM 7.40
CHEMBL97811 Ki = 302.0 nM 6.52
CHEMBL317218 Ki = 524.0 nM 6.28
CHEMBL431436 Ki = 3354.0 nM 5.47