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Assay Detail

CHEMBL652372

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

Binding
Inhibition of radiolabeled antagonist [3H]-Ro- 15-1788 binding to benzodiazepine receptor from rat cortical membranes
81
Total Activities
81
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Subcellular Membrane
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

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

Publication

Novel benzodiazepine receptor partial agonists: oxadiazolylimidazobenzodiazepines.
Watjen F, Baker R, Engelstoff M, Herbert R, MacLeod A, Knight A, Merchant K, Moseley J, Saunders J, Swain CJ.
J Med Chem (1989) 32 : 2282 -2291
PubMed 2552115 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 81 7.74 9.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL444045 1 9.22
CHEMBL74452 1 8.89
CHEMBL306048 1 8.85
CHEMBL306342 1 8.62
CHEMBL308265 1 8.55
CHEMBL308781 1 8.47
CHEMBL307957 1 8.47
CHEMBL307202 1 8.44
CHEMBL74801 1 8.42
CHEMBL407 FLUMAZENIL 4.0 1 8.42
CHEMBL75104 1 8.41
CHEMBL72321 1 8.39
CHEMBL54338 1 8.38
CHEMBL73085 1 8.28
CHEMBL76465 1 8.28
CHEMBL421120 1 8.22
CHEMBL307836 1 8.21
CHEMBL308035 1 8.19
CHEMBL305704 1 8.17
CHEMBL74162 1 8.16
CHEMBL308359 1 8.15
CHEMBL75463 1 8.14
CHEMBL73457 1 8.12
CHEMBL73795 1 8.09
CHEMBL307819 1 8.09
CHEMBL307005 1 8.08
CHEMBL306088 1 8.03
CHEMBL74092 1 8.01
CHEMBL74357 1 8.01
CHEMBL309091 1 7.96

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL444045 IC50 = 0.6 nM 9.22
CHEMBL74452 IC50 = 1.3 nM 8.89
CHEMBL306048 IC50 = 1.4 nM 8.85
CHEMBL306342 IC50 = 2.4 nM 8.62
CHEMBL308265 IC50 = 2.8 nM 8.55
CHEMBL308781 IC50 = 3.4 nM 8.47
CHEMBL307957 IC50 = 3.4 nM 8.47
CHEMBL307202 IC50 = 3.6 nM 8.44
CHEMBL74801 IC50 = 3.8 nM 8.42
CHEMBL407 FLUMAZENIL IC50 = 3.8 nM 8.42
CHEMBL75104 IC50 = 3.9 nM 8.41
CHEMBL72321 IC50 = 4.1 nM 8.39
CHEMBL54338 IC50 = 4.2 nM 8.38
CHEMBL76465 IC50 = 5.3 nM 8.28
CHEMBL73085 IC50 = 5.2 nM 8.28
CHEMBL421120 IC50 = 6.0 nM 8.22
CHEMBL307836 IC50 = 6.1 nM 8.21
CHEMBL308035 IC50 = 6.4 nM 8.19
CHEMBL305704 IC50 = 6.7 nM 8.17
CHEMBL74162 IC50 = 6.9 nM 8.16
CHEMBL308359 IC50 = 7.0 nM 8.15
CHEMBL75463 IC50 = 7.2 nM 8.14
CHEMBL73457 IC50 = 7.5 nM 8.12
CHEMBL73795 IC50 = 8.1 nM 8.09
CHEMBL307819 IC50 = 8.2 nM 8.09
CHEMBL307005 IC50 = 8.3 nM 8.08
CHEMBL306088 IC50 = 9.4 nM 8.03
CHEMBL74092 IC50 = 9.8 nM 8.01
CHEMBL74357 IC50 = 9.7 nM 8.01
CHEMBL309091 IC50 = 11.0 nM 7.96
CHEMBL306816 IC50 = 12.0 nM 7.92
CHEMBL74776 IC50 = 12.0 nM 7.92
CHEMBL73292 IC50 = 13.0 nM 7.89
CHEMBL73655 IC50 = 14.0 nM 7.85
CHEMBL74427 IC50 = 14.0 nM 7.85
CHEMBL76167 IC50 = 14.0 nM 7.85
CHEMBL444051 IC50 = 15.0 nM 7.82
CHEMBL75521 IC50 = 16.0 nM 7.80
CHEMBL305830 IC50 = 18.0 nM 7.75
CHEMBL309070 IC50 = 19.0 nM 7.72
CHEMBL308836 IC50 = 19.0 nM 7.72
CHEMBL73624 IC50 = 20.0 nM 7.70
CHEMBL306531 IC50 = 21.0 nM 7.68
CHEMBL307190 IC50 = 22.0 nM 7.66
CHEMBL75216 IC50 = 22.0 nM 7.66
CHEMBL309090 IC50 = 24.0 nM 7.62
CHEMBL310708 IC50 = 25.0 nM 7.60
CHEMBL75315 IC50 = 27.0 nM 7.57
CHEMBL73443 IC50 = 27.0 nM 7.57
CHEMBL74509 IC50 = 27.0 nM 7.57