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Assay Detail

CHEMBL3122360

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

Binding
Displacement of [3H]flumazenil from GABAA/BZD receptor in Sprague-Dawley rat cortical membrane after 35 mins by competition binding assay
ChEMBL ↗
44
Total Activities
22
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545) ↗
Type UNCHECKED

Publication

Synthesis, receptor affinity and effect on pentylenetetrazole-induced seizure threshold of novel benzodiazepine analogues: 3-Substituted 5-(2-phenoxybenzyl)-4H-1,2,4-triazoles and 2-amino-5-(phenoxybenzyl)-1,3,4-oxadiazoles.
Mashayekh S, Rahmanipour N, Mahmoodi B, Ahmadi F, Motaharian D, Shahhosseini S, Shafaroodi H, Banafshe HR, Shafiee A, Navidpour L.
Bioorg Med Chem (2014) 22 : 1929 -1937
PubMed 24530225 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 22 8.93 9.26
IC50 22 8.72 9.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3121253 — — 2 9.26
CHEMBL3121265 — — 2 9.12
CHEMBL3121251 — — 2 9.10
CHEMBL3121269 — — 2 9.09
CHEMBL3121262 — — 2 9.08
CHEMBL3121263 — — 2 9.08
CHEMBL3121268 — — 2 9.00
CHEMBL3121261 — — 2 8.96
CHEMBL3121255 — — 2 8.96
CHEMBL3121256 — — 2 8.94
CHEMBL3121254 — — 2 8.93
CHEMBL3121252 — — 2 8.92
CHEMBL3121259 — — 2 8.90
CHEMBL3121266 — — 2 8.90
CHEMBL3121258 — — 2 8.89
CHEMBL3121249 — — 2 8.87
CHEMBL3121267 — — 2 8.81
CHEMBL12 DIAZEPAM 4.0 2 8.76
CHEMBL3121260 — — 2 8.72
CHEMBL3121257 — — 2 8.67
CHEMBL3121250 — — 2 8.63
CHEMBL3121264 — — 2 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3121253 — Kd = 0.544 nM 9.26
CHEMBL3121265 — Kd = 0.75 nM 9.12
CHEMBL3121251 — Kd = 0.8 nM 9.10
CHEMBL3121269 — Kd = 0.82 nM 9.09
CHEMBL3121262 — Kd = 0.836 nM 9.08
CHEMBL3121263 — Kd = 0.84 nM 9.08
CHEMBL3121253 — IC50 = 0.892 nM 9.05
CHEMBL3121268 — Kd = 1.002 nM 9.00
CHEMBL3121261 — Kd = 1.09 nM 8.96
CHEMBL3121255 — Kd = 1.098 nM 8.96
CHEMBL3121256 — Kd = 1.156 nM 8.94
CHEMBL3121254 — Kd = 1.171 nM 8.93
CHEMBL3121252 — Kd = 1.213 nM 8.92
CHEMBL3121265 — IC50 = 1.238 nM 8.91
CHEMBL3121266 — Kd = 1.27 nM 8.90
CHEMBL3121259 — Kd = 1.26 nM 8.90
CHEMBL3121258 — Kd = 1.3 nM 8.89
CHEMBL3121251 — IC50 = 1.32 nM 8.88
CHEMBL3121249 — Kd = 1.36 nM 8.87
CHEMBL3121269 — IC50 = 1.35 nM 8.87
CHEMBL3121262 — IC50 = 1.36 nM 8.87
CHEMBL3121263 — IC50 = 1.38 nM 8.86
CHEMBL3121267 — Kd = 1.54 nM 8.81
CHEMBL3121268 — IC50 = 1.63 nM 8.79
CHEMBL12 DIAZEPAM Kd = 1.75 nM 8.76
CHEMBL3121255 — IC50 = 1.753 nM 8.76
CHEMBL3121261 — IC50 = 1.783 nM 8.75
CHEMBL3121256 — IC50 = 1.885 nM 8.72
CHEMBL3121254 — IC50 = 1.901 nM 8.72
CHEMBL3121260 — Kd = 1.9 nM 8.72
CHEMBL3121252 — IC50 = 1.968 nM 8.71
CHEMBL3121259 — IC50 = 2.07 nM 8.68
CHEMBL3121266 — IC50 = 2.069 nM 8.68
CHEMBL3121258 — IC50 = 2.13 nM 8.67
CHEMBL3121257 — Kd = 2.144 nM 8.67
CHEMBL3121249 — IC50 = 2.23 nM 8.65
CHEMBL3121250 — Kd = 2.32 nM 8.63
CHEMBL3121267 — IC50 = 2.52 nM 8.60
CHEMBL12 DIAZEPAM IC50 = 2.857 nM 8.54
CHEMBL3121260 — IC50 = 3.095 nM 8.51
CHEMBL3121257 — IC50 = 3.494 nM 8.46
CHEMBL3121250 — IC50 = 3.779 nM 8.42
CHEMBL3121264 — IC50 - — -
CHEMBL3121264 — Kd - — -