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Assay Detail

CHEMBL883335

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

Binding
Inhibitory concentration against [3H]flunitrazepam binding to benzodiazepine receptor from bovine cerebral cortex
42
Total Activities
42
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Cerebral cortex
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

GABA-A receptor; anion channel (CHEMBL2094107)
Type PROTEIN COMPLEX GROUP
Organism Bos taurus

Publication

Specific inhibition of benzodiazepine receptor binding by some N-(indol-3-ylglyoxylyl)amino acid derivatives: stereoselective interactions.
Primofiore G, Marini AM, Da Settimo F, Martini C, Bardellini A, Giannaccini G, Lucacchini A.
J Med Chem (1989) 32 : 2514 -2518
PubMed 2555510 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 42 5.17 7.16

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL307467 1 7.16
CHEMBL83734 1 7.00
CHEMBL85717 1 6.82
CHEMBL85845 1 6.75
CHEMBL314045 1 6.70
CHEMBL84859 1 6.30
CHEMBL309380 1 6.05
CHEMBL82845 1 5.55
CHEMBL306719 1 5.52
CHEMBL82638 1 5.52
CHEMBL312351 1 5.40
CHEMBL85966 1 5.32
CHEMBL84554 1 5.30
CHEMBL82672 1 5.21
CHEMBL314366 1 5.15
CHEMBL85298 1 5.12
CHEMBL311949 1 4.92
CHEMBL82283 1 4.89
CHEMBL83266 1 4.77
CHEMBL82723 1 4.72
CHEMBL85165 1 4.68
CHEMBL82221 1 4.66
CHEMBL82675 1 4.66
CHEMBL440501 1 4.60
CHEMBL81883 1 4.52
CHEMBL84362 1 4.40
CHEMBL83094 1 4.35
CHEMBL84364 1 4.34
CHEMBL83613 1 4.32
CHEMBL431790 1 4.32

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL307467 IC50 = 70.0 nM 7.16
CHEMBL83734 IC50 = 100.0 nM 7.00
CHEMBL85717 IC50 = 150.0 nM 6.82
CHEMBL85845 IC50 = 180.0 nM 6.75
CHEMBL314045 IC50 = 200.0 nM 6.70
CHEMBL84859 IC50 = 500.0 nM 6.30
CHEMBL309380 IC50 = 900.0 nM 6.05
CHEMBL82845 IC50 = 2800.0 nM 5.55
CHEMBL306719 IC50 = 3000.0 nM 5.52
CHEMBL82638 IC50 = 3000.0 nM 5.52
CHEMBL312351 IC50 = 4000.0 nM 5.40
CHEMBL85966 IC50 = 4800.0 nM 5.32
CHEMBL84554 IC50 = 5010.0 nM 5.30
CHEMBL82672 IC50 = 6200.0 nM 5.21
CHEMBL314366 IC50 = 7100.0 nM 5.15
CHEMBL85298 IC50 = 7500.0 nM 5.12
CHEMBL311949 IC50 = 12000.0 nM 4.92
CHEMBL82283 IC50 = 13000.0 nM 4.89
CHEMBL83266 IC50 = 17000.0 nM 4.77
CHEMBL82723 IC50 = 19000.0 nM 4.72
CHEMBL85165 IC50 = 21000.0 nM 4.68
CHEMBL82221 IC50 = 22000.0 nM 4.66
CHEMBL82675 IC50 = 22000.0 nM 4.66
CHEMBL440501 IC50 = 25000.0 nM 4.60
CHEMBL81883 IC50 = 30000.0 nM 4.52
CHEMBL84362 IC50 = 40010.0 nM 4.40
CHEMBL83094 IC50 = 45000.0 nM 4.35
CHEMBL84364 IC50 = 46010.0 nM 4.34
CHEMBL83613 IC50 = 48000.0 nM 4.32
CHEMBL431790 IC50 = 48000.0 nM 4.32
CHEMBL85731 IC50 = 52000.0 nM 4.28
CHEMBL311063 IC50 = 55000.0 nM 4.26
CHEMBL311445 IC50 = 60000.0 nM 4.22
CHEMBL85840 IC50 = 80000.0 nM 4.10
CHEMBL83216 IC50 = 170000.0 nM -
CHEMBL84445 IC50 = 110000.0 nM -
CHEMBL82002 IC50 = 105000.0 nM -
CHEMBL311128 IC50 = 180000.0 nM -
CHEMBL82617 IC50 = 220000.0 nM -
CHEMBL313285 IC50 = 304000.0 nM -
CHEMBL84571 IC50 = 245000.0 nM -
CHEMBL83535 IC50 = 158000.0 nM -