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Assay Detail

CHEMBL917141

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

Binding
Displacement of [3H]flumazenil from benzodiazepine receptor in bovine brain membranes
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Bos taurus
Subcellular Brain membranes
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Novel N-substituted indol-3-ylglyoxylamides probing the LDi and L1/L2 lipophilic regions of the benzodiazepine receptor site in search for subtype-selective ligands.
Primofiore G, Taliani S, Da Settimo F, Marini AM, La Motta C, Simorini F, Patrizi MP, Sergianni V, Novellino E, Greco G, Cosimelli B, Calderone V, Montali M, Besnard F, Martini C.
J Med Chem (2007) 50 : 1627 -1634
PubMed 17335185 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 20 6.62 9.07

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL452 CLONAZEPAM 4.0 1 9.07
CHEMBL407 FLUMAZENIL 4.0 1 9.05
CHEMBL12 DIAZEPAM 4.0 1 8.00
CHEMBL375367 1 7.24
CHEMBL223707 1 7.06
CHEMBL376508 1 7.03
CHEMBL222316 1 6.96
CHEMBL75307 1 6.93
CHEMBL75289 1 6.92
CHEMBL373871 1 6.79
CHEMBL220373 1 6.38
CHEMBL220737 1 6.22
CHEMBL373662 1 5.83
CHEMBL223152 1 5.78
CHEMBL385100 1 5.67
CHEMBL376064 1 5.57
CHEMBL373462 1 5.55
CHEMBL374536 1 5.49
CHEMBL223476 1 5.43
CHEMBL223480 1 5.39

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL452 CLONAZEPAM Ki = 0.85 nM 9.07
CHEMBL407 FLUMAZENIL Ki = 0.9 nM 9.05
CHEMBL12 DIAZEPAM Ki = 10.0 nM 8.00
CHEMBL375367 Ki = 57.8 nM 7.24
CHEMBL223707 Ki = 88.0 nM 7.06
CHEMBL376508 Ki = 93.0 nM 7.03
CHEMBL222316 Ki = 110.0 nM 6.96
CHEMBL75307 Ki = 117.0 nM 6.93
CHEMBL75289 Ki = 120.0 nM 6.92
CHEMBL373871 Ki = 164.0 nM 6.79
CHEMBL220373 Ki = 412.0 nM 6.38
CHEMBL220737 Ki = 606.0 nM 6.22
CHEMBL373662 Ki = 1480.0 nM 5.83
CHEMBL223152 Ki = 1650.0 nM 5.78
CHEMBL385100 Ki = 2160.0 nM 5.67
CHEMBL376064 Ki = 2690.0 nM 5.57
CHEMBL373462 Ki = 2800.0 nM 5.55
CHEMBL374536 Ki = 3275.0 nM 5.49
CHEMBL223476 Ki = 3720.0 nM 5.43
CHEMBL223480 Ki = 4100.0 nM 5.39