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Assay Detail

CHEMBL650823

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

Binding
Inhibition of [3H]-Ro- 15-1788 binding to GABA-A benzodiazepine receptor of bovine brain membranes
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Bos taurus
Subcellular Brain membranes
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

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

Publication

N'-Phenylindol-3-ylglyoxylohydrazide derivatives: synthesis, structure-activity relationships, molecular modeling studies, and pharmacological action on brain benzodiazepine receptors.
Da Settimo A, Primofiore G, Da Settimo F, Marini AM, Novellino E, Greco G, Gesi M, Martini C, Giannaccini G, Lucacchini A.
J Med Chem (1998) 41 : 3821 -3830
PubMed 9748357 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 22 6.81 7.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL308760 1 7.96
CHEMBL74448 1 7.96
CHEMBL75212 1 7.52
CHEMBL75306 1 7.28
CHEMBL127135 1 7.28
CHEMBL124323 1 7.24
CHEMBL124871 1 7.21
CHEMBL73288 1 7.17
CHEMBL306370 1 7.03
CHEMBL74280 1 6.97
CHEMBL75307 1 6.93
CHEMBL75289 1 6.92
CHEMBL306310 1 6.79
CHEMBL72505 1 6.69
CHEMBL332059 1 6.54
CHEMBL74013 1 6.37
CHEMBL127519 1 6.34
CHEMBL74589 1 6.31
CHEMBL127359 1 6.29
CHEMBL124212 1 5.92
CHEMBL123802 1 5.62
CHEMBL337913 1 5.47

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL308760 Ki = 11.0 nM 7.96
CHEMBL74448 Ki = 11.0 nM 7.96
CHEMBL75212 Ki = 30.0 nM 7.52
CHEMBL75306 Ki = 53.0 nM 7.28
CHEMBL127135 Ki = 52.0 nM 7.28
CHEMBL124323 Ki = 57.0 nM 7.24
CHEMBL124871 Ki = 62.0 nM 7.21
CHEMBL73288 Ki = 67.0 nM 7.17
CHEMBL306370 Ki = 94.0 nM 7.03
CHEMBL74280 Ki = 107.0 nM 6.97
CHEMBL75307 Ki = 117.0 nM 6.93
CHEMBL75289 Ki = 120.0 nM 6.92
CHEMBL306310 Ki = 163.0 nM 6.79
CHEMBL72505 Ki = 203.0 nM 6.69
CHEMBL332059 Ki = 290.0 nM 6.54
CHEMBL74013 Ki = 430.0 nM 6.37
CHEMBL127519 Ki = 455.0 nM 6.34
CHEMBL74589 Ki = 490.0 nM 6.31
CHEMBL127359 Ki = 510.0 nM 6.29
CHEMBL124212 Ki = 1200.0 nM 5.92
CHEMBL123802 Ki = 2400.0 nM 5.62
CHEMBL337913 Ki = 3400.0 nM 5.47