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Assay Detail

CHEMBL648647

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Binding
Binding affinity to rat benzodiazepine receptor
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Identification and structure-activity studies of novel ultrashort-acting benzodiazepine receptor agonists.
Stafford JA, Pacofsky GJ, Cox RF, Cowan JR, Dorsey GF, Gonzales SS, Jung DK, Koszalka GW, McIntyre MS, Tidwell JH, Wiard RP, Feldman PL.
Bioorg Med Chem Lett (2002) 12 : 3215 -3218
PubMed 12372537 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 28 7.19 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL655 MIDAZOLAM 4.0 1 8.70
CHEMBL108819 1 8.52
CHEMBL107782 1 8.52
CHEMBL108910 1 8.52
CHEMBL108991 1 8.15
CHEMBL108911 1 8.15
CHEMBL12 DIAZEPAM 4.0 1 7.85
CHEMBL107704 1 7.77
CHEMBL108233 1 7.64
CHEMBL324200 1 7.54
CHEMBL321474 1 7.47
CHEMBL107506 1 7.41
CHEMBL109154 1 7.35
CHEMBL327124 1 7.28
CHEMBL412571 1 7.09
CHEMBL111535 1 7.04
CHEMBL321487 1 6.93
CHEMBL324194 1 6.91
CHEMBL322111 1 6.79
CHEMBL109155 1 6.75
CHEMBL322930 1 6.72
CHEMBL111533 1 6.70
CHEMBL111025 1 6.62
CHEMBL325801 1 6.54
CHEMBL108080 1 6.32
CHEMBL108920 1 6.13
CHEMBL107816 1 5.84
CHEMBL107658 1 4.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL655 MIDAZOLAM Ki = 2.0 nM 8.70
CHEMBL108819 Ki = 3.0 nM 8.52
CHEMBL107782 Ki = 3.0 nM 8.52
CHEMBL108910 Ki = 3.0 nM 8.52
CHEMBL108991 Ki = 7.0 nM 8.15
CHEMBL108911 Ki = 7.0 nM 8.15
CHEMBL12 DIAZEPAM Ki = 14.0 nM 7.85
CHEMBL107704 Ki = 17.0 nM 7.77
CHEMBL108233 Ki = 23.0 nM 7.64
CHEMBL324200 Ki = 29.0 nM 7.54
CHEMBL321474 Ki = 34.0 nM 7.47
CHEMBL107506 Ki = 39.0 nM 7.41
CHEMBL109154 Ki = 45.0 nM 7.35
CHEMBL327124 Ki = 53.0 nM 7.28
CHEMBL412571 Ki = 81.0 nM 7.09
CHEMBL111535 Ki = 92.0 nM 7.04
CHEMBL321487 Ki = 118.0 nM 6.93
CHEMBL324194 Ki = 124.0 nM 6.91
CHEMBL322111 Ki = 163.0 nM 6.79
CHEMBL109155 Ki = 176.0 nM 6.75
CHEMBL322930 Ki = 189.0 nM 6.72
CHEMBL111533 Ki = 200.0 nM 6.70
CHEMBL111025 Ki = 242.0 nM 6.62
CHEMBL325801 Ki = 289.0 nM 6.54
CHEMBL108080 Ki = 480.0 nM 6.32
CHEMBL108920 Ki = 741.0 nM 6.13
CHEMBL107816 Ki = 1447.0 nM 5.84
CHEMBL107658 Ki = 100000.0 nM 4.00