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Assay Detail

CHEMBL648136

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

Binding
Binding affinity to peripheral benzodiazepine receptors using [3H]-PK11195 radioligand in rat kidney mitochondrial membrane
30
Total Activities
30
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Expert

Target

Translocator protein (CHEMBL4552)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

N,N-dialkyl-2-phenylindol-3-ylglyoxylamides. A new class of potent and selective ligands at the peripheral benzodiazepine receptor.
Primofiore G, Da Settimo F, Taliani S, Simorini F, Patrizi MP, Novellino E, Greco G, Abignente E, Costa B, Chelli B, Martini C.
J Med Chem (2004) 47 : 1852 -1855
PubMed 15027878 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 30 7.96 9.43

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL53430 1 9.43
CHEMBL55162 1 9.26
CHEMBL55781 1 9.21
CHEMBL292847 1 9.00
CHEMBL294625 1 8.85
CHEMBL55135 1 8.80
CHEMBL300762 1 8.72
CHEMBL54403 1 8.62
CHEMBL54627 1 8.55
CHEMBL431747 1 8.42
CHEMBL299487 1 8.37
CHEMBL294423 1 8.33
CHEMBL54066 1 8.31
CHEMBL53255 1 8.26
CHEMBL53259 1 8.24
CHEMBL54349 ALPIDEM 4.0 1 8.15
CHEMBL431938 1 8.12
CHEMBL481537 PK-11195 1 8.03
CHEMBL56058 1 7.91
CHEMBL291774 1 7.80
CHEMBL55190 1 7.77
CHEMBL286346 RO-54864 1 7.64
CHEMBL54740 1 7.48
CHEMBL55126 1 7.37
CHEMBL300128 1 7.23
CHEMBL301836 1 6.99
CHEMBL299975 1 6.18
CHEMBL53277 1 6.09
CHEMBL55316 1 5.93
CHEMBL55648 1 5.62

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL53430 Ki = 0.37 nM 9.43
CHEMBL55162 Ki = 0.55 nM 9.26
CHEMBL55781 Ki = 0.62 nM 9.21
CHEMBL292847 Ki = 1.0 nM 9.00
CHEMBL294625 Ki = 1.4 nM 8.85
CHEMBL55135 Ki = 1.6 nM 8.80
CHEMBL300762 Ki = 1.9 nM 8.72
CHEMBL54403 Ki = 2.4 nM 8.62
CHEMBL54627 Ki = 2.8 nM 8.55
CHEMBL431747 Ki = 3.8 nM 8.42
CHEMBL299487 Ki = 4.28 nM 8.37
CHEMBL294423 Ki = 4.65 nM 8.33
CHEMBL54066 Ki = 4.91 nM 8.31
CHEMBL53255 Ki = 5.5 nM 8.26
CHEMBL53259 Ki = 5.8 nM 8.24
CHEMBL54349 ALPIDEM Ki = 7.0 nM 8.15
CHEMBL431938 Ki = 7.5 nM 8.12
CHEMBL481537 PK-11195 Ki = 9.3 nM 8.03
CHEMBL56058 Ki = 12.2 nM 7.91
CHEMBL291774 Ki = 16.0 nM 7.80
CHEMBL55190 Ki = 17.0 nM 7.77
CHEMBL286346 RO-54864 Ki = 23.0 nM 7.64
CHEMBL54740 Ki = 33.0 nM 7.48
CHEMBL55126 Ki = 43.0 nM 7.37
CHEMBL300128 Ki = 58.4 nM 7.23
CHEMBL301836 Ki = 103.0 nM 6.99
CHEMBL299975 Ki = 665.0 nM 6.18
CHEMBL53277 Ki = 815.0 nM 6.09
CHEMBL55316 Ki = 1167.0 nM 5.93
CHEMBL55648 Ki = 2400.0 nM 5.62