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Assay Detail

CHEMBL829798

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

Binding
Displacement of [3H]PK11195 from peripheral benzodiazepine receptor of rat cerebral cortex
37
Total Activities
37
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Translocator protein (CHEMBL4552)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Structure-activity relationships and effects on neuroactive steroid synthesis in a series of 2-phenylimidazo[1,2-a]pyridineacetamide peripheral benzodiazepine receptors ligands.
Trapani G, Laquintana V, Denora N, Trapani A, Lopedota A, Latrofa A, Franco M, Serra M, Pisu MG, Floris I, Sanna E, Biggio G, Liso G.
J Med Chem (2005) 48 : 292 -305
PubMed 15634024 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 37 7.43 9.69

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL359841 1 9.69
CHEMBL180210 1 9.52
CHEMBL359593 1 9.05
CHEMBL430139 1 8.86
CHEMBL179432 1 8.77
CHEMBL180279 1 8.67
CHEMBL180523 1 8.57
CHEMBL2096767 1 8.53
CHEMBL179568 1 8.52
CHEMBL179476 1 8.52
CHEMBL360798 1 8.37
CHEMBL178705 1 8.33
CHEMBL178676 1 8.32
CHEMBL368040 1 8.17
CHEMBL179675 1 8.11
CHEMBL179565 1 7.93
CHEMBL369753 1 7.85
CHEMBL179748 1 7.79
CHEMBL179711 1 7.71
CHEMBL369327 1 7.63
CHEMBL361968 1 7.10
CHEMBL363217 1 7.02
CHEMBL362200 1 7.00
CHEMBL362596 1 6.90
CHEMBL362632 1 6.85
CHEMBL179459 1 6.77
CHEMBL179567 1 6.65
CHEMBL427317 1 6.28
CHEMBL178778 1 6.15
CHEMBL178518 1 6.12

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL359841 Ki = 0.203 nM 9.69
CHEMBL180210 Ki = 0.302 nM 9.52
CHEMBL359593 Ki = 0.884 nM 9.05
CHEMBL430139 Ki = 1.379 nM 8.86
CHEMBL179432 Ki = 1.685 nM 8.77
CHEMBL180279 Ki = 2.157 nM 8.67
CHEMBL180523 Ki = 2.679 nM 8.57
CHEMBL2096767 Ki = 2.969 nM 8.53
CHEMBL179568 Ki = 3.054 nM 8.52
CHEMBL179476 Ki = 3.012 nM 8.52
CHEMBL360798 Ki = 4.269 nM 8.37
CHEMBL178705 Ki = 4.639 nM 8.33
CHEMBL178676 Ki = 4.769 nM 8.32
CHEMBL368040 Ki = 6.78 nM 8.17
CHEMBL179675 Ki = 7.841 nM 8.11
CHEMBL179565 Ki = 11.73 nM 7.93
CHEMBL369753 Ki = 14.14 nM 7.85
CHEMBL179748 Ki = 16.03 nM 7.79
CHEMBL179711 Ki = 19.64 nM 7.71
CHEMBL369327 Ki = 23.64 nM 7.63
CHEMBL361968 Ki = 79.77 nM 7.10
CHEMBL363217 Ki = 95.91 nM 7.02
CHEMBL362200 Ki = 98.77 nM 7.00
CHEMBL362596 Ki = 125.65 nM 6.90
CHEMBL362632 Ki = 139.89 nM 6.85
CHEMBL179459 Ki = 169.95 nM 6.77
CHEMBL179567 Ki = 221.66 nM 6.65
CHEMBL427317 Ki = 529.98 nM 6.28
CHEMBL178778 Ki = 701.3 nM 6.15
CHEMBL178518 Ki = 757.47 nM 6.12
CHEMBL361857 Ki = 771.43 nM 6.11
CHEMBL176047 Ki = 1237.99 nM 5.91
CHEMBL179427 Ki = 1279.26 nM 5.89
CHEMBL362037 Ki = 2101.36 nM 5.68
CHEMBL180225 Ki = 2992.21 nM 5.52
CHEMBL435489 Ki = 5774.03 nM 5.24
CHEMBL180377 Ki = 12705.88 nM 4.90