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Assay Detail

CHEMBL841871

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

Binding
In vitro binding affinity determined against imidazoline receptor I-2 using rabbit kidney preparation
31
Total Activities
29
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Nischarin (CHEMBL3923)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and biological evaluation of new 2-(4,5-dihydro-1H-imidazol-2-yl)-3,4-dihydro-2H-1,4-benzoxazine derivatives.
Touzeau F, Arrault A, Guillaumet G, Scalbert E, Pfeiffer B, Rettori MC, Renard P, Mérour JY.
J Med Chem (2003) 46 : 1962 -1979
PubMed 12723959 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 31 7.04 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL13987 1 8.70
CHEMBL60186 1 8.46
CHEMBL14242 3 8.33
CHEMBL62107 1 8.15
CHEMBL14028 1 8.10
CHEMBL274784 1 8.00
CHEMBL300388 1 7.77
CHEMBL13955 1 7.48
CHEMBL60031 1 7.37
CHEMBL276035 1 7.33
CHEMBL13918 1 7.29
CHEMBL13958 1 7.27
CHEMBL274315 1 7.18
CHEMBL58187 1 7.00
CHEMBL13940 1 6.80
CHEMBL13810 1 6.76
CHEMBL61689 1 6.56
CHEMBL14110 1 6.33
CHEMBL13591 1 6.21
CHEMBL418716 1 6.19
CHEMBL13858 1 6.12
CHEMBL267074 1 6.10
CHEMBL13893 1 5.80
CHEMBL13721 1 5.07
CHEMBL14154 1 4.75
CHEMBL13938 1 -
CHEMBL58186 1 -
CHEMBL62095 1 -
CHEMBL13793 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL13987 Ki = 1.99 nM 8.70
CHEMBL60186 Ki = 3.5 nM 8.46
CHEMBL14242 Ki = 4.7 nM 8.33
CHEMBL62107 Ki = 7.0 nM 8.15
CHEMBL14028 Ki = 8.0 nM 8.10
CHEMBL274784 Ki = 10.0 nM 8.00
CHEMBL300388 Ki = 17.0 nM 7.77
CHEMBL14242 Ki = 17.0 nM 7.77
CHEMBL13955 Ki = 33.0 nM 7.48
CHEMBL60031 Ki = 43.0 nM 7.37
CHEMBL276035 Ki = 47.0 nM 7.33
CHEMBL13918 Ki = 51.0 nM 7.29
CHEMBL13958 Ki = 53.8 nM 7.27
CHEMBL14242 Ki = 60.0 nM 7.22
CHEMBL274315 Ki = 66.5 nM 7.18
CHEMBL58187 Ki = 100.0 nM 7.00
CHEMBL13940 Ki = 160.0 nM 6.80
CHEMBL13810 Ki = 173.0 nM 6.76
CHEMBL61689 Ki = 278.0 nM 6.56
CHEMBL14110 Ki = 470.0 nM 6.33
CHEMBL13591 Ki = 621.0 nM 6.21
CHEMBL418716 Ki = 643.0 nM 6.19
CHEMBL13858 Ki = 750.0 nM 6.12
CHEMBL267074 Ki = 800.0 nM 6.10
CHEMBL13893 Ki = 1600.0 nM 5.80
CHEMBL13721 Ki = 8530.0 nM 5.07
CHEMBL14154 Ki = 18000.0 nM 4.75
CHEMBL62095 Ki > 1000.0 nM -
CHEMBL58186 Ki > 1000.0 nM -
CHEMBL13938 Ki > 10000.0 nM -
CHEMBL13793 Ki > 1000.0 nM -