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Assay Detail

CHEMBL874098

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

Binding
In vitro binding affinity determined against imidazoline receptor I-1 from rabbit kidney preparation
30
Total Activities
29
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Oryctolagus cuniculus
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 30 6.65 7.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL60186 1 7.89
CHEMBL13987 1 7.66
CHEMBL13958 1 7.64
CHEMBL14242 2 7.51
CHEMBL60031 1 7.36
CHEMBL13955 1 7.32
CHEMBL14028 1 7.25
CHEMBL274315 1 7.11
CHEMBL62107 1 7.06
CHEMBL61689 1 7.03
CHEMBL13810 1 6.85
CHEMBL274784 1 6.82
CHEMBL58187 1 6.69
CHEMBL276035 1 6.58
CHEMBL13940 1 6.35
CHEMBL13858 1 6.25
CHEMBL267074 1 6.16
CHEMBL14110 1 6.12
CHEMBL13918 1 6.08
CHEMBL13591 1 5.84
CHEMBL418716 1 5.61
CHEMBL13893 1 5.42
CHEMBL14154 1 5.28
CHEMBL13721 1 5.25
CHEMBL13938 1 -
CHEMBL58186 1 -
CHEMBL62095 1 -
CHEMBL13793 1 -
CHEMBL300388 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL60186 Ki = 13.0 nM 7.89
CHEMBL13987 Ki = 21.7 nM 7.66
CHEMBL13958 Ki = 22.7 nM 7.64
CHEMBL14242 Ki = 31.0 nM 7.51
CHEMBL60031 Ki = 44.0 nM 7.36
CHEMBL13955 Ki = 48.0 nM 7.32
CHEMBL14028 Ki = 56.0 nM 7.25
CHEMBL14242 Ki = 57.0 nM 7.24
CHEMBL274315 Ki = 78.6 nM 7.11
CHEMBL62107 Ki = 88.0 nM 7.06
CHEMBL61689 Ki = 93.0 nM 7.03
CHEMBL13810 Ki = 140.0 nM 6.85
CHEMBL274784 Ki = 150.0 nM 6.82
CHEMBL58187 Ki = 204.0 nM 6.69
CHEMBL276035 Ki = 260.0 nM 6.58
CHEMBL13940 Ki = 450.0 nM 6.35
CHEMBL13858 Ki = 560.0 nM 6.25
CHEMBL267074 Ki = 690.0 nM 6.16
CHEMBL14110 Ki = 760.0 nM 6.12
CHEMBL13918 Ki = 840.0 nM 6.08
CHEMBL13591 Ki = 1430.0 nM 5.84
CHEMBL418716 Ki = 2440.0 nM 5.61
CHEMBL13893 Ki = 3800.0 nM 5.42
CHEMBL14154 Ki = 5300.0 nM 5.28
CHEMBL13721 Ki = 5590.0 nM 5.25
CHEMBL13938 Ki > 10000.0 nM -
CHEMBL58186 Ki > 1000.0 nM -
CHEMBL62095 Ki > 1000.0 nM -
CHEMBL13793 Ki > 1000.0 nM -
CHEMBL300388 Ki > 10000.0 nM -