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Assay Detail

CHEMBL900871

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

Binding
Displacement of [3H]-N-alpha methyl histamine from rat H3 receptor expressed in C6 cells
14
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Cell Type C6
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Histamine H3 receptor (CHEMBL4124)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Synthesis, potency, and in vivo profiles of quinoline containing histamine H3 receptor inverse agonists.
Altenbach RJ, Liu H, Banfor PN, Browman KE, Fox GB, Fryer RM, Komater VA, Krueger KM, Marsh K, Miller TR, Pan JB, Pan L, Sun M, Thiffault C, Wetter J, Zhao C, Zhou D, Esbenshade TA, Hancock AA, Cowart MD.
J Med Chem (2007) 50 : 5439 -5448
PubMed 17918921 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 14 8.98 9.31

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL237394 2 9.31
CHEMBL237191 2 9.14
CHEMBL393581 2 9.04
CHEMBL392573 2 9.03
CHEMBL351231 2 8.87
CHEMBL442242 2 8.79
CHEMBL263101 2 8.71

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL237394 Ki = 0.4898 nM 9.31
CHEMBL237394 Ki = 0.49 nM 9.31
CHEMBL237191 Ki = 0.7244 nM 9.14
CHEMBL237191 Ki = 0.72 nM 9.14
CHEMBL393581 Ki = 0.912 nM 9.04
CHEMBL393581 Ki = 0.91 nM 9.04
CHEMBL392573 Ki = 0.9333 nM 9.03
CHEMBL392573 Ki = 0.93 nM 9.03
CHEMBL351231 Ki = 1.349 nM 8.87
CHEMBL351231 Ki = 1.35 nM 8.87
CHEMBL442242 Ki = 1.622 nM 8.79
CHEMBL442242 Ki = 1.62 nM 8.79
CHEMBL263101 Ki = 1.95 nM 8.71
CHEMBL263101 Ki = 1.95 nM 8.71