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Assay Detail

CHEMBL900873

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

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

Assay Information

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

Target

Histamine H3 receptor (CHEMBL264) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

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 9.52 9.73

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL237394 — — 2 9.73
CHEMBL392573 — — 2 9.62
CHEMBL393581 — — 2 9.59
CHEMBL237191 — — 2 9.54
CHEMBL263101 — — 2 9.47
CHEMBL351231 — — 2 9.35
CHEMBL442242 — — 2 9.35

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL237394 — Ki = 0.1862 nM 9.73
CHEMBL237394 — Ki = 0.19 nM 9.72
CHEMBL392573 — Ki = 0.2399 nM 9.62
CHEMBL392573 — Ki = 0.24 nM 9.62
CHEMBL393581 — Ki = 0.257 nM 9.59
CHEMBL393581 — Ki = 0.26 nM 9.59
CHEMBL237191 — Ki = 0.2884 nM 9.54
CHEMBL237191 — Ki = 0.29 nM 9.54
CHEMBL263101 — Ki = 0.3388 nM 9.47
CHEMBL263101 — Ki = 0.34 nM 9.47
CHEMBL351231 — Ki = 0.4467 nM 9.35
CHEMBL351231 — Ki = 0.45 nM 9.35
CHEMBL442242 — Ki = 0.4467 nM 9.35
CHEMBL442242 — Ki = 0.45 nM 9.35