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Assay Detail

CHEMBL4606556

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

Binding
Displacement of [3H]-UR-PI294 from Galphai2/Gbeta1gamma2-coupled human recombinant H3R expressed in baculovirus infected Sf9 insect cell membranes
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Sf9
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

UR-DEBa242: A Py-5-Labeled Fluorescent Multipurpose Probe for Investigations on the Histamine H3 and H4 Receptors.
Bartole E, Grätz L, Littmann T, Wifling D, Seibel U, Buschauer A, Bernhardt G.
J Med Chem (2020) 63 : 5297 -5311
PubMed 32420741 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 10 6.83 9.04

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4642520 1 9.04
CHEMBL4635634 1 8.60
CHEMBL4636487 1 7.93
CHEMBL4634235 1 7.87
CHEMBL4646286 1 6.34
CHEMBL4633688 1 6.30
CHEMBL4640263 1 6.07
CHEMBL4634728 1 5.79
CHEMBL4639472 1 5.62
CHEMBL4634631 1 4.69

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4642520 Ki = 0.912 nM 9.04
CHEMBL4635634 Ki = 2.512 nM 8.60
CHEMBL4636487 Ki = 11.75 nM 7.93
CHEMBL4634235 Ki = 13.49 nM 7.87
CHEMBL4646286 Ki = 457.09 nM 6.34
CHEMBL4633688 Ki = 501.19 nM 6.30
CHEMBL4640263 Ki = 851.14 nM 6.07
CHEMBL4634728 Ki = 1621.81 nM 5.79
CHEMBL4639472 Ki = 2398.83 nM 5.62
CHEMBL4634631 Ki = 20417.38 nM 4.69