Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL5151459

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

Binding
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL ↗
86
Total Activities
43
Compounds Tested
3
Activity Types
0
Assay Parameters

Assay Information

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

Target

Histamine H4 receptor (CHEMBL3759) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Abolishing Dopamine D<sub>2long</sub>/D<sub>3</sub> Receptor Affinity of Subtype-Selective Carbamoylguanidine-Type Histamine H<sub>2</sub> Receptor Agonists.
Tropmann K, Bresinsky M, Forster L, Mönnich D, Buschauer A, Wittmann HJ, Hübner H, Gmeiner P, Pockes S, Strasser A.
J Med Chem (2021) 64 : 8684 -8709
PubMed 34110814 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 43 7.80 7.80
Ki 42 5.45 8.07
pKi 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5208722 — — 2 8.07
CHEMBL5179906 — — 2 7.80
CHEMBL5200771 — — 2 7.80
CHEMBL5207206 — — 2 7.80
CHEMBL5204739 — — 2 7.80
CHEMBL5209081 — — 2 7.80
CHEMBL5183205 — — 2 7.80
CHEMBL5207281 — — 2 7.80
CHEMBL301265 PRAMIPEXOLE 4.0 2 7.80
CHEMBL5170276 — — 2 7.80
CHEMBL5187758 — — 2 7.80
CHEMBL5173079 — — 2 7.80
CHEMBL5176229 — — 2 7.80
CHEMBL5174278 — — 2 7.80
CHEMBL5172675 — — 2 7.80
CHEMBL5194860 — — 2 7.80
CHEMBL5192993 — — 2 7.80
CHEMBL5198795 — — 2 7.80
CHEMBL5208113 — — 2 7.80
CHEMBL5173373 — — 2 7.80
CHEMBL5174342 — — 2 7.80
CHEMBL5202592 — — 2 7.80
CHEMBL5200106 — — 2 7.80
CHEMBL5180504 — — 2 7.80
CHEMBL5184911 — — 2 7.80
CHEMBL5188592 — — 2 7.80
CHEMBL5201074 — — 2 7.80
CHEMBL5208845 — — 2 7.80
CHEMBL5184846 — — 2 7.80
CHEMBL5208327 — — 2 7.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5208722 — Ki = 8.511 nM 8.07
CHEMBL5187758 — Kd = 16.0 nM 7.80
CHEMBL5183015 — Kd = 16.0 nM 7.80
CHEMBL5173079 — Kd = 16.0 nM 7.80
CHEMBL5176229 — Kd = 16.0 nM 7.80
CHEMBL5174278 — Kd = 16.0 nM 7.80
CHEMBL5172675 — Kd = 16.0 nM 7.80
CHEMBL5194860 — Kd = 16.0 nM 7.80
CHEMBL5179906 — Kd = 16.0 nM 7.80
CHEMBL5192993 — Kd = 16.0 nM 7.80
CHEMBL5198795 — Kd = 16.0 nM 7.80
CHEMBL5208113 — Kd = 16.0 nM 7.80
CHEMBL301265 PRAMIPEXOLE Kd = 16.0 nM 7.80
CHEMBL5174342 — Kd = 16.0 nM 7.80
CHEMBL5202592 — Kd = 16.0 nM 7.80
CHEMBL5200106 — Kd = 16.0 nM 7.80
CHEMBL5180504 — Kd = 16.0 nM 7.80
CHEMBL5184911 — Kd = 16.0 nM 7.80
CHEMBL5188592 — Kd = 16.0 nM 7.80
CHEMBL5201074 — Kd = 16.0 nM 7.80
CHEMBL5208845 — Kd = 16.0 nM 7.80
CHEMBL5208722 — Kd = 16.0 nM 7.80
CHEMBL90 HISTAMINE Kd = 16.0 nM 7.80
CHEMBL5207281 — Kd = 16.0 nM 7.80
CHEMBL5173373 — Kd = 16.0 nM 7.80
CHEMBL5209021 — Kd = 16.0 nM 7.80
CHEMBL5178472 — Kd = 16.0 nM 7.80
CHEMBL5206565 — Kd = 16.0 nM 7.80
CHEMBL5175558 — Kd = 16.0 nM 7.80
CHEMBL5197548 — Kd = 16.0 nM 7.80
CHEMBL5205197 — Kd = 16.0 nM 7.80
CHEMBL5204599 — Kd = 16.0 nM 7.80
CHEMBL5209479 — Kd = 16.0 nM 7.80
CHEMBL5184846 — Kd = 16.0 nM 7.80
CHEMBL5170276 — Kd = 16.0 nM 7.80
CHEMBL5176780 — Kd = 16.0 nM 7.80
CHEMBL5189006 — Kd = 16.0 nM 7.80
CHEMBL5186770 — Kd = 16.0 nM 7.80
CHEMBL5200771 — Kd = 16.0 nM 7.80
CHEMBL5207206 — Kd = 16.0 nM 7.80
CHEMBL5204739 — Kd = 16.0 nM 7.80
CHEMBL5209081 — Kd = 16.0 nM 7.80
CHEMBL5183205 — Kd = 16.0 nM 7.80
CHEMBL5208327 — Kd = 16.0 nM 7.80
CHEMBL90 HISTAMINE Ki = 25.12 nM 7.60
CHEMBL5172675 — Ki = 2137.96 nM 5.67
CHEMBL5174278 — Ki = 2344.23 nM 5.63
CHEMBL5208113 — Ki = 3388.44 nM 5.47
CHEMBL5194860 — Ki = 4073.8 nM 5.39
CHEMBL5202592 — Ki = 4466.84 nM 5.35