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

CHEMBL5151456

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

Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL ↗
86
Total Activities
43
Compounds Tested
2
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 H2 receptor (CHEMBL1941) ↗
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
Ki 43 6.91 8.52
Kd 43 7.91 7.91

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5207281 — — 2 8.52
CHEMBL5173079 — — 2 8.32
CHEMBL5206565 — — 2 8.30
CHEMBL5200771 — — 2 8.29
CHEMBL5176229 — — 2 8.28
CHEMBL5208722 — — 2 8.21
CHEMBL5180504 — — 2 8.19
CHEMBL5184911 — — 2 8.09
CHEMBL5179906 — — 2 7.91
CHEMBL5207206 — — 2 7.91
CHEMBL5194860 — — 2 7.91
CHEMBL5172675 — — 2 7.91
CHEMBL5174278 — — 2 7.91
CHEMBL5187758 — — 2 7.91
CHEMBL5183015 — — 2 7.91
CHEMBL301265 PRAMIPEXOLE 4.0 2 7.91
CHEMBL5183205 — — 2 7.91
CHEMBL5209081 — — 2 7.91
CHEMBL5204739 — — 2 7.91
CHEMBL5192993 — — 2 7.91
CHEMBL5198795 — — 2 7.91
CHEMBL5173373 — — 2 7.91
CHEMBL5208327 — — 2 7.91
CHEMBL5174342 — — 2 7.91
CHEMBL5202592 — — 2 7.91
CHEMBL5200106 — — 2 7.91
CHEMBL5188592 — — 2 7.91
CHEMBL5201074 — — 2 7.91
CHEMBL5208845 — — 2 7.91
CHEMBL5208113 — — 2 7.91

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5207281 — Ki = 3.02 nM 8.52
CHEMBL5173079 — Ki = 4.786 nM 8.32
CHEMBL5206565 — Ki = 5.012 nM 8.30
CHEMBL5200771 — Ki = 5.129 nM 8.29
CHEMBL5176229 — Ki = 5.248 nM 8.28
CHEMBL5208722 — Ki = 6.166 nM 8.21
CHEMBL5180504 — Ki = 6.457 nM 8.19
CHEMBL5184911 — Ki = 8.128 nM 8.09
CHEMBL5174342 — Kd = 12.2 nM 7.91
CHEMBL5176229 — Kd = 12.2 nM 7.91
CHEMBL5184846 — Kd = 12.2 nM 7.91
CHEMBL5208113 — Kd = 12.2 nM 7.91
CHEMBL5198795 — Kd = 12.2 nM 7.91
CHEMBL5192993 — Kd = 12.2 nM 7.91
CHEMBL5179906 — Kd = 12.2 nM 7.91
CHEMBL5194860 — Kd = 12.2 nM 7.91
CHEMBL5172675 — Kd = 12.2 nM 7.91
CHEMBL5174278 — Kd = 12.2 nM 7.91
CHEMBL90 HISTAMINE Kd = 12.2 nM 7.91
CHEMBL5202592 — Kd = 12.2 nM 7.91
CHEMBL5200106 — Kd = 12.2 nM 7.91
CHEMBL5180504 — Kd = 12.2 nM 7.91
CHEMBL5184911 — Kd = 12.2 nM 7.91
CHEMBL5188592 — Kd = 12.2 nM 7.91
CHEMBL5201074 — Kd = 12.2 nM 7.91
CHEMBL5208845 — Kd = 12.2 nM 7.91
CHEMBL5208722 — Kd = 12.2 nM 7.91
CHEMBL5183205 — Kd = 12.2 nM 7.91
CHEMBL5207281 — Kd = 12.2 nM 7.91
CHEMBL5183015 — Kd = 12.2 nM 7.91
CHEMBL5209479 — Kd = 12.2 nM 7.91
CHEMBL5173373 — Kd = 12.2 nM 7.91
CHEMBL5209021 — Kd = 12.2 nM 7.91
CHEMBL5178472 — Kd = 12.2 nM 7.91
CHEMBL5206565 — Kd = 12.2 nM 7.91
CHEMBL5175558 — Kd = 12.2 nM 7.91
CHEMBL5197548 — Kd = 12.2 nM 7.91
CHEMBL5205197 — Kd = 12.2 nM 7.91
CHEMBL5204599 — Kd = 12.2 nM 7.91
CHEMBL5204739 — Kd = 12.2 nM 7.91
CHEMBL5173079 — Kd = 12.2 nM 7.91
CHEMBL5170276 — Kd = 12.2 nM 7.91
CHEMBL5176780 — Kd = 12.2 nM 7.91
CHEMBL5189006 — Kd = 12.2 nM 7.91
CHEMBL5186770 — Kd = 12.2 nM 7.91
CHEMBL5200771 — Kd = 12.2 nM 7.91
CHEMBL5207206 — Kd = 12.2 nM 7.91
CHEMBL301265 PRAMIPEXOLE Kd = 12.2 nM 7.91
CHEMBL5208327 — Kd = 12.2 nM 7.91
CHEMBL5187758 — Kd = 12.2 nM 7.91