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Assay Detail

CHEMBL5151464

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

Binding
Displacement of [3H]N-methylspiperone from human D2 long receptor stably expressed in HEK293T cells co-expressing luciferase and CEK incubated for 140 mins by radioligand competition binding based assay
ChEMBL ↗
27
Total Activities
14
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293T
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

D(2) dopamine receptor (CHEMBL217) ↗
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 14 10.83 10.83
Ki 13 5.72 6.35

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5207281 — — 2 10.83
CHEMBL5183205 — — 2 10.83
CHEMBL5200771 — — 2 10.83
CHEMBL5204599 — — 2 10.83
CHEMBL5206565 — — 2 10.83
CHEMBL5178472 — — 2 10.83
CHEMBL5208845 — — 2 10.83
CHEMBL5201074 — — 2 10.83
CHEMBL5184911 — — 2 10.83
CHEMBL5180504 — — 2 10.83
CHEMBL5202592 — — 2 10.83
CHEMBL5198795 — — 2 10.83
CHEMBL5176229 — — 2 10.83
CHEMBL301265 PRAMIPEXOLE 4.0 1 10.83

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5176229 — Kd = 0.0149 nM 10.83
CHEMBL5207281 — Kd = 0.0149 nM 10.83
CHEMBL5183205 — Kd = 0.0149 nM 10.83
CHEMBL5200771 — Kd = 0.0149 nM 10.83
CHEMBL5204599 — Kd = 0.0149 nM 10.83
CHEMBL5206565 — Kd = 0.0149 nM 10.83
CHEMBL5178472 — Kd = 0.0149 nM 10.83
CHEMBL5201074 — Kd = 0.0149 nM 10.83
CHEMBL5184911 — Kd = 0.0149 nM 10.83
CHEMBL5180504 — Kd = 0.0149 nM 10.83
CHEMBL5202592 — Kd = 0.0149 nM 10.83
CHEMBL5198795 — Kd = 0.0149 nM 10.83
CHEMBL301265 PRAMIPEXOLE Kd = 0.0149 nM 10.83
CHEMBL5208845 — Kd = 0.0149 nM 10.83
CHEMBL5198795 — Ki = 446.68 nM 6.35
CHEMBL5202592 — Ki = 489.78 nM 6.31
CHEMBL5176229 — Ki = 954.99 nM 6.02
CHEMBL5180504 — Ki = 1071.52 nM 5.97
CHEMBL5204599 — Ki = 1621.81 nM 5.79
CHEMBL5183205 — Ki = 3467.37 nM 5.46
CHEMBL5178472 — Ki = 4570.88 nM 5.34
CHEMBL5206565 — Ki = 6309.57 nM 5.20
CHEMBL5207281 — Ki = 9549.93 nM 5.02
CHEMBL5184911 — Ki > 10000.0 nM -
CHEMBL5201074 — Ki > 10000.0 nM -
CHEMBL5208845 — Ki > 10000.0 nM -
CHEMBL5200771 — Ki > 10000.0 nM -