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Assay Detail

CHEMBL5151466

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

Binding
Displacement of [3H]N-methylspiperone from human D3 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK incubated for 140 mins by radioligand competition binding based assay
ChEMBL ↗
28
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(3) dopamine receptor (CHEMBL234) ↗
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 14 6.62 9.18
Kd 14 10.59 10.59

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL301265 PRAMIPEXOLE 4.0 2 10.59
CHEMBL5207281 — — 2 10.59
CHEMBL5183205 — — 2 10.59
CHEMBL5200771 — — 2 10.59
CHEMBL5204599 — — 2 10.59
CHEMBL5206565 — — 2 10.59
CHEMBL5178472 — — 2 10.59
CHEMBL5208845 — — 2 10.59
CHEMBL5201074 — — 2 10.59
CHEMBL5184911 — — 2 10.59
CHEMBL5180504 — — 2 10.59
CHEMBL5202592 — — 2 10.59
CHEMBL5198795 — — 2 10.59
CHEMBL5176229 — — 2 10.59

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5176229 — Kd = 0.0258 nM 10.59
CHEMBL5198795 — Kd = 0.0258 nM 10.59
CHEMBL5202592 — Kd = 0.0258 nM 10.59
CHEMBL5180504 — Kd = 0.0258 nM 10.59
CHEMBL5184911 — Kd = 0.0258 nM 10.59
CHEMBL5201074 — Kd = 0.0258 nM 10.59
CHEMBL5208845 — Kd = 0.0258 nM 10.59
CHEMBL5178472 — Kd = 0.0258 nM 10.59
CHEMBL5206565 — Kd = 0.0258 nM 10.59
CHEMBL5204599 — Kd = 0.0258 nM 10.59
CHEMBL5200771 — Kd = 0.0258 nM 10.59
CHEMBL5183205 — Kd = 0.0258 nM 10.59
CHEMBL5207281 — Kd = 0.0258 nM 10.59
CHEMBL301265 PRAMIPEXOLE Kd = 0.0258 nM 10.59
CHEMBL301265 PRAMIPEXOLE Ki = 0.6607 nM 9.18
CHEMBL5183205 — Ki = 31.62 nM 7.50
CHEMBL5176229 — Ki = 60.26 nM 7.22
CHEMBL5178472 — Ki = 74.13 nM 7.13
CHEMBL5202592 — Ki = 229.09 nM 6.64
CHEMBL5204599 — Ki = 234.42 nM 6.63
CHEMBL5198795 — Ki = 323.59 nM 6.49
CHEMBL5200771 — Ki = 588.84 nM 6.23
CHEMBL5184911 — Ki = 660.69 nM 6.18
CHEMBL5207281 — Ki = 794.33 nM 6.10
CHEMBL5180504 — Ki = 2041.74 nM 5.69
CHEMBL5206565 — Ki = 2630.27 nM 5.58
CHEMBL5208845 — Ki = 3235.94 nM 5.49
CHEMBL5201074 — Ki > 10000.0 nM -