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Assay Detail

CHEMBL5151485

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

Binding
Displacement of [3H]SCH23390 from human D1 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK incubated for 60 mins by scintillation counting analysis
8
Total Activities
4
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(1A) dopamine receptor (CHEMBL2056)
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 4 5.93 6.59
Kd 4 9.64 9.64

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4860528 2 9.64
CHEMBL5207281 2 9.64
CHEMBL5206565 2 9.64
CHEMBL5201074 2 9.64

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5207281 Kd = 0.23 nM 9.64
CHEMBL5206565 Kd = 0.23 nM 9.64
CHEMBL5201074 Kd = 0.23 nM 9.64
CHEMBL4860528 Kd = 0.23 nM 9.64
CHEMBL4860528 Ki = 257.04 nM 6.59
CHEMBL5206565 Ki = 1380.38 nM 5.86
CHEMBL5201074 Ki = 2187.76 nM 5.66
CHEMBL5207281 Ki = 2454.71 nM 5.61