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Assay Detail

CHEMBL4433967

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

Binding
Displacement of [3H]-SCH23390 from wild type human D1R expressed in HEK293 cell membranes incubated for 90 mins by scintillation counting based competition radioligand binding assay
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

D(1A) dopamine receptor (CHEMBL2056)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and Pharmacological Evaluation of Noncatechol G Protein Biased and Unbiased Dopamine D1 Receptor Agonists.
Wang P, Felsing DE, Chen H, Raval SR, Allen JA, Zhou J.
ACS Med Chem Lett (2019) 10 : 792 -799
PubMed 31098001 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 4 7.76 8.62

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4453318 1 8.62
CHEMBL353335 1 7.82
CHEMBL4469983 1 7.29
CHEMBL3697578 RAZPIPADON 2.0 1 7.29

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4453318 Ki = 2.4 nM 8.62
CHEMBL353335 Ki = 15.0 nM 7.82
CHEMBL4469983 Ki = 51.0 nM 7.29
CHEMBL3697578 RAZPIPADON Ki = 51.0 nM 7.29