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Assay Detail

CHEMBL2379237

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

Binding
Displacement of [3H]-raclopride from human dopamine D2L receptor expressed in HEK293 cells after 1 hr
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(2) dopamine receptor (CHEMBL217)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and biological evaluation of novel pyrrolidine-2,5-dione derivatives as potential antidepressant agents. Part 1.
Wróbel MZ, Chodkowski A, Herold F, Gomółka A, Kleps J, Mazurek AP, Pluciński F, Mazurek A, Nowak G, Siwek A, Stachowicz K, Sławińska A, Wolak M, Szewczyk B, Satała G, Bojarski AJ, Turło J.
Eur J Med Chem (2013) 63 : 484 -500
PubMed 23524160 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 4 7.05 7.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2377590 1 7.85
CHEMBL2377445 1 7.10
CHEMBL2377591 1 6.79
CHEMBL2377443 1 6.46

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2377590 Ki = 14.0 nM 7.85
CHEMBL2377445 Ki = 80.0 nM 7.10
CHEMBL2377591 Ki = 161.0 nM 6.79
CHEMBL2377443 Ki = 343.0 nM 6.46