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Assay Detail

CHEMBL2182832

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

Binding
Displacement of [3H]YM-09151-2 from human dopamine D2 receptor expressed in CHOp cells
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

D(2) dopamine receptor (CHEMBL217)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery and pharmacological evaluation of a diphenethylamine derivative (HS665), a highly potent and selective κ opioid receptor agonist.
Spetea M, Berzetei-Gurske IP, Guerrieri E, Schmidhammer H.
J Med Chem (2012) 55 : 10302 -10306
PubMed 23134120 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 8 6.33 7.19

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1188090 1 7.19
CHEMBL2180638 1 6.93
CHEMBL59 DOPAMINE 4.0 1 6.38
CHEMBL2180639 1 6.35
CHEMBL2180641 1 6.08
CHEMBL240773 QUINPIROLE 2.0 1 5.93
CHEMBL2180640 1 5.91
CHEMBL2180637 1 5.85

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1188090 Ki = 64.4 nM 7.19
CHEMBL2180638 Ki = 118.0 nM 6.93
CHEMBL59 DOPAMINE Ki = 422.0 nM 6.38
CHEMBL2180639 Ki = 450.0 nM 6.35
CHEMBL2180641 Ki = 831.0 nM 6.08
CHEMBL240773 QUINPIROLE Ki = 1185.0 nM 5.93
CHEMBL2180640 Ki = 1233.0 nM 5.91
CHEMBL2180637 Ki = 1420.0 nM 5.85