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Assay Detail

CHEMBL5046490

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

Binding
Displacement of [3H]-(R)-(+)7-OH-DPAT from human dopamine D2 receptor expressed in HEK293 cell membranes incubated for 90 mins by microbeta scintillation counting analysis
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Novel Dual-Target μ-Opioid Receptor and Dopamine D<sub>3</sub> Receptor Ligands as Potential Nonaddictive Pharmacotherapeutics for Pain Management.
Bonifazi A, Battiti FO, Sanchez J, Zaidi SA, Bow E, Makarova M, Cao J, Shaik AB, Sulima A, Rice KC, Katritch V, Canals M, Lane JR, Newman AH.
J Med Chem (2021) 64 : 7778 -7808
PubMed 34011153 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 12 7.07 7.69

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5088070 1 7.69
CHEMBL5073754 1 7.64
CHEMBL5085974 1 7.50
CHEMBL5089655 1 7.44
CHEMBL5074399 1 7.36
CHEMBL5075990 1 7.03
CHEMBL5071238 1 6.94
CHEMBL5087543 1 6.78
CHEMBL5080654 1 6.73
CHEMBL5077645 1 5.55
CHEMBL5091775 1 -
CHEMBL5091335 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5088070 Ki = 20.3 nM 7.69
CHEMBL5073754 Ki = 23.1 nM 7.64
CHEMBL5085974 Ki = 31.3 nM 7.50
CHEMBL5089655 Ki = 36.3 nM 7.44
CHEMBL5074399 Ki = 44.2 nM 7.36
CHEMBL5075990 Ki = 93.7 nM 7.03
CHEMBL5071238 Ki = 114.0 nM 6.94
CHEMBL5087543 Ki = 167.0 nM 6.78
CHEMBL5080654 Ki = 186.0 nM 6.73
CHEMBL5077645 Ki = 2790.0 nM 5.55
CHEMBL5091775 Ki > 100000.0 nM -
CHEMBL5091335 Ki > 100000.0 nM -