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Assay Detail

CHEMBL5228993

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 D3 receptor expressed in HEK293 cell membranes incubated for 90 mins by microbeta scintillation counting analysis
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

D(3) dopamine receptor (CHEMBL234)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Chiral Cyclic Aliphatic Linkers as Building Blocks for Selective Dopamine D<sub>2</sub> or D<sub>3</sub> Receptor Agonists.
Battiti FO, Zaidi SA, Katritch V, Newman AH, Bonifazi A.
J Med Chem (2021) 64 : 16088 -16105
PubMed 34699207 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 19 7.12 8.73

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4551160 1 8.73
CHEMBL5267958 1 8.24
CHEMBL5288831 1 8.13
CHEMBL5291065 1 8.09
CHEMBL5273118 1 7.71
CHEMBL4744811 1 7.68
CHEMBL5286161 1 7.66
CHEMBL5280481 1 7.65
CHEMBL5274609 1 7.51
CHEMBL5273776 1 7.11
CHEMBL5287555 1 6.97
CHEMBL5286603 1 6.81
CHEMBL4464060 1 6.73
CHEMBL4437740 1 6.55
CHEMBL4764883 1 6.37
CHEMBL5277640 1 6.20
CHEMBL419792 SUMANIROLE 3.0 1 6.11
CHEMBL5280797 1 5.86
CHEMBL5266180 1 5.16

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4551160 Ki = 1.85 nM 8.73
CHEMBL5267958 Ki = 5.72 nM 8.24
CHEMBL5288831 Ki = 7.41 nM 8.13
CHEMBL5291065 Ki = 8.13 nM 8.09
CHEMBL5273118 Ki = 19.5 nM 7.71
CHEMBL4744811 Ki = 21.0 nM 7.68
CHEMBL5286161 Ki = 22.1 nM 7.66
CHEMBL5280481 Ki = 22.6 nM 7.65
CHEMBL5274609 Ki = 31.0 nM 7.51
CHEMBL5273776 Ki = 77.1 nM 7.11
CHEMBL5287555 Ki = 106.0 nM 6.97
CHEMBL5286603 Ki = 154.0 nM 6.81
CHEMBL4464060 Ki = 185.0 nM 6.73
CHEMBL4437740 Ki = 282.0 nM 6.55
CHEMBL4764883 Ki = 423.0 nM 6.37
CHEMBL5277640 Ki = 625.0 nM 6.20
CHEMBL419792 SUMANIROLE Ki = 784.0 nM 6.11
CHEMBL5280797 Ki = 1380.0 nM 5.86
CHEMBL5266180 Ki = 6860.0 nM 5.16