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Assay Detail

CHEMBL4350892

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

Binding
Displacement of 2,3-dimethoxy-5-[125I]-iodo-N-[9-benzyl-9-azabicyclo[3.3.1]nonan-3beta-yl]benzamide from human dopamine D3 receptor expressed in HEK293 cells measured after 60 mins by gamma counting analysis
25
Total Activities
25
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(3) dopamine receptor (CHEMBL234)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design, synthesis, and evaluation of N-(4-(4-phenyl piperazin-1-yl)butyl)-4-(thiophen-3-yl)benzamides as selective dopamine D<sub>3</sub> receptor ligands.
Chen PJ, Taylor M, Griffin SA, Amani A, Hayatshahi H, Korzekwa K, Ye M, Mach RH, Liu J, Luedtke RR, Gordon JC, Blass BE.
Bioorg Med Chem Lett (2019) 29 : 2690 -2694
PubMed 31387791 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 25 8.30 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4567895 1 9.70
CHEMBL4571568 1 9.60
CHEMBL4590192 1 9.39
CHEMBL4583609 1 9.36
CHEMBL4579251 1 9.33
CHEMBL4437341 1 9.30
CHEMBL4450777 1 9.26
CHEMBL4587635 1 9.17
CHEMBL4535174 1 9.05
CHEMBL4476605 1 8.82
CHEMBL4438037 1 8.42
CHEMBL4586531 1 8.10
CHEMBL4446350 1 8.08
CHEMBL4565997 1 7.87
CHEMBL4459381 1 7.78
CHEMBL4570430 1 7.75
CHEMBL4577206 1 7.70
CHEMBL4438630 1 7.66
CHEMBL4438361 1 7.65
CHEMBL1739963 1 7.56
CHEMBL4442321 1 7.49
CHEMBL4545775 1 7.44
CHEMBL4521525 1 7.11
CHEMBL4438602 1 5.62
CHEMBL4462851 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4567895 Ki = 0.2 nM 9.70
CHEMBL4571568 Ki = 0.25 nM 9.60
CHEMBL4590192 Ki = 0.41 nM 9.39
CHEMBL4583609 Ki = 0.44 nM 9.36
CHEMBL4579251 Ki = 0.47 nM 9.33
CHEMBL4437341 Ki = 0.5 nM 9.30
CHEMBL4450777 Ki = 0.55 nM 9.26
CHEMBL4587635 Ki = 0.68 nM 9.17
CHEMBL4535174 Ki = 0.89 nM 9.05
CHEMBL4476605 Ki = 1.5 nM 8.82
CHEMBL4438037 Ki = 3.8 nM 8.42
CHEMBL4586531 Ki = 8.0 nM 8.10
CHEMBL4446350 Ki = 8.3 nM 8.08
CHEMBL4565997 Ki = 13.6 nM 7.87
CHEMBL4459381 Ki = 16.7 nM 7.78
CHEMBL4570430 Ki = 18.0 nM 7.75
CHEMBL4577206 Ki = 19.8 nM 7.70
CHEMBL4438630 Ki = 21.9 nM 7.66
CHEMBL4438361 Ki = 22.3 nM 7.65
CHEMBL1739963 Ki = 27.7 nM 7.56
CHEMBL4442321 Ki = 32.7 nM 7.49
CHEMBL4545775 Ki = 36.1 nM 7.44
CHEMBL4521525 Ki = 78.3 nM 7.11
CHEMBL4438602 Ki = 2378.0 nM 5.62
CHEMBL4462851 Ki > 30000.0 nM -