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Assay Detail

CHEMBL672800

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

Binding
Binding affinity at Dopamine D2 receptors in rat striatum by [3H]spiperone displacement.
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Striatum
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

4-bromo-1-methoxy-N-[2-(4-aryl-1-piperazinyl)ethyl]-2-naphthalenecarboxamides: Selective dopamine D3 receptor partial agonists
Glase SA, Akunne HC, Heffner TG, Johnson SJ, Kesten SR, MacKenzie RG, Manley PJ, Pugsley TA, Wright JL, Wise LD
Bioorg Med Chem Lett (1996) 6 : 1361 -1366
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 19 5.99 7.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL282083 1 7.15
CHEMBL29436 1 6.82
CHEMBL30146 1 6.52
CHEMBL28964 1 6.32
CHEMBL30206 1 6.29
CHEMBL442535 1 6.15
CHEMBL29610 1 6.00
CHEMBL29182 1 5.93
CHEMBL283034 1 5.92
CHEMBL29849 1 5.89
CHEMBL29435 1 5.89
CHEMBL30208 1 5.72
CHEMBL416939 1 5.60
CHEMBL29336 1 5.25
CHEMBL287443 1 5.25
CHEMBL284896 1 5.16
CHEMBL29529 1 -
CHEMBL30256 1 -
CHEMBL29649 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL282083 Ki = 71.0 nM 7.15
CHEMBL29436 Ki = 151.0 nM 6.82
CHEMBL30146 Ki = 303.0 nM 6.52
CHEMBL28964 Ki = 484.0 nM 6.32
CHEMBL30206 Ki = 517.0 nM 6.29
CHEMBL442535 Ki = 703.0 nM 6.15
CHEMBL29610 Ki = 996.0 nM 6.00
CHEMBL29182 Ki = 1173.0 nM 5.93
CHEMBL283034 Ki = 1207.0 nM 5.92
CHEMBL29849 Ki = 1288.0 nM 5.89
CHEMBL29435 Ki = 1288.0 nM 5.89
CHEMBL30208 Ki = 1892.0 nM 5.72
CHEMBL416939 Ki = 2529.0 nM 5.60
CHEMBL29336 Ki = 5692.0 nM 5.25
CHEMBL287443 Ki = 5692.0 nM 5.25
CHEMBL284896 Ki = 7000.0 nM 5.16
CHEMBL29529 Ki > 10000.0 nM -
CHEMBL30256 Ki > 10000.0 nM -
CHEMBL29649 Ki > 10000.0 nM -