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Assay Detail

CHEMBL678345

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

Binding
Affinity against striatal dopamine D2 receptors using [3H]spiperone as radioligand in rats.
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

D(2) dopamine receptor (CHEMBL339)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Substituted (S)-phenylpiperidines and rigid congeners as preferential dopamine autoreceptor antagonists: synthesis and structure-activity relationships.
Sonesson C, Lin CH, Hansson L, Waters N, Svensson K, Carlsson A, Smith MW, Wikström H.
J Med Chem (1994) 37 : 2735 -2753
PubMed 8064801 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 28 5.92 7.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL94811 1 7.10
CHEMBL7549 PRECLAMOL 2.0 1 7.00
CHEMBL93570 1 6.99
CHEMBL93646 1 6.98
CHEMBL93101 1 6.39
CHEMBL96191 1 6.21
CHEMBL93383 1 6.14
CHEMBL314536 1 6.12
CHEMBL413483 1 5.98
CHEMBL92183 1 5.94
CHEMBL93917 1 5.91
CHEMBL93946 1 5.78
CHEMBL93212 1 5.72
CHEMBL93679 1 5.70
CHEMBL93900 1 5.66
CHEMBL90798 1 5.63
CHEMBL93682 1 5.57
CHEMBL328894 1 5.51
CHEMBL329443 1 5.47
CHEMBL93582 1 5.46
CHEMBL93594 1 5.38
CHEMBL311730 1 5.20
CHEMBL90797 1 5.18
CHEMBL90662 1 5.08
CHEMBL92939 1 -
CHEMBL92232 1 -
CHEMBL91228 1 -
CHEMBL96726 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL94811 Ki = 80.0 nM 7.10
CHEMBL7549 PRECLAMOL Ki = 100.0 nM 7.00
CHEMBL93570 Ki = 102.0 nM 6.99
CHEMBL93646 Ki = 105.0 nM 6.98
CHEMBL93101 Ki = 410.0 nM 6.39
CHEMBL96191 Ki = 617.0 nM 6.21
CHEMBL93383 Ki = 717.0 nM 6.14
CHEMBL314536 Ki = 760.0 nM 6.12
CHEMBL413483 Ki = 1050.0 nM 5.98
CHEMBL92183 Ki = 1140.0 nM 5.94
CHEMBL93917 Ki = 1229.0 nM 5.91
CHEMBL93946 Ki = 1670.0 nM 5.78
CHEMBL93212 Ki = 1890.0 nM 5.72
CHEMBL93679 Ki = 2000.0 nM 5.70
CHEMBL93900 Ki = 2170.0 nM 5.66
CHEMBL90798 Ki = 2330.0 nM 5.63
CHEMBL93682 Ki = 2670.0 nM 5.57
CHEMBL328894 Ki = 3100.0 nM 5.51
CHEMBL329443 Ki = 3390.0 nM 5.47
CHEMBL93582 Ki = 3440.0 nM 5.46
CHEMBL93594 Ki = 4170.0 nM 5.38
CHEMBL311730 Ki = 6270.0 nM 5.20
CHEMBL90797 Ki = 6540.0 nM 5.18
CHEMBL90662 Ki = 8330.0 nM 5.08
CHEMBL92939 Ki > 172.0 nM -
CHEMBL92232 Ki > 15000.0 nM -
CHEMBL91228 Ki > 15000.0 nM -
CHEMBL96726 Ki > 172.0 nM -