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Assay Detail

CHEMBL678343

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

Binding
Affinity against recombinant dopamine receptor (DA) D2 expressed in CHO-K1 cells, using [3H]-spiperone as radioligand
48
Total Activities
47
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type CHO-K1
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

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 48 7.02 7.41

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL7549 PRECLAMOL 2.0 1 7.41
CHEMBL90359 1 7.32
CHEMBL94811 1 7.22
CHEMBL328119 1 7.14
CHEMBL329443 1 7.04
CHEMBL413483 1 7.01
CHEMBL93570 1 6.87
CHEMBL92578 1 6.84
CHEMBL92817 1 6.77
CHEMBL92183 1 6.58
CHEMBL93646 1 -
CHEMBL93283 1 -
CHEMBL94224 1 -
CHEMBL92232 1 -
CHEMBL93946 1 -
CHEMBL90797 1 -
CHEMBL93701 1 -
CHEMBL315890 1 -
CHEMBL93254 1 -
CHEMBL311730 1 -
CHEMBL327263 1 -
CHEMBL93594 1 -
CHEMBL329139 1 -
CHEMBL90662 1 -
CHEMBL328431 1 -
CHEMBL93212 1 -
CHEMBL93682 1 -
CHEMBL92630 1 -
CHEMBL2111566 2 -
CHEMBL93582 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL7549 PRECLAMOL Ki = 39.0 nM 7.41
CHEMBL90359 Ki = 48.0 nM 7.32
CHEMBL94811 Ki = 60.0 nM 7.22
CHEMBL328119 Ki = 73.0 nM 7.14
CHEMBL329443 Ki = 91.0 nM 7.04
CHEMBL413483 Ki = 98.0 nM 7.01
CHEMBL93570 Ki = 134.0 nM 6.87
CHEMBL92578 Ki = 145.0 nM 6.84
CHEMBL92817 Ki = 170.0 nM 6.77
CHEMBL92183 Ki = 265.0 nM 6.58
CHEMBL93900 Ki > 217.0 nM -
CHEMBL90798 Ki > 217.0 nM -
CHEMBL93917 Ki > 217.0 nM -
CHEMBL93679 Ki > 217.0 nM -
CHEMBL96726 Ki > 217.0 nM -
CHEMBL328894 Ki > 217.0 nM -
CHEMBL93534 Ki > 217.0 nM -
CHEMBL311730 Ki > 217.0 nM -
CHEMBL93234 Ki > 217.0 nM -
CHEMBL93254 Ki > 217.0 nM -
CHEMBL93101 Ki > 217.0 nM -
CHEMBL328785 Ki > 217.0 nM -
CHEMBL92938 Ki > 217.0 nM -
CHEMBL96191 Ki > 217.0 nM -
CHEMBL93383 Ki > 217.0 nM -
CHEMBL314536 Ki > 217.0 nM -
CHEMBL91228 Ki > 217.0 nM -
CHEMBL328448 Ki > 217.0 nM -
CHEMBL92682 Ki > 217.0 nM -
CHEMBL93646 Ki > 217.0 nM -
CHEMBL93682 Ki > 217.0 nM -
CHEMBL93212 Ki > 217.0 nM -
CHEMBL328431 Ki > 217.0 nM -
CHEMBL90662 Ki > 217.0 nM -
CHEMBL329139 Ki > 217.0 nM -
CHEMBL94224 Ki > 217.0 nM -
CHEMBL93594 Ki > 217.0 nM -
CHEMBL93582 Ki > 217.0 nM -
CHEMBL327263 Ki > 217.0 nM -
CHEMBL315890 Ki > 217.0 nM -
CHEMBL92232 Ki > 217.0 nM -
CHEMBL93946 Ki > 217.0 nM -
CHEMBL90797 Ki > 217.0 nM -
CHEMBL93701 Ki > 217.0 nM -
CHEMBL2111566 Ki > 217.0 nM -
CHEMBL2111566 Ki > 217.0 nM -
CHEMBL93283 Ki > 217.0 nM -
CHEMBL92630 Ki > 217.0 nM -