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Assay Detail

CHEMBL678864

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

Binding
Ability to displace [3H]spiperone from human dopamine receptor D3 (hD3) receptor stably expressed in HEK293 cells.
37
Total Activities
37
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type HEK293
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

4-Heterocyclylpiperidines as selective high-affinity ligands at the human dopamine D4 receptor.
Rowley M, Collins I, Broughton HB, Davey WB, Baker R, Emms F, Marwood R, Patel S, Patel S, Ragan CI, Freedman SB, Ball R, Leeson PD.
J Med Chem (1997) 40 : 2374 -2385
PubMed 9240352 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 37 6.23 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL54 HALOPERIDOL 4.0 1 8.70
CHEMBL78933 1 7.34
CHEMBL61195 1 7.10
CHEMBL78923 1 6.85
CHEMBL76090 1 6.80
CHEMBL42 CLOZAPINE 4.0 1 6.70
CHEMBL80833 1 6.62
CHEMBL309901 1 6.37
CHEMBL58296 1 6.37
CHEMBL293341 1 6.32
CHEMBL2112285 1 6.29
CHEMBL2112284 1 6.29
CHEMBL311832 1 6.22
CHEMBL420954 1 6.14
CHEMBL444309 1 6.11
CHEMBL61080 1 6.09
CHEMBL80318 1 6.08
CHEMBL77017 1 6.06
CHEMBL76355 1 6.04
CHEMBL80722 1 5.96
CHEMBL77743 1 5.96
CHEMBL61079 1 5.92
CHEMBL77744 1 5.92
CHEMBL310985 1 5.92
CHEMBL312255 1 5.89
CHEMBL80207 1 5.89
CHEMBL25938 1 5.85
CHEMBL80863 1 5.75
CHEMBL77148 1 5.68
CHEMBL77015 1 5.47

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL54 HALOPERIDOL Ki = 2.0 nM 8.70
CHEMBL78933 Ki = 46.0 nM 7.34
CHEMBL61195 Ki = 80.0 nM 7.10
CHEMBL78923 Ki = 140.0 nM 6.85
CHEMBL76090 Ki = 160.0 nM 6.80
CHEMBL42 CLOZAPINE Ki = 200.0 nM 6.70
CHEMBL80833 Ki = 240.0 nM 6.62
CHEMBL309901 Ki = 430.0 nM 6.37
CHEMBL58296 Ki = 430.0 nM 6.37
CHEMBL293341 Ki = 480.0 nM 6.32
CHEMBL2112285 Ki = 510.0 nM 6.29
CHEMBL2112284 Ki = 510.0 nM 6.29
CHEMBL311832 Ki = 600.0 nM 6.22
CHEMBL420954 Ki = 720.0 nM 6.14
CHEMBL444309 Ki = 770.0 nM 6.11
CHEMBL61080 Ki = 820.0 nM 6.09
CHEMBL80318 Ki = 830.0 nM 6.08
CHEMBL77017 Ki = 870.0 nM 6.06
CHEMBL76355 Ki = 920.0 nM 6.04
CHEMBL77743 Ki = 1100.0 nM 5.96
CHEMBL80722 Ki = 1100.0 nM 5.96
CHEMBL61079 Ki = 1200.0 nM 5.92
CHEMBL77744 Ki = 1200.0 nM 5.92
CHEMBL310985 Ki = 1200.0 nM 5.92
CHEMBL312255 Ki = 1300.0 nM 5.89
CHEMBL80207 Ki = 1300.0 nM 5.89
CHEMBL25938 Ki = 1400.0 nM 5.85
CHEMBL80863 Ki = 1800.0 nM 5.75
CHEMBL77148 Ki = 2100.0 nM 5.68
CHEMBL77015 Ki = 3400.0 nM 5.47
CHEMBL310819 Ki = 3600.0 nM 5.44
CHEMBL78287 Ki = 4300.0 nM 5.37
CHEMBL80552 Ki > 1900.0 nM -
CHEMBL79098 Ki > 4000.0 nM -
CHEMBL75691 Ki > 4400.0 nM -
CHEMBL6416 Ki > 4000.0 nM -
CHEMBL309460 Ki > 4200.0 nM -