Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL677456

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

Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
49
Total Activities
49
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

D(4) dopamine receptor (CHEMBL219)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Indoline and piperazine containing derivatives as a novel class of mixed D(2)/D(4) receptor antagonists. Part 1: identification and structure-activity relationships.
Zhao H, Thurkauf A, He X, Hodgetts K, Zhang X, Rachwal S, Kover RX, Hutchison A, Peterson J, Kieltyka A, Brodbeck R, Primus R, Wasley JW.
Bioorg Med Chem Lett (2002) 12 : 3105 -3109
PubMed 12372512 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 49 7.58 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL104716 1 8.70
CHEMBL104497 1 8.70
CHEMBL107742 1 8.52
CHEMBL108157 1 8.52
CHEMBL104273 1 8.52
CHEMBL104832 1 8.40
CHEMBL104788 1 8.40
CHEMBL106208 1 8.30
CHEMBL105011 1 8.30
CHEMBL419908 1 8.22
CHEMBL419356 1 8.22
CHEMBL321538 1 8.22
CHEMBL104719 1 8.15
CHEMBL104614 1 8.15
CHEMBL104800 1 8.15
CHEMBL104256 1 8.15
CHEMBL322326 1 8.10
CHEMBL105304 1 8.10
CHEMBL104579 1 8.00
CHEMBL104321 1 7.96
CHEMBL419916 1 7.92
CHEMBL320440 1 7.92
CHEMBL107804 1 7.92
CHEMBL104380 1 7.89
CHEMBL104238 1 7.85
CHEMBL104399 1 7.85
CHEMBL107020 1 7.82
CHEMBL323525 1 7.82
CHEMBL326202 1 7.68
CHEMBL321734 1 7.60

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL104716 Ki = 2.0 nM 8.70
CHEMBL104497 Ki = 2.0 nM 8.70
CHEMBL108157 Ki = 3.0 nM 8.52
CHEMBL104273 Ki = 3.0 nM 8.52
CHEMBL107742 Ki = 3.0 nM 8.52
CHEMBL104832 Ki = 4.0 nM 8.40
CHEMBL104788 Ki = 4.0 nM 8.40
CHEMBL106208 Ki = 5.0 nM 8.30
CHEMBL105011 Ki = 5.0 nM 8.30
CHEMBL419908 Ki = 6.0 nM 8.22
CHEMBL419356 Ki = 6.0 nM 8.22
CHEMBL321538 Ki = 6.0 nM 8.22
CHEMBL104800 Ki = 7.0 nM 8.15
CHEMBL104719 Ki = 7.0 nM 8.15
CHEMBL104614 Ki = 7.0 nM 8.15
CHEMBL104256 Ki = 7.0 nM 8.15
CHEMBL322326 Ki = 8.0 nM 8.10
CHEMBL105304 Ki = 8.0 nM 8.10
CHEMBL104579 Ki = 10.0 nM 8.00
CHEMBL104321 Ki = 11.0 nM 7.96
CHEMBL419916 Ki = 12.0 nM 7.92
CHEMBL320440 Ki = 12.0 nM 7.92
CHEMBL107804 Ki = 12.0 nM 7.92
CHEMBL104380 Ki = 13.0 nM 7.89
CHEMBL104238 Ki = 14.2 nM 7.85
CHEMBL104399 Ki = 14.0 nM 7.85
CHEMBL107020 Ki = 15.0 nM 7.82
CHEMBL323525 Ki = 15.0 nM 7.82
CHEMBL326202 Ki = 21.0 nM 7.68
CHEMBL321734 Ki = 25.0 nM 7.60
CHEMBL106914 Ki = 29.0 nM 7.54
CHEMBL104155 Ki = 40.0 nM 7.40
CHEMBL106007 Ki = 59.0 nM 7.23
CHEMBL106751 Ki = 67.0 nM 7.17
CHEMBL104063 Ki = 73.0 nM 7.14
CHEMBL323022 Ki = 134.0 nM 6.87
CHEMBL322567 Ki = 259.0 nM 6.59
CHEMBL324867 Ki = 281.0 nM 6.55
CHEMBL107351 Ki = 335.0 nM 6.47
CHEMBL108261 Ki = 522.0 nM 6.28
CHEMBL104498 Ki = 726.0 nM 6.14
CHEMBL104138 Ki = 1361.0 nM 5.87
CHEMBL104514 Ki = 3854.0 nM 5.41
CHEMBL431437 Ki = 5745.0 nM 5.24
CHEMBL106170 Ki = 7264.0 nM 5.14
CHEMBL104756 Ki > 10000.0 nM -
CHEMBL419911 Ki > 1000.0 nM -
CHEMBL104299 Ki > 1000.0 nM -
CHEMBL42 CLOZAPINE Ki = 9.0 nM -