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Assay Detail

CHEMBL675855

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

Binding
Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.
19
Total Activities
19
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

Design, synthesis, and discovery of 3-piperazinyl-3,4-dihydro-2(1H)-quinolinone derivatives: a novel series of mixed dopamine D2/D4 receptor antagonists.
Zhao H, Thurkauf A, Braun J, Brodbeck R, Kieltyka A.
Bioorg Med Chem Lett (2000) 10 : 2119 -2122
PubMed 10999484 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 19 6.95 8.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL69584 1 8.80
CHEMBL305276 1 8.40
CHEMBL68191 1 8.40
CHEMBL302075 1 8.30
CHEMBL42 CLOZAPINE 4.0 1 7.77
CHEMBL303692 1 7.23
CHEMBL67222 1 7.00
CHEMBL67414 1 5.82
CHEMBL63209 1 5.61
CHEMBL302340 1 5.53
CHEMBL305061 1 5.36
CHEMBL304584 1 5.15
CHEMBL67429 1 -
CHEMBL305453 1 -
CHEMBL68190 1 -
CHEMBL67042 1 -
CHEMBL303406 1 -
CHEMBL304777 1 -
CHEMBL66957 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL69584 Ki = 1.6 nM 8.80
CHEMBL305276 Ki = 4.0 nM 8.40
CHEMBL68191 Ki = 4.0 nM 8.40
CHEMBL302075 Ki = 5.0 nM 8.30
CHEMBL42 CLOZAPINE Ki = 17.0 nM 7.77
CHEMBL303692 Ki = 59.0 nM 7.23
CHEMBL67222 Ki = 100.0 nM 7.00
CHEMBL67414 Ki = 1511.0 nM 5.82
CHEMBL63209 Ki = 2469.0 nM 5.61
CHEMBL302340 Ki = 2960.0 nM 5.53
CHEMBL305061 Ki = 4377.0 nM 5.36
CHEMBL304584 Ki = 7018.0 nM 5.15
CHEMBL67429 Ki > 1000.0 nM -
CHEMBL305453 Ki > 1000.0 nM -
CHEMBL68190 Ki > 1000.0 nM -
CHEMBL67042 Ki > 1000.0 nM -
CHEMBL303406 Ki > 1000.0 nM -
CHEMBL304777 Ki > 1000.0 nM -
CHEMBL66957 Ki > 1000.0 nM -