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Assay Detail

CHEMBL674047

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

Binding
Displacement of [3H]-YM 09151 from D4 receptor
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

Design, synthesis, and discovery of 5-piperazinyl-1,2,6,7-tetrahydro-5H-azepino[3,2,1-hi]indol-4-one derivatives: a novel series of mixed dopamine D2/D4 receptor antagonist.
Zhao H, Zhang X, Hodgetts K, Thurkauf A, Hammer J, Chandrasekhar J, Kieltyka A, Brodbeck R, Rachwal S, Primus R, Manly C.
Bioorg Med Chem Lett (2003) 13 : 701 -704
PubMed 12639562 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 13 7.80 8.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL69584 1 8.80
CHEMBL351963 1 8.40
CHEMBL68191 1 8.40
CHEMBL352207 1 8.30
CHEMBL349833 1 8.05
CHEMBL345438 1 8.00
CHEMBL351989 1 7.92
CHEMBL42 CLOZAPINE 4.0 1 7.77
CHEMBL439646 1 7.72
CHEMBL354699 1 7.54
CHEMBL159742 1 7.47
CHEMBL351612 1 7.19
CHEMBL67414 1 5.82

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL69584 Ki = 1.6 nM 8.80
CHEMBL351963 Ki = 4.0 nM 8.40
CHEMBL68191 Ki = 4.0 nM 8.40
CHEMBL352207 Ki = 5.0 nM 8.30
CHEMBL349833 Ki = 9.0 nM 8.05
CHEMBL345438 Ki = 10.0 nM 8.00
CHEMBL351989 Ki = 12.0 nM 7.92
CHEMBL42 CLOZAPINE Ki = 17.0 nM 7.77
CHEMBL439646 Ki = 19.0 nM 7.72
CHEMBL354699 Ki = 29.0 nM 7.54
CHEMBL159742 Ki = 34.0 nM 7.47
CHEMBL351612 Ki = 65.0 nM 7.19
CHEMBL67414 Ki = 1511.0 nM 5.82