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Assay Detail

CHEMBL675946

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

Binding
Binding affinity towards human dopamine receptor D4
21
Total Activities
21
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

Current and novel approaches to the drug treatment of schizophrenia.
Rowley M, Bristow LJ, Hutson PH.
J Med Chem (2001) 44 : 477 -501
PubMed 11170639 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 21 7.89 9.37

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL267014 L-745870 1 9.37
CHEMBL357182 1 8.72
CHEMBL83894 FANANSERIN 2.0 1 8.54
CHEMBL51 KETANSERIN 3.0 1 8.46
CHEMBL444309 1 8.46
CHEMBL103772 1 8.44
CHEMBL422314 1 8.37
CHEMBL6416 1 8.26
CHEMBL148561 1 8.24
CHEMBL69759 SONEPIPRAZOLE 2.0 1 8.17
CHEMBL37170 1 8.11
CHEMBL59324 1 8.10
CHEMBL85 RISPERIDONE 4.0 1 7.80
CHEMBL59103 1 7.60
CHEMBL715 OLANZAPINE 4.0 1 7.55
CHEMBL708 ZIPRASIDONE 4.0 1 7.41
CHEMBL285802 ZOTEPINE 2.0 1 7.41
CHEMBL42 CLOZAPINE 4.0 1 7.40
CHEMBL61080 1 7.21
CHEMBL57478 1 6.24
CHEMBL716 QUETIAPINE 4.0 1 5.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL267014 L-745870 Ki = 0.43 nM 9.37
CHEMBL357182 Ki = 1.9 nM 8.72
CHEMBL83894 FANANSERIN Ki = 2.9 nM 8.54
CHEMBL51 KETANSERIN Ki = 3.5 nM 8.46
CHEMBL444309 Ki = 3.5 nM 8.46
CHEMBL103772 Ki = 3.6 nM 8.44
CHEMBL422314 Ki = 4.3 nM 8.37
CHEMBL6416 Ki = 5.5 nM 8.26
CHEMBL148561 Ki = 5.8 nM 8.24
CHEMBL69759 SONEPIPRAZOLE Ki = 6.8 nM 8.17
CHEMBL37170 Ki = 7.8 nM 8.11
CHEMBL59324 Ki = 8.0 nM 8.10
CHEMBL85 RISPERIDONE Ki = 16.0 nM 7.80
CHEMBL59103 Ki = 25.0 nM 7.60
CHEMBL715 OLANZAPINE Ki = 28.0 nM 7.55
CHEMBL708 ZIPRASIDONE Ki = 39.0 nM 7.41
CHEMBL285802 ZOTEPINE Ki = 39.0 nM 7.41
CHEMBL42 CLOZAPINE Ki = 40.0 nM 7.40
CHEMBL61080 Ki = 61.0 nM 7.21
CHEMBL57478 Ki = 570.0 nM 6.24
CHEMBL716 QUETIAPINE Ki = 1600.0 nM 5.80