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Assay Detail

CHEMBL671697

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Binding
Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Dopamine D3 and D4 receptor antagonists: synthesis and structure--activity relationships of (S)-(+)-N-(1-Benzyl-3-pyrrolidinyl)-5-chloro-4- [(cyclopropylcarbonyl) amino]-2-methoxybenzamide (YM-43611) and related compounds.
Ohmori J, Maeno K, Hidaka K, Nakato K, Matsumoto M, Tada S, Hattori H, Sakamoto S, Tsukamoto S, Usuda S, Mase T.
J Med Chem (1996) 39 : 2764 -2772
PubMed 8709107 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 24 8.25 9.26

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL327984 1 9.26
CHEMBL319597 1 9.17
CHEMBL329106 1 8.96
CHEMBL92192 1 8.89
CHEMBL93198 1 8.82
CHEMBL330318 1 8.72
CHEMBL96369 1 8.68
CHEMBL328866 1 8.68
CHEMBL54 HALOPERIDOL 4.0 1 8.68
CHEMBL92199 1 8.57
CHEMBL93021 1 8.52
CHEMBL96703 1 8.48
CHEMBL91859 1 8.47
CHEMBL94050 1 8.42
CHEMBL92924 1 8.36
CHEMBL315446 1 8.28
CHEMBL319079 1 8.25
CHEMBL316317 1 8.15
CHEMBL94200 1 7.75
CHEMBL92030 1 7.70
CHEMBL42 CLOZAPINE 4.0 1 7.41
CHEMBL91693 1 7.06
CHEMBL95096 1 6.96
CHEMBL96792 1 5.66

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL327984 Ki = 0.55 nM 9.26
CHEMBL319597 Ki = 0.67 nM 9.17
CHEMBL329106 Ki = 1.1 nM 8.96
CHEMBL92192 Ki = 1.3 nM 8.89
CHEMBL93198 Ki = 1.5 nM 8.82
CHEMBL330318 Ki = 1.9 nM 8.72
CHEMBL96369 Ki = 2.1 nM 8.68
CHEMBL328866 Ki = 2.1 nM 8.68
CHEMBL54 HALOPERIDOL Ki = 2.1 nM 8.68
CHEMBL92199 Ki = 2.7 nM 8.57
CHEMBL93021 Ki = 3.0 nM 8.52
CHEMBL96703 Ki = 3.3 nM 8.48
CHEMBL91859 Ki = 3.4 nM 8.47
CHEMBL94050 Ki = 3.8 nM 8.42
CHEMBL92924 Ki = 4.4 nM 8.36
CHEMBL315446 Ki = 5.2 nM 8.28
CHEMBL319079 Ki = 5.6 nM 8.25
CHEMBL316317 Ki = 7.0 nM 8.15
CHEMBL94200 Ki = 18.0 nM 7.75
CHEMBL92030 Ki = 20.0 nM 7.70
CHEMBL42 CLOZAPINE Ki = 39.0 nM 7.41
CHEMBL91693 Ki = 87.0 nM 7.06
CHEMBL95096 Ki = 110.0 nM 6.96
CHEMBL96792 Ki = 2200.0 nM 5.66