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Assay Detail

CHEMBL671579

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Binding
Binding affinity to rat Dopamine receptor D2 expressed in CHO cells was determined using [125 I ] iodosulpride as radioligand
25
Total Activities
25
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(2) dopamine receptor (CHEMBL339)
Type SINGLE PROTEIN
Organism Rattus norvegicus

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 25 7.27 9.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL20734 NEMONAPRIDE 2.0 1 9.80
CHEMBL319597 1 9.09
CHEMBL329106 1 9.01
CHEMBL54 HALOPERIDOL 4.0 1 8.96
CHEMBL327984 1 8.92
CHEMBL330318 1 7.92
CHEMBL92199 1 7.70
CHEMBL92192 1 7.57
CHEMBL96703 1 7.50
CHEMBL93198 1 7.50
CHEMBL93021 1 7.30
CHEMBL91859 1 7.09
CHEMBL96369 1 7.08
CHEMBL92924 1 6.96
CHEMBL94050 1 6.85
CHEMBL315446 1 6.77
CHEMBL319079 1 6.72
CHEMBL328866 1 6.66
CHEMBL316317 1 6.62
CHEMBL42 CLOZAPINE 4.0 1 6.58
CHEMBL91693 1 6.20
CHEMBL94200 1 6.16
CHEMBL92030 1 6.13
CHEMBL95096 1 5.92
CHEMBL96792 1 4.85

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL20734 NEMONAPRIDE Ki = 0.16 nM 9.80
CHEMBL319597 Ki = 0.81 nM 9.09
CHEMBL329106 Ki = 0.98 nM 9.01
CHEMBL54 HALOPERIDOL Ki = 1.1 nM 8.96
CHEMBL327984 Ki = 1.2 nM 8.92
CHEMBL330318 Ki = 12.0 nM 7.92
CHEMBL92199 Ki = 20.0 nM 7.70
CHEMBL92192 Ki = 27.0 nM 7.57
CHEMBL96703 Ki = 32.0 nM 7.50
CHEMBL93198 Ki = 32.0 nM 7.50
CHEMBL93021 Ki = 50.0 nM 7.30
CHEMBL91859 Ki = 82.0 nM 7.09
CHEMBL96369 Ki = 84.0 nM 7.08
CHEMBL92924 Ki = 110.0 nM 6.96
CHEMBL94050 Ki = 140.0 nM 6.85
CHEMBL315446 Ki = 170.0 nM 6.77
CHEMBL319079 Ki = 190.0 nM 6.72
CHEMBL328866 Ki = 220.0 nM 6.66
CHEMBL316317 Ki = 240.0 nM 6.62
CHEMBL42 CLOZAPINE Ki = 260.0 nM 6.58
CHEMBL91693 Ki = 630.0 nM 6.20
CHEMBL94200 Ki = 690.0 nM 6.16
CHEMBL92030 Ki = 740.0 nM 6.13
CHEMBL95096 Ki = 1200.0 nM 5.92
CHEMBL96792 Ki = 14000.0 nM 4.85