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Assay Detail

CHEMBL676141

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

Binding
In vitro binding affinity against cloned mammalian Dopamine receptor D3 expressed in CHO cells by, using [3H]-spiperone as radioligand
36
Total Activities
36
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(3) dopamine receptor (CHEMBL3138)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Structure-activity relationships in the 8-amino-6,7,8,9-tetrahydro-3H-benz[e]indole ring system. 2. Effects of 8-amino nitrogen substitution on serotonin receptor binding and pharmacology.
Ennis MD, Stjernlöf P, Hoffman RL, Ghazal NB, Smith MW, Svensson K, Wikström H, Haadsma-Svensson SR, Lin CH.
J Med Chem (1995) 38 : 2217 -2230
PubMed 7783153 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 36 7.11 8.26

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL71145 1 8.26
CHEMBL306197 1 8.00
CHEMBL72285 1 7.75
CHEMBL1744041 1 7.75
CHEMBL1788197 1 7.72
CHEMBL420748 1 7.70
CHEMBL302171 1 7.66
CHEMBL69943 1 7.54
CHEMBL302172 1 7.52
CHEMBL65196 1 7.43
CHEMBL70680 1 7.38
CHEMBL70606 1 7.37
CHEMBL72062 1 7.32
CHEMBL69729 1 7.30
CHEMBL71625 1 7.29
CHEMBL304426 1 7.16
CHEMBL309121 1 7.11
CHEMBL304767 1 7.09
CHEMBL305837 1 7.08
CHEMBL1744039 1 7.00
CHEMBL71409 1 6.95
CHEMBL305976 1 6.94
CHEMBL420191 1 6.94
CHEMBL304984 1 6.89
CHEMBL1788198 1 6.81
CHEMBL303921 1 6.80
CHEMBL71640 1 6.79
CHEMBL70980 1 6.70
CHEMBL71469 1 6.59
CHEMBL1744040 1 6.58

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL71145 Ki = 5.5 nM 8.26
CHEMBL306197 Ki = 10.0 nM 8.00
CHEMBL1744041 Ki = 18.0 nM 7.75
CHEMBL72285 Ki = 18.0 nM 7.75
CHEMBL1788197 Ki = 19.0 nM 7.72
CHEMBL420748 Ki = 20.0 nM 7.70
CHEMBL302171 Ki = 22.0 nM 7.66
CHEMBL69943 Ki = 29.0 nM 7.54
CHEMBL302172 Ki = 30.0 nM 7.52
CHEMBL65196 Ki = 37.0 nM 7.43
CHEMBL70680 Ki = 42.0 nM 7.38
CHEMBL70606 Ki = 43.0 nM 7.37
CHEMBL72062 Ki = 48.0 nM 7.32
CHEMBL69729 Ki = 50.0 nM 7.30
CHEMBL71625 Ki = 51.0 nM 7.29
CHEMBL304426 Ki = 70.0 nM 7.16
CHEMBL309121 Ki = 77.0 nM 7.11
CHEMBL304767 Ki = 81.0 nM 7.09
CHEMBL305837 Ki = 84.0 nM 7.08
CHEMBL1744039 Ki = 100.0 nM 7.00
CHEMBL71409 Ki = 113.0 nM 6.95
CHEMBL305976 Ki = 115.0 nM 6.94
CHEMBL420191 Ki = 115.0 nM 6.94
CHEMBL304984 Ki = 130.0 nM 6.89
CHEMBL1788198 Ki = 154.0 nM 6.81
CHEMBL303921 Ki = 159.0 nM 6.80
CHEMBL71640 Ki = 164.0 nM 6.79
CHEMBL70980 Ki = 199.0 nM 6.70
CHEMBL71469 Ki = 258.0 nM 6.59
CHEMBL1744040 Ki = 265.0 nM 6.58
CHEMBL303339 Ki = 270.0 nM 6.57
CHEMBL413105 Ki = 383.0 nM 6.42
CHEMBL423127 Ki = 450.0 nM 6.35
CHEMBL307786 Ki = 751.0 nM 6.12
CHEMBL2112317 Ki = 1270.0 nM 5.90
CHEMBL308934 Ki - nM -