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Assay Detail

CHEMBL673581

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

Binding
In vitro binding affinity against cloned mammalian Dopamine receptor D2 expressed in CHO cells using [3H]U-86170 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

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 25 7.34 8.26

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL72285 1 8.26
CHEMBL1744041 1 8.24
CHEMBL1788197 1 8.24
CHEMBL1744040 1 7.89
CHEMBL70680 1 7.89
CHEMBL305837 1 7.85
CHEMBL71625 1 7.77
CHEMBL72062 1 7.60
CHEMBL303921 1 7.55
CHEMBL1744039 1 7.55
CHEMBL304426 1 7.40
CHEMBL304984 1 7.23
CHEMBL312525 1 7.22
CHEMBL304767 1 7.21
CHEMBL1788198 1 7.21
CHEMBL420191 1 7.05
CHEMBL423127 1 6.87
CHEMBL71469 1 6.82
CHEMBL71640 1 6.64
CHEMBL1788196 1 6.60
CHEMBL307786 1 6.37
CHEMBL2112317 1 6.07
CHEMBL308934 1 -
CHEMBL70970 1 -
CHEMBL306198 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL72285 Ki = 5.5 nM 8.26
CHEMBL1744041 Ki = 5.7 nM 8.24
CHEMBL1788197 Ki = 5.8 nM 8.24
CHEMBL1744040 Ki = 13.0 nM 7.89
CHEMBL70680 Ki = 13.0 nM 7.89
CHEMBL305837 Ki = 14.0 nM 7.85
CHEMBL71625 Ki = 17.0 nM 7.77
CHEMBL72062 Ki = 25.0 nM 7.60
CHEMBL303921 Ki = 28.0 nM 7.55
CHEMBL1744039 Ki = 28.0 nM 7.55
CHEMBL304426 Ki = 40.0 nM 7.40
CHEMBL304984 Ki = 59.0 nM 7.23
CHEMBL312525 Ki = 60.0 nM 7.22
CHEMBL304767 Ki = 62.0 nM 7.21
CHEMBL1788198 Ki = 62.0 nM 7.21
CHEMBL420191 Ki = 90.0 nM 7.05
CHEMBL423127 Ki = 136.0 nM 6.87
CHEMBL71469 Ki = 151.0 nM 6.82
CHEMBL71640 Ki = 228.0 nM 6.64
CHEMBL1788196 Ki = 250.0 nM 6.60
CHEMBL307786 Ki = 423.0 nM 6.37
CHEMBL2112317 Ki = 859.0 nM 6.07
CHEMBL308934 Ki > 1000.0 nM -
CHEMBL70970 Ki - nM -
CHEMBL306198 Ki > 1000.0 nM -