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Assay Detail

CHEMBL671710

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

Binding
Dopamine receptor binding affinity by displacing the radioligand [3H]-dopamine from dopamine receptor.
29
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Bos taurus
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Structure-activity relationships of dopaminergic 5-hydroxy-2-aminotetralin derivatives with functionalized N-alkyl substituents.
Seiler MP, Stoll AP, Closse A, Frick W, Jaton A, Vigouret JM.
J Med Chem (1986) 29 : 912 -917
PubMed 3712381 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 29 7.03 7.75

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL531 PERGOLIDE 4.0 1 7.75
CHEMBL171440 3 7.46
CHEMBL355421 2 7.42
CHEMBL170661 1 7.42
CHEMBL109684 1 7.40
CHEMBL170825 1 7.39
CHEMBL367201 1 7.34
CHEMBL173352 1 7.32
CHEMBL172945 1 7.32
CHEMBL273273 5-OH-DPAT 1 7.31
CHEMBL174184 1 7.24
CHEMBL171330 1 7.17
CHEMBL173913 1 7.11
CHEMBL366718 1 7.04
CHEMBL170018 1 7.00
CHEMBL262538 1 6.96
CHEMBL38992 ETISULERGINE 2.0 1 6.92
CHEMBL174247 1 6.89
CHEMBL173926 1 6.85
CHEMBL422745 1 6.82
CHEMBL171126 1 6.73
CHEMBL171080 1 6.72
CHEMBL171187 1 6.66
CHEMBL174095 DELERGOTRILE 2.0 1 6.58
CHEMBL171688 1 6.30
CHEMBL171888 1 5.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL531 PERGOLIDE IC50 = 18.0 nM 7.75
CHEMBL171440 IC50 = 35.0 nM 7.46
CHEMBL171440 IC50 = 37.0 nM 7.43
CHEMBL355421 IC50 = 38.0 nM 7.42
CHEMBL170661 IC50 = 38.0 nM 7.42
CHEMBL109684 IC50 = 40.0 nM 7.40
CHEMBL170825 IC50 = 41.0 nM 7.39
CHEMBL355421 IC50 = 43.0 nM 7.37
CHEMBL367201 IC50 = 46.0 nM 7.34
CHEMBL173352 IC50 = 48.0 nM 7.32
CHEMBL172945 IC50 = 48.0 nM 7.32
CHEMBL273273 5-OH-DPAT IC50 = 49.0 nM 7.31
CHEMBL174184 IC50 = 58.0 nM 7.24
CHEMBL171330 IC50 = 68.0 nM 7.17
CHEMBL173913 IC50 = 77.0 nM 7.11
CHEMBL366718 IC50 = 91.0 nM 7.04
CHEMBL170018 IC50 = 100.0 nM 7.00
CHEMBL262538 IC50 = 110.0 nM 6.96
CHEMBL38992 ETISULERGINE IC50 = 120.0 nM 6.92
CHEMBL174247 IC50 = 130.0 nM 6.89
CHEMBL173926 IC50 = 140.0 nM 6.85
CHEMBL422745 IC50 = 150.0 nM 6.82
CHEMBL171126 IC50 = 185.0 nM 6.73
CHEMBL171080 IC50 = 190.0 nM 6.72
CHEMBL171187 IC50 = 220.0 nM 6.66
CHEMBL174095 DELERGOTRILE IC50 = 265.0 nM 6.58
CHEMBL171440 IC50 = 490.0 nM 6.31
CHEMBL171688 IC50 = 500.0 nM 6.30
CHEMBL171888 IC50 = 2000.0 nM 5.70