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Assay Detail

CHEMBL669147

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

Binding
Displacement of [3H]quinpirole from human dopamine D2A receptors expressed in LtK cells
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type LtK
Confidence 9 — Direct single protein target
Curated By Expert

Target

D(2) dopamine receptor (CHEMBL217)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Derivatives of (R)-2-amino-5-methoxytetralin: antagonists and inverse agonists at the dopamine D2A receptor.
Höök BB, Brege C, Linnanen T, Mikaels A, Malmberg A, Johansson AM.
Bioorg Med Chem Lett (1999) 9 : 2167 -2172
PubMed 10465538 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 13 7.40 9.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL54 HALOPERIDOL 4.0 1 9.80
CHEMBL59 DOPAMINE 4.0 1 8.72
CHEMBL68573 1 8.20
CHEMBL69985 1 7.58
CHEMBL67923 1 7.19
CHEMBL71599 1 7.16
CHEMBL68545 1 7.12
CHEMBL71275 1 7.08
CHEMBL303502 1 6.93
CHEMBL433121 1 6.67
CHEMBL69706 1 6.47
CHEMBL65896 1 5.88
CHEMBL69705 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL54 HALOPERIDOL Ki = 0.16 nM 9.80
CHEMBL59 DOPAMINE Ki = 1.89 nM 8.72
CHEMBL68573 Ki = 6.35 nM 8.20
CHEMBL69985 Ki = 26.0 nM 7.58
CHEMBL67923 Ki = 64.1 nM 7.19
CHEMBL71599 Ki = 69.7 nM 7.16
CHEMBL68545 Ki = 75.0 nM 7.12
CHEMBL71275 Ki = 82.3 nM 7.08
CHEMBL303502 Ki = 118.0 nM 6.93
CHEMBL433121 Ki = 215.0 nM 6.67
CHEMBL69706 Ki = 339.0 nM 6.47
CHEMBL65896 Ki = 1310.0 nM 5.88
CHEMBL69705 Ki > 5000.0 nM -