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Assay Detail

CHEMBL672183

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

Binding
Displacement of [3H]quinpirole from Dopamine receptor D2
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

Novel (R)-2-amino-5-fluorotetralins: dopaminergic antagonists and inverse agonists.
Malmberg A, Höök BB, Johansson AM, Hacksell U.
J Med Chem (1996) 39 : 4421 -4429
PubMed 8893836 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 13 7.16 9.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL54 HALOPERIDOL 4.0 1 9.80
CHEMBL59 DOPAMINE 4.0 1 8.72
CHEMBL138998 1 8.31
CHEMBL69985 1 7.58
CHEMBL139089 1 7.43
CHEMBL141510 1 7.34
CHEMBL139345 1 6.78
CHEMBL65847 1 6.75
CHEMBL141511 1 6.59
CHEMBL138792 1 6.23
CHEMBL141537 1 6.11
CHEMBL345087 1 5.82
CHEMBL342630 1 5.61

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
CHEMBL138998 Ki = 4.94 nM 8.31
CHEMBL69985 Ki = 26.0 nM 7.58
CHEMBL139089 Ki = 37.0 nM 7.43
CHEMBL141510 Ki = 45.6 nM 7.34
CHEMBL139345 Ki = 167.0 nM 6.78
CHEMBL65847 Ki = 179.0 nM 6.75
CHEMBL141511 Ki = 254.0 nM 6.59
CHEMBL138792 Ki = 585.0 nM 6.23
CHEMBL141537 Ki = 779.0 nM 6.11
CHEMBL345087 Ki = 1530.0 nM 5.82
CHEMBL342630 Ki = 2450.0 nM 5.61