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Assay Detail

CHEMBL672175

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

Binding
Binding affinity to human Dopamine receptor D2 by using radioligand [3H]spiperone in LTK cells
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

trans-2,6-,3,6- and 4,6-diaza-5,6,6a,7,8,12b-hexahydro-benzo[c]phenanthrene-10,11- diols as dopamine agonists.
Gu YG, Bayburt EK, Michaelides MR, Lin CW, Shiosaki K.
Bioorg Med Chem Lett (1999) 9 : 1341 -1346
PubMed 10360732 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 15 5.77 6.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL282136 1 6.40
CHEMBL26965 1 6.35
CHEMBL285924 1 6.28
CHEMBL28338 A-86929 -1.0 1 6.15
CHEMBL26365 1 6.05
CHEMBL28054 1 5.89
CHEMBL27117 1 5.85
CHEMBL25856 DIHYDREXIDINE 2.0 1 5.82
CHEMBL283247 1 5.72
CHEMBL27101 1 5.66
CHEMBL281932 1 5.60
CHEMBL287513 1 5.44
CHEMBL284644 1 5.36
CHEMBL284959 1 5.04
CHEMBL275379 1 4.92

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL282136 Ki = 400.0 nM 6.40
CHEMBL26965 Ki = 450.0 nM 6.35
CHEMBL285924 Ki = 520.0 nM 6.28
CHEMBL28338 A-86929 Ki = 710.0 nM 6.15
CHEMBL26365 Ki = 890.0 nM 6.05
CHEMBL28054 Ki = 1300.0 nM 5.89
CHEMBL27117 Ki = 1400.0 nM 5.85
CHEMBL25856 DIHYDREXIDINE Ki = 1520.0 nM 5.82
CHEMBL283247 Ki = 1900.0 nM 5.72
CHEMBL27101 Ki = 2200.0 nM 5.66
CHEMBL281932 Ki = 2500.0 nM 5.60
CHEMBL287513 Ki = 3600.0 nM 5.44
CHEMBL284644 Ki = 4400.0 nM 5.36
CHEMBL284959 Ki = 9100.0 nM 5.04
CHEMBL275379 Ki = 12000.0 nM 4.92