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Assay Detail

CHEMBL2427726

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

Binding
Displacement of [3H]-raclopride from dopamine D2 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysis
22
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Subcellular Membrane
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

D(2) dopamine receptor (CHEMBL339)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

2,3,9- and 2,3,11-trisubstituted tetrahydroprotoberberines as D2 dopaminergic ligands.
Párraga J, Cabedo N, Andujar S, Piqueras L, Moreno L, Galán A, Angelina E, Enriz RD, Ivorra MD, Sanz MJ, Cortes D.
Eur J Med Chem (2013) 68 : 150 -166
PubMed 23974015 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 22 6.14 7.55

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2425378 2 7.55
CHEMBL2425371 2 7.13
CHEMBL2425376 2 7.07
CHEMBL2425369 2 6.73
CHEMBL2425374 2 6.44
CHEMBL2425375 2 6.41
CHEMBL2425372 2 5.94
CHEMBL2425368 2 5.70
CHEMBL2425373 2 5.29
CHEMBL2425377 2 5.16
CHEMBL2425370 2 4.39

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2425378 Ki = 28.18 nM 7.55
CHEMBL2425378 Ki = 35.0 nM 7.46
CHEMBL2425371 Ki = 74.13 nM 7.13
CHEMBL2425371 Ki = 78.0 nM 7.11
CHEMBL2425376 Ki = 85.11 nM 7.07
CHEMBL2425376 Ki = 93.0 nM 7.03
CHEMBL2425369 Ki = 188.0 nM 6.73
CHEMBL2425369 Ki = 186.21 nM 6.73
CHEMBL2425374 Ki = 363.08 nM 6.44
CHEMBL2425375 Ki = 389.05 nM 6.41
CHEMBL2425374 Ki = 393.0 nM 6.41
CHEMBL2425375 Ki = 396.0 nM 6.40
CHEMBL2425372 Ki = 1148.15 nM 5.94
CHEMBL2425372 Ki = 1331.0 nM 5.88
CHEMBL2425368 Ki = 1995.26 nM 5.70
CHEMBL2425368 Ki = 2046.0 nM 5.69
CHEMBL2425373 Ki = 5128.61 nM 5.29
CHEMBL2425377 Ki = 6918.31 nM 5.16
CHEMBL2425377 Ki = 7506.0 nM 5.12
CHEMBL2425373 Ki = 8543.0 nM 5.07
CHEMBL2425370 Ki = 40866.0 nM 4.39
CHEMBL2425370 Ki = 41686.94 nM 4.38