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Assay Detail

CHEMBL673828

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

Binding
Binding affinity towards Dopamine receptor D3 by displacement of [3H](+)-7-OH-DPAT.
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

D(3) dopamine receptor (CHEMBL234)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and biological activities of (R)-5,6-dihydro-N,N-dimethyl-4H-imidazo[4,5,1-ij]quinolin-5-amine and its metabolites.
Heier RF, Dolak LA, Duncan JN, Hyslop DK, Lipton MF, Martin IJ, Mauragis MA, Piercey MF, Nichols NF, Schreur PJ, Smith MW, Moon MW.
J Med Chem (1997) 40 : 639 -646
PubMed 9057850 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 9 6.87 8.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL157138 LISURIDE 3.0 1 8.77
CHEMBL531 PERGOLIDE 4.0 1 8.40
CHEMBL589 ROPINIROLE 4.0 1 7.72
CHEMBL434665 1 7.44
CHEMBL493 BROMOCRIPTINE 4.0 1 7.06
CHEMBL422344 1 5.71
CHEMBL419792 SUMANIROLE 3.0 1 5.63
CHEMBL348285 1 5.61
CHEMBL345458 1 5.53

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL157138 LISURIDE Ki = 1.7 nM 8.77
CHEMBL531 PERGOLIDE Ki = 4.0 nM 8.40
CHEMBL589 ROPINIROLE Ki = 19.0 nM 7.72
CHEMBL434665 Ki = 36.0 nM 7.44
CHEMBL493 BROMOCRIPTINE Ki = 87.0 nM 7.06
CHEMBL422344 Ki = 1929.0 nM 5.71
CHEMBL419792 SUMANIROLE Ki = 2333.0 nM 5.63
CHEMBL348285 Ki = 2459.0 nM 5.61
CHEMBL345458 Ki = 2948.0 nM 5.53