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Assay Detail

CHEMBL670206

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

Binding
Displacement of [3H]spiroperidol from homogenized bovine pituitary Dopamine receptor D2
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Bos taurus
Confidence 9 — Direct single protein target
Curated By Expert

Target

D(2) dopamine receptor (CHEMBL3998)
Type SINGLE PROTEIN
Organism Bos taurus

Publication

Synthesis and evaluation of non-catechol D-1 and D-2 dopamine receptor agonists: benzimidazol-2-one, benzoxazol-2-one, and the highly potent benzothiazol-2-one 7-ethylamines.
Weinstock J, Gaitanopoulos DE, Stringer OD, Franz RG, Hieble JP, Kinter LB, Mann WA, Flaim KE, Gessner G.
J Med Chem (1987) 30 : 1166 -1176
PubMed 2955118 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 5.92 7.31

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL17231 1 7.31
CHEMBL587 SKF-89124A 1 6.28
CHEMBL279106 1 6.25
CHEMBL418548 1 6.00
CHEMBL275600 1 6.00
CHEMBL275155 1 5.92
CHEMBL588 FENOLDOPAM 4.0 1 5.80
CHEMBL17357 1 5.70
CHEMBL59 DOPAMINE 4.0 1 5.33
CHEMBL278188 1 5.31
CHEMBL589 ROPINIROLE 4.0 1 5.17
CHEMBL441220 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL17231 IC50 = 49.0 nM 7.31
CHEMBL587 SKF-89124A IC50 = 530.0 nM 6.28
CHEMBL279106 IC50 = 560.0 nM 6.25
CHEMBL418548 IC50 = 1000.0 nM 6.00
CHEMBL275600 IC50 = 1000.0 nM 6.00
CHEMBL275155 IC50 = 1200.0 nM 5.92
CHEMBL588 FENOLDOPAM IC50 = 1580.0 nM 5.80
CHEMBL17357 IC50 = 2000.0 nM 5.70
CHEMBL59 DOPAMINE IC50 = 4700.0 nM 5.33
CHEMBL278188 IC50 = 4850.0 nM 5.31
CHEMBL589 ROPINIROLE IC50 = 6810.0 nM 5.17
CHEMBL441220 IC50 > 10000.0 nM -