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Assay Detail

CHEMBL981460

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

Binding
Displacement of [3H]spiperone form human cloned dopamine D3 receptor expressed in CHO cells
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CHO
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Modulations of the amide function of the preferential dopamine D3 agonist (R,R)-S32504: improvements of affinity and selectivity for D3 versus D2 receptors.
Peglion JL, Poitevin C, Mannoury La Cour C, Dupuis D, Millan MJ.
Bioorg Med Chem Lett (2009) 19 : 2133 -2138
PubMed 19324548 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 22 6.87 8.38

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL484598 1 8.38
CHEMBL485128 1 8.12
CHEMBL484599 1 7.83
CHEMBL482556 1 7.72
CHEMBL449250 1 7.71
CHEMBL589 ROPINIROLE 4.0 1 7.44
CHEMBL484732 1 7.42
CHEMBL485352 1 7.40
CHEMBL482978 1 7.02
CHEMBL485325 1 6.92
CHEMBL485127 1 6.05
CHEMBL519201 1 5.66
CHEMBL500627 1 5.61
CHEMBL485018 1 5.58
CHEMBL485028 1 5.56
CHEMBL482977 1 5.48
CHEMBL485353 1 -
CHEMBL485017 1 -
CHEMBL484170 1 -
CHEMBL485029 1 -
CHEMBL519688 1 -
CHEMBL485027 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL484598 Ki = 4.169 nM 8.38
CHEMBL485128 Ki = 7.586 nM 8.12
CHEMBL484599 Ki = 14.79 nM 7.83
CHEMBL482556 Ki = 19.05 nM 7.72
CHEMBL449250 Ki = 19.5 nM 7.71
CHEMBL589 ROPINIROLE Ki = 36.31 nM 7.44
CHEMBL484732 Ki = 38.02 nM 7.42
CHEMBL485352 Ki = 39.81 nM 7.40
CHEMBL482978 Ki = 95.5 nM 7.02
CHEMBL485325 Ki = 120.23 nM 6.92
CHEMBL485127 Ki = 891.25 nM 6.05
CHEMBL519201 Ki = 2187.76 nM 5.66
CHEMBL500627 Ki = 2454.71 nM 5.61
CHEMBL485018 Ki = 2630.27 nM 5.58
CHEMBL485028 Ki = 2754.23 nM 5.56
CHEMBL482977 Ki = 3311.31 nM 5.48
CHEMBL485353 Ki > 10000.0 nM -
CHEMBL485017 Ki > 10000.0 nM -
CHEMBL484170 Ki > 10000.0 nM -
CHEMBL485029 Ki > 10000.0 nM -
CHEMBL519688 Ki > 10000.0 nM -
CHEMBL485027 Ki > 10000.0 nM -