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Assay Detail

CHEMBL672226

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

Binding
Displacement of [125I]iodosulpiride from human Dopamine receptor D2 expressed in CHO cells
13
Total Activities
13
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 Expert

Target

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

Publication

A novel series of 2-aminotetralins with high affinity and selectivity for the dopamine D3 receptor
Boyfield I, Coldwell MC, Hadley MS, Johnson CN, Riley GJ, Scott EE, Stacey R, Stemp G, Thewlis KM
Bioorg Med Chem Lett (1997) 7 : 1995 -1998
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 13 6.70 7.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL58669 1 7.60
CHEMBL294747 1 7.40
CHEMBL416508 1 7.00
CHEMBL59642 1 6.90
CHEMBL61717 1 6.90
CHEMBL291801 1 6.60
CHEMBL60038 1 6.60
CHEMBL59554 1 6.50
CHEMBL60713 1 6.50
CHEMBL57219 1 6.40
CHEMBL51977 1 6.40
CHEMBL59960 1 6.20
CHEMBL61444 1 6.10

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL58669 Ki = 25.12 nM 7.60
CHEMBL294747 Ki = 39.81 nM 7.40
CHEMBL416508 Ki = 100.0 nM 7.00
CHEMBL59642 Ki = 125.89 nM 6.90
CHEMBL61717 Ki = 125.89 nM 6.90
CHEMBL291801 Ki = 251.19 nM 6.60
CHEMBL60038 Ki = 251.19 nM 6.60
CHEMBL59554 Ki = 316.23 nM 6.50
CHEMBL60713 Ki = 316.23 nM 6.50
CHEMBL57219 Ki = 398.11 nM 6.40
CHEMBL51977 Ki = 398.11 nM 6.40
CHEMBL59960 Ki = 630.96 nM 6.20
CHEMBL61444 Ki = 794.33 nM 6.10