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Assay Detail

CHEMBL674943

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

Binding
Binding affinity at Dopamine receptor D2 expressed in CHO cells by [125I]iodosulpiride displacement.
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type CHO
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

Fused aminotetralins: novel antagonists with high selectivity for the dopamine D3 receptor.
Avenell KY, Boyfield I, Coldwell MC, Hadley MS, Healy MA, Jeffrey PM, Johnson CN, Nash DJ, Riley GJ, Scott EE, Smith SA, Stacey R, Stemp G, Thewlis KM.
Bioorg Med Chem Lett (1998) 8 : 2859 -2864
PubMed 9873637 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 18 6.38 7.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL99198 1 7.60
CHEMBL319116 1 7.20
CHEMBL318925 1 6.60
CHEMBL97856 1 6.50
CHEMBL99876 1 6.50
CHEMBL2111592 1 6.50
CHEMBL317996 1 6.40
CHEMBL2111591 1 6.30
CHEMBL97107 1 6.30
CHEMBL95759 1 6.30
CHEMBL95743 1 6.30
CHEMBL98452 1 6.30
CHEMBL419706 1 6.20
CHEMBL97118 1 6.20
CHEMBL97149 1 6.10
CHEMBL329702 1 6.00
CHEMBL319355 1 5.90
CHEMBL97440 1 5.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL99198 Ki = 25.12 nM 7.60
CHEMBL319116 Ki = 63.1 nM 7.20
CHEMBL318925 Ki = 251.19 nM 6.60
CHEMBL97856 Ki = 316.23 nM 6.50
CHEMBL99876 Ki = 316.23 nM 6.50
CHEMBL2111592 Ki = 316.23 nM 6.50
CHEMBL317996 Ki = 398.11 nM 6.40
CHEMBL2111591 Ki = 501.19 nM 6.30
CHEMBL97107 Ki = 501.19 nM 6.30
CHEMBL95759 Ki = 501.19 nM 6.30
CHEMBL95743 Ki = 501.19 nM 6.30
CHEMBL98452 Ki = 501.19 nM 6.30
CHEMBL419706 Ki = 630.96 nM 6.20
CHEMBL97118 Ki = 630.96 nM 6.20
CHEMBL97149 Ki = 794.33 nM 6.10
CHEMBL329702 Ki = 1000.0 nM 6.00
CHEMBL319355 Ki = 1258.93 nM 5.90
CHEMBL97440 Ki = 1995.26 nM 5.70