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Assay Detail

CHEMBL672227

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

Binding
Displacement [125I]iodosulpiride from human Dopamine receptor D2 expressed in CHO cells
27
Total Activities
27
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

Novel 1,2,3,4-tetrahydroisoquinolines with high affinity and selectivity for the dopamine D3 receptor.
Austin NE, Avenell KY, Boyfield I, Branch CL, Coldwell MC, Hadley MS, Jeffrey P, Johns A, Johnson CN, Nash DJ, Riley GJ, Smith SA, Stacey RC, Stemp G, Thewlis KM, Vong AK.
Bioorg Med Chem Lett (1999) 9 : 179 -184
PubMed 10021923 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 27 6.48 7.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL279925 1 7.00
CHEMBL54777 1 7.00
CHEMBL52724 1 6.90
CHEMBL297960 1 6.90
CHEMBL52466 1 6.80
CHEMBL291545 1 6.70
CHEMBL367129 1 6.70
CHEMBL52468 1 6.60
CHEMBL293347 1 6.60
CHEMBL55524 1 6.50
CHEMBL52901 1 6.50
CHEMBL52987 1 6.50
CHEMBL416842 1 6.50
CHEMBL55276 1 6.50
CHEMBL292577 1 6.50
CHEMBL57219 1 6.40
CHEMBL51977 1 6.40
CHEMBL52135 1 6.40
CHEMBL55090 1 6.40
CHEMBL53833 1 6.30
CHEMBL299038 1 6.30
CHEMBL52770 1 6.30
CHEMBL53351 1 6.30
CHEMBL301475 1 6.20
CHEMBL55840 1 6.00
CHEMBL54948 1 6.00
CHEMBL54715 1 5.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL279925 Ki = 100.0 nM 7.00
CHEMBL54777 Ki = 100.0 nM 7.00
CHEMBL52724 Ki = 125.89 nM 6.90
CHEMBL297960 Ki = 125.89 nM 6.90
CHEMBL52466 Ki = 158.49 nM 6.80
CHEMBL291545 Ki = 199.53 nM 6.70
CHEMBL367129 Ki = 199.53 nM 6.70
CHEMBL52468 Ki = 251.19 nM 6.60
CHEMBL293347 Ki = 251.19 nM 6.60
CHEMBL55524 Ki = 316.23 nM 6.50
CHEMBL52901 Ki = 316.23 nM 6.50
CHEMBL52987 Ki = 316.23 nM 6.50
CHEMBL416842 Ki = 316.23 nM 6.50
CHEMBL55276 Ki = 316.23 nM 6.50
CHEMBL292577 Ki = 316.23 nM 6.50
CHEMBL57219 Ki = 398.11 nM 6.40
CHEMBL51977 Ki = 398.11 nM 6.40
CHEMBL52135 Ki = 398.11 nM 6.40
CHEMBL55090 Ki = 398.11 nM 6.40
CHEMBL53833 Ki = 501.19 nM 6.30
CHEMBL299038 Ki = 501.19 nM 6.30
CHEMBL52770 Ki = 501.19 nM 6.30
CHEMBL53351 Ki = 501.19 nM 6.30
CHEMBL301475 Ki = 630.96 nM 6.20
CHEMBL55840 Ki = 1000.0 nM 6.00
CHEMBL54948 Ki = 1000.0 nM 6.00
CHEMBL54715 Ki = 1584.89 nM 5.80